Glaxo Group Limited

Glaxosmithkline Intellectual Property (no.2) Limited

Venenum Biodesign, LLC

Dongchuan Shi

David G Cooper

Ian Thomson Forbes

Jian Jin

Brian W Budzik

Graham Walker

Vincenzo Garzya

Paul William Smith

Philip D Stein

Brian F McGuinness

Joseph M Karpinski

Jeffrey John Letourneau

Chia-Yu Huang

Kelly M Aubart

Donghui Qin

Xiangmin Liao

James B Hoffman

Andrew B Benowitz

Steven G Kultgen

Andrew G Cole

Jared T Spletstoser

James R Beasley

Yuhong Fang

Andrew Nicholson Knox

David Gwyn Cooper

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. 

Non-systemic TGR5 agonists

The present invention relates to a compound of Formula (I): ora pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.

Peptide deformylase inhibitors

Compounds of formula (I) and salts and solvates are provided: wherein Ris fluoro, Ris selected from hydrogen, halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Calkoxy, and Calkoxy substituted with one or more fluorine atoms; and Ris selected from halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Ccycloalkyl, Ccycloalkyl substituted with one or more fluorine atoms, Calkoxy and Calkoxy substituted with one or more fluorine atoms, and Q is hydrogen or Calkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

Compounds which have activity at M1 receptor and their uses in medicine

Compounds of formula (I) and salts are provided: wherein Ris selected from hydrogen, halogen, Calkyl, Calkyl substituted with one or more fluorine atoms, Ccycloalkyl, Ccycloalkyl substituted with one or more fluorine atoms, Calkoxy, Calkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or Calkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

Benzimidazolones which have activity at M1 receptor

Compounds of formula (I) and salts are provided: wherein Ris selected from halogen, Calkyl, Calkyl substituted with one or more fluorine atoms, Calkoxy, Calkoxy substituted with one or more fluorine atoms, and cyano; Ris selected from halogen, Calkyl, Calkyl substituted with one or more fluorine atoms, Ccycloalkyl, Ccycloalkyl substituted with one or more fluorine atoms, Calkoxy, Calkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or Calkyl. The compounds are Magonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

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Compounds of formula (I) and salts are provided: wherein Ris fluoro, Ris selected from hydrogen, halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Calkoxy, and Calkoxy substituted with one or more fluorine atoms; and Ris selected from halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Ccycloalkyl, Ccycloalkyl substituted with one or more fluorine atoms, Calkoxy and Calkoxy substituted with one or more fluorine atoms, and Q is hydrogen or Calkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

Growing community of inventors

Collegeville, PA, United States of America

Dongchuan Shi