发明公开
- 专利标题： TYROSINE PHOSPHATASE INHIBITORS
- 专利标题（中）： 酪氨酸磷酸酶抑制剂
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申请号： EP01932153.8申请日： 2001-05-21
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公开(公告)号： EP1284260A1公开(公告)日： 2003-02-19
- 发明人: MATSUMOTO, Takahiro , KATAYAMA, Nozomi , MABUCHI, Hiroshi
- 申请人： Takeda Chemical Industries, Ltd.
- 申请人地址： 1-1 Doshomachi 4-chome, Chuo-ku Osaka-shi, Osaka 541-0045 JP
- 专利权人： Takeda Chemical Industries, Ltd.
- 当前专利权人： Takeda Chemical Industries, Ltd.
- 当前专利权人地址： 1-1 Doshomachi 4-chome, Chuo-ku Osaka-shi, Osaka 541-0045 JP
- 代理机构： Rickard, Timothy Mark Adrian
- 优先权： JP2000154441 20000522; JP2000247954 20000810
- 国际公布： WO01090067 20011129
- 主分类号： C07D207/333
- IPC分类号： C07D207/333 ; A61K31/402 ; A61P43/00 ; A61P3/10
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.
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.
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