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公开(公告)号：US07482368B2
公开(公告)日：2009-01-27
申请号：US11196563
申请日：2005-08-02
申请人： Peter Bertinato , Brian Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Brian Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/44
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如说明书中所定义，以及其药物组合物及其用途，以及制备该化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US07348355B2
公开(公告)日：2008-03-25
申请号：US11351571
申请日：2006-02-10
申请人： Peter Bertinato , Alan E. Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan E. Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/40 , C07D209/42
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及 制备化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US06720351B2
公开(公告)日：2004-04-13
申请号：US10177858
申请日：2002-06-20
申请人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31405
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及制备该化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US06949572B2
公开(公告)日：2005-09-27
申请号：US10639855
申请日：2003-08-13
申请人： Peter Bertinato , Brian S. Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Brian S. Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/44 , A61P3/00 , C07D40/00
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
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公开(公告)号：US06979692B2
公开(公告)日：2005-12-27
申请号：US10639854
申请日：2003-08-13
申请人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/44 , A61P3/00 , C07D213/28
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及 制备化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US20050288335A1
公开(公告)日：2005-12-29
申请号：US11196563
申请日：2005-08-02
申请人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
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公开(公告)号：US20050080108A1
公开(公告)日：2005-04-14
申请号：US10639854
申请日：2003-08-13
申请人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D333/66
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1—R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如说明书中所定义，以及其药物组合物及其用途，以及制备该化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US20060194772A1
公开(公告)日：2006-08-31
申请号：US11351571
申请日：2006-02-10
申请人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan Blize , Brian Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/655 , A61K31/405 , A61K31/381 , A61K31/343 , C07D333/56 , C07D307/87 , C07D209/42
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及 制备化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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9.发明授权公开(公告)号：US06649636B1
公开(公告)日：2003-11-18
申请号：US09723608
申请日：2000-11-28
申请人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
发明人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
IPC分类号： C07D40114
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译： 本发明涉及下式的化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地稠合于碳环或5至6个 杂芳基 R 2是任选被卤素，氨基或烷基氨基取代的（C 1 -C 4）烷基; R 3和R 4各自为氢，卤素，任选被卤素取代的（C 1 -C 4）烷基等; X 1至X 4各自为氢，卤素，羟基，任选被卤素取代的（C 1 -C 4）烷基等。 这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。
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10.发明授权Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents 失效杂环烷基磺酰基吡唑衍生物作为抗炎/止痛剂公开(公告)号：US06531492B1
公开(公告)日：2003-03-11
申请号：US09724446
申请日：2000-11-28
申请人： Kristin M. Lundy , Hengmiao Cheng , Subas M. Sakya , Jin Li , Martha L. Minich , Chikara Uchida
发明人： Kristin M. Lundy , Hengmiao Cheng , Subas M. Sakya , Jin Li , Martha L. Minich , Chikara Uchida
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D403/04 , C07D405/14
摘要： The present invention relates to compounds of the formula wherein R2, R3, R6 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
摘要翻译： 本发明涉及式R 2，R 3，R 6和A的化合物在说明书中定义为含有它们的药物组合物及其药物用途。 本发明的化合物可用于治疗或缓解哺乳动物（优选人，狗，猫和家畜）中的炎症和其它炎症相关疾病，例如骨关节炎，类风湿性关节炎，结肠癌和阿尔茨海默氏病。
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