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1. 发明公开

EP1692161A2 CHIMERIC CHEMOKINE RECEPTOR POLYPEPTIDES 有权
标题翻译： CHIMERIC趋化因子受体多肽
公开(公告)号：EP1692161A2
公开(公告)日：2006-08-23
申请号：EP04819114.2
申请日：2004-11-12
申请人： Bristol-Myers Squibb Company
发明人： DINCHUK, Joseph E. , DAVIES, Paul , ZHAO, Qihong , CARTER, Percy, H. , SOLOMON, Kimberly, A. , SCHERLE, Peggy Ann
IPC分类号： C07K14/00 , C07K14/52
CPC分类号： C07K14/7158 , C12N15/62
摘要： The present invention relates to a chimeric chemokine receptor comprising two components: a first sequence comprising the N terminus through the last residue of the seven helix TM region of a first chemokine receptor joined with a second sequence comprising the C terminus of a second chemokine receptor extending from the first intracellular residue of the chemokine receptor to the last residue of the chemokine receptor. The chimeric chemokine receptor can be employed in various applications, such as ligand binding and screening assays and signalling assays. The chimeric chemokine receptor can also form a component of a chemokine receptor modulator design program.
摘要翻译：本发明涉及包含两种组分的嵌合趋化因子受体：第一序列，其包含通过第一趋化因子受体的七螺旋TM区的最后一个残基的N末端与包含第二趋化因子受体的C末端的第二序列从趋化因子受体的第一个细胞内残基到趋化因子受体的最后一个残基。嵌合趋化因子受体可以用于各种应用，例如配体结合和筛选测定以及信号传导测定。嵌合趋化因子受体还可以形成趋化因子受体调节剂设计程序的组分。

2. 发明公开

EP2049486A2 PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：哌啶衍生物作为趋化因子受体活性的调节剂
公开(公告)号：EP2049486A2
公开(公告)日：2009-04-22
申请号：EP07763650.4
申请日：2007-01-25
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H. , CAVALLARO, Cullen, L. , DUNCIA, John, V. , GARDNER, Daniel, S. , HYNES, John , LIU, Rui-qin , SANTELLA, Joseph, B. , DODD, Dharmpal, S.
IPC分类号： C07D211/18 , C07D211/38 , C07D211/52 , C07D211/58 , C07D211/70 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D491/10 , A61K31/45
CPC分类号： C07D211/52 , C07D211/18 , C07D211/38 , C07D211/58 , C07D211/70 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/10 , C07D491/107
摘要： The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 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 said modulators are disclosed.

3. 发明公开

EP1656345A1 CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：周期性衍生物作为趋化因子受体活性的调节剂
公开(公告)号：EP1656345A1
公开(公告)日：2006-05-17
申请号：EP04781806.7
申请日：2004-08-20
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H. , CHERNEY, Robert, J. , BATT, Douglas, G. , DUNCIA, John, V. , GARDNER, Daniel, S. , KO, Soo, S. , SRIVASTAVA, Anurag, S. , YANG, Michael, G.
IPC分类号： C07D207/26 , A61K31/4015
CPC分类号： C07D207/273 , C04B35/632 , C07D207/34 , C07D211/86 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04
摘要： The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
摘要翻译：本申请描述了用于治疗类风湿性关节炎，多发性硬化，动脉粥样硬化和哮喘的式（I）的MCP-1或其药学上可接受的盐形式的调节剂。

4. 发明授权

EP2318352B1 CYCLOHEXENYL COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：趋化因子受体的CYCLOHEXENYLVERBINDUNGEN AS调节剂
公开(公告)号：EP2318352B1
公开(公告)日：2012-12-19
申请号：EP09790359.5
申请日：2009-07-14
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H. , BROWN, Gregory, D. , DE LUCCA, George, V. , BATT, Douglas, G. , LIU, Rui-Qin , QIU, Feng
IPC分类号： C07C61/15 , C07C61/28 , C07C61/39 , C07C61/40 , C07C62/32 , C07C62/34 , C07C233/47 , C07C311/51 , A61K31/18 , A61K31/192 , A61P19/02 , A61P9/12 , A61P11/06 , A61P31/18
CPC分类号： C07C311/51 , C07C61/40 , C07C62/34 , C07C233/47 , C07C2601/16

