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1. 发明申请

WO2006076575B1 SUBSTITUTED BIARYL COMPOUNDS AS FACTOR XIA INHIBITORS 审中-公开
标题翻译：作为因子XIA抑制剂的取代BIARYL化合物
公开(公告)号：WO2006076575B1
公开(公告)日：2006-11-30
申请号：PCT/US2006001224
申请日：2006-01-12
申请人： SQUIBB BRISTOL MYERS CO , CORTE JAMES R , QUAN MIMI L , SMALLHEER JOANNE M , PINTO DONALD J
发明人： CORTE JAMES R , QUAN MIMI L , SMALLHEER JOANNE M , PINTO DONALD J
IPC分类号： A61P7/02 , C07C237/24 , C07D261/20
CPC分类号： C07C255/44 , C07C237/24 , C07C271/28 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/73 , C07D213/75 , C07D215/04 , C07D215/227 , C07D231/56 , C07D233/88 , C07D257/04 , C07D277/40 , C07D295/135 , C07D333/40 , C07D409/04 , C07D413/12
摘要： The present invention provides compounds of Formula: (I); or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译：本发明提供了式（I）的化合物：或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，L，Z，R 3和环B如本文所定义。式（I）化合物可用作凝血级联和/或接触活化系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。具体而言，它涉及选择性因子XIa抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物以及使用该组合物治疗血栓栓塞性和/或炎症性疾病的方法。

2. 发明申请

WO2006076575A3 SUBSTITUTED BIARYL COMPOUNDS AS FACTOR XIA INHIBITORS 审中-公开
公开(公告)号：WO2006076575A3
公开(公告)日：2006-09-08
申请号：PCT/US2006001224
申请日：2006-01-12
申请人： SQUIBB BRISTOL MYERS CO , CORTE JAMES R , QUAN MIMI L , SMALLHEER JOANNE M , PINTO DONALD J
发明人： CORTE JAMES R , QUAN MIMI L , SMALLHEER JOANNE M , PINTO DONALD J
IPC分类号： A61P7/02 , C07C237/24 , C07D261/20
CPC分类号： C07C255/44 , C07C237/24 , C07C271/28 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/73 , C07D213/75 , C07D215/04 , C07D215/227 , C07D231/56 , C07D233/88 , C07D257/04 , C07D277/40 , C07D295/135 , C07D333/40 , C07D409/04 , C07D413/12
摘要： The present invention provides compounds of Formula: (I); or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

3. 发明申请

WO2004041776A2 SULFONYLAMINOVALEROLAC TAMS AND DERIVATIVES THEREOF AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：磺酰胺戊醇酸酯及其衍生物作为因子Xa抑制剂
公开(公告)号：WO2004041776A2
公开(公告)日：2004-05-21
申请号：PCT/US0314142
申请日：2003-05-05
申请人： SQUIBB BRISTOL MYERS CO , SMALLHEER JOANNE M , PINTO DONALD J , WANG SHUAIGE , QIAO JENNIFER X , HAN WEI , HU ZILIN
发明人： SMALLHEER JOANNE M , PINTO DONALD J , WANG SHUAIGE , QIAO JENNIFER X , HAN WEI , HU ZILIN
IPC分类号： C07D211/76 , C07D401/10 , C07D401/14 , C07D409/14 , C07D417/14 , C07D495/04 , C07D
CPC分类号： C07D409/14 , C07D211/76 , C07D401/10 , C07D401/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula (I), or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式（I）的磺酰氨基戊内酰胺及其衍生物或其药学上可接受的盐形式，其中环G为单环或双环碳环或杂环。本发明化合物可用作胰蛋白酶样丝氨酸蛋白酶，特别是Xa因子的抑制剂。

