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1. 发明申请

WO2013106614A1 TRIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：三唑基取代的吡啶化合物作为激酶抑制剂有用
公开(公告)号：WO2013106614A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/021096
申请日：2013-01-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DODD, Dharmpal, S. , MUSSARI, Christopher, P. , BHIDE, Rajeev, S. , NAIR, Satheesh Kesavan , PAIDI, Venkatram Reddy , KUMAR, Sreekantha Ratna , BANERJEE, Abhisek , SISTLA, Ramesh , PITTS, William, J. , HYNES, John
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/5025 , A61K31/506
CPC分类号： C07D471/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Compounds having the following formula:(I) wherein:A is an optionally substiuted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
摘要翻译：具有下式的化合物：（I）其中：A是任选取代的三唑或其立体异构体或其药学上可接受的盐，可用作激酶调节剂，包括IRAK-4调节。

2. 发明申请

WO2013013114A1 BIOAVAILABLE COMPOSITIONS OF AMORPHOUS PIPERIDINYL COMPOUNDS 审中-公开
标题翻译：不对称哌嗪化合物的生物可利用组合物
公开(公告)号：WO2013013114A1
公开(公告)日：2013-01-24
申请号：PCT/US2012/047517
申请日：2012-07-20
申请人： BRISTOL-MYERS SQUIBB COMPANY , VICKERY, Rodney D. , STEFANSKI, Kevin J. , SU, Ching-Chiang , HAGEMAN, Michael J. , VIG, Balvinder S. , BETIGERI, Seema
发明人： VICKERY, Rodney D. , STEFANSKI, Kevin J. , SU, Ching-Chiang , HAGEMAN, Michael J. , VIG, Balvinder S. , BETIGERI, Seema
IPC分类号： A61K9/14 , A61K31/445
CPC分类号： A61K31/4465 , A61K9/146 , A61K31/445
摘要： This invention relates to solid amorphous dispersions comprising Compound I having the formula (formula I), or stereoisomers thereof, and one or more polymers. More particularly, this invention relates to bioavailable amorphous solid dispersions of Compound I that are unexpectedly stable in suspension and in the solid state for extended periods of time that may be used for tabletting.
摘要翻译：本发明涉及包含具有式（式I）的化合物I或其立体异构体和一种或多种聚合物的固体无定形分散体。更具体地说，本发明涉及化合物I的生物可利用的无定形固体分散体，它们在悬浮液中和在固态下意想不到地稳定长时间可用于压片。

3. 发明申请

WO2011044309A1 PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：哌啶衍生物作为化合物受体活性调节剂的产物
公开(公告)号：WO2011044309A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/051731
申请日：2010-10-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , HYNES, John , CARTER, Percy H. , CORNELIUS, Lyndon A.M. , DHAR, T.G. Murali , DUNCIA, John V. , NAIR, Satheesh , SANTELLA, Joseph B. , WARRIER, Jayakumar S. , WU, Hong
发明人： HYNES, John , CARTER, Percy H. , CORNELIUS, Lyndon A.M. , DHAR, T.G. Murali , DUNCIA, John V. , NAIR, Satheesh , SANTELLA, Joseph B. , WARRIER, Jayakumar S. , WU, Hong
IPC分类号： C07D211/52
CPC分类号： C07D211/60 , C07D211/52 , C07F9/591 , C07F9/592
摘要： The present application describes prodrugs of the compound 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 using the prodrug compounds of the invention are disclosed.
摘要翻译：本申请描述了式（I）化合物的前药或其立体异构体或其药学上可接受的盐。此外，公开了使用本发明的前药化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫性病症如类风湿性关节炎的方法。

