摘要:
A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms, R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with an other ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl, R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbon atoms, R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.
摘要:
Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3 whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia ##STR4## and R.sub.1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.
摘要:
The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.
摘要:
A fungicidal compound of the formula: ##STR1## wherein A is C.sub.5-10 cycloalkyl, R is hydrogen, C.sub.1-6 alkyl, phenyl optionally substituted by one or more groups selected from C.sub.1-4 alkyl, nitro, hydroxy, carboxy, sulfo, sulfonylamino, halogen, C.sub.1-4 alkoxy, C.sub.1-4 acyloxy, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 acyl, and N-(C.sub.2-5 alkoxycarbonyl)-sulfonylamino, or phenyl-(C.sub.1-4 alkyl) or a salt thereof.
摘要:
An inclusion complex is disclosed of N-(1-phenylethyl)-3, 3-diphenyl-propylamine or its hydrochloride complexed with a cyclodextrin as well as a process for the preparation thereof and pharmaceutical compositions containing same. The new inclusion complexes have coronary dilatory activity and have greater water soluble than simple N-(1-phenylethyl)-3, 3-diphenyl-propyl amine or the hydrochloride thereof.
摘要:
A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms,R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with another ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl,R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbons,R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.
摘要:
The invention concerns new compounds of the general formula (I) ##STR1## wherein R.sup.1 is hydrogen or phenyl optionally substituted by one or more of the following substituents: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms or phenyl, optionally substituted with one or more of the following groups: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; or R.sup.2 is a naphthyl group;R.sup.3 is alkyl having 1 to 4 carbon atoms, acyl or hydrogen;R.sup.4 hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.5 is cycloalkyl having 5 to 7 carbon atoms, alkyl having 1 to 6 carbon atoms, phenyl-(C.sub.1-4 -alkyl) in which the phenyl moiety may optionally be substituted with alkoxy having 1 to 4 carbon atoms, halogen or nitro;or R.sup.4 and R.sup.5 together represent a group of the general formula (V) ##STR2## wherein R.sup.6 is hydrogen or alkoxy having 1 to 4 carbon atoms, m and n stand for 0, 1 or 2and acid addition and quaternary salts thereof.The compounds of the general formula (I) are potent peripheral vasodilators and hypotensive agents. They increase the coronary blood flow and in addition to their slight antiinflammatory and diuretic acidivity possess strong antiarrhythmic properties.A process for the preparation of these compounds and pharmaceutical compositions containing them are also within the scope of the invention.
摘要:
There are provided new compounds of the formula I ##STR1## wherein both R.sup.1 moieties stand for an alkyl group having 1 to 4 carbon atoms or form together a methylene bridge,R.sup.2 is cyano or an alkoxycarbonyl group having 1 to 4 carbon atoms in the alkoxy position,R.sup.3 is hydroxy or alkanoyloxy having 1 to 4 carbon atoms in the alkoxy position in .alpha.-position or .beta.-steric position,and acid addition salts thereof. There is also provided a process for the preparation of the compounds of the formula I.
摘要:
The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.
摘要翻译:本发明涉及式I的新型氧化噻唑烷基嘌呤衍生物及其药学上可接受的盐,其中A代表C1-4亚烷基,R1代表C1-6烷基,羟基烷基,卤代烷基,羧基烷基,C5-6环烷基 或其中基团n为整数1-3的式 - (CH 2)n -NR 2 R 3的氨基烷基; R 2和R 3各自代表氢或C 1-4烷基或与它们相连的相邻氮原子一起形成5-或6-元含氮杂环,其可以任选地包含另外的氮原子或氧原子作为杂原子; 或R 1代表苯基,羟基苯基,羧基苯基,苄基或二甲氧基苄基。式I化合物可以通过本身已知的方法制备,并且可用于作为止咳剂的治疗。
摘要:
Compounds of the formula ##STR1## are disclosed wherein R.sup.1 stands for hydrogen, C.sub.1-4 straight or branched alkyl or pharmacologically acceptable cation,R.sup.2 stands for hydrogen, C.sub.1-4 alkanoyl, benzoyl, or benzoyl substituted by C.sub.1-4 alkyl or halogen, and R.sup.2 can further represent tetrahydropyranyl, trialkylsilyl or alkoxyalkyl,A stands for ethylene, cis or trans-vinylene or --C.dbd.C--,n may represent 2, 3 or 4. The compounds are highly effective in the inhibition of thrombocyte aggregation while at the same time exert only a very small hypotensive effect.