Allergan, Inc.

Jose L Martos

David Frederick Woodward

Jenny W Wang

Jussi J Kangasmetsa

William Robert Carling

Steven Dabbs

Simon Neil Pettit

Hans G Fliri

Clive L Cornell

Ming Ni

William C Carling

David F Woodward

The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R, R, R, RA, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response

Compounds, processes for their preparation, pharmaceutical compositions containing such compounds and their use in treating therapeutic conditions, in particular conditions mediated by the action of ligands on the FP, DP, EP, EP, IP, DP, FP and TP prostaglandin (PG) receptors thereby providing a general anti-inflammatory response.

Antagonists acting at multiple prostaglandin receptors for the treatment of inflammation

The present invention provides a compound, that is wherein Y, W, Z, R1, R2, R4, R5 and R6 are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula 

Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula 

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein Ris selected from the group consisting of CORand CON(R)SORwherein R, R, R, R, and Rare as defined in the specification. The compounds may be administered to treat DP, FP, EP, EP, TP and/or EPreceptor mediated diseases or conditions.

The present invention provides a compound that is represented by the following general formula wherein R, R, R, R, R, R, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.

The present invention provides a method for treating inflammation in a patient in need thereof comprising administering to said patient an effective amount of a compound according to formula wherein R is H or lower alkyl, R1 is hydrocarbyl or substituted hydrocarbyl and the broken line represents a saturated or unsaturated bond, i.e a double bond. Preferably, R1 is an alkyl. More preferably, R1 is a n-alkyl or a cycloalkyl-n-alkyl, e.g. a cyclohexyl-n-alkyl, e.g. n-octyl, n-nonyl or cyclohexyl-n-butyl radical and prodrugs, isomers and pharmaceutically acceptable salts thereof.

Inhibition of inflammation by simultaneous blockade of multiple prostanoid receptors

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfon-amido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein Ris selected from the group consisting of CORand CON(R)SORwherein R, R, R, R, and Rare as defined in the specification. The compounds may be administered to treat DP, FP, EP, EP, TP and/or EPreceptor mediated diseases or conditions. 

Growing community of inventors

Basildon Essex, United Kingdom

Jose L Martos