4'-halogen-containing nucleotide and nucleoside therapeutic compositions and related uses
Halogen-containing nucleotide and nucleoside compositions effectively target viral RNA polymerase to treat or prevent a variety of viral infections, addressing the need for novel therapies against pathogens like Eastern and Western equine encephalitis and Chikungunya fever.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-11-27
- Publication Date
- 2026-04-10
AI Technical Summary
There is a need for novel compounds and treatments for viral infections, particularly those caused by mosquito-borne viruses such as Eastern and Western equine encephalitis and Chikungunya fever, as well as other viral pathogens like Ebola and influenza, which pose significant health risks and require effective therapeutic interventions.
Development of halogen-containing nucleotide and nucleoside therapeutic compositions, including compounds with phosphorus oxide derivatives, amino acid esters, lipids, and sphingolipids, formulated into pharmaceutical compositions for administration via various routes to treat or prevent viral infections.
These compositions demonstrate efficacy in treating or preventing a wide range of viral infections, including mosquito-borne diseases and influenza, by targeting viral RNA-dependent RNA polymerase and providing effective antiviral activity.
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Figure 2026062641000001_ABST
Abstract
Description
Detailed description of the invention
[0001] Cross-reference of related applications This application is a "4'-HALOGEN CONTAIN" application filed on March 7, 2018. ING NUCLEOTIDE AND NUCLEOSIDE THERAPEUTI C COMPOSITIONS AND USES RELATED THERETO” Claiming priority to U.S. Provisional Patent Application No. 62 / 639,725, titled, and the entirety of its disclosure This is incorporated herein by reference. Acknowledgment of government support This invention is supported by grant No. HDTRA1-13-C-0072 from the Defense Threat Reduction Agency. No. and No. HDTRA1-15-C-0075, and the National Institute of Allergy and Infectious Diseases Under grant number HHSN272201500008C granted by the organization, with government support This was done accordingly. The government has certain rights to this invention. [Technical field] This disclosure relates to halogen-containing nucleotide and nucleoside therapeutic compositions, and their This disclosure relates to the use of the virus in relation to the virus infection, for example, Toga. In certain embodiments, this disclosure relates to the use of the virus in relation to the virus infection, for example, Toga. Viridae, Bunyaviridae, Arenaviridae, Coronaviruses, Flaviviruses Family, Picornaviridae, Eastern Equine Encephalitis, Western Equine Encephalitis, and Venezuelan Equine Encephalitis ( (EEE, WEE, and VEE respectively), Chikungunya fever (CHIK), Ebola, Influenza Regarding the treatment or prevention of lupus, RSV, and Zika virus infection. [Background technology] Eastern equine encephalitis, Western equine encephalitis, and Venezuelan equine encephalitis (EEE and WEE, respectively) The causative agents for mosquito bites and mosquito-borne diseases (VEE) and chikungunya fever (CHIK) are transmitted through mosquito bites. It is a vector-borne virus (Togaviridae family, Alphavirus genus) that can be transmitted to humans. Yes. Equine encephalitis virus is a CDC Class B pathogen, and CHIK virus is a Class C pathogen. The virulent strain of the VEE virus, delivered via aerosol, is used as a biological weapon against soldiers. There are significant concerns regarding its use. Animal studies have shown that aerosol exposure can be a major factor. VEE virus infection can lead to rapid, widespread brain infection, resulting in high mortality and disease rates. This has been proven. Roy et al., Pathogenesis of aer osolized Eastern equine encephalitis vir us infection in guinea pigs.Virol J,2009 See 6:170.
[0002] Novel compounds and treatments are needed for viral infections. Disclosed herein The compounds and methods described address these needs. References cited herein are not accepted as prior art. [Overview of the prefecture] This disclosure relates to nucleotides and nucleos containing halogens, such as 4'-halogens. This relates to cytotherapy compositions and their associated uses. The following are optional. Nucleosides, prodrugs, or phosphorus oxidized compounds with phosphorus oxidized or its salts. Amino acid esters linked to nucleotides or nucleosides, lipids, or This is a complex compound containing a sphingolipid or a derivative, or a salt thereof. Specific Embodiments Therefore, this disclosure relates to a compound having formula A,
[0003] [ka] With regard to pharmaceutically acceptable salts, derivatives, or prodrugs thereof, as specified herein To be justified.
[0004] In certain embodiments, the disclosure relates to compounds containing one or more identical or different substituents. This includes derivatives of the compounds disclosed herein. In certain embodiments, the Disclosure relates to pharmaceutically acceptable excipients and the materials disclosed herein. The aim is to create a pharmaceutical composition comprising a compound. In a particular embodiment, the pharmaceutical composition is a tablet. It is in the form of a capsule, pill, or aqueous buffer such as saline or phosphate buffer. .
[0005] In certain embodiments, the disclosed pharmaceutical composition includes the compounds and sprays disclosed herein. It may contain a propellant. In certain embodiments, the propellant is compressed air, ethanol, nitrogen, or carbon dioxide. Carbon, nitrous oxide, hydrofluoroalkane (HFA), 1,1,1,2,-tetrafluorocarbon Oloethane, 1,1,1,2,3,3,3-heptafluoropropane, or combinations thereof It is a vaporized propellant used for combinations and other applications.
[0006] In certain embodiments, this disclosure relates to compounds or pharmaceutical compositions as described herein. The invention envisions a pressurized or non-pressurized vessel containing a manual pump. In certain embodiments, the vessel is a manual pump. Sprays, inhalers, measuring inhalers, dry powder inhalers, atomizers, vibrating mesh atomizers, jets It is a sprayer or an ultrasonic sprayer.
[0007] In certain embodiments, the disclosure relates to a bioabrasive used to treat or prevent viral infections. A method for increasing irritability, comprising an effective amount of the compound or medicine disclosed herein. The present invention relates to a method comprising administering a drug composition to a subject who requires it.
[0008] In certain embodiments, the present disclosure relates to a method for treating or preventing a viral infection, The efficacy of the compounds or pharmaceutical compositions disclosed herein is administered to subjects who require it. The present invention relates to a method that includes the following: In a particular embodiment, the viral infection is caused by the Togaviridae family. Bunyaviridae, Arenaviridae, Coronaviridae, Flaviviridae, Picorna Viridae, Zika virus infection, Eastern equine encephalitis, Western equine encephalitis, and Venezuelan horse encephalitis Flames (EEE, WEE, and VEE respectively), Chikungunya fever (CHIK), Ebola, Influenza and RSV.
[0009] In certain embodiments, the compound or pharmaceutical composition is administered orally, intravenously, or through the lungs. It is administered, that is, intrapulmonaryly. In certain embodiments, this disclosure applies to Eastern Equine Encephalitis, Western Equine Encephalitis, and Venezuelan Equine Encephalitis. Encephalitis (EEE, WEE, and VEE, respectively), Chikungunya fever (CHIK), Evo Treating viral infections such as rheumatism, influenza, RSV, or Zika virus infection or Regarding the use of compounds such as those described herein in the production of preventive agents .
[0010] In certain embodiments, the present disclosure uses the starting materials and reagents disclosed herein to form compounds The compounds disclosed herein are produced by mixing under conditions such that a certain condition is formed. Regarding the method of doing so.
[0011] Additional benefits are some described in the following explanation, some of which are evident from that explanation, or This can be learned by implementing the embodiments described below. The advantages described below are attached. Realized and attainable by the elements and combinations specifically pointed out in the claims of the patent. It will be done. Both the summary of the invention described above and the embodiments for carrying out the invention described below are simply It should be understood that these examples are illustrative and descriptive, and not restrictive. [Brief explanation of the drawing]
[0012] [Figure 1] This demonstrates the stability of EIDD-02749 in methanol. [Figure 2] This demonstrates the stability of EIDD-02749 underwater. [Figure 3] This demonstrates the stability of EIDD-02749 in 0.1N HCl. [Figure 4] This shows the stability of EIDD-02749 in PBS at pH 7.4. [Figure 5] This shows the stability of EIDD-02749 in a pH 9 buffer solution. [Figure 6] This shows the triphosphate concentration in Huh-7 cells incubated with EIDD-02749 or a prodrug. [Figure 7] This shows the triphosphate concentration in Vero cells incubated with EIDD-02749 or a prodrug. [Figure 8] The plasma PK curves from CD-1 mice that received single doses of EIDD-02749 at 50, 150, and 500 mg / kg PO or 10 mg / kg ip are shown. [Figure 9] This shows the changes in body weight of AG129 mice administered 10, 30, and 100 mg / kg of EIDD-02749QD for 10 days. [Modes for carrying out the invention]
[0013] Before describing this disclosure in more detail, it should be noted that this disclosure is not limited to the specific embodiments described. Therefore, it should be understood that these values are subject to change. The terms used are solely for the purpose of describing specific embodiments, and the scope of this disclosure does not extend to the attached patents. It should also be understood that the scope of the claim is not intended to be limited in order to be limited by the scope of the claim. That is the case.
[0014] Unless otherwise defined, all technical and scientific terms used herein are defined in this document. The terms used herein have the same meaning as those generally understood by those skilled in the art to which the disclosure pertains. Any methods and materials similar to or equivalent to those described herein may be used in the implementation of this disclosure. While these methods and materials may also be used in testing, preferred methods and materials are described below.
[0015] All publications and patents referenced herein refer to the respective publications or patents referenced in this specification. As if specifically and individually indicated by, this specification by reference is incorporated by To disclose and describe how and / or the materials used in the publication are incorporated and cited, This is incorporated herein by reference. Any citation of any publication is subject to the disclosure prior to the filing date. Therefore, this disclosure does not have the right to date such publications prior to prior disclosure. It should not be interpreted as acknowledging this. Furthermore, the provided publication date is independently The actual release date may differ, and may need to be verified.
[0016] As will become apparent to those skilled in the art through reading this disclosure, the individual Each of the embodiments has distinct components and features, and these are within the scope of this disclosure. Without departing from the scope or spirit, it is easily possible from any of several other embodiments. They can be separated or combined. Any enumerated method is enumerated The events may be performed in the order in which they occurred, or in any other logically possible order.
[0017] Embodiments of this disclosure, unless otherwise indicated, are medical, organic, or otherwise within the scope of the art. Techniques from chemistry, biochemistry, molecular biology, pharmacology, etc., will be used. This is fully explained in the table of contents.
[0018] This disclosure relates to 4'-halogen-containing nucleotide and nucleoside therapeutic compositions, as well as This relates to the use of those. In certain embodiments, this disclosure optionally relates to phosphorus oxidized The present disclosure relates to nucleosides complexed with salts thereof. In certain embodiments, the present disclosure relates to oxidized ri Amino acid esters linked to nucleotides or nucleosides by a molecule, as well as lipids. The term "or" refers to a complex compound containing a sphingolipid or derivative, or a salt thereof. Specific implementation form In this disclosure, these are intended for use in the treatment of infectious diseases, viral infections, and cancer. The aim is to create a pharmaceutical composition containing a compound.
[0019] In certain embodiments, this disclosure relates to a virus-encoded RNA-dependent RNA polymerase. By targeting the enzyme (RdRp), positive-sense and negative-sense Oxidized phosphorus proteopropyl alcohol for the treatment of 4'-halogen-containing nucleosides in RNA virus infections This disclosure relates to drugs. This disclosure also relates to nucleoside analogs for the treatment of infectious diseases and cancer. It also provides the common use of lipids and sphingolipids for delivery.
[0020] In certain embodiments, the present disclosure describes how phosphorus oxidizes nucleotides or nucleosides. This relates to a complex compound or salt thereof containing linked sphingolipids or derivatives. In the embodiment, phosphorus oxide is a phosphate, phosphonate, polyphosphate, or polyphosphate. It is a diphosphonate, a polyphosphate or a phosphate in a polyphosphonate, h Phosphates may optionally be phosphorothioates or phosphorothioates. It is an amino date. In certain embodiments, the lipid or sphingolipid is an amino group or It is covalently bonded to phosphorus oxidized via a hydroxyl group.
