Heterocycle-substituted and carbocycle-substituted steroid compounds and methods of use thereof

Abstract

In one aspect, the disclosure provides certain heterocycle-substituted and carbocycle-substituted steroid analogues and pharmaceutical compositions thereof. In certain embodiments, the compounds and compositions of the disclosure are useful for treating, preventing, and / or ameliorating cancer. In certain embodiments, the cancer is prostate cancer.

Description

[0001] TITLE

[0002] Heterocycle-Substituted and Carbocycle-Substituted Steroid Compounds and Methods of Use Thereof

[0003] CROSS-REFERENCE TO RELATED APPLICATIONS

[0004] This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Patent Application No. 63 / 701,256, filed September 30, 2024, which is incorporated herein by reference in its entirety.

[0005] BACKGROUND

[0006] The androgen receptor (AR), also known as NR3C4 (i.e., nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding androgens (e.g., testosterone and dihydrotestosterone). Upon activation, AR translocates to the cell nucleus, where it binds to specific DNA sequences to regulate the transcription of target genes involved in various physiological processes, including the development and maintenance of male characteristics, reproductive function, and anabolic effects on muscle.

[0007] Aberrant AR signaling is implicated in the pathogenesis of several disorders, including but not limited to prostate cancer, where androgens drive the growth and proliferation of cancer cells. Androgen receptor inhibitors function by blocking the binding of androgens to AR, thus inhibiting AR activation and subsequent gene transcription. This inhibition is therapeutically beneficial in conditions such as prostate cancer, where reducing androgenic stimulation can slow disease progression. Additionally, AR inhibitors have utility in treating other androgen-dependent conditions such as androgenetic alopecia, hirsutism, and certain types of breast cancer. By mitigating the effects of excessive androgen signaling, these inhibitors provide a valuable tool in managing and treating androgen-mediated disorders.

[0008] There is thus a need in the art for compounds and compositions for inhibiting AR signaling, targeting ARs for degradation, and / or for treating diseases and / or disorders, including but not limited to prostate cancer. The present disclosure addresses these needs.

[0009] BRIEF SUMMARY

[0010] In one aspect, the disclosure provides a compound formula (I), or a salt, solvate, stereoisomer, tautomer, or isotopologue thereof, wherein ring A, T1, T2, and X are defined elsewhere herein:

[0011] In another aspect, the disclosure provides a pharmaceutical composition comprising at least one compound of the disclosure and at least one pharmaceutically acceptable carrier.

[0012] In another aspect, the disclosure provides a method of treating, preventing, and / or ameliorating cancer in a subject in need thereof. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure or a pharmaceutical composition thereof.

[0013] In another aspect, the disclosure provides a method for impairing androgen receptor (AR) transactivation and / or androgen receptor dimerization in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure or a pharmaceutical composition thereof.

[0014] In another aspect, the disclosure provides a method for inhibiting cell growth in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure or a pharmaceutical composition thereof.

[0015] In another aspect, the disclosure provides a method for imaging malignant cells and / or hyperplastic cells in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure or a pharmaceutical composition thereof. In certain embodiments, the method comprises exposing the subject at least partially to electromagnetic radiation, such that the at least one compound and / or pharmaceutical composition is excited. In certain embodiments, the method comprises detecting excitation of the at least one compound and / or pharmaceutical composition. In certain embodiments, the method comprises imaging the subject or a portion thereof, wherein the malignant cells and / or hyperplastic cells are imaged.

[0016] DETAILED DESCRIPTION

[0017] Reference will now be made in detail to certain embodiments of the disclosed subject matter. While the disclosed subject matter will be described in conjunction with the enumerated claims, it will be understood that the exemplified subject matter is not intended to limit the claims to the disclosed subject matter.

[0018] Throughout this document, values expressed in a range format should be interpreted in a flexible manner to include not only the numerical values explicitly recited as the limits of the range, but also to include all the individual numerical values or sub-ranges encompassed within that range as if each numerical value and sub-range is explicitly recited. For example, a range of “about 0.1% to about 5%” or “about 0.1% to 5%” should be interpreted to include not just about 0.1% to about 5%, but also the individual values (e.g., 1%, 2%, 3%, and 4%) and the sub-ranges (e.g., 0.1% to 0.5%, 1.1% to 2.2%, 3.3% to 4.4%) within the indicated range. The statement “about X to Y” has the same meaning as “about X to about Y,” unless indicated otherwise. Likewise, the statement “about X, Y, or about Z” has the same meaning as “about X, about Y, or about Z,” unless indicated otherwise.

[0019] In this document, the terms “a,” “an,” or “the” are used to include one or more than one unless the context clearly dictates otherwise. The term “or” is used to refer to a nonexclusive “or” unless otherwise indicated. The statement “at least one of A and B” or “at least one of A or B” has the same meaning as “A, B, or A and B .” In addition, it is to be understood that the phraseology or terminology employed herein, and not otherwise defined, is for the purpose of description only and not of limitation. Any use of section headings is intended to aid reading of the document and is not to be interpreted as limiting; information that is relevant to a section heading may occur within or outside of that particular section. All publications, patents, and patent documents referred to in this document are incorporated by reference herein in their entirety, as though individually incorporated by reference.

[0020] In the methods described herein, the acts can be carried out in any order, except when a temporal or operational sequence is explicitly recited. Furthermore, specified acts can be carried out concurrently unless explicit claim language recites that they be carried out separately. For example, a claimed act of doing X and a claimed act of doing Y can be conducted simultaneously within a single operation, and the resulting process will fall within the literal scope of the claimed process.

[0021] Definitions

[0022] The term “about” as used herein can allow for a degree of variability in a value or range, for example, within 10%, within 5%, or within 1% of a stated value or of a stated limit of a range, and includes the exact stated value or range.

[0023] The term “alkenyl” as used herein refers to straight and branched chain and cyclic alkyl groups as defined herein, except that at least one double bond exists between two carbon atoms. Thus, alkenyl groups have from 2 to 40 carbon atoms, or 2 to about 20 carbon atoms, or 2 to 12 carbon atoms or, in some embodiments, from 2 to 8 carbon atoms. Examples include, but are not limited to vinyl, -CH=C=CCH2, -CH=CH(CH3), - CH=C(CH3)2, -C(CH3)=CH2, -C(CH3)=CH(CH3), -C(CH2CH3)=CH2, cyclohexenyl, cyclopentenyl, cyclohexadienyl, butadienyl, pentadienyl, and hexadienyl among others.

[0024] The term “alkoxy” as used herein refers to an oxygen atom connected to an alkyl group, including a cycloalkyl group, as are defined herein. Examples of linear alkoxy groups include but are not limited to methoxy, ethoxy, propoxy, butoxy, pentyloxy, hexyloxy, and the like. Examples of branched alkoxy include but are not limited to isopropoxy, sec-butoxy, tert-butoxy, isopentyloxy, isohexyloxy, and the like. Examples of cyclic alkoxy include but are not limited to cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, and the like. An alkoxy group can include about 1 to about 12, about 1 to about 20, or about 1 to about 40 carbon atoms bonded to the oxygen atom, and can further include double or triple bonds, and can also include heteroatoms. For example, an allyloxy group or a methoxyethoxy group is also an alkoxy group within the meaning herein, as is a methylenedioxy group in a context where two adjacent atoms of a structure are substituted therewith.

[0025] The term “alkyl” as used herein refers to straight chain and branched alkyl groups and cycloalkyl groups having from 1 to 40 carbon atoms, 1 to about 20 carbon atoms, 1 to 12 carbons or, in some embodiments, from 1 to 8 carbon atoms. Examples of straight chain alkyl groups include those with from 1 to 8 carbon atoms such as methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, n-heptyl, and n-octyl groups. Examples of branched alkyl groups include, but are not limited to, isopropyl, iso-butyl, sec-butyl, t-butyl, neopentyl, isopentyl, and 2,2- dimethylpropyl groups. As used herein, the term “alkyl” encompasses n-alkyl, isoalkyl, and anteisoalkyl groups as well as other branched chain forms of alkyl. Representative substituted alkyl groups can be substituted one or more times with any of the groups listed herein, for example, amino, hydroxy, cyano, carboxy, nitro, thio, alkoxy, and halogen groups.

[0026] The term “alkylene” or “alkylenyl” as used herein refers to a bivalent saturated aliphatic radical (e.g., -CH2-, -CH2CH2-, and -CH2CH2CH2-, inter alia). In certain embodiments, the term may be regarded as a moiety derived from an alkene by opening of the double bond or from an alkane by removal of two hydrogen atoms from the same (e.g., - CH2-) different (e.g., -CH2CH2-) carbon atoms.

[0027] The term “alkynyl” as used herein refers to straight and branched chain alkyl groups, except that at least one triple bond exists between two carbon atoms. Thus, alkynyl groups have from 2 to 40 carbon atoms, 2 to about 20 carbon atoms, or from 2 to 12 carbons or, in some embodiments, from 2 to 8 carbon atoms. Examples include, but are not limited to - C ≡CH, -OC(CH3), -C ≡C(CH2CH3), -CH2C ≡CH, -CH2C ≡C(CH3), and -CH2C ≡C(CH2CH3) among others.

[0028] The term “amine” as used herein refers to primary, secondary, and tertiary amines having, e.g., the formula N(group)3wherein each group can independently be H or non-H, such as alkyl, aryl, and the like. Amines include but are not limited to R-NH2, for example, alkylamines, arylamines, alkylarylamines; R2NH wherein each R is independently selected, such as dialkylamines, diarylamines, aralkylamines, heterocyclylamines and the like; and R3N wherein each R is independently selected, such as trialkylamines, dialkylarylamines, alkyldiarylamines, triarylamines, and the like. The term “amine” also includes ammonium ions as used herein.

[0029] The term “amino group” as used herein refers to a substituent of the form -NH2, - NHR, -NR2, or -NR3+, wherein each R is independently selected, and protonated forms of each, except for -NR3+, which cannot be protonated. Accordingly, any compound substituted with an amino group can be viewed as an amine. An “amino group” within the meaning herein can be a primary, secondary, tertiary, or quaternary amino group. An “alkylamino” group includes a monoalkylamino, dialkylamino, and trialkylamino group.

[0030] The terms “analogue” and “derivative” are used herein to refer to a compound having a chemical structure that contains a common core chemical structure as a parent or reference compound, but differs by having at least one structural difference, for example, by having one or more substituents or atoms added, removed, and / or substituted. For example, where the reference compound is benzene, derivatives and / or analogues can include toluene, benzylamine, d6-benzene, [13C]-benzene, fluorobenzene, and naphthalene, inter alia.

[0031] The term “aralkyl” as used herein refers to alkyl groups as defined herein in which a hydrogen or carbon bond of an alkyl group is replaced with a bond to an aryl group as defined herein. Representative aralkyl groups include benzyl and phenylethyl groups and fused (cycloalkylaryl)alkyl groups such as 4-ethyl-indanyl. Aralkenyl groups are alkenyl groups as defined herein in which a hydrogen or carbon bond of an alkyl group is replaced with a bond to an aryl group as defined herein.

[0032] The term “aryl” as used herein refers to cyclic aromatic hydrocarbon groups that do not contain heteroatoms in the ring. Thus aryl groups include, but are not limited to, phenyl, azulenyl, heptalenyl, biphenyl, indacenyl, fluorenyl, phenanthrenyl, triphenylenyl, pyrenyl, naphthacenyl, chrysenyl, biphenylenyl, anthracenyl, and naphthyl groups. In some embodiments, aryl groups contain about 6 to about 14 carbons in the ring portions of the groups. Aryl groups can be unsubstituted or substituted, as defined herein. Representative substituted aryl groups can be mono- substituted or substituted more than once, such as, but not limited to, a phenyl group substituted at any one or more of 2-, 3-, 4-, 5-, or 6-positions of the phenyl ring, or a naphthyl group substituted at any one or more of 2- to 8-positions thereof.

[0033] The term “carbocycle” as used herein refers to a saturated or unsaturated nonaromatic monocyclic, bicyclic, or polycyclic ring system having from 3 to 14 ring atoms (and all combinations and subcombinations of ranges and specific numbers of carbon atoms therein) wherein all of the ring atoms are carbon atoms.

[0034] The term “coumarin,” as used herein refers to any of a group of fluorogenic compounds related to benzopyrone or 2-chromenone that are capable of fluorescence modulation dependent on position of substitution and identity of functional groups.

[0035] The term “cycloalkyl” as used herein refers to cyclic alkyl groups such as, but not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl groups. In some embodiments, the cycloalkyl group can have 3 to about 8-12 ring members, whereas in other embodiments the number of ring carbon atoms range from 3 to 4, 5, 6, or 7. Cycloalkyl groups further include polycyclic cycloalkyl groups such as, but not limited to, norbomyl, adamantyl, bornyl, camphenyl, isocamphenyl, and carenyl groups, and fused rings such as, but not limited to, decalinyl, and the like. Cycloalkyl groups also include rings that are substituted with straight or branched chain alkyl groups as defined herein. Representative substituted cycloalkyl groups can be mono-substituted or substituted more than once, such as, but not limited to, 2,2-, 2,3-, 2,4- 2,5- or 2,6-disubstituted cyclohexyl groups or mono-, di- or tri-substituted norbornyl or cycloheptyl groups, which can be substituted with, for example, amino, hydroxy, cyano, carboxy, nitro, thio, alkoxy, and halogen groups. The term “cycloalkenyl” alone or in combination denotes a cyclic alkenyl group.

[0036] The term “cycloalkylene” or “cycloalkylenyl” as used herein refers to a bivalent saturated cycloalkyl radical (e.g., inter alia). In certain embodiments, the term may be regarded as a product of removal of two hydrogen atoms from the corresponding cycloalkane (e.g., cyclobutyl) by removal of two hydrogen atoms from the same (e.g., ) different (e.g., carbon atoms.

[0037] A “disease” is a state of health of an animal wherein the animal cannot maintain homeostasis, and wherein if the disease is not ameliorated then the animal’s health continues to deteriorate.

[0038] In contrast, a “disorder” in an animal is a state of health in which the animal is able to maintain homeostasis, but in which the animal’s state of health is less favorable than it would be in the absence of the disorder. Left untreated, a disorder does not necessarily cause a further decrease in the animal’s state of health.

[0039] A disease or disorder is “ameliorated” if the severity of a symptom of the disease or disorder, the frequency with which such a symptom is experienced by a patient, or both, is reduced.

[0040] As used herein, the terms “effective amount,” “pharmaceutically effective amount” and “therapeutically effective amount” refer to a nontoxic but sufficient amount of an agent to provide the desired biological result. That result may be reduction and / or alleviation of the signs, symptoms, or causes of a disease, or any other desired alteration of a biological system. An appropriate therapeutic amount in any individual case may be determined by one of ordinary skill in the art using routine experimentation.

[0041] The terms “halo,” “halogen,” or “halide” group, as used herein, by themselves or as part of another substituent, mean, unless otherwise stated, a fluorine, chlorine, bromine, or iodine atom.

[0042] The term “haloalkyl” group, as used herein, includes mono-halo alkyl groups, polyhalo alkyl groups wherein all halo atoms can be the same or different, and per-halo alkyl groups, wherein all hydrogen atoms are replaced by halogen atoms, such as fluoro. Examples of haloalkyl include trifluoromethyl, 1,1 -dichloroethyl, 1,2-di chloroethyl, 1,3-dibromo-3,3- difluoropropyl, perfluorobutyl, and the like.

[0043] The term “heteroaryl” as used herein refers to aromatic ring compounds containing 5 or more ring members, of which, one or more is a heteroatom such as, but not limited to, N, O, and S; for instance, heteroaryl rings can have 5 to about 8-12 ring members. A heteroaryl group is a variety of a heterocyclyl group that possesses an aromatic electronic structure. A heteroaryl group designated as a C2-heteroaryl can be a 5-ring with two carbon atoms and three heteroatoms, a 6-ring with two carbon atoms and four heteroatoms and so forth. Likewise a C4-heteroaryl can be a 5-ring with one heteroatom, a 6-ring with two heteroatoms, and so forth. The number of carbon atoms plus the number of heteroatoms sums up to equal the total number of ring atoms. Heteroaryl groups include, but are not limited to, groups such as pyrrolyl, pyrazolyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridinyl, thiophenyl, benzothiophenyl, benzofuranyl, indolyl, azaindolyl, indazolyl, benzimidazolyl, azabenzimidazolyl, benzoxazolyl, benzothiazolyl, benzothiadiazolyl, imidazopyridinyl, isoxazolopyridinyl, thianaphthal enyl, purinyl, xanthinyl, adeninyl, guaninyl, quinolinyl, isoquinolinyl, tetrahydroquinolinyl, quinoxalinyl, and quinazolinyl groups. Heteroaryl groups can be unsubstituted, or can be substituted with groups as is discussed herein. Representative substituted heteroaryl groups can be substituted one or more times with groups such as those listed herein.

[0044] Additional examples of aryl and heteroaryl groups include but are not limited to phenyl, biphenyl, indenyl, naphthyl (1 -naphthyl, 2-naphthyl), N-hydroxytetrazolyl, N- hydroxytriazolyl, N-hydroxyimidazolyl, anthracenyl (1-anthracenyl, 2-anthracenyl, 3- anthracenyl), thiophenyl (2 -thienyl, 3 -thienyl), furyl (2-furyl, 3 -furyl) , indolyl, oxadiazolyl, isoxazolyl, quinazolinyl, fluorenyl, xanthenyl, isoindanyl, benzhydryl, acridinyl, thiazolyl, pyrrolyl (2-pyrrolyl), pyrazolyl (3-pyrazolyl), imidazolyl (1 -imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl), triazolyl (1,2,3-triazol-1-1y,2l, ,3-triazol-2-1y,2l ,3-triazol-4-yl,1,2,4-triazol-3-yl), oxazolyl (2-oxazolyl, 4-oxazolyl, 5-oxazolyl), thiazolyl (2-thiazolyl, 4- thiazolyl, 5-thiazolyl), pyridyl (2-pyridyl, 3-pyridyl, 4-pyridyl), pyrimidinyl (2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 6-pyrimidinyl), pyrazinyl, pyridazinyl (3- pyridazinyl, 4- pyridazinyl, 5-pyridazinyl), quinolyl (2-quinolyl, 3-quinolyl, 4-quinolyl, 5-quinolyl, 6- quinolyl, 7-quinolyl, 8-quinolyl), isoquinolyl (1-isoquinolyl, 3 -isoquinolyl, 4-isoquinolyl, 5- isoquinolyl, 6-isoquinolyl, 7-isoquinolyl, 8-isoquinolyl), benzo[b]furanyl (2-benzo[b]furanyl, 3-benzo[b]furanyl, 4-benzo[b]furanyl, 5 -benzo[b] furanyl, 6-benzo[b]furanyl, 7- benzo[b]furanyl), 2,3-dihydro-benzo[b]furanyl (2-(2,3-dihydro-benzo[b]furanyl), 3-(2,3- dihydro-benzo[b]furanyl), 4-(2,3-dihydro-benzo[b]furanyl), 5-(2,3-dihydro-benzo[b]furanyl),

[0045] 6-(2,3-dihydro-benzo[b]furanyl), 7-(2,3-dihydro-benzo[b]furanyl), benzo [b]thiophenyl (2- benzo[b]thiophenyl, 3-benzo[b]thiophenyl, 4-benzo[b]thiophenyl, 5-benzo[b]thiophenyl, 6- benzo[b]thiophenyl, 7-benzo[b]thiophenyl), 2,3-dihydro-benzo[b]thiophenyl, (2-(2,3- dihydro-benzo[b]thiophenyl), 3-(2,3-dihydro-benzo[b]thiophenyl), 4-(2,3-dihydro- benzo[b]thiophenyl), 5-(2,3-dihydro-benzo[b]thiophenyl), 6-(2,3-dihydro- benzo[b]thiophenyl), 7-(2,3-dihydro-benzo[b]thiophenyl), indolyl (1-indolyl, 2-indolyl,

[0046] 3-indolyl, 4-indolyl, 5-indolyl, 6-indolyl, 7-indolyl), indazole (1-indazolyl, 3-indazolyl,

[0047] 4-indazolyl, 5-indazolyl, 6-indazolyl, 7-indazolyl), benzimidazolyl (1 -benzimidazolyl,

[0048] 2 -benzimidazolyl, 4-benzimidazolyl, 5-benzimidazolyl, 6-benzimidazolyl, 7-benzimidazolyl, 8-benzimidazolyl), benzoxazolyl (1-benzoxazolyl, 2-benzoxazolyl), benzothiazolyl (1- benzothiazolyl, 2-benzothiazolyl, 4-benzothiazolyl, 5 -benzothiazolyl, 6-benzothiazolyl,

[0049] 7-benzothiazolyl), carbazolyl (1-carbazolyl, 2-carbazolyl, 3-carbazolyl, 4-carbazolyl), 5H-dibenz[b,f]azepine (5H-dibenz[b,f]azepin-1-yl, 5H-dibenz[b,f]azepine-2-yl, 5H-dibenz[b,f]azepine-3-yl, 5H-dibenz[b,f]azepine-4-yl, 5H-dibenz[b,f]azepine-5-yl),10,11-dihydro-5H-dibenz[b,f]azepine (10,11-dihydro-5H-dibenz[b,f]azepine-1-yl, 10,11-dihydro-5H-dibenz[b,f]azepine-2-yl, 10,11-dihydro-5H-dibenz[b,f]azepine-3-yl, 10,11-dihydro-5H-dibenz[b,f]azepine-4-yl, 10,11-dihydro-5H-dibenz[b,f]azepine-5-yl), and the like.

[0050] The term “heteroarylalkyl” as used herein refers to alkyl groups as defined herein in which a hydrogen or carbon bond of an alkyl group is replaced with a bond to a heteroaryl group as defined herein.

[0051] The term “heteroarylene” or “heteroarylenyl” as used herein refers to a bivalent heteroaryl radical (e.g., 2,4-pyridylene). In certain embodiments, the term may be regarded as a divalent radical formed by the removal of two hydrogen atoms from one or more rings of a heteroaryl moiety, wherein the hydrogen atoms may be removed from the same or different rings, preferably the same ring.

[0052] The term “heterocycloalkyl” as used herein refers to an aliphatic, partially unsaturated or fully saturated, 3- to 14-membered ring system, including single rings of 3 to 8 atoms and bi- and tricyclic ring systems where at least one of the carbon atoms of the ring is replaced with a heteroatom such as, but not limited to, nitrogen, oxygen, sulfur, or phosphorus. A heterocycloalkyl can include one to four heteroatoms independently selected from oxygen, nitrogen, and sulfur, wherein a nitrogen and sulfur heteroatom optionally can be oxidized and a nitrogen heteroatom can be optionally substituted. Representative heterocycloalkyl groups include, but are not limited, to the following exemplary groups: pyrrolidinyl, pyrazolinyl, pyrazolidinyl, imidazolinyl, imidazolidinyl, piperidinyl, piperazinyl, oxazolidinyl, isoxazolidinyl, morpholinyl, thiazolidinyl, isothiazolidinyl, and tetrahydrofuryl. The term heterocycloalkyl group can also be a C2heterocycloalkyl, C2-C3heterocycloalkyl, C2-C4heterocycloalkyl, C2-C5heterocycloalkyl, C2-C6heterocycloalkyl, C2-C7heterocycloalkyl, C2-C8heterocycloalkyl, C2-C9heterocycloalkyl, C2-C10heterocycloalkyl, C2-Cn heterocycloalkyl, and the like, up to and including a C2-145heterocycloalkyl. For example, a C2heterocycloalkyl comprises a group which has two carbon atoms and at least one heteroatom, including, but not limited to, aziridinyl, diazetidinyl, oxiranyl, thiiranyl, and the like. Alternatively, for example, a C5heterocycloalkyl comprises a group which has five carbon atoms and at least one heteroatom, including, but not limited to, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, diazepanyl, and the like. It is understood that a heterocycloalkyl group may be bound either through a heteroatom in the ring, where chemically possible, or one of carbons comprising the heterocycloalkyl ring. The heterocycloalkyl group can be substituted or unsubstituted.

[0053] The term “heterocycloalkylene” or “heterocycloalkylenyl” as used herein refers to a bivalent saturated cycloalkyl radical (e.g., inter alia). In certain embodiments, the term may be regarded as a product of removal of two hydrogen atoms from the corresponding heterocycloalkane (e.g., piperidine) by removal of two hydrogen atoms from the same (e.g., ) different (e.g. ) carbon atom(s) and / or heteroatom(s).

[0054] The term “heterocyclyl” or “heterocycle” as used herein refers to aromatic and nonaromatic ring compounds containing three or more ring members, of which one or more is a heteroatom such as, but not limited to, N, O, and S. Thus, a heterocyclyl can be a heterocycloalkyl, or a heteroaryl, or if polycyclic, any combination thereof. In some embodiments, heterocyclyl groups include 3 to about 20 ring members, whereas other such groups have 3 to about 15 ring members. A heterocyclyl group designated as a C2- heterocyclyl can be a 5-ring with two carbon atoms and three heteroatoms, a 6-ring with two carbon atoms and four heteroatoms and so forth. Likewise a C4-heterocyclyl can be a 5-ring with one heteroatom, a 6-ring with two heteroatoms, and so forth. The number of carbon atoms plus the number of heteroatoms equals the total number of ring atoms. A heterocyclyl ring can also include one or more double bonds. A heteroaryl ring is an embodiment of a heterocyclyl group. The phrase “heterocyclyl group” includes fused ring species including those that include fused aromatic and non-aromatic groups. For example, a dioxolanyl ring and a benzdioxolanyl ring system (methylenedioxyphenyl ring system) are both heterocyclyl groups within the meaning herein. The phrase also includes polycyclic ring systems containing a heteroatom such as, but not limited to, quinuclidyl. Heterocyclyl groups can be unsubstituted, or can be substituted as discussed herein. Heterocyclyl groups include, but are not limited to, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, pyrrolyl, pyrazolyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridinyl, thiophenyl, benzothiophenyl, benzofuranyl, dihydrobenzofuranyl, indolyl, dihydroindolyl, azaindolyl, indazolyl, benzimidazolyl, azabenzimidazolyl, benzoxazolyl, benzothiazolyl, benzothiadiazolyl, imidazopyridinyl, isoxazolopyridinyl, thianaphthalenyl, purinyl, xanthinyl, adeninyl, guaninyl, quinolinyl, isoquinolinyl, tetrahydroquinolinyl, quinoxalinyl, and quinazolinyl groups. Representative substituted heterocyclyl groups can be mono-substituted or substituted more than once, such as, but not limited to, piperidinyl or quinolinyl groups, which are 2-, 3-, 4-, 5-, or 6-substituted, or disubstituted with groups such as those listed herein.

[0055] The term “hydrocarbon” or “hydrocarbyl” as used herein refers to a molecule or functional group that includes carbon and hydrogen atoms. The term can also refer to a molecule or functional group that normally includes both carbon and hydrogen atoms but wherein all the hydrogen atoms are substituted with other functional groups.

[0056] As used herein, the term “hydrocarbyl” refers to a functional group derived from a straight chain, branched, or cyclic hydrocarbon, and can be alkyl, alkenyl, alkynyl, aryl, cycloalkyl, acyl, or any combination thereof. Hydrocarbyl groups can be shown as (Ca- Cb)hydrocarbyl, wherein a and b are integers and mean having any of a to b number of carbon atoms. For example, (C1-C4)hydrocarbyl means the hydrocarbyl group can be methyl (C1), ethyl (C2), propyl (C3), or butyl (C4), and (C0-Cb)hydrocarbyl means in certain embodiments there is no hydrocarbyl group.

[0057] The term “independently selected from” as used herein refers to referenced groups being the same, different, or a mixture thereof, unless the context clearly indicates otherwise. Thus, under this definition, the phrase “X1, X2, and X3are independently selected from noble gases” would include the scenario where, for example, X1, X2, and X3are all the same, where X1, X2, and X3are all different, where X1and X2are the same but X3is different, and other analogous permutations.

[0058] The term “linker” as used herein refers to an organic moiety that connects two parts of a compound (e.g., a first small molecule drug and a second small molecule drug). The linker can be, in non-limiting examples, a direct bond, a single atom (e.g., -O-), a peptide, or a substituted or unsubstituted alkylene or heteroalkylene moiety (e.g., polyethylene glycol). One skilled in the art would be apprised of the common linkers suitable for use in drug-drug conjugates and methods of preparation thereof.

[0059] The term “monovalent” as used herein refers to a substituent connecting via a single bond to a substituted molecule. When a substituent is monovalent, such as, for example, F or Cl, it is bonded to the atom it is substituting by a single bond.

[0060] The term “organic group” as used herein refers to any carbon-containing functional group. Examples can include an oxygen-containing group such as an alkoxy group, aryloxy group, aralkyloxy group, oxo(carbonyl) group; a carboxyl group including a carboxylic acid, carboxylate, and a carboxylate ester; a sulfur-containing group such as an alkyl and aryl sulfide group; and other heteroatom-containing groups. Non-limiting examples of organic groups include OR, OOR, OC(O)N(R)2, CN, CF3, OCF3, R, C(O), methylenedioxy, ethylenedioxy, N(R)2, SR, SOR, SO2R, SO2N(R)2, SO3R, C(O)R, C(O)C(O)R, C(O)CH2C(O)R, C(S)R, C(O)OR, OC(O)R, C(O)N(R)2, OC(O)N(R)2, C(S)N(R)2, (CH2)O.2N(R)C(O)R, (CH2)O.2N(R)N(R)2, N(R)N(R)C(O)R, N(R)N(R)C(O)OR, N(R)N(R)CON(R)2, N(R)SO2R, N(R)SO2N(R)2, N(R)C(O)OR, N(R)C(O)R, N(R)C(S)R, N(R)C(O)N(R)2, N(R)C(S)N(R)2, N(COR)COR, N(OR)R, C(=NH)N(R)2, C(O)N(OR)R, C(=NOR)R, and substituted or unsubstituted (Ci-Cioo)hydrocarbyl, wherein R can be hydrogen (in examples that include other carbon atoms) or a carbon-based moiety, and wherein the carbon-based moiety can be substituted or unsubstituted.

