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1. 发明申请

WO2005105092A3 3,3-DISUBSTITUTED TETRAHYDROPYRANYL CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
公开(公告)号：WO2005105092A3
公开(公告)日：2005-11-10
申请号：PCT/US2005/013752
申请日：2005-04-22
申请人： MERCK & CO., INC. , YANG, Lihu , MILLS, Sander, G. , SHANKARAN, Kothandaraman
发明人： YANG, Lihu , MILLS, Sander, G. , SHANKARAN, Kothandaraman
IPC分类号： C07D471/02 , A61K31/435
摘要： Compounds of Formula I (wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 15 , R 16 , R 17 , R 18 , Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

2. 发明申请

WO2005105092A2 3,3-DISUBSTITUTED TETRAHYDROPYRANYL CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译： 3,5-取代的四氢叶酸环糊精酰化酶受体活性的调节剂
公开(公告)号：WO2005105092A2
公开(公告)日：2005-11-10
申请号：PCT/US2005013752
申请日：2005-04-22
申请人： MERCK & CO INC , YANG LIHU , MILLS SANDER G , SHANKARAN KOTHANDARAMAN
发明人： YANG LIHU , MILLS SANDER G , SHANKARAN KOTHANDARAMAN
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of Formula I (wherein n, R , R , R , R , R , R , R , R , R , R , R , R , R , R , Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：式I化合物（其中n，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8， R 10，R 15，R 16，R 17，R 18，Y 18和Z如本文所定义），其是趋化因子受体活性的调节剂，并且可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

3. 发明申请

WO1996014844A1 CYCLIC AMIDINE ANALOGS AS INHIBITORS OF NITRIC OXIDE SYNTHASE 审中-公开
标题翻译：作为氮氧化物合成酶抑制剂的循环胺类似物
公开(公告)号：WO1996014844A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014812
申请日：1995-11-13
申请人： MERCK & CO., INC. , GUTHIKONDA, Ravindra, N. , GRANT, Stephan, K. , MACCOSS, Malcolm , SHAH, Shrenik, K. , SHANKARAN, Kothandaraman , CALDWELL, Charles, G. , DURETTE, Philippe, L.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/44
CPC分类号： C07D215/38 , C07D207/22 , C07D211/72 , C07D211/74 , C07D211/78 , C07D221/04 , C07D223/12 , C07D225/02 , C07D241/06 , C07D241/44 , C07D243/08 , C07D243/14 , C07D265/36 , C07D267/10 , C07D279/12 , C07D279/16 , C07D471/04 , C07D487/04 , C07D491/04
摘要： Disclosed herein are the heterocyclic compounds and pharmaceutically acceptable salts thereof which have been found to be useful in the treatment of nitric oxide synthase mediated diseases and disorders.
摘要翻译：本文公开了已被发现可用于治疗一氧化氮合酶介导的疾病和病症的杂环化合物及其药学上可接受的盐。

4. 发明申请

WO2004041161A3 TETRAHYDROPYRANYL CYCLOPENTYL BENZYLAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：化合物受体活性的四氢环戊二烯基苯甲酰胺调节剂
公开(公告)号：WO2004041161A3
公开(公告)日：2005-03-24
申请号：PCT/US0333972
申请日：2003-10-24
申请人： MERCK & CO INC , BUTORA GABOR , MILLS SANDER G , PASTERNAK ALEXANDER , SHANKARAN KOTHANDARAMAN , YANG LIHU , ZHOU CHANGYOU , GOBLE STEPHEN D
发明人： BUTORA GABOR , MILLS SANDER G , PASTERNAK ALEXANDER , SHANKARAN KOTHANDARAMAN , YANG LIHU , ZHOU CHANGYOU , GOBLE STEPHEN D
IPC分类号： A61K31/00 , C07C237/24 , C07D211/58 , C07D211/96 , C07D305/08 , C07D307/22 , C07D309/14 , C07D311/00 , C07D311/02 , C07D311/68 , C07D311/74 , C07D313/04 , C07D319/06 , C07D333/36 , C07D335/02 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D493/08 , C07D498/04 , A61K31/351 , C07D257/04 , C07D263/48 , C07D491/02
CPC分类号： C07D311/00 , C07C237/24 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07D211/58 , C07D211/96 , C07D305/08 , C07D307/22 , C07D309/14 , C07D311/02 , C07D311/68 , C07D311/74 , C07D313/04 , C07D319/06 , C07D333/36 , C07D335/02 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/08
摘要： The present invention is directed to compounds of the formula (I) (wherein R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及式（I）的化合物（其中R 1，R 2，R 3，R 4，R 5，R 6，R 7， R 8，R 9，R 10，R 11，R 27，R 28，R 29，R 30，R 31，X，m，n 并且虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

