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    • 36. 发明申请
      US20050113566A1 Inhibitors of C-FMS kinase 审中-公开
    • Inhibitors of C-FMS kinase
    • US20050113566A1
    • 2005-05-26
    • US10970903
    • 2004-10-22
    • Mark Player , Nand Baindur , Benjamin Brandt , Naresh Chadha , Raymond Patch , Davoud Asgari , Taxiarchis Georgiadis
    • Mark Player , Nand Baindur , Benjamin Brandt , Naresh Chadha , Raymond Patch , Davoud Asgari , Taxiarchis Georgiadis
    • A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , C07D223/12 , C07D265/30 , C07D279/12 , C07D307/68 , C07D405/12 , C07D409/12
    • C07D405/12 , C07D307/68 , C07D409/12
    • The invention relates to compounds of Formula I: wherein A is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —CORA, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; or a 5- to 7-membered mono- or a 8- to 10-membered bicyclic heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with one or more of -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; R1 is —H, aryl, —CORa, —CORa, —COORa, —CONRaRb, —SO2Ra or —SO2NRaRb; X is —CO—, —C(═NH)—, —CS—, —CON(Ra)—, —CS(NRa)—, —SO2— or —CRaRb—; Y is —S—, —SO—, —SO2—, —O— or direct link; R2 is alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, each of which may be optionally substituted with one or more halogens; and W is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of C1-4 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, halogen, hydroxy, —CF3, alkoxy, aryloxy, arylalkoxy, —OCF3, —CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —NHCORaRb, —NHSO2Ra, —NO2, —SORa, —SO3Ra or —SO2NRaRb; or a 5- to 6-membered mono- or a 8- to 10-membered bicyclic heterocyclic or heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —OCO-alkylamino, —OCO-alkylamido, CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 37. 发明授权
      US5646285A Combinatorial non-peptide libraries 失效
    • Combinatorial non-peptide libraries
    • 组合非肽库
    • US5646285A
    • 1997-07-08
    • US483496
    • 1995-06-07
    • Nand Baindur , Virender M. Labroo
    • Nand Baindur , Virender M. Labroo
    • C07B61/00 , C07K1/00 , C07D207/04 , C07D211/06
    • C40B50/14 , C07D207/04 , C07D211/06 , C07K1/00 , Y02P20/55
    • The present invention relates to an orthogonally-protected compound of the formula: ##STR1## wherein PG.sub.1 is a first protecting group that is unreactive to a chemistry used at another position within the compound, and that is capable of selective removal without affecting PG.sub.2 or linkage to a solid support; PG.sub.2 is a second protecting group that is unreactive to a chemistry used at another position within the compound, and that is capable of selective removal without affecting PG.sub.1 or linkage to a solid support; Y is CH.sub.2 COOH, CH.sub.2 SO.sub.2 OH, CH.sub.2 PO.sub.2 ROH, CH.sub.2 Ph--COOH, CH.sub.2 Ph--SO.sub.2 OH, or CH.sub.2 Ph--PO.sub.2 ROH; R is H or a substituted or unsubstituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and n is 1 or 2. PG.sub.1 is preferably a carbamate group, a trityl group, or a trifluoroacetyl group; and PG.sub.2 is preferably an ester.
    • 本发明涉及具有下式的正交保护的化合物：其中PG1是对化合物中另一位置使用的化学物质不起反应的第一保护基，并且能够在没有 影响PG2或与固体支持物的连接; PG2是与在化合物中另一位置使用的化学物质不反应的第二保护基团，并且能够选择性去除而不影响PG1或与固体支持物的连接; Y是CH 2 COOH，CH 2 SO 2 OH，CH 2 PO2ROH，CH 2 Ph-COOH，CH 2 Ph-SO 2 OH或CH 2 Ph-PO 2 ROH; R是H或取代或未取代的烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基; 并且n为1或2.PG1优选为氨基甲酸酯基，三苯甲基或三氟乙酰基; PG2优选为酯。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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