[0061] The terms “patient,” “subject,” or “individual” are used interchangeably herein, and refer to any animal, or cells thereof whether in vitro or in situ, amenable to the methods described herein. In a non-limiting embodiment, the patient, subject or individual is a human.

[0062] As used herein, the term “pharmaceutically acceptable” refers to a material, such as a carrier or diluent, which does not abrogate the biological activity or properties of the compound, and is relatively non-toxic, ie., the material may be administered to an individual without causing undesirable biological effects or interacting in a deleterious manner with any of the components of the composition in which it is contained.

[0063] As used herein, the language “pharmaceutically acceptable salt” refers to a salt of the administered compounds prepared from pharmaceutically acceptable non-toxic acids or bases, including inorganic acids or bases, organic acids or bases, solvates, hydrates, or clathrates thereof.

[0064] Suitable pharmaceutically acceptable acid addition salts may be prepared from an inorganic acid or from an organic acid. Examples of inorganic acids include hydrochloric, hydrobromic, hydriodic, nitric, carbonic, sulfuric (including sulfate and hydrogen sulfate), and phosphoric acids (including hydrogen phosphate and dihydrogen phosphate). Appropriate organic acids may be selected from aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic, carboxylic and sulfonic classes of organic acids, examples of which include formic, acetic, propionic, succinic, glycolic, gluconic, lactic, malic, tartaric, citric, ascorbic, glucuronic, maleic, malonic, saccharin, fumaric, pyruvic, aspartic, glutamic, benzoic, anthranilic, 4-hydroxybenzoic, phenylacetic, mandelic, embonic (pamoic), methanesulfonic, ethanesulfonic, benzenesulfonic, pantothenic, trifluoromethanesulfonic, 2- hydroxyethanesulfonic, p-toluenesulfonic, sulfanilic, cyclohexylaminosulfonic, stearic, alginic, P-hydroxybutyric, salicylic, galactaric and galacturonic acid.

[0065] As used herein, the term “pharmaceutically acceptable carrier” or “pharmaceutically acceptable excipient” means a pharmaceutically acceptable material, composition or carrier, such as a liquid or solid filler, stabilizer, dispersing agent, suspending agent, diluent, excipient, thickening agent, solvent or encapsulating material, involved in carrying or transporting a compound described herein within or to the patient such that it may perform its intended function. Typically, such compounds are carried or transported from one organ, or portion of the body, to another organ, or portion of the body. Each carrier must be “acceptable” in the sense of being compatible with the other ingredients of the formulation, including the compound(s) described herein, and not injurious to the patient. Some examples of materials that may serve as pharmaceutically acceptable carriers include: sugars, such as lactose, glucose and sucrose; starches, such as com starch and potato starch; cellulose, and its derivatives, such as sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; powdered tragacanth; malt; gelatin; talc; excipients, such as cocoa butter and suppository waxes; oils, such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, com oil and soybean oil; glycols, such as propylene glycol; polyols, such as glycerin, sorbitol, mannitol and polyethylene glycol; esters, such as ethyl oleate and ethyl laurate; agar; buffering agents, such as magnesium hydroxide and aluminum hydroxide; surface active agents; alginic acid; pyrogen-free water; isotonic saline; Ringer’s solution; ethyl alcohol; phosphate buffer solutions; and other non-toxic compatible substances employed in pharmaceutical formulations. As used herein, “pharmaceutically acceptable carrier” also includes any and all coatings, antibacterial and antifungal agents, and absorption delaying agents, and the like that are compatible with the activity of the compound(s) described herein, and are physiologically acceptable to the patient. Supplementary active compounds may also be incorporated into the compositions. The “pharmaceutically acceptable carrier” may further include a pharmaceutically acceptable salt of the compound(s) described herein. Other additional ingredients that may be included in the pharmaceutical compositions used with the methods or compounds described herein are known in the art and described, for example in Remington’s Pharmaceutical Sciences (Genaro, Ed., Mack Publishing Co., 1985, Easton, PA), which is incorporated herein by reference.

[0066] The term “phenylene” or “phenylenyl” as used herein refers to a bivalent phenyl radical (e.g., 1,4-phenylene). In certain embodiments, the term may be regarded as a divalent radical formed by the removal of two hydrogen atoms from a benzene moiety.

[0067] The term “solvent” as used herein refers to a liquid that can dissolve a solid, liquid, or gas. Non-limiting examples of solvents are silicones, organic compounds, water, alcohols, ionic liquids, and supercritical fluids.

[0068] The term “substantially” as used herein refers to a majority of, or mostly, as in at least about 50%, 60%, 70%, 80%, 90%, 95%, 96%, 97%, 98%, 99%, 99.5%, 99.9%, 99.99%, or at least about 99.999% or more, or 100%. The term “substantially free of’ as used herein can mean having none or having a trivial amount of, such that the amount of material present does not affect the material properties of the composition including the material, such that the composition is about 0 wt% to about 5 wt% of the material, or about 0 wt% to about 1 wt%, or about 5 wt% or less, or less than, equal to, or greater than about 4.5 wt%, 4, 3.5, 3, 2.5, 2, 1.5, 1, 0.9, 0.8, 0.7, 0.6, 0.5, 0.4, 0.3, 0.2, 0.1, 0.01, or about 0.001 wt% or less. The term “substantially free of’ can mean having a trivial amount of, such that a composition is about 0 wt% to about 5 wt% of the material, or about 0 wt% to about 1 wt%, or about 5 wt% or less, or less than, equal to, or greater than about 4.5 wt%, 4, 3.5, 3, 2.5, 2, 1.5, 1, 0.9, 0.8, 0.7, 0.6, 0.5, 0.4, 0.3, 0.2, 0.1, 0.01, or about 0.001 wt% or less, or about 0 wt%.

[0069] The term “substituted” as used herein in conjunction with a molecule or an organic group as defined herein refers to the state in which one or more hydrogen atoms contained therein are replaced by one or more non-hydrogen atoms. The term “functional group” or “substituent” as used herein refers to a group that can be or is substituted onto a molecule or onto an organic group. Examples of substituents or functional groups include, but are not limited to, a halogen (e.g., F, Cl, Br, and I); an oxygen atom in groups such as hydroxy groups, alkoxy groups, aryloxy groups, aralkyloxy groups, oxo(carbonyl) groups, carboxyl groups including carboxylic acids, carboxylates, and carboxylate esters; a sulfur atom in groups such as thiol groups, alkyl and aryl sulfide groups, sulfoxide groups, sulfone groups, sulfonyl groups, and sulfonamide groups; a nitrogen atom in groups such as amines, hydroxyamines, nitriles, nitro groups, N-oxides, hydrazides, azides, and enamines; and other heteroatoms in various other groups. Non-limiting examples of substituents that can be bonded to a substituted carbon (or other) atom include F, Cl, Br, I, OR, OC(O)N(R)2, CN, NO, NO2, ONO2, azido, CF3, OCF3, R, O (oxo), S (thiono), C(O), S(O), methylenedioxy, ethylenedioxy, N(R)2, SR, SOR, SO2R, SO2N(R)2, SO3R, C(O)R, C(O)C(O)R, C(O)CH2C(O)R, C(S)R, C(O)OR, OC(O)R, C(O)N(R)2, OC(O)N(R)2, C(S)N(R)2, (CH2)O.2N(R)C(O)R, (CH2)O.2N(R)N(R)2, N(R)N(R)C(O)R, N(R)N(R)C(O)OR, N(R)N(R)CON(R)2, N(R)SO2R, N(R)SO2N(R)2, N(R)C(O)OR, N(R)C(O)R, N(R)C(S)R, N(R)C(O)N(R)2, N(R)C(S)N(R)2, N(COR)COR, N(0R)R, C(=NH)N(R)2, C(O)N(OR)R, and C(=NOR)R, wherein R can be hydrogen or a carbon-based moiety; for example, R can be hydrogen, (C1C100) hydrocarbyl, alkyl, acyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroarylalkyl; or wherein two R groups bonded to a nitrogen atom or to adjacent nitrogen atoms can together with the nitrogen atom or atoms form a heterocyclyl.

[0070] A “therapeutic” treatment is a treatment administered to a subject who exhibits signs of pathology, for the purpose of diminishing or eliminating those signs.

[0071] The terms “treat,” “treating” and “treatment,” as used herein, means reducing the frequency or severity with which symptoms of a disease or condition are experienced by a subject by virtue of administering an agent or compound to the subject.

[0072] Compounds and Compositions

[0073] In one aspect, the disclosure provides a compound of formula (I), or a salt, solvate, stereoisomer, tautomer, or isotopologue thereof: wherein: ring 4 is

[0074] T1is CH3;

[0075] T2is H or absent;

[0076] X is selected from the group consisting of

[0077] Y1is selected from the group consisting of a bond and -[C(R3a)(R3b)]i.2-;

[0078] Y2is selected from the group consisting of -C(R3c)(R3d)-, -N(R4a)-, and -C(=O)-;

[0079] Y3is selected from the group consisting of -C(R3e)(R3f)-, -N(R4b)-, -C(=O)-, and - C(=NOR5)-; or Y2and Y3combine with the atoms to which they are bound to form an optionally substituted C2-C6heteroaryl-fused ring A;

[0080] Y4is -[C(R3g)(R3h)]1-2-;

[0081] R1is selected from the group consisting of H,

[0082] R2is selected from the group consisting of H and optionally substituted C1-C6alkyl; each occurrence of R3a, R3b, R3c, R3d, R3e, R3f, R3g, and R3h, if present, is independently selected from the group consisting of H, halogen, CN, NO2, ORA, OC(=O)RA, N(RA)(RB), N(RA)C(=O)RB, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl;

[0083] R4aand R4bare each independently selected from the group consisting of H and optionally substituted C1-C6alkyl;

[0084] R5is selected from the group consisting of H and optionally substituted C1-C6alkyl;

[0085] R6is selected from the group consisting of optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl; each occurrence of L is independently selected from the group consisting of L1, L2, L3, and L4;

[0086] L1is selected from the group consisting of optionally substituted C1-C6alkylenyl and optionally substituted C2-C6alkenylenyl;

[0087] L2is selected from the group consisting of -C(=O)-, -C(=O)N(RA)-, -N(RA)C(=O)-, -

[0088] N(RA)C(=O)N(RB)-, -C(=O)O-, -OC(=O)-, -OC(=O)O-,

[0089] L3is selected from the group consisting of -O-, -N(RA)-, and -S-;

[0090] L4is selected from the group consisting of -S(=O)-, -S(=O)N(RA)-, -N(RA)S(=O)-, - S(=O)2-, -N(RA)S(=O)2-, and -S(=O)2N(RA)-; ring B is selected from the group consisting of optionally substituted C2-C8heterocycloalkyl and optionally substituted C2-C8heterocycloalkylenyl; ring C is optionally substituted coumarin, or an analogue or derivative thereof; ring D is selected from the group consisting of

[0091] R7a, R7b, R7c, R7d, and R7e, if present, are each independently selected from the group consisting of H, halogen, CN, NO2, ORA, OC(=O)RA, N(RA)(RB), N(RA)C(=O)RB, C(=O)RA, C(=O)ORA, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl;

[0092] Z1is selected from the group consisting of -O-, -S-, and -N(RA)-; bond a is a single bond or double bond; and s are each independently selected from the group consisting of 1, 2, 3, 4, and 5; o is selected from the group consisting of 0, 1, 2, and 3; and each occurrence of RAand RB, if present, is independently selected from the group consisting of H, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C8heteroaryl.

[0093] In certain embodiments, wherein R1comprises ring C, X is (CH2)C(=O)NH(CH2)2- or -(CH2)2NH(CH2)2-.

[0094] In certain embodiments, wherein R1comprises ring C, X is wherein R2is H, ring C is selected from the group consisting of , and ring A is not or wherein R5is substituted alkyl.

[0095] In certain embodiments, wherein R1comprises ring C, no more than two of the following apply:

[0096] (a) X is wherein R2is H, and ring C is selected from the group consisting of (b) L and p are selected such that -[L]p- is -(CH2)C(=O)NH(CH2)2- or -(CH2)2NH(CH2)2-;

[0097] (c) ring A is wherein R5is substituted alkyl.

[0098] In certain embodiments, R3ais H. In certain embodiments, R3ais F. In certain embodiments, R3ais OH. In certain embodiments, R3ais NH2. In certain embodiments, R3ais

[0099] NHC(=O)CH3. In certain embodiments, R3ais CN. In certain embodiments, R3ais

[0100] In certain embodiments, R3bis H. In certain embodiments, R3bis F. In certain embodiments, R3bis OH. In certain embodiments, R3bis NH2. In certain embodiments, R3bis

[0101] NHC(=O)CH3. In certain embodiments, R3bis CN. In certain embodiments, R3bis

[0102] In certain embodiments, R3cis H. In certain embodiments, R3cis F. In certain embodiments, R3cis OH. In certain embodiments, R3cis NH2. In certain embodiments, R3cis

[0103] NHC(=O)CH3. In certain embodiments, R3cis CN. In certain embodiments, R3cis

[0104] In certain embodiments, R3dis H. In certain embodiments, R3dis F. In certain embodiments, R3dis OH. In certain embodiments, R3dis NH2. In certain embodiments, R3dis

[0105] NHC(=O)CH3. In certain embodiments, R3dis CN. In certain embodiments, R3dis

[0106] In certain embodiments, R3eis H. In certain embodiments, R3eis F. In certain embodiments, R3eis OH. In certain embodiments, R3eis NH2. In certain embodiments, R3eis

[0107] NHC(=O)CH3. In certain embodiments, R3eis CN. In certain embodiments, R3eis

[0108] In certain embodiments, R3fis H. In certain embodiments, R3fis F. In certain embodiments, R3fis OH. In certain embodiments, R3fis NH2. In certain embodiments, R3fis

[0109] NHC(=O)CH3. In certain embodiments, R3fis CN. In certain embodiments, R3fis

[0110] In certain embodiments, R3gis H. In certain embodiments, R3gis F. In certain embodiments, R3gis OH. In certain embodiments, R3gis NH2. In certain embodiments, R3gis

[0111] NHC(=O)CH3. In certain embodiments, R3gis CN. In certain embodiments, R3gis In certain embodiments, R3his H. In certain embodiments, R3his F. In certain embodiments, R3his OH. In certain embodiments, R3his NH2. In certain embodiments, R3his

[0112] NHC(=O)CH3. In certain embodiments, R3his CN. In certain embodiments, R3his

[0113] In certain embodiments, Y2and Y3combine with the atoms to which they are bound to form a ring A which is In certain embodiments, Y2and Y3combine with the atoms to which they are bound to form a ring A which is . In certain embodiments, Y2and Y3combine with the atoms to which they are bound to form a ring A which is

[0114] In certain embodiments, the compound of formula (I) is a compound of formula (la):

[0115] (la). In certain embodiments, the compound of formula (I) is a compound of formula (lb): (lb). In certain embodiments, the compound of formula (I) is a compound of formula (Ic): embodiments, the compound of formula (I) is a compound of formula (Id): (Id). In certain embodiments, the compound of formula (I) is a (le). In certain embodiments, the compound of formula (I) is a compound of formula (If): (If). In certain embodiments, the compound of formula (I) is a compound of formula (Ig): (Ig). in certain embodiments, the compound of formula (I) is a compound of formula (Ih): (Ih). In certain embodiments, the compound of formula (I) is a compound of formula (li): (li). In certain embodiments, the compound of formula (I) is a compound of formula (Ij): (Ij). In certain embodiments, the compound of formula (I) is a compound of formula (Ik): (Ik). In certain embodiments, the compound of formula (I) is a compound of formula (II): (II). In certain embodiments, the compound of formula (I) is a compound of formula (Im):

[0116] (Im). In certain embodiments, the compound of formula (I) is a compound of formula (In): (In). In certain embodiments, the compound of formula (I) is a compound of formula (Io): embodiments, the compound of formula (I) is a compound of formula (Ip):

[0117] (Ip). In certain embodiments, the compound of formula (I) is a compound of formula (Iq): (Iq). In certain embodiments, the compound of formula (I) is a compound of formula (Ir): (Ir). In certain embodiments, the compound of formula (I) is a compound of formula (Is): (Is). In certain embodiments, the compound of formula (I) is a compound of formula (It): (It). In certain embodiments, the compound of formula (I) is a compound of formula (lu):

[0118] In certain embodiments, the compound of formula (I) is a compound of formula (Ic- (Ic-1). In certain embodiments, the compound of formula (I) is a compound of formula (Ic-2): (Ic-2). In certain embodiments, the compound of formula (I) is a compound of formula (If- 1): (If-1). In certain embodiments, the compound of formula (I) is a compound of formula (If-2): (If-2). In certain embodiments, the compound of formula (I) is a compound of formula (Ig-1): (Ig-1). In certain embodiments, the compound of formula (I) is a compound of formula (Ig-2): (Ig-2). In certain embodiments, the compound of formula (I) is a compound of formula (Ih- 1 ): (Ih-1). In certain embodiments, the compound of formula (I) is a compound of formula (Ih-2): (Ih-2). In certain embodiments, the compound of formula (I) is a compound of formula (Ij - 1): (Ij - 1). In certain embodiments, the compound of formula (I) is a compound of formula (Ij-2):

[0119] (Ij-2). In certain embodiments, the compound of formula (I) is a compound of formula (11-1) : (II- 1 ). In certain embodiments, the compound of formula (I) is a compound of formula (II-2): (Il-2).

[0120] In certain embodiments, R1is . In certain embodiments, R1is In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is In certain embodiments, R1is In certain embodiments, R1is In certain embodiments, R1is

[0121] In certain embodiments, R1is In certain embodiments, R1is . In certain embodiments, R1is . In ) certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is In certain embodiments, R1is In certain embodiments, R1is

[0122] In certain embodiments, Lla, Llb, and Llcare each independently selected from the group consisting of optionally substituted C1-C6alkylenyl and optionally substituted C2-C6alkenylenyl.

[0123] In certain embodiments, L2aand L2bare each independently selected from the group consisting of -C(=O)-, -C(=O)O-, -N(RA)C(=O)O-, -C(=O)N(RA)-, -N(RA)C(=O)-, -

[0124] N(RA)C(=O)N(RB)-,

[0125] In certain embodiments, L3is selected from the group consisting of -O- and -N(RA)-.

[0126] In certain embodiments, L4is selected from the group consisting of -S(=O)-, -S(=O)2-, and -S(=O)2N(RA)-. In certain embodiments, ring B is . In certain embodiments, ring B is In certain embodiments, ring B is . In certain embodiments, ring

[0127] B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is

[0128] In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring

[0129] B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is

[0130] In certain embodiments, R8a, R8b, R8c, R8d, R8e, R8f, R8g, R8h, and R81are each independently selected from the group consisting of H, halogen, CN, NO2, C(=O)ORA, C(=O)N(RA)(RB), and optionally substituted C1-C6alkyl, or two geminal substituents selected from the group consisting of R8a, R8b, R8c, R8d, R8e, R8f, R8g, R8h, and R81can combine with the carbon atom to which they are bound to form -C(=O)-.

[0131] In certain embodiments, R9is H.

[0132] In certain embodiments, ring B is In certain embodiments, ring B is In certain embodiments, ring B is In certain embodiments, ring B is . In certain embodiments, ring B . In certain embodiments, ring In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is

[0133] . In certain embodiments, ring B is In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B is . In certain embodiments, ring B In certain embodiments, ring B is In certain embodiments, In certain embodiments, ring B is . In certain embodiments, ring B is In certain embodiments, ring C is . In certain embodiments, ring C

[0134] In certain embodiments, R10a, R10b, R10c, and R10dare each independently selected from the group consisting of H, halogen, CN, NO2, and optionally substituted C1-C6alkyl.

[0135] In certain embodiments, Rl laand Rl lbare each independently selected from the group consisting of H and optionally substituted C1-C6alkyl, wherein Rl laand R10bor R10ccan combine with the atoms to which they are bound to form an optionally susbtituted C3-C5 heterocycloalkyl, and wherein Rl lband R10bor R10ccan combine with the atoms to which they are bound to form an optionally substituted C3-C5 heterocycloalkyl.

[0136] In certain embodiments, Z2is selected from the group consisting of -O- and -N(R12)-.

[0137] In certain embodiments, R12is selected from the group consisting of H and optionally substituted C1-C6alkyl.

[0138] In certain embodiments, ring C is in certain embodiments, ring C is . In certain embodiments, ring C is . In certain embodiments, ring C is . In certain embodiments, ring C is ring C is . In certain embodiments, ring C is . In certain embodiments, ring C is . In certain embodiments, ring C is

[0139] In certain embodiments, R7ais H. In certain embodiments, R7ais F. In certain embodiments, R7ais OCH3. In certain embodiments, R7ais NH2. In certain embodiments, R7ais NHC(=O)CH3. In certain embodiments, R7ais CN. In certain embodiments, R7ais 2- pyridyl. In certain embodiments, R7ais Z-Bu. In certain embodiments, R7ais OCF3. In certain embodiments, R7ais OPh. In certain embodiments, R7ais C(=O)OEt. In certain embodiments, R7ais C(=O)OZ-Bu. In certain embodiments, R7ais benzyl. In certain embodiments, R7ais 3- methoxyphenyl.

[0140] In certain embodiments, R7bis H. In certain embodiments, R713is F. In certain embodiments, R713is OCH3. In certain embodiments, R7bis NH2. In certain embodiments, R7bis NHC(=O)CH3. In certain embodiments, R713is CN. In certain embodiments, R7bis 2- pyridyl. In certain embodiments, R7bis Z-Bu. In certain embodiments, R7bis OCF3. In certain embodiments, R713is OPh. In certain embodiments, R713is C(=O)OEt. In certain embodiments, R7bis C(=O)OZ-Bu. In certain embodiments, R7bis benzyl. In certain embodiments, R713is 3- methoxyphenyl.

[0141] In certain embodiments, R7cis H. In certain embodiments, R7cis F. In certain embodiments, R7cis OCH3. In certain embodiments, R7cis NH2. In certain embodiments, R7cis NHC(=O)CH3. In certain embodiments, R7cis CN. In certain embodiments, R7cis 2- pyridyl. In certain embodiments, R7cis Z-Bu. In certain embodiments, R7cis OCF3. In certain embodiments, R7cis OPh. In certain embodiments, R7cis C(=O)OEt. In certain embodiments, R7cis C(=O)OZ-Bu. In certain embodiments, R7cis benzyl. In certain embodiments, R7cis 3- methoxyphenyl.

[0142] In certain embodiments, R7dis H. In certain embodiments, R7dis F. In certain embodiments, R7dis OCH3. In certain embodiments, R7dis NH2. In certain embodiments, R7d is NHC(=O)CH3. In certain embodiments, R7dis CN. In certain embodiments, R7dis 2- pyridyl. In certain embodiments, R7dis / -Bii. In certain embodiments, R7dis OCF3. In certain embodiments, R7dis OPh. In certain embodiments, R7dis C(=O)OEt. In certain embodiments, R7dis C(=O)Ot-Bu. In certain embodiments, R7dis benzyl. In certain embodiments, R7dis 3- methoxyphenyl.

[0143] In certain embodiments, R7eis H. In certain embodiments, R7eis F. In certain embodiments, R7eis OCH3. In certain embodiments, R7eis NH2. In certain embodiments, R7eis NHC(=O)CH3. In certain embodiments, R7eis CN. In certain embodiments, R7eis 2- pyridyl. In certain embodiments, R7eis / -Bu. In certain embodiments, R7eis OCF3. In certain embodiments, R7eis OPh. In certain embodiments, R7eis C(=O)OEt. In certain embodiments, R7eis C(=O)Ot-Bu. In certain embodiments, R7eis benzyl. In certain embodiments, R7eis 3- methoxyphenyl.

[0144] In certain embodiments, ring D is in certain embodiments, ring D In certain embodiments, ring D is . In certain embodiments, ring D is ring D is In certain embodiments, ring D is In certain embodiments, ring D is

[0145] In certain embodiments, ring D is In certain embodiments, ring D is . In certain embodiments, ring / J is . In certain embodiments, In certain embodiments, ring D is . In certain

[0146] In certain embodiments, Llais -CH2-. In certain embodiments, Llais -(CH2)2-. In certain embodiments, Llais -(CH2)3-. In certain embodiments, Llais -CH=CH-. In certain embodiments, Llbis -CH2-. In certain embodiments, Llbis -(CH2)2-. In certain embodiments, Llbis -(CH2)3-. In certain embodiments, Llbis -CH=CH-. In certain embodiments, Llcis - CH2-. In certain embodiments, Llcis -(CH2)2-. In certain embodiments, Llcis -(CH2)3-. In certain embodiments, Llcis -CH=CH-.

[0147] In certain embodiments, L2ais -NHC(=O)-. In certain embodiments, L2ais -

[0148] C(=O)NH-. In certain embodiments, L2ais -C(=O)N(CH3)-. In certain embodiments, L2ais -

[0149] NHC(=O)NH-. In certain embodiments, L2ais -NHC(=O)N(CH3)-. In certain embodiments, L2ais -N(CH3)C(=O)NH-. In certain embodiments, L2ais -NHC(=O)O-. In certain embodiments, L2ais -C(=O)-. In certain embodiments, L2ais -C(=O)O-. In certain embodiments, L2:is In certain embodiments, L2ais In certain embodiments, L2ais In certain embodiments, L2ais . In certain embodiments, L2ais In certain embodiments, L2ais In certain embodiments, L2ais

[0150] In certain embodiments, L2bis -NHC(=O)-. In certain embodiments, L2bis - C(=O)NH-. In certain embodiments, L2bis -C(=O)N(CH3)-. In certain embodiments, L2bis - NHC(=O)NH-. In certain embodiments, L2bis -NHC(=O)N(CH3)-. In certain embodiments, L2bis -N(CH3)C(=O)NH-. In certain embodiments, L2bis -NHC(=O)O-. In certain embodiments, L2bis -C(=O)-. In certain embodiments, L2bis -C(=O)O-. In certain embodiments, L2bis In certain embodiments, L2bis In certain embodiments, L2bis . In certain embodiments, L2bis . In certain embodiments, L2bis . In certain embodiments, L2bis . In certain embodiments, L2bis

[0151] In certain embodiments, L3is -O-. In certain embodiments, L3is -NH-.

[0152] In certain embodiments, L4is -S(=O)2-. In certain embodiments, L4is -S(=O)2NH-. In certain embodiments, L4is -S(=O)-.