5. 发明申请

WO2004041161A2 TETRAHYDROPYRANYL CYCLOPENTYL BENZYLAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：化合物受体活性的四氢环戊二烯基苯甲酰胺调节剂
公开(公告)号：WO2004041161A2
公开(公告)日：2004-05-21
申请号：PCT/US2003/033972
申请日：2003-10-24
申请人： MERCK & CO., INC. , BUTORA, Gabor , MILLS, Sander, G. , PASTERNAK, Alexander , SHANKARAN, Kothandaraman , YANG, Lihu , ZHOU, Changyou , GOBLE, Stephen, D.
发明人： BUTORA, Gabor , MILLS, Sander, G. , PASTERNAK, Alexander , SHANKARAN, Kothandaraman , YANG, Lihu , ZHOU, Changyou , GOBLE, Stephen, D.
IPC分类号： A61K
CPC分类号： C07D311/00 , C07C237/24 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07D211/58 , C07D211/96 , C07D305/08 , C07D307/22 , C07D309/14 , C07D311/02 , C07D311/68 , C07D311/74 , C07D313/04 , C07D319/06 , C07D333/36 , C07D335/02 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/08
摘要： The present invention is directed to compounds of the formula (I) (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 27 , R 28 , R 29 , R 30 , R 31 , X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及式（I）的化合物（其中R 1，R 2，R 3，R 4，R 5，R 6，R 7， R 8，R 9，R 10，R 11，R 27，R 28，R 29，R 30，R 31，X，m，n 并且虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

6. 发明申请

WO2005110409A3 TETRAHYDROPYRANYL CYCLOPENTYL 1-SUBSTITUTED AND 1,1-DISUBSTITUTED TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：四氢叶酸环己基1取代和1,1-取代的四氢喹啉调节剂的化合物受体活性
公开(公告)号：WO2005110409A3
公开(公告)日：2006-02-16
申请号：PCT/US2005013856
申请日：2005-04-22
申请人： MERCK & CO INC , YANG LIHU , MILLS SANDER G , MORRIELLO GREGORI J , GUIADEEN DEODIALSINGH , SHANKARAN KOTHANDARAMAN
发明人： YANG LIHU , MILLS SANDER G , MORRIELLO GREGORI J , GUIADEEN DEODIALSINGH , SHANKARAN KOTHANDARAMAN
IPC分类号： A61K31/353 , A61K31/47 , C07D405/12 , C07D471/04 , C07D217/00
CPC分类号： C07D471/04 , C07D405/12
摘要： Compounds of Formula I: I (wherein n, R
摘要翻译：式I的化合物：I（其中n，R'

7. 发明申请

WO2005110409A2 TETRAHYDROPYRANYL CYCLOPENTYL 1-SUBSTITUTED AND 1,1-DISUBSTITUTED TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：四氢叶酸环己基1取代和1,1-取代的四氢喹啉调节剂的化合物受体活性
公开(公告)号：WO2005110409A2
公开(公告)日：2005-11-24
申请号：PCT/US2005/013856
申请日：2005-04-22
申请人： MERCK & CO., INC. , YANG, Lihu , MILLS, Sander, G. , MORRIELLO, Gregori, J. , GUIADEEN, Deodialsingh , SHANKARAN, Kothandaraman
发明人： YANG, Lihu , MILLS, Sander, G. , MORRIELLO, Gregori, J. , GUIADEEN, Deodialsingh , SHANKARAN, Kothandaraman
IPC分类号： A61K31/47
CPC分类号： C07D471/04 , C07D405/12
摘要： Compounds of Formula I: I (wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 15 , R 16 , Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：式I化合物I（其中n，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R15，R16，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫性病症如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

