Abstract: The present invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4, R5, R6, R7, R8 and m are as defined herein, pharmaceutical compositions comprising these compounds and methods of use of these compounds for treating a TGR5 mediated disease or condition.

Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.

Abstract: Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ?CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n; R12 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH3]COOCH3, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)

Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Abstract: The present invention relates to a composition for preventing or treating renal diseases. The composition of the present invention improves lipid metabolism, prevents histological damage including renal fibrosis, alleviates microalbuminuria, and maintains nephrons of renal glomeruli. Therefore, the composition is useful for treating renal diseases.

Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Abstract: The present disclosure is generally directed to neuroactive 13, 17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause or for fertility control and emergency contraception.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

Abstract: Formulations and methods for providing progestin-only contraception to a woman while minimizing various side effects, such as breakthrough bleeding, that are normally associated with progestin-only contraception are disclosed and described. In one aspect, the method can include transdermally administering a formulation having a contraceptively effective amount of a single progestin as the sole active hormonal agent to the woman as part of a contraceptive regimen.

Abstract: A double conjugate molecule made of a retinoid, an organic acid, particularly an a-hydroxy acid, and an alcohol or acyl group, is provided which is useful in treating skin conditions, particularly aging. The retinoid, organic acid, and alcohol/acyl group are preferably linked via ester bonds.

Abstract: The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.