Glaxo Group Limited

Paul William Smith

Ian Thomson Forbes

David G Cooper

Jian Jin

Brian W Budzik

Dongchuan Shi

Graham Walker

Vincenzo Garzya

Alan D Borthwick

Andrew McMurtrie Mason

Nigel Stephen Watson

Chuen Chan

Simon Edward Ward

Henry Anderson Kelly

Robert John Young

Nigel Paul King

Matthew Campbell

Stefan Senger

Savvas Kleanthous

Frank P Harrington

David Gwyn Cooper

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.

Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; b is 1, 2 or 3 and c is 1, 2 or 3, wherein b+c is 2, 3, 4 or 5; X is carbon, Y is CH, is a double bond and e is 0; or X is carbon, Y is CHor oxygen, is a single bond and e is 1; or X is nitrogen, Y is CH, is a single bond and e is 0; R1 is hydrogen, cyano, halogen, Calkyl, Calkoxy, CalkoxyCalkyl, NHCOCHor OCONR5R6, wherein R5 and R6 are independently hydrogen or Calkyl; R2 is halogen, cyano or Calkoxy; d is 0, 1, 2 or 3; R3 is hydrogen, Calkyl, Calkanoyl, fluoroCalkanoyl, Calkylsulfonyl, fluoroCalkylsulfonyl, carbamoyl, Calkylcarbamoyl or arylCalkyl; and R4, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring, provided that when a compound of formula (I) has the following structure: wherein A, b, c, R1, e, X, Y, R2 and d are as defined above and R3 is hydrogen, Calkyl or arylCalkyl, then (i) X is carbon, Y is CH and is a double bond; or (ii) b and c are both 1; or (iii) the carbon atom adjacent to the oxo-substituted carbon atom in the morpholinyl ring, marked '&#x2605;', is substituted. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same. 

2-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors

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Harlow, United Kingdom

Paul William Smith