公开(公告)号：USRE39384E1

公开(公告)日：2006-11-07

申请号：US10389381

申请日：2003-03-17

申请人： Philip Christopher Buxton ,  Donald Colin Mackenzie

发明人： Philip Christopher Buxton ,  Donald Colin Mackenzie

IPC分类号： C07D417/04 ,  A61K31/44

CPC分类号： C07D417/12

摘要： A compound of formula (I): or a tautomeric form thereof, wherein: R1 represents a hydrogen atom, C1-12 alkyl, C1-12 alkoxy, C1-12 alkylcarbonyl or arylC1-12 alkyl; A1 represents hydrogen or 1 to 4 optional substituents selected from the group consisting of: C1-12 alkyl, C1-12 alkoxy, aryl, and halogen; aryl represents phenyl or naphthyl optionally substituted with up to five groups selected from halogen, C1-12 alkyl, phenyl, C1-12 alkoxy, haloC1-12 alkyl, hydroxy, nitro, C1-12 alkoxycarbonyl, C1-12 alkoxycarbonyl C1-12 alkyl, C1-12 alkoxycarbonyloxy, or C1-12 alkylcarbonyl: A2 represents a benzene ring having 1 to 3 optional substituents selected from hydrogen, halogen, C1-12 alkyl, C1-12 alkoxy; and M− represents a counter-ion other than the maleate ion.

摘要翻译： 式（I）的化合物：<？insert-start id =“INS-S-00001”date =“20061107”？>或其互变异构形式，<？insert-end id =“INS-S-00001”？ 其中：R 1表示氢原子，C 1-12烷基，C 1-12烷氧基，C 1-12 烷基羰基或芳基C 1-12烷基; A 1表示氢或1至4个选自以下的任选取代基：C 1-12烷基，C 1-12烷氧基， 芳基和卤素; 芳基表示任选被至多五个选自卤素，C 1-12烷基，苯基，C 1-12烷氧基，卤代C 1 -C 12烷基的基团取代的苯基或萘基， 12个烷基，羟基，硝基，C 1-12烷氧基羰基，C 1-12烷氧基羰基C 1-12烷基，C 1-12烷氧基羰基氧基或C 1-12烷基羰基：A2-2表示具有1至3个任选的取代基的苯环，所述取代基选自氢，卤素 ，C 1-12烷基，C 1-12烷氧基; 而M + - 表示除了马来酸根离子之外的抗衡离子。

公开(公告)号：US20080206336A1

公开(公告)日：2008-08-28

申请号：US10567803

申请日：2004-08-09

申请人： Peter John Coles ,  Donald Colin Mackenzie ,  Paul Norman Mudd

发明人： Peter John Coles ,  Donald Colin Mackenzie ,  Paul Norman Mudd

IPC分类号： A61K9/28 ,  A61K31/4439 ,  A61K31/155 ,  A61P3/10

CPC分类号： A61K9/2866 ,  A61K45/06

摘要： An oral dosage form comprising an erodable core, which core comprises Compound A or a pharmaceutically acceptable salt or solvate thereof and another antidiabetic agent, the core having a coating with one or more openings, characterised in that the coating is erodable under predetermined pH conditions; a process for preparing such a dosage form and the use of such a dosage form in medicine.

摘要翻译： 包含可侵蚀核心的口服剂型，其核心包含化合物A或其药学上可接受的盐或溶剂合物和另一种抗糖尿病剂，所述核心具有包含一个或多个开口的涂层，其特征在于，所述涂层在预定pH条件下是可侵蚀的; 制备这种剂型的方法以及在药物中使用这种剂型。