The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo- 1,2,3,4-tetrahydrothieno [3 ,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.

The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I:

##STR00001##

wherein W, X, Y, Z, R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are as described herein.

The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscinsmitochondrial-based therapeutic compounds having anti-cancer and antibiotic propertiesto prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.

The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscinsmitochondrial-based therapeutic compounds having anti-cancer and antibiotic propertiesto prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.

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.

The present invention provides for compounds of formula (I)

##STR00001##

wherein R.sup.x, R.sup.y, R.sup.x1, L.sup.1, G.sup.1, A.sup.1, A.sup.2, A.sup.3, and A.sup.4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Provided herein are soluble adenylyl cyclase (sAC) inhibitors and uses thereof. In one aspect, provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, and pharmaceutical compositions thereof. The compounds provided herein are soluble adenylyl cyclase (sAC) inhibitors and are therefore useful for the treatment and/or prevention of various diseases and conditions (e.g., ocular conditions (e.g., ocular hypotony), liver diseases (e.g., non-alcoholic steatohepatitis (NASH)), inflammatory diseases, autoimmune diseases (e.g., psoriasis)). Compounds provided herein are also useful as contraceptive agents (e.g., for male and female contraception).

##STR00001##

Provided herein are soluble adenylyl cyclase (sAC) inhibitors and uses thereof. In one aspect, provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, and pharmaceutical compositions thereof. The compounds provided herein are soluble adenylyl cyclase (sAC) inhibitors and are therefore useful for the treatment and/or prevention of various diseases and conditions (e.g., ocular conditions (e.g., ocular hypotony), liver diseases (e.g., non-alcoholic steatohepatitis (NASH)), inflammatory diseases, autoimmune diseases (e.g., psoriasis)). Compounds provided herein are also useful as contraceptive agents (e.g., for male and female contraception).

##STR00001##

An antibody-conjugated nanoparticle, 50 to 1000 nm in size, containing an anti-Mullerian hormone receptor II (AMHRII) antibody that is conjugated to a nanocomplex formed of a lipid-based delivery agent and a cytotoxin, the delivery agent and the cytotoxin being non-covalently bonded to each other. Also disclosed are a method of preparing such an antibody-conjugated nanoparticle and use thereof for inducing sterilization in a subject and for treating an AMHRII-associated condition.