[0153] In certain embodiments, R6is Me. In certain embodiments, R6is Et. In certain embodiments, R6is z-Pr. In certain embodiments, R6is CF3. In certain embodiments, R6is

[0154] CH2NH2. In certain embodiments, R6is C(CH3)3. In certain embodiments, R6is certain embodiments, certain embodiments, R6is . In certain embodiments, R6is embodiments, R6is . In certain embodiments, R6is , in certain embodiments, R6is . In certain embodiments, R6is . In certain H embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is incertain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . INcertain embodiments, R6is In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is in certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is . In certain embodiments, R6is

[0155] In certain embodiments, R1is . In certain embodiments,

[0156] R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is

[0157] . In certain embodiments, R1is In certain embodiments, R1is In certain embodiments, R1is . In certain embodiments, R1is

[0158] In certain embodiments, R1is . In certain embodiments, R1is

[0159] O . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is

[0160] In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is

[0161] . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is

[0162] . In certain embodiments, R1is In certain embodiments, R1is . In certain embodiments, R1is

[0163] . In certain embodiments, R1is

[0164] In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments, R1is . In certain embodiments,

[0165] R1is . In certain embodiments, R1is . In certain embodiments, R1is In certain embodiments, R1is , embodiments, R1is In certain embodiments, certain embodiments, R1is In certain embodiments, R1is certain embodiments, certain embodiments, R1is , embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is embodiments, certain embodiments, R1is , embodiments, certain embodiments, R1is certain embodiments, R1is y ( ) certain embodiments, R1is , embodiments, certain embodiments, R1is , embodiments, certain embodiments, R1is y ( ) , embodiments, certain embodiments, R1is certain embodiments, R1is ,

[0166]

[0167] In certain embodiments, certain embodiments, R1is

[0168] . In certain embodiments, certain embodiments, R1is , embodiments, certain embodiments, R1is , certain embodiments, R1is In certain embodiments, R1is certain embodiments, R1is , certain embodiments, certain embodiments, R1is , certain embodiments, certain embodiments, R1is , . ,

[0169] , certain embodiments, certain embodiments, R1is embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is

[0170] In certain embodiments, certain embodiments, R1is , certain embodiments, certain embodiments, R1is

[0171] . In certain embodiments, certain embodiments, R1

[0172] In certain embodiments, certain embodiments, R1

[0173] . In certain embodiments, certain embodiments, R1is certain embodiments, R1is ,

[0174] In certain embodiments, certain embodiments,

[0175] In certain embodiments, certain embodiments, R1is

[0176] In certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is

[0177] embodiments, R1is In certain embodiments, R1is certain embodiments, certain embodiments, R1is , certain embodiments, certain embodiments, R1is , certain embodiments, R1is In certain embodiments, R1is certain embodiments, R1is In certain embodiments, R1is

[0178] embodiments, certain embodiments, R1is , embodiments, certain embodiments, certain embodiments, certain embodiments, R1is embodiments, certain embodiments, R1is y ( ) , embodiments, certain embodiments, R1is , certain embodiments, certain embodiments, R1is , , embodiments, certain embodiments, certain embodiments, R1is embodiments, R1is O . In certain embodiments, R1is

[0179] In certain embodiments, R1is In certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, certain embodiments, R1is certain embodiments, R1is In certain embodiments, R1is ,

[0180] In certain embodiments, the compound is selected from the group consisting of: 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-picolinoylpiperidin-4-yl)acetamide;

[0181] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-nicotinoylpiperidin-4-yl)acetamide;

[0182] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-isonicotinoylpiperidin-4-yl)acetamide;

[0183] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-hydroxybenzoyl)piperidin-4-yl)acetamide;

[0184] N-(l -(6-aminopicolinoyl)piperidin-4-yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0185] N-(1-(2-aminoisonicotinoyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0186] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-hydroxybenzoyl)piperidin-4-yl)acetamide;

[0187] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-methoxybenzoyl)piperidin-4-yl)acetamide;

[0188] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxybenzoyl)piperidin-4-yl)acetamide;

[0189] N-(l -(6-aminonicotinoyl)piperidin-4-yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0190] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-hydroxybenzoyl)piperidin-4-yl)acetamide;

[0191] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide; 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-picolinoylpyrrolidin-3-yl)methyl)acetamide;

[0192] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-picolinoylpyrrolidin-3 -yl)methyl)acetamide;

[0193] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-picolinoylpyrrolidin-3 -yl)methyl)acetamide;

[0194] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-nicotinoylpyrrolidin-3-yl)methyl)acetamide;

[0195] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-nicotinoylpyrrolidin-3 -yl)methyl)acetamide;

[0196] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-nicotinoylpyrrolidin-3 -yl)methyl)acetamide;

[0197] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-isonicotinoylpyrrolidin-3-yl)methyl)acetamide;

[0198] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-isonicotinoylpyrrolidin-3- yl)methyl)acetamide;

[0199] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-isonicotinoylpyrrolidin-3 - yl)methyl)acetamide;

[0200] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0201] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0202] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0203] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0204] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(2-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0205] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(2-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0206] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-picolinoylpyrrolidin-3-yl)acetamide;

[0207] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-picolinoylpyrrolidin-3 -yl)acetamide;

[0208] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-picolinoylpyrrolidin-3-yl)acetamide;

[0209] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-nicotinoylpyrrolidin-3-yl)acetamide;

[0210] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-nicotinoylpyrrolidin-3 -yl)acetamide;

[0211] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-nicotinoylpyrrolidin-3-yl)acetamide;

[0212] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-isonicotinoylpyrrolidin-3-yl)acetamide;

[0213] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((R)-1-isonicotinoylpyrrolidin-3-yl)acetamide;

[0214] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-isonicotinoylpyrrolidin-3-yl)acetamide;

[0215] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;

[0216] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(3 -hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0217] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(3-hydroxybenzoyl)pyrrolidin-3- yl)acetamide;

[0218] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;

[0219] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(4-hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0220] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(4-hydroxybenzoyl)pyrrolidin-3- yl)acetamide;

[0221] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-methoxybenzoyl)pyrrolidin-3-yl)acetamide;

[0222] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(2-methoxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0223] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(2-methoxybenzoyl)pyrrolidin-3- yl)acetamide;

[0224] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)pyrrolidin-3-yl)acetamide;

[0225] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0226] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(3-methoxybenzoyl)pyrrolidin-3- yl)acetamide;

[0227] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxybenzoyl)pyrrolidin-3-yl)acetamide;

[0228] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0229] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(4-methoxybenzoyl)pyrrolidin-3- yl)acetamide;

[0230] N-(1-(6-aminonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0231] N-((R)-1-(6-aminonicotinoyl)pyrrolidin-3 -yl)-2-(((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0232] N-((S)-1-(6-aminonicotinoyl)pyrrolidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;

[0233] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;

[0234] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(2-hydroxybenzoyl)pyrrolidin-3- yl)acetamide;

[0235] N-(1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0236] N-((R)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0237] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0238] N-((S)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0239] 10,13 -dimethyl-3 -oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0240] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(4-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0241] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0242] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0243] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(3-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0244] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0245] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0246] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(3-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0247] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(3 -hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0248] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(3 -hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;

[0249] N-((1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0250] N-(((R)-1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-

[0251] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0252] N-(((S)-1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-

[0253] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0254] N-(1-(6-aminopicolinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0255] N-((R)-1-(6-aminopicolinoyl)pyrrolidin-3 -yl)-2-(((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0256] N-((S)-1-(6-aminopicolinoyl)pyrrolidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)pyrrolidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)pyrrolidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)pyrrolidine-1- carboxylate;

[0257] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(pyrrolidin-3-yl)acetamide;

[0258] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-(pyrrolidin-3-yl)acetamide;

[0259] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-(pyrrolidin-3-yl)acetamide;

[0260] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-ylmethyl)pyrrolidine-3- carboxamide;

[0261] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(R)-(pyridin-4-ylmethyl)pyrrolidine-3- carboxamide;

[0262] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(S)-(pyridin-4-ylmethyl)pyrrolidine-3- carboxamide;

[0263] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-yl)pyrrolidine-3-carboxamide;

[0264] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(R)-(pyridin-2-yl)pyrrolidine-3-carboxamide;

[0265] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(S)-(pyridin-2-yl)pyrrolidine-3-carboxamide;

[0266] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(pyrrolidin-3-ylmethyl)acetamide;

[0267] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-(pyrrolidin-3-ylmethyl)acetamide;

[0268] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-(pyrrolidin-3-ylmethyl)acetamide;

[0269] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0270] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0271] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;

[0272] N-((1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide; N-(((R)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2-

[0273] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0274] N-(((S)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2-

[0275] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0276] N-((1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0277] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0278] N-(((R)-1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-

[0279] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0280] N-(((S)-1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-

[0281] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide; tert-butyl 3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine-1-carboxylate; tert-butyl (A)-3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine-1- carboxylate; tert-butyl (S)-3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine-1- carboxylate; tert-butyl 4-(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0282] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(piperidin-4-yl)acetamide;

[0283] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0284] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0285] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0286] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3- carboxamide;

[0287] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3- carboxamide;

[0288] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3- carboxamide;

[0289] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0290] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0291] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;

[0292] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;

[0293] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;

[0294] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;

[0295] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide;

[0296] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide; (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide;

[0297] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;

[0298] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;

[0299] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;

[0300] N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-

[0301] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0302] (R )-N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-

[0303] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0304] (5)-N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-

[0305] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0306] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;

[0307] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;

[0308] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;

[0309] N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-

[0310] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cyclopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0311] (R )-N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-

[0312] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cyclopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0313] (5)-N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;

[0314] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;

[0315] (A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;

[0316] (5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;

[0317] N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;

[0318] (R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;

[0319] (5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;

[0320] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)-N- methylacetamide;

[0321] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0322] (A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0323] (5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0324] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0325] (A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0326] (5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0327] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0328] (A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0329] (5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;

[0330] N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;

[0331] (R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;

[0332] (5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;

[0333] N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;

[0334] (R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;

[0335] (5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;

[0336] 2-(((5S,8R,9S,10S,13S,14S,17R)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide; tert-butyl (1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)carbamate; tert-butyl 4-((2-(((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)methyl)piperidine-1-carboxylate;

[0337] N-(1-acetylpiperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; tert-butyl ((1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)methyl)carbamate;

[0338] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-4-yl)acetamide; N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)-3-methoxybenzamide;

[0339] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-4-yl)acetamide;

[0340] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide;

[0341] N-(1-(N-(tert-butyl)sulfamoyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0342] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0343] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-4-yl)acetamide;

[0344] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(3-methoxyphenyl)piperidine-4-carboxamide; methyl 4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0345] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-methoxybenzoyl)piperidin-4- yl)methyl)acetamide; ethyl 4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0346] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-4-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (A)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;

[0347] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;

[0348] (A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;

[0349] (5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;

[0350] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;

[0351] N-((1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)methyl)-3-methoxybenzamide;

[0352] N-(1-(tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0353] N-(1-((A)-tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0354] N-(1-((5)-tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0355] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-4-yl)acetamide;

[0356] (E)-1-(4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperazin-1-yl)-4-(4-methoxyphenyl)but-2-ene- 1, 4-dione;

[0357] N-(1-(tert-butylsulfonyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0358] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxypyridin-2-yl)piperidin-4-yl)acetamide;

[0359] 4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;

[0360] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide; 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide;

[0361] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide;

[0362] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-( 1 -((2-(2,6-dioxopiperidin-3 -yl)- 1,3- dioxoisoindolin-4-yl)glycyl)piperidin-4-yl)acetamide;

[0363] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-( 1 -((2-(2,6-dioxopiperidin-3-yl)- 1,3- dioxoisoindolin-5-yl)glycyl)piperidin-4-yl)acetamide;

[0364] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0365] (A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0366] (5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide; tert-butyl 4-(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0367] N-(1-acetylpiperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0368] (R)-N-( 1 -acetylpiperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 -dimethyl-3 - oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0369] (S)-N-(1-acetylpiperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; methyl 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; methyl (R)-3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; methyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0370] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide; (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide;

[0371] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide; ethyl 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; ethyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; ethyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;

[0372] N-(1-(tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0373] N-((S)-1-((S)-tert-butylsulfinyl)piperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)-

[0374] 10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0375] N-((S)-1-((R)-tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0376] 10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0377] N-((R)-1-((S)-tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0378] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0379] N-((R)-1-((R)-tert-butylsulfinyl)piperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)-

[0380] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0381] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;

[0382] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;

[0383] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;

[0384] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;

[0385] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;

[0386] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;

[0387] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide; (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide;

[0388] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide;

[0389] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;

[0390] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;

[0391] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;

[0392] 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;

[0393] (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;

[0394] (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;

[0395] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-(4-(pyridin-2-yl)phenoxy)acetyl)piperidin-4- yl)acetamide;

[0396] N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0397] 10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0398] (R)-N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0399] 10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0400] (S)-N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0401] 10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0402] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide;

[0403] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide;

[0404] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide; 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;

[0405] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;

[0406] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;

[0407] N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0408] (R)-N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0409] (S)-N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0410] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-(4-(pyridin-2-yl)phenyl)propanoyl)piperidin-4- yl)acetamide;

[0411] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;

[0412] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;

[0413] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;

[0414] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide;

[0415] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide;

[0416] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide; tert-butyl 5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3-difluoropiperidine-1-carboxylate; tert-butyl (R)-5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3- difluoropiperidine-1 -carboxylate; tert-butyl (S)-5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3- difluoropiperidine-1-carboxylate;

[0417] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide;

[0418] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide;

[0419] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4-difluoropiperidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4- difluoropiperidine-1 -carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4- difluoropiperidine-1 -carboxylate;

[0420] N-(5, 5-difluoro-1-(3 -methoxybenzyl)piperidin-3 -yl)-2-

[0421] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0422] (R)-N-(5,5-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-

[0423] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0424] (S)-N-(5,5-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-

[0425] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0426] N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-

[0427] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0428] (R)-N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-

[0429] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0430] (S)-N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-

[0431] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0432] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;

[0433] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;

[0434] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;

[0435] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)-N- methylacetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-methylacetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-methylacetamido)piperidine- 1 -carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-methylacetamido)piperidine- 1 -carboxylate;

[0436] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;

[0437] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide;

[0438] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide;

[0439] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)azetidine-1-carboxylate; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;

[0440] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-(4-methoxyphenyl)-4-oxobutanoyl)piperidin- 4-yl)acetamide;

[0441] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;

[0442] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;

[0443] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;

[0444] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;

[0445] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;

[0446] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;

[0447] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;

[0448] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;

[0449] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;

[0450] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;

[0451] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;

[0452] (S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;

[0453] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(p-tolyl)but-2-enoyl)piperidin-4- yl)acetamide;

[0454] N-(1-(3-(N-(3-cyano-4-methyl-1H-indol-5-yl)sulfamoyl)benzoyl)piperidin-4-yl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0455] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-hydroxyphenyl)-4-oxobut-2- enoyl)piperidin-4-yl)acetamide;

[0456] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(4-(trifluoromethyl)phenyl)but-2- enoyl)piperidin-4-yl)acetamide;

[0457] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(4-(trifluoromethoxy)phenyl)but-2- enoyl)piperidin-4-yl)acetamide;

[0458] 2-(((5S,8R,9S,10S,13S,14S,17S)-3,3-difluoro-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0459] 2-(((5 S, 8R, 9S,10S,13S,14S,17 S)-2-fluoro- 10,13 -dimethyl-3 -oxohexadecahydro-1H- ey cl openta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0460] 2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0461] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0462] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0463] 2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0464] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0465] 2-(((5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0466] 2-(((5aS,5bS,7aS,8S,10aS,10bR,12aS)-5a,7a-dimethyl-2- oxooctadecahydrocyclopenta[5,6]naphtho[1,2-d]azepin-8-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;

[0467] 2-(((5S,8R,9S,10S,13S,14S,17S)-3-cyano-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0468] (R)-2-(((5S,8R,9S,10S,13S,14S,17S)-3-cyano-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0469] (S)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17 S)-3 -cyano- 10,13 -dimethylhexadecahydro- 1 Iley cl openta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0470] 2-(((5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;

[0471] 2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;

[0472] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;

[0473] 2-(((5R,8R,9S,10S,13S,14S,17S)-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0474] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-4,5,6,7,8,9,10,11,12,13,14,15,16,17- tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin- 4-yl)acetamide;

[0475] 2-(((5aR,5bS,7aS,8S,10aS,10bR,12aR)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[2,1-c]azepin-8-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;

[0476] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0477] 2-(((4aS,4bS,6aS,7S,9aS,9bR,l laS)-4a,6a-dimethyl-2-oxohexadecahydro-1H- indeno[4,5-h]isoquinolin-7-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0478] 2-(((4aR,4bS,6aS,7S,9aS,9bR,l laR)-4a,6a-dimethyl-3-oxohexadecahydro-1H- indeno[5,4-f]isoquinolin-7-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0479] 2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin- 4-yl)acetamide;

[0480] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 1,2,3,3a,3b,4,5,5a,6,8,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2- f]indazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0481] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0482] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate;

[0483] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0484] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;

[0485] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0486] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0487] (R)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0488] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0489] (S)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0490] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate;

[0491] 2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 4-yl)acetamide;

[0492] 2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;

[0493] (R)-2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;

[0494] (S)-2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;

[0495] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0496] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0497] (R)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0498] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0499] (S)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0500] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;

[0501] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0502] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-4- yl)acetamide;

[0503] (E)-1-(4-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0504] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetyl)piperazin-1-yl)-4-(4-methoxyphenyl)but-2-ene- 1 ,4-dione; 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0505] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3- yl)acetamide;

[0506] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0507] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3- yl)acetamide;

[0508] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0509] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3- yl)acetamide;

[0510] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0511] 2-(((5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0512] 2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0513] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;

[0514] 3-((5S,8R,9S,10S,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;

[0515] 3-((5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;

[0516] 3-((5S,8R,9S,10S,13S,14S)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;

[0517] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)acetamide;

[0518] N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-(11-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-9-yl)acetamide;

[0519] N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-N-methyl-2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)acetamide;

[0520] 1-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(11-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;

[0521] 3-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-1-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;

[0522] 1-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;

[0523] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-3 -(2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;

[0524] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-(2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;

[0525] 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-3-((11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;

[0526] 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-1-(2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;

[0527] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(9-methyl-2-oxo-6,7,8,9-tetrahydro-2H- pyrano[3,2-g]quinolin-4-yl)ethyl)acetamide;

[0528] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methyl-2-oxo-7,8,9,10-tetrahydro-2H- pyrano[2,3-f]quinolin-4-yl)ethyl)acetamide;

[0529] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- f]pyrido[3 ,2, 1 -ij ]quinolin- 10-yl)methyl)acetamide;

[0530] N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methoxy)acetamide; 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)urea;

[0531] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((7-methoxy-2-oxo-2H-chromen-4-yl)methyl)-N- methylacetamide;

[0532] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((7-methoxy-2-oxo-2H-chromen-4- yl)methyl)acetamide;

[0533] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy -2-oxo- 1,2-dihy droquinolin-4- yl)ethyl)acetamide;

[0534] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-1-methyl-2-oxo- 1 ,2-dihydroquinolin- 4-yl)ethyl)acetamide;

[0535] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(7-methoxy-2-oxo-2H-chromen-4- yl)propyl)acetamide;

[0536] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)-N- methylacetamide;

[0537] N-(2-(7-(2-amino-2-oxoethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2-

[0538] (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0539] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-morpholinoethoxy)-2-oxo-2H-chromen-4- yl)ethyl)acetamide;

[0540] N-(2-(7-(cyanomethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0541] 2-((4-(2-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)ethyl)-2-oxo-2H-chromen-7-yl)oxy)acetic acid;

[0542] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-hydroxyethoxy)-2-oxo-2H-chromen-4- yl)ethyl)acetamide; ethyl 2-((4-(2-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)ethyl)-2-oxo-2H- chromen-7-yl)oxy)acetate;

[0543] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-2-methyl-1-oxo- 1 ,2- dihydroisoquinolin-4-yl)ethyl)acetamide;

[0544] N-(2-(2-benzyl-7-methoxy-1-oxo- 1 ,2-dihydroisoquinolin-4-yl)ethyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0545] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-1-oxo-1H-isochromen-4- yl)ethyl)acetamide;

[0546] N-(2-(7-(2-aminoethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;

[0547] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-(4-methylpiperazin-1-yl)ethoxy)-2-oxo-2H- chromen-4-yl)ethyl)acetamide;

[0548] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;

[0549] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0550] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)acetamide;

[0551] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0552] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)acetamide;

[0553] 2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H- chromen-4-yl)ethyl)acetamide;

[0554] 2-(((4aR,4bS,6aS,7S,9aS,9bR,11aR)-4a,6a-dimethyl-3-oxohexadecahydro-1H- indeno[5,4-f]isoquinolin-7-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide;

[0555] 2-(((4aS,4bS,6aS,7S,9aS,9bR,11aS)-4a,6a-dimethyl-2-oxohexadecahydro-1H- indeno[4,5-h]isoquinolin-7-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide;

[0556] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0557] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-m ethyl-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;

[0558] 2-(((5aS,5bS,7aS,8S,10aS,10bR,12aS)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[1,2-c]azepin-8-yl)oxy)-N-(2-(7-methoxy-2-oxo- 2H-chromen-4-yl)ethyl)acetamide;

[0559] 2-(((5aR,5bS,7aS,8S,10aS,10bR,12aR)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[2,l-c]azepin-8-yl)oxy)-N-(2-(7-methoxy-2-oxo- 2H-chromen-4-yl)ethyl)acetamide;

[0560] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0561] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-methyl-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;

[0562] 2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide;

[0563] 2-(((5 S, 8R, 9S,10S,13S,14S,17 S,E)-3 -(methoxyimino)- 10,13 -dimethylhexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(11 -oxo-2, 3,6, 7-tetrahy dro-lH,5H,l 1H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;

[0564] 2-(((5 S, 8R, 9S,10S,13S,14S,17 S,E)-3 -(hy droxyimino)- 10,13 -dimethylhexadecahy dro--1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(11 -oxo-2, 3, 6, 7-tetrahy dro-lH,5H,l 1H- pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)acetamide;

[0565] 3-((5S,8R,9S,10S,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)propenamide;

[0566] 2-((((5S,8R,9S,10S,13S,14S,E)-10,13-dimethyl-3-oxohexadecahydro-17H- cyclopenta[a]phenanthren-17-ylidene)amino)oxy)-N-(2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;

[0567] 2-((((5S,8R,9S,10S,13S,14S,E)-10,13-dimethyl-3-oxohexadecahydro-17H- cyclopenta[a]phenanthren-17-ylidene)amino)oxy)-N-((11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)acetamide;

[0568] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)acetamide;

[0569] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)acetamide;

[0570] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)-N-methylacetamide;

[0571] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)acetamide;

[0572] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)-N-methylacetamide;

[0573] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)-N-methylacetamide;

[0574] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)-N-methylacetamide;

[0575] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)acetamide;

[0576] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)-N-methylacetamide;

[0577] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)-N-methylacetamide;

[0578] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)acetamide;

[0579] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)propyl)acetamide;

[0580] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-fluoropyridin-3-yl)ethyl)acetamide;

[0581] N-(3-(6-amino-5-cyanopyridin-3-yl)propyl)-2-(((8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0582] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(imidazo[ 1 ,2-a]pyridin-2-yl)ethyl)acetamide;

[0583] N-(2-(1H-pyrrolo[2,3-b]pyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0584] N-(3-(6-acetamido-5-cyanopyridin-3-yl)propyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0585] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0586] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(5-fluoropyridin-3-yl)propyl)acetamide;

[0587] N-(2-(6-amino-5-cyanopyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;

[0588] N-(2-(6-acetamido-5-cyanopyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-

[0589] 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;

[0590] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(4-(pyridin-2-yl)benzyl)acetamide;

[0591] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(4-(pyrimidin-2-yl)pyridin-2-yl)acetamide;

[0592] (5S,8R,9S,10S,13S,14S,17S)-17-((6-(tert-butyl)-1H-benzo[d]imidazol-2-yl)methoxy)- 10,13-dimethylhexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0593] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((6-phenoxy-1H-benzo[d]imidazol- 2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0594] (5S,8R,9S,10S,13S,14S,17S)-17-((4-methoxy-1H-benzo[d]imidazol-2-yl)methoxy)- 10,13-dimethylhexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0595] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((6-(trifluoromethoxy)-1H- benzo[d]imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl 3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)m ethyl)- 1 ,2,4-oxadiazol-3 -yl)piperidine-1- carboxylate; tert-butyl (S)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1,2,4-oxadiazol-3- yl)piperidine-1-carboxylate; tert-butyl (R)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1,2,4-oxadiazol-3- yl)piperidine-1-carboxylate; tert-butyl 3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)m ethyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidine-1- carboxylate; tert-butyl (S)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1,3,4-oxadiazol-2- yl)piperidine-1-carboxylate; tert-butyl (R)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1,3,4-oxadiazol-2- yl)piperidine-1-carboxylate; tert-butyl 2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-benzo[d]imidazole-6-carboxylate; tert-butyl 3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl (R)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate;

[0596] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide; tert-butyl 3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine- 1 -carboxylate; tert-butyl (R)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine-

[0597] 1 -carboxylate; tert-butyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)ethyl)carbamate;

[0598] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0599] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0600] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate;

[0601] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-pivaloylpiperidin-3-yl)-1H- imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0602] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-pivaloylpiperidin-3-yl)- 1H-imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0603] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-pivaloylpiperidin-3-yl)- 1H-imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0604] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-phenylpiperidin-3-yl)oxazol-

[0605] 2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0606] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-phenylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0607] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-phenylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl 4-(2-((((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-4-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl (R)-4-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl ((2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)methyl)carbamate; ethyl 2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-benzo[d]imidazole-7-carboxylate; tert-butyl 4-(2-((((5 S,8R,9S, 10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine-1-carboxylate;

[0608] N-(1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0609] N-((R)-1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0610] N-((S)-1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0611] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(4-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0612] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(4-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0613] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(4-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0614] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(2-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0615] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0616] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(2-fluorobenzyl)piperidin-3-yl)-N-methylacetamide

[0617] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0618] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0619] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0620] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0621] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;

[0622] N-(1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0623] N-((R)-1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0624] N-((S)-1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0625] N-(1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0626] N-((R)-1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0627] N-((S)-1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0628] N-(1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0629] N-((R)-1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0630] N-((S)-1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide; 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0631] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridin-2-ylmethyl)piperidin-3-yl)acetamide;

[0632] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0633] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridin-2-ylmethyl)piperidin-3 -yl)acetamide;

[0634] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0635] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyridin-2-ylmethyl)piperidin-3-yl)acetamide;

[0636] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0637] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;

[0638] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0639] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;

[0640] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0641] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;

[0642] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0643] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrimidin-2-ylmethyl)piperidin-3-yl)acetamide;

[0644] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0645] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrimidin-2-ylmethyl)piperidin-3 -yl)acetamide;

[0646] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0647] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrimidin-2-ylmethyl)piperidin-3 -yl)acetamide;

[0648] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0649] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;

[0650] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0651] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;

[0652] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;

[0653] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0654] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrazin-2-ylmethyl)piperidin-3-yl)acetamide;

[0655] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0656] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrazin-2-ylmethyl)piperidin-3 -yl)acetamide;

[0657] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0658] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrazin-2-ylmethyl)piperidin-3 -yl)acetamide;

[0659] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0660] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((3-fluoropyridin-2-yl)methyl)piperidin-3-yl)-N-methylacetamide;

[0661] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0662] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((3-fluoropyridin-2-yl)methyl)piperidin-3-yl)-N- methylacetamide;

[0663] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0664] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((3 -fluoropyridin-2-yl)methyl)piperidin-3 -yl)-N- methylacetamide;

[0665] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0666] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((5-fluoropyridin-3-yl)methyl)piperidin-3-yl)-N-methylacetamide;

[0667] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0668] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((5-fluoropyridin-3-yl)methyl)piperidin-3-yl)-N- methylacetamide;

[0669] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0670] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((5-fluoropyridin-3 -yl)methyl)piperidin-3 -yl)-N- methylacetamide;

[0671] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-((1-methyl-1H-imidazol-2-yl)methyl)piperidin-3- yl)acetamide;

[0672] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0673] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(( 1 -methyl- 1H-imidazol-2-yl)methyl)piperidin-3 - yl)acetamide;

[0674] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0675] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(( 1 -methyl- 1H-imidazol -2 -yl)methyl)piperidin-3 - yl)acetamide;

[0676] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0677] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0678] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0679] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0680] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0681] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0682] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0683] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(thiazol-4-ylmethyl)piperidin-3-yl)acetamide;

[0684] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0685] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(thiazol-4-ylmethyl)piperidin-3-yl)acetamide;

[0686] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0687] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(thiazol-4-ylmethyl)piperidin-3-yl)acetamide;

[0688] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0689] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0690] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0691] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0692] 2-(((1S,3aS,3bR,5aS, 10aS,10bS, 12aS)-10a, 12a-dimethyl-

[0693] 2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;

[0694] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-( 1 -(3 -fluoropyridin-2 -yl)piperidin-3 -yl)-

[0695] 1,3,4-oxadiazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0696] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(3 -fluoropyri din-2-yl)piperidin-3 -yl)-

[0697] 1,3,4-oxadiazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0698] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((S)-1-(3 -fluoropyri din-2-yl)piperidin-3 -yl)-

[0699] 1.3.4-oxadiazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0700] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-( 1 -(3 -fluoropyri din-2 -yl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a,10b,11, 12, 12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0701] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(3 -fluoropyri din-2-yl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a,10b,11, 12, 12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0702] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((S)-1-(3 -fluoropyri din-2-yl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a,10b,11, 12, 12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0703] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -( 1 -(3 -fluoropyri din-2 -yl)piperidin-3 -yl)-

[0704] 1.2.4-oxadiazol-5-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0705] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -((R)-1-(3 -fluoropyri din-2-yl)piperidin-3 -yl)-

[0706] 1,2,4-oxadiazol-5-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0707] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -((S)-1-(3 -fluoropyri din-2-yl)piperidin-3 -yl)-

[0708] 1,2,4-oxadiazol-5-yl)methoxy)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10, 10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS, 10aS,10bS, 12aS)-1-((5-(1-(2-fluorobenzyl)piperidin-3-yl)-1,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6, 10,10a, 10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(2-fluorobenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(2-fluorobenzyl)piperidin-3-yl)oxazol-2- yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0709] ( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(2-fluorobenzyl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(2-fluorobenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-(1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-((S)-1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)pyrrolidin-3-yl)-1H- imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)pyrrolidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)pyrrolidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0710] 1-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0711] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-4H- 1,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- 4H-1,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- 4H-1,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)oxazol- 2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro- 1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(piperidin-3-yl)oxazol-2- yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-piperidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-piperidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0712] 1-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one;

[0713] 1-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one;

[0714] 1-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0715] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- 1,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- 1,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0716] 1-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one;

[0717] 1-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; 1-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0718] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; l-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0719] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one;

[0720] 1-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0721] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one;

[0722] 1-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0723] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0724] 4-(2-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0725] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-l,3,4-oxadiazol-2-yl)ethyl)-7-methoxy-2H-chromen-2-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-1H- imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; benzyl (2-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate; benzyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate;

[0726] 2-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0727] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)ethan-1-amine;

[0728] 1-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;

[0729] 1-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0730] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;

[0731] 1-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0732] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one;

[0733] 1-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0734] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one;

[0735] 1-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0736] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(pyrrolidin-3-yl)oxazol-2- yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-pyrrolidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-pyrrolidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;

[0737] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(piperidin-3-yl)acetamide;

[0738] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((R)-piperidin-3-yl)acetamide;

[0739] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-piperidin-3-yl)acetamide;

[0740] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(piperidin-3-yl)acetamide;

[0741] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-piperidin-3-yl)acetamide;

[0742] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0743] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-piperidin-3-yl)acetamide;

[0744] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-pivaloylpiperidin-3-yl)acetamide;

[0745] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-pivaloylpiperidin-3 -yl)acetamide;

[0746] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0747] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-pivaloylpiperidin-3 -yl)acetamide;

[0748] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0749] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;

[0750] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;

[0751] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0752] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;

[0753] 4-((5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0754] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-l,3,4-oxadiazol-2-yl)methyl)-7-methoxy-2H-chromen-2-one;

[0755] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0756] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(piperidin-3-yl)acetamide;

[0757] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0758] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-piperidin-3-yl)acetamide;

[0759] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0760] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-piperidin-3-yl)acetamide;

[0761] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0762] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0763] (5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;

[0764] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-(piperidin-3-yl)acetamide;

[0765] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-((R)-piperidin-3-yl)acetamide;

[0766] 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-((S)-piperidin-3-yl)acetamide; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0767] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0768] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0769] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0770] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0771] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;

[0772] 1-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0773] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;

[0774] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0775] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-oxopiperidin-3-yl)acetamide;

[0776] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0777] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-2-oxopiperidin-3-yl)acetamide;

[0778] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0779] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-2-oxopiperidin-3-yl)acetamide;

[0780] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0781] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(2,2,2-trifluoroacetyl)piperidin-3-yl)acetamide;

[0782] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0783] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(2,2,2-trifluoroacetyl)piperidin-3-yl)acetamide;

[0784] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0785] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(2,2,2-trifluoroacetyl)piperidin-3 -yl)acetamide;

[0786] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0787] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6,6-dimethylpiperidin-3-yl)acetamide; 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0788] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-6,6-dimethylpiperidin-3-yl)acetamide;

[0789] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0790] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-6,6-dimethylpiperidin-3-yl)acetamide;

[0791] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0792] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-methylpiperidin-3-yl)acetamide;

[0793] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0794] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3S,6R)-6-methylpiperidin-3-yl)acetamide;

[0795] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0796] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3S,6S)-6-methylpiperidin-3-yl)acetamide;

[0797] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0798] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3R,6S)-6-methylpiperidin-3-yl)acetamide;

[0799] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0800] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3R,6R)-6-methylpiperidin-3-yl)acetamide;

[0801] 5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0802] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;

[0803] (2S,5S)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0804] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;

[0805] (2S,5R)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0806] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;

[0807] (2R,5S)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0808] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;

[0809] (2R,5R)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;

[0810] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0811] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-oxopiperidin-3-yl)acetamide;

[0812] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0813] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-6-oxopiperidin-3-yl)acetamide;

[0814] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0815] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-6-oxopiperidin-3-yl)acetamide;

[0816] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0817] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-(3-methoxyphenyl)pyridin-3-yl)acetamide;

[0818] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0819] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-methyl-2-oxopiperidin-3-yl)acetamide;

[0820] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0821] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-methyl-2-oxopiperidin-3-yl)acetamide;

[0822] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0823] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-methyl-2-oxopiperidin-3 -yl)acetamide;

[0824] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0825] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(4-methylpyrimidin-2-yl)piperidin-3-yl)acetamide;

[0826] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0827] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(4-methylpyrimidin-2-yl)piperidin-3 -yl)acetamide;

[0828] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0829] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(4-methylpyrimidin-2-yl)piperidin-3 -yl)acetamide;

[0830] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0831] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;

[0832] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0833] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrimidin-2-yl)piperidin-3 -yl)acetamide;

[0834] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0835] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrimidin-2-yl)piperidin-3 -yl)acetamide;

[0836] N-(6-benzylpyridin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0837] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamide;

[0838] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0839] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;

[0840] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0841] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;

[0842] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0843] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;

[0844] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0845] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(6-methylpyri din-2 -yl)piperidin-3 -yl)acetamide;

[0846] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0847] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(6-methylpyri din-2-yl)piperidin-3 -yl)acetamide;

[0848] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-

[0849] 2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;

[0850] N-((R)-1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-

[0851] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-

[0852] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0853] N-((S)-1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-

[0854] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0855] N-(1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-

[0856] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-

[0857] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0858] N-((R)-1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-

[0859] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-

[0860] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0861] N-((S)-1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-

[0862] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-

[0863] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;

[0864] N-(1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-

[0865] (((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-

[0866] 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide; tert-butyl 2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2S,5S)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2S,5R)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2R,5S)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2R,5R)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate;

[0867] N-(6-benzylpyridin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamide;

[0868] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;

[0869] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3 - yl)acetamide;

[0870] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3 - yl)acetamide;

[0871] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-phenylpiperidin-3-yl)acetamide;

[0872] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-phenylpiperidin-3 -yl)acetamide; and

[0873] 2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-phenylpiperidin-3 -yl)acetamide.

