摘要:
(Di-tert-butylhydroxyphenyl)thio substituted hydroxamic acid derivatives of the formula: ##STR1## wherein X is straight or branched C.sub.1 to C.sub.15 alkylene which may be attached to Y through phenylene, provided that X is not n-butylmethylene; Y is CO--N(OH) or N(OH)--CO; and R is hydrogen or straight or branched C.sub.1 to C.sub.9 alkyl, C.sub.3 to C.sub.9 cycloalkyl, aryl, or aralkyl, provided that R is not hydrogen when Y--R is N(OH)--CO--R; or a pharmaceutically acceptable salt thereof; useful in treating arteriosclerosis, ulcer, inflammation, allergy, or the like.
摘要:
(Di-tert-butylhydroxyphenyl)thio derivatives of the formula: ##STR1## wherein R is cyano, carbamoyl, or 5-tetrazolyl; n is an integer of 2 to 6; provided that when R is cyano, n is not 2; or a pharmaceutically acceptable salt thereof; useful in treating arterioschlerosis, ulcer, inflammation, allergy, or the like.
摘要:
Phenolic thioethers of the formula: ##STR1## wherein R is a hydrogen atom or a protective group for carboxyl, X is a straight or branched C.sub.4 -C.sub.15 alkylene group, a straight or branched C.sub.1 -C.sub.15 alkylene group having a phenylene group or a straight or branched C.sub.2 -C.sub.15 alkenylene group, and their salts, which inhibit the denaturation of low density lipoproteins (LDL) and the incorporation of LDL by macrophages and are useful as anti-arteriosclerosis agents.
摘要:
9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.
摘要:
Highly effective anti-ulcer agents, i.e. Quassinoids of the following formula: ##STR1## wherein R is hydrogen or hydroxy;X is >C.dbd.CH.sub.2, >CH--CH.sub.3, or ##STR2## and the 3,4-dotted line indicates the presence or absence of a double bond.
摘要翻译:高效抗溃疡剂,即下式的类醌类:其中R是氢或羟基; X是> C = CH 2,> CH-CH 3或,并且3,4-虚线表示存在或不存在双键。
摘要:
A compound of the formula: ##STR1## [wherein R is dimethylamino or 1-pyrrolidinyl;R.sup.1 and R.sup.2 each is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl (optionally substituted by one member selected from the group consisting of cyano, C.sub.1 -C.sub.3 alkoxy, phenyl, and 5- or 6-membered heterocyclic group), C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.5 alkenyl (optionally substituted by one member selected from the group consisting of C.sub.1 -C.sub.3 alkoxy, phenyl, and phenoxy), C.sub.6 -C.sub.10 aryl (optionally substituted by one or two members selected from the group consisting of hydroxy, halogen, nitro, sulfamoyl, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkanoyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.3 alkanesulfonyl), or 5- or 6-membered heterocyclic group (optionally substituted by one member selected from the group consisting of oxo, halogen, C.sub.1 -C.sub.3 alkyl, and C.sub.1 -C.sub.3 alkoxy);and X is oxygen or sulfur]and its pharmaceutically acceptable acid addition salts is useful as histamine H.sub.2 blockers.
摘要:
An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;Y is oxo, thioxo, or cyanoimino;a is an integer of 1 to 3;b is an integer of 0 to 3;c is an integer of 1 to 4;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl; orR.sup.1 and R.sup.2 taken together represent pyrrolidinyl;R is hydrogen, cycloalkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: ##STR2## (wherein R.sup.3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy;R.sup.4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; orR.sup.3 and R.sup.4 taken together represent alkylidene or aralkylidene;with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents] and its pharmaceutically acceptable acid addition salts being useful as histamine H.sub.2 blockers, especially peptic ulcer remedies, are provided via several routes.