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11. 发明专利

IL268614D0 Aminotriazolopyridines as kinase inhibitors 未知
公开(公告)号：IL268614D0
公开(公告)日：2019-10-31
申请号：IL26861419
申请日：2019-08-09
申请人： SQUIBB BRISTOL MYERS CO , GUO JUNQING , HART AMY C , MACOR JOHN E , MERTZMAN MICHAEL E , PITTS WILLIAM J , SPERGEL STEVEN H , WATTERSON SCOTT HUNTER , ANDAPPAN MURUGAIAH SUBBAIAH MURUGAIAH , CHEN JIE , DZIERBA CAROLYN DIANE , LUO GUANGLIN , SHI JIANLIANG , SIT SING YUEN
发明人： GUO JUNQING , HART AMY C , MACOR JOHN E , MERTZMAN MICHAEL E , PITTS WILLIAM J , SPERGEL STEVEN H , WATTERSON SCOTT HUNTER , ANDAPPAN MURUGAIAH SUBBAIAH MURUGAIAH , CHEN JIE , DZIERBA CAROLYN DIANE , LUO GUANGLIN , SHI JIANLIANG , SIT SING-YUEN
IPC分类号： C07D20060101
摘要： Compounds having formula (I) (IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

12. 发明申请

WO2012154354A1 CGRP RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CGRP受体拮抗剂
公开(公告)号：WO2012154354A1
公开(公告)日：2012-11-15
申请号：PCT/US2012/032677
申请日：2012-04-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , LUO, Guanglin , DUBOWCHIK, Gene M. , MACOR, John E. , CHEN, Ling
发明人： LUO, Guanglin , DUBOWCHIK, Gene M. , MACOR, John E. , CHEN, Ling
IPC分类号： C07D487/04 , A61K31/437 , A61P25/06
CPC分类号： C07D471/04 , C07D487/04
摘要： The disclosure generally relates to the novel compounds of formula (I), including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
摘要翻译：本公开一般涉及式（I）的新化合物，其包括药学上可接受的盐，其为CGRP受体拮抗剂。本公开还涉及用于治疗CGRP相关疾病（包括偏头痛和其他头痛，神经源性血管舒张，神经源性炎症，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘）的药物组合物和方法，和慢性阻塞性肺疾病（COPD）。

13. 发明申请

WO2011137313A1 AZA-BICYCLIC AMINE N-OXIDE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGAND PRO-DRUGS 审中-公开
标题翻译： AZA-BICYCLIC胺N-氧化物作为ALPHA-7 NICOTINIC乙酰胆碱受体配体药物
公开(公告)号：WO2011137313A1
公开(公告)日：2011-11-03
申请号：PCT/US2011/034497
申请日：2011-04-29
申请人： BRISTOL-MYERS SQUIBB COMPANY , LENTZ, Kimberley A. , DENTON, Rex , COOK, James H., II , MCDONALD, Ivar M. , KING, Dalton , OLSON, Richard E. , WANG, Nenghui , MATE, Robert A. , IWUAGWU, Christiana I. , ZUSI, F. Christopher , MACOR, John E. , HILL, Matthew D. , FANG, Haiquan
发明人： LENTZ, Kimberley A. , DENTON, Rex , COOK, James H., II , MCDONALD, Ivar M. , KING, Dalton , OLSON, Richard E. , WANG, Nenghui , MATE, Robert A. , IWUAGWU, Christiana I. , ZUSI, F. Christopher , MACOR, John E. , HILL, Matthew D. , FANG, Haiquan
IPC分类号： C07D498/10 , A61K31/435 , A61K31/47 , A61K31/497 , A61K31/506 , A61P25/00
CPC分类号： C07D498/10
摘要： The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译：本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。这些化合物是用于烟碱型α7受体的配体，激动剂和部分激动剂的前药，并且可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。

