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1. 发明申请

WO2003027240A3 RHESUS MONKEY, DOG AND FERRET MELANIN-CONCENTRATING HORMONE TYPE 1 RECEPTOR 审中-公开
公开(公告)号：WO2003027240A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/029932
申请日：2002-09-20
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , TAN, Carina , SAILER, Andreas, W. , PAN, Jie , SANO, Hideki
发明人： TAN, Carina , SAILER, Andreas, W. , PAN, Jie , SANO, Hideki
IPC分类号： C07K1/00
摘要： The present invention features polypeptide and nucleic acid sequences related to the dog, ferret and rhesus monkey MCH-1R. Preferred polypeptides and nucleic acid contain a region common to the dog, ferret and rhesus monkey MCH-1R, which is not present in the human, rat, or mouse MCH-1R.

2. 发明申请

WO2003027240A2 RHESUS MONKEY, DOG AND FERRET MELANIN-CONCENTRATING HORMONE TYPE 1 RECEPTOR 审中-公开
标题翻译：罗氏猴，狗和麦芽单糖浓缩激素1型受体
公开(公告)号：WO2003027240A2
公开(公告)日：2003-04-03
申请号：PCT/US2002/029932
申请日：2002-09-20
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , TAN, Carina , SAILER, Andreas, W. , PAN, Jie , SANO, Hideki
发明人： TAN, Carina , SAILER, Andreas, W. , PAN, Jie , SANO, Hideki
IPC分类号： C12N
CPC分类号： C07K14/72
摘要： The present invention features polypeptide and nucleic acid sequences related to the dog, ferret and rhesus monkey MCH-1R. Preferred polypeptides and nucleic acid contain a region common to the dog, ferret and rhesus monkey MCH-1R, which is not present in the human, rat, or mouse MCH-1R.
摘要翻译：本发明涉及与狗，白鼬和恒河猴MCH-1R相关的多肽和核酸序列。优选的多肽和核酸含有与人，大鼠或小鼠MCH-1R中不存在的狗，白鼬和恒河猴MCH-1R共有的区域。

3. 发明申请

WO2003027239A3 MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONIST BINDING PROTEIN 审中-公开
公开(公告)号：WO2003027239A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/029931
申请日：2002-09-20
申请人： MERCK & CO., INC. , HOWARD, Andrew, D. , PAN, Jie , FONG, Tung, M. , MARSH, Donald, J. , SAILER, Andreas, W.
发明人： HOWARD, Andrew, D. , PAN, Jie , FONG, Tung, M. , MARSH, Donald, J. , SAILER, Andreas, W.
IPC分类号： C07K1/00
摘要： The present invention features MCH-1R antagonist binding proteins. MCH-1R antagonist binding proteins described herein are based on an MCH-1R having one or more alterations to the second intracellular loop or carboxy terminus that render the receptor substantially inactive to MCH binding. An MCH-1R antagonist binding protein can bind MCH-1R antagonists, but does not exhibit high affinity MCH binding and is not activated by the MCH.

4. 发明申请

WO2005035793A2 CCKAR MARKERS AND HAPLOTYPES ASSOCIATED WITH EXTREME WEIGHT CONDITIONS 审中-公开
标题翻译： CCKAR标记和HAPLOTYPES与极度重量条件相关
公开(公告)号：WO2005035793A2
公开(公告)日：2005-04-21
申请号：PCT/US2004/033192
申请日：2004-10-08
申请人： DECODE GENETICS EHF. , ROSETTA INPHARMATICS LLC , MERCK & CO., INC. , EMILSSON, Valur , GULCHER, Jeffrey, R. , WALTERS, Gudmundur, Bragi , SCHADT, Eric, E. , VAN DER PLOEG, Leonardus, H., T. , REITMAN, Marc, L. , LAMB, John, R. , SAILER, Andreas, W.
发明人： EMILSSON, Valur , GULCHER, Jeffrey, R. , WALTERS, Gudmundur, Bragi , SCHADT, Eric, E. , VAN DER PLOEG, Leonardus, H., T. , REITMAN, Marc, L. , LAMB, John, R. , SAILER, Andreas, W.
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/156 , C12Q2600/158 , C12Q2600/172
摘要： Methods for diagnosis of obesity or a susceptibility or resistance to obesity based on detection of at risk haplotypes associated with human Cholecystokinin Type A Receptor gene are disclosed.
摘要翻译：公开了基于与人类胆囊收缩素A型受体基因相关的风险单倍体的检测来诊断肥胖或易感性或抵抗肥胖症的方法。