[0021] A nucleotide or nucleoside contains a heterocycle with two or more nitrogen heteroatoms. The substituted heterocycle can optionally contain one or more of the same or different alkyl, halogen, Alternatively, it may be substituted with a cycloalkyl group.
[0022] In certain embodiments, the sphingolipid is optionally substituted with one or more substituents. , saturated or unsaturated 2-aminoalkyl or 2-aminooctadecane. Specific fruits In the application form, the sphingolipid derivative is optionally substituted with one or more substituents, It is a saturated or unsaturated 2-aminooctadecane-3-ol. In certain embodiments, sulf Ingolipid derivatives are saturated or unsaturated 2-dimethyl phosphates, optionally substituted with one or more substituents. It is -aminooctadecane-3,5-diol.
[0023] In certain embodiments, this disclosure may involve any compound disclosed herein and a pharmaceutically acceptable The aim is to create a pharmaceutical composition comprising an excipient. In a particular embodiment, the pharmaceutical composition is pi It is in the form of a liquid, capsule, tablet, or saline buffer containing sugars. Specific embodiments The composition includes analgesics, anti-inflammatory agents, non-steroidal anti-inflammatory agents, antiviral agents, and antibiotics. Alternatively, it may contain a second active agent, such as an anticancer agent.
[0024] In certain embodiments, the present disclosure relates to a method for treating or preventing an infection, comprising an effective amount of A method relating to administering a compound disclosed in the specification to a subject in need thereof. Typically, the subject is diagnosed with an infection caused by a virus, bacteria, fungus, protozoa, or parasite. It is being done, or there is a risk of it happening.
[0025] In certain embodiments, the present disclosure relates to a method for treating a viral infection, wherein an effective amount of the present invention A method relating to administering a pharmaceutical composition disclosed in this document to a subject in need thereof. In certain embodiments, the subject is a mammal, such as a human. In certain embodiments, The subjects have been diagnosed with a chronic viral infection. In certain applications, the viral infection is more likely to be It is administered under conditions where it cannot be detected. In certain embodiments, the subject is an RNA virus It is diagnosed as a DNA virus or retroviral infection. In certain embodiments, The targets are viruses, namely double-stranded DNA viruses and sense single-stranded DNA viruses. Double-stranded RNA viruses, sense single-stranded RNA viruses, antisense single-stranded RNA viruses S, sense, diagnosed as a single-stranded RNA retrovirus or a double-stranded DNA retrovirus. It is being done.
[0026] In certain embodiments, the target is subtype H1N1, H3N2, H7N9, or H Influenza A virus, influenza B virus, including 5N1, influenza Rotavirus C, Rotavirus A, Rotavirus B, Rotavirus C, Rotavirus D Rotavirus E, human coronavirus, SARS coronavirus, MERS coronavirus Human adenovirus (HAdV-1~55 types), human papillomavirus (HPV) Models 16, 18, 31, 33, 35, 39, 45, 51, 52, 56, 58, and 59, Parvovirus B19, molluscum contagiosum virus, JC virus (JCV), BK virus Merkel cell polyomavirus, Coxsackie A virus, Coxsackie B virus Norovirus, rubella virus, lymphocytic choriomeningitis virus (LCMV), Chikungu Nia, Eastern Equine Encephalitis Virus (EEEV), Western Equine Encephalitis Virus (WEEV), Venezu Erauma encephalitis virus (VEEV), Ross River virus, Berma Forest virus, Measles virus, mumps virus, RSV, rinderpest virus, California encephalitis virus Viruses, hantaviruses, rabies viruses, Ebola viruses, Marburg viruses, single Pure herpesvirus-1 (HSV-1), herpes simplex virus-2 (HSV-2), water Smallpox and zoster virus (VZV), Epstein-Barr virus (EBV), cytomegalovirus Virus (CMV), lymphocytotropic herpesvirus, roseolovirus, or kapo D'sarcoma-associated herpesvirus, hepatitis A, hepatitis B, hepatitis D, hepatitis E, or human immunotherapy Diagnosed with HIV (incomplete virology).
[0027] In certain embodiments, the target is subtype H1N1, H3N2, H7N9, H5N1( Influenza A viruses, including low-pathogenic and H5N1 (high-pathogenic), influenza Influenza type B virus, influenza type C virus, rotavirus A, rotavirus B, Rotavirus C, Rotavirus D, Rotavirus E, SARS coronavirus, MERS Coronavirus, human adenovirus (HAdV-1~55) type, papillomavirus ( HPV) 16, 18, 31, 33, 35, 39, 45, 51, 52, 56, 58, and Type 59, Parvovirus B19, Molluscum contagiosum virus, JC virus (JCV), BK Viruses, Merkel cell polyomavirus, Coxsackie A virus, Coxsackie B Viruses, norovirus, rubella virus, lymphocytic choriomeningitis virus (LCMV), Measles virus, mumps virus, RSV, parainfluenza virus 1 and Type 3, Rinderpest virus, Chikungunya, Eastern Equine Encephalitis Virus (EEEV), Venezuela Western equine encephalitis virus (WEEV), Western equine encephalitis virus (VEEV), California encephalitis Viruses, Rift Valley fever virus (RVFV), Heartland virus, Lacrosse virus Rus, Malpol virus, Severe fever with thrombocytopenia syndrome virus, Pichinde virus, Ha Ntavirus, Takaribevirus, Funin, Rabies virus, Ebola virus, Marlborovirus Herpes simplex virus, adenovirus, herpes simplex virus-1 (HSV-1), herpes simplex Herpes zoster virus-2 (HSV-2), varicella-zoster virus (VZV), Epstein-Barr Virus (EBV), cytomegalovirus (CMV), lymphotropic herpesvirus Roseolovirus, or Kaposi's sarcoma-associated herpesvirus, hepatitis A, hepatitis B, You are diagnosed with hepatitis D, hepatitis E, or human immunodeficiency virus (HIV).
[0028] In certain embodiments, this disclosure relates to the treatment of infectious diseases, viral infections, or cancer or Regarding the use of the compounds disclosed herein in the production or manufacture of preventive agents. ru.
[0029] In certain embodiments, this disclosure refers to any of the compounds or formulas disclosed herein. Regarding derivatives of [the substance]. Embodiments of this disclosure, unless otherwise indicated, are medical, organic, or otherwise within the scope of the art. Techniques from chemistry, biochemistry, molecular biology, pharmacology, etc., will be used. This is fully explained in the table of contents.
[0030] In certain embodiments, the drug may be in the form of a salt or a prodrug, which are disclosed herein. It is administered in the specified manner and identified by weight. This refers to the weight of the listed compounds. If it is in the form of a salt or prodrug, the weight is the same as the weight of the corresponding salt or prodrug. This is molar equivalent.
[0031] As used herein and in the appended claims, the singular "one (a)" is used. "An" and "the" are plural unless the context explicitly indicates otherwise. It should be noted that references are included in this specification and the following claims. Refer to some terms, and unless the opposite intention is clear, they have the following meanings. It shall be defined as follows.
[0032] Before describing the various embodiments, the following definitions are provided and will be used unless otherwise specified. It should be done. As used herein, the term “deuterium” or “D” means D in relation to H (hydrogen). The isotopic abundance is at least 50%, at least 75%, or at least 90%. This refers to the matter.
[0033] As used herein, the term "phosphorus oxide" refers to phosphorus-oxygen (PO or P=O) This refers to any various chemical moieties that contain a bond. When used as a linking group in this specification, The bonded molecule may be bonded to oxygen, or it may be directly bonded to a phosphorus atom. This term refers to phosphoric acid, in which phosphorus is typically bonded to four oxygen atoms, and phosphorus is typically bonded to four oxygen atoms. It is intended to contain phosphonic acid bonded to one carbon and three oxygen atoms, , but not limited to these. "Polyphosphate" generally refers to at least one phosphorus-oxygen-lyphosphate. This refers to phosphate groups linked together by POP bonds. "Polyphosphonic acid" is... This refers to polyphosphate containing at least one phosphorus-carbon (CPOP) bond. -In addition to containing oxygen bonds, oxidized phosphorus is phosphorus-thiol (PS or P=S ) may also include a phosphoro-amine (PN) bond and / or a phosphoro-amine (PN) bond, each of which is a phosphoro-amine bond. It is called OHET or phosphoramidate. In phosphorus oxide, the oxygen atom is phosphorus... These combinations may form double or single bonds, and oxygen may also form double or single bonds with carbon and other elements. It may further bond with atoms, or with cations, such as metals or quaternary amines. It may also exist as an anion in equilibrium.
[0034] "Subject" refers to any animal, preferably a human patient, livestock, or household pet. As used herein, the terms “prevent” and “prevent” mean “to prevent recurrence.” This includes preventing the spread or outbreak of the disease. This disclosure is not intended to be limited to complete prevention. In some embodiments, the onset of the disease is delayed, or the severity of the disease is reduced.
[0035] As used herein, the terms “to treat” and “to treat” are used in relation to the subject matter. This disclosure is not limited to cases where (for example, a patient) is cured and the disease is eradicated. Rather, it is not limited to cases where (for example, a patient) is cured and the disease is eradicated. Embodiments may also attempt to provide treatment that merely alleviates symptoms and / or slows the progression of the disease. To illustrate.
[0036] As used herein, the term “in combination with” means administration by additional treatment. When used to describe, the medication should be used before, together with, or after additional treatment. Or, it means that they can be administered in combination.
[0037] As used herein, "alkyl" refers to a compound containing 1 to 10 carbon atoms. This refers to a straight-chain or branched-chain saturated hydrocarbon moiety. "Higher alkyl" means 11 or more molecules. This refers to saturated hydrocarbons containing carbon atoms. 16 " contains 6 to 16 carbon atoms It refers to the alkyl group it contains. Similarly, "C6~C 22 " contains 6 to 22 carbon atoms This refers to alkyl groups. Typical saturated linear alkyl groups include methyl, ethyl, n-propyl, and n- Butyl, n-pentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, etc. The saturated branched alkyl groups include isopropyl, sec-butyl, isobutyl, and tert - Contains butyl, isopentyl, etc.
[0038] As used herein, the term "alkenyl" refers to an unsaturated compound containing a double bond. This refers to the straight-chain or branched hydrocarbon portion. Unless otherwise specified, C2-C 24 (for example , C2~C 22 , C2~C 20 , C2~C 18 , C2~C16 , C2 to C 14 , C2 to C 12 , C2 to C 10 , (C2 - C8, C2 - C6, or C2 - C4) alkenyl groups are contemplated. The alkenyl group may contain more than one unsaturated bond. Examples include ethenyl, 1 -propenyl, 2-propenyl, 1-methylethenyl, 1-butenyl, 2-butenyl, 3 -butenyl, 1-methyl-1-propenyl, 2-methyl-1-propenyl, 1-methyl- 2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3- pentenyl, 4-pentenyl, 1-methyl-1-butenyl, 2-methyl-1-butenyl, 3-methyl-1-butenyl, 1-methyl-2-butenyl, 2-methyl-2-butenyl, 3 -methyl-2-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl, 3- methyl-3-butenyl, 1,1-dimethyl-2-propenyl, 1,2-dimethyl-1-prop enyl, 1,2-dimethyl-2-propenyl, 1-ethyl-1-propenyl, 1-ethyl -2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl , 5-hexenyl, 1-methyl-1-pentenyl, 2-methyl-1-pentenyl, 3- methyl-1-pentenyl, 4-methyl-1-pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl , 1-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pent enyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4- pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dime thyl-2-propenyl, 1,2-dimethyl-1-propenyl, 1,2-dimethyl-2-prop Tyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-1-butenyl Lu, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl Tyl-1-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl Lu, 2,2-dimethyl-3-butenyl, 2,3-dimethyl-1-butenyl, 2,3-dimethyl Tyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl L, 3,3-dimethyl-2-butenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl Tenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl Nyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1-ethyl 1-methyl-2-propenyl, 1-ethyl-2-methyl-1-propenyl, and 1 -Ethyl-2-methyl-2-propenyl is an example. The term "vinyl" refers to the structure - This refers to a group having CH=CH2, while 1-propenyl has the structure -CH=CH-CH3. The term refers to a group, and 2-propenyl refers to a group having the structure -CH2-CH=CH2. (Z 1 Z 2 )C=C(Z 3 Z 4 Asymmetrical structures such as those mentioned above are intended to contain both E and Z isomers. This is illustrated. This is assumed in the structural formulas herein when asymmetric alkenes are present. It can be obtained or explicitly indicated by the joining symbol C=C.
