发明名称 Phenylalanine enamide derivatives possessing a cyclobutene group, for use as integrin inhibitors
摘要 Phenylalanine enamide derivatives of formula (I) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain -CH2-CH(R)-, -CH=C(R)- or -CH(CH2R)- X is an -N(R2) group; V is an oxygen (O) or sulphur (S) atom; RX and RY are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and RZ represents a halogen atom, or, -L1(Alk1)n(R3)v in which L is a covalent bond or a linker atom or group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain, R3 is a hydrogen or halogen atom or group selected from -OR3a [where R3a is a hydrogen atom or an optionally substituted alkyl or cycloalkyl], SR3a, -CN or an optionally substituted cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaIiphatic, aromatic or heteroaromatic group, n is zero or the integer 1 and v is the integer 1, 2 or 3 provided that when n is zero and L is a covalent bond v is the integer 1; and the salts, solvates, hydrates and N-oxides thereof. Furthermore compounds of formula (I) are able to inhibit the binding of integrins to their ligands and described is the use of compounds of formula (I) for the manufacture of a medicament for the treatment and/or prevention of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.
申请公布号 NZ528134(A) 申请公布日期 2005.09.30
申请号 NZ20020528134 申请日期 2002.01.18
申请人 CELLTECH R&D LIMITED 发明人 BAILEY,STUART;BROWN, JULIEN ALISTAIR;BRAND, STEPHEN;JOHNSON, JAMES ANDREW;PORTER, JOHN ROBERT;HEAD, JOHN CLIFFORD
分类号 A61K31/198;A61K31/4375;A61K31/44;A61K31/4406;A61K31/497;A61P3/10;A61P9/00;A61P17/00;A61P17/06;A61P19/02;A61P25/00;A61P29/00;A61P37/00;A61P37/06;A61P43/00;C07C229/34;C07C229/46;C07C233/82;C07C321/22;C07C323/30;C07D213/81;C07D213/89;C07D401/12;C07D405/12;C07D409/12;C07D413/12;C07D471/04;(IPC1-7):C07D213/81;C07C229/36 主分类号 A61K31/198
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