4. 发明申请

WO2004108892A3 1,1-DISUBSTITUTEDCYCLOALKYL-, GLYCINAMIDYL-, SULFONYL-AMIDINO-, AND TETRAHYDROPYRIMIDINYL-CONTAINING DIAMINOALKYL, beta-AMINOACIDS, alpha-AMINOACIDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 审中-公开
标题翻译：作为因子XA抑制剂的1,1-DISUBSTITUTEDCYCLOALKYL-，GLYCINAMIDYL-，SULFONYL-AMIDINO-和含有二氨基亚氨基的DIAMINOALKYL，β-氨基酸，α-氨基酸及其衍生物
公开(公告)号：WO2004108892A3
公开(公告)日：2005-02-17
申请号：PCT/US2004017296
申请日：2004-06-02
申请人： SQUIBB BRISTOL MYERS CO , QIAO JENNIFER X , PINTO DONALD J
发明人： QIAO JENNIFER X , PINTO DONALD J
IPC分类号： A01N37/18 , A01N43/06 , A01N43/36 , A01N43/38 , A61K31/165 , A61K31/38 , A61K31/40 , A61K31/501 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C12N20060101
CPC分类号： C07D409/12 , C07C237/34 , C07C2601/02 , C07D207/09 , C07D209/40 , C07D209/42 , C07D213/75 , C07D239/06 , C07D295/135 , C07D295/15 , C07D295/155 , C07D295/16 , C07D333/34 , C07D333/36 , C07D333/38 , C07D401/12 , C07D403/12 , C07D409/14 , C07D417/12
摘要： The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives therof of Formula(I) or pharmaceutically acceptable salt forms thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式（I）的1,1-二取代的环烷基 - ，磺酰基 - 脒基 - 和四氢嘧啶基的二氨基烷基，β-氨基酸，α-氨基酸和衍生物或其药学上可接受的盐形式，其中M是线性核心。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

5. 发明申请

WO2008076805B1 ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 审中-公开
标题翻译：芳基丙酰胺，芳基丙烯酰胺，芳基丙酰胺或芳基甲基类似物作为因子XIA抑制剂
公开(公告)号：WO2008076805B1
公开(公告)日：2008-11-13
申请号：PCT/US2007087396
申请日：2007-12-13
申请人： SQUIBB BRISTOL MYERS CO , PINTO DONALD J
发明人： PINTO DONALD J
IPC分类号： C07D401/12 , A61K31/4178 , A61K31/4439 , A61P7/02 , C07D403/12
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14
摘要： The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L 1 , R 3 , R 4 , R 8a , R 11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译：本发明提供式（I）或（II）的化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂化物形式，其中变量A，L 1，R 3， R 4，R 8，R 11，M和M如本文所定义。式（I）或（II）的化合物是凝血级联和/或接触活化系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别涉及选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物以及使用该组合物治疗血栓栓塞性和/或炎症性疾病的方法。

6. 发明申请

WO2008076805A2 ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 审中-公开
公开(公告)号：WO2008076805A2
公开(公告)日：2008-06-26
申请号：PCT/US2007087396
申请日：2007-12-13
申请人： SQUIBB BRISTOL MYERS CO , PINTO DONALD J
发明人： PINTO DONALD J
IPC分类号： C07D401/12 , A61K31/4178 , A61K31/4439 , A61P7/02 , C07D403/12
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14
摘要： The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L 1 , R 3 , R 4 , R 8a , R 11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

7. 发明申请

WO2004083174A3 SULFONYL-AMIDINO CONTAINING AND TETRAHYDROPYRIMIDINO CONTAINING COMPOUNDS AS FACTOR XA INHIBITORS 审中-公开
标题翻译：含有氨基甲酰胺和含有四氢呋喃的化合物作为因子XA抑制剂
公开(公告)号：WO2004083174A3
公开(公告)日：2004-11-25
申请号：PCT/US2004008033
申请日：2004-03-17
申请人： SQUIBB BRISTOL MYERS CO , PINTO DONALD J , QIAO JENNIFER X , GANGOR TIMUR , LAM PATRICK Y S , LI YUN-LONG
发明人： PINTO DONALD J , QIAO JENNIFER X , GANGOR TIMUR , LAM PATRICK Y S , LI YUN-LONG
IPC分类号： A61K31/437 , A61K31/4709 , A61K31/498 , A61K31/503 , A61K31/506 , A61K31/517 , A61K31/536 , A61P7/02 , C07D20060101 , C07D207/16 , C07D209/30 , C07D213/75 , C07D231/14 , C07D233/44 , C07D265/02 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D471/04
CPC分类号： C07D213/75 , C07D207/16 , C07D209/30 , C07D231/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D471/04
摘要： The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula (I): P4-P-M-M4 or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式（I）的含磺酰基脒基和四氢嘧啶基的化合物及其衍生物：P4-PM-M4或其药学上可接受的盐形式，其中M为环，P为任选的环，P4和 M4如下所述。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