[0039] As used herein, the term "alkynyl" refers to a linear compound containing a triple bond. The 't' represents the branched-chain hydrocarbon portion. Unless otherwise specified, C2~C 24 (For example, C2~ C 24 , C2~C20 , C2~C 18 , C2~C 16 , C2~C 14 , C2~C 12 , C 2~C 10 The intended groups are alkynyl groups (C2-C8, C2-C6, or C2-C4). Alkynyl groups can contain more than one unsaturated bond. Examples include ethynyl and 1-propyl groups. Nyl, 2-propynyl (or propargyl), 1-butynyl, 2-butynyl, 3-butynyl Nyl, 1-methyl-2-propynyl, 1-pentinyl, 2-pentinyl, 3-pentinyl , 4-pentynyl, 3-methyl-1-butynyl, 1-methyl-2-butynyl, 1-methyl -3-Butynyl, 2-Methyl-3-Butynyl, 1,1-Dimethyl-2-Propynyl, 1- Ethyl-2-propynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hex Synyl, 5-hexynyl, 3-methyl-1-pentynyl, 4-methyl-1-pentynyl, 1-methyl-2-pentynyl, 4-methyl-2-pentynyl, 1-methyl-3-pentynyl L, 2-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl-4-pentynyl Zynyl, 3-methyl-4-pentynyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl Tyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl Lu, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl Zynyl, 2-ethyl-3-butynyl, and 1-ethyl-1-methyl-2-propynyl Which C2-C6 alkynyl compounds are listed?
[0040] Non-aromatic monocyclic or polycyclic alkyls are referred to herein as "carbocyclic" or "carbo This is called the "cyclyl" group. Typical saturated carbon rings include cyclopropyl and cyclobutyl. Examples include cyclopentyl and cyclohexyl, and as for unsaturated carbon rings, cyclopentyl Examples include tenyl and cyclohexenyl.
[0041] A "heterocarbocyclic" group is formed from nitrogen, oxygen, and sulfur. A carbon ring containing 1 to 4 independently selected heteroatoms, which are saturated or It can be unsaturated (but not aromatic), monocyclic or polycyclic, and a nitrogen and sulfur heterogen. The atom may be optionally oxidized, and the nitrogen heteroatom may be optionally quaternized. Examples of heterocarbon rings include morpholinyl, pyrrolidinonyl, pyrrolidinyl, piperidinyl, Hydantoinyl, Valerolactamyl, Oxyranil, Oxetanil, Tetrahydrofurani Tetrahydropyranil, tetrahydropyridinyl, tetrahydroprimidinyl, tetrahydroprimidinyl, tetra Lahydrothiophenyl, tetrahydrothiopyranil, tetrahydropyrimidinil, tetra Examples include hydrothiophenyl and tetrahydrothiopyranil.
[0042] The term "aryl" preferably refers to phenyl, naphthyl, and biphenyl. Monocyclic, bicyclic, and aromatic homocyclic (i.e., hydrocarbon) compounds having 6 to 12 members. This refers to a tricyclic ring-containing group. Phenylen is a preferred aryl group. "Substituting aryl" The term preferably includes alkyl, substituted alkyl, alkenyl (optionally substituted) (substituted), aryl (optionally substituted), heterocyclo (optionally substituted) ), halo, hydroxy, alkoxy (optionally substituted), aryloxy (optional) (Selectively substituted), alkanoyl (optionally substituted), aroyl, (optionally Selectively substituted, alkyl ester (optionally substituted), aryl ester (Optionally substituted), cyano, nitro, amino, substituted amino, amide, lactam aryl substituted with one or more groups selected from urea, urethane, sulfonyl, etc. A group is defined as a molecule with 3 to 7 members, optionally consisting of one or more substituents that are bonded to the atom to which they are bonded. It forms a ring.
[0043] As used herein, "heteroaryl" or "heteroaromatic" refers to nitrogen, acid It has 1 to 4 heteroatoms selected from element and sulfur, and is monocyclic and polycyclic. This refers to an aromatic heterocarbon ring containing at least one carbon atom, including both rings. A polycyclic ring system contains one or more non-aromatic rings, as long as one of the rings is aromatic. While it is possible to do so, these are not necessary. Typical heteroaryls include furyl and benzofuryl. Nyl, thiophenyl, benzothiophenyl, pyrrolyl, indolyl, isoindolyl, a Zaindolyl, Pyridyl, Quinolinyl, Isoquinolinyl, Oxazolyl, Isooxazoli Lu, Benzoxazolyl, Pyrazolyl, Imidazolyl, Benzimimidazolyl, Thiazolyl, Benzothiazolyl, isothiazolyl, pyridadinil, pyrimidinil, pyrazinil, tria These are dinyl, cinolinyl, phthalazinyl, and quinazolinyl. "Heteroaryl" and The use of this term refers to N-alkylation induction such as 1-methylimidazole-5-yl substituents. It is intended to include the body.
[0044] As used herein, "heterocyclic" refers to a ring containing nitrogen, oxygen, and It has 1 to 4 heteroatoms selected from and sulfur, and at least 1 carbon atom This refers to monocyclic and polycyclic ring systems that are contained within. Monocyclic and polycyclic ring systems are aromatic rings, It may be a non-aromatic ring, or a mixture of aromatic and non-aromatic rings. Heterocyclic rings include hetero This includes carbon rings, heteroaryl compounds, and other similar elements.
[0045] "Alkylthio" has the indicated number of carbon atoms bonded through sulfur crosslinks. This refers to alkyl groups as defined above. An example of alkylthio is methylthio (i.e. It is -S-CH3).
[0046] "Alkoxy" is a compound having the indicated number of carbon atoms bonded through oxygen crosslinks. This refers to alkyl groups as defined below. Examples of alkoxy groups include methoxy and ethoxy. n-propoxy, i-propoxy, n-butoxy, s-butoxy, t-butoxy, n- Examples include, but are not limited to, pentoxy and s-pentoxy. The lucoxy group consists of methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, These are s-butoxy and t-butoxy.
[0047] "Alkylamino" has the indicated number of carbon atoms bonded through amino crosslinks. This refers to alkyl groups as defined above. An example of alkylamino is methylamino( That is, -NH-CH3).
[0048] "Alkanoyl" has the indicated number of carbon atoms bonded through carbonyl crosslinks. This refers to alkyl groups as defined above (i.e., -(C=O)alkyl groups). "Alkyl sulfonyl" is shown to be bonded through sulfonyl crosslinks such as mesyl. Alkyl (i.e., -S(=O)2) having a certain number of carbon atoms as defined above. Alkyl refers to an alkyl group, and "arylsulfonyl" is an aryl group that is bonded through a sulfonyl crosslink. It refers to the -S(=O)2 aryl compound.
[0049] "Alkyl sulfamoyl" is a number of elements that are bonded through sulfamoyl crosslinks. Alkyl (i.e., -NHS(=O)2) having carbon atoms as defined above. Alkyl refers to an alkyl group, and "arylsulfamoyl" is linked through sulfamoyl crosslinking. It refers to the aryl compound (i.e., the -NHS(=O)2 aryl compound).
[0050] "Alkyl sulfinyl" is a group of carbon atoms linked together through sulfinyl crosslinks. Alkyls having elementary atoms as defined above (i.e., -S(=O) alkyls) It refers to.
[0051] The terms "cycloalkyl" and "cycloalkenyl" refer to fully saturated compounds, respectively. and partially unsaturated monocyclic, dicyclic, or tricyclic homocyclic groups of 3 to 15 carbon atoms It refers to a compound that is not aromatic as a whole, but has an aromatic part. For example, containing fluorene, tetrahydronaphthalene, dihydroindene, etc. This includes cyclic and tricyclic ring systems. The ring of a polycyclic cycloalkyl group is connected by one or more spirobonds. They can be fused, crosslinked, and / or joined. "substituted cycloalkyl" and "substituted cycloalkyl" The term "chloroalkenyl" is preferably an aryl, substituted aryl, or heterochloroalkenyl. Rocyclo, substituted heterocyclo, carbocyclo, substituted carbocyclo, halo, hydroxy, a Lucoxy (optionally substituted), aryloxy (optionally substituted), A Lukyl esters (optionally substituted), aryl esters (optionally substituted) ), alkanoyl (optionally substituted), ariol (optionally substituted) ), cyano, nitro, amino, substituted amino, amide, lactam, urea, urethane, sulfo Cycloalkyl and cycloalchemic compounds substituted with one or more groups selected from yl groups, etc. It refers to the nyl group.
[0052] The terms "halogen" and "halo" refer to fluorine, chlorine, bromine, and iodine. . The term "substituted" refers to a molecule in which at least one hydrogen atom is substituted by a substituent. If substituted, one or more of the groups are "substituents". Molecules can be multiple substituted. In the case of an oxo substituent ("=O"), two hydrogen atoms are substituted. Exemplary examples in this context. Suitable substituents include halogens, hydroxyls, alkyls, alkoxys, nitros, cyanos, and oxys. Kiso, carbocyclyl, carbocycloalkyl, heterocarbocykryl, heterocarbocy Chloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl , -NRaRb, -NRaC(=O)Rb, -NRaC(=O)NRaNRb, -NRa C(=O)ORb, -NRaSO2Rb, -C(=O)Ra, -C(=O)ORa, -C (=O)NRaRb, -OC(=O)NRaRb, -ORa, -SRa, -SORa, - Possible examples include S(=O)2Ra, -OS(=O)2Ra, and -S(=O)2ORa. In this context, Ra and Rb are either the same or different, and independently of hydrogen, Halogenated hydroxyl, alkyl, alkoxy, alkyl, amino, alkylamino, di Alkylamino, carbocykyl, carbocyalkyl, heterocarbocykyl, hetero Locarbocycloalkyl, aryl, arylalkyl, heteroaryl, heteroaryl It may be an alkyl group.
[0053] As used herein, the term “optionally substituted” means “in addition to the basis of The substitution is arbitrary, and therefore, the specified atom may not be substituted. This means that, therefore, the use of the term "optionally substituted" implies that this is true. The examples include both substituted and unsubstituted versions of the base.