14. 发明申请

WO2006026204A3 NOVEL GAMMA-LACTAMS AS BETA-SECRETASE INHIBITORS 审中-公开
标题翻译：新颖的γ-内酰胺作为β分泌酶抑制剂
公开(公告)号：WO2006026204A3
公开(公告)日：2006-07-27
申请号：PCT/US2005029669
申请日：2005-08-23
申请人： SQUIBB BRISTOL MYERS CO , THOMPSON LORIN A , BOY KENNETH M , SHI JIANLIANG , MACOR JOHN E
发明人： THOMPSON LORIN A , BOY KENNETH M , SHI JIANLIANG , MACOR JOHN E
IPC分类号： A61K31/44 , C07D401/12
CPC分类号： C07D277/42 , C07D417/12 , C07K5/06139
摘要： There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 4 , R 5 , and R 6 as defined herein,their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by beta-secretase and, more specifically, inhibit the production of alpha-beta -peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to beta-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供了一系列式（I）的新型取代的γ-内酰胺或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 4，R 5，R 5和R 5独立地选自氢，如本文所定义，其药物组合物和使用方法。这些新型化合物抑制β-分泌酶对淀粉样前体蛋白（APP）的加工，更具体地说，抑制α-β-肽的产生。本公开涉及用于治疗与β-淀粉样蛋白产生有关的神经障碍例如阿尔茨海默氏病和受抗淀粉样蛋白活性影响的其他病症的化合物。

15. 发明申请

WO2006034390A3 INHIBITORS OF 15-LIPOXYGENASE 审中-公开
标题翻译： 15-LIPOXYGENASE的抑制剂
公开(公告)号：WO2006034390A3
公开(公告)日：2006-06-01
申请号：PCT/US2005033954
申请日：2005-09-22
申请人： SQUIBB BRISTOL MYERS CO , MURUGESAN NATESAN , MACOR JOHN E , GU ZHENGXIANG , FADNIS LEENA
发明人： MURUGESAN NATESAN , MACOR JOHN E , GU ZHENGXIANG , FADNIS LEENA
IPC分类号： A61K31/4045 , C07D209/16
CPC分类号： C07D209/16 , C07D209/14 , C07D405/12 , C07D409/12
摘要： The present invention provides inhibitors of 15-LO according to Formula I, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. (I)
摘要翻译：本发明提供了根据式I的15-LO抑制剂，含有这些抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。（一世）

16. 发明申请

WO2006034390A2 INHIBITORS OF 15-LIPOXYGENASE 审中-公开
标题翻译： 15-LIPOXYGENASE的抑制剂
公开(公告)号：WO2006034390A2
公开(公告)日：2006-03-30
申请号：PCT/US2005/033954
申请日：2005-09-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , MURUGESAN, Natesan , MACOR, John, E. , GU, Zhengxiang , FADNIS, Leena
发明人： MURUGESAN, Natesan , MACOR, John, E. , GU, Zhengxiang , FADNIS, Leena
IPC分类号： A61K31/405 , C07D209/18
CPC分类号： C07D209/16 , C07D209/14 , C07D405/12 , C07D409/12
摘要： The present invention provides inhibitors of 15-LO according to Formula I, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. (I)
摘要翻译：本发明提供了根据式I的15-LO的抑制剂，含有这些抑制剂的药物组合物以及使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。（I）

17. 发明申请

WO2004026237A2 COMPOUNDS FOR THE TREATMENT OF PREMATURE EJACULATION 审中-公开
标题翻译：化合物治疗早泄性皮炎
公开(公告)号：WO2004026237A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/029055
申请日：2003-09-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , DENHART, Derek, John , DITTA, Jonathan, L. , KING, Dalton , MACOR, John, E. , MARCIN, Lawrence, R. , MATTSON, Ronald, J. , MENG, Zhaoxing
发明人： DENHART, Derek, John , DITTA, Jonathan, L. , KING, Dalton , MACOR, John, E. , MARCIN, Lawrence, R. , MATTSON, Ronald, J. , MENG, Zhaoxing
IPC分类号： A61K
CPC分类号： C07D209/14
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds [INSERT CHEMICAL STRUCTURE HERE] (I) useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐或溶剂化物和药学上可接受的制剂，其包含用于治疗早泄的所述化合物[插入化学结构式（I）]（I）抑郁症，注意力缺陷多动障碍，强迫症，创伤后应激障碍和药物滥用障碍。

