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1. 发明申请

WO2004071440A3 THIAZOLYL-BASED COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：基于噻唑基的化合物可用作激酶抑制剂
公开(公告)号：WO2004071440A3
公开(公告)日：2004-12-09
申请号：PCT/US2004003879
申请日：2004-02-06
申请人： SQUIBB BRISTOL MYERS CO , HYNES JOHN , WU HONG , LEFTHERIS KATERINA , LIU CHUNJIAN , DAS JAGABANDHU , MOQUIN ROBERT V
发明人： HYNES JOHN , WU HONG , LEFTHERIS KATERINA , LIU CHUNJIAN , DAS JAGABANDHU , MOQUIN ROBERT V
IPC分类号： A61K20060101 , A61K31/426 , A61K31/4439 , C07D277/34 , C07D277/46 , C07D277/56 , C07D417/02 , C07D417/12
CPC分类号： C07D277/56 , C07D417/12
摘要： The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R , R , Z m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了用于治疗p38激酶相关病症的式（I）的基于噻唑基的化合物，其中环A是苯基或吡啶基，并且X，Y，B，R 2，R 3， m和n如本文所定义。本发明进一步涉及含有至少一种用于治疗p38激酶相关病症的根据本发明的化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

2. 发明申请

WO2004098518A3 PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡唑酰胺化合物可用作激酶抑制剂
公开(公告)号：WO2004098518A3
公开(公告)日：2005-01-27
申请号：PCT/US2004013594
申请日：2004-05-03
申请人： SQUIBB BRISTOL MYERS CO , DYCKMAN ALARIC , DAS JAGABANDHU , LEFTHERIS KATERINA , LIU CHUNJIAN , MOQUIN ROBERT V , WROBLESKI STEPHEN T
发明人： DYCKMAN ALARIC , DAS JAGABANDHU , LEFTHERIS KATERINA , LIU CHUNJIAN , MOQUIN ROBERT V , WROBLESKI STEPHEN T
IPC分类号： A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中G，X，R 1，R 2，R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

3. 发明申请

WO2004098528A3 PYRAZOLE-AMINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡唑胺化合物作为激酶抑制剂有用
公开(公告)号：WO2004098528A3
公开(公告)日：2005-07-14
申请号：PCT/US2004013786
申请日：2004-05-03
申请人： SQUIBB BRISTOL MYERS CO , DYCKMAN ALARIC , DAS JAGABANDHU , LEFTHERIS KATERINA , LIU CHUNJIAN , MOQUIN ROBERT V , WROBLESKI STEPHEN T
发明人： DYCKMAN ALARIC , DAS JAGABANDHU , LEFTHERIS KATERINA , LIU CHUNJIAN , MOQUIN ROBERT V , WROBLESKI STEPHEN T
IPC分类号： A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中W，X，R 1，R 2，R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

4. 发明申请

WO2008057775A3 HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：杂环化合物作为激酶抑制剂有用
公开(公告)号：WO2008057775A3
公开(公告)日：2008-07-31
申请号：PCT/US2007082471
申请日：2007-10-25
申请人： SQUIBB BRISTOL MYERS CO , WROBLESKI STEPHEN T , DAS JAGABANDHU , DHAR T G MURALI , DYCKMAN ALARIC J , HYNES JOHN , LEFTHERIS KATERINA , LIN JAMES , LIN SHUQUN
发明人： WROBLESKI STEPHEN T , DAS JAGABANDHU , DHAR T G MURALI , DYCKMAN ALARIC J , HYNES JOHN , LEFTHERIS KATERINA , LIN JAMES , LIN SHUQUN
IPC分类号： A61K31/381 , C07D207/456 , C07D209/08 , C07D209/42 , C07D211/62 , C07D213/81 , C07D213/82 , C07D231/56 , C07D233/90 , C07D235/06 , C07D249/06 , C07D261/18 , C07D271/06 , C07D271/10 , C07D275/02
CPC分类号： C07D261/18 , C07C237/42 , C07C2601/02 , C07D207/456 , C07D209/08 , C07D209/42 , C07D211/62 , C07D213/81 , C07D213/82 , C07D231/56 , C07D233/90 , C07D235/06 , C07D249/06 , C07D271/06 , C07D271/10 , C07D275/03 , C07D295/192 , C07D307/68 , C07D333/38 , C07D409/04 , C07D487/04 , C07D513/04
摘要： A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式I化合物及其对映异构体，非对映异构体和药学上可接受的盐。还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

