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51. 发明申请

WO2007109456A3 SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES AS DUAL ANGIOTENSIN ENDOTHELIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为双抗血管紧张素内皮素受体拮抗剂的替代联苯噻唑磺酰胺
公开(公告)号：WO2007109456A3
公开(公告)日：2007-12-06
申请号：PCT/US2007063862
申请日：2007-03-13
申请人： PHARMACOPEIA INC , MURUGESAN NATESAN , EWING WILLIAM , GU ZHENGXIANG , YU GUIXUE , MACOR JOHN E
发明人： MURUGESAN NATESAN , EWING WILLIAM , GU ZHENGXIANG , YU GUIXUE , MACOR JOHN E
IPC分类号： C07D413/12 , A61K31/42 , C07D413/14 , C07D487/04
CPC分类号： C07D413/12 , C07D261/16
摘要： The present invention provides N-isoxazolyl biphenyl sulfonamide compounds of Formula (I), wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. These compounds are dual angiotensin and endothelin receptor antagonists, and as such are useful in the treatment of conditions such as hypertension and other diseases.
摘要翻译：本发明提供式（I）的N-异恶唑基联苯磺酰胺化合物，其中R 1，R 2，R 3，R SUP > 4 和R 5 5如本文所定义。这些化合物是双重血管紧张素和内皮素受体拮抗剂，因此可用于治疗诸如高血压等疾病的病症。

52. 发明申请

WO2006099352A1 NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS 审中-公开
标题翻译：新的ISOPHTHALATEATE作为分子抑制剂
公开(公告)号：WO2006099352A1
公开(公告)日：2006-09-21
申请号：PCT/US2006/008994
申请日：2006-03-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , THOMPSON III, Lorin, A. , BOY, Kenneth, M. , SHI, Jianliang , MACOR, John, E.
发明人： THOMPSON III, Lorin, A. , BOY, Kenneth, M. , SHI, Jianliang , MACOR, John, E.
IPC分类号： C07D207/12 , A61K31/401 , A61P25/28
CPC分类号： C07D265/30 , C07D207/09 , C07D207/12 , C07D207/27 , C07D265/32 , C07D403/12 , C07D413/12 , C07D413/14
摘要： There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R 3 , 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 β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供了一系列取代的式（I）的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐，其中W，R 3，R 5和R 6如本文所定义，其药物组合物和使用方法。这些新型化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地，抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默氏病和受抗淀粉样蛋白活性影响的其它病症。

53. 发明申请

WO2005065779A1 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：WO2005065779A1
公开(公告)日：2005-07-21
申请号：PCT/US2003/038799
申请日：2003-12-05
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEGNAN, Andrew, P. , CHEN, Ling , CIVIELLO, Rita , DUBOWCHIK, Gene, M. , HAN, Xiaojun , JIANG, Xiang, Jun, J. , MACOR, John, E. , TORA, George
发明人： DEGNAN, Andrew, P. , CHEN, Ling , CIVIELLO, Rita , DUBOWCHIK, Gene, M. , HAN, Xiaojun , JIANG, Xiang, Jun, J. , MACOR, John, E. , TORA, George
IPC分类号： A61P25/06
CPC分类号： C07D471/04 , C07D209/08 , C07D231/56 , C07D249/18 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/10 , C07D491/10
摘要： The present 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”）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治疗中的用途神经源性血管舒张，神经源性炎症，偏头痛和其他头痛，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘和慢性阻塞性肺疾病（COPD）以及其他治疗可以通过 CGRP受体的拮抗作用。

54. 发明申请

WO2005056550A2 HETEROCYCLIC ANTI-MIGRAINE AGENTS 审中-公开
标题翻译：杂环抗原代谢物
公开(公告)号：WO2005056550A2
公开(公告)日：2005-06-23
申请号：PCT/US2004/040721
申请日：2004-12-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , LUO, Guanglin , CHEN, Ling , DEGNAN, Andrew, P. , DUBOWCHIK, Gene, M. , MACOR, John, E. , TORA, George, O. , CHATURVEDULA, Prasad, V.
发明人： LUO, Guanglin , CHEN, Ling , DEGNAN, Andrew, P. , DUBOWCHIK, Gene, M. , MACOR, John, E. , TORA, George, O. , CHATURVEDULA, Prasad, V.
IPC分类号： C07D413/00
CPC分类号： C07D471/10 , C07D401/14 , C07D413/14
摘要： The present 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”）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治疗中的用途神经源性血管舒张，神经源性炎症，偏头痛和其他头痛，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘和慢性阻塞性肺疾病（COPD）以及其他治疗可以通过 CGRP受体的拮抗作用。

