82 results about "Hormone Receptor Modulators" patented technology

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Compounds of formula (I) or (II)wherein Rx, Rz, R9, R10, R14, R14′, R15, R15′, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

A compound represented by the formula (I)wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R6, R7 and R8,R1 is an electron-withdrawing group,R2, R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,R6 is a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,R7 is a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or R6 and R7 optionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), andR8 is a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, or a salt thereof has a superior action as an androgen receptor modulator, and is useful for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia, osteoporosis and the like.

This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.

This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of nonsteroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.

Methods for treating hormone associated conditions, such as endometriosis, uterine leiomata, ovarian cancer, breast cancer, or vaginal bleeding, using LHRH antagonists and selective estrogen receptor modulators are disclosed. The methods include administering to a subject a combination of an LHRH antagonist and a selective estrogen receptor modulator. Pharmaceutical compositions and kits for use in the methods of the invention are also provided.

The invention relates to an acrylic acid derivative, a preparation method thereof and medical application of the acrylic acid derivative. Particularly, the invention relates to the acrylic acid derivative as shown in a general formula (I) defined in the description, the preparation method thereof, a pharmaceutical composition containing the derivative and application of the derivative serving an estrogen receptor modulator for treating estrogen receptor mediated or dependent diseases or symptoms, and the disease of a breast cancer is particularly preferable. All substituents of the formula (I) are the same as the definition in the description.

The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

The invention relates to a non-steroidal androgen receptor modulator compound containing 1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I), or relative medical acceptable salt and a relative preparation method. The invention also relates to a drug compound of 1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I) and relative medical acceptable salt. The1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I) or relative medical acceptable salt has androgen receptor antagonistic activity, therefore, the compound can be used to prepare the non-steroidal drug for preventing or / treating prostatic hyperplasia, prostate cancer, hirsutism, serious androgen dependence alopecia and acne or the like.

A compound represented by the formula (I)wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R6, R7 and R8,R1 is an electron-withdrawing group,R2, R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,R6 is a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,R7 is a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or R6 and R7 optionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), andR8 is a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, or a salt thereof has a superior action as an androgen receptor modulator, and is useful for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia, osteoporosis and the like.

Triazine derivatives of formula (I), which exhibit pharmacological activity at estrogen receptors alpha (ER alpha) and beta (ER beta) are described herein. The described invention also includes compositions and medicaments containing the triazine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.

This invention provides estrogen receptor modulators of formula: (I), having the structure wherein, R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.

The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as novel non-steroidal selective glucocorticoid receptor modulators for treating a variety of autoimmune and inflammatory diseases or conditions, and possess advantages over steroidal glucocorticoid ligands with respect to undesireable side-effects, efficacy, toxicity and / or metabolism. Pharmaceutical compositions and methods of use are also included.

The invention relates to a non-steroidal androgen receptor modulator containing N-aryl-beta-aromatic amine-propionamide compound (I) and a relative preparation method. The invention also relates to a drug compound containing the N-aryl-beta-aromatic amine-propionamide compound (I). The N-aryl-beta-aromatic amine-propionamide compound (I) has androgen receptor antagonistic activity, therefore, the compound can be used to prepare the non-steroidal drug for preventing or / treating prostatic hyperplasia, prostate cancer, hirsutism, serious androgen dependence alopecia and acne or the like.

The invention belongs to the technical field of medicines, and relates to a phenylindole derivative and application thereof.The phenylindole derivative comprises stereisomer and pharmaceutically-applicable salt of a phenylindole compound and has the structural formula (please see the formula in the description).The phenylindole derivative and the acid-added pharmaceutically-applicable salt of the phenylindole compound can be used in cooperation with existing medicines or used independently as an estrogen receptor regulator for treating or preventing various diseases related to estrogen functions such as bone loss, fractures, bone rarefaction, hectic fever, LDL cholesterol level rise, cardiovascular diseases, cognitive deficits, brain degeneration diseases, anxiety, depression caused by estrogen deficiency, sexual dysfunction, hypertension, retinal degeneration, cancers and especially osteoporosis.

The invention belongs to the technical field of medicine and relates to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and application thereof used as an estrogen receptor, in particular to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and a pharmaceutically acceptable salt, or a stereoisomer thereof and a prodrug as well as a pharmaceutically acceptable vector in compatibility or a diluent used as an estrogen receptor. The structural general formula of the derivative is disclosed in the specification, and in the structural formula, n R1 can be independently selected from a substituted or unsubstituted amido group, and R2 can be independently selected from H or an acetyl group. The derivative can be used for treating and preventing various diseases related to estrogen functions, such as diseases related to estrogen deficiency, estrogen sensitive cancer and hyperplasia, endometriosis, uterus myoma and osteoarthritis. Compounds or compositions of the derivative can also be independently used or combined with progestogen or a hormoneantagonist as a contraceptive.