[0054] Examples of prodrugs that can be used to improve bioavailability include, Stel, optionally substituted ester, branched ester, optionally substituted branched Esters, carbonates, optionally substituted carbonates, carbamates, optionally Selectively substituted carbamates, thioesters, optionally substituted thioesters, Branched thioesters, optionally substituted branched thioesters, thiocarbonates, optional Selectively substituted thiocarbonates, S-thiocarbonates, and arbitrarily substituted S-thiocarbonates, dithiocarbonates, optionally substituted dithiocarbonates thiocarbamates, optionally substituted thiocarbamates, oxymethoxycal Bonyl, optionally substituted oxymethoxycarbonyl, oxymethoxythiocarbon Nyl, optionally substituted oxymethoxythiocarbonyl, oxymethylcarbonyl , optionally substituted oxymethylcarbonyl, oxymethylthiocarbonyl, optional Selectively substituted oxymethylthiocarbonyl, L-amino acid ester, and D-amino acid Ester, N-substituted L-amino acid ester, N,N-disubstituted L-amino acid ester, N- Substitutive D-amino acid esters, N,N-disubstituted D-amino acid esters, sulfenyl, optional Selectively substituted sulfenyl, imidate, arbitrarily substituted imidate, hi Drazonate, optionally substituted hydrazonate, oxymyl, optionally substituted Oxymil, imidinyl, optionally substituted imidinyl, imidyl, optionally Selectively substituted imidyl, aminal, arbitrarily substituted aminal, hemiami Nar, optionally substituted hemiaminal, acetal, optionally substituted Acetal, hemiacetal, optionally substituted hemiacetal, carbon imitation , optionally substituted with thiocarboneimidate, optionally Optionally substituted thiocarboneimidate, carboneimidyl, and optionally substituted carboxymethyl Carboimidyl, carbamimidate, optionally substituted carbamimidate, Lubamuimidil, optionally substituted with carbamuimidil, thioacetal, optional Optionally substituted thioacetals, S-acyl-2-thioethyls, optionally substituted S-acyl-2-thioethyl, bis-(acyloxybenzyl) ester, optionally Substituted bis-(acyloxybenzyl) esters, (acyloxybenzyl) esters Lu, optionally substituted (acyloxybenzyl) esters, and BAB esters These are some examples.
[0055] As used herein, "salt" means that the parent compound forms an acid salt or base salt of it. This refers to derivatives of the disclosed compound that have been modified in a certain way. Examples of salts include amines and alkyl groups. Mineral or organic salts of basic residues such as amines, or dialkylamines, and carboxylic acids. Examples include, but are not limited to, alkalis or organic salts of acidic residues. In typical embodiments, the salt is a conventional, non-toxic, pharmaceutically acceptable salt, and the formed familial The compound contains a quaternary ammonium salt and a non-toxic inorganic or organic acid. Preferred salt is For example, it is derived from inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, sulfamic acid, phosphoric acid, and nitric acid. These include acetic acid, propionic acid, succinic acid, glycolic acid, stearic acid, lactic acid, and phosphorus. Go acid, tartaric acid, citric acid, ascorbic acid, pamoic acid, maleic acid, hydroxymaleic acid Phenylacetic acid, glutamic acid, benzoic acid, salicylic acid, sulfanilic acid, 2-acetoxide benzoic acid, fumaric acid, toluenesulfonic acid, methanesulfonic acid, ethanedisulfonic acid, Examples include salts prepared from organic acids such as oxalic acid and isethionic acid.
[0056] The term "prodrug" refers to a drug that is converted into a biologically active form in vivo. It refers to the fact that, in some situations, prodrugs may be easier to administer than their parent compounds. Often useful. For example, even if they are bioavailable through oral administration, parental This is not always the case with compound drugs. Prodrugs can also outperform the parent drug in a pharmaceutical composition. Improved solubility may also be observed. Prodrugs undergo enzymatic processes and metabolic hydration. It can be converted to the parent drug through various mechanisms, including degradation.
[0057] As used herein, the term “derivative” means the full functionality of the identified analogue. This refers to structurally similar compounds that retain the same properties. Derivatives are structurally similar. There is one or more substituents, salts, that are substituted with one or more substituents in different hydrated / oxidized states. Perhaps because it lacks an atom (for example, by substituting a single or double bond, or a hydroxyl group) This is because (a atom is replaced with a ketone) or because one or more atoms in the molecule are transposed. (Not limited to, but including substitution of an oxygen atom with a sulfur or nitrogen atom, or replacing an amino group with a hydrogen atom) Substitution with a droxyl group, or vice versa. Substitution of a carbon atom with nitrogen in an aromatic ring. The intended derivative is a prodrug. Any various synthesis methods presented in chemical literature or textbooks on synthesis or organic chemistry It can be prepared by appropriate adaptation, for example, March's Advanced Organic Chemistry:Reactions, Mechanisms, and Structure,Wiley,6th Edition(2007)Mi Chael B. Smith, or Domino Reactions in Org anic Synthesis, Wiley (2006) to Lutz F. Tietze. These are provided in the document and are incorporated herein by reference. compound In certain embodiments, the disclosure relates to a compound with a phosphorus moiety or a pharmaceutically acceptable salt thereof. Regarding nucleosides.
[0058] In certain embodiments, the Disclosure relates to compounds of formula I or their pharmaceutically or physiological salts. Regarding
[0059] [ka]
[0060] During the ceremony, X is CH2, CHMe, CMe2, CHF, CF2, or CD2. U is O, S, NH, NR7, CH2, CHF, CF2, CCH2, or CCF2. can be, Q is a natural or unnatural nucleic acid base. R 1 H,
[0061] [ka] TIFF2026062641000005.tif237170TIFF2026062641000006.tif79170
[0062] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 , optionally, one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, aryl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl, wherein, the lipid is C 11 ~C 22 higher alkyl, C 11 ~C 22 higher alkoxy, polyethylene glycol, or aryl substituted with an alkyl group, or a lipid described herein is.
[0063] In certain embodiments, the lipid is an aliphatic alcohol, aliphatic amine, or aliphatic thiol derived from essential and / or non-essential fatty acids. In certain embodiments, the lipid is an unsaturated, polyunsaturated, omega-unsaturated, or omega-polyunsaturated aliphatic alcohol, aliphatic amine, or aliphatic thiol derived from essential and / or non-essential fatty acids. or aliphatic thiol.
[0064] In certain embodiments, the lipid is an aliphatic alcohol, aliphatic amine, or aliphatic thiol derived from essential and non-essential fatty acids having one or more of its carbon units substituted with oxygen, nitrogen, or sulfur.
[0065] In certain embodiments, the lipid is an unsaturated, polyunsaturated, omega-unsaturated, or omega-polyunsaturated aliphatic alcohol, aliphatic amine, or aliphatic thiol derived from essential and / or non-essential fatty acids having one or more of its carbon units substituted with oxygen, nitrogen, or sulfur. or aliphatic thiol.
[0066] In certain embodiments, the lipid is an optionally substituted essential and / or non-essential lipid These are aliphatic alcohols, aliphatic amines, or aliphatic thiols derived from fatty acids. In certain embodiments, lipids are optionally substituted essential and / or non-essential lipids. unsaturated, polyunsaturated, omegaunsaturated, or omega-polyunsaturated aliphatic acids derived from fatty acids These are alcohols, aliphatic amines, or aliphatic thiols.
[0067] In certain embodiments, the lipids are optionally substituted with oxygen, nitrogen, or sulfur. Essential and / or non-essential fatty acids having one or more of their carbon units. The resulting aliphatic alcohol, aliphatic amine, or aliphatic thiol is an aliphatic alcohol, aliphatic amine, or aliphatic thiol.
[0068] In certain embodiments, the lipids are optionally substituted with oxygen, nitrogen, or sulfur. Essential and / or non-essential fatty acids having one or more of their carbon units. unsaturated, polyunsaturated, omegaunsaturated, or omegapolyunsaturated aliphatic alcohols They are aliphatic amines or aliphatic thiols.
[0069] In certain embodiments, the lipid is hexadecyloxypropyl. In certain embodiments, the lipid is 2-aminohexadecyloxypropyl. In certain embodiments, the lipid is 2-aminoarachidyl.
[0070] In certain embodiments, the lipid is 2-benzyloxyhexadecyloxypropyl. . In certain embodiments, the lipids are lauryl, myristyl, palmityl, stearyl, and ara. It is qizyl, behenil, or lignoseryl.
[0071] In certain embodiments, the lipid is a sphingolipid of the following formula:
[0072] [Chemical formula] In the formula,
[0073] R of the sphingolipid 12 is hydrogen, alkyl, C(=O)R 16 , C(=O)OR 16 , or C(=O)NHR 16 and R of the sphingolipid 13 is hydrogen, fluoro, OR 16 , OC(=O)R 16 , OC( =O)OR 16 , or OC(=O)NHR 16 and R of the sphingolipid 14 is a saturated or unsaturated alkyl chain having more than 6 and less than 22 carbon atoms and is optionally substituted with one or more halogens or hydroxy or a structure of the following formula as:
[0074] [Chemical formula]
[0075] n is 8 to 14 or 8 or more and 14 or less, o is 9 to 15 or 9 or more and 15 or less and the sum of m and n is 8 to 14 or 8 or more and 14 or less, and the sum of m and o is 9 to 15 or 9 or more and 15 or less, or
[0076] [Chemical formula]
[0077] n is 4 to 10 or 4 or more and 10 or less, o is 5 to 11 or 5 or more and 11 or less and the sum of m and n is 4 to 10 or 4 or more and 10 or less, and the sum of m and o is 5 to 11 or 5 or more and 11 or less,
[0078] [ka]
[0079] n is between 6 and 12, or n is between 6 and 12, and the sum of m and n is , is between 6 and 12, or n is between 6 and 12, Sphingolipid R 15 is OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , Or OC(=O)NHR 16 And, Sphingolipid R 16 These are hydrogen, cyano, alkyl, alkenyl, alkynyl, and carboxyl. Bosicrill, heterocarbosicrill, aryl, heteroaryl, heterocyclyl, cyclyl Roalkyl, cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclo Oxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy C, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycloamino , heterocarbocycloamino, arylamino, heteroarylamino, heterocyclo Mino, cycloalkamino, cycloalkeneamino, alkylthio, carbocycrylthio, Heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, Cycloalkylthio, cycloalkenylthio, allenyl, or lipid, R 16 teeth, Selectively choose one or more of the same or different R 17 Replaced by, Sphingolipid R 17 These are deuterium, hydroxy, azide, thiol, amino, and cyano , halogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocykryl aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, Alkoxy, carbocyclooxy, heterocarbocyclooxy, aryloxy, hetero Aryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkyl (alkyl)2-amino, (alkyl)2-amino, carbocycloamino, heterocarbocycloamino, a Rylamino, heteroarylamino, heterocycloamino, cycloalcamino, cyclo Alkenamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, ali HCl, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloal Kenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, ma It is a carbonyl group.
[0080] In certain embodiments, sphingolipids R 12 H, methyl, ethyl, propyl, n -Butyl, isopropyl, 2-butyl, 1-ethylpropyl, 1-propylbutyl, thiopropyl Ropropyl, cyclobutyl, cyclopentyl, cyclohexyl, benzyl, or phenyl It is.
[0081] In certain embodiments, the sphingolipid is a sphingolipid of the following formula:
[0082] [ka]
[0083] During the ceremony, Sphingolipid R 12 is hydrogen, hydroxyl, fluoro, OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 13 is hydrogen, hydroxyl, fluoro, OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 14 This refers to saturated or unsaturated alkyl chains with more than 6 carbon atoms and less than 22 carbon atoms. And, optionally, one or more halogens or structures of the following formulas may be substituted:
[0084] [ka]
[0085] n is between 8 and 14 or between 8 and 14, and the sum of m and n is between 8 and 14 or 8 The structure of the expression is such that the number is between 14 and above. Sphingolipid R 16 These are hydrogen, cyano, alkyl, alkenyl, alkynyl, and carboxyl. Bosicrill, heterocarbosicrill, aryl, heteroaryl, heterocyclyl, cyclyl Roalkyl, cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclo Oxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy C, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycloamino , heterocarbocycloamino, arylamino, heteroarylamino, heterocyclo Mino, cycloalkamino, cycloalkeneamino, alkylthio, carbocycrylthio, Heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, Cycloalkylthio, cycloalkenylthio, allenyl, or lipid, R 16 teeth, Selectively choose one or more of the same or different R 17 Replaced by, Sphingolipid R 17 These are deuterium, hydroxy, azide, thiol, amino, and cyano , halogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocykryl aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, Alkoxy, carbocyclooxy, heterocarbocyclooxy, aryloxy, hetero Aryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkyl (alkyl)2-amino, (alkyl)2-amino, carbocycloamino, heterocarbocycloamino, a Rylamino, heteroarylamino, heterocycloamino, cycloalcamino, cyclo Alkenamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, ali HCl, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloal Kenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, e These are steryl, formyl, carboxy, carbamoyl, amide, or acyl.
