Glaxosmithkline Intellectual Property Development Limited

Seble Lemma

Panayiotis Alexandrou Procopiou

Niall Andrew Anderson

John Martin Pritchard

Ashley Paul Hancock

Matthew Howard James Campbell-Crawford

Simon John Fawcett MacDonald

Ian B Campbell

Stephen Swanson

Steven Leslie Sollis

Simon John Fawcett Macdonald

Ian Baxter Campbell

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) 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

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Stevenage, United Kingdom

Seble Lemma