Glaxosmithkline Intellectual Property Development Limited

Niall Andrew Anderson

John Martin Pritchard

Ashley Paul Hancock

Matthew Howard James Campbell-Crawford

Gemma Victoria White

Panayiotis Alexandrou Procopiou

Seble Lemma

Philip Anthony Harris

Alain Claude-Marie Daugan

Clark A Sehon

Bryan Wayne King

Simon John Fawcett MacDonald

Jae U Jeong

Patrick M Eidam

Deepak Bandyopadhyay

Frederic G Donche

David Duff Wisnoski

Nicolas S George

Nicolas Eric Faucher

Joanna Mary Redmond

Julie Nicole Hamblin

Andrew Sharpe

Vipulkumar Kantibhai Patel

Ian B Campbell

Anthony William James Cooper

Graham George Adam Inglis

Kenneth David Down

Sebastien Andre Campos

Simon Peace

Nicholas Paul Barton

Edward Paul Cannons

Brendan John Fallon

Armelle Le Gall

Stephen Swanson

Steven Leslie Sollis

Ian Baxter Campbell

Simon John Fawcett Macdonald

Disclosed are compounds having the formula: 

Heterocyclic amides as kinase inhibitors

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Chemical compounds

Disclosed are compounds having the formula (I): 

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.

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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 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.

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Stevenage, United Kingdom

Niall Andrew Anderson