[0086] In certain embodiments, sphingolipids R 16 H, methyl, ethyl, propyl, n -Butyl, isopropyl, 2-butyl, 1-ethylpropyl, 1-propylbutyl, thiopropyl These are rhozyl, cyclobutyl, cyclopentyl, cyclohexyl, or benzyl.
[0087] Suitable sphingolipids include sphingosine, ceramide, or sphingomyelia. Examples include 2-aminoalkyl groups, or optionally, 2-aminoalkyl groups substituted with one or more substituents. However, it is not limited to these.
[0088] Other suitable sphingolipids can be optionally substituted with one or more substituents. , 2-aminooctadecane-3,5-diol, (2S,3S,5S)-2-aminooc Tadecane-3,5-diol, (2S,3R,5S)-2-aminooctadecane-3,5 -diol, 2-(methylamino)octadecane-3,5-diol, (2S,3R,5 S)-2-(methylamino)octadecane-3,5-diol, 2-(dimethylamino) Octadecane-3,5-diol, (2R,3S,5S)-2-(dimethylamino)oc Tadecane-3,5-diol, 1-(pyrrolidine-2-yl)hexadecane-1,3-diol All, (1S,3S)-1-((S)-pyrrolidine-2-yl)hexadecane-1,3 -diol, 2-amino-11,11-difluorooctadecane-3,5-diol, ( (2S,3S,5S)-2-amino-11,11-difluorooctadecane-3,5-di 11,11-difluoro-2-(methylamino)octadecane-3,5-diol (2S,3S,5S)-11,11-difluoro-2-(methylamino)octadecane -3,5-diol, N-((2S,3S,5S)-3,5-dihydroxyoctadecane -2-yl)acetamide, N-((2S,3S,5S)-3,5-dihydroxyocta Decane-2-yl)palmitamide, 1-(1-aminocyclopropyl)hexadecane-1 ,3-diol, (1S,3R)-1-(1-aminocyclopropyl)hexadecane-1 ,3-diol, (1S,3S)-1-(1-aminocyclopropyl)hexadecane-1 ,3-diol, 2-amino-2-methyloctadecane-3,5-diol, (3S,5 S)-2-amino-2-methyloctadecane-3,5-diol, (3S,5R)-2- Amino-2-methyloctadecane-3,5-diol, (3S,5S)-2-methyl-2 -(methylamino)octadecane-3,5-diol,2-amino-5-hydroxy-2 -Methyloctadecane-3-one, (Z)-2-amino-5-hydroxy-2-methylo Kutadecane-3-one oxime, (2S,3R,5R)-2-amino-6,6-difluo Looctadecane-3,5-diol, (2S,3S,5R)-2-amino-6,6-diol Luoroctadecane-3,5-diol, (2S,3S,5S)-2-amino-6,6- Difluorooctadecane-3,5-diol, (2S,3R,5S)-2-amino-6, 6-Difluorooctadecane-3,5-diol, and (2S,3S,5S)-2-A Mino-18,18,18-trifluorooctadecane-3,5-diol is one example. , but not limited to these.
[0089] In an exemplary embodiment of formula I, R 1 is hydrogen,
[0090] [ka]
[0091] That is the case. In an exemplary embodiment of formula I, X is CH2. In an exemplary embodiment of formula I, U is O.
[0092] In exemplary embodiments of Formula I, Q is uracil, cytosine, adenine, and guanine. That is the case. In an exemplary embodiment of formula I, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl, Amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, eth These are nyl and chloroethynyl.
[0093] In an exemplary embodiment of formula I, R 5 Lipids, methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0094] In an exemplary embodiment of formula I, R 6 is hydrogen, hydroxyl, fluoro, chloro, amine No, lipids, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, he Xyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopentyl Cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, tert -Butoxide, N-Propylamino, N-Isopropylamino, N-tert-Butylamino Mino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's mino.
[0095] In an exemplary embodiment of formula I, R 7 These are methyl, ethyl, propyl, isopropyl, and b Chil, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclobutyl 2,6-dimethylphenyl, isopropyl Poxide, tert-butoxide, N-propylamino, N-isopropylamino, N- tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and N It is N-dipropylamino.
[0096] In an exemplary embodiment of formula I, R 8 These are methyl, ethyl, propyl, isopropyl, and b Chil, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclobutyl 2,6-dimethylphenyl, isopropyl Poxide, tert-butoxide, N-propylamino, N-isopropylamino, N- tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and N It is N-dipropylamino.
[0097] In an exemplary embodiment of formula I, R 9 These are methyl, ethyl, propyl, isopropyl, and b Chil, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclobutyl 2,6-dimethylphenyl, isopropyl Poxide, tert-butoxide, N-propylamino, N-isopropylamino, N- tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and N It is N-dipropylamino.
[0098] In certain embodiments, the present disclosure relates to a compound of formula II,
[0099] [ka]
[0100] or relating to its pharmaceutical or physiological salt, in the formula, X is CH2, CHMe, CMe2, CHF, CF2, or CD2. U is O, S, NH, NR7, CH2, CHF, CF2, CCH2, or CCF2. can be, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0101] [ka] TIFF2026062641000016.tif239170TIFF2026062641000017.tif77170
[0102] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0103] In an exemplary embodiment of formula II, R 1 is hydrogen,
[0104] [ka]
[0105] That is the case. In an exemplary embodiment of formula II, X is CH2. In an exemplary embodiment of formula II, U is O.
[0106] In an exemplary embodiment of formula II, W is CR'. In an exemplary embodiment of formula II, Z is CR''. In an exemplary embodiment of formula II, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0107] In the exemplary embodiment of Formula II, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0108] In an exemplary embodiment of formula II, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl , amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, ery These are thinyl and chloroethynyl.
[0109] In an exemplary embodiment of formula II, R 5 These are lipids, methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cy Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0110] In an exemplary embodiment of formula II, R 6 is hydrogen, hydroxyl, fluoro, chloro, a Mino, lipids, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopentyl , cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, ter t-butoxide, N-propylamino, N-isopropylamino, N-tert-butyl Amino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropyl It is amino.
[0111] In an exemplary embodiment of formula II, R 7 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0112] In an exemplary embodiment of formula II, R 8 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0113] In an exemplary embodiment of formula II, R 9 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0114] In certain embodiments, the present disclosure relates to a compound of formula III,
[0115] [ka]
[0116] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0117] [ka] TIFF2026062641000021.tif209170TIFF2026062641000022.tif80170
[0118] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0119] In an exemplary embodiment of Equation III, R 1 is hydrogen,
[0120] [ka]
[0121] That is the case. In an exemplary embodiment of Equation III, W is CR'. In an exemplary embodiment of Equation III, Z is CR''.
[0122] In exemplary embodiments of Formula III, R' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0123] In exemplary embodiments of Formula III, R'' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0124] In an exemplary embodiment of Equation III, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl Lu, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, These are ethynyl and chloroethynyl.
[0125] In an exemplary embodiment of Equation III, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0126] In an exemplary embodiment of Equation III, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0127] In an exemplary embodiment of Equation III, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0128] In an exemplary embodiment of Equation III, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0129] In an exemplary embodiment of Equation III, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0130] In certain embodiments, this disclosure relates to compounds of formula IV,
[0131] [ka]
[0132] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0133] In an exemplary embodiment of formula IV, W is CR'. In an exemplary embodiment of formula IV, Z is CR''. In an exemplary embodiment of formula IV, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0134] In the exemplary embodiment of formula IV, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0135] In an exemplary embodiment of formula IV, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl , amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, ery These are thinyl and chloroethynyl.
[0136] In certain embodiments, the Disclosure relates to compounds of formula V or their pharmaceutically or physiological salts. Regarding
[0137] [ka]
[0138] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0139] In an exemplary embodiment of formula V, W is CR'. In an exemplary embodiment of formula V, Z is CR''. In an exemplary embodiment of formula V, R' is H, F, Cl, OH, methyl, hydroxymethyl fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It is a mill.
[0140] In exemplary embodiments of formula V, R'' is H, F, Cl, OH, methyl, hydroxymethyl fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It is a mill.
[0141] In an exemplary embodiment of formula V, R 2 , R2’ , R 3 , R 3’ is hydrogen, hydroxyl, Amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, eth These are nyl and chloroethynyl.
[0142] In certain embodiments, this disclosure relates to compounds of formula VI,
[0143] [ka]
[0144] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 4 is hydrogen or deuterium, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0145] In an exemplary embodiment of formula VI, W is CR'. In an exemplary embodiment of formula VI, Z is CR''. In the exemplary embodiment of formula VI, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0146] In the exemplary embodiment of formula VI, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0147] In an exemplary embodiment of formula VI, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl , amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, ery These are thinyl and chloroethynyl.
[0148] In an exemplary embodiment of formula VI, R 6 , R 6’ , R 6” , and R 6’’’ all It is hydrogen. In an exemplary embodiment of formula VI, R 6 , R 6’ , and R 6” is hydrogen, and R 6’ ’’ It is methyl.
[0149] In an exemplary embodiment of formula VI, R 6 , R 6’ , and R 6” is hydrogen, and R 6’ ’’ It is methoxy. In an exemplary embodiment of formula VI, R 6 , R 6” , and R 6’’’ is hydrogen, and R 6’ It is methyl.
[0150] In an exemplary embodiment of formula VI, R 6 , R 6” , and R 6’’’ is hydrogen, and R 6’ It is methoxy. In an exemplary embodiment of formula VI, R6 , R 6” , and R 6’’’ is hydrogen, and R 6’ It is fluoro.
[0151] In an exemplary embodiment of formula VI, R 6 , R 6” , and R 6’’’ is hydrogen, and R 6’ It is tert-butyl. In an exemplary embodiment of formula VI, R 6 , R 6” , and R 6’’’ is hydrogen, and R 6’ That is Chlorophyll.
[0152] In an exemplary embodiment of formula VI, R 6 and R 6” is hydrogen, and R 6’ and R 6 ’’’ It is methyl. In an exemplary embodiment of formula VI, R 6’ , R 6” , and R 6’’’ It is hydrogen, R 6 It is fluoro.
[0153] In an exemplary embodiment of formula VI, R 6” is hydrogen, and R 6’ and R 6’’’ teeth, It is tert-butyl, and R 6 It is fluoro. In certain embodiments, the present disclosure relates to compounds of formula VII,
[0154] [ka]
[0155] or relating to its pharmaceutical or physiological salt, in the formula, X is CH2, CHMe, CMe2, CHF, CF2, or CD2. U is O, S, NH, NR7, CH2, CHF, CF2, CCH2, or CCF2. can be, Q is a natural or unnatural nucleic acid base. R 1 H,
[0156] [ka] TIFF2026062641000029.tif237170TIFF2026062641000030.tif80170
[0157] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0158] In an exemplary embodiment of formula VII, R 1 is hydrogen,
[0159] [ka]
[0160] That is the case. In an exemplary embodiment of formula VII, X is CH2. In an exemplary embodiment of formula VII, U is O.
[0161] In exemplary embodiments of formula VII, Q is uracil, cytosine, adenine, and gua. It is a ninja. In an exemplary embodiment of formula VII, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl Lu, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, These are ethynyl and chloroethynyl.
[0162] In an exemplary embodiment of formula VII, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0163] In an exemplary embodiment of formula VII, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0164] In an exemplary embodiment of formula VII, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0165] In an exemplary embodiment of formula VII, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0166] In an exemplary embodiment of formula VII, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0167] In certain embodiments, the present disclosure relates to compounds of formula VIII,
[0168] [ka]
[0169] or relating to its pharmaceutical or physiological salt, in the formula, X is CH2, CHMe, CMe2, CHF, CF2, or CD2. U is O, S, NH, NR7, CH2, CHF, CF2, CCH2, or CCF2. can be, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0170] [ka] TIFF2026062641000034.tif204170TIFF2026062641000035.tif77170
[0171] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0172] In an exemplary embodiment of formula VIII, R 1 is hydrogen,
[0173] [ka]
[0174] That is the case. In an exemplary embodiment of formula VIII, X is CH2. In an exemplary embodiment of formula VIII, U is O.