[0874] The compounds described herein can possess one or more stereocenters, and each stereocenter can exist independently in either the (R) or (S) configuration. In certain embodiments, compounds described herein are present in optically active or racemic forms. It is to be understood that the compounds described herein encompass racemic, optically-active, regioisomeric and stereoisomeric forms, or combinations thereof that possess the therapeutically useful properties described herein. Preparation of optically active forms is achieved in any suitable manner, including by way of non-limiting example, by resolution of the racemic form with recrystallization techniques, synthesis from optically-active starting materials, chiral synthesis, or chromatographic separation using a chiral stationary phase. In certain embodiments, a mixture of one or more isomer is utilized as the therapeutic compound described herein. In other embodiments, compounds described herein contain one or more chiral centers. These compounds are prepared by any means, including stereoselective synthesis, enantioselective synthesis and / or separation of a mixture of enantiomers and / or diastereomers. Resolution of compounds and isomers thereof is achieved by any means including, by way of non-limiting example, chemical processes, enzymatic processes, fractional crystallization, distillation, and chromatography.

[0875] The methods and formulations described herein include the use of N-oxides (if appropriate), crystalline forms (also known as polymorphs), solvates, amorphous phases, and / or pharmaceutically acceptable salts of compounds having the structure of any compound(s) described herein, as well as metabolites and active metabolites of these compounds having the same type of activity. Solvates include water, ether (e.g., tetrahydrofuran, methyl tert-butyl ether) or alcohol (e.g., ethanol) solvates, acetates and the like. In certain embodiments, the compounds described herein exist in solvated forms with pharmaceutically acceptable solvents such as water, and ethanol. In other embodiments, the compounds described herein exist in unsolvated form.

[0876] In certain embodiments, the compound(s) described herein can exist as tautomers. All tautomers are included within the scope of the compounds presented herein.

[0877] In certain embodiments, compounds described herein are prepared as prodrugs. A “prodrug” refers to an agent that is converted into the parent drug in vivo. In certain embodiments, upon in vivo administration, a prodrug is chemically converted to the biologically, pharmaceutically or therapeutically active form of the compound. In other embodiments, a prodrug is enzymatically metabolized by one or more steps or processes to the biologically, pharmaceutically or therapeutically active form of the compound.

[0878] In certain embodiments, sites on, for example, the aromatic ring portion of compound(s) described herein are susceptible to various metabolic reactions. Incorporation of appropriate substituents on the aromatic ring structures may reduce, minimize or eliminate this metabolic pathway. In certain embodiments, the appropriate substituent to decrease or eliminate the susceptibility of the aromatic ring to metabolic reactions is, by way of example only, a deuterium, a halogen, or an alkyl group.

[0879] Compounds described herein also include isotopically-labeled compounds wherein one or more atoms is replaced by an atom having the same atomic number, but an atomic mass or mass number different from the atomic mass or mass number usually found in nature. Examples of isotopes suitable for inclusion in the compounds described herein include and are not limited to2H,3H,nC,13C,14C,36C1,18F,123I,125I,13N,15N,15O,17O,18O,32P, and35S. In certain embodiments, isotopically-labeled compounds are useful in drug and / or substrate tissue distribution studies. In other embodiments, substitution with heavier isotopes such as deuterium affords greater metabolic stability (for example, increased in vivo half-life or reduced dosage requirements). In yet other embodiments, substitution with positron emitting isotopes, such asnC,18F,15O, and13N, is useful in Positron Emission Topography (PET) studies for examining substrate receptor occupancy. Isotopically-labeled compounds are prepared by any suitable method or by processes using an appropriate isotopically-labeled reagent in place of the non-labeled reagent otherwise employed.

[0880] In certain embodiments, the compounds described herein are labeled by other means, including, but not limited to, the use of chromophores or fluorescent moieties, bioluminescent labels, or chemiluminescent labels.

[0881] The compounds described herein, and other related compounds having different substituents are synthesized using techniques and materials described herein and as described, for example, in Fieser & Fieser’s Reagents for Organic Synthesis, Volumes 1-17 (John Wiley and Sons, 1991); Rodd’s Chemistry of Carbon Compounds, Volumes 1-5 and Suppiementals (Elsevier Science Publishers, 1989); Organic Reactions, Volumes 1-40 (John Wiley and Sons, 1991), Larock’s Comprehensive Organic Transformations (VCH Publishers Inc., 1989), March, Advanced Organic Chemistry 4thEd., (Wiley 1992); Carey & Sundberg, Advanced Organic Chemistry 4th Ed., Vols. A and B (Plenum 2000,2001), and Green & Wuts, Protective Groups in Organic Synthesis 3rd Ed., (Wiley 1999) (all of which are incorporated by reference for such disclosure). General methods for the preparation of compound as described herein are modified by the use of appropriate reagents and conditions, for the introduction of the various moieties found in the formula as provided herein.

[0882] Compounds described herein are synthesized using any suitable procedures starting from compounds that are available from commercial sources, or are prepared using procedures described herein.

[0883] In certain embodiments, reactive functional groups, such as hydroxyl, amino, imino, thio or carboxy groups, are protected in order to avoid their unwanted participation in reactions. Protecting groups are used to block some or all of the reactive moieties and prevent such groups from participating in chemical reactions until the protective group is removed. In other embodiments, each protective group is removable by a different means. Protective groups that are cleaved under totally disparate reaction conditions fulfill the requirement of differential removal.

[0884] In certain embodiments, protective groups are removed by acid, base, reducing conditions (such as, for example, hydrogenolysis), and / or oxidative conditions. Groups such as trityl, dimethoxytrityl, acetal and t-butyldimethyl silyl are acid labile and are used to protect carboxy and hydroxy reactive moieties in the presence of amino groups protected with Cbz groups, which are removable by hydrogenolysis, and Fmoc groups, which are base labile. Carboxylic acid and hydroxy reactive moieties are blocked with base labile groups such as, but not limited to, methyl, ethyl, and acetyl, in the presence of amines that are blocked with acid labile groups, such as t-butyl carbamate, or with carbamates that are both acid and base stable but hydrolytically removable.

[0885] In certain embodiments, carboxylic acid and hydroxy reactive moieties are blocked with hydrolytically removable protective groups such as the benzyl group, while amine groups capable of hydrogen bonding with acids are blocked with base labile groups such as Fmoc. Carboxylic acid reactive moieties are protected by conversion to simple ester compounds as exemplified herein, which include conversion to alkyl esters, or are blocked with oxidatively-removable protective groups such as 2,4-dimethoxybenzyl, while coexisting amino groups are blocked with fluoride labile silyl carbamates.

[0886] Allyl blocking groups are useful in the presence of acid- and base- protecting groups since the former are stable and are subsequently removed by metal or pi-acid catalysts. For example, an allyl-blocked carboxylic acid is deprotected with a palladium-catalyzed reaction in the presence of acid labile t-butyl carbamate or base-labile acetate amine protecting groups. Yet another form of protecting group is a resin to which a compound or intermediate is attached. As long as the residue is attached to the resin, that functional group is blocked and does not react. Once released from the resin, the functional group is available to react.

[0887] Typically blocking / protecting groups may be selected from allyl, benzyl (Bn), benzyloxycarbonyl (Cbz), allyloxycarbonyl (Alloc), methyl, ethyl, t-butyl, t- butyldimethylsilyl (TBDMS), 2-(trimethylsilyl)ethoxycarbonyl (Teoc), / -butyl oxy carbonyl (Boc), para-methoxybenzyl (PMB), triphenylmethyl (trityl), acetyl, and fluorenylmethoxycarbonyl (FMOC).

[0888] Other protecting groups, plus a detailed description of techniques applicable to the creation of protecting groups and their removal are described in Greene & Wuts, Protective Groups in Organic Synthesis, 3rd Ed., John Wiley & Sons, New York, NY, 1999, and Kocienski, Protective Groups, Thieme Verlag, New York, NY, 1994, which are incorporated herein by reference for such disclosure.

[0889] Table 1. Exemplary compounds of the disclosure

[0890] Methods

[0891] In one aspect, the disclosure provides a method of treating, preventing, and / or ameliorating cancer in a subject in need thereof. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure and / or the pharmaceutical composition of the disclosure.

[0892] In certain embodiments, the cancer is associated with malignant cell growth and / or hyperplastic cell growth.

[0893] In certain embodiments, the cancer is selected from the group consisting of prostate cancer, breast cancer, ovarian cancer, uterine cancer, endometrial cancer, salivary gland carcinoma, bladder cancer (e.g., urothelial carcinoma), gastrointestinal cancer (e.g., gastric carcinoma and esophageal carcinoma), kidney cancer, oral squamous cell carcinoma, and brain cancer (e.g., glioblastoma). In certain embodiments, the cancer is prostate cancer. In certain embodiments, the prostate cancer is castration-resistant prostate cancer. In certain embodiments, the prostate cancer comprises cells expressing AR-V7.

[0894] In another aspect, the disclosure provides a method of impairing androgen receptor (AR) transactivation and / or androgen receptor dimerization in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure and / or the pharmaceutical composition of the disclosure. In certain embodiments, the subject is further administered at least one additional agent, optionally wherein the at least one additional agent is selected from the group consisting of flutamide, bicalutamide, enzalutamide, apalutamide, darolutamide, dilutamide, finasteride, and dutasteride.

[0895] In another aspect, the disclosure provides a method of inhibiting cell growth in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure and / or the pharmaceutical composition of the disclosure.

[0896] In certain embodiments, the subject is further administered at least one additional agent, optionally wherein the at least one additional agent is selected from the group consisting of flutamide, bicalutamide, enzalutamide, apalutamide, darolutamide, dilutamide, finasteride, dutasteride, abiraterone acetate, abiraterone acetate fine particle, and ketoconazole.

[0897] In certain embodiments, the cell growth inhibited is malignant cell growth and / or hyperplastic cell growth. In certain embodiments, the malignant cell growth is cancer cell growth. In certain embodiments, the cancer cell growth is a hormonal cancer cell growth. In certain embodiments, the hormonal cancer is at least one selected from the group consisting of prostate cancer, breast cancer, ovarian cancer, uterine cancer, endometrial cancer, salivary gland carcinoma, bladder cancer (e.g., urothelial carcinoma), gastrointestinal cancer (e.g., gastric carcinoma and esophageal carcinoma), kidney cancer, oral squamous cell carcinoma, and brain cancer (e.g., glioblastoma). In certain embodiments, the hormonal cancer cell growth is prostate cancer cell growth. In certain embodiments, the prostate cancer cell growth is castration-resistant prostate cancer cell growth. In certain embodiments, the castrationresistant prostate cancer cells express AR-V7.

[0898] In another aspect, the disclosure provides a method of imaging malignant cells and / or hyperplastic cells in a subject. In certain embodiments, the method comprises administering to the subject at least one compound of the disclosure and / or the pharmaceutical composition of the disclosure. In certain embodiments, the method further comprises at least partially exposing the subject to electromagnetic radiation, such that the at least one compound and / or pharmaceutical composition is excited. In certain embodiments, the method further comprises detecting excitation of the at least one compound and / or pharmaceutical composition. In certain embodiments, the method further comprises imaging the subject or a portion thereof, wherein the malignant cells and / or hyperplastic cells are imaged.

[0899] In certain embodiments, the malignant cells are cancer cells. In certain embodiments, the cancer cells are hormonal cancer cells. In certain embodiments, the hormonal cancer cells are at least one selected from the group consisting of prostate cancer cells, breast cancer cells, ovarian cancer cells, uterine cancer cells, endometrial cancer cells, salivary gland cancer cells, bladder cancer cells (e.g., urothelial cancer cells), gastrointestinal cancer cells (e.g., gastric cancer cells and esophageal cancer cells), kidney cancer cells, liver cancer cells, oral squamous cancer cells, and brain cancer cells. In certain embodiments, the hormonal cancer cells are prostate cancer cells. In certain embodiments, the prostate cancer cells are castration-resistance prostate cancer cells. In certain embodiments, the castration-resistance prostate cancer cells express AR-V7. In certain embodiments, the imaging is repeated such that activity of androgen metabolism is measured.

[0900] Administration / Dosage / Formulations

[0901] The regimen of administration may affect what constitutes an effective amount. The therapeutic formulations may be administered to the subject either prior to or after the onset of the disease or disorder. Further, several divided dosages, as well as staggered dosages may be administered daily or sequentially, or the dose may be continuously infused, or may be a bolus injection. Further, the dosages of the therapeutic formulations may be proportionally increased or decreased as indicated by the exigencies of the therapeutic or prophylactic situation.

[0902] Administration of the compositions described herein to a patient, preferably a mammal, more preferably a human, may be carried out using known procedures, at dosages and for periods of time effective to treat the disease or disorder in the patient. An effective amount of the therapeutic compound necessary to achieve a therapeutic effect may vary according to factors such as the state of the disease or disorder in the patient; the age, sex, and weight of the patient; and the ability of the therapeutic compound to treat the disease or disorder in the patient. Dosage regimens may be adjusted to provide the optimum therapeutic response. For example, several divided doses may be administered daily or the dose may be proportionally reduced as indicated by the exigencies of the therapeutic situation. A nonlimiting example of an effective dose range for a therapeutic compound described herein is from about 1 and 5,000 mg / kg of body weight / per day. One of ordinary skill in the art would be able to study the relevant factors and make the determination regarding the effective amount of the therapeutic compound without undue experimentation.

[0903] Actual dosage levels of the active ingredients in the pharmaceutical compositions described herein may be varied so as to obtain an amount of the active ingredient that is effective to achieve the desired therapeutic response for a particular patient, composition, and mode of administration, without being toxic to the patient.

[0904] In particular, the selected dosage level depends upon a variety of factors including the activity of the particular compound employed, the time of administration, the rate of excretion of the compound, the duration of the treatment, other drugs, compounds or materials used in combination with the compound, the age, sex, weight, condition, general health and prior medical history of the patient being treated, and like factors well, known in the medical arts.

[0905] A medical doctor, e.g., physician or veterinarian, having ordinary skill in the art may readily determine and prescribe the effective amount of the pharmaceutical composition required. For example, the physician or veterinarian could start doses of the compounds described herein employed in the pharmaceutical composition at levels lower than that required in order to achieve the desired therapeutic effect and gradually increase the dosage until the desired effect is achieved.

[0906] In particular embodiments, it is especially advantageous to formulate the compound in dosage unit form for ease of administration and uniformity of dosage. Dosage unit form as used herein refers to physically discrete units suited as unitary dosages for the patients to be treated; each unit containing a predetermined quantity of therapeutic compound calculated to produce the desired therapeutic effect in association with the required pharmaceutical vehicle. The dosage unit forms of the compound(s) described herein are dictated by and directly dependent on (a) the unique characteristics of the therapeutic compound and the particular therapeutic effect to be achieved, and (b) the limitations inherent in the art of compounding / formulating such a therapeutic compound.

[0907] In certain embodiments, the compositions described herein are formulated using one or more pharmaceutically acceptable excipients or carriers. In certain embodiments, the pharmaceutical compositions described herein comprise a therapeutically effective amount of a compound described herein and a pharmaceutically acceptable carrier.

[0908] The carrier may be a solvent or dispersion medium containing, for example, water, ethanol, polyol (for example, glycerol, propylene glycol, and liquid polyethylene glycol, and the like), suitable mixtures thereof, and vegetable oils. The proper fluidity may be maintained, for example, by the use of a coating such as lecithin, by the maintenance of the required particle size in the case of dispersion and by the use of surfactants. Prevention of the action of microorganisms may be achieved by various antibacterial and antifungal agents, for example, parabens, chlorobutanol, phenol, ascorbic acid, thimerosal, and the like. In many cases, it is preferable to include isotonic agents, for example, sugars, sodium chloride, or polyalcohols such as mannitol and sorbitol, in the composition. Prolonged absorption of the injectable compositions may be brought about by including in the composition an agent which delays absorption, for example, aluminum monostearate or gelatin.

[0909] In certain embodiments, the compositions described herein are administered to the patient in dosages that range from one to five times per day or more. In other embodiments, the compositions described herein are administered to the patient in range of dosages that include, but are not limited to, once every day, every two, days, every three days to once a week, and once every two weeks. It is readily apparent to one skilled in the art that the frequency of administration of the various combination compositions described herein varies from individual to individual depending on many factors including, but not limited to, age, disease or disorder to be treated, gender, overall health, and other factors. Thus, administration of the compounds and compositions described herein should not be construed to be limited to any particular dosage regime and the precise dosage and composition to be administered to any patient is determined by the attending physician taking all other factors about the patient into account.

[0910] The compound(s) described herein for administration may be in the range of from about 1 pg to about 10,000 mg, about 20 pg to about 9,500 mg, about 40 pg to about 9,000 mg, about 75 pg to about 8,500 mg, about 150 pg to about 7,500 mg, about 200 pg to about 7,000 mg, about 350 pg to about 6,000 mg, about 500 pg to about 5,000 mg, about 750 pg to about 4,000 mg, about 1 mg to about 3,000 mg, about 10 mg to about 2,500 mg, about 20 mg to about 2,000 mg, about 25 mg to about 1,500 mg, about 30 mg to about 1,000 mg, about 40 mg to about 900 mg, about 50 mg to about 800 mg, about 60 mg to about 750 mg, about 70 mg to about 600 mg, about 80 mg to about 500 mg, and any and all whole or partial increments therebetween.

[0911] In some embodiments, the dose of a compound described herein is from about 1 mg and about 2,500 mg. In some embodiments, a dose of a compound described herein used in compositions described herein is less than about 10,000 mg, or less than about 8,000 mg, or less than about 6,000 mg, or less than about 5,000 mg, or less than about 3,000 mg, or less than about 2,000 mg, or less than about 1,000 mg, or less than about 500 mg, or less than about 200 mg, or less than about 50 mg. Similarly, in some embodiments, a dose of a second compound as described herein is less than about 1,000 mg, or less than about 800 mg, or less than about 600 mg, or less than about 500 mg, or less than about 400 mg, or less than about 300 mg, or less than about 200 mg, or less than about 100 mg, or less than about 50 mg, or less than about 40 mg, or less than about 30 mg, or less than about 25 mg, or less than about 20 mg, or less than about 15 mg, or less than about 10 mg, or less than about 5 mg, or less than about 2 mg, or less than about 1 mg, or less than about 0.5 mg, and any and all whole or partial increments thereof.

[0912] In certain embodiments, a composition as described herein is a packaged pharmaceutical composition comprising a container holding a therapeutically effective amount of a compound described herein, alone or in combination with a second pharmaceutical agent; and instructions for using the compound to treat, or reduce one or more symptoms of a disease or disorder in a patient.

[0913] Formulations may be employed in admixtures with conventional excipients, z.e., pharmaceutically acceptable organic or inorganic carrier substances suitable for oral, parenteral, nasal, intravenous, subcutaneous, enteral, or any other suitable mode of administration, known to the art. The pharmaceutical preparations may be sterilized and if desired mixed with auxiliary agents, e.g., lubricants, preservatives, stabilizers, wetting agents, emulsifiers, salts for influencing osmotic pressure buffers, coloring, flavoring and / or aromatic substances and the like. They may also be combined where desired with other active agents, e.g., other analgesic agents.

[0914] Routes of administration of any of the compositions described herein include oral, nasal, rectal, intravaginal, parenteral, buccal, sublingual or topical. The compounds for use in the compositions described herein can be formulated for administration by any suitable route, such as for oral or parenteral, for example, transdermal, transmucosal (e.g., sublingual, lingual, (trans)buccal, (trans)urethral, vaginal (e.g, trans- and perivaginally), (intra)nasal and (trans)rectal), intravesical, intrapulmonary, intraduodenal, intragastrical, intrathecal, subcutaneous, intramuscular, intradermal, intra-arterial, intravenous, intrabronchial, inhalation, and topical administration.

[0915] Suitable compositions and dosage forms include, for example, tablets, capsules, caplets, pills, gel caps, troches, dispersions, suspensions, solutions, syrups, granules, beads, transdermal patches, gels, powders, pellets, magmas, lozenges, creams, pastes, plasters, lotions, discs, suppositories, liquid sprays for nasal or oral administration, dry powder or aerosolized formulations for inhalation, compositions and formulations for intravesical administration and the like. It should be understood that the formulations and compositions described herein are not limited to the particular formulations and compositions that are described herein.

[0916] Oral Administration

[0917] For oral application, particularly suitable are tablets, dragees, liquids, drops, suppositories, or capsules, caplets and gelcaps. The compositions intended for oral use may be prepared according to any method known in the art and such compositions may contain one or more agents selected from the group consisting of inert, non-toxic pharmaceutically excipients that are suitable for the manufacture of tablets. Such excipients include, for example an inert diluent such as lactose; granulating and disintegrating agents such as cornstarch; binding agents such as starch; and lubricating agents such as magnesium stearate. The tablets may be uncoated or they may be coated by known techniques for elegance or to delay the release of the active ingredients. Formulations for oral use may also be presented as hard gelatin capsules wherein the active ingredient is mixed with an inert diluent.

[0918] For oral administration, the compound(s) described herein can be in the form of tablets or capsules prepared by conventional means with pharmaceutically acceptable excipients such as binding agents (e.g., polyvinylpyrrolidone, hydroxypropylcellulose or hydroxypropyl methylcellulose); fillers (e.g., cornstarch, lactose, microcrystalline cellulose or calcium phosphate); lubricants (e.g., magnesium stearate, talc, or silica); disintegrates (e.g., sodium starch glycollate); or wetting agents (e.g., sodium lauryl sulphate). If desired, the tablets may be coated using suitable methods and coating materials such as OPADRY™ film coating systems available from Colorcon, West Point, Pa. (e.g, OPADRY™ OY Type, OYC Type, Organic Enteric OY-P Type, Aqueous Enteric OY-A Type, OY-PM Type and OPADRY™ White, 32K18400). Liquid preparation for oral administration may be in the form of solutions, syrups or suspensions. The liquid preparations may be prepared by conventional means with pharmaceutically acceptable additives such as suspending agents (e.g., sorbitol syrup, methyl cellulose or hydrogenated edible fats); emulsifying agent (e.g., lecithin or acacia); non-aqueous vehicles (e.g., almond oil, oily esters or ethyl alcohol); and preservatives (e.g., methyl or propyl p-hydroxy benzoates or sorbic acid).

[0919] Parenteral Administration

[0920] For parenteral administration, the compounds as described herein may be formulated for injection or infusion, for example, intravenous, intramuscular or subcutaneous injection or infusion, or for administration in a bolus dose and / or continuous infusion. Suspensions, solutions or emulsions in an oily or aqueous vehicle, optionally containing other formulatory agents such as suspending, stabilizing and / or dispersing agents may be used.

[0921] Sterile injectable forms of the compositions described herein may be aqueous or oleaginous suspension. These suspensions may be formulated according to techniques known in the art using suitable dispersing or wetting agents and suspending agents. The sterile injectable preparation may also be a sterile injectable solution or suspension in a non-toxic parenterally-acceptable diluent or solvent, for example as a solution in 1, 3 -butanediol. Among the acceptable vehicles and solvents that may be employed are water, Ringer’s solution and isotonic sodium chloride solution. Sterile, fixed oils are conventionally employed as a solvent or suspending medium. For this purpose, any bland fixed oil may be employed including synthetic mono- or di-glycerides. Fatty acids, such as oleic acid and its glyceride derivatives are useful in the preparation of injectables, as are natural pharmaceutically acceptable oils, such as olive oil or castor oil, especially in their polyoxyethylated versions. These oil solutions or suspensions may also contain a long-chain alcohol diluent or dispersant, such as Ph. Helv or similar alcohol.

[0922] Additional Administration Forms

[0923] Additional dosage forms suitable for use with the compound(s) and compositions described herein include dosage forms as described in U.S. Patents Nos. 6,340,475; 6,488,962; 6,451,808; 5,972,389; 5,582,837; and 5,007,790. Additional dosage forms suitable for use with the compound(s) and compositions described herein also include dosage forms as described in U.S. Patent Applications Nos. 20030147952; 20030104062; 20030104053; 20030044466; 20030039688; and 20020051820. Additional dosage forms suitable for use with the compound(s) and compositions described herein also include dosage forms as described in PCT Applications Nos. WO 03 / 35041; WO 03 / 35040; WO 03 / 35029; WO 03 / 35177; WO 03 / 35039; WO 02 / 96404; WO 02 / 32416; WO 01 / 97783; WO 01 / 56544; WO 01 / 32217; WO 98 / 55107; WO 98 / 11879; WO 97 / 47285; WO 93 / 18755; and WO 90 / 11757.

[0924] Controlled Release Formulations and Drug Delivery Systems

[0925] In certain embodiments, the formulations described herein can be, but are not limited to, short-term, rapid-offset, as well as controlled, for example, sustained release, delayed release and pulsatile release formulations.

[0926] The term sustained release is used in its conventional sense to refer to a drug formulation that provides for gradual release of a drug over an extended period of time, and that may, although not necessarily, result in substantially constant blood levels of a drug over an extended time period. The period of time may be as long as a month or more and should be a release which is longer that the same amount of agent administered in bolus form.

[0927] For sustained release, the compounds may be formulated with a suitable polymer or hydrophobic material which provides sustained release properties to the compounds. As such, the compounds for use with the method(s) described herein may be administered in the form of microparticles, for example, by injection or in the form of wafers or discs by implantation. In some cases, the dosage forms to be used can be provided as slow or controlled- release of one or more active ingredients therein using, for example, hydropropylmethyl cellulose, other polymer matrices, gels, permeable membranes, osmotic systems, multilayer coatings, microparticles, liposomes, or microspheres or a combination thereof to provide the desired release profile in varying proportions. Suitable controlled-release formulations known to those of ordinary skill in the art, including those described herein, can be readily selected for use with the pharmaceutical compositions described herein. Thus, single unit dosage forms suitable for oral administration, such as tablets, capsules, gelcaps, and caplets that are adapted for controlled-release are encompassed by the compositions and dosage forms described herein.

[0928] Most controlled-release pharmaceutical products have a common goal of improving drug therapy over that achieved by their non-controlled counterparts. Ideally, the use of an optimally designed controlled-release preparation in medical treatment is characterized by a minimum of drug substance being employed to cure or control the condition in a minimum amount of time. Advantages of controlled-release formulations include extended activity of the drug, reduced dosage frequency, and increased patient compliance. In addition, controlled-release formulations can be used to affect the time of onset of action or other characteristics, such as blood level of the drug, and thus can affect the occurrence of side effects.

[0929] Most controlled-release formulations are designed to initially release an amount of drug that promptly produces the desired therapeutic effect, and gradually and continually release of other amounts of drug to maintain this level of therapeutic effect over an extended period of time. In order to maintain this constant level of drug in the body, the drug must be released from the dosage form at a rate that will replace the amount of drug being metabolized and excreted from the body.

[0930] Controlled-release of an active ingredient can be stimulated by various inducers, for example pH, temperature, enzymes, water, or other physiological conditions or compounds. The term “controlled-release component” is defined herein as a compound or compounds, including, but not limited to, polymers, polymer matrices, gels, permeable membranes, liposomes, or microspheres or a combination thereof that facilitates the controlled-release of the active ingredient. In some embodiments, the compound(s) described herein are administered to a patient, alone or in combination with another pharmaceutical agent, using a sustained release formulation. In some embodiments, the compound(s) described herein are administered to a patient, alone or in combination with another pharmaceutical agent, using a sustained release formulation.

