22 results about "Steroids Receptors" patented technology

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.

Small molecule stimulators of steroid receptor coactivator-3 (SRC-3) and methods of their use as cardioprotective agents are provided. The small molecule stimulators are useful for promoting cardiac protection and repair and vascular regeneration after myocardial infarction. The compounds are also useful in preventing cardiac hypertrophy and collagen deposition and improving cardiac post-infarction function.

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

A compound having chemical structural formula I:where R1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof, and / or a pharmaceutically acceptable salt thereof; where R4′ is H or an alkoxy group; where both R5 and R3′ are OH, and where one or both OH groups is modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof, wherein the prodrug form thereof comprises an ester selected from: an amino acid ester, a phosphate ester, and a sulfonate ester.

The invention relates to a pyran compound as shown in a formula (I), and an isotope form, a stereoisomer, a tautomer, a cis-trans-isomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a hydrate, a prodrug and a polymorphic substance of the pyran compound. The compound shows high inhibitory activity and high selectivity, so that the compound has a good application prospect in the aspect of preparing medicines for treating steroid receptor dependent diseases.

The present invention relates to a compound of formula (I) wherein A, B, R1, R2, R3, R4 and R5 are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, for example androgen receptor or estrogen receptor, dependent diseases and conditions, such as cancer including prostate cancer and breast cancer.

The present invention relates to pyran derivatives as CYP11A1 inhibitors. More specifically, the present invention relates to therapeutically active compounds for the treatment of steroid receptor, in particular androgen receptor (AR), dependent disorders and diseases and pharmaceutical compositions comprising such compounds.

Provided herein are methods of modulating cellular stress pathways using small molecule steroid receptor coactivators (SRC) stimulators. A method of repairing tissue in a subject comprises administering to the subject an effective amount of a pharmaceutical composition comprising a compound as described herein. Methods of protecting tissue adjacent to an injury site or reducing tissue loss in a subject, preserving insulin production and preventing diabetes in a subject, and / or inhibiting kidney fibrosis in a subject are further provided herein.

Small molecule stimulators of steroid receptor coactivator-3 (SRC-3) and methods for their use as cardioprotectants are provided. Small molecule stimulators can be used to promote cardioprotection and repair and angiogenesis after myocardial infarction. The compounds can also be used to prevent cardiac hypertrophy and collagen deposition and improve function after myocardial infarction.

The present invention provides in vitro test kits, assays and methods useful for screening for the presence of a ligand in a test sample, the ligand being characterized by its ability, when in a cell, to form a complex with a steroid hormone receptor and cause a genomic response. Advantageously, the activity-based assays that form the basis of the test kits and methods described herein are particularly suitable for detecting the presence of ligands of unknown structure, such as designer drugs used by equine, canine and human athletes in sports doping. Different assay prototypes are disclosed, in which, for example, through the activation of a reporter, hormone receptor activation caused by ligand binding interactions can be detected. In certain instances, the present invention provides test kits, assays and methods involving aptamer:fluorophore reporter constructs for detecting ligands in samples (e.g., collected from athletes at the side of a race track).

The present invention provides novel compounds of formula (I) as CYP11A1 inhibitors, useful for the treatment of symptoms and diseases affected by steroid hormone receptors, such as symptoms and diseases dependent on androgen receptor (AR), including prostate cancer. The invention also discloses a preparation method, a pharmaceutical composition and application thereof.

The disclosure relates to fusion proteins comprising a tBID polypeptide and a steroid hormone receptor domain, and methods of using same to induce apoptosis in cells.

A method of neutralizing or mitigating a drug-induced mitochondrial dysfunction or impairment for an individual, the method including providing to the individual an effective amount of a composition containing glycine or a functional derivative thereof and N-acetylcysteine or a functional derivative thereof. The drug-induced mitochondrial dysfunction or impairment is from at least one drug consumed by the individual selected from the group consisting of an anticonvulsant; a psychotropic other than an antipsychotic drug; an analgesic / anti-inflammatory drug other than acetaminophen; an antibiotic; an anti-arrhythmic drug; a steroid; a beta-blocker; and an immunization.

In some embodiments, the present disclosure provides steroid hormone receptor ligand binding peptides comprising at least 6 contiguous amino acid residues found within the carboxy terminal receptor binding domain of the PRAC1 protein. Methods for the use of the peptides and their derivatives, pharmaceutical compositions comprising the peptides and their derivatives in treating a steroid hormone driven cancer and inhibiting the interaction between the steroid hormone receptor, its co-factors, and its ligand are also provided. Additionally, provided herein is a method of overcoming resistance or restoring sensitivity to a therapy targeting the androgen receptor signaling axis in a subject suffering from a steroid hormone driven cancer.

A pharmaceutical composition, comprising a compound having chemical structural formula I:where R1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and / or a pharmaceutically acceptable salt thereof;where R4′ is H or an alkoxy group; where both R5 and R3′ are OH, and where one or both OH groups is modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof, wherein the prodrug form thereof comprises an ester selected from: an amino acid ester, a phosphate ester, and a sulfonate ester.

Small molecule stimulators of steroid receptor coactivator-3 (SRC-3) and methods of their use as cardioprotective agents are provided. The small molecule stimulators are useful for promoting cardiac protection and repair and vascular regeneration after myocardial infarction. The compounds are also useful in preventing cardiac hypertrophy and collagen deposition and improving cardiac post-infarction function.

The present invention relates to small molecule stimulators of steroid receptor coactivation-3 and methods of their use as cardiac protective agents and / or revascularization agents. Small molecule stimulators of steroid receptor co-activator-3 (SRC-3) and methods of their use as cardiac protective agents are provided. The small molecule stimulant can be used for promoting cardiac protection and repair and vascular regeneration after myocardial infarction. The compounds may also be used to prevent cardiac hypertrophy and collagen deposition and to improve post-cardiac infarction function.

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

The invention discloses a compound shown in a general formula (I), and a stereoisomer, a tautomer, a deuterated derivative or a pharmaceutically acceptable salt thereof. Compared with the prior art, the compound disclosed by the invention is a brand new skeleton, and the compound disclosed by the invention unexpectedly shows that the compound has a good inhibition effect on CYP11A1 and blocks biosynthesis of downstream steroids. Clinically, the pharmaceutical composition can be used for treating diseases dependent on steroid receptors.

There are provided therapeutically active CYP11A1 inhibitor compounds of Formula (I) and pharmaceutical compositions thereof that are useful in the treatment of steroid receptor-dependent conditions and diseases, in particular androgen receptor-dependent conditions and diseases such as endocrine cancer, prostate cancer, castration-resistant prostate cancer, and breast cancer.

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

A method for treating a subject having a retinal eye condition that is refractory to anti-VEGF treatments is disclosed. The method comprises administering a therapeutically effective amount of one or more steroids subsequent to anti-VEGF treatment, thereby treating the retinal eye condition. Also disclosed is a method for treating a subject having a retinal eye condition that is refractory to anti-VEGF treatments, the method comprising a therapeutically effective amount of one or more compounds capable of modulating an activity of a steroid receptor, subsequent to anti-VEGF treatment. Further disclosed is a method for treating a subject having a retinal eye condition that is refractory to anti-VEGF treatments comprising administering a therapeutically acceptable formulation of a steroid, and at least a second therapeutically active compound in a concentration and dose sufficient to ameliorate the retinal eye condition, subsequent to anti-VEGF treatment.