11 results about "Oestrogen receptor" patented technology

Disclosed herein are compounds of Formula (I) or pharmaceutically acceptable salts thereof: wherein R1 and R2 independently represent a hydrogen atom or a deuterium atom; r3'and R3 ''independently represent a hydrogen atom, a methyl group, a methoxyl group, a chlorine atom, a fluorine atom, or a cyano group; r4 represents a hydrogen atom or a fluorine atom; r5 and R5'independently represent a hydrogen atom or a fluorine atom; y represents-CH2-,-CH =,-CR9 =,-O-or-NH-wherein R9 represents a fluorine atom or a (C1-C3) alkyl group; represents a single bond or a double bond; p is 0 or 1; x represents-CH =,-N = or-CR ''= wherein R'' represents a (C1-C3) alkyl or halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; r7 independently represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; n is 0, 1 or 2; and R6 represents a (C1-C6) alkyl group, said alkyl group being optionally substituted; r8 represents a hydrogen atom, a (C1-C3) alkyl group, a-CH2F group, a-CHF2 group, a-CF3 group, or a (C3-C4) cycloalkyl group. Further disclosed are processes for preparing the same, pharmaceutical compositions comprising the same and the compounds of formula (I) for use as inhibitors and degrading agents of estrogen receptors, in particular for use in the treatment of ovulation dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hyperplasia or inflammation. # imgabs0 #

The present application relates to treating and / or preventing breast cancer, including locally advanced or metastatic, ER+, HER2- breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof.

The current invention is in the field of molecular biology / pharmacology and provides novel 3-oxabicyclo[3.3.1]nonene compounds and derivatives that modulate the effects of the classical estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the G protein-coupled estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and / or antagonists of one or more of the disclosed classical estrogen receptors. Diseases that are mediated through one or more of these receptors include cancer (including but not limited to breast (particularly endocrine or anti-hormone resistant, and for the prevention / reduction of endocrine or anti-hormone resistance), reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometritis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders (such as Parkinson's disease and Alzheimer's disease), as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine, among numerous others as described herein. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

The present invention relates to compounds of formula (I) wherein A is a 3-10 membered carbocyclic ring or a 4-12 membered heterocyclic ring containing 1-4 heteroatoms selected from O, N or S; B is any one of the following groups (1), (2) or (3); C is any one of the following groups (1'), (2'), (3') or (4'); G1 is CH2, NH or O; G2 and G3 are independently of each other CH or N; Z is -C(O)-, -SO2-, -C 1‑3 alkyl- or -CH2-C(O)-; L is a bond, -C 1‑7 alkyl- or -C 1‑7 alkenyl-. The compounds of formula (I) are inhibitors of cytochrome P450 monooxygenase 11A1 (CYP11A1). The compounds are useful as medicaments for the treatment of steroid receptor, e.g. androgen receptor or estrogen receptor dependent diseases and disorders such as cancer including prostate cancer and estrogen cancer.

Disclosed are novel compounds for use in treating a proliferative disorder such as a cancer. Further disclosed are compositions comprising the novel compounds. Methods of using the disclosed compounds and compositions are further described. The methods include administering one or more of the disclosed compounds for treatment of various proliferative disorders, including an HRAS-driven cancer, a KRAS-driven cancer, a NRAS-driven cancer, Ewing sarcoma, B-cell acute lymphoblastic leukemia, leukemia, lung cancer, non-small cell lung cancer (NSCLC), solid tumor, breast cancer, triple-negative breast cancer (TNBC), hormone-resistant triple negative breast cancer. Further described are combination therapies in which a novel compound is administered in combination with one or more of a MEK inhibitor, a KRAS G12C inhibitor, or a Selective Estrogen Receptor Degrader (SERD) to an individual in need thereof.

Provided herein are methods of treating diseases, disorders, or conditions including cancers, where the methods comprise administration of Compound 1, or a pharmaceutically acceptable salt thereof, in combination with a CDK inhibitor or a selective estrogen receptor degrader (SERB), as described herein. Such methods may comprise the treatment of cancer, such as breast cancer.

Disclosed herein are compounds having formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 independently represent a hydrogen atom or a deuterium atom; r3 and R3'represent a hydrogen atom or a fluorine atom; r4 represents a hydrogen atom or a fluorine atom; r5 and R5'independently represent a hydrogen atom or a fluorine atom; y represents-CH2-,-CH =,-CR9 =,-O-or-NH-; (AA) represents a single bond or a double bond; p is 0 or 1; x represents-CH =,-N =, or-CR ''=; r6 represents a group selected from the group consisting of phenyl; a fused phenyl group; phenyl fused with a hetero (C4-C6) cyclic hydrocarbon group; a bicyclic group comprising from 5 to 12 carbon atoms; a heteroaryl group; a cyclic hydrocarbon group; (C3-C6) cycloalkyl (C1-C3) alkyl; a 4 to 7 membered heterocyclic hydrocarbon group; (C1-C6) alkyl groups; a (C1-C6) alkenyl group; and a phenyl (C1-C2) alkyl group; r7 independently represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; r8 represents a hydrogen atom or a (C1-C3) alkyl group or cyclopropyl group; and n is 0, 1 or 2. Further disclosed are processes for their preparation, pharmaceutical compositions comprising them and the compounds of formula (I) for use as inhibitors and degradation agents of estrogen receptors, in particular in the treatment of ovulation dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hyperplasia or inflammation. # imgabs0 #

The present invention provides methods for treating and / or preventing breast cancer, including locally advanced or metastatic ER+ and HER2- breast cancers in patients requiring treatment, compounds for use in treatment, and combinations thereof. [Solution] Administer a compound of formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotope derivative thereof, or a prodrug thereof. JPEG2026136114000154.jpg65134

The present application provides a compound, which is an adamantane derivative, comprising a ligand R1 that specifically binds to a target protein (i.e., an estrogen receptor), a ligand R2 that recruits an E3 ubiquitin ligase, and a chemical chain Linker connecting the two parts. Linker is an alkyl chain of varying lengths, wherein the number of carbon atoms in the alkyl chain is n, where 1≤n≤20, and n is an integer; or Linker is a polyethylene glycol chain of varying lengths, wherein the number of oxygen atoms in the polyethylene glycol chain is m, where 1≤m≤5, and m is an integer. The compound provided herein exhibits significant anti-tumor activity through the PROTAC mechanism; in the breast cancer MCF-7 cell line, the proliferation of tumor cells is inhibited by degrading Erα protein, providing a new strategy for the treatment of breast cancer.

The present invention provides a preparation method and application of a class of compounds, relating to the field of pharmaceutical chemistry technology. Such compounds are compounds represented by Formula I, or salts thereof, or stereoisomers thereof, or solvates thereof, or hydrates thereof, or prodrugs thereof. Such compounds can effectively inhibit the proliferation activity of various breast cancer cells, among which triple-negative breast cancer cells and doxorubicin-resistant cells have good proliferation inhibition activity, and can also effectively inhibit their migration; at the same time, such compounds have good estrogen receptor α downregulation activity, showing the application prospects of such compounds in cancer treatment, especially in breast cancer treatment. In addition, studies have found that such compounds have good inhibitory activity against coronaviruses, without obvious toxic side effects, and can be used as a new choice of drugs for the prevention and treatment of coronaviruses.

The present application relates to treating and / or preventing breast cancer, including locally advanced or metastatic, ER+, HER2− breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I),or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, R4, m, and n are defined herein.