[0931] The term delayed release is used herein in its conventional sense to refer to a drug formulation that provides for an initial release of the drug after some delay following drug administration and that mat, although not necessarily, includes a delay of from about 10 minutes up to about 12 hours.

[0932] The term pulsatile release is used herein in its conventional sense to refer to a drug formulation that provides release of the drug in such a way as to produce pulsed plasma profiles of the drug after drug administration.

[0933] The term immediate release is used in its conventional sense to refer to a drug formulation that provides for release of the drug immediately after drug administration.

[0934] As used herein, short-term refers to any period of time up to and including about 8 hours, about 7 hours, about 6 hours, about 5 hours, about 4 hours, about 3 hours, about 2 hours, about 1 hour, about 40 minutes, about 20 minutes, or about 10 minutes and any or all whole or partial increments thereof after drug administration after drug administration.

[0935] As used herein, rapid-offset refers to any period of time up to and including about 8 hours, about 7 hours, about 6 hours, about 5 hours, about 4 hours, about 3 hours, about 2 hours, about 1 hour, about 40 minutes, about 20 minutes, or about 10 minutes, and any and all whole or partial increments thereof after drug administration.

[0936] Dosing

[0937] The therapeutically effective amount or dose of a compound described herein depends on the age, sex and weight of the patient, the current medical condition of the patient and the progression of the disease or disorder in the patient being treated. The skilled artisan is able to determine appropriate dosages depending on these and other factors.

[0938] A suitable dose of a compound described herein can be in the range of from about 0.01 mg to about 5,000 mg per day, such as from about 0.1 mg to about 1,000 mg, for example, from about 1 mg to about 500 mg, such as about 5 mg to about 250 mg per day. The dose may be administered in a single dosage or in multiple dosages, for example from 1 to 4 or more times per day. When multiple dosages are used, the amount of each dosage may be the same or different. For example, a dose of 1 mg per day may be administered as two 0.5 mg doses, with about a 12-hour interval between doses.

[0939] It is understood that the amount of compound dosed per day may be administered, in non-limiting examples, every day, every other day, every 2 days, every 3 days, every 4 days, or every 5 days. For example, with every other day administration, a 5 mg per day dose may be initiated on Monday with a first subsequent 5 mg per day dose administered on Wednesday, a second subsequent 5 mg per day dose administered on Friday, and so on.

[0940] In the case wherein the patient’s status does improve, upon the doctor’s discretion the administration of the compound(s) described herein is optionally given continuously; alternatively, the dose of drug being administered is temporarily reduced or temporarily suspended for a certain length of time (i.e., a “drug holiday”). The length of the drug holiday optionally varies between 2 days and 1 year, including by way of example only, 2 days, 3 days, 4 days, 5 days, 6 days, 7 days, 10 days, 12 days, 15 days, 20 days, 28 days, 35 days, 50 days, 70 days, 100 days, 120 days, 150 days, 180 days, 200 days, 250 days, 280 days, 300 days, 320 days, 350 days, or 365 days. The dose reduction during a drug holiday includes from 10%-100%, including, by way of example only, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 100%.

[0941] Once improvement of the patient’s conditions has occurred, a maintenance dose is administered if necessary. Subsequently, the dosage or the frequency of administration, or both, is reduced to a level at which the improved disease is retained. In certain embodiments, patients require intermittent treatment on a long-term basis upon any recurrence of symptoms and / or infection.

[0942] The compounds described herein can be formulated in unit dosage form. The term “unit dosage form” refers to physically discrete units suitable as unitary dosage for patients undergoing treatment, with each unit containing a predetermined quantity of active material calculated to produce the desired therapeutic effect, optionally in association with a suitable pharmaceutical carrier. The unit dosage form may be for a single daily dose or one of multiple daily doses (e.g., about 1 to 4 or more times per day). When multiple daily doses are used, the unit dosage form may be the same or different for each dose.

[0943] Toxicity and therapeutic efficacy of such therapeutic regimens are optionally determined in cell cultures or experimental animals, including, but not limited to, the determination of the LD50(the dose lethal to 50% of the population) and the ED50(the dose therapeutically effective in 50% of the population). The dose ratio between the toxic and therapeutic effects is the therapeutic index, which is expressed as the ratio between LD50and ED50. The data obtained from cell culture assays and animal studies are optionally used in formulating a range of dosage for use in human. The dosage of such compounds lies preferably within a range of circulating concentrations that include the ED50with minimal toxicity. The dosage optionally varies within this range depending upon the dosage form employed and the route of administration utilized. Those skilled in the art will recognize, or be able to ascertain using no more than routine experimentation, numerous equivalents to the specific procedures, embodiments, claims, and examples described herein. Such equivalents are considered to be within the scope of this disclosure and covered by the claims appended hereto. For example, it should be understood, that modifications in reaction conditions, including but not limited to reaction times, reaction size / volume, and experimental reagents, such as solvents, catalysts, pressures, atmospheric conditions, e.g., nitrogen atmosphere, and reducing / oxi dizing agents, with art- recognized alternatives and using no more than routine experimentation, are within the scope of the present application.

[0944] It is to be understood that wherever values and ranges are provided herein, all values and ranges encompassed by these values and ranges, are meant to be encompassed within the scope of the present disclosure. Moreover, all values that fall within these ranges, as well as the upper or lower limits of a range of values, are also contemplated by the present application.

[0945] The following examples further illustrate aspects of the present disclosure. However, they are in no way a limitation of the teachings or disclosure of the present disclosure as set forth herein.

[0946] EXAMPLES

[0947] Various embodiments of the present application can be better understood by reference to the following Examples which are offered by way of illustration. The scope of the present application is not limited to the Examples given herein.

[0948] Materials and Methods

[0949] Unless otherwise noted, reagents and solvents were used as received from commercial suppliers. All non-aqueous reactions were carried out, stirred under an atmosphere of dry nitrogen or argon (unless otherwise noted). Proton nuclear magnetic resonance spectra were obtained on a Bruker AVANCE 400 spectrometer at 400 MHz. Spectra are given in ppm (6) and coupling constants, J values, are reported in hertz (Hz). Tetramethyl silane was used as an internal standard for proton nuclear magnetic resonance.19F (376 MHz) were taken with 'H decoupling and chemical shifts were not corrected with an external standard. Mass spectra and LCMS analyses were obtained using a Waters Acquity UPLC-MS spectrometer using Electron spray Ionization. NMR and MS data for certain exemplary compounds are provided herein. Key proton NMR resonances (e.g., methyl) are separately reported where appropriate when obscured by other overlapping resonances.

[0950] Method A: To an ice-cold solution of alcohol (1.0 eq.) in CH2Cl2(10 Vol), indium (III) chloride (0.25 Eq.) was added. After 20 min, ethyl diazoacetate 90% in CH2Cl2(2.0 eq.) was slowly added at the same temperature over a period of 20 min. The reaction mixture was stirred for 20 min at 0 °C and then allowed to warm to room temperature. After 18 hr, the reaction mixture was diluted with ice water and extracted with CH2Cl2(2 x 20 Vol). The combined organic layers were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude compound. ESI MS analysis did not show desired product mass due to poor ionization.

[0951] Method B: To an ice-cold solution of ester (1.0 eq) in a mixture of THF (10 Vol.) and water (10 Vol.) was added LiOH. H2O (3.0 eq.). The reaction was allowed to warm to room temperature and stirred. After 18 hr, the reaction mixture was diluted with chilled 2 N HC1 solution and the pH adjusted to ~2. The resulting mixture was extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude acid.

[0952] Method C: To an ice-cold solution of acid (1.0 eq.) in CH2Cl2(20 Vol.) was added triethylamine (4.0 eq.) followed by l-ethyl-3-(3-dimethylaminopropyl)carbodiimide (1.5 eq.) and hydroxybenzotriazole hydrate (1.5 eq). After 10 min, the amine (1.2 eq.) was added and the reaction was stirred at room temperature for 18 hr. The reaction mixture was diluted with chilled satd. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amide.

[0953] Method D: To an ice-cold solution of the N-Boc intermediate (1.0 eq.) in 2,2,2- trifluoroethan-1-ol (6 Vol) was added chlorotrimethylsilane (2.0 eq.). After 3 hr, the reaction mixture was concentrated under reduced pressure to give the crude amine.

[0954] Method E: To a solution of acid (1.0 eq) in CH2Cl2(10 Vol.) was added triethylamine (4.0 eq.), propyl phosphonic anhydride in ethyl acetate (50%) (2.0 eq.) and amine hydrochloride or amine (1.2 eq.). After 18 hr, the reaction mixture was diluted with satd. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give crude amide.

[0955] Method F: To a solution of potassium 3 -m ethoxy-3 -oxopropanoate (1.5 eq.) in THF (20 Vol.), magnesium chloride (1.0 eq.) was added. The reaction mixture was heated to 50 °C and stirred for 4h. In parallel, a second flask was charged with the CBz protected acid (1.0 eq.) and N-ethyl-N-isopropylpropan-2-amine (2.0 eq.) in THF (10 Vol). Di(U / -imidazol-1- yl)methanone (1.2 eq.) was added portion-wise at 0 °C. The mixture was allowed to warm to 25 °C. After 1 hr, the resulting reaction mixture was added to the malonate suspension slowly at 0 °C.

[0956] After 16 h, the solvent was evaporated. The crude residue was diluted with EtOAc (20 Vol.) and then washed with saturated NaHCO3solution (10 Vol.). The combined organics layers were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ketone.

[0957] Method G: To a solution of phenol (1.0 eq.) in toluene (10 vol.) was added the ketone intermediate (1.0 eq.) and indium (III) chloride (0.4 eq.) at 25 °C. The mixture was heated to 80 °C. After 12h, reaction was diluted with DCM (20 Vol.) and washed with water (10 Vol.). The organic layer was dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude N-Cbz protected product.

[0958] Method H: To a solution of N-Cbz intermediate (1.0 eq.) in methanol (10 Vol.) and CH2Q2 (10 Vol.) was added palladium on carbon 50 wt% wet (0.2 eq) under hydrogen bladder pressure at 25 °C. After 8 hr, the reaction mixture was filtered through a celite pad using methanol. The filtrate was concentrated under reduced pressure to give the crude amine.

[0959] Method I: To a solution of acetal (1.0 eq.) in CH2Cl2(10 vol.) trifluoroacetic acid (1.0 eq.) was added at room temperature. After 8 hr, the reaction mass was diluted with sat. sodium bicarbonate solution and then extracted with ethyl acetate (2 x 20 Vol.). The combined organic layers were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ketone.

[0960] Method J: To a solution of ketone intermediate (1.0 eq.) in toluene (20 vol.) was added / ?-toluenesulfonic acid monohydrate (0.1 eq.) and ethylene glycol (5.0 eq.). The reaction was heated to 80 °C for 6 hr. Afterwards, the reaction mixture was diluted with satd. sodium bicarbonate solution and extracted with CH2Q2 (2 x 30 vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude acetal.

[0961] Method K: A solution of amide (1.0 eq.) in THF (20 Vol.) was added LAH (2 M) in THF (3.0 eq.) at 0 °C. The mixture was carefully warmed to 68 °C. After 8 hr, the reaction mixture was cooled to 0 °C and then treated with sat. sodium sulphate solution. The reaction mixture was filtered through a celite pad using ethyl acetate (30 Vol.). The filtrate was dried over anhydrous sodium sulphate and concentrated under reduced pressure to give the crude amine.

[0962] Method L: To a solution of ester (1.0 eq.) in methanol (2 Vol) was added the amine in methanol (7 N) (25 Vol.) in a sealed tube at 25 °C. After 8 h, the reaction mixture was concentrated under reduced pressure to give the crude amide.

[0963] Method M: To a solution of alcohol (1.0 eq.) in CH2Cl2(30 Vol.) was added rhodium(II) acetate dimer (0.12 eq.) at 0 °C. After 15 min, ethyl diazoacetate 90% in CH2Cl2(6.0 eq.) was added slowly over 15 min. After 2 hr, the reaction mixture was filtered through a celite pad using DCM (2 x 20 Vol.). The filtrate was concentrated under reduced pressure to give the crude ether.

[0964] Method N: To an ice-cold solution of amine intermediate I (1.0 eq.) in CH2Cl2(10 vol.) was added amine intermediate II (1.0 eq.), bis(trichloromethyl) carbonate (0.3 eq.) and triethylamine (3.0 eq.). After 4 hr, the reaction mixture was diluted with water (10 vol.) and extracted using CH2Cl2(2 x 30 vol). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude unsymmetrical urea.

[0965] Method O. To a solution of alcohol (1.0 eq.) in toluene (20 Vol.) was added dimethyl 3 -oxopentanedioate (1.0 eq) and triisopropoxytitanium(IV) chloride (2.0 eq.) in toluene (10 Vol.) at 0 °C. The mixture was then heated to 110 °C. After 16h, the reaction was cooled and then concentrated. The resulting residue was diluted with CH2Cl2(50 Vol.) and washed with saturated potassium sodium tartrate solution (20 Vol.). The organic layer was dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ester.

[0966] Method P: To an ice-cold solution of di(U / -imidazol-1-yl)methanone (1.2 eq.) in THF (10 vol.) was added potassium 3-methoxy-3-oxopropanoate (1.5 eq.), magnesium chloride (1.0 eq.), and the acid intermediate (1.0 eq.). After 18 hr, the reaction mixture was diluted with water (10 vol.) and extracted with EtOAc (2 x 30 vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ketone.

[0967] Method Q. To a solution of alcohol (1.0 eq.) and either N-Cbz or N-Boc ketone intermediate (1.0 eq.) in toluene (20 Vol.) was added indium(III) chloride (0.4 eq.) at room temperature. The reaction was heated to 80 °C. After 16h, the solvent was evaporated. The residue was diluted with water (20 Vol.) and the mixture extracted with CH2Cl2(50 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude compound.

[0968] Method R: To an ice-cold solution of alcohol intermediate (1.0 eq.) in acetonitrile (10 vol.) was added potassium carbonate (3.0 eq.) and bromide intermediate (1.2 eq.). The reaction was heated to 80 °C for 16 hr. Afterwards, the reaction mixture was diluted with water and then extracted with CH2Cl2(2 x 30 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ether.

[0969] Method S: To an ice-cold solution of Cbz protected intermediate (1.0 eq.) in hexafluoroisopropanol (10 vol.) was added methanesulfonic acid (3.0 eq.). After 16 hr, the reaction mixture was diluted with satd. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 30 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude amine.

[0970] Method T: To a solution of the N-Boc intermediate (1.0 eq.) in CH2Cl2(10 Vol.) was added (4.0 M HC1 in 1,4-dioxane (5 Vol.) at 0 °C. After 5 h, The reaction mixture was concentrated under reduced pressure to give the amine.

[0971] Method U: To a solution of the O-TBDMS intermediate (1.0 eq.) in THF (15 Vol.) was added TBAF (IM) (2.0 eq.) at 0 °C. After 3 hr at room temperature, the reaction mixture was diluted with chilled ice water and extracted with ethyl acetate (2 x 30 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give crude alcohol.

[0972] Method V: To a solution of amide (1.0 eq.) in THF (20 Vol.) was added the BH3.DMS (2.5 eq.) at 0 °C. After 20 min, the reaction was allowed to warm to room temperature. After 16 hr, the reaction mixture was diluted with ice water and then extracted with ethyl acetate (2 x 40 Vol.). The combined organic layers were washed with brine and water. The organic layer was dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give amine.

[0973] Method W: To an ice-cold solution of amide or amine (1.0 eq.) in DMF (20 Vol.) was added K2CO3(4.0 eq.). After 20 min, iodomethane (1.2 eq.) was slowly added. The reaction was allowed to warm slowly to room temperature. After 16 hr, the reaction mixture was diluted with ice water and then extracted with ethyl acetate (2 x 50 Vol.). The combined organics were washed with brine and then dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude methyl amide or amine.

[0974] Method X: To an ice-cold solution of alcohol (1.0 eq) in DMF (20 Vol.) and triethylamine (1.0 eq.) was added TBDMSC1 (1.0 eq.) in DMF (5 Vol.) slowly. The reaction was allowed to slowly warm to room temperature. After 16 hr, the reaction mixture was diluted with sat. sodium bicarbonate solution and then extracted with ethyl acetate (2 x 50 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the silyl ether.

[0975] Method Y: To an ice-cold solution of alcohol intermediate (1.0 eq.) in CH2Cl2(10 vol.) was added triethylamine (2.0 eq.). After 15 min, mesyl chloride (1.2 eq.) was added. After 1 hr, the reaction mixture was diluted with satd. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 30 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude mesylate.

[0976] Method Z: To an ice-cold solution of alcohol intermediate (1.0 eq.) in CH2Cl2(10 vol.) was added pyridinium dichromate (1.0 eq.). After 4 hr, the reaction mixture was filtered through celite using CH2Cl2(2 x 30 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ketone.

[0977] Method AA: To a solution of the aldehyde intermediate (1.0 eq.) in toluene (20 Vol.) was added molecular sieves (0.5). DBU (1 eq.) in toluene (1 Vol.) was added. The reaction was heated to 50 °C and then to 90 °C. After 18 hr, the reaction mixture was concentrated to give the crude product.

[0978] Method AB: To an ice-cold solution of acid (1.3 eq.) in DCM (15 vol.) was added DMAP (0.25 eq.) and diisopropylmethanediimine (1.2 eq.). After 20 min, salicylaldehyde (1.0 eq.) was added as a solution in DCM (2 Vol.) at room temperature. After 18 hr, the reaction mixture was diluted with chilled ice water and then extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the crude ester.

[0979] Method AC: To a solution of lactone (1.0 eq.) in AcOH (10 Vol.) was added methylamine hydrochloride (3.0 eq.). The reaction was heated to 100 °C. After 18 hr, the reaction mixture was concentrated under reduced pressure to give the crude methyl lactam.

[0980] Method AD: To an argon deoxygenated solution of bromo ester (1.0 eq.) and dry 4 Ang. molecular sieves in 1,4-dioxane (15 Vol.) was added XanthphosPdG3 (O. leq.), tertbutyl (4-oxobutyl)carbamate (1.5 eq.) and Cs2CO3(2.0 eq.). The mixture was further sparged with argon for 5 min then heated to 110 °C. After 18 hr, the reaction mixture was filtered and concentrated under reduced pressure to give the crude product.

[0981] Method AE: To a -78 °C solution of DMSO (3.0 eq.) in CH2Cl2(20 Vol.) was added oxalyl chloride (1.3 eq.) in CH2Cl2(10 Vol.) slowly. After 30 min, a solution of tert-butyl (4- hydroxybutyl)carbamate (1.0 eq.) in CH2Cl2(10 Vol.) was added. After 45 min, triethylamine (5.0 eq.) was added. The reaction was allowed to warm to 0 °C. Upon completion, the reaction mixture was concentrated to half volume, diluted with water, and then extracted with MTBE (2 x 150 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the aldehyde.

[0982] Method AF: To a solution of lactone (1.0 eq.) in AcOH (10 Vol) was added phenylmethanamine (2.0 eq.). The reaction was heated to 100 °C. After 18 hr, the reaction mixture was concentrated under reduced pressure. The residue was treated with sat. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 30 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amide.

[0983] Method AG: To a solution of amine hydrochloride (1.0 eq.) in CH2Cl2(10 Vol.) was added triethylamine (3.0 eq.) and (Boc)2O (1.2 eq.). After 18 hr, the reaction mixture was diluted with ice water and then extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried (Na2SO4), filtered and concentrated under reduced pressure to give the crude N- Boc product.

[0984] Method AH: To a solution of ketone (1.0 eq.) in ethanol (10 Vol.) was added triethylamine (5.0 eq.), O-methylhydroxylamine hydrochloride (4.0 eq.) at 0 °C. The reaction was allowed to warm to room temperature. After 2 hr, the reaction mixture was concentrated to dryness. The residue was treated with water and then extracted with DCM (2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the oxime.

[0985] Method Al: To a solution of amide (1.0 eq.) in DMF (10 Vol.) was added potassium carbonate (3.0 eq.). After 1 hr, the halide (1.5 eq.) was added. After 16 hr, the reaction mixture was treated with water and then extracted with EtOAc (2 x 20 Vol). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the N-alkylated product.

[0986] Method AJ: To a solution of KOH (1.0 eq.) in water (10 Vol.) was added thione (1.0 eq.). The suspension was stirred until full dissolution. Then a solution of KMnO4(2.0 eq.) in (30 Vol.) water was added slowly. The reaction was judged complete when the color of a drop of solution on filter paper was pale pink, indicating a small excess of permanganate. The precipitated MnO2was removed by filtration. The filtrate was acidified with cone. HC1 to pH 1 and boiled until the emission of SO2had ceased. The solution was cooled and the resulting precipitate was collected by filtration. The solid was rinsed with water and then dried to give the product thiazolidinone. Method AK: To a solution of alcohol (1.0 eq.) in THF (10 Vol.) was added triphenylphosphine (1.5 eq.) and CBr4(1.5 eq.) at 0 °C. The reaction was allowed to warm to room temperature. After 1 hr, the reaction mixture was filtered through celite using THF, concentrated under reduced pressure to give the bromide.

[0987] Method AL: To an ice-cold solution of amine (1.0 eq.) in CH2Cl2(10 Vol) was added acid chloride (1.2 eq.). After 2 hr, the reaction was treated with water and then extracted with CH2Cl2(2 x 30 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the carbamate.

[0988] Method AM: To an ice-cold solution of amine (1.0 eq.) in CH2Cl2(10 Vol) was added aldehyde (5.0 eq.). After 2 hr, sodium triacetoxyhydroborate (3.0 eq) was added. After 16 hr, the reaction mixture was diluted with sat. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 30 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amine.

[0989] Method AN: To an ice-cold solution of sulfmamide (1.0 eq.) in CH2Cl2(10 Vol) was added m-CPBA (1.1 eq.). After 2 hr, was added sodium triacetoxyborohydride (3.0 eq). After 16 hr, the reaction mixture was diluted with sat. sodium bicarbonate solution and then extracted with CH2Cl2(2 x 30 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the sulfonamide.

[0990] Method AO: To a solution of amine (1.0 eq.) in toluene (10 Vol) was added the aryl halide (1.2 eq.) BINAP (0.1 eq.), Pd2(dba)3(5 mol%) and KO / Bu (1.2 eq.). The mixture was sparged with argon for 5-10 min and then heated to 150 °C in a microwave. After 1 hr, the reaction mixture was filtered through a celite pad using CH2Cl2. The filtrate was concentrated to give crude N- aryl product.

[0991] Method AP: To a solution of azide (1.0 eq.) in MeOH (10 Vol.) was added nickel chloride hexahydrate (2.0 eq.) at 0 °C. The reaction was allowed to warm to room temperature. After 4 hr, the reaction mixture was concentrated under reduced pressure to give the amine.

[0992] Method AQ: To a solution of ketone (1.0 eq.) in THF (20 Vol.) was added lithium tri- / c / 7-butoxyaluminum hydride (2.0 eq.) at -78 °C. After 2 hr., the reaction mixture was diluted with a satd. aqueous solution of sodium potassium tartrate at -78 °C slowly. After 15 min, the reaction was allowed to warm to 25°C. The reaction mixture was diluted with water extracted with EtOAc (2 x 40 Vol.). The organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the alcohol.

[0993] Method AR: To a solution of alcohol (1.0 eq.) in THF (10 Vol.) was added triphenylphosphine (2.0 eq.) and diisopropyl azodi carb oxy late (2.0 eq.) at 0 °C. After 10 min, diphenylphosphoryl azide (1.5 eq.) was added and the reaction was allowed to slowly warm to 25 °C. After 18 hr, the reaction mixture was diluted with water (20 Vol.) and extracted with EtOAc (2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the azide.

[0994] Method AS: To a solution of oxime (1.0 eq.) in acetonitrile (10 Vol.) was added cyanuric chloride (0.2 eq.) at 25°C. The reaction was heated to 80 °C. After 3h, the reaction mixture was diluted with water and then extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the lactam.

[0995] Method AT: To a solution of ketoaldehyde (1.0 eq.) in EtOH (Vol.) was added hydrazine monohydrate or hydroxyl amine hydrochloride (1.0 eq.) at 25 °C. The reaction was heated to 110 °C. After 6 hr., the reaction mixture was poured into cold water and then extracted with CH2Cl2(2 x 30 Vol.). The combined organics were washed with 2 N HC1, dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the pyrazole.

[0996] Method AU: To a solution of ketone (1.0 eq.) in pyridine (10 Vol.) was added ethyl formate (7.0 eq.) and sodium methoxide (2.0 eq.) at 25 °C. After 16 hr, the reaction mixture was acidified with cold acetic acid and then further diluted with water. The mixture was extracted with CH2Cl2(2 x 20 Vol.). The combined organics were washed with 2 N HC1, dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give crude ketoaldehyde.

[0997] Method AV: To a solution of ketoaldehyde (1.0 eq.) in pyridine (10 Vol.) was added hydroxylamine hydrochloride (4.0 eq.) at 25 °C. The reaction was then heated to 110°C. After 6 hr, the reaction mixture was diluted with ice water and acidified with 2 N HC1. The resulting mixture was extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered, and concentrated under reduced pressure to give the isoxazole.

[0998] Method AW: To a solution of ketone (1.0 eq.) in THF (10 Vol.) was added sodium borohydride (3.0 eq.) at 0 °C. After 1 hr, the reaction was allowed to warm to room temperature. After 16 hr, the reaction mixture was diluted with ice water and then extracted with EtOAc (2 x 50 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the alcohol.

[0999] Method AX: To a solution of amine-I (1.0 eq.) in DCM (10 Vol.) was added 1,1'- carbonyldiimidazole (1.2 eq.) and triethylamine (3.0 eq.) at 0 °C. The reaction was allowed to warm to room temperature. After 15 min, the reaction was cooled to 0 °C and then amine-II (1.0 eq.) was added. Upon completion, the reaction mixture was diluted with water and extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the asymmetric urea.

[1000] Method AY: To a solution of acetal (1.0 eq.) in THF (10 Vol.) and water (10 Vol.) was added p-TsOH (0.6 eq.). After 8 hr, the reaction mixture was diluted with brine and then extracted with ethyl acetate (2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the ketone.

[1001] Method AZ: To a solution of aryl bromide (1.0 eq.) in 1,4-dioxane (20 Vol.) was added copper(I) iodide (0.4 eq.) and tert-butyl prop-2-yn-1-ylcarbamate (1.5 eq.). After sparging with argon for 10 min., triethylamine (4.0 eq.), di-mu-chlorobis[(l,2,3-4)-1-phenyl- 2-propenyl]dipalladium(II) (0.2 eq.) and (9,9-dimethyl-9H -xanthene-4,5- diyl)bis(diphenylphosphane) (0.4 eq.) were added. The reaction was heated to 100 °C. After 18 hr, the reaction mixture was diluted with water and then extracted with EtOAc (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the alkyne.

[1002] Method BA: To a solution of alkyne (1.0 eq.) in EtOH (20 Vol.) was added Pd / C (50% wet) (20%), and triethylamine (1.0 eq.). After 4 hr, under hydrogen gas atmosphere, the reaction mixture was filtered through celite bed using ethyl acetate (50 mL). The filtrate was concentrated to obtain the alkane product.

[1003] Method BB: To a solution of ethyl propiolate (5.0 eq.) in THF (10 Vol.) was added lithium bis(trimethylsilyl)amide (1 M in THF) (3.0 eq.) slowly at -78 °C. The reaction was warmed to -20 °C. After 30 min, the reaction was cooled to -35 °C and then the ketone (1.0 eq.) in THF (5 Vol.) was added. The reaction was allowed to warm to -15 to -20 °C over 45 min. The reaction was treated with sat. ammonium chloride solution and then extracted with ethyl acetate (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate and then concentrated under reduced pressure to give the tertiary alcohol.

[1004] Method BC: To a solution of aryl bromide (1.0 eq.) in toluene (10 vol.) and water (3 vol.) was added tert-butyl (2-(trifluoro-14-boranyl)ethyl)carbamate, potassium salt (1.3 eq.), Cs2CO3(2 eq). After sparging with argon for 10 min, (1,1'-bis(diphenylphosphino)ferrocene)- dichloropalladium(II) (10 mol%) was added. The reaction was heated to 90 °C for 12 hr. Afterwards, the reaction mixture was diluted with water and then extracted with EtOAc (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the desired cross-coupled product.

[1005] Method BD: To an ice-cold solution of amine (1.0 eq.) in DMF (10 vol.) was added HATU (1.4 eq.), DIPEA (5.0 eq.). After 8 hr, the reaction mixture was diluted with water extracted with EtOAc (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amide.

[1006] Method BE: To an ice-cold solution of oxime (1.0 eq.) in THF (10 vol.) was added thionyl chloride (10 eq.). After 2 hr, the reaction was treated with 2 N NaOH solution and then extracted with EtOAc (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the lactam.

[1007] Method BE: To a solution of ketone (1.0 eq.) in pyridine (15 Vol.) was added hydroxyl amine derivative (1.0 eq.). The reaction was then heated to 64°C. After 6 hr, the reaction was treated with 2 N HC1 solution under cooling and then extracted with CH2Cl2(2 x 20 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the oxime.

[1008] Method BG: To a solution of azide (1.0 eq.) in EtOAc (10 Vol.) and water (10 Vol.) was added Zn (5.0 eq.) and ammonium chloride (5.0 eq.). After 16 hr, the reaction mixture was filtered. The filtrate was diluted with water and then extracted with ethyl acetate (2 x 10 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amine.

[1009] Method BH: To a solution of phenol derivative (1.0 eq.) in toluene (10. Vol.) was added methyl N-Cbz derivative (0.6 eq.), and methanesulfonic acid (0.5 eq.) at 0 °C. The reaction was allowed to warm to room temperature. After 12h, the reaction was diluted with CH2Cl2(10 Vol.). The resulting mixture was washed with water (20 Vol.). The organic layer was dried over anhydrous sodium sulphate and concentrated under reduced pressure to give the lactone.

