C07D211/72

NK1 ANTAGONISTS

A NK.sub.1 antagonist having the formula (I),

##STR00001##

wherein Ar.sup.1 and Ar.sup.2 are optionally substituted phenyl or heteroaryl, X.sup.1 is an ether, thio or imino linkage, R.sup.4 and R.sup.5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

Synthesis of 2-carboxamide cycloamino urea derivatives

Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.

Cyclohexene derivative, preparation method therefor, and pharmaceutical composition for preventing or treating metabolic diseases, containing same as active ingredient

The present invention relates to: a cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.

Trientine prodrugs, pharmaceutical compositions thereof, and methods of use
09738620 · 2017-08-22 · ·

Trientine prodrugs, pharmaceutical compositions comprising the trientine prodrugs, and methods of using trientine prodrugs and pharmaceutical compositions thereof for treating Wilson's disease.

Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof

Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.

NK1 antagonists

A NK.sub.1 antagonist having the formula (I), ##STR00001##
wherein Ar.sup.1 and Ar.sup.2 are optionally substituted phenyl or heteroaryl, X.sup.1 is an ether, thio or imino linkage, R.sup.4 and R.sup.5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

NK1 antagonists

A NK.sub.1 antagonist having the formula (I), ##STR00001##
wherein Ar.sup.1 and Ar.sup.2 are optionally substituted phenyl or heteroaryl, X.sup.1 is an ether, thio or imino linkage, R.sup.4 and R.sup.5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

METHOD FOR MANUFACTURING 3-(ALKYLSULFONYL)PYRIDINE-2-CARBOXYLIC ACID

A 3-(alkylsulfonyl)pyridine-2-carboxylic acid or a salt thereof can be manufactured by comprising: a step of allowing a compound represented by formula (1-N):

##STR00001## (wherein X represents a halogen atom) to react with a compound represented by formula (2):


R.sup.2SM.sup.2(2) (wherein R.sup.2 represents a C.sub.1-8 straight-chain alkyl group, and M.sup.2 represents a hydrogen atom or an alkali metal) to give a compound represented by formula (3-N):

##STR00002## (wherein R.sup.2 and X are as defined above); a step of allowing the compound represented by formula (3-N) to react with hydrogen peroxide in the presence of a tungsten catalyst and an acid to give a compound represented by formula (6-N):

##STR00003## (wherein R.sup.2 and X are as defined above); a step of reducing the compound represented by formula (6-N) in the presence of a base and a heterogeneous transition metal catalyst to give a compound represented by formula (8-N):

##STR00004## (wherein R.sup.2 is as defined above); and a step of hydrolyzing the compound represented by formula (8-N) in the presence of a base to give a compound represented by formula (7) or a salt thereof:

##STR00005## (wherein R.sup.2 is as defined above).

Class of HDAC inhibitors expands the renal progenitor cells population and improves the rate of recovery from acute kidney injury

Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.

N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides

The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) ##STR00001## in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, n have the meanings given in the descriptionto their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.