4. 发明申请

WO2009158446A2 CRYSTALLINE FORMS OF ((((4-((5-(CYCLOPROPYLCARBAMOYL)-2-METHYLPHENYL)AMINO)-5-METHYLPYRROLO[2,1-F][1,2,4]TRIAZIN-6-YL)CARBONYL)(PROPYL)CARBAMOYL)OXY)METHYL (4-(PHOSPHONOOXY)PHENYL)ACETATE, METHOD OF PREPARATION AND USE THEREOF 审中-公开
标题翻译：（（（（（（5-（环丙基甲酰基）-2-甲基苯基）氨基）-5-甲基吡咯并[2,1-F] [1,2,4]三嗪-6-基）羰基）（丙基）碳酸酯）氧基）甲基（4-（磷酸苯酯）苯酯）乙酸酯，其制备方法及其用途
公开(公告)号：WO2009158446A2
公开(公告)日：2009-12-30
申请号：PCT/US2009/048547
申请日：2009-06-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , GALELLA, Michael , GOUGOUTAS, Jack, Z.
发明人： GALELLA, Michael , GOUGOUTAS, Jack, Z.
IPC分类号： C07F9/6561 , A61K31/675 , A61P29/00 , A61P25/00 , A61P19/00
CPC分类号： C07F9/6561 , A61K31/675 , Y02A50/411 , Y02A50/463
摘要： The present invention generally relates to crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate. The present invention also generally relates to a pharmaceutical composition comprising said crystalline form, as well of methods of obtaining and using the crystalline form for the treatment of inflammatory-associated diseases or disorders.
摘要翻译：本发明一般涉及（（（（（（4 - （（5-（环丙基氨基甲酰基）-2-甲基苯基）氨基）-5-甲基吡咯并[2,1-f] [1,2,4]三嗪-6- - 基）羰基）（丙基）氨基甲酰基）氧基）甲基（4-（膦酰氧基）苯基）乙酸酯。本发明还通常涉及包含所述结晶形式的药物组合物，以及获得和使用结晶形式用于治疗炎性相关疾病或病症的方法。

5. 发明申请

WO2009155388A1 IMIDAZOPYRIDINE AND IMIDAZOPYRAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂有用的咪唑并吡嗪和咪唑并噻嗪化合物
公开(公告)号：WO2009155388A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/047727
申请日：2009-06-18
申请人： BRISTOL-MYERS SQUIBB COMPANY , HYNES, John , DE LUCCA, George, V. , WU, Hong
发明人： HYNES, John , DE LUCCA, George, V. , WU, Hong
IPC分类号： C07D471/04 , A61K31/437 , A61P29/02
CPC分类号： C07D401/04
摘要： A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）或式（II）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。还公开了含有式（I）或式（II）的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。

6. 发明申请

WO2008057862A2 MODULATORS OF 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：WO2008057862A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/083094
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei Vera , DOWEYKO, Lidia M. , VACCARO, Wayne , HUYNH, Tram N. , TORTOLANI, David R. , DHAR, T.g. Murali
发明人： YANG, Bingwei Vera , DOWEYKO, Lidia M. , VACCARO, Wayne , HUYNH, Tram N. , TORTOLANI, David R. , DHAR, T.g. Murali
IPC分类号： C07C235/36 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D241/20
CPC分类号： C07D211/58 , C07C235/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/10 , C07D417/12
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-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R 6 and R 7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C 1 -C 4 alkyl, and substituted C 1 -C 4 alkyl; or (ii) Q and R 6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M a M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO 2 , and N which ring may be optionally substituted with 0-2 R 5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and M a , Z a , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using 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）结构的炎性和免疫疾病，肥胖症和糖尿病，对映体，非对映异构体，互变异构体，溶剂化物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基，则 R 6和R 7与它们所连接的碳原子一起选自除环烷基之外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和M a a M与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自由O，S，SO 2和N组成的基团可以任选地被0-2个R 5基团或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 和M a a，Z a，R 1，R 2，R 3， R 4，R 6，R 7和R 22如本文所定义。还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