[1010] Method BJ: To a solution of aryl bromide (1.0 eq.) in DMF (10 Vol.) was added copper(I) iodide (0.1 eq.), picolinic acid (0.2 eq.) and tert-butyl piperidin-3 -ylcarbamate (1.2 eq.). The reaction mixture was sparged with argon for 10 min. Potassium carbonate (2.0 eq.) was added and the reaction mixture heated to 160 °C in a microwave. After 2.5 hr, the reaction mixture was concentrated under reduced pressure to give N-arylated product.

[1011] Method BK. To a solution of diamide (1.0 eq.) in toluene (10 Vol.) was added the Burgess reagent [methyl N-(triethylammoniumsulfonyl)carbamate] (5.0 eq.). The mixture was heated to 125 °C using a microwave reactor. After 2 hr, the oxadiazole was isloated as a solid.

[1012] Method BL. To a solution of PMB protected amine (1.0 eq.) in DCE (10 Vol.) was added 1-chloroethyl chloroformate (5.0 eq.). The reaction was heated to 90 °C. After 16 hr, the mixture was diluted with methanol and then heated to reflux. After 30 min, reaction mixture was concentrated under reduced pressure to give the amine hydrochloride salt.

[1013] Method BM. To a solution of oxadiazole (1.0 eq.) in AcOH (10 Vol.) was added methyl amine acetic acid salt (40 eq.). The reaction was heated to 140 °C in a microwave reactor. After 8 hr, the reaction mixture was diluted with ice water and then extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the triazole.

[1014] Method BN. To a solution alcohol (1.0 eq.) in DCM (20 Vol.) was added pyridinium chlorochromate (7.0 eq.) portion-wise. After 16 hr, the reaction mixture was filtered through a celite bed using DCM (2 x 10 Vol.). The filtrate was concentrated under reduced pressure to give the ketone.

[1015] Method BO. To an epoxide (1.0 eq.) was added ammonia (50 Vol.). The reaction vessel was sealed. After 16 hr at rt, the reaction mixture was diluted with ice water and then extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the amino alcohol.

[1016] Method BP. To a solution of olefin (1.0 eq.) in dichloromethane (20 Vol.) was added m-CPBA (50% wet) (2.8 eq.) portion wise at room temperature. After 16 hr, the reaction mixture was diluted with ice water and then extracted with CH2Cl2(2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the epoxide.

[1017] Method BQ. To a solution of methyltriphenylphosphonium bromide (1.3 eq.) in THF (20 Vol.) was added n-butyllithium (2.5 M in n-hexane) (1.2 eq.) at -78 °C, After 10 min, allowed to 25 °C, after 30 min allowed to -78 °C was added aldehyde (1.0 eq.) in THF (10 Vol.) slowly and then stirred at 25 °C by slowly allowed from cooling, After 2 hr. the reaction mixture was diluted with ice water and then extracted with ethyl acetate (2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the olefin.

[1018] Method BR. To a solution of ester (1.0 eq.) in EtOH (15 mL) was added hydrazine hydrate (5.0 eq.). After 16 hr, the reaction mixture was concentrated under reduced pressure to give the hydrazide.

[1019] Method BS. To a solution of diketo (1.0 eq.) in toluene (10 Vol.) was added ammonium acetate (15 eq.). The reaction was heated to 140 °C. After 20 hr, reaction mixture was concentrated under reduced pressure. The residue was washed with chilled sat. sodium bicarbonate solution and then extracted with ethyl acetate (2 x 50 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the imidazole.

[1020] Method BT. A solution of sodium hydride (3.7 eq.) in DMSO (10 Vol.) was heated to 55 °C, After 90 min, the mixture was cooled to 0 °C and then a solution of trimethyl sulfonium iodide (2.25 eq.) in THF (10 Vol.) was added dropwise. After 15 min, tert-butyl 3 -formylpiperidine-1-carboxylate (1.0 eq.) was added. The reaction was allowed to warm to rt. After 1.5 h, the reaction mixture was treated with ice water and then extracted with MTBE (2 x 30 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the epoxide.

[1021] Method BU. To the aniline (1.0 eq.) was added AcOH (10 Vol.). The reaction was heated to 120 °C. After 18 hr, the reaction mixture was concentrated under reduced pressure to give the imidazole.

[1022] Method BV. To a solution of amine (1.0 eq.) in DCM (10 vol.) was added triethylamine (8.0 eq.), pyridine (2.0 eq.), and phenylboronic acid (1.2 eq). After sparging with argon for 10 min, copper (II) acetate (20 mol%) was added. The reaction was stirred at rt for 16 hr. The reaction mixture was diluted with water then extracted with EtOAc (2 x 40 Vol.). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give the A-aryl product.

[1023] Preparative HPLC Method A. Purification was performed using a Waters mass triggered auto-purification HPLC with a binary solvent system A and B using a gradient elution; Column: Gemini-NX lOum C18, 150 x 30 mm; Mobile phase A: CAN; Mobile phase B: 10 mM ammonium bicarbonate in water; Flow rate: 30 mL / min; Run time: 20 min.

[1024] Intermediate Preparation

[1025] Preparation of 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl) oxy) acetic acid

[1026] Step-1: To an ice-cold solution of NaH (60%) (1.14 g, 47.8 mmol) in THF (20 mL) was added (55, 87?, 95, 105, 135, 145, 175)- 10, 13 - dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17-ol (4.00 g, 11.9 mmol) slowly followed by tetra-n-butylammonium iodide (2.20 g, 5.98 mmol) and then 3 -bromoprop- 1-ene (4.34 g, 35.9 mmol). After 10 min, the reaction was heated to reflux. After 24 hr, the reaction mixture was cooled to room temperature, treated with ice water and then extracted with ethyl acetate (2 x 50 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure. Purification by flash chromatography (silica gel n-hexane to 20% ethyl acetate / n-hexane) gave (5S,8R,, 95, 105, 135, 145, 175)- 17-(allyloxy)- 10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolane] (2.20 g, 49%) as an off-white solid.1H NMR (400 M Hz, CDCl3): 5.91-5.85 (m, 1H), 5.28-5.22 (m, 1H), 5.15-5.11 (m, 1H), 4.00-3.98 (m, 2H), 3.94-3.92 (m, 4H), 3.35 (t, J= 8.4 Hz, 1H), 2.00-1.86 (m, 2H), 1.68-1.65 (m, 4H), 1.57-1.34 (m, 7H), 1.31-1.09 (m, 6H), 0.98-0.85 (m, 2H), 0.82 (s, 3H), 0.77 (s, 3H), 0.75-0.67 (m, 1H).

[1027] Step-2: To a solution of (5S,8R,9S, 10S,13S, 14S, 17S)-17-(allyloxy)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolane] (1.0 g, 2.67 mmol) in acetone (20 mL) and water (5 mL) was added K2CO3(0.29 g, 2.13 mmol) followed by portionwise addition of KMnO4(1.47 g, 9.34 mmol.). After 12 hr, the reaction was acidified with 2 N HC1 and then extracted with ethyl acetate (2 x 50 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure. Purification by flash chromatography (silica gel n-hexane to 50% ethyl acetate / n- hexane) gave 2-(((55,85,95,105,135,145,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)acetic acid (10% yield) as an off-white solid.1H NMR (400 MHz, CDCl3): 4.11 (d, J = 6.0 Hz, 2H), 3.93 (d, J= 1.2 Hz, 4H), 3.44 (t, J= 8.0 Hz, 1H), 2.05-2.01 (m, 1H), 1.90-1.85 (m, 1H), 1.69-1.51 (m, 7H), 1.44-1.35 (m, 4H), 1.34-1.13 (m, 6H), 1.00-0.86 (m, 3H), 0.82 (s, 3H), 0.79 (s, 3H), 0.76-0.68 (m, 1H).

[1028] Preparation of tert-butyl 2-(((5S,8R,9S,10S,13S,14S,l 7S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-l 7- yl) oxy) acetate

[1029] To an ice-cold solution of (5S,8R,95,105,135,145,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17-ol (5.0 g, 14.95 mmol.) in toluene (100 mL) was added tert-butyl bromoacetate (6.64 mL, 44.8 mmol)) and tetrabutylammonium hydrogen sulfate (1.52 g, 4.48 mmol) followed by slow addition of NaOH (50% in water) (17.9 g, 448 mmol). The rapidly stirred mixture was allowed to warm to rt. After 12 hr, the reaction mixture was treated with ice water and then extracted with ethyl acetate (2 x 200 mL), the combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure, Purification by flash chromatography (silica gel n-hexane to 20% ethyl acetate / n-hexane) gave tert-butyl 2- (((55, 85,95, 105, 135, 145, 175)- 10, 13 - dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)acetate (2.1 g, 31% yield) as an off-white solid.1H-NMR (400 MHz, CDCl3): 3.97 (d, J= 1.2 Hz, 2H), 3.93 (d, J= 1.2 Hz, 4H), 3.38 (t, J= 8.8 Hz, 1H), 2.03-1.97 (m, 1H), 1.94- 1.89 (m, 1H), 1.73 (s, 2H), 1.68-1.54 (m, 6H), 1.47 (s, 9H), 1.44-1.34 (m, 3H), 1.32-1.11 (m, 5H), 0.98-0.85 (m, 2H), 0.81 (s, 3H), 0.79 (s, 3H), 0.75-0.66 (m, 1H).

[1030] Example 1: Preparation of 2-(((5S,8R, 9S, 105, 135, 145, 175) -10,13-dimethyI-3- oxohexadecahydro-1H -cydopenta[n]phenanthren-17-yI)oxy)-A’-((ll-oxo-2,3,6,7- tetrahydro- 1H,5H,11H -pyrano[2,3-f]pyrido[3, 2, 1-y]quinoIin-9-yl)methyI)aeetamide

[1031] (Compound 171) 1H-NMR (400 MHz, CDCl3): δ 7.00 (s, 1H), 6.88 (t, J= 6.0 Hz, 1H), 4.05 (d, J= 4.4 Hz, 2H), 3.39 (t, J= 8.4 Hz, 1H), 3.26 (dd, J= 7.2, 11.6 Hz, 4H), 2.89 (t, J= 6.4 Hz, 2H), 2.76 (t, J= 6.4 Hz, 2H), 2.42-2.23 (m, 3H), 2.11-1.96 (m, 7H), 1.88-1.83 (m, 1H), 1.72-1.68 (m, 1H), 1.46-1.26 (m, 9H), 1.20-1.10 (m, 1H), 1.02 (s, 3H, CH3), 0.99-0.83 (m, 3H), 0.79 (s, 3H, CH3), 0.76-0.69 (m, 1H). Key Resonances: 1.02 (s, 3H, CH3), 0.79 (s, 3H, CH3).

[1032] Step-1: Prepared by Method F. Purification by flash chromatography (silica gel, n-hexane to 30% EtOAc / n-hexane) gave methyl 4-(((benzyloxy)carbonyl)amino)-3-oxobutanoate (55% yield). The material was taken directly on to the next step.

[1033] Step-2: Prepared by Method G. Purification by flash chromatography (silica gel, n-hexane to 30% EtOAc / n-hexane) gave benzyl ((1 l-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- / |pyrido[3,2,l-ij]quinolin-9-yl)methyl)carbamate (41%) as yellow solid. ESI (m z ) [C24H24N2O4+H]+405. Step-3: Prepared by Method H. Obtained crude 9-(aminomethyl)-2,3,6,7-tetrahydro--1H,5H,11H-pyrano[2, 3-f]pyrido[3, 2, l-zj]quinolin-l 1-one (90 % yield) as yellow solid. (ESI (m / z) [C16H18N2O2+H]+ 271.

[1034] Step-4: Prepared by Method C. Purification by flash chromatography (silica gel, n-hexane to 70% EtOAc / n-hexane) gave 2-(((5S',10S',13S',17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)-N -((11 -oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,l-zj]quinolin-9-yl)methyl)acetamide (20 % yield) as light yellow solid. ESI (m / z) [C37H48N2O5+H]+601.

[1035] Example 2: Preparation of N-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10.13-dimethyl-3- oxohexadecahydro-lH-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-( 11-oxo-2,3,6,7- tetrahydro-1H,5H,11H-pyrano |2.3-f]pyrido [3.2.1 -ij] quinolin-9-yl)acet amide (Compound 172) 1H-NMR (400 MHz, CDCl3): δ 7.02 (s, 1H), 3.64-3.55 (m, 2H), 3.43-3.32 (m, 4H), 3.28-

[1036] 3.24 (m, 4H), 3.11-3.07 (m, 1H), 2.89 (t, J = 6.0 Hz, 2H), 2.76 (t, J = 6.4 Hz, 2H), 2.43-2.23 (m, 3H), 2.11-1.93 (m, 7H), 1.82-1.75 (m, 1H), 1.68-1.65 (m, 2H), 1.57-1.47 (m, 8H), 1.42- 1.26 (m, 7H), 1.21-1.11 (m, 2H), 1.06-0.96 (m, 5H), 0.90-0.79 (m, 2H), 0.71-0.64 (m, 1H), 0.55 (s, 3H, CH3). Key Resonances: 0.55 (s, 3H, CH3).

[1037] Step-1: Prepared by Method J. Purification by flash chromatography (silica gel, hexanes to 60% EtOAc / hexanes) gave (55, 105, 135,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17-ol (87 % yield) as an off-white solid. The material was taken directly on to the next step.

[1038] Step-2: Prepared by Method M. Purification by flash chromatography (silica gel, hexanes to 70% EtOAc / hexanes) gave ethyl 2-(((55,105,135,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)acetate (31% yield) as an off-white solid. The material was taken directly on to the next step.

[1039] Step-3: Prepared by Method L. Purification by flash chromatography (silica gel, hexanes to 70% EtO Ac / hexanes)2-(((55, 105, 135, 175)- 10, 13 - imethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)acetamide (81 % yield) as off-white solid. The material was taken directly on to the next step.

[1040] Step-4: Prepared by Method K. Obtained crude 2-(((55,105,135,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethan-l -amine (99%) as a gum. The material was taken directly on to the next step.

[1041] Step-5: Prepared by Method O. Obtained crude methyl 2-(11-oxo-2,3,6,7-tetrahydro--1H,5H,11H-pyrano[2,3-ij]pyrido[3, 2, l-z / ]quinolin-9-yl)acetate (90%) as a yellow gum. ESI (m z) [CI8HI9NO4+H]+314. The material was taken directly on to the next step. Step-6: Prepared by Method B. The crude was washed with n-hexane to give 2-(11-oxo- 2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)acetic acid. ESI (m / z) [CI7HI7NO4+H]+300. Step-7: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to

[1042] 70% EtOAc / hexanes) gave 2-(((55, 105, 135, 175)-10, 13 dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17-yl)oxy)-A-

[1043] (2-(11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,l-z / ]quinolin-9- yl)ethyl)acetamide (82% yield) as a yellow gum. ESI (m z) [C40H54N2O6+H]+659.

[1044] Step-8: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 65% EtOAc / hexanes) gave A-(2-(((55',105',135',175)-10,13-dimethyl-3-oxohexadecahydro- 17 / -cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-2-(11 -oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)acetamide (49% yield) as a light yellow solid. ESI (m / z) [C38H50N2O5+H]+ 615.

[1045] Example 3: Preparation of \-(2-(((5.S.8 / ?.9.S.10.S.13.S.14.S.17.S)-l().13-diinethyl-3- oxohexadecahydro-lH-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-7V-methyl-2-(ll-oxo- 2.3.6.7-tetrahydro-l / / .5 / / .l lH-pyrano[2,3- / ]pyrido[3,2,l-i / ]quinolin-9-yl)acetamide (Compound 173) 1H-NMR (400 MHz, CDCl3): δ 7.00 (d, J= 18.0 Hz, 1H), 3.88 (s, 1H), 3.72 (s, 1H), 3.59- 3.54 (m, 3H), 3.43 (d, J= 4.0 Hz, 1H), 3.31-3.23 (m, 5H), 3.11 (s, 1H), 2.99 (s, 2H), 2.89 (t, J = 6.4 Hz, 2H), 2.76 (d, J= 4.0 Hz, 2H), 2.43-2.20 (m, 3H), 2.10-1.95 (m, 8H), 1.89-1.63 (m, 3H), 1.50-1.08 (m, 9H), 1.01 (d, J= 5.6 Hz, 3H), 0.98-0.83 (m, 3H), 0.78-0.72 (m, 4H).

[1046] Step-1: Prepared by Method J. Purification by flash chromatography (silica gel, hexanes to 60% EtOAc / hexanes) gave ethyl 2-(((55,105,135,175)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)acetate (13% yield) as an off-white solid. The material was directly taken on to the next step.

[1047] Step-2: Prepared by Method L. The residue was washed with n-hexane to give 2- (((55, 105, 135, 175)- 10,13 -di methyl hexadecahydrospi rofcycl openta[a]phenanthrene-3 ,2'- [l,3]dioxolan]-17-yl)oxy)-A-methylacetamide (71% yield) as an off-white solid. ESI (m z )

[1048] [C24H39NO4+H]+406.

[1049] Step-3: Prepared by Method K. Obtained crude 2-(((55, 105, 135, 175)-10, 13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17-yl)oxy)-N - methylethan-1 -amine (99%). The material was directly taken on to the next step.

[1050] Step-4: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 70% EtO Ac / hexanes)N-(2-(((5 S, 10S, 13 S, 17S)- 10, 13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-A-methyl-2-(11-oxo-2, 3,6, 7-tetrahydro- 177, 577,1177-pyrano[2,37 / ]pyrido[3, 2,1- z / ]quinolin-9-yl)acetamide (84 % yield) as a gum. ESI (m / z) [C4IH56N2O6+H]+674.

[1051] Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 75% EtOAc / hexanes) gave A-(2-(((55',105',135',175)-10,13-dimethyl-3-oxohexadecahydro- 1H -cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-N -methyl-2-(11 -oxo-2, 3,6, 7-tetrahydro--1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)acetamide (15% yield) as a light yellow solid. ESI (m / z) [C39H52N2O5+H]+629.

[1052] Example 4: Preparation of 1-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-lH-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(11-oxo-2,3,6,7- tetrahydro-1H,5H,11H-pyrano[ 2,3- / ]pyrido [3, 2,1 -ij] quinolin-9-yl)ethyl)urea (Compound 174)

[1053] 1H-NMR (400 MHz, DMSO- d6): δ 7.22 (s, 1H), 3.41-3.35 (m, 1H), 3.27-3.21 (m, 7H), 3.11- 3.07 (m, 2H), 2.77-2.70 (m, 6H), 2.45-2.25 (m, 3H), 2.11-2.05 (m, 1H), 1.92-1.86 (m, 7H), 1.83-1.75 (m, 1H), 1.62-1.58 (m, 1H), 1.50-1.43 (m, 3H), 1.39-1.31 (m, 3H), 1.27-1.19 (m, 4H), 1.19-1.06 (m, 3H), 0.96 (s, 3H, CH3), 0.90-0.79 (m, 2H), 0.69 (s, 4H). Key Resonances: 0.96 (s, 3H, CH3).

[1054] Step-1: Prepared by Method F. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave methyl 5-(((benzyloxy)carbonyl)amino)-3-oxopentanoate. ESI

[1055] (m / z) [CI4H17NO5+H]+280.

[1056] Step-2: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave benzyl (2-(11 -oxo-2,3,6,7-tetrahydro1H,5H,11H pyrano[2,3- / |pyrido[3,2,1-ij]quinolin-9-yl)ethyl)carbamate (49% yield) as a yellow solid. ESI (m / z) [C25H26N2O4+H]+419.

[1057] Step-3: Prepared by Method H. Residue was washed with n-hexane to give 9-(2- aminoethyl)-2,3,6,7-tetrahydro1H,5H,11H pyrano[2,3-ij]pyrido[3,2, 1-z / ] quinolin- 11-one (60% yield) as a yellow solid. ESI (m / z) [CI7H20N2O2+H]+285.

[1058] Step-4: Prepared by Method N. Purification by flash chromatography (silica gel, hexanes to 70% EtOAc / hexanes) gave 1 -(2-(((55, 1 OS, 135, 175)- 10, 13 - dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-3-(2-(11-oxo-2, 3,6, 7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3, 2,1- zj]quinolin-9-yl)ethyl)urea (20% yield). ESI (zzz / z) [C41H57N3O6+H]+688.

[1059] Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 80% EtOAc / hexanes) gave 1-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(11-oxo-2,3,6,7- tetrahydro1H,5H,11H pyrano[2,3-ij]pyrido[3,2,l-zj]quinolin-9-yl)ethyl)urea (35% yield) as a yellow solid. ESI (m / z)

[1060] Example 5: Preparation of 3-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-1-methyl-1-((11-oxo- 2.3.6.7-tetrahydro-1H,5h,11H-pyrano[2,3- / ]pyrido[3,2,l-i / ]quinolin-9-yl)methyl)urea (Compound 175) 1H-NMR 400 MHz , DMSO-d6): δ 7.16 (s, 1H), 3.43-3.36 (m, 2H), 3.28-3.22 (m, 5H), 3.18- 3.07 (m, 2H), 3.14-3.17 (H, 3H) 2.82 (s, 3H), 2.74-2.69 (m, 4H), 2.33-2.24 (m, 1H), 2.10- 2.07 (m, 2H), 1.95-1.83 (m, 7H), 1.80-1.72 (m, 1H), 1.62-1.58 (m, 1H), 1.51-1.40 (m, 3H), 1.40-1.33 (m, 2H), 1.30-1.21 (m, 5H), 1.18-1.05 (m, 2H), 0.96 (s, 3H), 0.92-0.81 (m, 2H), 0.71-0.66 (m, 4H). Key Resonances: 0.96 (s, 3H, CH3). Step-1: Prepared by Method F. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) methyl 4-(((benzyloxy)carbonyl)(methyl)amino)-3-oxobutanoate (62% yield) as a colourless liquid. The material was directly taken on to the next step. Step-2: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) benzyl methyl((11-oxo-2, 3, 6, 7-tetrahydro-1H,5H,11H-pyrano[2, 3- y]pyrido[3,2,1-ij]quinolin-9-yl)methyl)carbamate (52% yield) as a yellow solid. ESI (m / z) [C25H26N2O4+H]+ 419. Step-3: Prepared by Method H. The residue was washed with n-hexane to give 9- ((methylamino)methyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin- 11-one (58% yield) as a yellow solid. ESI (m / z) [Ci7H2oN202+H]+285. Step-4: Prepared by Method N. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave 3-(2-(((105, 135, 175)- 10, 13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-1-methyl-1-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1- z / ]quinolin-9-yl)methyl)urea (54% yield) as a yellow solid.

[1061] Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 80% EtOAc / hexanes) gave 3 -(2-((( 10S, 13S, 17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-1-methyl-1-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2, 3- / |pyrido[3,2,1-ij]quinolin-9-yl)methyl)urea (25% yield) as a yellow solid. ESI (m / z) [C39H53N3O5+H]+644.

[1062] Example 6: Preparation of 1-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-lH-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(( 11-oxo-2,3,6,7- tetrahydro-1H,5H,11H-pyrano| 2,3-f]pyrido [3.2.1 -ij] qiiinolin-9-yl)inethyl)urea (Compound 176) 1H-NMR (400 MHz, DMSO-d6): δ 7.18 (s, 1H), 6.53 (t, J = 6.0 Hz, 1H), 3.44-3.39 (m, 1H), 3.28-3.21 (m, 5H), 3.14 (dd, J = 6.0, 11.4 Hz, 2H), 2.72 (t, J = 6.4 Hz, 4H), 2.42-2.37 (m, 2H), 2.33-2.26 (m, 2H), 2.10-2.06 (m, 1H), 1.97-1.86 (m, 7H), 1.82-1.79 (m, 1H), 1.63-1.59 (m, 1H), 1.51-1.46 (m, 3H), 1.39-1.35 (m, 2H), 1.34-1.31 (m, 1H), 1.28-1.08 (m, 7H), 0.97- 0.94 (m, 4H), 0.92-0.82 (m, 2H), 0.71 (s, 4H).

[1063] Step-1: Prepared by Method F. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave methyl 4-(((benzyloxy)carbonyl)amino)-3-oxobutanoate (75% yield) as a yellow liquid. The material was taken directly on to the next step.

[1064] Step-2: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to

[1065] 30% EtOAc / hexanes) gave benzyl ((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H -pyrano[2,3- f|pyrido[3,2,1-z / ]quinolin-9-yl)methyl)carbamate (41% yield) as yellow solid. ESI (m z) [C24H24N2O4+H]+405.

[1066] Step-3: Prepared by Method H. The residue was washed with n-hexane to give to get 9- (aminomethyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-11-one (75% yield) as a yellow solid. ESI (m / z) [C16H18N2O2+H]+271.

[1067] Step-4: Prepared by Method N. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave 1 -(2-(((10S, 13S,17S)- 10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[1,3]dioxolan]-17- yl)oxy)ethyl)-3-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1- z / ]quinolin-9-yl)methyl)urea (46% yield) as a yellow solid. ESI (m / z) [C40H55N3O6+H] 675. Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 80% EtOAc / hexanes) gave 1 -(2-((( 105, 135, 175)- 10,13 -dimethyl-3 -oxohexadecahydro- 1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-ij]pyrido[3,2,l-zj]quinolin-9-yl)methyl)urea (8% yield) as a yellow solid. ESI (m / z) [C38H51N3O5+H]+630.

[1068] Example 7: Preparation of 1-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-1-methyl-3-(2-(ll- oxo-2.3.6.7-tetrahydro-1H,5H,11H-pyrano [2.3-f]pyrido[3.2.1-17]quinolin-9-yl)ethyl)urea (Compound 177) 1H NMR 400 MHz, CDCl3): δ 7.18 (s, 1H), 3.51-3.55 (m, 2H), 3.51-3.43 (m, 2H), 3.40- 3.23 (m, 8H), 2.92 (s, 3H), 2.90-2.85 (m, 5H), 2.79 (t, J = 6.4 Hz, 2H), 2.43-2.23 (m, 4H),

[1069] 2.10 (s, 1H), 2.07-1.91 (m, 7H), 1.78-1.65 (m, 3H), 1.53-1.47 (m, 2H), 1.41-1.28 (m, 6H), 1.24-1.09 (m, 3H), 1.01 (s, 3H), 0.98-0.83 (m, 3H), 0.75-0.68 (m, 1H), 0.66 (s, 3H). Key Resonances: 1.01 (s, 3H, CH3), 0.66 (s, 3H, CH3).

[1070]

[1071] Step-1: Prepared by Method N. Purification by flash chromatography (silica gel, CH2Cl2to 6% CH3OH / CH2Cl2) gave 1-(2-(((10S, 13S,17S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[1,3]dioxolan]-17- yl)oxy)ethyl)-1-methyl-3-(2-(11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- y]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)urea (40% yield) as a yellow solid. ESI (m z ) [C42H59N3O6+H]+702. Step-2: Prepared by Method I. Purification by flash chromatography (silica gel, CH2Cl2to 6% CH3OH / CH2Cl2) gave 1-(2-(((10S,13S,17S -10,13-dimethyl-3-oxohexadecahydro-177- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-3-(2-111-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)urea (43% yield) as a yellow solid. ESI (m / z) [C40H55N3O5+H]+658.

[1072] Example 8: Preparation of 2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)- N-methyl-7V-(2-(11-oxo- 2.3.6.7-tetrahydro-1H,5H,11H-pyrano|2.3: / ]pyrido|3.2.1- / / |quinolin-9- yl)ethyl)acetamide (Compound 178)

[1073] 1H-NMR (400 MHz, CDCl3): δ 7.26 (s, 1H), 4.14-4.08 (m, 3H), 3.61-3.57 (m, 2H), 3.41-

[1074] 3.23 (m, 7H), 3.03 (s, 3H), 2.99 (s, 1H), 2.96-2.87 (m, 5H), 2.83-2.77 (m, 3H), 2.43-2.22 (m,

[1075] 4H), 2.07-1.88 (m, 8H), 1.72-1.67 (m, 2H), 1.34-1.26 (m, 6H), 1.01 (s, 3H, CH3), 0.99 (s, 2H), 0.81 (s, 3H, CH3). Key Resonances: 1.01 (s, 3H, CH3), 0.81 (s, 3H, CH3).

[1076] Step-1: Prepared by Method F. Purification by flash chromatography (silica gel, hexanes to

[1077] 30% EtOAc / hexanes) gave methyl 5-((tert-butoxycarbonyl)(methyl)amino)-3-oxopentanoate (67% yield) as a colourless liquid. The material was taken directly on to the next step.

[1078] Step-2: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave tert-butyl methyl(2-(11-oxo-2, 3,6, 7-tetrahydro-1H,5H,11H- pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)carbamate (19% yield) as a colourless liquid. ESI (m / z) [C23H30N2O4+H]+399. Step-3: Prepared by Method T. The residue was washed with n-hexane to give 9-(2- (methylamino)ethyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-11- one hydrochloride (95% yield) as a brown solid. ESI ( m / z) [C18H22N2O2C1H+H]+- HC1 299.

[1079] Step-4: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 40% EtOAc / hexanes) gave 2-(((5S,10S,13S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)- N-methyl-N -(2-(11-oxo-2,3,6,7-tetrahydro- -1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)acetamide (25% yield) as yellow solid. ESI (m / z) [C39H52N2O5+H]+629.

