Title:
【発明の名称】酢酸誘導体、その製造法、それを含む製薬調製剤、及びその製薬調製剤製造への利用
Document Type and Number:
Japanese Patent JP2501252
Kind Code:
B2
Abstract:
Acetic acid derivatives of formula H2N(NH)C-X-Y-CO-Z-CH(Q1)COOQ2 (I), their hydrates, solvates and salts. In (I), Q1 = H, CH3 or phenyl. Q2 = H, phenyl-alkyl or physiologically-cleavable alkyl. X = 1,4-phenylene, 2,5- or 3,6-pyridylene or 1,4-piperidylene, which is bound to Y via the 4-C atom. Y = -(CH2)n-CONH-CH(Q3)-(CH2)m- (where n = 0-2 and m = 1-3); -CONH-CH2-CH(Q4)-, -(CH2)2-NHCO-CH2-, -NHCO-(CH2)3-, or a group of formula (a), (b) or (c). In the formulae, Q3 = H, CH3, phenyl, COOH, -COO-alkyl, -CONH-(CH2)2-COOH or -CONH-(CH2)2-COO-alkyl. Q4 = H, CH3 or phenyl. Z = 1,4-piperazinyl, 1,4-piperidinyl (which is bound to the CO group via the 1-N atom) or a group of formula -NH-CH(R1)- or -NH-CH(COR2). R1 = H, CH3, phenyl or COO-alkyl. R2 = an alpha-amino carboxylic acid linked via the amino group (or its ester or amide) or a group of formula -NH-(CH2)2-Ar, -CO2R2, an optionally mono- or dialkylated -CONH2 group, or a pyrrolidinoyl or piperidinoyl. Ar = phenyl optionally substituted by alkyl, alkoxy, -COOH, -CO-alkyl, -O(CH2)p-COOH (p = 1-4), O(CH2)p-COO-alkyl, -CONH2, -CONH-alkyl, -CO(alkyl)2, pyrrolidinoyl or piperidinoyl.
Inventors:
ALIG LEO (CH)
EDENHOFER ALBRECHT (CH)
MULLER MARCEL (CH)
TRZECIAK ARNOLD (CH)
WELLER THOMAS (CH)
EDENHOFER ALBRECHT (CH)
MULLER MARCEL (CH)
TRZECIAK ARNOLD (CH)
WELLER THOMAS (CH)
Application Number:
JP6531691A
Publication Date:
May 29, 1996
Filing Date:
March 07, 1991
Export Citation:
Assignee:
HOFFMANN LA ROCHE (CH)
International Classes:
A01N43/40; A61K31/195; A61K31/24; C07K5/097; A61K31/395; A61K31/40; A61K31/44; A61K31/445; A61K31/495; A61K38/00; A61K38/04; A61K38/06; A61P7/02; A61P9/10; A61P35/00; C07C227/14; C07C229/32; C07C237/20; C07C237/36; C07C257/18; C07C257/20; C07C271/64; C07D207/00; C07D207/04; C07D207/08; C07D207/09; C07D207/16; C07D211/34; C07D211/60; C07D211/62; C07D227/04; C07D227/06; C07D241/04; C07D295/185; C07D295/192; C07K5/00; C07K5/02; C07K5/023; C07K5/06; C07K5/062; C07K5/065; C07K5/072; C07K5/08; C07K5/083; C07K5/093; C07K5/12; C07K14/75; A61K; C07C; C07D; C07K; (IPC1-7): C07C237/36; A61K38/00; C07C237/20; C07K5/06
Attorney, Agent or Firm:
Heiyoshi Odashima