Abstract:
The invention is concerned with the new use of known catechol derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms; X is nitro, halogen or cyano and R.sub.3 is chlorine, nitro, cyano or a radical of the formula ##STR2## wherein R.sub.4 is hydrogen, cyano, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms and R.sub.5 is cyano, alkanoyl having 2 to 5 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, carboxyl or phenylcarbonyl unsubstituted or substituted with one to three methoxy groups or pharmaceutically acceptable salt thereof. The new use is the treatment and prophylaxis of ulcers and lesions in the gastrointestinal tract.
Abstract:
Dyes suitable for dyeing and printing cellulose-containing fiber materials which produce blue dyeings and prints having good fastness properties. These dyes are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenoxy, carboxyl carbamoyl or C.sub.1 -C.sub.4 alkanoylamino; R.sub.3 is hydrogen, sulfo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, carboxyl, carbamoyl, N-C.sub.1 -C.sub.4 alkylcarbamoyl, N,N-di-C.sub.1 -C.sub.4 alkylcarbamoyl, C.sub.1 -C.sub.4 alkylsulfonyl, sulfamoyl, N-C.sub.1 -C.sub.4 alkylsulfamoyl or N,N-di-C.sub.1 -C.sub.4 alkylsulfamoyl; R.sub.4 is a radical of the formula ##STR2## R.sub.5 and R.sub.6 are independently of each other hydrogen or unsubstituted or hydroxyl-, sulfo-, sulfato-, carboxyl-, cyano-, halogen-, C.sub.1 -C.sub.4 alkoxycarbonyl-, C.sub.1 -C.sub.4 alkanoyloxy- or carbamoyl-substituted and uninterrupted or, except in the case of methyl, --O--, --S-- or --NH--interrupted C.sub.1 -C.sub.6 alkyl; R' is hydrogen or C.sub.1 -C.sub.6 alkyl; t is an integer from 0 to 4; the phenyl radical (a) is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl substituted by hydroxyl-, sulfo or sulfato, C.sub.1 -C.sub.4 alkoxy, halogen, sulfo, carboxyl or hydroxy, and A is a radical of the formula ##STR3## where R' is as defined above, (alk) is C.sub.1 -C.sub.6 alkylene, T is hydrogen, halogen, hydroxyl, sulfato, carboxyl, cyano, C.sub.1 -C.sub.4 alkanoyloxy, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl or a radical --SO.sub.2 --Z, V is hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 alkyl or a radical of the formula -(alk)--CH.sub.2 --SO.sub.2 --Z, where (alk) is as defined above, Z is a radical of the formula --CH.dbd.CH.sub.2 l or --CH.sub.2 --CH.sub.2 --Y, Y is a leaving group selected from the group consisting of --OSO.sub.3 H, --SSO.sub.3 H, --OCOCH.sub.3, --OCO--C.sub.6 H.sub.5, OPO.sub.3 H.sub.2, --Cl, Br, --F, ##STR4## p, q and r are each independently of the others an integer from 1 to 6.
Abstract:
Aminobenzamide derivatives of the formula (I) ##STR1## wherein: R.sub.1 and R.sub.2 each represents a lower alkoxy group,R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower acyl group, a lower alkoxycarbonyl group or --R.sub.5 --SO.sub.3 Z, wherein R.sub.5 represents a lower alkylene group and Z represents an alkali metal or an alkaline earth metal,R.sub.4 represents an amino group, a morpholino group or a lower alkylamino group which may be substituted with a hydroxyl group at the alkyl moiety thereof, with the proviso that, when R.sub.3 represents a hydrogen atom, R.sub.4 cannot be an amino group,Y represents a hydrogen atom, a halogen atom or a lower alkoxy group,n represents an integer of from 1 to 6,and salts thereof; are disclosed. These compounds have excellent anti-peptic ulcer activities, and chemical and physical stabilities.
Abstract:
New chemical reactions of 1,1,2-trifluoro-1,3-butadiene provide simple access to a series of new fluorinated alkene derivatives. These derivatives provide a simple, general methodology for the stereocontrolled preparation of 2-fluoro-2-alkenoate esters and related monofluoroalkene derivatives which include fluoro analogs of known insecticides, pheromones or pharmaceuticals. A new method for the preparation of 1,1,2-trifluoro-1,3-butadiene is also provided.