[1080] Example 9: Preparation of 1-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-1-methyl-3-(( 11-oxo- 2.3.6.7-tetrahydro-1H,5H,11H-pyrano[2,3- / ]pyrido[3,2,l-i / ]quinolin-9-yl)methyl)urea (Compound 179) 1H-NMR (400 MHz, CDCl3): δ 7.06 (s, 1H), 3.64 3.55 (m, 2H), 3.50-3.38 (m, 2H), 3.32 (t, J = 8.4 Hz, 1H), 3.25 (dd, J = 6.8 , 11.6 Hz, 4H), 2.97 (s, 3H), 2.89 (t, J= 6.4 Hz, 2H), 2.77 (t, J= 6.4 Hz, 2H), 2.42-2.22 (m, 3H), 2.10-2.04 (m, 1H), 2.02-1.94 (m, 5H), 1.80-1.65 (m, 2H), 1.55-1.48 (m, 3H), 1.38-1.24 (m, 7H), 1.22-1.10 (m, 2H), 0.99 (s, 3H), 0.96-0.80 (m, 2H), 0.73-0.67 (m, 1H), 0.66 (s, 3H). Key Resonances: 0.99 (s, 3H, CH3), 0.66 (s, 3H, CH3).

[1081] Step-1: Prepared by Method N. Purification by flash chromatography (silica gel, CH2Cl2to 5% CH3OH / CH2Cl2) gave 1-(2-(((105, 135,17S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[1,3]dioxolan]-17- yl)oxy)ethyl)-1-methyl-3-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3, 2,1- z / ]quinolin-9-yl)methyl)urea (24% yield) as a yellow solid. ESI (m / z) [

[1082] Step-2: Prepared by Method I. Purification by prep HPLC gave 1 -(2-(((l OS, 135, 175)- 10,13 -dimethyl-3 -oxohexadecahydro- 17 / -cyclopenta[a] phenanthren- 17 -yl)oxy)ethyl)- 1 - methyl-3-((11-oxo-2, 3, 6, 7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9- yl)methyl)urea (30% yield) as a yellow solid. ESI (m / z) [ ]

[1083] Example 10: Preparation of 3-(2-(((5S,8R ,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro- 1H-cyclopenta [a] phenanthren-17-yl)oxy)ethyl)-1-methyl-1-(2-(11- oxo-2, 3, 6, 7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)urea (Compound 180) 1H-NMR (400 MHz, CDCl3) : δ 7.17 (s, 1H), 3.59-3.48 (m, 4H), 3.43-3.38 (m, 2H), 3.34- 3.23 (m, 5H), 2.91-2.87 (m, 6H), 2.80 (t, J= 6.4 Hz, 2H), 2.43-2.26 (m, 3H), 2.03-1.96 (m, 6H), 1.87-1.83 (m, 1H), 1.71-1.61 (m, 6H), 1.34-1.13 (m, 8H), 1.01 (s, 3H, CH3), 0.98-0.82 (m, 4H), 0.76 (s, 3H, CH3). Key Resonances: 1.01 (s, 3H, CH3), 0.76 (s, 3H, CH3).

[1084] Step-1: Prepared by Method N. Purification by flash chromatography (silica gel, hexanes to 30% EtOAc / hexanes) gave 3-(2-(((5S,8R,9S, 10S,13S, 14S, 17S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-1 -methyl-1-(2-(11-oxo-2, 3,6, 7-tetrahydro-1H,5H,11H-pyrano[2, 3- y]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)urea (45% yield) as a yellow solid. ESI (m z ) [C42H59N3O6+H]+ 702.

[1085] Step-2: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 80% EtOAc / hexanes) gave 3-(2-(((5S,8R,9S, 10S,13S, 14S, 17S)-10,13-dimethyl-3- oxohexadecahydro- 17 / -cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-1-(2-(11-oxo- 2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)ethyl)urea (28% yield) as a yellow solid. ESI (m / z) [C4oH55N305+H] 658.

[1086] Example 11: Preparation of 2-(((5S,8R,9S,10S,13S,14S,17S )-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta [a] phenanthren- 17-yl)oxy)-\-(2-(9-methyl-2-oxo- 6,7,8,9-tetrahydro-2Z / -pyrano[3,2-g]quinolin-4-yl)ethyl)acetamide (Compound 181)

[1087] 1H-NMR (400 MHz, CDCl3): δ 7.22 (s, 1H), 6.73 (t, J= 5.6 Hz, 1H), 3.93 (s, 2H), 3.62 (dd, J= 6.8 , 13.2 Hz, 2H), 3.36 (t, J= 6.0 Hz, 2H), 3.26 (t, J= 11.2 Hz, 1H), 2.97 (s, 3H), 2.94- 2.90 (m, 2H), 2.79 (t, J= 6.0 Hz, 3H), 2.42-2.23 (m, 3H), 2.13-1.90 (m, 4H), 1.80-1.67 (m, 2H), 1.60-1.50 (m, 4H), 1.46-1.21 (m, 6H), 1.10-1.03 (m, 1H), 1.01 (s, 3H, CH3), 0.96-0.85 (m, 3H), 0.74-0.67 (m, 4H). Key Resonances: 1.01 (s, 3H, CH3).

[1088] Step-1: Prepared by Method X. Residue 7-((tert-butyldimethylsilyl)oxy)-3,4- dihydroquinolin-2(1H)-one (95 % yield) as yellow liquid. The material was directly taken on to the next step.

[1089] Step-2: Prepared by Method W. Purification by flash chromatography (silica gel, hexanes to 25% EtOAc / hexanes) gave 7-((tert-butyldimethylsilyl)oxy)-1-methyl-3,4-dihydroquinolin- 2(1H)-one (53 % yield) as a yellow liquid. The material was directly taken on to the next

[1090] Step-3: Prepared by Method V. Purification by flash chromatography (silica gel, hexanes to 25% EtOAc / hexanes) gave 7-((tert-butyldimethylsilyl)oxy)-1-methyl-1,2,3,4- tetrahydroquinoline (88% yield) as a yellow liquid. The material was directly taken on to the next step.

[1091] Step-4: Prepared by Method U. Purification by flash chromatography (silica gel, hexanes to 20% EtOAc / hexanes) gave 1-methyl-1,2,3,4-tetrahydroquinolin-7-ol (88% yield) as an off- white solid. The material was directly taken on to the next step.

[1092] Step-5: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 60% EtOAc / hexanes) gave benzyl (2-(9-methyl-2-oxo-6,7,8,9-tetrahydro-2H -pyrano[3,2- g]quinolin-4-yl)ethyl)carbamate (32 % yield) as a yellow solid. ESI (m / z) [C23H24N2O4+H]+393.

[1093] Step-6: Prepared by Method H. The residue was washed with MTBE to give 4-(2- aminoethyl)-9-methyl-6,7,8,9-tetrahydro-2H -pyrano[3,2-g]quinolin-2-one (65% yield) as a yellow solid. The material was directly taken on to the next step. Step-7: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 100% EtOAc / hexanes) gave 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro- 1H -cyclopenta[a]phenanthren-17-yl)oxy)-A-(2-(9-methyl-2-oxo-6,7,8,9- tetrahydro-2Z / -pyrano[3,2-g]quinolin-4-yl)ethyl)acetamide (43% yield) as light brown solid. ESI (m / z) [C36H48N2O5+H]+589.

[1094] Example 12: Preparation of 2-(((5S,8R,9S,10S,13S,14S,17S) -10,13-dimethyl-3- oxohexadecahydro- 1 H-cyclopenta [a] phenanthren- 17-yl)oxy)-N-(2-(7-methyl-2-oxo- 7,8,9,10-tetrahydro-2H -pyrano[2,3- / ]quinolin-4-yl)ethyl)acetamide (Compound 182)

[1095] 1H-NMR (400 MHz, CDCl3): δ 7.43 (d, J= 9.2 Hz, 1H), 6.72 (t, J= 6.0 Hz, 1H), 6.57 (d, J = 8.8 Hz, 1H), 3.97-3.89 (m, 2H), 3.62 (dd, J= 6.8 , 13.2 Hz, 2H), 3.34-3.24 (m, 3H), 3.01 (s, 3H), 2.96-2.89 (m, 4H), 2.39-2.23 (m, 3H), 2.11-2.06 (m, 1H), 2.04-1.89 (m, 4H), 1.80-1.76 (m, 1H), 1.71-1.67 (m, 1H), 1.60 (s, 2H), 1.54-1.23 (m, 8H), 1.12-1.04 (m, 1H), 1.01 (s, 3H, CH3), 0.96-0.79 (m, 2H), 0.74-0.68 (m, 4H). Key Resonances: 1.01 (s, 3H, CH3).

[1096] Step-1: Prepared by Method X. Purification by flash chromatography (silica gel, hexanes to 20% EtOAc / hexanes) gave 5-((tert-butyldimethylsilyl)oxy)-1,2,3,4-tetrahydroquinoline (47% yield) as a light brown gum. The material was directly taken on to the next step.

[1097] Step-2: Prepared by Method W. Purification by flash chromatography (silica gel, hexanes to 20% EtOAc / hexanes) gave l-methyl-l,2,3,4-tetrahydroquinolin-5-ol (250 mg, 1.532 mmol, 16% yield) as a dark brown colour solid. The material was directly taken on to the next step.

[1098] Step-3: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 70% EtOAc / hexanes) gave benzyl (2-(7-methyl-2-oxo-7,8,9,10-tetrahydro-2H -pyrano[2,3- / |quinolin-4-yl)ethyl)carbamate (47% yield) as a yellow gum. The material was directly taken on to the next step.

[1099] Step-4: Prepared by Method H. The residue was washed with n-hexane to give 4-(2- aminoethyl)-7-methyl-7,8,9,10-tetrahydro-2Z / -pyrano[2,3-ij]quinolin-2-one (95% yield) as a yellow solid. ESI (m / z) [CI5H18N2O2+H]+259.

[1100] Step-5: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 50% EtOAc / hexanes) gave 2-(((5S,8R,9S, 10S,13S, 14S, 17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-A-(2-(7-methyl-2-oxo-7,8,9,10- tetrahydro-2H -pyrano[2,3-ij]quinolin-4-yl)ethyl)acetamide (59% yield) as a yellow solid. ESI

[1101] (m / z) [C36H48N2O5+H]+589.

[1102] Example 13: Preparation of 2-(((5S,8R,9S, 10S,13S, 14S, 17S )-10,13-dimethyl-3- oxohexadecahydro- 1H -cyclopenta|i / |phenanthren-17-yl)oxy)-N-((11-oxo-2.3,6,7- tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-10)-yl)methyl )acetainide

[1103] 1H-NMR (400 MHz, CDCl3): δ 7.53 (s, 1H), 7.34 (t, J= 6.4 Hz, 1H), 6.83 (s, 1H), 4.31 (d, J = 6.4 Hz, 2H), 3.94 (s, 2H), 3.34 (t, J= 8.0 Hz, 1H), 3.25 (dd, J= 5.6 , 11.2 Hz, 4H), 2.87 (t, J= 6.4 Hz, 2H), 2.75 (t, J= 6.4 Hz, 2H), 2.43-2.23 (m, 3H), 2.10-2.05 (m, 1H), 2.05-1.89 (m, 6H), 1.71-1.66 (m, 1H), 1.57-1.24 (m, 10H), 1.17-1.10 (m, 1H), 1.01 (s, 3H, CH3), 0.98-0.85 (m, 3H), 0.80 (s, 3H, CH3), 0.74-0.67 (m, 1H). Key Resonances: 1.01 (s, 3H, CH3), 0.80 (s, 3H, CH3).

[1104] Step-1: Prepared by Method AB. Purification by flash chromatography (silica gel, hexanes to 50% EtOAc / hexanes) gave 9-formyl-2,3,6,7-tetrahydro-lZ / ,5Z / -pyrido[3,2,1-ij]quinolin-8- yl 3-(( / c77-butoxycarbonyl)amino)propanoate (91% yield) as a yellow solid. ESI (m z) [C21H28N2O5+H]+ 389.

[1105] Step-2: Prepared by Method AA. Purification by flash chromatography (silica gel, hexanes to 25% EtOAc / hexanes) gave tert-butyl ((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- y]pyrido[3,2,1-ij]quinolin-10-yl)methyl)carbamate (28% yield) as a yellow solid. ESI (m z ) [C2IH26N2O4+H]+371. Step-3: Prepared by Method T. The residue was washed with MTBE (10 mL) to give 10- (aminomethyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-11-one hydrochloride (91% yield) as a yellow solid. ESI (m / z) [C16H19ClN2O2+H-53]+254.

[1106] Step-4: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 70% EtOAc / hexanes) gave 2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-A-((11-oxo-2,3,6,7-tetrahydro--1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-10-yl)methyl)acetamide (54% yield) as a yellow solid. ESI (m / z) [C37H48N2O5+H]+601.

[1107] Example 14: Preparation of N-(2-(((5S,8R,9S,10S,13S,14S,17S) -10.13-diinethyl-3- oxohexadecahydro-lH-cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-((ll-oxo-2,3,6,7- tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)inethoxy)acetamide (Compound 184)

[1108] 1H-NMR (400 MHz, CDCl3): δ 6.92 (s, 1H), 6.84 (s, 1H), 4.12 (s, 1H), 3.53-3.38 (m, 6H), 3.28-3.24 (m, 5H), 2.89 (t, J= 6.4 Hz, 2H), 2.75 (t, J= 6.4 Hz, 2H), 2.34-2.23 (m, 3H), 2.09- 2.05 (m, 2H), 1.99-1.92 (m, 6H), 1.80-1.66 (m, 4H), 1.40-1.23 (m, 7H), 0.99 (s, 3H, CH3), 0.96-0.83 (m, 4H), 0.77 (s, 1H), 0.69 (s, 3H, CH3). Key Resonances: 0.99 (s, 3H, CH3), 0.69 (s, 3H, CH3).

[1109] Step-1: Prepared by Method F. Obtained methyl 4-(2-(tert-butoxy)-2-oxoethoxy)-3- oxobutanoate (54% yield) as a yellow gum. The material was directly taken on to the next step.

[1110] Step-2: Prepared by Method Q. Purification by flash chromatography (silica gel, hexanes to 40% EtOAc / hexanes) gave tert-butyl 2-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- _ / ]pyrido[3,2,1-ij]quinolin-9-yl)methoxy)acetate (4.0 g, 8% yield) as a yellow solid. ESI (m z) [C22H27NO5+H]+386.

[1111] Step-3: To a solution of tert-butyl 2-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- _ / ]pyrido[3,2,1-ij]quinolin-9-yl)methoxy)acetate (4.00 g, 10.3 mmol) in CH2Cl2(50 mL) was added TFA (40 mL, 519 mmol) at 10 °C and then the mixture was allowed to warm to room temperature. After 18 hr, the reaction mixture was diluted with chilled sat. sodium bicarbonate. The mixture was washed with CH2Cl2(2 x 50 mL). The aqueous layer was acidified using citric acid solution and then extracted with CH2Cl2(2 x 100 mL). The combined organics were dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure to give 2-((11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- _ / ]pyrido[3,2,1-ij]quinolin-9-yl)methoxy)acetic acid (2.3 g, 67% yield) as a yellow solid. ESI (m / z) [C18H19NO5+H]+330.

[1112] Step-4: Prepared by Method C. Purification by flash chromatography (silica gel, hexanes to 75% EtOAc / hexanes) gave A-(2-(((5S,8R,9S, 10S,13S, 14S, 17S)-10,13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-2-((11-oxo-2, 3,6, 7-tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3, 2,1- z / ]quinolin-9-yl)methoxy)acetamide (43% yield) as a yellow solid. ESI (m z ) [C4IH56N2O7+H]+689.

[1113] Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexanes to 60% EtOAc / hexanes) gave A-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H -cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-((11-oxo-2,3,6,7- tetrahydro-1H,5H,11H-pyrano[2,3-ij]pyrido[3,2,1-ij]quinolin-9-yl)methoxy)acetamide (39 % yield) as a yellow solid. ESI (m / z) [C39H52N2O6+H] 645. Example 15: Preparation of 1-(2-(((5S,8R,9S, 10S,13S, 14S, 17S )-10,13-dimethyl-3- oxohexadecahydro- 1 H -cyclopenta [a] phenanthren- 17-yl)oxy)ethyl)-3-(2-(7-methoxy-2- oxo-2 / / -chromen-4-yl)ethyl)ure:i (Compound 185)

[1114] 1H-NMR (400 MHz, CDCl3): δ 7.72 (d, J= 8.8 Hz, IH), 6.90-6.88 (m, IH), 6.81 (d, J= 2.4 Hz, 1H), 6.13 (s, 1H), 5.26 (s, 1H), 4.75 (t, J= 5.6 Hz, 1H), 3.87 (s, 3H), 3.54-3.47 (m, 4H), 3.30 (t, J= 8.4 Hz, 3H), 2.98 (t, J= 7.2 Hz, 2H), 2.39-2.23 (m, 3H), 2.10-1.92 (m, 4H), 1.83- 1.80 (m, 1H), 1.69-1.64 (m, 5H), 1.42-1.28 (m, 4H), 1.25-1.13 (m, 3H), 1.00 (s, 3H, CH3), 0.71 (s, 3H, CH3). Key Resonances: 1.00 (s, 3H, CH3), 0.71 (s, 3H, CH3).

[1115] Step-1: Prepared by Method P. Purification by flash chromatography (silica gel, hexane to 30% EtOAc / hexane) gave methyl 5-(((benzyloxy)carbonyl)amino)-3-oxopentanoate as a pale yellow liquid (59% yield). ESI (m / z) [C14H17NO5+H]+280.2.

[1116] Step-2: Prepared by Method O. Obtained crude benzyl (2-(7-methoxy-2-oxo-2Z / -chromen- 4-yl)ethyl)carbamate (35% yield) as a colourless liquid. ESI (m / z) [C20H19N05+H]+354.0. Step-3: Prepared by Method H. Obtained crude 4-(2-aminoethyl)-7-methoxy-2Z / -chromen-

[1117] 2-one (77 % yield). ESI (m / z) [C14H17NO5+H]+220. Step-4: Prepared by Method N. Crude 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10, 13- dimethylhexadecahydrospiro[cyclopenta[a]phenanthrene-3,2'-[l,3]dioxolan]-17- yl)oxy)ethyl)-3-(2-(7-methoxy-2-oxo-2Z / -chromen-4-yl)ethyl)urea (60% yield). ESI (m / z) [C36H50N2O7+H]+ 623.3.

[1118] Step-5: Prepared by Method I. Purification by flash chromatography (silica gel, hexane to 80% EtOAc / hexane) gave 1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-l / / -cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(7-methoxy-2-oxo- 2Z / -chromen-4-yl)ethyl)urea (7% yield). ESI (m / z) [C34H46N2O6+H]+579.3.

[1119] Example 16: Preparation of 2-(((5S,8R,9S,10S,13S,14S,17S )-10,13-dimethyl-3- oxohexadecahydro- 1 H -cyclopenta [a] phenanthren- 17-yl )oxy )-N-( ( 7-methoxy -2-oxo-2H - chronien-4-yl)niethyl)-N-methylacetamide (Compound 186)

[1120] 1H-NMR (400 MHz, CDCl3): δ 7.57 (d, J= 8.8 Hz, 1H), 6.88-6.84 (m, 2H), 6.08 (s, 1H), 4.85-4.76 (m, 2H), 4.63 (d, J = 16.4 Hz, 1H), 4.28-4.13 (m, 3H), 3.87 (s, 3H), 3.39-3.31 (m, 1H), 3.08 (s, 3H), 3.02 (s, 1H), 2.39-2.23 (m, 4H), 2.10-1.99 (m, 4H), 1.87-1.84 (m, 1H), 1.72-1.68 (m, 2H), 1.34-1.26 (m, 7H), 1.01 (s, 3H, CH3), 0.98 (s, 1H), 0.80 (s, 3H, CH3). Key Resonances: 1.01 (s, 3H, CH3), 0.80 (s, 3H, CH3).

[1121] Prepared by Method C. Purification by flash chromatography (silica gel, hexane to 30% EtO Ac / hexane) gave 2-(((5S,8R,9S,10S,13S,14S,17S)- 10, 13 -dimethyl-3 -oxohexadecahydro- 1H -cyclopenta[a]phenanthren-17-yl)oxy)-N-((7-methoxy-2-oxo-2H -chromen-4-yl)methyl)- A-methylacetamide (22 % yield) as an off white solid. ESI (m / z) [C33H43NO6+H]+550.2.

[1122] Example 17...

Claims

1. CLAIMSWhat is claimed is:

1. A compound of formula (I), or a salt, solvate, stereoisomer, tautomer, or isotopologue thereof:wherein: ringT1is CH3;T2is H or absent;y y liX is selected from the group consisting of '' '' , '' "" , and '' ''Y1is selected from the group consisting of a bond and -[C(R3a)(R3b)]i.2-;Y2is selected from the group consisting of -C(R3c)(R3d)-, -N(R4a)-, and -C(=O)-;Y3is selected from the group consisting of -C(R3e)(R3f)-, -N(R4b)-, -C(=O)-, and -C(=NOR5)-; or Y2and Y3combine with the atoms to which they are bound to form an optionally substituted C2-C6heteroaryl-fused ring ^;Y4is -[C(R3g)(R3h)]!.2-;R1is selected from the group consisting of H,R2is selected from the group consisting of H and optionally substituted C1-C6alkyl; each occurrence of R3a, R3b, R3c, R3d, R3e, R3f, R3g, and R3h, if present, is independently selected from the group consisting of H, halogen, CN, NO2, ORA, OC(=O)RA, N(RA)(RB), N(RA)C(=O)RB, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl;R4aand R4bare each independently selected from the group consisting of H and optionally substituted C1-C6alkyl;R5is selected from the group consisting of H and optionally substituted C1-C6alkyl;R6is selected from the group consisting of optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl; each occurrence of L is independently selected from the group consisting of L1, L2, L3, and L4;L1is selected from the group consisting of optionally substituted C1-C6alkylenyl and optionally substituted C2-C6alkenylenyl;L2is selected from the group consisting of -C(=O)-, -C(=O)N(RA)-, -N(RA)C(=O)-, -L3is selected from the group consisting of -O-, -N(RA)-, and -S-;L4is selected from the group consisting of -S(=O)-, -S(=O)N(RA)-, -N(RA)S(=O)-, - S(=O)2-, -N(RA)S(=O)2-, and -S(=O)2N(RA)-; ring B is selected from the group consisting of optionally substituted C2-C8heterocycloalkyl and optionally substituted C2-C8heterocycloalkylenyl; ring C is optionally substituted coumarin, or an analogue or derivative thereof; ring D is selected from the group consisting ofR7a, R7b, R7c, R7d, and R7e, if present, are each independently selected from the group consisting of H, halogen, CN, NO2, ORA, OC(=O)RA, N(RA)(RB), N(RA)C(=O)RB, C(=O)RA, C(=O)ORA, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C10heteroaryl;Z1is selected from the group consisting of -O-, -S-, and -N(RA)-; bond a is a single bond or double bond; m, / / , o, / ?, q, r, and 5 are each independently an integer selected from the group consisting of 1, 2, 3, 4, and 5; o is an integer selected from the group consisting of 0, 1, 2, and 3; each occurrence of RAand RB, if present, is independently selected from the group consisting of H, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted C6-C10aryl, and optionally substituted C2-C8heteroaryl; wherein if ring C is present, then no more than two of the following apply:N'OR’ R1O R2yY. A(a) X is ' ' or '' '' , wherein R2is H, and ring C is selected from the(b) L and p are selected such that -[L]p- is -(CH2)C(=O)NH(CH2)2- or -(CH2)2NH(CH2)2-;(c) ring, wherein R5is substituted alkyl.

2. The compound of claim 1, wherein R3a, R3b, R3c, R3d, R3e, R3f, R3g, and R3hare each independently selected from the group consisting of H, F, OH, NH2, NHC(=O)CH3, CN, and3. The compound of claim 1 or 2, wherein Y2and Y3combine with the atoms to which they are bound to form a ring A selected from the group consisting of4. The compound of any one of claims 1-3, wherein the compound of formula (I) is selected from the group consisting of:

5. The compound of any one of claims 1-4, wherein the compound of formula (I) is selected from the group consisting of:

6. The compound of any one of claims 1-5, wherein R1is selected from the groupwherein:Lla, Llb, and Llc, if present, are each independently selected from the group consistingof optionally substituted C1-C6alkylenyl and optionally substituted C2-C6alkenylenyl;L2aand L2b, if present, are each independently selected from the group consisting of - C(=O)-, -C(=O)O-, -N(RA)C(=O)O-, -C(=O)N(RA)-, -N(RA)C(=O)-, -N(RA)C(=O)N(RB)-,L3is selected from the group consisting of -O- and -N(RA)-; andL4is selected from the group consisting of -S(=O)-, -S(=O)2-, and -S(=O)2N(RA)-.

7. The compound of any one of claims 1-6, wherein one of the following applies:(a) ring B is a C2-C8heterocycloalkyl selected from the group consisting of(b) ring B is a C2-C8heterocycloalkylenyl selected from the group consisting ofwherein:R8a, R8b, R8c, R8d, R8e, R8f, R8§, R8h, and R81, if present, are each independently selected from the group consisting of H, halogen, CN, NO2, C(=O)ORA, C(=O)N(RA)(RB), and optionally substituted C1-C6alkyl, or two geminal substituents selected from the group consisting of R8a, R8b, R8c, R8d, R8e, R8f, R8g, R8h, and R81can combine with the carbon atom to which they are bound to form -C(=O)-; andR9is H.

8. The compound of any one of claims 1-7, wherein one of the following applies:(a) ring B is a C2-C8heterocycloalkyl selected from the group consisting of(b) ring B is a C2-C8heterocycloalkylenyl selected from the group consisting of9. The compound of any one of claims 1-8, wherein ring C is selected from the groupwherein:Ri°a, R10b, R10c, and R10dare each independently selected from the group consisting of H, halogen, CN, NO2, and optionally substituted C1-C6alkyl;Rl laand Rl lbare each independently selected from the group consisting of H and optionally substituted C1-C6alkyl, wherein Rl laand R10bor R10ccan combine with the atoms to which theyare bound to form an optionally susbtituted C3-C5 heterocycloalkyl, and wherein Rl lband R10bor R10ccan combine with the atoms to which they are bound to form an optionally substituted C3-C5 heterocycloalkyl;Z2is selected from the group consisting of -O- and -N(R12)-; andR12is selected from the group consisting of H and optionally substituted C1-C6alkyl.

10. The compound of any one of claims 1-9, wherein ring C is selected from the group consisting of:

11. The compound of any one of claims 1-6, wherein R7a, R7b, R7c, R7d, and R7eare eachindependently selected from the group consisting of H, F, t-Bu, benzyl, OCH3, OCF3, OPh, NH2, NHC(=O)CH3, CN, 3 -methoxyphenyl, 2-pyridyl, C(=O)OEt, and C(=O)Ot-Bu.

12. The compound of any one of claims 1-6 and 11, wherein ring D is selected from the group consisting of:

13. The compound of any one of claims 1-12, wherein Lla, Llb, and Llcare each independently selected from the group consisting of -CH2-, -(CH2)2-, -(CH2)3-, and -CH=CH-14. The compound of any one of claims 1-13, wherein L2aand L2bare each independently selected from the group consisting of -NHC(=O)-, -C(=O)NH-, -C(=O)N(CH3)-, - NHC(=O)NH-, -NHC(=O)N(CH3)-, -N(CH3)C(=O)NH-, -NHC(=O)O-, -C(=O)-, -C(=O)O-,15. The compound of any one of claims 1-14, wherein L3is selected from the group consisting of -O- and -NH-.

16. The compound of any one of claims 1-15, wherein L4is selected from the group consisting of -S(=O)2-, -S(=O)2NH-, and -S(=O)-.