18. 发明申请

WO2003104236A1 CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CALCITONIN基因相关肽受体拮抗剂
公开(公告)号：WO2003104236A1
公开(公告)日：2003-12-18
申请号：PCT/US2003/016576
申请日：2003-05-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHATURVEDULA, Prasad, V. , CHEN, Ling , CIVIELLO, Rita , CONWAY, Charles, Mark , DEGNAN, Andrew, P. , DUBOWCHIK, Gene, M. , HAN, Xiaojun , KARAGEORGE, George, N. , LUO, Guanglin , MACOR, John, E. , POINDEXTER, Graham , VIG, Shikha
发明人： CHATURVEDULA, Prasad, V. , CHEN, Ling , CIVIELLO, Rita , CONWAY, Charles, Mark , DEGNAN, Andrew, P. , DUBOWCHIK, Gene, M. , HAN, Xiaojun , KARAGEORGE, George, N. , LUO, Guanglin , MACOR, John, E. , POINDEXTER, Graham , VIG, Shikha
IPC分类号： C07D487/14
CPC分类号： A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/106 , A01K2267/0306 , A61K49/0008 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D487/04 , C07D487/14 , C07D491/10 , C12N15/8509 , G01N33/566 , G01N2500/10 , G01N2800/2807
摘要： The presnt invention relates to compounds of Formula (I), as antagonists of calcitonin gene-related peptide receptors ("CGRP-receptor"), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译：本发明涉及作为降钙素基因相关肽受体（“CGRP受体”）的拮抗剂的式（I）化合物，包含它们的药物组合物，鉴定它们的方法，使用它们的治疗方法及其在治疗中的用途治疗神经源性血管舒张，神经源性炎症，偏头痛和其他头痛，热损伤，循环休克，与绝经相关的潮红，气道炎症性疾病如哮喘和慢性阻塞性肺疾病（COPD）以及其他可治疗的病症通过CGRP受体的拮抗作用。

19. 发明申请

WO1995006636A1 5-ARYLINDOLE DERIVATIVES 审中-公开
公开(公告)号：WO1995006636A1
公开(公告)日：1995-03-09
申请号：PCT/IB1994000195
申请日：1994-07-04
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D209/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07F7/2208
摘要： Compounds of formula (I), wherein A, B, D, E, and F are each independently nitrogen or carbon; R1 is hydrogen, C1 to C6 alkyl, -(CH2)nR7, or C1 to C3 alkyl-aryl; R2, R3, R4, R5, and R6 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkyl-aryl, halogen, cyano, nitro, -(CH2)mNR8R9, -(CH2)mOR9, -SR9, -SO2NR8R9, -(CH2)mNR8SO2R9, -(CH2)mNR8CO2R9, -(CH2)mNR8COR9, -(CH2)mCONR7R9, or -(CH2)mCO2R9; R2 and R3, R3 and R4, R4 and R5, and R5 and R6 may be taken together to form a 5- to 7-membered alkyl ring, a 6-membered aryl ring, a 5- to 7-membered heteroalkyl ring, having 1 heteroatom of N, O, or S, or a 5- to 6-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R7 is -OR10, -SR10, -SO2NR10R11, -NR10SO2R11, -NR10CO2R11, -NR10COR11, -CONR10R11, or -CO2R10; R8, R9, R10 and R11 are each independently hydrogen, C1 to C6 alkyl, or C1 to C3 alkyl-aryl; m is 0, 1, or 2; n is 2, 3, or 4; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are each independently phenyl or substituted phenyl, wherein said substituted phenyl may be substituted with 1 to 3 of C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, or C1 to C4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders and are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hermicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
摘要翻译：式（I）的化合物，其中A，B，D，E和F各自独立地为氮或碳; R1是氢，C1-C6烷基， - （CH2）nR7或C1-C3烷基 - 芳基; R 2，R 3，R 4，R 5和R 6各自独立地为氢，C 1至C 6烷基，芳基，C 1至C 3烷基 - 芳基，卤素，氰基，硝基， - （CH 2）m NR 8 R 9， - （CH 2）mOR 9，（CH2）mNR8CO2R9， - （CH2）mNR8COR9， - （CH2）mCONR7R9或 - （CH2）mCO2R9; - （CH2）mNR8R9， - （CH2）mNR8SO2R9， - R 2和R 3，R 3和R 4，R 4和R 5以及R 5和R 6可以一起形成5-至7-元烷基环，6-元芳基环，5-至7-元杂烷基环，其具有 1个N，O或S的杂原子，或具有1或2个N，O或S杂原子的5-至6-元杂芳基环; R7是-OR10，-SR10，-SO2NR10R11，-NR10SO2R11，-NR10CO2R11，-NR10COR11，-CONR10R11或-CO2R10; R 8，R 9，R 10和R 11各自独立地为氢，C 1至C 6烷基或C 1至C 3烷基 - 芳基; m为0,1或2; n为2,3或4; 上述芳基和上述烷基 - 芳基的芳基部分各自独立地为苯基或取代的苯基，其中所述取代的苯基可以被1至3个C 1 -C 4烷基，卤素，羟基，氰基，甲酰氨基，硝基或C 1〜C 4烷氧基，及其药学上可接受的盐。这些化合物可用于治疗偏头痛和其他疾病，并且是新的。这些化合物是有用的精神治疗药物，并且是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性乳头瘤和头痛相关血管疾病和由血清素能神经传递缺陷引起的其他疾病。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

