专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2004000214A3 USE OF COMPOUNDS HAVING AN AMINE NUCLEUS IN MANUFACTURE OF A MEDICAMENT USEFUL FOR TREATING FACTOR VIIA-ASSOCIATED CONDITIONS 审中-公开
公开(公告)号：WO2004000214A3
公开(公告)日：2003-12-31
申请号：PCT/US2003/019155
申请日：2003-06-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , HERPIN, Timothy , BISACCHI, Gregory, S. , PI, Zulan , PRIESTLEY, E., Scott , DHAR, T.G., Murali
发明人： HERPIN, Timothy , BISACCHI, Gregory, S. , PI, Zulan , PRIESTLEY, E., Scott , DHAR, T.G., Murali
IPC分类号： C07C233/32
摘要： Use of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof, in the manufacture of a medicament useful for treating conditions associated with the activity of Factor VIIa is described.

2. 发明申请

WO2004072101A2 PHENYLGLYCINE DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：苯乙烯衍生物有效用作丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004072101A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/003961
申请日：2004-02-10
申请人： BRISTOL-MYERS SQUIBB COMPANY , GLUNZ, Peter, W. , BISACCHI, Gregory, S. , MORTON, George, C. , HOLUBEC, Alexandra, A. , PRIESTLEY, E. Scott , ZHANG, Xiaojun , TREUNER, Uwe, D.
发明人： GLUNZ, Peter, W. , BISACCHI, Gregory, S. , MORTON, George, C. , HOLUBEC, Alexandra, A. , PRIESTLEY, E. Scott , ZHANG, Xiaojun , TREUNER, Uwe, D.
IPC分类号： C07K
CPC分类号： C07D231/56 , C07C311/51 , C07D217/02 , C07D217/06 , C07D217/22 , C07D233/36 , C07D235/30 , C07D239/94 , C07D261/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is NR 6 S(O) p R 16 ; W is hydrogen or (CR 7 R 8 ) q - W 1 ; W 1 is hydrogen or a bond with R 6 ; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R 1 , R 2 , R 3 , R6, R 7 , and R 16 are as defined in the specification.
摘要翻译：具有式（I）化合物或其立体异构体或药学上可接受的盐或其水合物可用作因子VIIa抑制剂，其中X为NR 6 S（O）p R 16; W是氢或（CR7R8）q-W1; W1是氢或与R6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，以及R1，R2，R3，R6，R7和R16 如本说明书中所定义。

3. 发明申请

WO1997037646A1 CATECHOLAMINE SURROGATES USEFUL AS 'beta'3 AGONISTS 审中-公开
标题翻译： CATECHOLAMINE SURROGATES有用作β3激动剂
公开(公告)号：WO1997037646A1
公开(公告)日：1997-10-16
申请号：PCT/US1997005324
申请日：1997-04-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , BISACCHI, Gregory, S. , GAVAI, Ashvinikumar, V. , POSS, Kathleen, M. , RYONO, Denis, E. , SHER, Philip, M. , SUN, Chong-Qing , WASHBURN, William, N.
IPC分类号： A61K31/18
CPC分类号： C07C311/46 , C07C311/08 , C07C311/39 , C07D263/32 , C07D277/28 , C07F9/4056
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof. As used in formula (I), and throughout the specification, the symbols have the following meanings: R is lower alkyl, aryl or arylalkyl; R is hydrogen, hydroxyl, hydroxymethyl or halogen; R is hydrogen or alkyl; R and R are independently hydrogen, alkoxy, alkoxymethyl, hydroxyl, -CN, -CON(R )R 2 , -N(R )R , -NR COR , -NR SO2R ; or R and R may together with the carbon atoms to which they are bonded form a heterocycle; R , R and R are independently A or B, wherein A is hydrogen, alkyl, cylcoalkyl, halogen, hydroxyl, aryl, alkoxy, cyano, -SR , -SOR , -SO2R , -N(R )R , -NR COR , -OCH2CON(R )R , -OCH2CO2R , CON(R )R , -CO2R ; and B is -(CH2)nN(R )R , -(CH2)mPO(OR )OR , -(CH2)nNR COR , -O-aryl, -OCH2CH2N(R )R , -COR , -SO2N(R )R , -NR CO2R , -NR CO(N(R )R ), heterocycle or -R and R may together with the carbon atoms to which they are bonded form a heterocycle, provided that at least one of R , R and R is B; R and R are independently hydrogen or lower alkyl; R is lower alkyl; R is hydrogen, lower alkyl, aryl or arylalkyl; m is an integer of 0 to 6; and n is an integer of 1 to 6. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
摘要翻译：式（I）化合物及其药学上可接受的盐。在式（I）中使用，并且在整个说明书中，符号具有以下含义：R 1是低级烷基，芳基或芳基烷基; R 2是氢，羟基，羟甲基或卤素; R 3是氢或烷基; R 4和R 4独立地是氢，烷氧基，烷氧基甲基，羟基，-CN，-CON（R 6）R 6'，-CO 2，R 6， R 6）R 6，-NR 6 COR 8，-NR 6 SO 2 R 1; 或R 4和R 4'可以与它们所键合的碳原子一起形成杂环; R 5，R 5和R 5独立地是A或B，其中A是氢，烷基，环烷基，卤素，羟基，芳基，烷氧基，氰基，-SR 7，-SOR -SO 2 R 7，-N（R 6）R 6'，-NR 6 COR 8，-OCH 2 CON（R 6）R 6，-OCH 2 CO 2 R CON（R 6）R 6，-CO 2 R 6; 并且B是 - （CH 2）n N（R 6）R 6'， - （CH 2）m PO（OR 6）OR 6， - （CH 2）n NR 6 COR 8， -O-芳基，-OCH 2 CH 2 N（R 6）R 6'，-COR 7，-SO 2 N（R 6）R 6'，-NR 6 CO 2 R 7， NR 6 CO（N（R 6）R 6'），杂环或-R 5和R 5可以与它们所键合的碳原子一起形成杂环，条件是 R 5，R 5'和R 5“中的至少一个是B; R 6和R 6独立地是氢或低级烷基; R 7是低级烷基; R 8是氢，低级烷基，芳基或芳基烷基; m为0〜6的整数。并且n是1至6的整数。这些化合物是β三肾上腺素能受体激动剂，因此可用于例如糖尿病，肥胖症和胃肠道疾病的治疗。

