Glaxosmithkline Intellectual Property Development Limited

Glaxo Group Limited

Ashley Paul Hancock

Niall Andrew Anderson

John Martin Pritchard

Matthew Howard James Campbell-Crawford

Panayiotis Alexandrou Procopiou

Seble Lemma

Simon John Fawcett MacDonald

Joanna Mary Redmond

Ian B Campbell

Stephen Andrew Thomson

Stephen Swanson

Simon Teanby Hodgson

Sadie Vile

Paul Martin Gore

Steven Leslie Sollis

Eugene L Stewart

Barry George Shearer

Emilie Despagnet Smith

Yu Guo

David Norman Deaton

Christie Schulte

A compound of formula (I) wherein R, R, R, R, Y, Y, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

1,3 di-substituted cyclobutane or azetidine derivatives as hematopoietic prostaglandin D synthase inhibitors

A compound of formula (I) or a salt thereof: wherein Rrepresents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected from a hydrogen atom, a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when Rrepresents an N-linked mono- or di-substituted pyrazole, Rdoes not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.

Naphthyridine derivatives as alpha V beta 6 integrin antagonists for the treatment of E.G. fibrotic diseases

The invention relates to compounds of Formula (I): wherein R, Rand Rare as defined in the description and claims, or pharmaceutically acceptable salts thereof, having &#x3b1;&#x3b2;integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an &#x3b1;&#x3b2;integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.

Naphthyridines as integrin antagonists

A compound of formula (I): being 4-(3-Fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl) ethyl) pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy) phenyl) butanoic acid, or a salt thereof.

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A compound of formula (I) or a salt thereof: wherein Rrepresents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when Rrepresents an N-linked mono- or di-substituted pyrazole, Rdoes not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.

Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of E.G. fibrotic diseases

A compound according to formula (I) wherein Ris hydrogen, cyclopropyl, or pyrazolyl, wherein said pyrazolyl is optionally substituted by one or two methyl groups; or a pharmaceutically acceptable salt thereof.

Compounds alpha v beta 6 integrin antagonists

A compound of formula (I): wherein R is H or F; or a salt thereof.

A compound of formula (I): which is 4-(3-fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl)butanoic acid, or a salt thereof.

The present invention relates to a compound which is N-(4-{4-[(6-butyl-8-quinolinyl)oxy]-1-piperidinyl}butyl)ethanesulfonamide and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various diseases, such as allergic rhinitis.

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Auburn Hills, MI, United States of America

Ashley Paul Hancock