Abstract:
The present invention relates to 1-substituted derivatives of 4-methoxy-2,3,6-trimethylbenzene which are useful in cosmetic or pharmaceutical preparations for use in the treamtnet of dermatological complaints connected with a keratinisation disorder, dermatological complaints having an inflammatory and/or immuno-alleric component or ophthalmological complaints.
Abstract:
The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.8, together with the nitrogen atom to which they are bound, constitute a fully or partly saturated heterocyclic ring consisting of 5-8 ring atoms and which may comprise in addition an O, N or S-atom as the second hetero atom, and may be substituted.
Abstract:
Compound, corresponding to the formulaC.sub.8 H.sub.17 --(C.tbd.C--CH.sub.2).sub.3 --CH.sub.2 CH.sub.2 CH.sub.2 R O (I)in which R is a C.sub.1 -C.sub.8 lower alkoxy or C.sub.4 -C.sub.6 cycloalkoxy group, substituted with one or more hydroxyl groups and/or interrupted by one or more hetero atoms chosen from oxygen and sulphur, an amino group of structure ##STR1## in which R.sub.1 or R.sub.2, which may be identical or different, denote a hydrogen atom or a linear or branched C.sub.1 -C.sub.8 lower alkyl radical, optionally interrupted by one or more hetero atoms chosen from oxygen, sulphur and nitrogen, this alkyl radical being able to be substituted with one or more hydroxyl groups, R.sub.1 and R.sub.2 not being able to denote hydrogen simultaneously, or alternatively R.sub.1 and R.sub.2 form, together with the nitrogen atom, a heterocyclic system optionally containing oxygen, sulphur or nitrogen as an additional hetero atom, one of the radicals R.sub.1 and R.sub.2 also being able to denote, when the other is a hydrogen atom, an aryl radical of formula (II): ##STR2## or alternatively a benzyl radical of formula (III): ##STR3## in which formulae R.sub.3 and R.sub.4, denote, independently of each other, a hydrogen atom, a C.sub.1 -C.sub.4 alkyl radical, a hydroxyl group, a halogen atom or a carboxyl or trifluoromethyl group, the amine group also being able to originate from a sugar, and also the isomers and salts thereof which are pharmaceutically and cosmetically acceptable.
Abstract translation:对应于式C 8 H 17 1-(C 3 B c C -CH 2)3 -CH 2 CH 2 CH 2 COR(I)的化合物,其中R是被一个或多个羟基取代和/或被一个或多个羟基取代的C 1 -C 8低级烷氧基或C 4 -C 6环烷氧基 一个或多个选自氧和硫的杂原子,结构“IMAGE”的氨基,其中可以相同或不同的R 1或R 2表示氢原子或直链或支链C 1 -C 8低级烷基,任选地中断 通过一个或多个选自氧,硫和氮的杂原子,该烷基能够被一个或多个羟基取代,R1和R2不能同时表示氢,或者R1和R2与 氮原子,任选地含有氧,硫或氮作为另外的杂原子的杂环体系,当另一个是氢原子时,基团R 1和R 2之一也可以表示式(II)的芳基: (II)或苄基r 式(III)的化合物:其中式R3和R4彼此独立地表示氢原子,C1-C4烷基,羟基,卤素原子或羧基或三氟甲基的式(III) 基团,也可以来自糖的胺基,以及其药学和化学上可接受的异构体和盐。
Abstract:
The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and stand for hydrogen or halogen or a trihalomethyl, lower alkyl, lower alkoxy, nitro, hydroxyl, aralkyloxy or an 1-(2-propenyl-4-piperazinyl) group;R.sub.5 stands for hydrogen or a C.sub.1-4 alkyl group;R.sub.6 represents a C.sub.3-6 alkyl, alkenyl, alkynyl group or a ##STR2## group, wherein R.sub.7 means a C.sub.2-5 alkyl, alkenyl or alkinyl group; andis 2 or 3,with the provisos that:R.sub.6 is different from isopropyl, n-butyl and isobutyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2;R.sub.6 is different from isopropyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2; or when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-methyl group and n is 2; andR.sub.6 is different from propionyl group when R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen and n means 2.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.
Abstract:
The present invention relates to new diselenobis-benzoic acid amides of primary and secondary amines of the general formula (I): ##STR1## and processes for the treatment of diseases in humans caused by a cell injury.
Abstract:
Dihydrodibenzocycloheptyliden-ethylene derivatives of the general formula: ##STR1## in which, R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; andR.sub.3 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or --CO--(C.sub.1 -C.sub.4 alkyl),are disclosed. These compounds are useful in the treatment of ulcer conditions.