4. 发明申请

WO2005009392A2 DIHYDROPYRIMIDONE INHIBITORS OF CALCIUM CHANNEL FUNCTION 审中-公开
标题翻译：钙通道功能的二氢吲哚酮抑制剂
公开(公告)号：WO2005009392A2
公开(公告)日：2005-02-03
申请号：PCT/US2004/023909
申请日：2004-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , BISACCHI, Gregory, S. , MURUGESAN, Natesan , EWING, William, R. , YU, Guixue , GU, Zhengxiang , FRIENDS, Todd, J. , ZHANG, Minsheng
发明人： BISACCHI, Gregory, S. , MURUGESAN, Natesan , EWING, William, R. , YU, Guixue , GU, Zhengxiang , FRIENDS, Todd, J. , ZHANG, Minsheng
IPC分类号： A61K
CPC分类号： C07D239/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds having the Formula (I) enantiomers, diastereomers, solvates and salts thereof, where R 1 , R 2 , R 3 , R 4 , A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.
摘要翻译：其中R 1，R 2，R 3，R 4，A，X和J在本文中描述的具有式（I）对映异构体，非对映异构体，溶剂合物和盐的化合物是钙通道功能，并且可用于治疗钙通道依赖性疾病，包括高血压。

5. 发明申请

WO2004000788A1 UREIDO-SUBSTITUTED ANILINE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：尿素替代苯胺化合物有效用作丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004000788A1
公开(公告)日：2003-12-31
申请号：PCT/US2003/019605
申请日：2003-06-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , SLUSASRCHYK, William, A. , BOLTON, Scott, A. , HERPIN, Timothy , BISACCHI, Gregory, S. , PI, Zulan , PRIESTLEY, E., Scott
发明人： SLUSASRCHYK, William, A. , BOLTON, Scott, A. , HERPIN, Timothy , BISACCHI, Gregory, S. , PI, Zulan , PRIESTLEY, E., Scott
IPC分类号： C07C233/32
CPC分类号： C07D263/48 , A61K31/136 , A61K31/4155 , A61K31/422 , A61K45/06 , A61K2300/00
摘要： Compounds having formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.
摘要翻译：具有式（I）化合物或其药学上可接受的盐，水合物或前体药物作为因子VIIa的抑制剂是有效的。

6. 发明申请

WO2003047512A2 COMPOUNDS DERIVED FROM AN AMINE NUCLEUS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 审中-公开
标题翻译：从氨基核和由其组成的药物组合物衍生的化合物
公开(公告)号：WO2003047512A2
公开(公告)日：2003-06-12
申请号：PCT/US2002/038038
申请日：2002-11-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , LIU, Chunjian , DHAR, Murali, T., G. , GU, Henry, H. , IWANOWICZ, Edwin, J. , LEFTHERIS, Katerina , PITTS, William, J. , HERPIN, Timothy, F. , PI, Zulan , BISACCHI, Gregory, S.
发明人： LIU, Chunjian , DHAR, Murali, T., G. , GU, Henry, H. , IWANOWICZ, Edwin, J. , LEFTHERIS, Katerina , PITTS, William, J. , HERPIN, Timothy, F. , PI, Zulan , BISACCHI, Gregory, S.
IPC分类号： A61K
CPC分类号： C07D413/12 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D263/48 , C07D413/14 , C07D417/12
摘要： Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C 1-4 alkyl, and A, R 1 , R 2 and R 4 are as defined in the specification.
摘要翻译：具有式（I）的化合物作为IMPDH酶和/或丝氨酸蛋白酶因子VIIa的抑制剂是有效的，其中B是单环或双环碳环或杂环，D是单环或双环的碳环或杂环，除了当A是那么D是杂环体系，R是氢或C 1-4烷基，A，R 1，R 2和R 4如本说明书中所定义。

