公开(公告)号：US06646150B1

公开(公告)日：2003-11-11

申请号：US10149674

申请日：2002-06-13

申请人： Fuminori Sato ,  Tomoki Omodani ,  Ryotaro Shiratake ,  Yasunao Inoue ,  Takashi Deguchi

发明人： Fuminori Sato ,  Tomoki Omodani ,  Ryotaro Shiratake ,  Yasunao Inoue ,  Takashi Deguchi

IPC分类号： C07C21302

CPC分类号： C07C213/02 ,  C07C269/06 ,  Y02P20/55 ,  C07C215/08 ,  C07C271/16

摘要： The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.

摘要翻译： 本发明提供工业上制备（氨基甲基）三甲基甲醇衍生物的方法，特别是其光学活性化合物，其可用作药物如蛋白酶抑制剂等的起始化合物。

公开(公告)号：US06835714B1

公开(公告)日：2004-12-28

申请号：US09913538

申请日：2001-08-15

申请人： Fuminori Sato ,  Yasunao Inoue ,  Tomoki Omodani ,  Ryotaro Shiratake ,  Seiji Honda ,  Masanobu Komiya ,  Tadashi Takemura

发明人： Fuminori Sato ,  Yasunao Inoue ,  Tomoki Omodani ,  Ryotaro Shiratake ,  Seiji Honda ,  Masanobu Komiya ,  Tadashi Takemura

IPC分类号： C07K506

CPC分类号： C07D403/12 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0222 ,  C07K5/0806 ,  C07K5/0821 ,  C07K5/1008

摘要： The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc. wherein A and B are the same or different and each is a lower alkylene group being optionally substituted by an oxo group, D is a heteromonocyclic or heterobicyclic group being optionally substituted by an oxo group, R1 and R2 are the same or different and each is a lower alkyl group, R3 and R4 are different from each other, and each is a hydrogen atom or a hydroxy group, or both combine together to form an oxo group, and R5 is 2-benzoxazolyl, trifluoromethyl, benzylamino-carbonyl, etc.

摘要翻译： 本发明涉及下式（Ia）的杂环化合物，其酯或其盐，以及含有与活性成分相同的人嗜中性弹性蛋白酶抑制剂等。其中A和B相同或不同， 每个是任选被氧代基取代的低级亚烷基，D是任选被氧代基取代的杂单环或杂双环基团，R 1和R 2相同或不同，并且各自为低级烷基 R 3和R 4彼此不同，各自为氢原子或羟基，或两者结合在一起形成氧代基，R 5为2-苯并恶唑基，三氟甲基，苄基氨基 羰基等