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1. 发明申请

WO2010042682A1 AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：阿莫洛芬酮麦拉宁浓缩HORMONE受体-1拮抗剂
公开(公告)号：WO2010042682A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059941
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WASHBURN, William N. , RENDUCHINTALA, Kishore V. , SRIDHAR, Radhakrishnan
发明人： DEVASTHALE, Pratik , WASHBURN, William N. , RENDUCHINTALA, Kishore V. , SRIDHAR, Radhakrishnan
IPC分类号： C07D487/04 , A61K31/53 , A61P3/04
CPC分类号： C07D487/04 , A61K31/53 , A61K31/541
摘要： The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I, wherein R 1 , is selected from the group consisting of monocyclic aryl or monocyclic heteroaryl; W is selected from the group consisting of a direct bond, -O-, and -N(R 6 )-; provided that if W is a direct bond, D is a cyclic amine that is attached to A via the nitrogen atom of the cyclic amine; D is selected from the group consisting of a direct bond, substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkylalkyl, and 4- to 6-membered cyclic amines, provided that if D is a direct bond, R 2a , R 2b , and R 2c must be selected from H, alkyl, or cycloalkyl; E and G are independently N or CH provided that both are not N; R 1 is substituted or unsubstituted phenyl or substituted or unsubstituted monocyclic heteroaryl; R 2a , R 2b , and R 2c are independently selected from the group consisting of hydrogen, halo, cyano, hydroxyl, -NR 5 R 5a , -SO 2 R 34 , -CO 2 R 35 -NR 5 CO 2 R 21 , -NR 5 COR 21 , substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, substituted or unsubstituted 4- to 6-membered cyclic amines wherein said cyclic amine is optionally substituted with -OH, carbonylamino, alkoxycarbonylamino, or at least one of R 2a , R 2b , and R 2c is a prodrug moiety selected from amino acid esters or phosphoric acid esters wherein said amino acid ester has the formula -OC(O)CH(NH 2 )R 31 , wherein R 31 is H or C 1 to C 4 alkyl; or any two of R 2a , R b , or R 2c , may be taken together to form a ring; R 3 and R 3a are each independently selected from the group consisting of hydrogen, hydroxyl, lower alkoxy, halo, CN, substituted or unsubstituted C 1 to C 4 alkyl, perfluoroalkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkoxy, amino, alkylamino, dialkylamino, and aminoalkyl, wherein R 3 or R 3a and D may optionally be taken together with the atoms to which they are attached to form a 5- to 7-membered ring; R 5 and R 5a are the same or different and are independently selected from the group consisting of hydrogen, substituted or unsubstituted lower alkyl, hydroxyalkyl, hydroxyalkylcycloalkyl, substituted or unsubstituted heterocycloalkyl, acyl, alkoxycarbonyl, carboxyalkyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted cycloalkylalkyl, wherein the R 5 and R 5a groups and the N atom to which they are attached may form a ring; R 21 and R 31 are each H or C 1 to C 4 alkyl; R 34 is alkyl; R 35 is H or alkyl; and R 6 is selected from the group consisting of H, C 1 to C 4 alkyl and C 3 to C 7 cycloalkyl.
摘要翻译：本申请提供了可用作MCHR1拮抗剂的化合物，特别是用于治疗肥胖症，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式，其中R 1选自单环芳基或单环杂; W选自直接键，-O-和-N（R6） - ; 条件是如果W是直接键合，D是通过环胺的氮原子连接到A的环胺; D选自直链，取代或未取代的C1至C4烷基，取代或未取代的C3至C7环烷基，环烷基烷基和4-至6-元环胺，条件是如果D为直接键，则R2a R2b和R2c必须选自H，烷基或环烷基; E和G独立地为N或CH，条件是两者不是N; R1是取代或未取代的苯基或取代或未取代的单环杂芳基; R2a，R2b和R2c独立地选自氢，卤素，氰基，羟基，-NR5R5a，-SO2R34，-CO2R35 -NR5CO2R21，-NR5COR21，取代或未取代的C1至C4烷基，取代或未取代的C3至C7 环烷基，取代或未取代的4-至6-元环胺，其中所述环胺任选被-OH，羰基氨基，烷氧基羰基氨基或R 2a，R 2b和R 2c中的至少一个取代为选自氨基酸酯或磷酸酯酸酯，其中所述氨基酸酯具有式-OC（O）CH（NH 2）R 31，其中R 31是H或C 1至C 4烷基; 或R 2a，R b或R 2c中的任何两个可以一起形成环; R3和R3a各自独立地选自氢，羟基，低级烷氧基，卤素，CN，取代或未取代的C1至C4烷基，全氟烷基，取代或未取代的C3至C7环烷基，环烷氧基，氨基，烷基氨基，二烷基氨基和氨基烷基，其中R3或R3a和D可以任选地与它们所连接的原子一起形成5-至7-元环; R5和R5a相同或不同，并且独立地选自氢，取代或未取代的低级烷基，羟基烷基，羟基烷基环烷基，取代或未取代的杂环烷基，酰基，烷氧基羰基，羧基烷基，取代或未取代的环烷基和取代或未取代的环烷基烷基其中R5和R5a基团和它们所连接的N原子可以形成环; R 21和R 31各自为H或C 1至C 4烷基; R34是烷基; R35是H或烷基; 并且R 6选自H，C 1至C 4烷基和C 3至C 7环烷基。

