Patent classifications
C07D303/48
METHOD FOR PREPARING A TETRAFLUORO-1,2-EPOXYPROPANE
A method for preparing atetrafluoro-1,2-epoxypropane comprising reacting a 2-bromo-tetrafluoropropan-3-ol with an alkaline or alkaline earth metal hydroxide solution, a compound which is 2,3,3,3-tetrafluoro-1,2-epoxypropane, and partially fluorinated polyethers of formula [OCRR.sub.1CR.sub.2R.sub.3].sub.n wherein n is from 5 to 100, R is F or H, R.sub.1 is CF.sub.3, R.sub.2 is F or H and R.sub.3 is H.
Cysteine protease inhibitors and uses thereof
The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
Cysteine protease inhibitors and uses thereof
The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
2,3-epoxy succinyl derivative, preparation method and use thereof
The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma. ##STR00001##
2,3-epoxy succinyl derivative, preparation method and use thereof
The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma. ##STR00001##
TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF
The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF
The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
PROCESSES FOR PREPARING PARTIALLY FLUORINATED EPOXIDES AND PERFLUORINATED EPOXIDES AND COMPOSITIONS RELATED THERETO
This application relates to the preparation of partially fluorinated epoxides and perfluorinated epoxides which may be useful in various applications including refrigerants, heat transfer media, high-temperature heat pumps, organic Rankine cycles, fire extinguishing/fire suppression, propellants, foam blowing, solvents, gaseous dielectrics, and/or cleaning fluids. Compositions comprising the fluorinated epoxide compounds are also provided.
PROCESSES FOR PREPARING PARTIALLY FLUORINATED EPOXIDES AND PERFLUORINATED EPOXIDES AND COMPOSITIONS RELATED THERETO
This application relates to the preparation of partially fluorinated epoxides and perfluorinated epoxides which may be useful in various applications including refrigerants, heat transfer media, high-temperature heat pumps, organic Rankine cycles, fire extinguishing/fire suppression, propellants, foam blowing, solvents, gaseous dielectrics, and/or cleaning fluids. Compositions comprising the fluorinated epoxide compounds are also provided.