[0175] In an exemplary embodiment of formula VIII, W is CR'. In an exemplary embodiment of formula VIII, Z is CR''. In exemplary embodiments of formula VIII, R' is H, F, Cl, OH, methyl, hydroxyl methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl It is formyl.
[0176] In exemplary embodiments of formula VIII, R'' is H, F, Cl, OH, methyl, hydroxyl methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl It is formyl.
[0177] In an exemplary embodiment of formula VIII, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxy Sil, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl These are ethynyl and chloroethynyl.
[0178] In an exemplary embodiment of formula VIII, R 5 These are lipids, methyl, ethyl, propyl, and iso Propyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, Neopentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Amino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino It is , and N,N-dipropylamino.
[0179] In an exemplary embodiment of formula VIII, R 6These are hydrogen, hydroxyl, fluoro, and chloro. , amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Chil, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pinch 4-Heptyl, Cyclopropyl, Cyclobutyl, Cyclop Nthyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, t ert-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide Tylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is pyramino.
[0180] In an exemplary embodiment of formula VIII, R 7 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0181] In an exemplary embodiment of formula VIII, R 8 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0182] In an exemplary embodiment of formula VIII, R 9 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0183] In certain embodiments, this disclosure relates to compounds of formula IX,
[0184] [ka]
[0185] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0186] [ka] TIFF2026062641000039.tif239170TIFF2026062641000040.tif78170
[0187] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0188] In an exemplary embodiment of formula IX, R 1 is hydrogen,
[0189] [ka]
[0190] That is the case. In an exemplary embodiment of formula IX, W is CR'. In an exemplary embodiment of formula IX, Z is CR''.
[0191] In an exemplary embodiment of formula IX, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0192] In exemplary embodiments of formula IX, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0193] In an exemplary embodiment of formula IX, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl , amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, ery These are thinyl and chloroethynyl.
[0194] In an exemplary embodiment of formula IX, R 5 These are lipids, methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cy Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0195] In an exemplary embodiment of formula IX, R 6 is hydrogen, hydroxyl, fluoro, chloro, a Mino, lipids, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopentyl , cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, ter t-butoxide, N-propylamino, N-isopropylamino, N-tert-butyl Amino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropyl It is amino.
[0196] In an exemplary embodiment of formula IX, R 7 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0197] In an exemplary embodiment of formula IX, R 8 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0198] In an exemplary embodiment of formula IX, R 9 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0199] In certain embodiments, this disclosure relates to compounds of formula X,
[0200] [ka]
[0201] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0202] In an exemplary embodiment of formula X, W is CR'. In an exemplary embodiment of formula X, Z is CR''. In an exemplary embodiment of formula X, R' is H, F, Cl, OH, methyl, hydroxymethyl fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It is a mill.
[0203] In exemplary embodiments of formula X, R'' is H, F, Cl, OH, methyl, hydroxymethyl fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It is a mill.
[0204] In an exemplary embodiment of formula X, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl, Amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, eth These are nyl and chloroethynyl.
[0205] In certain embodiments, this disclosure relates to compounds of formula XI,
[0206] [ka]
[0207] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0208] In an exemplary embodiment of formula XI, W is CR'. In an exemplary embodiment of formula XI, Z is CR''. In an exemplary embodiment of formula XI, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0209] In exemplary embodiments of formula XI, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0210] In an exemplary embodiment of formula XI, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl , amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, ery These are thinyl and chloroethynyl.
[0211] In certain embodiments, the present disclosure relates to a compound of formula XII,
[0212] [ka]
[0213] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0214] In an exemplary embodiment of formula XII, W is CR'. In an exemplary embodiment of formula XII, Z is CR''. In exemplary embodiments of formula XII, R' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0215] In exemplary embodiments of formula XII, R'' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0216] In an exemplary embodiment of formula XII, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl Lu, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, These are ethynyl and chloroethynyl.
[0217] In an exemplary embodiment of formula XII, R 6 , R 6’ , R 6” , and R 6’’’ all And it's hydrogen. In an exemplary embodiment of formula XII, R 6 , R 6’ , and R 6” is hydrogen, and R 6 ’’’ It is methyl.
[0218] In an exemplary embodiment of formula XII, R 6 , R 6’ , and R 6” is hydrogen, and R 6 ’’’ It is methoxy. In an exemplary embodiment of formula XII, R 6 , R 6” , and R 6’’’ It is hydrogen, R 6’ It is methyl.
[0219] In an exemplary embodiment of formula XII, R 6 , R 6” , and R 6’’’ It is hydrogen, R 6’ It is methoxy. In an exemplary embodiment of formula XII, R 6 , R 6” , and R 6’’’ It is hydrogen, R 6’ It is fluoro.
[0220] In an exemplary embodiment of formula XII, R 6 , R 6” , and R 6’’’ It is hydrogen, R 6’ It is tert-butyl. In an exemplary embodiment of formula XII, R 6 , R 6” , and R 6’’’ It is hydrogen, R 6’ That is Chlorophyll.
[0221] In an exemplary embodiment of formula XII, R 6 and R 6” is hydrogen, and R 6’ and R 6’’’ It is methyl. In an exemplary embodiment of formula XII, R 6’ , R 6” , and R 6’’’It is hydrogen. , R 6 It is fluoro.
[0222] In an exemplary embodiment of formula XII, R 6” is hydrogen, and R 6’ and R 6’’’ teeth , tert-butyl, R 6 It is fluoro. In certain embodiments, this disclosure relates to a compound of formula XIII,
[0223] [ka]
[0224] or relating to its pharmaceutical or physiological salt, in the formula, X is CH2, CHMe, CMe2, CHF, CF2, or CD2. U is S, NH, NR7, CH2, CHF, CF2, CCH2, or CCF2. , W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1H,
[0225] [ka] TIFF2026062641000047.tif208170TIFF2026062641000048.tif79170
[0226] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with thioesters that have been selectively substituted, branched thioesters that have been selectively substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teroaryl amino, heterocyclo amino, cycloalkyl amino, cycloalkene amino, alkyl thio, carbocyclic thio, heterocarbocyclic thio, aryl thio, hetero aryl thio, heterocyclic thio, cycloalkyl thio, cycloalkenyl thio, are nil, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 10 is optionally substituted with one or more identical or different R 11 and R 11 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, al kyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, he teroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, car bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al kyl)2amino, carbocycloamino, heterocarbocycloamino, arylamino, he teroaryl amino, heterocyclo amino, cycloalkyl amino, cycloalkene amino, alkyl thio, carbocyclic thio, heterocarbocyclic thio, aryl thio, hetero aryl thio, heterocyclic thio, cycloalkyl thio, cycloalkenyl thio, are nil, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and lipid is C 11 ~C 22 higher alkyl, C 11 ~C 22 higher alkoxy, polyethylene glycol, or aryl substituted with an alkyl group, or a lipid described herein is.
[0227] In an exemplary embodiment of formula XIII, R 1 is hydrogen,
[0228]
Chemical formula
[0229] and so on. In an exemplary embodiment of formula XIII, X is CH2. In an exemplary embodiment of formula XIII, W is CR'.
[0230] In an exemplary embodiment of formula XIII, Z is CR". In an exemplary embodiment of formula XIII, R' is H, F, Cl, OH, methyl, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, dimethyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, and formyl.
[0231] In an exemplary embodiment of formula XIII, R" is H, F, Cl, OH, methyl, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, dimethyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, and formyl.
[0232] In an exemplary embodiment of formula XIII, R 2 R 2’ R 3 R 3’ is hydrogen, hydroxymethyl, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, dimethyl, fluoromethyl, methoxy, vinyl, ethynyl, and chloroethynyl. and chloroethynyl.
[0233] In an exemplary embodiment of formula XIII, R 5 is lipid, methyl, ethyl, propyl, iso propyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, Neopentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Amino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino It is , and N,N-dipropylamino.
[0234] In an exemplary embodiment of formula XIII, R 6 These are hydrogen, hydroxyl, fluoro, and chloro. , amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Chil, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pinch 4-Heptyl, Cyclopropyl, Cyclobutyl, Cyclop Nthyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, t ert-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide Tylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is pyramino.
[0235] In an exemplary embodiment of formula XIII, R 7 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0236] In an exemplary embodiment of formula XIII, R 8 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0237] In an exemplary embodiment of formula XIII, R 9 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0238] In certain embodiments, this disclosure relates to compounds of formula XIV,
[0239] [ka]
[0240] or relating to its pharmaceutical or physiological salt, in the formula, X is CHMe, CMe2, CHF, CF2, or CD2. W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0241] [ka] TIFF2026062641000052.tif237170TIFF2026062641000053.tif79170
[0242] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 , R 2’ , R 3 , R 3’ These are, independently, hydrogen, deuterium, alkyl, and alke. Nyl, alkynyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, ho Lumil, Acyl, Cyano, Halogen, Aryl, Heteroaryl, Heterocyclyl, Cal Bocyclyl, heterocarbocyclyl, sulfinyl, sulfamoyl, or sulfonyl Selected from, R 2 , R 2’ , R 3 , R 3’ This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 2 and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different Rs above 10 are substituted with R 7 and R 7’ can form a ring together with the α-carbon to which they are attached, and the ring is optionally substituted with one or more of the same or different Rs 10 and R R 8 and R 9 can form a ring together with the α-carbon to which they are attached, and the ring is optionally substituted with one or more of the same or different Rs 10 and R R 10 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocarbocycloamino, arylamino, heteroaryl amino, heterocycloamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroaryl thio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, aryl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R is optionally substituted with one or more of the same or different Rs and R is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, R 10 is optionally substituted with one or more of the same or different Rs 11 and R R 11 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0243] In an exemplary embodiment of formula XIV, R 1 is hydrogen,
[0244] [ka]
[0245] That is the case. In an exemplary embodiment of formula XIV, W is CR'. In an exemplary embodiment of formula XIV, Z is CR''.
[0246] In exemplary embodiments of formula XIV, R' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0247] In exemplary embodiments of formula XIV, R'' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0248] In an exemplary embodiment of formula XIV, R 2 , R 2’ , R 3 , R 3’ is hydrogen, hydroxyl Lu, amino, fluoro, chloro, cyano, methyl, fluoromethyl, methoxy, vinyl, These are ethynyl and chloroethynyl.
[0249] In an exemplary embodiment of formula XIV, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0250] In an exemplary embodiment of formula XIV, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0251] In an exemplary embodiment of formula XIV, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0252] In an exemplary embodiment of formula XIV, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0253] In an exemplary embodiment of formula XIV, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0254] In certain embodiments, this disclosure relates to compounds of formula XV,
[0255] [ka]
[0256] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0257] [ka] TIFF2026062641000057.tif237170TIFF2026062641000058.tif77170
[0258] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and hydro Xyl, thiol, amino, azide, formyl, acyl, cyano, halogen, aryl, he Teloaryl, heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl Selected from sulfamoyl or sulfonyl, R 2 This is an optional choice of one or more Same or different R 10 Replaced by, R 2’ These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and thio. aryl, amino, azide, formyl, acyl, cyano, halogen, aryl, heteroaryl L, heterocyclyl, carbocyclyl, heterocarbocykrill, sulfinyl, sulfa Selected from moyl or sulfonyl, R 2’ This is, optionally, one or more of the same These are different R 10 Replaced by, R 3 hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, Hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, alley Sulfur, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sulfur Selected from ynyl, sulfamoyl, or sulfonyl, R 3 You can choose one of them. The above are the same or different R 10 Replaced by, R 3’ These are hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, and alkoxy. hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, ali sul, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sul Selected from finyl, sulfamoyl, or sulfonyl, R 3’ This is optional, One or more identical or different R 10 Replaced by, R 2and R 2’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0259] In an exemplary embodiment of formula XV, R1 is hydrogen,
[0260] [ka]
[0261] That is the case. In an exemplary embodiment of formula XV, W is CR'. In an exemplary embodiment of formula XV, Z is CR''.