2. 发明申请

WO2003040114A1 SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：替代的酸衍生物作为抗真菌剂和抗菌药物和方法有用
公开(公告)号：WO2003040114A1
公开(公告)日：2003-05-15
申请号：PCT/US2002/035704
申请日：2002-11-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , JEON, Yoon, T.
发明人： DEVASTHALE, Pratik , JEON, Yoon, T.
IPC分类号： C07D263/56
CPC分类号： C07D413/06 , A61K31/421 , A61K45/06 , A61K2300/00
摘要： Compounds are provided which have the structure (I) wherein Q is C or N, X 1 is CH or N and, A, E, M, G, X 2 , X 3 , X 4 , R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
摘要翻译：提供具有结构（I）的化合物，其中Q是C或N，X 1是CH或N，且A，E，M，G，X 2，X 3，X 4，R 1，R 2， R 2a，R 2c，R 3，Y，x，m和n如本文所定义，该化合物可用作抗糖尿病，降血脂症和抗肥胖剂。

3. 发明申请

WO2021226002A1 SMALL MOLECULE INHIBITORS OF GALECTIN-3 审中-公开
公开(公告)号：WO2021226002A1
公开(公告)日：2021-11-11
申请号：PCT/US2021/030540
申请日：2021-05-04
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： JALAGAM, Prasada Rao , NAIR, Satheesh Kesavan , NARA, Susheel Jethanand , PANDA, Manoranjan , DEVASTHALE, Pratik , REGUEIRO-REN, Alicia
IPC分类号： C07D407/14 , C07H17/02 , A61P29/00 , A61K31/4192
摘要： The present disclosure relates to compounds of Formula (I) or Formula (II), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

4. 发明申请

WO2013082345A1 ARYL DIHYDROPYRIDINONE AND PIPERIDINONE AS MGAT2 INHIBITORS 审中-公开
标题翻译： ARYL DIHYDROPRIDINONE和PIPERIDINONE作为MGAT2抑制剂
公开(公告)号：WO2013082345A1
公开(公告)日：2013-06-06
申请号：PCT/US2012/067173
申请日：2012-11-30
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： TURDI, Huji , HANGELAND, Jon J. , LAWRENCE, R. Michael , CHENG, Dong , AHMAD, Saleem , MENG, Wei , BRIGANCE, Robert Paul , DEVASTHALE, Pratik
IPC分类号： C07D211/86 , C07D211/90 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14 , C07F9/40 , A61K31/4418 , A61K31/4427 , A61P3/00
CPC分类号： A61K31/438 , A61K31/4418 , A61K31/4439 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D211/86 , C07D211/90 , C07D221/20 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/4006 , C07F9/5352 , C07F9/598
摘要： The present invention provides compounds of Formula (I), or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
摘要翻译：本发明提供式（I）化合物或其立体异构体或其药学上可接受的盐，其中所有变量如本文所定义。这些化合物是可用作药物的单酰基甘油酰基转移酶2型（MGAT2）抑制剂。

5. 发明申请

WO2004004665A3 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
公开(公告)号：WO2004004665A3
公开(公告)日：2004-01-15
申请号：PCT/US2003/022149
申请日：2003-07-02
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
发明人： CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
IPC分类号： C07D403/06
摘要： Formula, wherein Z 1 is (CH 2 ) q or C=O; Z 2 is (CH 2 ) p or C=O; D is -CH= or C=O or (CH 2 ) m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH 2 ) x where x is 1 to 5, or A is (CH 2 ) x 1 , where x 1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH 2 ) x 2 -O-(CH 2 ) x 3 - where x 2 is 0 to 5 and x 3 is 0 to 5, provided that at least one of x 2 and x 3 is other than 0; B is a bond or is (CH 2 ) x 4 where x 4 is 1 to 5; X is CH or N; X 2 is C, N, O or S; X 3 is C, N, O or S; X 4 is C, N, O or S; X 5 is C, N, O or S; X 6 is C, N, O or S; provided that at least one of X 2 , X 3 , X 4 X 5 and X 6 is N; and at least one of X 2 , X 3 , X 4 X 5 and X 6 is C. R 1 is H or alkyl; R 2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R 2a , R 2b and R 2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R 3 , E, Z and Y are as defined herein.

