Glaxosmithkline Intellectual Property Development Limited

Glaxo Group Limited

John Martin Pritchard

John Liddle

Panayiotis Alexandrou Procopiou

Paul Bamborough

Ian B Campbell

Michael David Barker

Niall Andrew Anderson

Ashley Paul Hancock

Matthew Howard James Campbell-Crawford

Seble Lemma

Simon John Fawcett MacDonald

Brendan John Fallon

Stephen Swanson

Jeremy John Payne

Caroline Whitworth

Richard Peter Charles Cousins

Sebastien Andre Campos

Joanna Mary Redmond

Steven Leslie Sollis

Daniel Terence Tape

Heather Hobbs

Paul Faulder

Simon Peace

Duncan Stuart Holmes

Robert Charles Wheeler

Simon John Fawcett Macdonald

Ian Baxter Campbell

Michael John Johnston

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 

Naphthyridine derivatives useful as alpha-V-beta-6 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.

[object Object]

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 of formula (I) or a salt thereof whereinRrepresents a hydrogen atom, a methyl group or a ethyl groupRrepresents a hydrogen atom or a fluorine atomRrepresents a hydrogen atom, a methyl group or an ethyl group.

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 compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.

Growing community of inventors

Stevenage, United Kingdom

John Martin Pritchard