5. 发明申请

WO0158869B1 CANNABINOID RECEPTOR MODULATORS, THEIR PROCESSES OF PREPARATION, AND USE OF CANNABINOID RECEPTOR MODULATORS IN TREATING RESPIRATORY AND NON-RESPIRATORY DISEASES 审中-公开
标题翻译： CANNABINOID受体调节剂，其制备方法和CANNABINOID受体调节剂在治疗呼吸道疾病和非呼吸系统疾病中的应用
公开(公告)号：WO0158869B1
公开(公告)日：2002-02-21
申请号：PCT/US0104131
申请日：2001-02-08
申请人： SQUIBB BRISTOL MYERS CO , LEFTHERIS KATERINA , ZHAO RULIN , CHEN BANG CHI , KIENER PETER , WU HONG , PANDIT CHENNAGIRI R , WROBLESKI STEPHEN , CHEN PING , HYNES JOHN JR , LONGPHRE MALINDA , NORRIS DEREK J , SPERGEL STEVEN , TOKARSKI JOHN
发明人： LEFTHERIS KATERINA , ZHAO RULIN , CHEN BANG-CHI , KIENER PETER , WU HONG , PANDIT CHENNAGIRI R , WROBLESKI STEPHEN , CHEN PING , HYNES JOHN JR , LONGPHRE MALINDA , NORRIS DEREK J , SPERGEL STEVEN , TOKARSKI JOHN
IPC分类号： A61K31/40 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4353 , A61K31/438 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/00 , A61P11/00 , A61P11/06 , C07D207/337 , C07D207/40 , C07D207/416 , C07D209/08 , C07D209/42 , C07D231/14 , C07D231/56 , C07D233/90 , C07D257/04 , C07D263/32 , C07D271/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D498/04 , C07D498/06 , C07D207/34 , C07D401/14 , C07D407/12
CPC分类号： C07D207/416 , A61K31/40 , A61K31/415 , A61K31/44 , C07D209/42 , C07D231/14 , C07D231/56 , C07D233/90 , C07D257/04 , C07D263/32 , C07D271/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/08
摘要： Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form a six-membered aryl or heteroaryl ring, optionally having a substituent R6 forming a ring with R3.
摘要翻译：公开了在化合物是大麻素受体调节剂的哺乳动物中用于治疗呼吸系统疾病的化合物的用途。用作治疗呼吸道和非呼吸性白细胞活化相关疾病的大麻素受体调节剂的化合物包括式（I）化合物，其中A和B为氮或碳，只提供A和B之一为氮; 和R 1 -R 6如说明书中所定义，其中R 2与R 5可以形成环，和/或两个R 4基团可以形成六元芳基或杂芳基环，任选地具有与R 3形成环的取代基R 6。

6. 发明申请

WO0158869A3 CANNABINOID RECEPTOR MODULATORS, THEIR PROCESSES OF PREPARATION, AND USE OF CANNABINOID RECEPTOR MODULATORS IN TREATING RESPIRATORY AND NON-RESPIRATORY DISEASES 审中-公开
标题翻译： CANNABINOID受体调节剂，其制备方法和CANNABINOID受体调节剂在治疗呼吸道疾病和非呼吸系统疾病中的应用
公开(公告)号：WO0158869A3
公开(公告)日：2002-01-24
申请号：PCT/US0104131
申请日：2001-02-08
申请人： SQUIBB BRISTOL MYERS CO , LEFTHERIS KATERINA , ZHAO RULIN , CHEN BANG CHI , KIENER PETER , WU HONG , PANDIT CHENNAGIRI R , WROBLESKI STEPHEN , CHEN PING , HYNES JOHN JR , LONGPHRE MALINDA , NORRIS DEREK J , SPERGEL STEVEN , TOKARSKI JOHN
发明人： LEFTHERIS KATERINA , ZHAO RULIN , CHEN BANG-CHI , KIENER PETER , WU HONG , PANDIT CHENNAGIRI R , WROBLESKI STEPHEN , CHEN PING , HYNES JOHN JR , LONGPHRE MALINDA , NORRIS DEREK J , SPERGEL STEVEN , TOKARSKI JOHN
IPC分类号： A61K31/40 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4353 , A61K31/438 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/00 , A61P11/00 , A61P11/06 , C07D207/337 , C07D207/40 , C07D207/416 , C07D209/08 , C07D209/42 , C07D231/14 , C07D231/56 , C07D233/90 , C07D257/04 , C07D263/32 , C07D271/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D498/04 , C07D498/06 , C07D207/34 , C07D401/14 , C07D407/12
CPC分类号： C07D207/416 , A61K31/40 , A61K31/415 , A61K31/44 , C07D209/42 , C07D231/14 , C07D231/56 , C07D233/90 , C07D257/04 , C07D263/32 , C07D271/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/08
摘要： Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R>1 6 2 5 4 6 3
摘要翻译：公开了在化合物是大麻素受体调节剂的哺乳动物中用于治疗呼吸系统疾病的化合物的用途。用作治疗呼吸道和非呼吸性白细胞活化相关疾病的大麻素受体调节剂的化合物包括式（I）化合物，其中A和B为氮或碳，只提供A和B之一为氮; 和R 1'-R 6如说明书中所定义，其中R> 2 可以形成环，和/或两个R 4基团可以形成六元芳基或杂芳基环，任选地具有取代基R> 6 <形成具有R> 3的环。