17. The compound of any one of claims 1-16, wherein R6is selected from the group18. The compound of any one of claims 1-17, wherein R1is selected from the group consisting of:y ( )y ( )y ( )y ( )y Docket No. 378676- 1002 WO 1(00007)y ( )19. The compound of any one of claims 1-18, which is selected from the group consisting of:2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-picolinoylpiperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-nicotinoylpiperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-isonicotinoylpiperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-hydroxybenzoyl)piperidin-4-yl)acetamide;N-(l -(6-aminopicolinoyl)piperidin-4-yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-(1-(2-aminoisonicotinoyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-hydroxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxybenzoyl)piperidin-4-yl)acetamide;N-(l -(6-aminonicotinoyl)piperidin-4-yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-hydroxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-picolinoylpyrrolidin-3-yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-picolinoylpyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-picolinoylpyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-nicotinoylpyrrolidin-3-yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-nicotinoylpyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-nicotinoylpyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-isonicotinoylpyrrolidin-3-yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-isonicotinoylpyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-isonicotinoylpyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(2-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(2-methoxybenzoyl)pyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-picolinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-picolinoylpyrrolidin-3 -yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-picolinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-nicotinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-nicotinoylpyrrolidin-3 -yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-nicotinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-isonicotinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((R)-1-isonicotinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-isonicotinoylpyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(3 -hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(3-hydroxybenzoyl)pyrrolidin-3- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(4-hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(4-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-methoxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(2-methoxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(2-methoxybenzoyl)pyrrolidin-3- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(3-methoxybenzoyl)pyrrolidin-3- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(4-methoxybenzoyl)pyrrolidin-3- yl)acetamide;N-(1-(6-aminonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-((R)-1-(6-aminonicotinoyl)pyrrolidin-3 -yl)-2-(((5 S,8R,9S, 10S,13S,14S,17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((S)-1-(6-aminonicotinoyl)pyrrolidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-hydroxybenzoyl)pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-(2-hydroxybenzoyl)pyrrolidin-3 - yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-(2-hydroxybenzoyl)pyrrolidin-3- yl)acetamide;N-(1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-((R)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((S)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(4-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(4-methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(3-methoxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(3 -methoxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(3-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((R)-1-(3 -hydroxybenzoyl)pyrrolidin-3 -yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(((S)-1-(3 -hydroxybenzoyl)pyrrolidin-3 - yl)methyl)acetamide;N-((1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-(((R)-1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(((S)-1-(6-aminonicotinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(1-(6-aminopicolinoyl)pyrrolidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-((R)-1-(6-aminopicolinoyl)pyrrolidin-3 -yl)-2-(((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((S)-1-(6-aminopicolinoyl)pyrrolidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 - dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)pyrrolidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)pyrrolidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)pyrrolidine-1- carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-(pyrrolidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-(pyrrolidin-3-yl)acetamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-ylmethyl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(R)-(pyridin-4-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(S)-(pyridin-4-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-yl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(R)-(pyridin-2-yl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(S)-(pyridin-2-yl)pyrrolidine-3-carboxamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(pyrrolidin-3-ylmethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-(pyrrolidin-3-ylmethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-(pyrrolidin-3-ylmethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(R)-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(S)-((1-(4-hydroxybenzoyl)pyrrolidin-3- yl)methyl)acetamide;N-((1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(((R)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(((S)-1-(2-aminoisonicotinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-((1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-(((R)-1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(((S)-1-(6-aminopicolinoyl)pyrrolidin-3-yl)methyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide; tert-butyl 3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine-1-carboxylate; tert-butyl (R )-3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine- 1 - carboxylate; tert-butyl (S)-3-((2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)methyl)pyrrolidine- 1 - carboxylate; tert-butyl 4-(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(piperidin-4-yl)acetamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-2-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3-carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3- carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyrazin-2-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyrimidin-2- ylmethyl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-methyl-N-(quinolin-4-ylmethyl)pyrrolidine-3- carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-4-yl)pyrrolidine-3-carboxamide;N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;(R )-N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;(5)-N-((1H-pyrrolo[2,3-b]pyridin-4-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;(R )-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(imidazo[1,2-a]pyridin-3- ylmethyl)pyrrolidine-3-carboxamide;N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;(R )-N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;(5)-N-((1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17- yl)oxy)acetyl)pyrrolidine-3-carboxamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;(A)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;(5)-1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(pyridin-3-yl)pyrrolidine-3-carboxamide;N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;(R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;(5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(4-methoxyphenyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)-N- methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;(A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;(5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(2-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;(A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;(5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(3-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3-yl)methyl)acetamide;(R )-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;(5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-(4-methoxyphenyl)acetyl)pyrrolidin-3- yl)methyl)acetamide;N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;(R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;(5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(2-methoxyphenyl)acetamide;N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;(R )-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;(5)-N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)pyrrolidin-3-yl)-2-(3-methoxyphenyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17R)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide; tert-butyl (1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)carbamate; tert-butyl 4-((2-(((5 S,8R,9S, 10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)methyl)piperidine-1-carboxylate;N-(1-acetylpiperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; tert-butyl ((1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)methyl)carbamate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-4-yl)acetamide;N-(1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)-3-methoxybenzamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide;N-(1-(N-(tert-butyl)sulfamoyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-4-yl)acetamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)-N-(3-methoxyphenyl)piperidine-4-carboxamide; methyl 4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((1-(2-methoxybenzoyl)piperidin-4- yl)methyl)acetamide; ethyl 4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-4-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R )-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;(A)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;(5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;N-((1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperidin-4-yl)methyl)-3-methoxybenzamide;N-(1-(tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-(1-((R )-tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-(1-((5)-tert-butylsulfinyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-4-yl)acetamide;(E)-1-(4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetyl)piperazin-1-yl)-4-(4-methoxyphenyl)but-2-ene- 1,4-dione;N-(1-(tert-butylsulfonyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxypyridin-2-yl)piperidin-4-yl)acetamide;4-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-((R)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2- enoyl)piperidin-3 -yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-( 1 -((2-(2,6-dioxopiperidin-3 -yl)- 1,3- dioxoisoindolin-4-yl)glycyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-( 1 -((2-(2,6-dioxopiperidin-3 -yl)- 1,3- dioxoisoindolin-5-yl)glycyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(R )-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(5)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide; tert-butyl 4-(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;N-(1-acetylpiperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;(R)-N-( 1 -acetylpiperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 -dimethyl-3 - oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;(S)-N-(1-acetylpiperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide; methyl 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; methyl (R)-3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; methyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(methylsulfonyl)piperidin-3-yl)acetamide; ethyl 3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; ethyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; ethyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate;N-(1-(tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-((S)-1-((S)-tert-butylsulfinyl)piperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((S)-1-((R)-tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((R)-1-((S)-tert-butylsulfinyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;N-((R)-1-((R)-tert-butylsulfinyl)piperidin-3 -yl)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-pivaloylpiperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-phenylpiperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-methoxyphenyl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(m-tolyl)piperidin-3-yl)acetamide;3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;(R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;(S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-N-methylpiperidine-1-carboxamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2-(4-(pyridin-2-yl)phenoxy)acetyl)piperidin-4- yl)acetamide;N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;(R)-N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;(S)-N-(1-(N-(tert-butyl)sulfamoyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(7-methoxy-2-oxo-2H-chromen-4-yl)piperidin-3- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(N-methylsulfamoyl)piperidin-3-yl)acetamide;N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;(R)-N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;(S)-N-(1-(tert-butylsulfonyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-(4-(pyridin-2-yl)phenyl)propanoyl)piperidin-4- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyridin-2-yl)piperidin-3-yl)acetamide; tert-butyl 5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3-difluoropiperidine-1-carboxylate; tert-butyl (R)-5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3- difluoropiperidine-1 -carboxylate; tert-butyl (S)-5-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-3,3- difluoropiperidine-1 -carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-3-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4-difluoropiperidine-l -carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4- difluoropiperidine-1 -carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)-4,4- difluoropiperidine-1 -carboxylate;N-(5, 5-difluoro-1-(3 -methoxybenzyl)piperidin-3 -yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;(R)-N-(5,5-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;(S)-N-(5,5-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;(R)-N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;(S)-N-(4,4-difluoro-1-(3-methoxybenzyl)piperidin-3-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N- methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)-N- methylacetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- IH-cyclopenta[a]phenanthren- 17-yl)oxy)-N-methylacetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-methylacetamido)piperidine- 1 -carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-methylacetamido)piperidine- 1 -carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)acetamide; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)azetidine-1-carboxylate; tert-butyl 3 -(2-(((5 S, 8R, 9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahy dro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate; tert-butyl (S)-3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren- 17-yl)oxy)acetamido)piperidine-1- carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(4-(4-methoxyphenyl)-4-oxobutanoyl)piperidin- 4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(oxetan-3-yl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-fluoropyridin-2-yl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;(S)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(5-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(p-tolyl)but-2-enoyl)piperidin-4- yl)acetamide;N-(1-(3-(N-(3-cyano-4-methyl-1H-indol-5-yl)sulfamoyl)benzoyl)piperidin-4-yl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-(4-hydroxyphenyl)-4-oxobut-2- enoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(4-(trifluoromethyl)phenyl)but-2- enoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-((E)-4-oxo-4-(4-(trifluoromethoxy)phenyl)but-2- enoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-3,3-difluoro-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5 S, 8R, 9S,10S,13S,14S,17 S)-2-fluoro- 10,13 -dimethyl-3 -oxohexadecahydro- 1 Eley cl openta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-amino-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-3-acetamido-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5aS,5bS,7aS,8S,10aS,10bR,12aS)-5a,7a-dimethyl-2- oxooctadecahydrocyclopenta[5,6]naphtho[1,2-d]azepin-8-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-3-cyano-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;(R)-2-(((5S,8R,9S,10S,13S,14S,17S)-3-cyano-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;(S)-2-(((5 S, 8R,9S, 10S, 13 S, 14S, 17 S)-3 -cyano- 10,13 -dimethylhexadecahydro- 1 Iley cl openta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(l -(3- methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(l -(3- methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-(1H-imidazol-1-yl)-10,13- dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(l -(3- methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5R,8R,9S,10S,13S,14S,17S)-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-4,5,6,7,8,9,10,l l,12,13,14,15,16,17- tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin- 4-yl)acetamide;2-(((5aR,5bS,7aS,8S,10aS,10bR,12aR)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[2,l-c]azepin-8-yl)oxy)-N-(1-(3- methoxybenzoyl)piperidin-4-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((4aS,4bS,6aS,7S,9aS,9bR,l laS)-4a,6a-dimethyl-2-oxohexadecahydro-1H- indeno[4,5-h]isoquinolin-7-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((4aR,4bS,6aS,7S,9aS,9bR,l laR)-4a,6a-dimethyl-3-oxohexadecahydro-1H- indeno[5,4-f]isoquinolin-7-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin- 4-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- l,2,3,3a,3b,4,5,5a,6,8,10,10a,10b,l l,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2- f]indazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-4-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(R)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(S)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide; tert-butyl 3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (R)-3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7-oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (S)-3-(2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)acetamido)piperidine-1-carboxylate;2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 4-yl)acetamide;2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;(R)-2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;(S)-2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin- 3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(R)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;(S)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-4- yl)acetamide;(E)-1-(4-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetyl)piperazin-1-yl)-4-(4-methoxyphenyl)but-2-ene- 1 ,4-dione;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3- yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((E)-4-(4-methoxyphenyl)-4-oxobut-2-enoyl)piperidin-3 - yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)acetamide;3-((5S,8R,9S,10S,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;3-((5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;3-((5S,8R,9S,10S,13S,14S)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)-N-(1-(3-methoxybenzoyl)piperidin-4-yl)propenamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((l l-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)acetamide;N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-(11-oxo-2,3,6,7-tetrahydro-lH,5H, 11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)acetamide;N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-N-methyl-2-(l l-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)acetamide;1-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-3-(2-(11-oxo-2, 3,6, 7-tetrahydro-lH, 5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;3-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-1-((11 -oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;1-(2-(((8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-((11-oxo-2,3,6,7-tetrahydro-lH,5H, 11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-3 -(2-( 11 -oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-(2-(l l-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-3-((11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)urea;3-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)ethyl)-1-methyl-1-(2-(11-oxo-2,3,6,7-tetrahydro- 1H,5H,11H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)urea;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(9-methyl-2-oxo-6,7,8,9-tetrahydro-2H- pyrano[3,2-g]quinolin-4-yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methyl-2-oxo-7, 8,9,10-tetrahydro-2H- pyrano[2,3-f]quinolin-4-yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((l l-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3- f]pyrido[3 ,2, 1 -ij ]quinolin- 10-yl)methyl)acetamide;N-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-2-((11-oxo-2,3,6,7-tetrahydro-lH,5H, 11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methoxy)acetamide;1-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)ethyl)-3-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)urea;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((7-methoxy-2-oxo-2H-chromen-4-yl)methyl)-N- methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((7-methoxy-2-oxo-2H-chromen-4- yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy -2-oxo- 1,2-dihy droquinolin-4- yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-1-methyl-2-oxo- 1 ,2-dihydroquinolin- 4-yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(7-methoxy-2-oxo-2H-chromen-4- yl)propyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)-N- methylacetamide;N-(2-(7-(2-amino-2-oxoethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-morpholinoethoxy)-2-oxo-2H-chromen-4- yl)ethyl)acetamide;N-(2-(7-(cyanomethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-((4-(2-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)acetamido)ethyl)-2-oxo-2H-chromen-7-yl)oxy)acetic acid;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-hydroxyethoxy)-2-oxo-2H-chromen-4- yl)ethyl)acetamide; ethyl 2-((4-(2-(2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamido)ethyl)-2-oxo-2H- chromen-7-yl)oxy)acetate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-2-methyl-1-oxo- 1 ,2- dihydroisoquinolin-4-yl)ethyl)acetamide;N-(2-(2-benzyl-7-methoxy-1-oxo- 1 ,2-dihydroisoquinolin-4-yl)ethyl)-2- (((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-1-oxo-1H-isochromen-4- yl)ethyl)acetamide;N-(2-(7-(2-aminoethoxy)-2-oxo-2H-chromen-4-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-(2-(4-methylpiperazin-1-yl)ethoxy)-2-oxo-2H- chromen-4-yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(7-methoxy-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)acetamide;2-(((1S,3aS,3bR,5aS,8aS,8bS,10aS)-8a,10a-dimethyl-7- oxohexadecahydrodicyclopenta[a,f]naphthalen-1-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H- chromen-4-yl)ethyl)acetamide;2-(((4aR,4bS,6aS,7S,9aS,9bR,l laR)-4a,6a-dimethyl-3-oxohexadecahydro-1H- indeno[5,4-f]isoquinolin-7-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide;2-(((4aS,4bS,6aS,7S,9aS,9bR,l laS)-4a,6a-dimethyl-2-oxohexadecahydro-1H- indeno[4,5-h]isoquinolin-7-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4-yl)ethyl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-m ethyl-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;2-(((5aS,5bS,7aS,8S,10aS,10bR,12aS)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[1,2-c]azepin-8-yl)oxy)-N-(2-(7-methoxy-2-oxo- 2H-chromen-4-yl)ethyl)acetamide;2-(((5aR,5bS,7aS,8S,10aS,10bR,12aR)-5a,7a-dimethyl-3- oxooctadecahydrocyclopenta[5,6]naphtho[2,l-c]azepin-8-yl)oxy)-N-(2-(7-methoxy-2-oxo- 2H-chromen-4-yl)ethyl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2- d]isoxazol-1-yl)oxy)-N-(2-(7-methoxy-2-methyl-1-oxo- 1 ,2-dihydroisoquinolin-4- yl)ethyl)acetamide;2-(((3S,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethylhexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide;2-(((5 S, 8R, 9S,10S,13S,14S,l 7 S,E)-3 -(methoxyimino)- 10,13 -dimethylhexadecahy dro- IH-cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(11-oxo-2, 3,6, 7-tetrahy dro-lH,5H,l 1H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;2-(((5 S, 8R, 9S,10S,13S,14S,l 7 S,E)-3 -(hy droxyimino)- 10,13 -dimethylhexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(l l-oxo-2,3,6,7-tetrahydro-1H,5H,11H- pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;3-((5S,8R,9S,10S,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)propenamide;2-((((5S,8R,9S,10S,13S,14S,E)-10,13-dimethyl-3-oxohexadecahydro-17H- cyclopenta[a]phenanthren-17-ylidene)amino)oxy)-N-(2-(l l-oxo-2,3,6,7-tetrahydro- lH,5H,l 1H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)ethyl)acetamide;2-((((5S,8R,9S,10S,13S,14S,E)-10,13-dimethyl-3-oxohexadecahydro-17H- cyclopenta[a]phenanthren-17-ylidene)amino)oxy)-N-((l l-oxo-2,3,6,7-tetrahydro- lH,5H,l 1H-pyrano[2,3-f]pyrido[3,2,l-ij]quinolin-9-yl)methyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)-N-methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)-N-methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]oxazol-3(2H)- yl)ethyl)-N-methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)-N-m ethylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(6-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)-N-methylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxo-2,3-dihydro-1H- benzo[d]imidazol-1-yl)ethyl)-N-m ethylacetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-methoxy-2-oxobenzo[d]thiazol-3(2H)- yl)ethyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(6-methoxy-2-oxobenzo[d]oxazol-3(2H)-yl)propyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(5-fluoropyridin-3-yl)ethyl)acetamide;N-(3-(6-amino-5-cyanopyridin-3-yl)propyl)-2-(((8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren- 17-yl)oxy)-N-(2-(imidazo[ 1 ,2-a]pyridin-2-yl)ethyl)acetamide;N-(2-(1H-pyrrolo[2,3-b]pyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-(3-(6-acetamido-5-cyanopyridin-3-yl)propyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(3-(5-fluoropyridin-3-yl)propyl)acetamide;N-(2-(6-amino-5-cyanopyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)-10,13- dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)acetamide;N-(2-(6-acetamido-5-cyanopyridin-3-yl)ethyl)-2-(((5S,8R,9S,10S,13S,14S,17S)- 10,13 -dimethyl-3 -oxohexadecahydro- 1 H-cy clopenta[a]phenanthren- 17 -yl)oxy)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(4-(pyridin-2-yl)benzyl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(4-(pyrimidin-2-yl)pyridin-2-yl)acetamide;(5S,8R,9S,10S,13S,14S,17S)-17-((6-(tert-butyl)-1H-benzo[d]imidazol-2-yl)methoxy)- 10,13-dimethylhexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((6-phenoxy-1H-benzo[d]imidazol- 2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-17-((4-methoxy-1H-benzo[d]imidazol-2-yl)methoxy)- 10,13-dimethylhexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((6-(trifluoromethoxy)-1H- benzo[d]imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl 3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)m ethyl)- 1 ,2,4-oxadiazol-3 -yl)piperidine-1- carboxylate; tert-butyl (S)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-l,2,4-oxadiazol-3-y l)piperidine-1-carboxylate; tert-butyl (R)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-l,2,4-oxadiazol-3- yl)piperidine-1-carboxylate; tert-butyl 3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren- 17-yl)oxy)m ethyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidine-1- carboxylate; tert-butyl (S)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-l,3,4-oxadiazol-2- yl)piperidine-1-carboxylate; tert-butyl (R)-3-(5-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-l,3,4-oxadiazol-2- yl)piperidine-1-carboxylate; tert-butyl 2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-benzo[d]imidazole-6-carboxylate; tert-butyl 3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl (R)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(2-(7-methoxy-2-oxo-2H-chromen-4- yl)ethyl)acetamide; tert-butyl 3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine- 1 -carboxylate; tert-butyl (R)-3-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine- 1 -carboxylate;tert-butyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)ethyl)carbamate;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-pivaloylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-pivaloylpiperidin-3-yl)-1H- imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-pivaloylpiperidin-3-yl)- 1H-imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-pivaloylpiperidin-3-yl)- 1H-imidazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(1-phenylpiperidin-3-yl)oxazol- 2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-1-phenylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-1-phenylpiperidin-3- yl)oxazol-2-yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one; tert-butyl 4-(2-((((5 S,8R,9S, 10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5-yl)piperidine-1-carboxylate; tert-butyl (S)-4-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl (R)-4-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3- oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-imidazol-5- yl)piperidine-1-carboxylate; tert-butyl ((2-((((5 S,8R,9S, 10S,13S,14S,17S)-10,13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)methyl)carbamate; ethyl 2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)methyl)-1H-benzo[d]imidazole-7-carboxylate;tert-butyl 4-(2-((((5 S,8R,9S, 10S, 13 S, 14S, 17S)- 10, 13 -dimethyl-3 -oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)piperidine-1-carboxylate;N-(1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((R)-1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-benzylpiperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(4-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(4-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(4-fluorobenzyl)piperidin-3 -yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(2-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(2-fluorobenzyl)piperidin-3 -yl)-N-methylacetamide2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-((R)-1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-fluorobenzyl)piperidin-3-yl)-N-methylacetamide;N-(1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((R)-1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-(4-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-(1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((R)-1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-(3-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-(1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((R)-1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-(2-cyanobenzyl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)- 10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridin-2-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridin-2-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyri din-2 -ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyridin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrimidin-2-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrimidin-2-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrimidin-2-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyridazin-3-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrazin-2-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrazin-2-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrazin-2-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((3-fluoropyridin-2-yl)methyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((3-fluoropyridin-2-yl)methyl)piperidin-3-yl)-N- methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((3 -fluoropyridin-2-yl)methyl)piperidin-3 -yl)-N- methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-((5-fluoropyridin-3-yl)methyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-((5-fluoropyridin-3-yl)methyl)piperidin-3-yl)-N- methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-((5-fluoropyri din-3 -yl)methyl)piperidin-3 -yl)-N- methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-((1-methyl-1H-imidazol-2-yl)methyl)piperidin-3- yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(( 1 -methyl- 1H-imidazol-2-yl)methyl)piperidin-3 - yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(( 1 -methyl- IH-imidazol -2 -yl)methyl)piperidin-3 - yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(thiazol-5-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(thiazol-4-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(thiazol-4-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(thiazol-4-ylmethyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(oxazol-5-ylmethyl)piperidin-3-yl)acetamide;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S , 12aS)-1-((5-( 1 -(3 -fluoropyri din-2 -yl)piperi din-3 -yl)- l,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(3 -fluoropyri din-2-yl)piperi din-3 -yl)- l,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((S)-1-(3 -fluoropyri din-2-yl)piperi din-3 -yl)-1.3.4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-( 1 -(3 -fluoropyri din-2 -yl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(3 -fluoropyri din-2-yl)piperi din-3 - yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((S)-1-(3 -fluoropyri din-2-yl)piperi din-3 - yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -( 1 -(3 -fluoropyri din-2 -yl)piperi din-3 -yl)-1.2.4-oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -((R)-1-(3 -fluoropyri din-2-yl)piperi din-3 -yl)- l,2,4-oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((3 -((S)-1-(3 -fluoropyri din-2-yl)piperi din-3 -yl)- l,2,4-oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(2-fluorobenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole;(1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(2-fluorobenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(2-fluorobenzyl)piperidin-3-yl)oxazol-2- yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;( 1 S,3 aS,3bR,5aS, 1 OaS, 1 Ob S, 12aS)-1-((5-((R)-1-(2-fluorobenzyl)piperidin-3 - yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(2-fluorobenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-(1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-((R)-1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((3-((S)-1-(2-fluorobenzyl)piperidin-3-yl)-l,2,4- oxadiazol-5-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)pyrrolidin-3-yl)-1H- imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)pyrrolidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)pyrrolidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; l-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; l-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; l-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1 ,3 ,4-oxadiazol-2-yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-4H- l,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- 4H-l,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- 4H-l,2,4-triazol-3-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)pyrrolidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)oxazol- 2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro- 1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3- yl)oxazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(piperidin-3-yl)oxazol-2- yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-piperidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-piperidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1H-imidazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- l,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- l,3,4-oxadiazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; l-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; l-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one; l-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2-dimethylpropan- 1 -one;l-(3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one; l-((R)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one; l-((S)-3-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-4-methyl-4H- 1 ,2,4-triazol-3 -yl)piperidin-1-yl)-2,2- dimethylpropan-1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-piperidin-3-yl)-l,3,4- oxadiazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;4-(2-(5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-l,3,4-oxadiazol-2-yl)ethyl)-7-methoxy-2H-chromen-2-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-(1-(4-methoxybenzyl)piperidin-3-yl)-1H- imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((R)-1-(4-methoxybenzyl)piperidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-1-((5-((S)-1-(4-methoxybenzyl)piperidin-3-yl)- 1H-imidazol-2-yl)methoxy)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11, 12,,12a- tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazole; benzyl (2-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate; benzyl (2-(2-((((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro- 1H-cyclopenta[a]phenanthren-17-yl)oxy)methyl)oxazol-5-yl)ethyl)carbamate;2-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)ethan-1-amine; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one; l-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-1-methyl- 1H-imidazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan- 1-one; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-(pyrrolidin-3-yl)oxazol-2- yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole; (1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((R)-pyrrolidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;(1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-1-((5-((S)-pyrrolidin-3- yl)oxazol-2-yl)methoxy)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazole;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-(piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((R)-piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-((S)-piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-pivaloylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-pivaloylpiperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-pivaloylpiperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-methoxybenzyl)piperidin-3-yl)-N-methylacetamide;4-((5-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)-l,3,4-oxadiazol-2-yl)methyl)-7-methoxy-2H-chromen-2-one;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-piperidin-3-yl)acetamide;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-(piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((R)-piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-17-((5-((S)-piperidin-3-yl)oxazol-2- yl)methoxy)hexadecahydro-3H-cyclopenta[a]phenanthren-3-one;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-(piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-((R)-piperidin-3-yl)acetamide;2-(((5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxohexadecahydro-1H- cyclopenta[a]phenanthren-17-yl)oxy)-N-methyl-N-((S)-piperidin-3-yl)acetamide; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)pyrrolidin-1-yl)-2,2-dimethylpropan-1-one; l-(3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one; l-((R)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;1-((S)-3-(2-((((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)methyl)oxazol-5-yl)piperidin-1-yl)-2,2-dimethylpropan-1-one;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(2-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-2-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-2-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(2,2,2-trifluoroacetyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(2,2,2-trifluoroacetyl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(2,2,2-trifluoroacetyl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6,6-dimethylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-6,6-dimethylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-6,6-dimethylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-methylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3S,6R)-6-methylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3S,6S)-6-methylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3R,6S)-6-methylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((3R,6R)-6-methylpiperidin-3-yl)acetamide;5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;(2S,5S)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;(2S,5R)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;(2R,5S)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;(2R,5R)-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-2-carboxamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-6-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-6-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(6-(3-methoxyphenyl)pyridin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-methyl-2-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-methyl-2-oxopiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-methyl-2-oxopiperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(4-methylpyrimidin-2-yl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(4-methylpyrimidin-2-yl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(4-methylpyrimidin-2-yl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(pyrimidin-2-yl)piperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(pyrimidin-2-yl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(pyrimidin-2-yl)piperidin-3 -yl)acetamide;N-(6-benzylpyridin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((R)-1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-((S)-1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-(1-(3-fluoropyridin-2-yl)piperidin-3-yl)-N-methylacetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(6-methylpyri din-2 -yl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(6-methylpyri din-2-yl)piperidin-3 -yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(6-methylpyridin-2-yl)piperidin-3-yl)acetamide;N-((R)-1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-(((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-(((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-(1-(4,6-difluoropyrimidin-2-yl)piperidin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((R)-1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-(((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-((S)-1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-(((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide;N-(1-(2,6-difluoropyrimidin-4-yl)piperidin-3-yl)-2-(((1 S,3aS,3bR,5aS, 10aS, 10bS, 12aS)-10a, 12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methylacetamide; tert-butyl 2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2S,5S)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2S,5R)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2R,5S)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate; tert-butyl (2R,5R)-2-cyano-5-(2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a- dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,l l,12,12a-tetradecahydro-1H- cyclopenta[7,8]phenanthro[2,3-c]isoxazol-1-yl)oxy)acetamido)piperidine-1-carboxylate;N-(6-benzylpyridin-3-yl)-2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl- 2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3- yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3 - yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-3 - yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-(1-phenylpiperidin-3-yl)acetamide;2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((R)-1-phenylpiperidin-3 -yl)acetamide; and2-(((1S,3aS,3bR,5aS,10aS,10bS,12aS)-10a,12a-dimethyl-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3- c]isoxazol-1-yl)oxy)-N-methyl-N-((S)-1-phenylpiperidin-3 -yl)acetamide.

20. A pharmaceutical composition comprising at least one compound of any one of claims 1-19 and at least one pharmaceutically acceptable carrier.

21. A method of treating, preventing, and / or ameliorating cancer in a subject in need thereof, the method comprising administering to the subject at least one compound of any one of claims 1-19 and / or the pharmaceutical composition of claim 20.

22. The method of claim 21, wherein the cancer is associated with malignant cell growth and / or hyperplastic cell growth.

23. The method of claim 21 or 22, wherein the cancer is selected from the group consisting of prostate cancer, breast cancer, ovarian cancer, uterine cancer, endometrialcancer, salivary gland carcinoma, bladder cancer, gastrointestinal cancer, kidney cancer, liver cancer, oral squamous cell carcinoma, and brain cancer.

24. The method of claim 23, wherein the cancer is prostate cancer.

25. The method of claim 24, wherein the prostate cancer is castration-resistant prostate cancer.

26. The method of claim 24 or 25, wherein the prostate cancer comprises cells expressing AR-V7.

27. A method of impairing androgen receptor (AR) transactivation and / or androgen receptor dimerization in a subject, the method comprising administering to the subject at least one compound of any one of claims 1-19 and / or the pharmaceutical composition of claim 20.

28. The method of claim 27, wherein the subject is further administered at least one additional agent, optionally wherein the at least one additional agent is selected from the group consisting of flutamide, bicalutamide, enzalutamide, apalutamide, darolutamide, dilutamide, finasteride, and dutasteride.

29. A method of inhibiting cell growth in a subject, the method comprising administering to the subject at least one compound of any one of claims 1-19 and / or the pharmaceutical composition of claim 20.

30. The method of claim 29, wherein the subject is further administered at least one additional agent, optionally wherein the at least one additional agent is selected from the group consisting of flutamide, bicalutamide, enzalutamide, apalutamide, darolutamide, dilutamide, finasteride, dutasteride, abiraterone acetate, abiraterone acetate fine particle, and ketoconazole.

31. The method of claim 29 or 30, wherein the cell growth inhibited is malignant cell growth and / or hyperplastic cell growth.

32. The method of claim 31, wherein the malignant cell growth is cancer cell growth.

33. The method of claim 32, wherein the cancer cell growth is a hormonal cancer cell growth.

34. The method of claim 33, wherein the hormonal cancer is at least one selected from the group consisting of prostate cancer, breast cancer, ovarian cancer, uterine cancer, endometrial cancer, salivary gland carcinoma, bladder cancer, gastrointestinal cancer, kidney cancer, liver cancer, oral squamous cell carcinoma, and brain cancer.

35. The method of claim 33 or 34, wherein the hormonal cancer cell growth is prostate cancer cell growth.

36. The method of claim 35, wherein the prostate cancer cell growth is castration-resistant prostate cancer cell growth.

37. The method of claim 36, wherein the castration-resistant prostate cancer cells express AR-V7.

38. A method of imaging malignant cells and / or hyperplastic cells in a subject, the method comprising:(a) administering to the subject at least one compound of any one of claims 1-19 and / or the pharmaceutical composition of claim 20;(b) exposing the subject at least partially to electromagnetic radiation, such that the at least one compound and / or pharmaceutical composition is excited;(c) detecting excitation of the at least one compound and / or pharmaceutical composition; and(d) imaging the subject or a portion thereof, wherein the malignant cells and / or hyperplastic cells are imaged.

39. The method of claim 38, wherein the malignant cells are cancer cells.

40. The method of claim 39, wherein the cancer cells are hormonal cancer cells.

41. The method of claim 40, wherein the hormonal cancer cells are at least one selectedfrom the group consisting of prostate cancer cells, breast cancer cells, ovarian cancer cells, uterine cancer cells, endometrial cancer cells, salivary gland cancer cells, bladder cancer cells, gastrointestinal cancer cells, kidney cancer cells, liver cancer cells, oral squamous cancer cells, glioblastoma cancer cells, and brain cancer cells.

42. The method of claim 41, wherein the hormonal cancer cells are prostate cancer cells.

43. The method of claim 42, wherein the prostate cancer cells are castration-resistance prostate cancer cells.

44. The method of claim 43, wherein the castration-resistance prostate cancer cells express AR-V7.

45. The method of any one of claims 38-44, wherein the imaging is repeated such that activity of androgen metabolism is measured.

Images