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1. 发明申请

WO2008021926A2 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF 审中-公开
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-κB活性及其用途
公开(公告)号：WO2008021926A2
公开(公告)日：2008-02-21
申请号：PCT/US2007/075543
申请日：2007-08-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , WEINSTEIN, David, S. , GONG, Hua , DUAN, Jingwu , DHAR, T.G. Murali , YANG, Bingwei Vera , CHEN, Ping , JIANG, Bin
发明人： WEINSTEIN, David, S. , GONG, Hua , DUAN, Jingwu , DHAR, T.G. Murali , YANG, Bingwei Vera , CHEN, Ping , JIANG, Bin
CPC分类号： C07D417/12 , C07D277/46 , C07D405/12 , C07D417/14 , C07D491/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-KB activity, including inflammatory and immune diseases, having the structure of formula (I), an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8- membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R 5 , R 6 , R 7 , and R 8 ; J 1 , J 2 , and J3 are at each occurrence the same or different and are independently -A 1 QA 2 -; Q is a bond, O, S, S(O), or S(O)2; A 1 and A 2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C 1 - 3 alkylene, C 2 -4alkenylene, and substituted C 2 - 4 alkenylene, provided that A 1 and A 2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R 1 to R 11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与式（I）结构的糖皮质激素受体，AP-1和/或NF-κB活性（包括炎症和免疫疾病）的调节相关的疾病，对映异构体，非对映体或其互变异构体，或其前药酯或其药学上可接受的盐，其中：Z是杂环或杂芳基; A是5-至8-元碳环或5-至8-元杂环; B是环烷基，环烯基，芳基，杂环或杂芳基环，其中每个环与相邻原子上的A环稠合，并且任选地被一至四个相同或不同的基团取代，并且独立地选自R 1， R 5，R 6，R 7和R 8; J 1，J 2和J 3在每次出现时相同或不同，并且独立地为-A 1 N 2 QA 2， SUB> - ; Q是键，O，S，S（O）或S（O）2; A 1和A 2各自相同或不同，并且在每次出现时独立地选自键，C 1-3亚烷基，取代的C 1 H 3，

2. 发明申请

WO2007005631A1 PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡咯烷酮化合物可用作激酶抑制剂
公开(公告)号：WO2007005631A1
公开(公告)日：2007-01-11
申请号：PCT/US2006/025632
申请日：2006-06-29
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHEN, Ping , NORRIS, Derek J. , GAVAI, Ashvinikumar V.
发明人： CHEN, Ping , NORRIS, Derek J. , GAVAI, Ashvinikumar V.
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to at least one pyrrolotriazine derivative of formula (I), at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
摘要翻译：本发明涉及式（I）的至少一种吡咯并三嗪衍生物，至少一种包含至少一种吡咯并三嗪衍生物的药物组合物和至少一种使用至少一种吡咯并三嗪衍生物以治疗至少一种激酶相关病症的方法。

3. 发明申请

WO2005065266A3 DI-SUBSTITUTED PYRROLOTRIAZINE COMPOUNDS 审中-公开
公开(公告)号：WO2005065266A3
公开(公告)日：2005-07-21
申请号：PCT/US2004/043282
申请日：2004-12-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , GAVAI, Ashvinikumar V. , HAN, Wen-Ching , CHEN, Ping , RUEDIGER, Edward H. , MASTALERZ, Harold , FINK, Brian E. , NORRIS, Derek J.
发明人： GAVAI, Ashvinikumar V. , HAN, Wen-Ching , CHEN, Ping , RUEDIGER, Edward H. , MASTALERZ, Harold , FINK, Brian E. , NORRIS, Derek J.
IPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

4. 发明申请

WO2006104971A1 ATP COMPETITIVE KINASE INHIBITORS 审中-公开
标题翻译： ATP竞争性激酶抑制剂
公开(公告)号：WO2006104971A1
公开(公告)日：2006-10-05
申请号：PCT/US2006/011023
申请日：2006-03-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , GAVAI, Ashvinikumar V. , CHEN, Ping , ZHAO, Yufen
发明人： GAVAI, Ashvinikumar V. , CHEN, Ping , ZHAO, Yufen
IPC分类号： C07D401/06 , C07D471/04 , C07D401/14 , A61K31/495 , A61P35/00 , A61P19/02
CPC分类号： C07D471/04 , C07D401/06 , C07D401/14
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式（I）化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其可用作抗增殖剂。式（I）化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

5. 发明申请

WO2004078714A3 PROCESSES FOR PREPARING IMIDAZOQUINOXALINONES, HETEROCYCLIC-SUBSTITUTED IMIDAZOPYRAZINONES, IMIDAZOUINOXALINES AND HETEROCYCLIC-SUBSTITUTED IMIDAZOPYRAZINES 审中-公开
公开(公告)号：WO2004078714A3
公开(公告)日：2004-09-16
申请号：PCT/US2004/006549
申请日：2004-03-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHEN, Bang-Chi , SUNDEEN, Joseph, E. , BEDNARZ, Mark, S. , CHEN, Ping
发明人： CHEN, Bang-Chi , SUNDEEN, Joseph, E. , BEDNARZ, Mark, S. , CHEN, Ping
IPC分类号： C07D241/36
摘要： Novel processes for the preparation of imidazoquinoxalinones, heterocyclic-substituted imidazopyrazinones, imidazoquinoxalines and heterocyclic-substituted imidazopyrazines are described.