[0262] In an exemplary embodiment of formula XV, R' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0263] In exemplary embodiments of formula XV, R'' is H, F, Cl, OH, methyl, hydroxymethyl Tyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, hol It's Lumil.
[0264] In an exemplary embodiment of formula XV, R 5 These are lipids, methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cy Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0265] In an exemplary embodiment of formula XV, R 6is hydrogen, hydroxyl, fluoro, chloro, a Mino, lipids, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopentyl , cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, ter t-butoxide, N-propylamino, N-isopropylamino, N-tert-butyl Amino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropyl It is amino.
[0266] In an exemplary embodiment of formula XV, R 7 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0267] In an exemplary embodiment of formula XV, R 8 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0268] In an exemplary embodiment of formula XV, R 9 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0269] In certain embodiments, this disclosure relates to compounds of formula XVI,
[0270] [ka]
[0271] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0272] [ka] TIFF2026062641000062.tif236170TIFF2026062641000063.tif79170
[0273] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 3 hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, Hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, alley Sulfur, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sulfur Selected from ynyl, sulfamoyl, or sulfonyl, R 3 You can choose one of them. The above are the same or different R 10 Replaced by, R 3’ These are hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, and alkoxy. hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, ali sul, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sul Selected from finyl, sulfamoyl, or sulfonyl, R 3’ This is optional, One or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0274] In an exemplary embodiment of formula XVI, R 1 is hydrogen,
[0275] [ka]
[0276] That is the case. In an exemplary embodiment of formula XVI, W is CR'. In an exemplary embodiment of formula XVI, Z is CR''.
[0277] In exemplary embodiments of formula XVI, R' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0278] In exemplary embodiments of formula XVI, R'' is H, F, Cl, OH, methyl, hydroxy Methyl, fluoromethyl, difluoromethyl, trifluoromethyl, vinyl, ethynyl, It is holmil.
[0279] In an exemplary embodiment of formula XVI, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0280] In an exemplary embodiment of formula XVI, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0281] In an exemplary embodiment of formula XVI, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0282] In an exemplary embodiment of formula XVI, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0283] In an exemplary embodiment of formula XVI, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0284] In certain embodiments, this disclosure relates to compounds of formula XVII,
[0285] [ka]
[0286] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents deuterium, halogen, hydroxyl, amino, thiol, alkyl, or alkenyl , alkynyl, aryl, heteroaryl, carbocykrill, heterocarbocykrill, cy It is a chloroalkyl, heterocyclyl, or acyl, and R' is optionally one or more. The same or different R 10 Replaced by, R represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R is a cycloalkyl, heterocyclyl, or acyl, and R is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0287] [ka] TIFF2026062641000067.tif239170TIFF2026062641000068.tif79170
[0288] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2 These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and thio. aryl, amino, azide, formyl, acyl, cyano, halogen, aryl, heteroaryl Heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl, sulfamyl Selected from yl or sulfonyl, R 2 This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 3 and R 3’ These are, independently, hydrogen, deuterium, alkyl, alkenyl, and aldehyde. Quinyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, formyl, A Sil, cyano, halogen, aryl, heteroaryl, heterocyclyl, carbocyrkyl Selected from heterocarbocyrill, sulfinyl, sulfamoyl, or sulfonyl Re, R 3 and R 3’ This is an optional choice of one or more identical or different R 10 Replaced by , R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0289] In an exemplary embodiment of formula XVII, R 1 is hydrogen,
[0290] [ka]
[0291] That is the case. In an exemplary embodiment of formula XVII, R 5 These are lipids, methyl, ethyl, propyl, and iso Propyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, Neopentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Amino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino It is , and N,N-dipropylamino.
[0292] In an exemplary embodiment of formula XVII, R 6 These are hydrogen, hydroxyl, fluoro, and chloro. , amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Chil, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pinch 4-Heptyl, Cyclopropyl, Cyclobutyl, Cyclop Nthyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, t ert-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide Tylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is pyramino.
[0293] In an exemplary embodiment of formula XVII, R 7 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0294] In an exemplary embodiment of formula XVII, R 8 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0295] In an exemplary embodiment of formula XVII, R 9 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0296] In certain embodiments, this disclosure relates to compounds of formula XVIII,
[0297] [ka]
[0298] or relating to its pharmaceutical or physiological salt, in the formula, Z is N or CR, R stands for deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl , alkynyl, aryl, heteroaryl, carbocykrill, heterocarbocykrill, cy It is a chloroalkyl, heterocyclyl, or acyl, and R'' is optionally one or more. The same or different R 10 Replaced by, R 1 H,
[0299] [ka] TIFF2026062641000072.tif236170TIFF2026062641000073.tif82170
[0300] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 2These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and thio. aryl, amino, azide, formyl, acyl, cyano, halogen, aryl, heteroaryl Heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl, sulfamyl Selected from yl or sulfonyl, R 2 This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 3 and R 3’ These are, independently, hydrogen, deuterium, alkyl, alkenyl, and aldehyde. Quinyl, allenyl, alkoxy, hydroxy, thiol, amino, azide, formyl, A Sil, cyano, halogen, aryl, heteroaryl, heterocyclyl, carbocyrkyl Selected from heterocarbocyrill, sulfinyl, sulfamoyl, or sulfonyl Re, R 3 and R 3’ This is an optional choice of one or more identical or different R 10 Replaced by , R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0301] In an exemplary embodiment of formula XVIII, R 1 is hydrogen,
[0302] [ka]
[0303] That is the case. In an exemplary embodiment of formula XVIII, R 5 Lipids, methyl, ethyl, propyl, Sopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl Neopentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl 2,6-dimethylphenyl Nyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Luamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino These are mino and N,N-dipropylamino.
[0304] In an exemplary embodiment of formula XVIII, R 6 is hydrogen, hydroxyl, fluoro, chloro Ro, amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Tyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclo Pentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert- Butylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is Ropilamino.
[0305] In an exemplary embodiment of formula XVIII, R 7 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0306] In an exemplary embodiment of formula XVIII, R 8 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0307] In an exemplary embodiment of formula XVIII, R 9 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0308] In certain embodiments, this disclosure relates to compounds of formula XIX,
[0309] [ka]
[0310] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', Z is N or CR, R' represents hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R stands for deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl , alkynyl, aryl, heteroaryl, carbocykrill, heterocarbocykrill, cy It is a chloroalkyl, heterocyclyl, or acyl, and R'' is optionally one or more. The same or different R 10 Replaced by, R 1 H,
[0311] [ka] TIFF2026062641000077.tif208170TIFF2026062641000078.tif80170
[0312] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 3 hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, Hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, alley Sulfur, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sulfur Selected from ynyl, sulfamoyl, or sulfonyl, R 3 You can choose one of them. The above are the same or different R 10 Replaced by, R 3’ These are hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, and alkoxy. hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, ali sul, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sul Selected from finyl, sulfamoyl, or sulfonyl, R 3’ This is optional, One or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0313] In an exemplary embodiment of formula XIX, R 1 is hydrogen,
[0314] [ka]
[0315] That is the case. In an exemplary embodiment of formula XIX, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0316] In an exemplary embodiment of formula XIX, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0317] In an exemplary embodiment of formula XIX, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0318] In an exemplary embodiment of formula XIX, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0319] In an exemplary embodiment of formula XIX, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0320] In certain embodiments, this disclosure relates to compounds of formula XX,
[0321] [ka]
[0322] or relating to its pharmaceutical or physiological salt, in the formula, W is either N or CR', R' represents deuterium, chloro, iodine, hydroxyl, amino, thiol, alkyl, and ammonium. Kenil, Alkinyl, Aryl, Heteroaryl, Carbocyclyl, Heterocarbocycyl R' is a cycloalkyl, heterocyclyl, or acyl, and R' is optionally 1 More than one or more of the same or different R 10 Replaced by, R 1 H,
[0323] [ka] TIFF2026062641000082.tif240170TIFF2026062641000083.tif80170
[0324] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 3 These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and hydro Xyl, thiol, amino, azide, formyl, acyl, cyano, halogen, aryl, he Teloaryl, heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl Selected from sulfamoyl or sulfonyl, R 3 This is an optional choice of one or more Same or different R 10 Replaced by, R 3’ These are hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, and alkoxy. hydroxy, thiol, amino, azide, formyl, acyl, cyano, halogen, ali sul, heteroaryl, heterocyclyl, carbocyclyl, heterocarbocykrill, sul Selected from finyl, sulfamoyl, or sulfonyl, R 3’ This is optional, One or more identical or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0325] In an exemplary embodiment of formula XX, R 1 is hydrogen,
[0326] [ka]
[0327] That is the case. In an exemplary embodiment of formula XX, R 5 These are lipids, methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cy Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0328] In an exemplary embodiment of formula XX, R 6 is hydrogen, hydroxyl, fluoro, chloro, a Mino, lipids, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopentyl , cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, ter t-butoxide, N-propylamino, N-isopropylamino, N-tert-butyl Amino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropyl It is amino.
[0329] In an exemplary embodiment of formula XX, R 7 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0330] In an exemplary embodiment of formula XX, R 8 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0331] In an exemplary embodiment of formula XX, R 9 methyl, ethyl, propyl, isopropyl, Butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopliers 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Cyclob Tyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isop Lopoxide, tert-butoxide, N-propylamino, N-isopropylamino, N -tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0332] In certain embodiments, this disclosure relates to compounds of formula XXI,
[0333] [ka]
[0334] or relating to its pharmaceutical or physiological salt, in the formula, R 1 H,
[0335] [ka] TIFF2026062641000087.tif236170TIFF2026062641000088.tif76170
[0336] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 3 These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and thio. aryl, amino, azide, formyl, acyl, cyano, halogen, aryl, heteroaryl Heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl, sulfamyl Selected from yl or sulfonyl, R 3 This is an optional choice of one or more identical or different options. Naru R 10 Replaced by, R 3’ These are hydrogen, deuterium, alkyl, alkenyl, alkynyl, allenyl, and alkoxy. thiol, amino, azide, formyl, acyl, cyano, halogen, aryl, hetero Aryl, heterocyclyl, carbocykrill, heterocarbocykrill, sulfinyl, s Selected from rufamoyl or sulfonyl, R 3’ This is an optional choice of one or more of the same The same or different R 10 Replaced by, R 3 and R 3’ They can form a ring together with the carbon atoms to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0337] In an exemplary embodiment of formula XXI, R 1 is hydrogen,
[0338] [ka]
[0339] That is the case. In an exemplary embodiment of formula XXI, R 5 Lipids, methyl, ethyl, propyl, isop Ropil, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, ne Opentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Mino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino , and N,N-dipropylamino.
[0340] In an exemplary embodiment of formula XXI, R 6 is hydrogen, hydroxyl, fluoro, chloro Amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s-butyl Lu, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclopene Tyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, te rt-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It's Luamino.
[0341] In an exemplary embodiment of formula XXI, R 7 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0342] In an exemplary embodiment of formula XXI, R 8 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0343] In an exemplary embodiment of formula XXI, R 9 These are methyl, ethyl, propyl, and isopropyl , butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopen Tyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Butyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, iso Propoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, and It is N,N-dipropylamino.