55. 发明申请

WO2004026236A3 CYCLOPENTYL INDOLE DERIVATIVES 审中-公开
标题翻译：环丙基吲哚衍生物
公开(公告)号：WO2004026236A3
公开(公告)日：2004-06-03
申请号：PCT/US0328989
申请日：2003-09-15
申请人： SQUIBB BRISTOL MYERS CO , KING DALTON , DESKUS JEFFREY A , MACOR JOHN E , MATTSON RONALD J , MENG ZHAOXING , SLOAN CHARLES P
发明人： KING DALTON , DESKUS JEFFREY A , MACOR JOHN E , MATTSON RONALD J , MENG ZHAOXING , SLOAN CHARLES P
IPC分类号： A61K20060101 , A61K31/405 , C07D209/04 , C07D209/30 , C07D209/40 , C07D209/42 , C07D403/08
CPC分类号： C07D209/30 , C07D209/42 , C07D403/08
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 of Formula (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合物和药学上可接受的制剂，其包含用于治疗早泄，抑郁症，注意力缺陷多动症，强迫症，创伤后应激障碍和物质滥用障碍。

56. 发明申请

WO2002069905A3 CO-ADMINISTRATION OF MELANOCORTIN RECEPTOR AGONIST AND PHOSPHODIESTERASE INHIBITOR FOR TREATMENT OF CYCLIC-AMP ASSOCIATED DISORDERS 审中-公开
公开(公告)号：WO2002069905A3
公开(公告)日：2002-09-12
申请号：PCT/US2002/006805
申请日：2002-03-04
申请人： BRISTOL-MYERS SQUIBB COMPANY , MACOR, John, E. , CARLSON, Kenneth, E.
发明人： MACOR, John, E. , CARLSON, Kenneth, E.
IPC分类号： A61K31/445
摘要： Co-administration of a melanocortin receptor agonist, particularly an MC-1R or MC-4R agonist, and a cAMP phosphodiesterase inhibitor is described for modulating levels of cyclic adenoise 3',5' monophosphate (cAMP) in a mammal. The inventive co-administration is useful in the treatment of diseases affected by activity of cAMP-PDE, including without limitation, inflammatory bowel disease, irritable bowel syndrome, rheumatoid arthritis, osteoarthritis, pancreatis, psoriasis, migraine, Alzheimer's Disease, Parkinson's disease, transplant rejection, asthma, acute respiratory distress syndrome, chronic obstructive pulmonary disease, stroke, and neurodegeneration of, and consequences of traumatic brain injury.

57. 发明申请

WO1996000720A1 ARYL AND HETEROARYL ALKOXYNAPHTHALENE DERIVATIVES 审中-公开
标题翻译： ARYL和HETEROARYL ALKOXYNPHTHALENE DERIVATIVES
公开(公告)号：WO1996000720A1
公开(公告)日：1996-01-11
申请号：PCT/IB1995000381
申请日：1995-05-18
申请人： PFIZER INC. , CHENARD, Bertrand, L. , DESAI, Kishor, A. , HOWARD, Harry, R., Jr. , MACOR, John, E. , SHENK, Kevin, D.
发明人： PFIZER INC.
IPC分类号： C07C271/06
CPC分类号： C07D213/30 , C07D209/34 , C07D213/64 , C07D213/85 , C07D215/14 , C07D237/14 , C07D239/34 , C07D239/42 , C07D257/04 , C07D263/56 , C07D271/06 , C07D271/107 , C07D277/24 , C07D277/64 , C07D295/155 , C07D333/28 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I) wherein R , R , R , R , R , R and R are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.
摘要翻译：其中R 1，R 2，R 4，R 23，R 24，R 25和R 26的式（I）化合物如说明书中所定义。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）激动剂和拮抗剂。

58. 发明申请

WO1993021180A1 ACYLAMINOINDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
公开(公告)号：WO1993021180A1
公开(公告)日：1993-10-28
申请号：PCT/US1993001807
申请日：1993-03-04
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D403/06
CPC分类号： C07D403/06 , C07D403/14
摘要： Compounds of formula (I) where n is 0, 1, or 2; m is 0 or 1; Y and W are each an amino acid residue; R1 is hydrogen, C1-C6 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, aryl, C1-C3 alkylaryl, or C1-C3 alkylheteroaryl, and -(CH2)pR3; R2 is CF3, C1-C6 alkyl, aryl, C1-C3 alkylaryl, and -OR5; R3 is cyano, trifluoromethyl, or -OR4; R4 is hydrogen, C1-C6 alkyl, C1-C3 alkylaryl, or aryl; R5 is C1-C6 alkyl, C1-C3 alkylaryl, or aryl; R6 is hydrogen, -OR7, or -NHCOR7; R7 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkyl-aryl; p is 1, 2, or 3; 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, carboxamide, nitro, and C1 to C4 alkoxy and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. 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 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n为0,1或2的式（I）化合物; m为0或1; Y和W各自为氨基酸残基; R 1是氢，C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基，芳基，C 1 -C 3烷基芳基或C 1 -C 3烷基杂芳基，和 - （CH 2）p R 3; R2是CF3，C1-C6烷基，芳基，C1-C3烷基芳基和-OR5; R3是氰基，三氟甲基或-OR4; R4是氢，C1-C6烷基，C1-C3烷基芳基或芳基; R5是C1-C6烷基，C1-C3烷基芳基或芳基; R6是氢，-OR7或-NHCOR7; R 7为氢，C 1至C 6烷基，芳基或C 1至C 3烷基 - 芳基; p为1,2或3; 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，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和其他疾病。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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