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1. 发明授权

US07084156B2 2-Aminoquinoline compounds 失效
标题翻译： 2-氨基喹啉化合物
公开(公告)号：US07084156B2
公开(公告)日：2006-08-01
申请号：US10496615
申请日：2002-11-22
申请人： Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
发明人： Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
IPC分类号： C07D215/38 , C07D215/16 , A61K31/47
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。

2. 发明申请

US20090012061A1 A Method of Treating Cancer 审中-公开
标题翻译：一种治疗癌症的方法
公开(公告)号：US20090012061A1
公开(公告)日：2009-01-08
申请号：US11662396
申请日：2005-09-09
申请人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
发明人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
IPC分类号： G01N33/574 , C12N9/99 , A61K31/403 , A61K31/428 , C07C271/06 , A61K31/27 , A61K31/47 , C07D215/38 , C07C39/12 , A61K31/05 , C07C275/28 , A61K31/17 , A61K31/165 , A61K31/415 , A61K31/44 , A61K31/5415 , A61K31/551 , A61P35/00
CPC分类号： C12Q1/42 , G01N33/6893 , G01N2500/00
摘要： The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要翻译：本发明涉及一种治疗细胞增殖性疾病，特别是癌症的方法，其包括施用有丝分裂驱动蛋白KSP活性的调节剂，其中KSP调节剂的活性取决于微管的存在。相信本方法中使用的KSP调节剂以先前未报道的方式结合KSP蛋白质，因为化合物相对于微管或ATP（KSP的底物）竞争性结合。在本方法中有用的调节剂还不能抵抗KSP的非微管刺激活性。可以使用本文公开的方法治疗的细胞增殖性疾病是例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。

3. 发明申请

US20050026915A1 2-Aminoquinoline compounds 失效
标题翻译： 2-氨基喹啉化合物
公开(公告)号：US20050026915A1
公开(公告)日：2005-02-03
申请号：US10496615
申请日：2002-11-22
申请人： Robert DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer , Jonathan Young
发明人： Robert DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer , Jonathan Young
IPC分类号： C07D215/38 , A61K31/403 , A61K31/407 , A61K31/439 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P1/14 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P19/02 , A61P21/00 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , A61P43/00 , C07D215/22 , C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/00 , C07D471/08 , C07D487/08 , C07D487/10 , C07D491/04 , C07D491/08 , C07D495/10 , A61K31/541 , C07D413/02 , C07D417/02 , C07
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。

4. 发明申请

US20050009815A1 4-Aminoquinoline compounds 审中-公开
标题翻译： 4-氨基喹啉化合物
公开(公告)号：US20050009815A1
公开(公告)日：2005-01-13
申请号：US10496614
申请日：2002-11-22
申请人： Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
发明人： Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
IPC分类号： A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/519 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61P31/18 , A61P35/00 , A61P43/00 , C07D215/42 , C07D215/48 , C07D219/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07D521/00 , C07F7/22 , A61K31/541 , A61K31/5377
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 , C07F7/2208
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。

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