C07C2601/02

CYCLOBUTANE CONTAINING CARBOXYLIC ACID GPR120 MODULATORS
20170247311 · 2017-08-31 ·

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

##STR00001##

NOVEL PROCESS FOR THE PREPARATION OF SPIRO[2.5]OCTANE-5,7-DIONE AND SPIRO[3.5]NONANE-6,8-DIONE

This invention relates to methods for the synthesis of spiro[2.5]octane-5, 7-dione and spiro[3.5]nonane-6, 8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.

EBNA1 inhibitors and their method of use

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

Isoprenyl compounds and methods thereof

Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.

Immunoregulatory agents

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Carboxamide compounds

Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides. ##STR00001##

ROR gamma (RORγ) modulators

A.sub.11-14 are N or CR.sub.11-14, respectively, maximum two of the four positions A simultaneously N; R.sub.1 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(1-6)alkylamino, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino, all alkyl and cycloalkyl group carbon atoms optionally substituted with F and F or methyl, respectively; R.sub.2 and R.sub.3 independently H, F, methyl, ethyl, hydroxy, methoxy or R.sub.2 and R.sub.3 together is carbonyl, all present alkyl groups optionally substituted with F; R.sub.4 is H or C(1-6)alkyl; R.sub.5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano; the sulfonyl group with R.sub.1 represented by one of R.sub.7-9; the remaining R.sub.6-14 are independently H, halogen, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl, all alkyl groups optionally substituted with F; and R.sub.15-16 are independently H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano. ##STR00001##

COMPOUNDS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS

The present disclosure relates to compounds of Formula I:

##STR00001## suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein preferably inhibit the CIC-1 ion channel.

PROCESS FOR THE SYNTHESIS OF (+) AND (-)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE
20170233333 · 2017-08-17 ·

The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

Immunomodulator compounds

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): ##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.