6. 发明申请

WO2003059269A3 ACRIDONE INHIBITORS OF IMPDH ENZYME 审中-公开
公开(公告)号：WO2003059269A3
公开(公告)日：2003-07-24
申请号：PCT/US2002/041530
申请日：2002-12-20
申请人： BRISTOL-MYERS SQUIBB COMPANY , IWANOWICZ, Edwin, J. , WATTERSON, Scott, H. , CHEN, Ping , DHAR, T., G., Murali , GU, Henry, H. , ZHAO, Yufen
发明人： IWANOWICZ, Edwin, J. , WATTERSON, Scott, H. , CHEN, Ping , DHAR, T., G., Murali , GU, Henry, H. , ZHAO, Yufen
IPC分类号： A61K31/473
摘要： Compounds having formula (I), wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from =O and =S; W is -C(=O)-, -S(=O)-, or -S(O) 2 -; or W may be -CH 2 - if X is -C(=O)-; X is selected from -CH 2 -, -N(R 4 )-, and -O-, except that when W is -CH 2 -, X is -C(=O)-; Y is a bond or -C(R 40 )(R 45 )-; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R 1 , R 2 , R 24 and R 25 are as defined in the specification.

7. 发明申请

WO2006069395A2 SYNTHETIC PROCESS 审中-公开
标题翻译：合成方法
公开(公告)号：WO2006069395A2
公开(公告)日：2006-06-29
申请号：PCT/US2005/047630
申请日：2005-12-21
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHEN, Ping , NORRIS, Derek, J. , GAVAI, Ashvinikumar, V.
发明人： CHEN, Ping , NORRIS, Derek, J. , GAVAI, Ashvinikumar, V.
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00 , C07D239/94 , C07D401/06
CPC分类号： C07D487/04 , C07D239/94 , C07D401/06
摘要： The present invention provides a process for preparing compounds of formula (IV), or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
摘要翻译：本发明提供制备式（Ⅳ）化合物或其可药用盐的方法。通过本发明的方法制备的化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其可用作治疗癌症和其它疾病的抗增殖剂。

8. 发明申请

WO2009100375A1 SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂有用的替加氟唑啶
公开(公告)号：WO2009100375A1
公开(公告)日：2009-08-13
申请号：PCT/US2009/033455
申请日：2009-02-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , FINK, Brian E. , CHEN, Libing , CHEN, Ping , DODD, Dharmpal S. , GAVAI, Ashvinikumar V. , KIM, Soong-Hoon , VACCARO, Wayne , ZHANG, Litai H. , ZHAO, Yufen
发明人： FINK, Brian E. , CHEN, Libing , CHEN, Ping , DODD, Dharmpal S. , GAVAI, Ashvinikumar V. , KIM, Soong-Hoon , VACCARO, Wayne , ZHANG, Litai H. , ZHAO, Yufen
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I咪唑并哒嗪抑制蛋白激酶活性，从而使其成为抗癌剂。

9. 发明申请

WO2008021859A1 PYRROLOTRIAZINE KINASE INHIBITORS 审中-公开
标题翻译：吡咯啉激酶抑制剂
公开(公告)号：WO2008021859A1
公开(公告)日：2008-02-21
申请号：PCT/US2007/075436
申请日：2007-08-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , FINK, Brian E. , CHEN, Ping
发明人： FINK, Brian E. , CHEN, Ping
IPC分类号： C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB and TrkC thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式（I）化合物抑制Trk受体如TrkA，TrkB和TrkC的酪氨酸激酶活性，从而使其可用作治疗癌症和其它疾病的抗增殖剂。

10. 发明申请

WO2007061882A2 PYRROLOTRIAZINE KINASE INHIBITORS 审中-公开
标题翻译：吡咯啉激酶抑制剂
公开(公告)号：WO2007061882A2
公开(公告)日：2007-05-31
申请号：PCT/US2006/044756
申请日：2006-11-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHEN, Ping , ZHAO, Yufen , FINK, Brian, E. , KIM, Soong-hoon
发明人： CHEN, Ping , ZHAO, Yufen , FINK, Brian, E. , KIM, Soong-hoon
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as antiproliferative agents.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制Trk受体如TrkA，TrkB，TrkC或Flt-3的酪氨酸激酶活性，从而使其成为抗增殖剂。

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