6. 发明申请

WO2021231243A1 SMALL MOLECULE INHIBITORS OF GALECTIN-3 审中-公开
公开(公告)号：WO2021231243A1
公开(公告)日：2021-11-18
申请号：PCT/US2021/031479
申请日：2021-05-10
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： JALAGAM, Prasada Rao , NARA, Susheel Jethanand , PANDA, Manoranjan , NATESAN, Murugesan , DEVASTHALE, Pratik
IPC分类号： C07D405/04 , C07D405/14 , C07D413/14 , C07D487/04 , C07D487/08 , A61P1/16 , A61P9/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61K31/4192 , C07H19/056
摘要： The present disclosure relates to compounds of Formula (I), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions. (Formula (I))

7. 发明申请

WO2018089358A1 AZOLE AMIDES AND AMINES AS ALPHA V INTEGRIN INHIBITORS 审中-公开
标题翻译： AZOLE酰胺和胺作为ALPHA V INTEGRIN抑制剂
公开(公告)号：WO2018089358A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060390
申请日：2017-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DEVASTHALE, Pratik , WANG, Wei
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/00
摘要： The present invention provides compounds of Formula (I): (Formula (I)), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to αv-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
摘要翻译：本发明提供式（I）化合物：（式（I））或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中所有变量如本文所定义。这些化合物是含αv整联蛋白的抑制剂。本发明还涉及包含这些化合物的药物组合物以及通过使用所述化合物治疗与包含αv的整联蛋白失调相关的疾病，病症或病症（例如病理性纤维化，移植排斥，癌症，骨质疏松症和炎性病症）的方法和药物组合物。

8. 发明申请

WO2018089353A1 3-SUBSTITUTED PROPIONIC ACIDS AS ALPHA V INTEGRIN INHIBITORS 审中-公开
标题翻译： 3-取代丙酸作为αV整合蛋白抑制剂
公开(公告)号：WO2018089353A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060376
申请日：2017-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , DEVASTHALE, Pratik , YE, Xiang-Yang , SELVAKUMAR, Kumaravel , DHANUSU, Suresh , BALASUBRAMANIAN, Palanikumar , GUERNON, Leatte R. , CIVIELLO, Rita , HAN, Xiaojun , PARKER, Michael F. , JACUTIN-PORTE, Swanee E.
IPC分类号： C07D471/04 , C07D491/04 , A61K31/4375 , A61P11/00
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to α ν - containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ay- containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
摘要翻译：本发明提供式（I）的化合物：或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中所有变量如本文所定义。这些化合物是含有αvβ的整联蛋白的拮抗剂。本发明还涉及包含这些化合物的药物组合物以及通过使用所述化合物治疗与含有ay的整联蛋白失调相关的疾病，病症或病症（例如病理性纤维化，移植排斥，癌症，骨质疏松症和炎性病症）的方法和药物组合物。

9. 发明申请

WO2010047956A1 AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：阿莫洛林粉红素浓缩激素受体-1拮抗剂
公开(公告)号：WO2010047956A1
公开(公告)日：2010-04-29
申请号：PCT/US2009/059924
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
发明人： DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
IPC分类号： C07D487/04 , A61K31/4015 , A61P3/00
CPC分类号： C07D487/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) including all pharmaceutically acceptable salts and stereoisomers thereof: wherein A is a monocyclic aryl or monocyclic heteroaryl; W is a direct bond, -0-, or -N(R 6 )-, provided that if W is a direct bond, D must be a cyclic amine that is attached to A via the nitrogen atom of said cyclic amine; D is a direct bond, substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkylalkyl, or a 4 to 6 membered cyclic amine; B and E are independently N or CH provided that both are not CH;
摘要翻译：本申请提供了包括其所有药学上可接受的盐和立体异构体的根据式（I）的所有立体异构体，溶剂化物，前药和药学上可接受的形式的化合物：其中A是单环芳基或单环杂芳基; W是直接键，-O-或-N（R6） - ，条件是如果W是直接键，则D必须是通过所述环胺的氮原子连接到A的环胺; D是直接键，取代或未取代的C1至C4烷基，取代或未取代的C3至C7环烷基，环烷基烷基或4至6元环胺; B和E独立地为N或CH，条件是两者都不是CH;

10. 发明申请

WO2009146365A1 HYDROXY SUBSTITUTED THIENO PYRIMIDINONES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：羟基取代的三苯基嘧啶酮作为富含浓度的HORMONE受体-1拮抗剂的MELANIN
公开(公告)号：WO2009146365A1
公开(公告)日：2009-12-03
申请号：PCT/US2009/045452
申请日：2009-05-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William, N. , AHMAD, Saleem , DEVASTHALE, Pratik , ROBL, Jeffrey, A. , GOSWAMI, Animesh , GUO, Zhiwei , PATEL, Ramesh, N.
发明人： WASHBURN, William, N. , AHMAD, Saleem , DEVASTHALE, Pratik , ROBL, Jeffrey, A. , GOSWAMI, Animesh , GUO, Zhiwei , PATEL, Ramesh, N.
IPC分类号： C07D495/04 , A61K31/522 , A61P5/00 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供具有以下式IA和IB的化合物，其可用作MCHR1拮抗剂，并且包括前药及其药学上可接受的盐。

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