Title:
【発明の名称】新規なアミジン誘導体,その製法,及びLTB↓4拮抗剤としての使用
Document Type and Number:
Japanese Patent JPH07503718
Kind Code:
A
Abstract:
Amidine derivs. of formula (I), in the form of their racemates, enantiomer pure or enriched forms, diastereomer pairs, cis- and trans-isomers, free bases or salts (pref. with physiologically acceptable acids) are new. In (I), R1 and R2 are each CF3, halogen, R5, OR5, COR6, SR6, SOR6, SO2R6, SO2NR5R7, C(OH)R5R7, or R1 and R2 connect neighbouring C atoms on the benzene ring to which they are attached with -CR8=CR9CH=CH-, -CH=CR8CR9=CH-, -CR8=CHCR9=CH-, -OCHR10CH2-, -OCH2O-, -OCH2CH2O-, -(CH2)3-4-, -NHCOO-, -NHCOCH2O-, -COCH2O- or -COCH2CH2O-, each of these gps. being opt. substd. with 1-4C alkyl; R3 is H, OH, CF3, R5, OR6, COR6, CONR5R7, CH2OH, CH2O(1-4C alkyl), SR6, SOR6, SO2R6, SO2NR5R7, NHCO(1-4C alkyl), NHSO2(1-4C alkyl), NR5R7 or C(OH)R5R7 or a heterocyclic 5-ring contg. 1-3 heteroatoms and of formulae (a), (b) or (c); provided that if R3 is R5, R5 can only be H if at least one of R1 and R2 is not H; D, E and G are each CH, N, C(1-4C alkyl) or C-Ph; L is O or S; R4 is halogen, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, OH, 1-4C alkoxy; R5 is H, 1-12C alkyl, phenyl(1-4C)alkyl or Ph (opt. substd. with halogen, 1-4C alkyl, 1-4C alkoxy or 2-5C acyl); R6 is 1-12C alkyl, Ph (opt. substd. with halogen, 1-4C alkyl, 1-4C alkoxy or 2-5C acyl); R7 is H or 1-12C alkyl; R8 and R9 are each H, OH, 1-4C alkyl, 1-4C alkoxy or 2-5C acyl; R10 is H or 1-4C alkyl; R11 and R12 are each H, OH, halogen, CF3, 1-4C alkyl or 1-4C alkoxy; A is (d), (e), X1A1X2, X2A2X3, X4A2X2, (CH2)1-2NHCO(CH2)1-3X2, -CH=CHA2X2; B is CH=CH, CH=N, S or (f); A1 is 2-4C alkylene, cis- or trans-CH2CH=CHCH2, CH2CCCH2, etc.; A2 is 1-5C alkylene; X1 is O, NH, S, SO, SO2, CO, CH2 or a gp. of formula (d); X2 is O, NH, S or a gp. of formula (e); X3 is NHCO, CONH, SO2NH or a gp. of formula (d); X4 is NHCO, CONH, NHSO2, SO2NH or NHCONH.
Inventors:
Anderskovitz Ralph
Shrom Kurt
Rent Ernst Otto
Himmelsbach Frank
Birke Franz
Fuchner Armin
Shrom Kurt
Rent Ernst Otto
Himmelsbach Frank
Birke Franz
Fuchner Armin
Application Number:
JP51370193A
Publication Date:
April 20, 1995
Filing Date:
January 14, 1993
Export Citation:
Assignee:
BOEHRINGER INGELHEIM KOMMANDITGESELLSCHAFT
International Classes:
A61K31/155; A61K31/34; A61K31/343; A61K31/35; A61K31/352; A61K31/357; A61K31/40; A61K31/415; A61K31/42; A61K31/421; A61K31/44; A61P1/04; A61P11/00; A61P11/06; A61P17/06; A61P29/00; A61P37/08; C07C257/18; C07C303/40; C07C311/29; C07C315/04; C07C317/18; C07C317/22; C07C317/44; C07C319/20; C07C323/18; C07C323/20; C07C323/32; C07C323/62; C07D213/78; C07D231/00; C07D263/32; C07D277/00; C07D307/78; C07D307/79; C07D311/22; C07D317/66; C07D319/18; C07D333/38; C07D333/00; (IPC1-7): C07C257/18; A61K31/155; A61K31/34; A61K31/35; A61K31/40; A61K31/415; A61K31/42; C07C311/29; C07C317/22; C07C323/32; C07D231/00; C07D263/32; C07D277/00; C07D307/79; C07D311/22; C07D317/66; C07D319/18
Attorney, Agent or Firm:
Minoru Nakamura (6 outside)