EP 0680472 A1 19951108 - 4,5-DIPHENYLIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ACYL COENZYME A: CHOLESTEROL-0-ACYL-TRANSFERASE (ACAT) INHIBITOR.
Title (en)
4,5-DIPHENYLIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ACYL COENZYME A: CHOLESTEROL-0-ACYL-TRANSFERASE (ACAT) INHIBITOR.
Title (de)
4,5-DIPHENYLIMIDAZOL DERIVATE, DEREN HERSTELLUNG UND DEREN VERWENDUNG ALS ACYL COENZYM A: CHOLESTERIN-O-ACYL-TRANSFERASE (ACAT) INHIBITOR.
Title (fr)
DERIVES DE 4,5-DIPHENYLIMIDAZOLE, LEUR PREPARATION ET LEUR UTILISATION EN TANT QU'INHIBITEUR DE L'ACYL-COENZYME-A: CHOLESTEROL-O-ACYL-TRANSFERASE (ACAT).
Publication
Application
Priority
- EP 9403684 W 19941109
- IT MI932468 A 19931122
Abstract (en)
[origin: WO9514673A1] The invention provides new diphenylimidazoles of formula (I) wherein: Ph is phenyl; and wherein A) when Z is 4,5-diphenylimidazol-2-ylthio, then p is zero and Y is a --(Ch2)m--X--(CH2)n-- group in which a) m and n being the same are 1 or 2 and X is (1), (2) or (3), wherein R is hydrogen or an optionally omega-hydroxy substituted C1-C10 alkyl chain, or b) m and n are 2 and X is (4), (5), (6) or (7), in which q is 1 or 2; or B) when Z is an aryloxy group unsubstituted or substituted by a substituent chosen from C1-C6 alkyl, halo-C1-C6 alkyl, C1-C6 alcoxy, halogen, amino or an aryloxy group substituted by two substituents chosen from C1-C6 alkyl, halo-C1-C6 alkyl, C1-C6 alkoxy, halogen, amino, nitro, C1-C6 alkoxy-carbonyl, di(C1-C6 alkyl) amino and --NHCONH-C1-C6 alkyl, or an aryloxy or arylthio group substituted by three sustituents chosen independently from hydroxy and C1-C6 alkyl, or a group chosen from 2-pyridyloxy, an optionally substituted imidazo[1,2-b]pyrazol-1-yl group, 2,3--dihydro-1H-imidazo[1,2--b]pyrazol-1-yl and (8) in which R1 is (9), (10) or (11), in which each of R2, R3 and R4 independently is hydrogen, C1-C4 alkyl or C1-C4 alkoxy; then p is zero or 1 and Y is a --(CH2)m--X--(CH2)n-- group wherein m and n are 1, X is a --(CH A)t-- group wherein A is hydrogen or hydroxy and t is zero or an integer of 1 to 10, or a group chosen from (12), (13), (14), (15) in which R is as defined above; or C) when Z is thiazolidin--2,4--dione--5--yl, then p is zero and Y is a bond or a --(CH2)m--X--(CH2)n-- group in which m and n are 1, X is a --(CH2)t-- group in which t is as defined above, and the pharmaceutically acceptable forming salts thereof, which have an ACAT inhibiting activity and are thus useful in the treatment of dyslipidemia, atherosclerosis and coronary diseases.
IPC 1-7
C07D 233/84; C07D 401/12; C07D 417/12; C07D 405/12; C07D 487/04; A61K 31/415; A61K 31/44; A61K 31/335; A61K 31/425
IPC 8 full level
A61K 31/415 (2006.01); A61K 31/425 (2006.01); A61K 31/44 (2006.01); A61K 31/4427 (2006.01); A61K 31/443 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 13/02 (2006.01); A61P 15/00 (2006.01); A61P 43/00 (2006.01); C07D 233/84 (2006.01); C07D 401/12 (2006.01); C07D 405/12 (2006.01); C07D 417/12 (2006.01); C07D 487/04 (2006.01)
CPC (source: EP)
A61P 9/08 (2018.01); A61P 9/10 (2018.01); A61P 13/02 (2018.01); A61P 15/00 (2018.01); A61P 43/00 (2018.01); C07D 233/84 (2013.01); C07D 401/12 (2013.01); C07D 417/12 (2013.01); C07D 487/04 (2013.01)
Designated contracting state (EPC)
DE ES FR GB IT NL SE
DOCDB simple family (publication)
WO 9514673 A1 19950601; AU 8061894 A 19950613; CA 2154475 A1 19950601; EP 0680472 A1 19951108; IT 1265209 B1 19961031; IT MI932468 A0 19931122; IT MI932468 A1 19950522; JP H08506122 A 19960702
DOCDB simple family (application)
EP 9403684 W 19941109; AU 8061894 A 19941109; CA 2154475 A 19941109; EP 94931591 A 19941109; IT MI932468 A 19931122; JP 51478494 A 19941109