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1. 发明申请

US20070275961A1 Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine 审中-公开
标题翻译： Triazolo'1，5-A！嘧啶及其在医学中的应用
公开(公告)号：US20070275961A1
公开(公告)日：2007-11-29
申请号：US10558694
申请日：2004-06-02
申请人： Justin Bower , Andrew Cansfield , Allan Jordan , Martin Parratt , Lee Walmsley , Douglas Williamson
发明人： Justin Bower , Andrew Cansfield , Allan Jordan , Martin Parratt , Lee Walmsley , Douglas Williamson
IPC分类号： A61K31/519 , A61K31/496 , A61K31/5377 , A61P17/06 , A61P35/00 , A61P9/00 , C07D413/14 , C07D487/04
CPC分类号： A61K31/519 , C07D487/04
摘要： Compounds of formula (IA) or (AB) are kinase inhibitors, especially of CDK2, and/or PDK1 and/or CHK1: wherein Ring A is an optionally substituted aryl, heteroaryl, carbocyclic or heterocyclic radical, Alk represents an optionally substituted clivaient C1-C6 alkylene radical; n is 0 or 1; Q represents a radical of formula -(Alk1)p-(X),(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring, p, r and s are 0 or 1, and Alk1, Alk2, X, are as described in the specification, and R1 represents a radical 3 4 3 (CYC)k-(Alk3)a-(Y)b-(Alk4)d-B wherein k, a, b and d are 0 or 1, and Cyc, Alk3, Alk4 and B are as described in the specification.
摘要翻译：式（IA）或（AB）的化合物是激酶抑制剂，特别是CDK2和/或PDK1和/或CHK1的激酶抑制剂：其中环A是任选取代的芳基，杂芳基，碳环或杂环基，Alk表示任选取代的亲水性C C 1 -C 6亚烷基; n为0或1; Q表示式 - （Alk-1）对 - （X），（Alk 2 O 3）-SZ的基团，其中以任何相容的组合 Z是氢或任选取代的碳环或杂环，p，r和s是0或1，并且Alk 1，Alk 2 X，如规格，R 1表示基团3 4 3（CYC）3 - （烷基）（Y）b - 其中k，a，b和d分别为0或1，并且Cyc，Alk 3号，3号，4号和B号如说明书中所述。

2. 发明申请

US20070179161A1 Pyrazolopyrimidine compounds and their use in medicine 审中-公开
公开(公告)号：US20070179161A1
公开(公告)日：2007-08-02
申请号：US10551177
申请日：2004-03-18
申请人： Martin Parratt , Justin Bower , Douglas Williamson , Andrew Cansfield
发明人： Martin Parratt , Justin Bower , Douglas Williamson , Andrew Cansfield
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , A61K31/519
摘要： Compounds of formula (I) or salts, N-oxides, hydrates or solvates thereof are inhibitors of kinase activity, and useful for the treatment of, for example, cancer, psoriasis or restenosis: wherein ring A is an optionally substituted carbocyclic or heterocyclic radical. Alk represents an optionally substituted divalent C1-C6 alkylene radical. n is 0 or 1. Q represents a radical of formula -(Alk1)p (X)r-(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring; Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene radicals which may contain a —O—, —S— or —NRA— link, wherein RA is hydrogen or C1-C6 alkyl; X represents —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —SO—, —C(═O)O—, —OC(═O)—, —C(═O)NRA—, —NR AC(═O)—, —C(═S)NRA, —NRAC(═S)—, —SO2NRA—, —NRASO2—, —OC(═O)NRA—, —NRAC(═O)O—, or —NRA— wherein RA is hydrogen or C1-C6 alkyl. p, r and s are independently 0 or 1. R1 represents a radical -(Alk3)a-(Y)b-(Alk4)d-B wherein a, b and d are independently 0 or 1; Alk3 and Alk4 are optionally substituted divalent C,-C3 alkylene radicals; Y represents a monocyclic divalent carbocyclic or heterocyclic radical having from 5 to 8 ring atoms, —O—, —S—, or —NRA— wherein RA is hydrogen or C1-C6 alkyl; B represents hydrogen or halo, or an optionally substituted monocyclic carbocyclic or heterocyclic ring having from 5 to 8 ring atoms, or in the case where Y is —NRA— and b is 1, then RA and the radical -(Alk4)d-B taken together with the nitrogen to which they are attached may form an optionally substituted heterocyclic ring. R represents hydrogen, halo, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, phenyl, benzyl, cycloalkyl with 3 to 6 ring atoms, or a monocyclic heterocyclic group having 5 or 6 ring atoms.

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