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1. 发明公开

EP0196849A3 Aminohydroxyalkylbenzene anti-obesity and/or anti-hyperglycaemic agents 失效
标题翻译：氨基甲基苯乙酮抗体和/或抗高血压药物
公开(公告)号：EP0196849A3
公开(公告)日：1988-01-07
申请号：EP86302145
申请日：1986-03-24
申请人： BEECHAM GROUP PLC
发明人： Smith, David Glynn , White, Susan Mary
IPC分类号： C07C91/18 , C07C93/06 , C07C91/34 , C07C91/40 , A61K31/135 , C07C87/18 , C07C93/08
CPC分类号： A61K31/135 , A23K20/111 , A61K31/165
摘要： A compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R A is a group of formula (a):
wherein T represents a group of formula (b):
wherein Q is
, and where
R' is a hydrogen or halogen atom or a -CF 3 , OR 4 , NHR 4 , -NHCOR 4 , -NHCONH 2 , NHSO 2 R 4 , CH 2 OR 4 or -CH 2 SO 2 R 4 group: R 2 is a hydrogen or halogen atom or an -OR 4 group; R 3 is a hydrogen or halogen atome; and R 4 is hydrogen, C 1-6 alkyl or benzyl; X' is a bond or -OCH 2 -; X 2 is a group of formula -CR 5 R 6 -CH 2 -A-wherein R 5 and R 6 are independently hydrogen or methyl; and A is a bond, -CH 2 -, or O; T' represents a hydrogen atom or a group of formula (b) as defined above in respect of T, such that T' and T may be the same or different; R C represents a group (a) as defined above in respect of R A , such that R C and R A may be the same or different; provided that when R A and R C each represent a group of formula:
wherein R is oH or -O-benzyl; then when A is a bond, -CH 2 - or -0, R' is not -CH 2 OH or NHSO 2 -C 1-4 alkyl; processes for the preparation of such compounds and their use in medicine and agriculture.

2. 发明公开

EP0196849A2 Aminohydroxyalkylbenzene anti-obesity and/or anti-hyperglycaemic agents 失效
标题翻译：氨基羟基烷基苯Agenzien gegen Fettleibigkeit und / oder Hyperglycemie。
公开(公告)号：EP0196849A2
公开(公告)日：1986-10-08
申请号：EP86302145.7
申请日：1986-03-24
申请人： BEECHAM GROUP PLC
发明人： Smith, David Glynn , White, Susan Mary
IPC分类号： C07C215/28 , C07C215/46 , C07C215/68 , C07C215/76 , A61K31/135
CPC分类号： A61K31/135 , A23K20/111 , A61K31/165
摘要： A compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R A is a group of formula (a):
wherein T represents a group of formula (b):
wherein Q is
, and where

R' is a hydrogen or halogen atom or a -CF 3 , OR 4 , NHR 4 , -NHCOR 4 , -NHCONH 2 , NHSO 2 R 4 , CH 2 OR 4 or -CH 2 SO 2 R 4 group:
R 2 is a hydrogen or halogen atom or an -OR 4 group;
R 3 is a hydrogen or halogen atome; and R 4 is hydrogen, C 1-6 alkyl or benzyl;
X' is a bond or -OCH 2 -;
X 2 is a group of formula -CR 5 R 6 -CH 2 -A-wherein R 5 and R 6 are independently hydrogen or methyl; and
A is a bond, -CH 2 -, or O;
T' represents a hydrogen atom or a group of formula (b) as defined above in respect of T, such that T' and T may be the same or different; R C represents a group (a) as defined above in respect of R A , such that R C and R A may be the same or different; provided that when R A and R C each represent a group of formula:
wherein R is oH or -O-benzyl; then when A is a bond, -CH 2 - or -0, R' is not -CH 2 OH or NHSO 2 -C 1-4 alkyl; processes for the preparation of such compounds and their use in medicine and agriculture.
摘要翻译：式（I）的化合物：其中R A为式（a）的基团：其中T表示式（b）的基团：QX 1 - 其中Q是，其中R 1是氢或卤素原子或-CF 3，OR 4，NHR 4，-NHCOR 4，-NHCONH 2， NHSO 2 R 4，CH 2 O 4或-CH 2 SO 2 R 4基团：R 2是氢或卤素原子或-OR 4基团; R 3是氢或卤素原子; 和R 4是氢，C 1-6烷基或苄基; X 1是键或-OCH 2 - ; X 2是式-CR 5 R 6 -CH 2 -A - ，其中R 5和R 6独立地是氢或甲基; 并且A是键，-CH 2 - 或O; T 1表示氢原子或上述关于T定义的式（b）的基团，使得T 1和T可以相同或不同; R C表示如上面关于R aA定义的基团（a），使得R c和R AA可以相同或不同; 条件是当R A和R C各自表示下式的基团时：其中R 2为oH或-O-苄基; 那么当A为键时，-CH 2 - 或-O，R 1不是-CH 2 OH或NHSO 2 -C 1-4烷基; 这些化合物的制备方法及其在医药和农业中的应用。

