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Title:
AZEPINE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2001/055121
Kind Code:
A1
Abstract:
Azepine derivatives of the general formula (I) or salts thereof, and drugs containing the derivatives or the salts as the active ingredient. In said Formula, R?1¿ is hydrogen, alkyl, aryl, or the like; R?2¿ is hydrogen or a carboxyl-protecting group; R?3¿ is alkylene, a divalent aromatic hydrocarbon group, or the like; R?4¿ is hydrogen, alkyl, or the like; X is an aromatic carbocycle or a heterocycle; m is an integer of 1 to 3; Y is nitrogen, oxygen, or the like; and Z is a group of the general formula (II): R?8¿ - R?7¿ - R?6¿ - A?1¿ -, (wherein A?1¿ is methylene, sulfonyl, or the like; R?6¿ is alkylene, a divalent group derived from an arylalkane, or the like; R?7¿ is methylene, carbonyl, or the like; and R?8¿ is alkyl, arylalkyl, or the like). The drugs are excellent in peroral absorbability and in vivo fate and exhibit VLA-4 antagonism.

Inventors:
IKEGAMI SATORU (JP)
INOGUCHI KIYOSHI (JP)
FUKUI HIDETO (JP)
SUMITA YUJI (JP)
MARUYAMA TATSUYA (JP)
WATANUKI MITSURU (JP)
Application Number:
PCT/JP2001/000521
Publication Date:
August 02, 2001
Filing Date:
January 26, 2001
Export Citation:
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Assignee:
KAKEN PHARMA CO LTD (JP)
IKEGAMI SATORU (JP)
INOGUCHI KIYOSHI (JP)
FUKUI HIDETO (JP)
SUMITA YUJI (JP)
MARUYAMA TATSUYA (JP)
WATANUKI MITSURU (JP)
International Classes:
A61K31/5513; A61K31/553; A61P1/04; A61P3/10; A61P9/10; A61P11/06; A61P13/12; A61P19/02; A61P25/00; A61P29/00; A61P35/00; A61P37/06; A61P37/08; A61P43/00; C07D243/24; C07D491/052; C08L23/02; C08L25/06; C08L71/12; C08L53/02; (IPC1-7): C07D243/24; C07D267/14; C07D413/12; C07D401/12; C07D403/12; C07D417/12; C07D491/052; C07D471/04; A61K31/553; A61K31/5513; A61P43/00; A61P29/00; A61P19/02; A61P13/12; A61P1/04; A61P37/06; A61P25/00; A61P11/06; A61P37/08; A61P9/10; A61P3/10; A61P35/00
Foreign References:
EP0842944A21998-05-20
Attorney, Agent or Firm:
Kamata, Junji (Kyobashi-Nisshoku Bldg. 8-7 Kyobashi 1-chome Chuo-ku, Tokyo, JP)
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