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11. 发明申请

WO2007073503A2 INDANE MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF 审中-公开
标题翻译：葡萄糖激素受体，AP-1和/或NF-κB活性的调节因子及其用途
公开(公告)号：WO2007073503A2
公开(公告)日：2007-06-28
申请号：PCT/US2006/049075
申请日：2006-12-21
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , JIANG, Bin
发明人： DUAN, Jingwu , JIANG, Bin
CPC分类号： C07D285/135 , C07D233/76 , C07D249/12 , C07D277/46 , C07D285/08
摘要： Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): [INSERT CHEMICAL STRUCTURE HERE] (I) or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, -C(=O)-, -OC(O)-, -C(=O)NR5-, -SOp-, -SOpNR5-, -C(O)O-, - NR5C(O)-, -OC(O)NR5-, -NR5C(O)O-, - S(O)pNR5C(O)-, -C(O)NR5S(O)p- - NR5S(O)p-, or -NR5C(=O)NR6-. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1 - R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病，：[INSERT CHEMICAL STRUCTURE HERE]（I）或其对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为-A1QA2-; Q是键，-C（= O） - ， - OC（O） - ， - C（= O）NR5-，-SOp-，-SOpNR5-，-C（O）O-，-NR5C（O） - （O）NR 5 - ， - NR 5 C（O）O-，-S（O）pNR 5 C（O） - ， - C（O）NR 5 S（O） NR 5 C（= O）NR 6 - 。 Y选自氢，C 1-6烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A1和A2独立地选自键，C1-3亚烷基或C1-3亚烯基，并且R1-R11在本文中定义。还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

12. 发明申请

WO2006076633A1 MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB 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：WO2006076633A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001329
申请日：2006-01-13
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei Vera , DOWEYKO, Lidia M. , DOWEYKO, Arthur M.
发明人： YANG, Bingwei Vera , DOWEYKO, Lidia M. , DOWEYKO, Arthur M.
IPC分类号： C07D277/56 , C07D233/90 , A61K31/426 , A61K31/4168 , A61P37/00
CPC分类号： C07D277/46 , C07D233/90 , C07D277/56
摘要： A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I), where X is S, O or N; Z is -T-COOR 1 or çT-COR 1 ;and T, R, R 1 R a , R b , R c , R d , Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供了一类新型非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并具有结构式（I）的化合物，其中X是S，O或N; Z是-T-COOR 1或çT-COR 1;以及T，R，R 1，R 2， R b，R c，R d，Z，A和B在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

13. 发明申请

WO2006065908A1 CRYSTALLINE FORMS OF6- [(5S, 9R) -9- (4-CYANOPHENYL) -3-(3, 5-DICHLOROPHENYL) -1-METHYL-2, 4-DIOXO-1, 3, 7-TRIAZASPIRO [4.4] NON-7-YL] NICOTINIC 审中-公开
标题翻译： 6 - [（5S，9R）-9-（4-氰基苯基）-3-（3,5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三唑并[4.4] NON的晶体形式 -7-YL] NICOTINIC
公开(公告)号：WO2006065908A1
公开(公告)日：2006-06-22
申请号：PCT/US2005/045251
申请日：2005-12-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , DELMONTE, Albert J. , DHAR, T. G. Murali , GALELLA, Michael , GLEESON, Margaret , GOUGOUTAS, Jack Z. , MCLEOD, Douglas D. , ZHANG, Huiping , CHEN, Bang Chi
发明人： DELMONTE, Albert J. , DHAR, T. G. Murali , GALELLA, Michael , GLEESON, Margaret , GOUGOUTAS, Jack Z. , MCLEOD, Douglas D. , ZHANG, Huiping , CHEN, Bang Chi
IPC分类号： C07D487/10 , A61P37/06 , A61P19/02
CPC分类号： C07D487/10
摘要： The invention provides crystalline forms of 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid, its pharmaceutically acceptable salts, or solvates, thereof Further, a process is provided for preparing substituted spiro-hydantoin compounds of the formula I, wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and methylene precursor compound with an alkene compound. The substituted spiro-hydantoin compounds of formulae I and II are useful in the treatment of immune and/or inflammatory diseases.
摘要翻译：本发明提供6 - [（5S，9R）-9-（4-氰基苯基）-3-（3,5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[ [4.4]非7-基]烟酸，其药学上可接受的盐或溶剂化物。此外，提供了制备式I的取代的螺 - 乙内酰脲化合物的方法，其中Z是N或CR4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A1，A2，G和Q是接头; R2，R4a，R4c和R16在说明书中定义。该方法包括N-取代的甘氨酸化合物和亚甲基前体化合物与烯烃化合物的反应。式I和II的取代的螺 - 乙内酰脲化合物可用于治疗免疫和/或炎性疾病。

14. 发明申请

WO2012125886A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：WO2012125886A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/029334
申请日：2012-03-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , WROBLESKI, Stephen T. , BROWN, Gregory D. , DOWEYKO, Lidia M. , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , SPERGEL, Steven, H. , TOKARSKI, John S. , WU, Hong , YANG, Bingwei Vera
发明人： WROBLESKI, Stephen T. , BROWN, Gregory D. , DOWEYKO, Lidia M. , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , SPERGEL, Steven, H. , TOKARSKI, John S. , WU, Hong , YANG, Bingwei Vera
IPC分类号： A61K31/5025 , A61P37/00 , A61P29/00 , A61P17/00 , A61P19/00 , C07D519/00 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

