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公开(公告)号：EP1284260A1
公开(公告)日：2003-02-19
申请号：EP01932153.8
申请日：2001-05-21
IPC分类号： C07D207/333 , A61K31/402 , A61P43/00 , A61P3/10
CPC分类号： C07D207/333 , A61K31/402 , C07D209/12
摘要： A compound of the formula (I):
wherein X 1 and X 2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain;
one of R 1 and R 2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C 1-6 alkoxy group and 2) an optionally substituted carboxy-C 1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and
R 3 , R 4 and R 5 are the same or different and each is a hydrogen atom or a substituent, or R 4 may link together with R 3 or R 5 to form an optionally substituted ring;
provided that when R 3 is a hydrogen atom, R 4 is a hydrogen atom and R 5 is methyl, X 2 -R 2 is not 4-cyclohexylphenyl; when R 3 is 4-methoxyphenyl, R 4 is a hydrogen atom and R 5 is methyl, X 2 -R 2 is not 4-methoxyphenyl; and when R 1 or R 2 is a hydrogen atom, the adjacent X 1 or X 2 is not a C 1-7 alkylene;
or a salt thereof exhibits a protein tyrosine phosphatase inhibitory action and is useful as a prophylactic or therapeutic agent for diabetes or the like.摘要翻译： 式（I）的化合物：其中X1和X2相同或不同，并且各自为主链中的键或具有1至20个原子的间隔基; R 1和R 2之一是具有选自1）任选取代的羧基-C 1-6烷氧基和2）任选取代的羧基-C 1-6脂族烃基的取代基的环状基团，其中所述循环基团任选具有附加 取代基，另一个是任选取代的环状基团或氢原子; 并且R 3，R 4和R 5相同或不同，各自为氢原子或取代基，或者R 4可与R 3或R 5连接形成任选取代的环; 条件是当R3为氢原子时，R4为氢原子，R5为甲基，X2-R2不为4-环己基苯基; 当R3是4-甲氧基苯基时，R4是氢原子，R5是甲基，X2-R2不是4-甲氧基苯基; 当R1或R2为氢原子时，相邻的X1或X2不是C1-7亚烷基; 或其盐表现出蛋白酪氨酸磷酸酶抑制作用，可用作糖尿病等的预防或治疗剂。
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2.发明公开4,1-BENZOXAZEPINES, THEIR ANALOGUES, AND THEIR USE AS SOMATOSTATIN AGONISTS 失效4,1-benzoxazepines及其类似物，其使用生长抑素受体激动剂
公开(公告)号：EP0979227A1
公开(公告)日：2000-02-16
申请号：EP98914096.7
申请日：1998-04-20
IPC分类号： C07D267/14 , C07D243/24 , C07D281/10 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12 , A61K31/55
CPC分类号： C07D231/12 , C07D233/56 , C07D243/24 , C07D249/08 , C07D267/14 , C07D281/10 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention provides a compound of formula (I), wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; Z is an optionally substituted cyclic group or linear hydrocarbon group; R1 is a hydrogen atom, an optionally substituted hydrocarbon group or heterocyclic ring; R2 is an optionally substituted amino group; D is a bond or an optionally substituted divalent hydrocarbon ring; E is a bond, -CON(Ra)-, -N(Ra)CO-, -N(R?b)CON(Rc¿)-, -N(Rd)COO-, -N(Re)SO2-, -COO-, -N(Rf)-, -O-, -S-, -SO-, -SO¿2?-, and formula (a) or (b) (in which R?a, Rb, Rc, Rd, Re and Rf¿ are respectively a hydrogen atom or an optionally substituted hydrocarbon group); G is a bond or an optionally divalent substituted hydrocarbon group; L is a divalent group; ring B may form an optionally substituted non-aromatic condensed nitrogen-containing heterocyclic ring by combining with R2; X is two hydrogen atoms, an oxygen atom or a sulfur atom; ......... is a single bond or a double bond, and Y is a nitrogen atom when ......... is a double bond, or an oxygen atom, -N(R4)-, (in which R4 is a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group) or S(O)¿n? (in which n is 0, 1 or 2) when ......... is a single bond, or a salt thereof, which have somatostatin receptor agonistic action.
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