7. 发明申请

WO2015069310A1 ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNALPHA RESPONSES 审中-公开
标题翻译：用作IL-12，IL-23和/或IFNALPHA反应调节剂的烷基酰胺取代的吡啶化合物
公开(公告)号：WO2015069310A1
公开(公告)日：2015-05-14
申请号：PCT/US2014/011769
申请日：2014-01-16
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： MOSLIN, Ryan M. , WEINSTEIN, David S. , WROBLESKI, Stephen T. , ZHANG, Yanlei , TOKARSKI, John S. , MERTZMAN, Michael E. , LIU, Chunjian
IPC分类号： C07D213/82 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/506 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61P29/00 , A61P37/00
CPC分类号： A61K31/455 , A61K31/44 , A61K31/444 , A61K31/506 , C07B59/002 , C07B2200/05 , C07D213/56 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds having the following formula (I): or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
摘要翻译：具有下式（I）的化合物或其立体异构体或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义，可用于调节IL-12，IL-23和 /或IFNα作用于Tyk-2以引起信号转导抑制。

8. 发明申请

WO2013106641A1 THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂有用的三唑基或噻二唑基取代的吡啶化合物
公开(公告)号：WO2013106641A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/021134
申请日：2013-01-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： PAIDI, Venkatram Reddy , KUMAR, Sreekantha Ratna , NAIR, Satheesh Kesavan , BANERJEE, Abhisek , SISTLA, Ramesh , PITTS, William J. , HYNES, John
IPC分类号： C07D417/04 , C07D417/14 , A61K31/4439 , A31P37/00 , A61P29/00
CPC分类号： C07D417/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C-R 7 , are useful as kinase modulators, including IRAK-4 modulation.
摘要翻译：具有下式（I）的化合物或其对映体，非对映异构体或其药学上可接受的盐，其中X为N或C-R7，可用作激酶调节剂，包括IRAK-4调节。

9. 发明申请

WO2009155389A1 TRIAZOLOPYRIDINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：三唑吡啶化合物作为激酶抑制剂有用
公开(公告)号：WO2009155389A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/047728
申请日：2009-06-18
申请人： BRISTOL-MYERS SQUIBB COMPANY , HYNES, John
发明人： HYNES, John
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P3/00 , A61P19/00
CPC分类号： C07D471/04
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）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。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。

10. 发明申请

WO2009100171A1 FUSED HETEROARYL 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活性的融合异源调节剂及其用途
公开(公告)号：WO2009100171A1
公开(公告)日：2009-08-13
申请号：PCT/US2009/033134
申请日：2009-02-05
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , WEINSTEIN, David, S. , JIANG, Bin
发明人： DUAN, Jingwu , WEINSTEIN, David, S. , JIANG, Bin
IPC分类号： C07D491/04 , A61P3/00 , A61P29/00 , A61P37/00 , A61K31/436 , C07D491/147
CPC分类号： C07D491/147
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or taυtomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; • A is a S- to 8- membered carbocyclic ring or a S- to 8-membered heterocyclic ring; B 1 and B 2 rings are pyridyl rings, wherein the B 1 and B 2 rings are each fused to the A ring and the B 1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R 1 , R 2 , and R 4 , and the B 2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R 5 , R 7 , and R 3 J 1 , J 2 , and J 3 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, C 1 - 3 alkylene, substituted C 1-3 alkylene, C 2-4 alkenylene, 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....
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（包括代谢和炎症和免疫疾病或病症）相关的疾病或障碍，其具有以下结构：式（I）：其对映异构体，非对映异构体或其衍生物或其前药酯或其药学上可接受的盐，其中：Z是杂环基或杂芳基; A为S-至8-元碳环或S至8-元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代并且B2环任选地被一至三个相同或不同并且独立地选自R 5，R 7和R 3的基团取代，J 1，J 2和J 3在每次出现时相同或不同，并且独立地为-AlQA2- ; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是A1和A2被选择为该环A为5-至8-元碳环或杂环; R1至R11如本文所定义。

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