[0344] In certain embodiments, this disclosure relates to compounds of formula XXII,
[0345] [ka]
[0346] or relating to its pharmaceutical or physiological salt, in the formula, R 1 H,
[0347] [ka] TIFF2026062641000092.tif210170TIFF2026062641000093.tif84170
[0348] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 3’ These are deuterium, alkyl, alkenyl, alkynyl, allenyl, alkoxy, and thio. aryl, amino, azide, formyl, acyl, cyano, halogen, aryl, heteroaryl L, heterocyclyl, carbocyclyl, heterocarbocykrill, sulfinyl, sulfa Selected from moyl or sulfonyl, R 3’ This is, optionally, one or more of the same These are different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0349] In an exemplary embodiment of formula XXII, R 1 is hydrogen,
[0350] [ka]
[0351] That is the case. In an exemplary embodiment of formula XXII, R 5 These are lipids, methyl, ethyl, propyl, and iso Propyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, Neopentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Amino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino It is , and N,N-dipropylamino.
[0352] In an exemplary embodiment of formula XXII, R 6 These are hydrogen, hydroxyl, fluoro, and chloro. , amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Chil, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pinch 4-Heptyl, Cyclopropyl, Cyclobutyl, Cyclop Nthyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, t ert-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide Tylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is pyramino.
[0353] In an exemplary embodiment of formula XXII, R 7 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0354] In an exemplary embodiment of formula XXII, R8 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0355] In an exemplary embodiment of formula XXII, R 9 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0356] In certain embodiments, this disclosure relates to compounds of formula XXIII,
[0357] [ka]
[0358] or relating to its pharmaceutical or physiological salt, in the formula, R 1 H,
[0359] [ka] TIFF2026062641000097.tif206170TIFF2026062641000098.tif80170
[0360] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1 This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro or carbonyl the law of nature, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0361] In an exemplary embodiment of formula XXIII, R 1 is hydrogen,
[0362] [ka]
[0363] That is the case. In an exemplary embodiment of formula XXIII, R 5 Lipids, methyl, ethyl, propyl, Sopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl Neopentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl 2,6-dimethylphenyl Nyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Luamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino These are mino and N,N-dipropylamino.
[0364] In an exemplary embodiment of formula XXIII, R 6 is hydrogen, hydroxyl, fluoro, chloro Ro, amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl Tyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclobutyl, cyclo Pentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert- Butylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is Ropilamino.
[0365] In an exemplary embodiment of formula XXIII, R 7 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0366] In an exemplary embodiment of formula XXIII, R 8 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0367] In an exemplary embodiment of formula XXIII, R 9 These are methyl, ethyl, propyl, and isopropyl. Pill, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neo Pentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl, Clobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, Isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, And N,N-dipropylamino.
[0368] In certain embodiments, this disclosure relates to compounds of formula XXIV,
[0369] [ka]
[0370] or relating to its pharmaceutical or physiological salt, in the formula, R 1 H,
[0371] [ka] TIFF2026062641000102.tif231170TIFF2026062641000103.tif21170
[0372] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid No acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Imidates that are selectively substituted, hydrazonates that are selectively substituted, and hydrazonates that are selectively substituted. Oxymyl, optionally substituted imidinyl, optionally substituted imidinyl Lu, optionally substituted aminal, optionally substituted hemiaminal, optional Selectively substituted acetals, arbitrarily substituted hemiacetals, arbitrarily Substituted carvonimide, optionally substituted thiocarboneimide, optional Selectively substituted carvoneimidyl, arbitrarily substituted carbamimidate, Selectively substituted carbamuimidyl, selectively substituted thioacetal, optional Selectively substituted S-acyl-2-thioethyl, optionally substituted bis-(acyl-2-thioethyl) (Oxybenzyl) ester, optionally substituted with (acyloxybenzyl) ester Selected from R and BAB-ester, 1This is, optionally, one or more of the same These are different R 10 Replaced by, Y is either O or S, Y 1 , OH, OY 3 , or BH3 - M + And, Y 2 is OH or BH3 - M + And, Y 3 Y is an aryl, heteroaryl, or heterocyclyl. 3 This is optional. Specifically, one or more of the same or different R 10 Replaced by, R 5 hydrogen, alkyl, alkenyl, alkynyl, carbocykryl, heterocarbocy Krill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkeni It is a lipid, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 , R 6’ , R 6” , and R 6’’’ These are, independently, hydrogen, deuterium, and hydride. Roxyl, amino, azide, thiol, acyl, formyl, halogen, nitro, alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hetero Aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbosis Chlooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, hetero Rocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl )2 amino, carbocycloamino, heterocarbocycloamino, arylamino, hetero Arylamino, heterocycloamino, cycloalcamino, cycloalkenamino, arylamino Kirtio, Carbocyclilthio, Heterocarbocycrylthio, Arylthio, Heteroari Calcio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, sulfi Selected from yl, sulfamoyl, sulfonyl, allenyl, cyano, or lipid, R 6 , R 6’ , R 6” , and R 6’’’ Each of these can optionally choose one or more of the same or Different R 10 It can be replaced by, R 7 and R 7’ These are, independently, hydrogen, deuterium, hydroxyl, azide, and thiol. L, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, Heterocarbocyrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, Cycloalkenyl, alkoxy, carbocyclooxy, heterocarbocyclooxy, ant aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloa Lukenoxy, alkylamino, (alkyl)2amino, carbocycloamino, heterocar Bocycloamino, arylamino, heteroarylamino, heterocycloamino, cyclo Alkamino, cycloalkenamino, alkylthio, carbocicrulthio, heterocarb Cyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkyl Luthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl Selected from lipids, nitro or carbonyl, R 7 This is an optional choice of one or more of the same or different R 10 Replaced by, R 8 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and alkyl Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, Hete Roaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Cyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, he Terocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl (L) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, hetero Roarylamino, heterocycloamino, cycloalcamino, cycloalkenamino, a Lucurutio, Carbocyclilutio, Heterocarbocycrylutio, Arylthio, Hetero Rilthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, areni Sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 7’ , R 8 , and R 9 These are the α-carbons to which they are bonded, and the α-carbons It can form a ring with the amino group attached to it, and the ring can be optionally formed with one or more The same or different R above 10 Replaced by, R 7 and R 7’ They can form a ring together with the α-carbon to which they are bonded. The ring is one or more identical or different R's, which can be chosen arbitrarily. 10 Replaced by, R 8 and R 9 They can form a ring together with the α-carbon to which they are bonded, This is an optional choice of one or more identical or different R 10 Replaced by, R 10 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl Yes, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxyl, azide, thiol, amino, cyano, halogen, and aluminum. Kill, Alkenyl, Alkinyl, Carbocyclyl, Heterocarbocykrill, Aryl, He Teloaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carboxy Bocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, Heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (al Kill) 2 amino acids, carbocycloamino acids, heterocarbocycloamino acids, arylamino acids, he Teloarylaminos, heterocycloaminos, cycloalcaminos, cycloalkenaminos, Alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, hetero Arylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, all With nyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl can be, Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 High-grade alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. That is the case.
[0373] In an exemplary embodiment of formula XXIV, R 1 is hydrogen,
[0374] [ka]
[0375] That is the case. In an exemplary embodiment of formula XXIV, R 5 These are lipids, methyl, ethyl, propyl, and iso Propyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, Neopentyl, 3-Pentyl, Hexyl, t-Hexyl, 4-Heptyl, Cyclopropyl Cyclobutyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl Isopropoxide, tert-butoxide, N-propylamino, N-isopropyl Amino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino It is , and N,N-dipropylamino.
[0376] In an exemplary embodiment of formula XXIV, R 6 These are hydrogen, hydroxyl, fluoro, and chloro. , amino, lipid, methyl, methoxy, ethyl, propyl, isopropyl, butyl, s- Chil, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pinch 4-Heptyl, Cyclopropyl, Cyclobutyl, Cyclop Nthyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, isopropoxide, t ert-butoxide, N-propylamino, N-isopropylamino, N-tert-butoxide Tylamino, N,N-dimethylamino, N,N-diethylamino, and N,N-dipropylamino It is pyramino.
[0377] In an exemplary embodiment of formula XXIV, R 7 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0378] In an exemplary embodiment of formula XXIV, R 8 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0379] In an exemplary embodiment of formula XXIV, R 9 methyl, ethyl, propyl, isopropyl Lu, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neope Pentyl, 3-pentyl, hexyl, t-hexyl, 4-heptyl, cyclopropyl, cyclo Robyl, cyclopentyl, cyclohexyl, phenyl, 2,6-dimethylphenyl, i Sopropoxide, tert-butoxide, N-propylamino, N-isopropylamino N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, It is also known as N,N-dipropylamino.
[0380] In certain embodiments, this disclosure relates to compounds of formula XXV,
[0381] [ka]
[0382] or relating to its pharmaceutical or physiological salt, in the formula, R 1 teeth,
[0383] [ka] TIFF2026062641000107.tif207170TIFF2026062641000108.tif78170
[0384] Optionally substituted esters, optionally substituted branched esters, optional Carbonates substituted with, carbamates optionally substituted with, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted Thiocarbonate, optionally substituted S-thiocarbonate, optionally substituted Dithiocarbonates, optionally substituted thiocarbamates, optionally substituted Oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl L, optionally substituted oxymethylcarbonyl, optionally substituted oxymethyl Tylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino a...
Claims
1. Pharmaceutical compositions in the manufacture of pharmaceuticals for the treatment or prevention of viral infections in a subject The use is such that the composition comprises a pharmaceutically acceptable excipient and a compound of formula XXVIII. or its pharmaceutical or physiological salt, 【Chemistry 1】 During the ceremony, R 1 teeth, 【Chemistry 2】 And R 6 This is one or more identical or different Rs chosen at will. 10 The aryl that was replaced by And, R 2 and R 3 Each of these is one or more R 10 It is an alkoxy substituted with, R 10 These are independently deuterium, hydroxyl, azide, thiol, amino, cyano, and halo Gen, alkyl, alkenyl, alkynyl, carbocyclyl, heterocarbocyclyl, A Riesl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alco Xy, carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryl oxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamine No, (alkyl) 2 Amino, carbocycloamino, heterocarbocycloamino, aryl Amino, heteroarylamino, heterocycloamino, cycloalcamino, cycloalchem Namino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio O, heteroarylthio, heterocyclilthio, cycloalkylthio, cycloalkenyl Thio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipids, nitro, and cal Selected from Bonil, The lipid is C 11 to C 22 higher alkyl, C 11 to C 22 higher alkoxy, polyethylene Glycols, or alkyl-substituted aryls, or lipids as described herein. It is used.
2. R 6 This is one or more identical or different Rs chosen at will. 10 It is an aryl that has been replaced by , R 6 Substituted R in 10 These are independently hydroxy, halogen, alkyl, and aldehyde. Coxy, alkylamino, and (alkyl) 2 Selected from amino acids, according to claim 1 use.
3. R 6 is one R 10 Replaced with R 6 Substituted R in 10 It is a halogen. , the use described in claim 2.
4. R 2 and R 3 is one R 10 Replaced with R 2 and R 3 Substituted R in 10 teeth The use according to any one of claims 1 to 3, wherein the carbonyl group is used.
5. The aforementioned viral infections belong to the Togaviridae, Coronaviridae, and Orthomyxoviridae families. Pneumoviridae, Arenaviridae, Bunyaviridae, or Picornaviridae The use according to any one of claims 1 to 4, caused by the virus 。
6. The aforementioned viruses include Eastern Equine Encephalitis Virus, Western Equine Encephalitis Virus, and Venezuelan Equine Encephalitis Virus. Viruses, Chikungunya virus, Ross River virus, Human coronavirus, SARS Coronavirus, MERS coronavirus, influenza A virus, influenza The virus type B, RSV, Takaribe virus, Pichinde virus, Funin virus, Rash Fever Scab virus, lymphocytic choriomeningitis virus, Rift Valley fever virus, Punta Toro Viruses, Lacrosse virus, Maporal virus, Heartland virus, severe fever blood Thrombocytopenia syndrome virus, poliovirus, coxsackievirus, and enterovirus A use according to any one of claims 1 to 5, selected from S.