摘要:
A new series of azulene derivatives are disclosed. These compounds are stable to light and heat and are useful as anti-ulcerative and anti-inflammatory agents. Such compounds can be synthesized by reacting 2H-cyclohepta(b) furan-2-one or its derivative substituted by a lower alkyl with a suitable enamine derived from a corresponding aldehyde or ketone, and then sulfonating the compound resulting from said reaction.
摘要:
A series of new azulene analogues are disclosed, which are represented by the following formula: ##STR1## wherein: R.sub.1 is --COOH, --COOR.sub.4 (R.sub.4 represents a lower alkyl), --CH.dbd.CH--COOH, --CH.sub.2 --COOH or --SO.sub.3 H;R.sub.2 is a hydrogen atom or lower-alkyl group;R.sub.3 is a hydrogen atom, a lower alkyl or benzyl group;A is --SO.sub.2 --, ##STR2## (R.sub.5 represents a lower alkyl); B is a phenyl, a lower alkylphenyl, a lower alkoxyphenyl, nitrophenyl, trifluoroalkylphenyl, mono-or di-halogenated-phenyl, naphthyl or tetrahydroaphthyl group;Y is an alkylene or alkenylene group.The compounds of the present invention are useful as thromboxane A.sub.2 and prostagrandin endoperoxide receptor antagonists.
摘要:
New therapeutic agent of carboxymethylidenecycloheptimidazole derivatives and method for the manufacture thereof are disclosed, which are represented by the following formula or its alkali addition salts ##STR1## (wherein R.sub.1 represents a lower alkyl; R.sub.2 represents H or isopropyl group; R.sub.3 represent H, a lower alkyl or --C(CH.sub.3)H--OCOOR.sub.4 (R.sub.4 is a lower alkyl or cyclohexyl) and .dbd.CHCOOR.sub.3 is substituted group at 4 or 8 position; A represents ##STR2## These compounds are useful as anti-hypertensive, anti-congestive heart failure agents and intraocular pressure lowering agents.
摘要翻译:公开了新的羧甲基环己烯并咪唑衍生物的治疗剂及其制备方法,其由下式表示,或其碱加成盐(1)(其中R 1表示低级烷基; R 2表示H或异丙基; R 3表示 H,低级烷基或-C(CH 3)H-OCOOR 4(R4是低级烷基或环己基)和= CHCOOR3是4或8位的取代基; A代表这些化合物可用作抗高血压, - 全身心力衰竭剂和眼压降低剂。
摘要:
New therapeutic agents of carboxylic acid derivatives are disclosed, which are represented by the compounds of the following formula (I) or its pharmaceutically acceptable salts, ##STR1## These compounds are useful as a matrix metalloproteinases (MMPs) inhibitors.
摘要:
New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line "- - - -" is two double bonds or saturated single bonds).These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.
摘要:
New agents of carbacyclin derivatives are disclosed, which are represented by the following formula: ##STR1## wherein A is a --CH.dbd.CH-- or --C.tbd.C-- group. B is a substituted or unsubstituted indanyl group, substituted or unsubstituted benzodioxanyl group, substituted or unsubstituted benzodioxolanyl group or 2,3,5,6,7, 8-hexahydrobenzodioxanyl group. D is --CH.sub.2 -- or --O--. .about.OH group represents .alpha. or .beta. configuration of OH group; and ##STR2## These compounds are useful as anit-ulcer, anti-hypertensive or anti-thrombotic agents.
摘要:
New antiarrythmic diamines are disclosed. pa These new compounds are represented by the following general formula: ##STR1## wherein: A is NO.sub.2, RSO.sub.2 NH or RSO.sub.2, whereinR represents a lower alkyl group.B is >CH.sub.2 or >C.dbd.O,Y is a lower alkyl group,Z is a lower alkyl or benzyl group,n is an integer 2 or 3.The compounds of the present invention are useful as antiarrhythmic agents.
摘要:
A series of new 1,3-dioxane derivatives are disclosed. These compounds have an outstanding anti-peptic ulcerative activity and are useful as novel anti-peptic ulcer agents. Such compounds are synthesized by reacting a 1,3-butanediol derivative with suitable ketone.
摘要:
Ether and amide derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment of diabetes. R1—A—R2 (I) wherein (with the provisos that (i) when A is —O—, then n is 2 or 3 (ii) when then n is 1 or 2. R3 is OH—, CH3SO2NH—, CF3SO2NH—, CH3SO2NHCH2—, CF3SO2NHCH2—, HOOC—, CH3OOC—, HOOC—CH2SO2NH—, CF3—CH2SO2NH—, R8—NHSO2—, R8—NHSO2—CH2—, HOOC—CH2—O—, HSO3N═CH—, or R9—SO2NHCO—; R4 is H, OH, O-alkyl or O—CH2OCH3; R5 is H, halogen atom, —CH2COOH or OH; R6 and R7 are hydrogen, t-butyl or pyrolidyl; R8 is hydrogen or lower alkyl; R9 is alkyl or thienyl; R10 is lower alkyl) or a pharmaceutically acceptable salt.
摘要翻译:公开了醚和酰胺衍生物,其由下式(I)及其药学上可接受的盐表示,并且其可用于治疗糖尿病。其中(条件是(i)当A为-O-时,则 R3是OH-,CH3SO2NH-,CF3SO2NH-,CH3SO2NHCH2-,CF3SO2NHCH2-,HOOC-,CH3OOC-,HOOC-CH2SO2NH-,CF3-CH2SO2NH-,R8-NHSO2 - ,R8-NHSO2-CH2-,HOOC-CH2-O-,HSO3N = CH-或R9-SO2NHCO-; R4是H,OH,O-烷基或O-CH2OCH3; R5是H,卤素原子,-CH2COOH 或OH; R 6和R 7为氢,叔丁基或吡咯烷基; R 8为氢或低级烷基; R 9为烷基或噻吩基; R 10为低级烷基)或其药学上可接受的盐。
摘要:
A new series of benzofuran and benzothiophene derivatives are disclosed. These compounds have a structure which can be obtained by substituting the third position of 2-lower alkyl-benzofuran or 2-lower alkyl-benzothiophene with a substituted benzene derivative, itaconic acid derivative or a substituted phenoxymethyl tetrazole derivative. They are useful as diuretics without side effects of elevating serum uric acid levels and can be used in the treatment of hyperuricemia.