Amide derivatives having ACAT inhibitory activity, their prepara

Details Amide derivatives having ACAT inhibitory activity, their prepara Amide derivatives having ACAT inhibitory activity, their prepara

1996-09-18

1999-03-09

Kumar, Shailendra

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514464, 514465, 514469, 514524, 514563, 514617, 514618, 514619, 549377, 549378, 549441, 549467, 549468, 554 35, 554 36, 554 37, 558412, 558411, 558415, 564154, 564155, 564158, A61K 31335, A61K 31165, C07D31916, C07C23305

Patent

active

058801472

ABSTRACT:
Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen;
R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).

REFERENCES:
patent: 4536346 (1985-08-01), Shepherd et al.
patent: 5534529 (1996-07-01), Yoshida et al.
patent: 5614550 (1997-03-01), Yoshida et al.
Chemical Abstracts, O'Brien et al., "Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents", vol. 121, No. 1, Jul. 4, 1994, Abstract No. 8837r.

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