3. 发明公开

EP0028883A3 Benzimidazoline derivatives, processes for their preparation and pharmaceutical compositions containing them 无效转让
标题翻译：苯并咪唑衍生物，其制备方法及含有它们的药物组合物
公开(公告)号：EP0028883A3
公开(公告)日：1981-06-03
申请号：EP80303610
申请日：1980-10-14
申请人： BEECHAM GROUP PLC
发明人： Cantello, Barrie Christian Charles , White, Susan Mary
IPC分类号： C07D235/30 , A61K31/415
CPC分类号： C07D235/30 , Y10S514/866
摘要： A compound with hypoglycaemic activity having formula (II) or a pharmaceutically acceptable ammonium or acid addition salt thereof:
wherein
R' and R 2 are the same or different and represent hydrogen, Ci-6 alkyl, C 1-6 alkoxy, hydroxy or halogen; R 3 and R' are the same or different and represent hydrogen or C 1-6 alkyl; R' represents hydrogen or C 1-6 alkyl; R 6 represents C 1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl, and C 1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl and C 1-6 alkoxy; or R 5 and R 6 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C 1-6 alkyl, carboxy or C 1-6 alkoxycarbonyl; and R' represents phenyl, optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl and C 1-6 alkoxy, C 1-6 alkoxy carbonyl, C 1-6 alkanoyl, C 1-6 alkyanoyloxy, nitro, hydro, amino, substituted amino, and carboxy.

4. 发明公开

EP0028883A2 Benzimidazoline derivatives, processes for their preparation and pharmaceutical compositions containing them 无效转让
标题翻译： Benzimidazoline衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0028883A2
公开(公告)日：1981-05-20
申请号：EP80303610.2
申请日：1980-10-14
申请人： BEECHAM GROUP PLC
发明人： Cantello, Barrie Christian Charles , White, Susan Mary
IPC分类号： C07D235/30 , A61K31/415
CPC分类号： C07D235/30 , Y10S514/866
摘要： A compound with hypoglycaemic activity having formula (II) or a pharmaceutically acceptable ammonium or acid addition salt thereof:
wherein

R' and R 2 are the same or different and represent hydrogen, Ci-6 alkyl, C 1-6 alkoxy, hydroxy or halogen;
R 3 and R' are the same or different and represent hydrogen or C 1-6 alkyl;
R' represents hydrogen or C 1-6 alkyl;
R 6 represents C 1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl, and C 1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl and C 1-6 alkoxy; or R 5 and R 6 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C 1-6 alkyl, carboxy or C 1-6 alkoxycarbonyl; and
R' represents phenyl, optionally substituted with up to 3 groups selected from halogen, C 1-6 alkyl and C 1-6 alkoxy, C 1-6 alkoxy carbonyl, C 1-6 alkanoyl, C 1-6 alkyanoyloxy, nitro, hydro, amino, substituted amino, and carboxy.

5. 发明公开

EP0000816A1 Substituted amino-pyridine derivatives, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：取代的氨基 - 吡啶衍生物，涉及它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0000816A1
公开(公告)日：1979-02-21
申请号：EP78300190.2
申请日：1978-07-25
申请人： BEECHAM GROUP PLC
发明人： Baggaley, Keith Howard, Dr. , Thorne, David Edward, Dr. , White, Susan Mary
IPC分类号： C07D213/74 , C07D213/80 , C07D213/85 , C07D401/04 , A61K31/44 , A61K31/455
CPC分类号： C07D213/74 , A61K31/44 , A61K31/455 , C07D213/80 , C07D213/85
摘要： A class of substituted amino pyridine derivatives are of value in the treatment of diabetes. Some of the compounds also possess hypolipidaemic activity.
The compounds are represented by the formula (I):

wherein R 3 is hydrogen, alkyl or an acidic function;
R 2 is hydrogen or alkyl;
R 4 and R' are hydrogen, alkyl or halogen;
Z is hydrogen, phenyl, alkyl or aralkyl;
Alk is alkylene and x is 0 or 1;
R 1 is optionally substituted phenyl or naphthyl.

Most of the compounds of formula (I) are novel.
摘要翻译：一类substituiertem氨基吡啶衍生物的是在糖尿病的治疗价值。一些化合物具有这样降血脂活性。该化合物由式（I）表示： worin - [R <3>是氢，烷基或在酸性功能; [R <2>是氢或烷基; [R <4>和R <5>是氢，烷基或卤素; Z是氢，苯基，烷基或芳烷基; Alk是亚烷基，x是0或1; [R <1>是苯基或萘基OPTIONALLY substituiertem。大多数式（I）的化合物是新的。

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