20. 发明申请

WO1993020073A1 INDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
标题翻译：单独使用衍生物作为5-HT1激动剂
公开(公告)号：WO1993020073A1
公开(公告)日：1993-10-14
申请号：PCT/US1993001967
申请日：1993-03-10
申请人： PFIZER INC. , MACOR, John, E. , WYTHES, Martin, J.
发明人： PFIZER INC.
IPC分类号： C07D413/14
CPC分类号： C07D403/06 , C07D403/14 , C07D413/10 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) where W is (i), (ii), (iii), (iv), (v), (vi), or (vii); n is 0, 1 or 2; m is 0, 1, 2, or 3; Y and G are each independently oxygen or sulfur; Z is -O-, -S-, -NH-, or -CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or -Q-R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, -COR9, -CO2R9, -CONR9R10, -OR9, -SO2NR9R10, or -S(O)qR9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three-to seven-membered alkyl ring or a three-to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, -OR12, or -NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkylaryl; q is 0, 1, or 2; a first chiral carbon is designated by an asterisk; a second chiral carbon is designated by #; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders are new. These compounds are useful phsychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
摘要翻译：其中W为（i），（ii），（iii），（iv），（v），（vi）或（vii）的式（I） n为0,1或2; m为0,1,2或3; Y和G各自独立地为氧或硫; Z是-O - ， - S - ， - NH-或-CH 2; R1是氢，C1至C8烷基，被一个羟基取代的C1至C8烷基，C3至C8烯基，C3至C8炔基，芳基，C1至C3烷基芳基，C1至C3烷基杂芳基或-Q-R4; R2和R3各自独立地为氢，C1至C6烷基，芳基，C1至C3烷基芳基或C1至C3烷基杂芳基; R 4是氰基，三氟甲基，-COR 9，-CO 2 R 9，-CONR 9 R 10，-OR 9，-SO 2 NR 9 R 10或-S（O）q R 9; R 9和R 10各自独立地为氢，C 1至C 8烷基，C 1至C 3烷基芳基，芳基或R 9和R 10可以一起取代形成三至七元烷基环或三至七元杂烷基环， 1个O的杂原子; Q为C1至C3烷基; R 11是氢，-OR 12或-NHCOR 12; R 12是氢，C 1至C 6烷基，芳基或C 1至C 3烷基芳基; q是0,1或2; 第一手性碳由星号表示; 第二个手性碳由＃指定; 并且上述芳基和上述烷基 - 芳基的芳基部分独立地选自苯基和取代的苯基，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基，甲酰胺基，硝基和C1至C4烷氧基，及其药学上可接受的盐。这些化合物可用于治疗偏头痛，其他疾病是新的。这些化合物是有用的精神治疗药物，是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性血尿素和头痛相关血管疾病和由血清素能神经传递缺陷引起的其他疾病。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

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