8. 发明申请

WO02085353A9 1,4,5,6-TETRAHYDROPYRAZOLO-[3,4-C]-PYRIDIN-7-ONES AS FACTOR XA INHIBITORS 审中-公开
标题翻译： 1,4,5,6-四氢吡唑并[3,4-C] - 吡啶-7-酮作为因子XA抑制剂
公开(公告)号：WO02085353A9
公开(公告)日：2003-01-03
申请号：PCT/US0212204
申请日：2002-04-17
申请人： SQUIBB BRISTOL MYERS CO
发明人： PINTO DONALD J , GALEMMO ROBERT A
IPC分类号： A61P7/02 , C07D471/04 , A61K31/437 , A61K31/415 , C07D221/00 , C07D231/00
CPC分类号： C07D471/04
摘要： The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of Formula (I) or pharmaceutically acceptable salt forms thereof, wherein ring R is 3-amido or 4-methoxy, R is trifluoromethyl or amido, and R is aminomethyl, N-methylaminomethyl, and N,N-dimethylaminomethyl. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式（I）的1,4,5,6-四氢吡唑并[3,4-c]吡啶-7-酮或其药学上可接受的盐形式，其中R是3-酰氨基或4-甲氧基 R 1是三氟甲基或酰氨基，R 2是氨基甲基，N-甲基氨基甲基和N，N-二甲基氨基甲基。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

9. 发明公开

EP1603562A4 SULFONYL-AMIDINO CONTAINING AND TETRAHYDROPYRIMIDINO CONTAINING COMPOUNDS AS FACTOR XA INHIBITORS 审中-公开
标题翻译：磺酰基脒基和TETRAHYDROPYRIMIDINO含氮化合物Xa因子抑制剂
公开(公告)号：EP1603562A4
公开(公告)日：2008-10-22
申请号：EP04757516
申请日：2004-03-17
申请人： SQUIBB BRISTOL MYERS CO
发明人： PINTO DONALD J , QIAO JENNIFER X , GANGOR TIMUR , LAM PATRICK Y S , LI YUN-LONG
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4709 , A61K31/498 , A61K31/503 , A61K31/506 , A61K31/517 , A61K31/536 , A61P7/02 , C07D20060101 , C07D207/16 , C07D209/30 , C07D213/75 , C07D231/14 , C07D233/44 , C07D265/02 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/04 , C07D413/12
CPC分类号： C07D213/75 , C07D207/16 , C07D209/30 , C07D231/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D471/04
摘要： The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula (I): P4-P-M-M4 or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

10. 发明公开

EP1505966A4 1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译： 1,1-二取代的环烷基衍生物AS因子Xa抑制剂
公开(公告)号：EP1505966A4
公开(公告)日：2006-08-30
申请号：EP03755341
申请日：2003-05-05
申请人： SQUIBB BRISTOL MYERS CO
发明人： QIAO JENNIFER X , PINTO DONALD J , ORWAT MICHAEL J , HAN WEI , FRIEDRICH SARAH R
IPC分类号： A61K31/41 , A61K31/435 , A61K31/44 , A61P7/02 , C07D209/30 , C07D213/14 , C07D213/75 , C07D333/38 , C07D401/04 , C07D409/12 , C07D471/04
CPC分类号： C07D213/75 , C07D209/30 , C07D333/38 , C07D401/04 , C07D409/12 , C07D471/04
摘要： The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

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