8. 发明申请

WO1997016430A1 HEXAHYDRO-5-IMINO-1,4-HETEROAZEPINE DERIVATIVES AS INHIBITORS OF NITRIC OXIDE SYNTHASES 审中-公开
标题翻译：作为氮氧化物合成酶抑制剂的十六氢-5-IMINO-1,4-HETEROAZEPINE衍生物
公开(公告)号：WO1997016430A1
公开(公告)日：1997-05-09
申请号：PCT/US1996017447
申请日：1996-10-28
申请人： MERCK & CO., INC. , CALDWELL, Charles, G. , HAGMANN, William, K. , MacCOSS, Malcolm , SHAH, Shrenik, K. , SHANKARAN, Kothandaraman , FURMAN, Karla, L.
发明人： MERCK & CO., INC.
IPC分类号： C07D243/08
CPC分类号： C07D243/08 , C07D267/16 , C07D281/06
摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
摘要翻译：本文公开了已经发现可用于治疗一氧化氮合酶介导的疾病和病症的式（I）化合物及其药学上可接受的盐，包括神经变性疾病，胃肠蠕动和炎症的病症。这些疾病和障碍包括低血压，败血性休克，中毒性休克综合征，血液透析，诸如癌症患者中的IL-2治疗，恶病质，免疫抑制如移植治疗，自身免疫和/或炎性指征，包括晒伤，湿疹或银屑病和呼吸状况例如支气管炎，哮喘，氧化剂诱导的肺损伤和急性呼吸窘迫（ARDS），肾小球性肾炎，再狭窄，病毒感染的炎症后遗症，心肌炎，心力衰竭，动脉粥样硬化，骨关节炎，类风湿性关节炎，脓毒性关节炎，慢性或炎性肠病，溃疡性结肠炎，克罗恩病，系统性红斑狼疮（SLE），眼部疾病如眼高压，视网膜炎和葡萄膜炎，1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。

9. 发明申请

WO1996014842A1 SUBSTITUTED HETEROCYCLES AS INHIBITORS OF NITRIC OXIDE SYNTHASE 审中-公开
标题翻译：作为氮氧化物合成酶抑制剂的替代杂合物
公开(公告)号：WO1996014842A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014512
申请日：1995-11-13
申请人： MERCK & CO., INC. , SHAH, Shrenik, K. , GRANT, Stephan, K. , MACCOSS, Malcolm , SHANKARAN, Kothandaraman , QI, Hongbo , GUTHIKONDA, Ravindra, N.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/33
CPC分类号： C07D215/38 , C07D217/22 , C07D221/04 , C07D277/18 , C07D279/06 , C07D279/08 , C07D487/04
摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. Theses diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acute respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula (I) are also useful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Korsakoff's disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.
摘要翻译：本文公开了已经发现可用于治疗一氧化氮合酶介导的疾病和病症（包括神经变性疾病，胃肠蠕动和炎症病症）的式（I）化合物及其药学上可接受的盐。这些疾病和障碍包括低血压，脓毒性休克，中毒性休克综合征，血液透析，诸如癌症患者的IL-2治疗，恶病质，免疫抑制如移植治疗，自身免疫和/或炎性指征，包括晒伤或牛皮癣和呼吸病症，例如支气管炎，哮喘和急性呼吸窘迫（ARDS），心肌炎，心力衰竭，动脉粥样硬化，关节炎，类风湿性关节炎，慢性或炎性肠病，溃疡性结肠炎，系统性红斑狼疮（SLE），眼部疾病如眼高压和葡萄膜炎 1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。式（I）的化合物还可用于治疗缺氧，高压氧惊厥和毒性，痴呆，Sydenham's舞蹈病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，多发性硬化，柯萨科夫病，与脑血管障碍有关的不育症，缺血性脑水肿，睡眠障碍，精神分裂症，抑郁症，PMS，焦虑症，药物成瘾症，疼痛，偏头痛，免疫复合物疾病，免疫抑制剂和预防或逆转对阿片剂和地西泮的耐受性。

10. 发明授权

US07166614B2 Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢异喹啉调节剂
公开(公告)号：US07166614B2
公开(公告)日：2007-01-23
申请号：US10512925
申请日：2003-04-25
申请人： Richard Jiao , Stephen D. Goble , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Lihu Yang , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes
发明人： Richard Jiao , Stephen D. Goble , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Lihu Yang , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes
IPC分类号： C07D217/02 , A61K31/47
CPC分类号： C07D231/12 , C07D217/06 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D491/04 , C07D491/052
摘要： The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2
摘要翻译：本发明涉及式I化合物（其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，X，n和虚线在本文中定义）趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂

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