7. 发明申请

WO2006017054A3 TRICYCLIC-HETEROARYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC-HETEROARYL化合物作为激酶抑制剂有用
公开(公告)号：WO2006017054A3
公开(公告)日：2006-03-16
申请号：PCT/US2005023683
申请日：2005-06-30
申请人： SQUIBB BRISTOL MYERS CO , LIN JAMES , WROBLESKI STEPHEN T , LIU CHUNJIAN , LEFTHERIS KATERINA
发明人： LIN JAMES , WROBLESKI STEPHEN T , LIU CHUNJIAN , LEFTHERIS KATERINA
IPC分类号： C07D487/14 , A61K31/53 , A61P3/10 , A61P9/04 , A61P19/02
CPC分类号： C07D487/14
摘要： The present invention relates to compounds having the formula (I) wherein, Q is optionally substituted aryl or heteroaryl, R
摘要翻译：本发明涉及具有式（I）的化合物，其中Q是任选取代的芳基或杂芳基，R 1是

8. 发明申请

WO2007016392A3 BENZOTHIAZOLE AND AZABENZOTHIAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：苯并噻唑和亚苄基唑类化合物作为激酶抑制剂有用
公开(公告)号：WO2007016392A3
公开(公告)日：2007-05-24
申请号：PCT/US2006029520
申请日：2006-07-28
申请人： SQUIBB BRISTOL MYERS CO , LIU CHUNJIAN , LEFTHERIS KATERINA , LIN JAMES
发明人： LIU CHUNJIAN , LEFTHERIS KATERINA , LIN JAMES
IPC分类号： C07D417/04 , A61K31/428 , C07D513/04
CPC分类号： C07D513/04 , C07D417/04
摘要： A compound of Formula (I), or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: (a); (b); (c); or (d), further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II), or an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: (a); (b); (c); (d); or (e), further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中A独立地选自：（a）; （B）; （C）; 或（d），其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和W如本文所述。还公开了式（II）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中G，X和Y各自独立地为CH或N，其中在每次出现时，G，X 或Y为N，G，X或Y中的两个为CH; 和B独立地选自：（a）; （B）; （C）; （D）; 或（e），其中R1，R2，R3，R4，R5，R8，R9和Z如本文所述。还公开了含有式（I）和式（II）化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

9. 发明申请

WO2004043912A3 METHODS FOR THE PREPARATION OF PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：用于制备可用作激酶抑制剂的吡咯并三嗪化合物的方法
公开(公告)号：WO2004043912A3
公开(公告)日：2004-07-01
申请号：PCT/US0335220
申请日：2003-11-03
申请人： SQUIBB BRISTOL MYERS CO , GODFREY JOLLIE DUAINE JR , HYNES JOHN JR , DYCKMAN ALARIC J , LEFTHERIS KATERINA , SHI ZHONGPING , WROBLESKI STEPHEN T , DOUBLEDAY WENDEL WILLIAM , GROSSO JOHN A
发明人： GODFREY JOLLIE DUAINE JR , HYNES JOHN JR , DYCKMAN ALARIC J , LEFTHERIS KATERINA , SHI ZHONGPING , WROBLESKI STEPHEN T , DOUBLEDAY WENDEL WILLIAM , GROSSO JOHN A
IPC分类号： A61P11/06 , A61P19/02 , A61P19/10 , C07D207/50 , C07D487/04 , C07D519/00 , A61K31/53
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译：制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂合物的方法，其中R 1至R 6和Z如说明书中所述。根据本发明的方法利用胺化方法，其中吡咯与卤代胺，优选氯胺反应。该步骤之后是环化以形成吡咯并三嗪核心。

10. 发明申请

WO2008116064A3 FUSED HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF PROLIFERATIVE, ALLERGIC, AUTOIMMUNE OR INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗增生性，过敏性，自身免疫性或炎性疾病的融合的杂环化合物
公开(公告)号：WO2008116064A3
公开(公告)日：2010-01-21
申请号：PCT/US2008057656
申请日：2008-03-20
申请人： SQUIBB BRISTOL MYERS CO , LIU CHUNJIAN , LEFTHERIS KATERINA , TEBBEN ANDREW J
发明人： LIU CHUNJIAN , LEFTHERIS KATERINA , TEBBEN ANDREW J
IPC分类号： C07D487/04 , A61K31/4188 , A61K31/53 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.
摘要翻译：具有式（I）的化合物及其对映异构体和非对映体药学上可接受的盐可用作激酶调节剂，包括Btk调节，其中R1，R2，R4，Q， Y，A和D如本文所定义。

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