5. 发明申请

WO2003045920A1 4-AMINOQUINOLINE COMPOUNDS 审中-公开
标题翻译： 4-氨基喹啉化合物
公开(公告)号：WO2003045920A1
公开(公告)日：2003-06-05
申请号：PCT/US2002/037510
申请日：2002-11-22
申请人： MERCK & CO., INC. , DEVITA, Robert, J. , CHANG, Lehua , HOANG, MyLe Thi , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W.
发明人： DEVITA, Robert, J. , CHANG, Lehua , HOANG, MyLe Thi , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W.
IPC分类号： C07D213/42
CPC分类号： C07D231/12 , C07D215/42 , C07D219/10 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07F7/2212
摘要： The present invention is concerned with compounds of the general Formula I : and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington s disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译：本发明涉及通式I的化合物及其药学上可接受的盐，其可用作黑色素浓缩激素受体拮抗剂，特别是MCH-1R拮抗剂。因此，本发明的化合物可用于治疗或预防与食物过量摄取及其并发症，骨关节炎，某些癌症，艾滋病消瘦，恶病质，虚弱（特别是老年人）相关的肥胖或进食障碍，精神障碍压力，认知障碍，性功能，生殖功能，肾功能，运动障碍，注意力缺陷障碍（ADD），药物滥用障碍和运动障碍，亨廷顿疾病，癫痫，记忆功能和脊髓性肌肉萎缩。因此，式I化合物可用于治疗这些病症，以及制备用于治疗这些病症的药物。作为制备这些化合物的方法，公开了包含式（I）化合物之一作为活性成分的药物制剂。

6. 发明申请

WO2003045313A2 2-AMINOQUINOLINE COMPOUNDS 审中-公开
标题翻译： 2-氨基喹啉化合物
公开(公告)号：WO2003045313A2
公开(公告)日：2003-06-05
申请号：PCT/US2002/037556
申请日：2002-11-22
申请人： MERCK & CO. INC. , DEVITA, Robert, J. , CHANG, Lehua , CHAUNG, Danny , HOANG, MyLe , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W. , YOUNG, Jonathan, R.
发明人： DEVITA, Robert, J. , CHANG, Lehua , CHAUNG, Danny , HOANG, MyLe , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W. , YOUNG, Jonathan, R.
IPC分类号： A61K
CPC分类号： C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/10
摘要： The present invention is concerned with compounds of the general Formula I : and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists.As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington s disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译：本发明涉及通式I的化合物及其药学上可接受的盐，其可用作黑色素浓缩激素受体拮抗剂，特别是MCH-1R拮抗剂。因此，本发明的化合物可用于治疗或预防与过量食物摄取和并发症相关的肥胖症或进食障碍，骨关节炎，某些癌症，艾滋病浪费，恶病质，虚弱（特别是老年人），精神障碍压力，认知障碍，性功能，生殖功能，肾功能，运动障碍，注意力缺陷障碍（ADD），药物滥用障碍和运动障碍，亨廷顿病，癫痫，记忆功能和脊髓性肌肉萎缩。因此，式I化合物可用于治疗这些病症，以及制备用于治疗这些病症的药物。作为制备这些化合物的方法，公开了包含式（I）化合物之一作为活性成分的药物制剂。

7. 发明公开

EP1451156A1 4-AMINOQUINOLINE COMPOUNDS 审中-公开
标题翻译： 4-氨基喹啉化合物
公开(公告)号：EP1451156A1
公开(公告)日：2004-09-01
申请号：EP02789827.9
申请日：2002-11-22
申请人： Merck & Co., Inc.
发明人： DEVITA, Robert, J. , CHANG, Lehua , HOANG, MyLe Thi , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W.
IPC分类号： C07D213/42
CPC分类号： C07D231/12 , C07D215/42 , C07D219/10 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07F7/2212
摘要： The present invention is concerned with compounds of the general Formula I : and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington s disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译：本发明涉及用作黑色素浓集激素受体拮抗剂，特别是MCH-1R拮抗剂的通式I的化合物及其药学上可接受的盐。因此，本发明的化合物可用于治疗或预防与过量食物摄入及其并发症，骨关节炎，某些癌症，AIDS消瘦，恶病质，虚弱（特别是在老年人中），精神障碍压力相关的肥胖或进食障碍，认知障碍，性功能，生殖功能，肾功能，运动障碍，注意力缺陷障碍（ADD），药物滥用障碍和运动障碍，亨廷顿舞蹈病，癫痫，记忆功能和脊髓性肌萎缩。式I化合物因此可用于治疗这些病症，并用于制备用于治疗这些病症的药物。公开了包含式（I）化合物之一作为活性成分的药物制剂，以及制备这些化合物的方法。

8. 发明公开

EP1450801A2 2-AMINOQUINOLINE COMPOUNDS 审中-公开
标题翻译： 2-氨基喹啉CONNECTIONS
公开(公告)号：EP1450801A2
公开(公告)日：2004-09-01
申请号：EP02789837.8
申请日：2002-11-22
申请人： Merck & Co., Inc.
发明人： DEVITA, Robert, J. , CHANG, Lehua , CHAUNG, Danny , HOANG, MyLe , JIANG, Jinlong , LIN, Peter , SAILER, Andreas, W. , YOUNG, Jonathan, R.
IPC分类号： A61K31/47 , C07D215/38 , C07D215/44
CPC分类号： C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/10
摘要： The present invention is concerned with compounds of the general Formula I : and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists.As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington s disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

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