5. 发明授权

EP1667966B1 N-ALKYLATED DIAMINOPROPANE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译： N-烷基化的DIAMINOPROPANDERIVATE作为趋化因子受体的调节剂
公开(公告)号：EP1667966B1
公开(公告)日：2012-02-29
申请号：EP04781964.4
申请日：2004-08-20
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H.
IPC分类号： C07D205/04
CPC分类号： C07D295/205 , C07C237/22 , C07C237/36 , C07C237/44 , C07C271/28 , C07C275/42 , C07D205/04 , C07D239/94
摘要： The present application describes modulators of MCP-1 of formula (I), or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

6. 发明公开

EP2046779A2 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 有权
标题翻译：趋化因子受体活性调节剂，结晶形式和过程
公开(公告)号：EP2046779A2
公开(公告)日：2009-04-15
申请号：EP07813363.4
申请日：2007-07-26
申请人： Bristol-Myers Squibb Company
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
CPC分类号： C07D403/12 , C07D207/273 , 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 R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.
摘要翻译： N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-2-氧代-3 - （6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺，或其药学上可接受的盐，溶剂化物或前药，其具有理想药理学特性的意想不到的组合。还提供了本发明的晶体形式。含有其的药物组合物及其作为治疗炎性疾病，变应性疾病，自身免疫疾病，代谢疾病，癌症和/或心血管疾病的药物的方法也是本发明的目的。本发明还提供了制备式（I）化合物的方法，其包括N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-2-氧代-3- （三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺：其中R 1，R 8，R 9，R 10和'HET'如本文所述。本文还提供了作为该方法的有用中间体的化合物。

7. 发明公开

EP1667966A1 N-ALKYLATED DIAMINOPROPANE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译： N-烷基化的DIAMINOPROPANDERIVATE作为趋化因子受体的调节剂
公开(公告)号：EP1667966A1
公开(公告)日：2006-06-14
申请号：EP04781964.4
申请日：2004-08-20
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H.
IPC分类号： C07D205/04
CPC分类号： C07D295/205 , C07C237/22 , C07C237/36 , C07C237/44 , C07C271/28 , C07C275/42 , C07D205/04 , C07D239/94
摘要： The present application describes modulators of MCP-1 of formula (I), or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

8. 发明公开

EP2776409A1 MACROCYCLIC COMPOUNDS FOR INHIBITION OF INHIBITORS OF APOPTOSIS 有权
标题翻译： FOR抑制细胞凋亡的大环化合物抑制剂
公开(公告)号：EP2776409A1
公开(公告)日：2014-09-17
申请号：EP12787341.2
申请日：2012-11-09
申请人： Ensemble Therapeutics , Bristol-Myers Squibb Company
发明人： SEIGAL, Benjamin, Adam , TERRETT, Nicholas , CARTER, Percy, H. , BORZILLERI, Robert, M. , ZHANG, Yong , MILLER, Michael, M.
IPC分类号： C07D249/04 , A61P35/00
CPC分类号： C07D498/22 , A61K38/00 , C07D249/04 , C07D498/16 , C07K5/1008 , C07K7/56 , Y02A50/411 , Y02A50/414
摘要： The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.

9. 发明授权

EP1973880B1 PIPERAZINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 失效
标题翻译：哌嗪衍生物调节蛋白激酶
公开(公告)号：EP1973880B1
公开(公告)日：2013-08-07
申请号：EP07710312.5
申请日：2007-01-25
申请人： Bristol-Myers Squibb Company
发明人： CARTER, Percy, H. , CAVALLARO, Cullen, L. , DE LUCCA, George, V.
IPC分类号： C07D213/56 , C07D295/18 , A61K31/4965 , A61P19/00
CPC分类号： C07D295/185 , C07D213/56

10. 发明授权

EP2046779B1 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 有权
标题翻译：趋化因子受体，晶体形式和过程的调节剂
公开(公告)号：EP2046779B1
公开(公告)日：2011-05-18
申请号：EP07813363.4
申请日：2007-07-26
申请人： Bristol-Myers Squibb Company
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
CPC分类号： C07D403/12 , C07D207/273 , 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 R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.

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