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    Modulators of peroxisome proliferator activated receptors
    1.
    发明授权
    Modulators of peroxisome proliferator activated receptors 失效
    过氧化物酶体增殖物激活受体的调节剂

    公开(公告)号：US06825222B2

    公开(公告)日：2004-11-30

    申请号：US10434425

    申请日：2003-05-07

    申请人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

    发明人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

    IPC分类号： A61K31425

    CPC分类号： C07D413/10 ,  C07D263/32 ,  C07D277/24

    摘要： The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and R6 is H, a C1-C4 alkyl, or an aminoalkyl.

    摘要翻译： 本发明涉及由结构式I表示的化合物及其药学上可接受的盐，溶剂合物和水合物及其制备方法，使用方法和具有由结构式I表示的化合物的药物组合物及其药学上可接受的盐，溶剂化物和水合物： 在结构式Ⅰ中，n为2,3或4; V为O或S; W是O，S或SO 2; R1是H，C1-C4烷基，苯基或三氟甲基; R 2各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基，环烷基，或与它们所连接的苯基一起形成萘基或1 ，2,3,4-四氢萘基; R 3各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基或环烷基; R 4各自独立地为H，C 1 -C 4烷基，芳基或苄基; R5各自独立地为H，取代或未取代的芳基或杂芳基，条件是至少一个R 5为取代或未取代的芳基或取代或未取代的杂芳基; 并且R 6是H，C 1 -C 4烷基或氨基烷基。

    Modulators of peroxisome proliferator activated receptors
    3.
    发明授权
    Modulators of peroxisome proliferator activated receptors 失效
    过氧化物酶体增殖物激活受体的调节剂

    公开(公告)号：US06417212B1

    公开(公告)日：2002-07-09

    申请号：US09644457

    申请日：2000-08-23

    申请人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

    发明人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

    IPC分类号： C07D26336

    CPC分类号： C07D413/10 ,  C07D263/32 ,  C07D277/24

    摘要： The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and R6 is H, a C1-C4 alkyl, or an aminoalkyl.

    摘要翻译： 本发明涉及由结构式I表示的化合物及其药学上可接受的盐，溶剂合物和水合物及其制备方法，使用方法和具有由结构式I表示的化合物的药物组合物及其药学上可接受的盐，溶剂化物和水合物： 在结构式I中，n为2,3或4; V为O或S; W是O，S或SO 2; R1是H，C1-C4烷基，苯基或三氟甲基; R 2各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基，环烷基，或与它们所连接的苯基一起形成萘基或1 ，2,3,4-四氢萘基; R 3各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基或环烷基; R 4各自独立地为H，C 1 -C 4烷基，芳基或苄基; R5各自独立地为H，取代或未取代的芳基或杂芳基，条件是至少一个R 5为取代或未取代的芳基或取代或未取代的杂芳基; 并且R 6是H，C 1 -C 4烷基或氨基烷基。

    1-Carboxylmethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12
    6.
    发明授权
    1-Carboxylmethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12 失效
    可用作MMP-12的选择性抑制剂的1-羧甲基-2-氧代 - 氮杂衍生物

    公开(公告)号：US06770640B1

    公开(公告)日：2004-08-03

    申请号：US09467292

    申请日：1999-12-17

    申请人： Alan M. Warshawsky ,  Michael J. Janusz

    发明人： Alan M. Warshawsky ,  Michael J. Janusz

    IPC分类号： C07D22312

    CPC分类号： C07D403/12 ,  C07D223/12

    摘要： The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selective inhibitors of MMP-12. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

    摘要翻译： 本发明涉及作为基质金属蛋白酶（MMPs）抑制剂的某些新型1-羧甲基-2-氧代 - 氮杂衍生物。 式（1）的化合物特别可用作MMP-12的选择性抑制剂。 本文还要求含有所述化合物的药物组合物以及治疗对基质金属蛋白酶抑制作用的各种疾病状态的方法。

    Carboxyalkyl derivatives useful as inhibitors of enkephalinase and ace
    10.
    发明授权
    Carboxyalkyl derivatives useful as inhibitors of enkephalinase and ace 失效
    可用作脑啡肽酶抑制剂的羧甲基烷基衍生物

    公开(公告)号：US5472959A

    公开(公告)日：1995-12-05

    申请号：US348778

    申请日：1994-12-01

    申请人： Alan M. Warshawsky ,  Gary A. Flynn

    发明人： Alan M. Warshawsky ,  Gary A. Flynn

    IPC分类号： A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61K38/00 ,  A61P7/10 ,  A61P9/00 ,  A61P9/12 ,  A61P25/04 ,  A61P25/28 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D507/00 ,  C07D513/04 ,  C07K5/078

    CPC分类号： C07K5/06139 ,  A61K38/00

    摘要： The invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur, NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group; R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; and n is an integer 1 to 3,that are useful as inhibitors of enkephalinase and ACE.

    摘要翻译： 本发明涉及下式化合物：其中B1和B2各自独立地为氢; 羟基; -OR 2，其中R 2是C 1 -C 4烷基或Ar-Y基团，其中Ar是芳基，Y是氢或C 1 -C 4烷基; 或者其中B1和B2连接到相邻的碳原子上，可以将B1和B2与所述相邻的碳原子一起形成苯环或亚甲二氧基; A是键，亚甲基或氧，硫，NR 4或NCOR 5，其中R 4是氢，C 1 -C 4烷基或Ar-Y-基，R 5是-CF 3，C 1 -C 10烷基或Ar-Y-基团; R3是氢或-CH2OC（O）C（CH3）3; R1是氢，C1-C4烷基或-CH2OC（O）-C（CH3）3; 且n为1〜3的整数，可用作脑啡肽酶和ACE的抑制剂。