15. 发明申请

WO2011046916A1 N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE, A DUAL MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESSES 审中-公开
标题翻译： N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-A] [1,3,5]三嗪 4-YLAMINO）-2-氧代吡咯烷-1-基）环己基）乙酰胺，化合物受体活性的双重调节剂，结晶形式和方法
公开(公告)号：WO2011046916A1
公开(公告)日：2011-04-21
申请号：PCT/US2010/052288
申请日：2010-10-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy H. , CHERNEY, Robert J. , ROSSO, Victor W. , LI, Jun
发明人： CARTER, Percy H. , CHERNEY, Robert J. , ROSSO, Victor W. , LI, Jun
IPC分类号： C07D487/04 , A61K31/53 , A61P37/00
CPC分类号： A61K31/53 , C07D487/04
摘要： The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
摘要翻译：本发明提供新的拮抗剂：N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-a] 1,3,5]三嗪-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺：或其药学上可接受的盐，溶剂合物或前药，具有意想不到的双重CCR-2和CCR-5受体活性。还公开了结晶形式，代谢物，含有其的药物组合物和使用其作为治疗炎性疾病，过敏性，自身免疫性，代谢性，癌症和/或心血管疾病的药剂的方法。本公开还提供了制备本文提供的式（I）化合物的方法，包括N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）叔丁基吡唑并[1,5-α] [1,3,5]三嗪-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺。本文还提供了该方法有用中间体的化合物。

16. 发明申请

WO2011044197A1 SPIROCYCLIC COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：作为化合物受体活性调节剂的螺旋化合物
公开(公告)号：WO2011044197A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/051577
申请日：2010-10-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , DHAR, T. G. Murali , DUNCIA, John V. , GARDNER, Daniel S. , GUO, Weiwei , HYNES, John
发明人： DHAR, T. G. Murali , DUNCIA, John V. , GARDNER, Daniel S. , GUO, Weiwei , HYNES, John
IPC分类号： C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04 , A61K31/4427
CPC分类号： C07D471/10 , A61K31/4427 , C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的趋化因子受体活性的调节剂或其立体异构体或其药学上可接受的盐。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和移植排斥反应的自身免疫病态的方法。

17. 发明申请

WO2009158380A1 CYCLOPENTATHIOPHENE MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KAPPA B ACTIVITY AND USE THEREOF 审中-公开
标题翻译： GLUCOCORTICOID受体，AP-1和/或NF-KAPPA B活性及其用途的环磷酰胺调节剂
公开(公告)号：WO2009158380A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048396
申请日：2009-06-24
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei, Vera
发明人： YANG, Bingwei, Vera
IPC分类号： C07D417/12 , A61K31/433 , A61P29/00
CPC分类号： C07D417/12
摘要： A compound of Formula( I ) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
摘要翻译：式（I）的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，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。还公开了含有式I化合物的药物组合物和组合以及治疗包括代谢和炎症或免疫相关疾病或病症的疾病或病症的方法。

18. 发明申请

WO2009058944A2 NONSTEROIDAL COMPOUNDS USEFUL AS MODULATORS OF GLUCOCORTICOID RECEPTOR AP-1 AND/OR NF-κB ACTIVITY AND USE THEREOF 审中-公开
标题翻译：非甾体化合物作为葡萄糖激素受体AP-1和/或NF-κB活性的调节剂和其使用有用
公开(公告)号：WO2009058944A2
公开(公告)日：2009-05-07
申请号：PCT/US2008/081702
申请日：2008-10-30
申请人： BRISTOL-MYERS SQUIBB COMPANY , DHAR, T.G. Murali , XIAO, Hai-Yun
发明人： DHAR, T.G. Murali , XIAO, Hai-Yun
CPC分类号： C07D471/04
摘要： Disclosed are compounds of Formula (I) wherein: one of A and D is -N- and the other of A and D is -C-; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.
摘要翻译：公开了式（I）的化合物，其中：A和D之一是-N-，A和D中的另一个是-C-; 或其对映异构体，非对映异构体或其药学上可接受的盐。还公开了使用这些化合物调节糖皮质激素受体活性的功能的方法和包含这些化合物的药物组合物。

19. 发明申请

WO2008057859A3 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I AND/OR NF-KAPPAB ACTIVITY AND USE THEREOF 审中-公开
公开(公告)号：WO2008057859A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/083090
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei, Vera , DOWEYKO, Lidia, M.
发明人： YANG, Bingwei, Vera , DOWEYKO, Lidia, M.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/433 , A61P29/00
摘要： Novel non-steroidal compounds are provided which are useful in. treating diseases associated with modulation of the glucocorticoid receptor AP-I and/or NF- kB activity, including metabolic and inflammatory or immune associated diseases or disorders havin the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups R 1 , R 2 , R 3 , and/or R 4 ; M is selected from alky!, cycloalkyl, aryl, heterocyclo, and heteroaryl; Z is selected from alkyl, CF3, OH, cycloalkyl, heterocyclo, aryl, heteroaryl, -CC=O)NR 8 R 9 , -CC=O)R 8 , -C(NCN)NR 8 R 9 , -CC=O)OR 8 , -SO 2 R 8 , and -SO 2 NR 8 R 9 . Also provided are pharmaceutical compositions, combinations and methods of treating metabolic and inflammatory or immune associated diseases or disorders using said compounds.

20. 发明申请

WO2008014360A3 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 审中-公开
公开(公告)号：WO2008014360A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074377
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
发明人： CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
IPC分类号： C07D403/12 , C07D207/273 , A61K31/4025 , C07D317/72
摘要： The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-( tert -butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((lR,2S,5R)-5-( tert -butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R 1 , R 8 , R 9 , R 10 , and "HET" are as described herein. Compounds that are useful intermediates of the process are also provided herein.

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