7. 发明申请

WO2002042273A3 ACID DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2002042273A3
公开(公告)日：2002-05-30
申请号：PCT/US2001/046884
申请日：2001-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , BISACCHI, Gregory, S. , SUTTON, James, C., Jr. , SLUSARCHYK, William, A. , TREUNER, Uwe, D. , ZHAO, Guohua , CHENEY, Daniel, L. , WU, Shung, C. , SHI, Yan
发明人： BISACCHI, Gregory, S. , SUTTON, James, C., Jr. , SLUSARCHYK, William, A. , TREUNER, Uwe, D. , ZHAO, Guohua , CHENEY, Daniel, L. , WU, Shung, C. , SHI, Yan
IPC分类号： C07D401/12
摘要： Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, Ixa, Xa, and/or Xia, wherein ring B is phenyl or pyridyl, W is preferably C(=O)NR 4 R 5 , L is a linker group, X 2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification.

8. 发明申请

WO2005007124A2 SUBSTITUTED DIHYDROPYRIMIDINE INHIBITORS OF CALCIUM CHANNEL FUNCTION 审中-公开
标题翻译：钙离子通道功能的取代二氢嘧啶抑制剂
公开(公告)号：WO2005007124A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/023929
申请日：2004-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , MURUGESAN, Natesan , BISACCHI, Gregory, S. , EWING, William, R. , GU, Zhengxiang
发明人： MURUGESAN, Natesan , BISACCHI, Gregory, S. , EWING, William, R. , GU, Zhengxiang
IPC分类号： A61K
CPC分类号： C07D403/12 , C07D239/26 , C07D239/36
摘要： The present invention relates to substituted dihydropyrimidine inhibitors of calcium channel function having formula (I) where A, a, J, R 1 , R 2 , R 3 , R 4 , and R 5 , are defined herein; pharmaceutical compositions comprising said compounds; and methods of treating calcium channel-dependent disorders, including hypertension.
摘要翻译：本发明涉及具有式（I）的钙通道官能团的取代二氢嘧啶抑制剂，其中A，a，J，R 1，R 2，R 3，R 4和R 5，在本文中定义; 包含所述化合物的药物组合物; 以及治疗钙通道依赖性疾病（包括高血压）的方法。

9. 发明申请

WO2004094372A2 BIARYLMETHYL INDOLINES, INDOLES AND TETRAHYDROQUINOLINES, USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：二异丙基吲哚，吲哚和四氢喹啉，有用的丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004094372A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011856
申请日：2004-04-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , SMALLHEER, Joanne, M. , QUAN, Mimi, L. , WANG, Shuaige , BISACCHI, Gregory, S.
发明人： SMALLHEER, Joanne, M. , QUAN, Mimi, L. , WANG, Shuaige , BISACCHI, Gregory, S.
IPC分类号： C07D
CPC分类号： C07D209/08 , C07D209/22
摘要： The present invention provides compounds of Formula (I) or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W 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：本发明提供式（I）化合物或其立体异构体或药学上可接受的盐或水合物形式，其中变量A，B，L1，L2，X1，X2，X3，X4和W如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活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。特别地，它涉及作为选择性因子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和使用其制备血栓栓塞和/或炎症性疾病的方法。

10. 发明申请

WO2004072102A2 BENZENE ACETAMIDE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：苯乙烯类化合物可用作丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004072102A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/003962
申请日：2004-02-10
申请人： BRISTOL-MYERS SQUIBB COMPANY , BISACCHI, Gregory, S. , TREUNER, Uwe, D. , MORTON, George, C.
发明人： BISACCHI, Gregory, S. , TREUNER, Uwe, D. , MORTON, George, C.
IPC分类号： C07K
CPC分类号： C07D217/22 , C07C237/20 , C07C271/20 , C07D217/06 , C07D401/12
摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, or prodrugs thereof, are useful as serine protease inhibitors, wherein X is OH, O(alkyl), O(aryl), O(arylalkyl), NR 5 (aryl), or NR 5 (arylalkyl); W is hydrogen or (CR 7 R 8 ) q -W 1; W 1 is hydrogen or a bond with R 6 ; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R 1 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 16 are as defined in the specification.
摘要翻译：具有式（I）化合物及其药学上可接受的盐，水合物或前药可用作丝氨酸蛋白酶抑制剂，其中X是OH，O（烷基），O（芳基），O（芳基烷基），NR 5 ）或NR 5（芳基烷基）; W是氢或（CR7R8）q-W1; W1是氢或与R6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，以及R1，R2，R3，R5，R6，R7，和R 16如说明书中所定义。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式