摘要:
Compounds of formula (I): wherein n, R1, R2, R3 and R7 are disclosed herein, are useful in treating disease-states associated with nuclear receptor activity. Pharmaceutical compositions comprising and methods of using said compounds are also disclosed herein.
摘要:
Compounds of formula (I): wherein n, R1, R2, R3 and R7 are disclosed herein, are useful in treating disease-states associated with nuclear receptor activity. Pharmaceutical compositions comprising and methods of using said compounds are also disclosed herein.
摘要:
A process for preparing a compound of formula (I'): ##STR1## comprising reacting a compound of formula (II'): ##STR2## with a compound of formula (III'): A'SH (III') wherein the reaction of the compound of formula (II') and the compound of formula (III') are carried out in the presence of a salt of a metal of Group II or III of the Periodic Table of Elements, wherein A' is an alkyl, aryl, aralkyl or heterocyclic, R.sup.1' is hydrogen or a carboxy protecting group, R.sup.2' and R.sup.3' can be hydrogen or alkyl, X' can be sulfur, k' is 1 or 2 and R.sup.4' is alkyl, alkenyl, aryl, aralkyl, cycloalkyl or heterocyclic.
摘要:
ConstitutionTricyclic heterocyclyl compounds having a general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 each represents H, a lower alkyl or lower alkoxy group, a halogen atom or halogeno-lower alkyl; R.sup.3 represents H or a lower alkyl group; R.sup.4 represents a substituted phenyl or naphthyl group; R.sub.5 represents H or a lower alkyl group; A represents a lower alkylene group; B represents an --O-- or --S-- group; and n is 0-1.EffectThe compounds have an excellent activity in the inhibition of acyl-CoA: cholesterol acyltransferase (ACAT) and are useful for the treatment and prophylaxis of atherosclerosis.
摘要:
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).
摘要:
A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.
摘要翻译:制备式(I)化合物的方法:其中:R1是氢或羟基保护基; R 2是烷基,烷氧基,卤素,任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基,任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基,其中Y是氧或硫,R 5和R 6各自是烷基,芳基或芳烷基,或者R 5和R 6以及它们 一起形成杂环基; R4是氢或氨基保护基; Z是硫或氧。 该方法包括使式(II)化合物:其中R 8,R 9和R 10相同或不同并且各自表示具有1至4个碳原子的烷基或苯基的式(II)化合物与 式(III)化合物:其中R 11表示酰氧基,烷基磺酰基,芳基磺酰基,烷基亚磺酰基或芳基亚磺酰基。
摘要:
A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;R.sup.41' is hydrogen or a hydroxy-protecting group;R.sup.42' is a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a halogen, an aryl or an aryloxy; R.sup.43' is hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a hydroxy, a halogen, a cyano, a nitro or a group of the formula --NR.sup.8' R.sup.9', where R.sup.8' and R.sup.9' are independently selected from the group consisting of hydrogen, amino-protecting groups, C.sub.1 -C.sub.6 alkyl groups and phenyl groups, or R.sup.8' and R.sup.9' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1, provided that (q'+s') is an integer of at least 2; R.sup.45' and R.sup.46' are independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and aryl groups, or R.sup.45' and R.sup.46' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1; Y' is oxygen or sulfur; and j' is 0, 1 or 2.
摘要:
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 or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.