摘要:
The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.
摘要:
The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkylaminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6, acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要:
The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要:
Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,R.sub.2 represents alkyl having from 1 to 4 carbon atoms, andn is equal to 0 or 1,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.Two different reactions are described for making these compounds. They can be formulated into pharmaceutical compositions in the usual manner and exhibit central nervous system affecting activities.
摘要:
This invention relates to novel triazolo derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said triazolo derivatives for the treatment of diseases and also for the preparation of pharmaceutical compositions suitable for the treatment of the said diseases.The new triazolo derivatives of the general formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s); or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl); or q represents a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chain C.sub.1-12 alkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-4 alkyl);R.sup.4 and R.sup.7 each represent hydrogen, C.sub.1-6 alkyl or phenyl-(C.sub.1-4 alkyl) optionally bearing one or more halogen substituent(s);R.sup.5 and R.sup.6 each stand for C.sub.1-4 alkyl optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a heterocyclic group or a phenyl group optionally bearing one or more halogen, hydroxyl, cyano, nitro, alkyl, methylene dioxy and carbamoylmethoxy, di-(C.sub.1-4 alkyl)-amino or C.sub.1-4 alkoxy substituent(s) which latter may carry a di-(C.sub.1-4 alkyl)-amino group; furthermore one of R.sup.5 and R.sup.6 may represent hydrogen, orR.sup.5 and R.sup.6 together stand for C.sub.4-15 alkylene, or together with the adjacent carbon atom they are attached to form a heterocyclic group bearing a phenyl(C.sub.1-4 alkyl) substituent,possess valuable antianginal and tranquillant/sedative properties and are useful in therapy.
摘要:
The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom, with the proviso that if Q represents methylthio, dimethylamino, piperidino or morpholino, Y is other than benzyl,and pharmaceutically acceptable acid additional salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spasmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要:
The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl optionally bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom,and pharmaceutically acceptable acid addition salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spacmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要:
The compounds of the general Formula I ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different and each stands for hydrogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy or phenyl-(C.sub.1-3 alkoxy), or R.sup.1 and R.sup.2 together form C.sub.1-2 alkylenedioxy; with the proviso that at least one of symbols R.sup.1 and R.sup.2 is other than hydrogen and with the further proviso that R.sup.1 and R.sup.2 can not represent 3,4-dimethoxy substitution) andtheir pharmaceutically acceptable acid addition salts exhibit useful analgesic, antipyretic, anti-inflammatory, anti-anginal and antioxidant effect.
摘要:
The invention relates to pharmaceutical compositions having analgesic and/or anti-inflammatory effect comprising as active ingredient 2,4-diamino-5-(3,4-dimethoxy-benzyl)-pyrimidine or a pharmaceutically acceptable acid addition salt thereof.The pharmaceutical compositions of the present invention exhibit the desired analgesic and anti-inflammatory effect without causing undesired ulcerogenic side-effects.
摘要:
The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; orA represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, whereinR.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; andR denotes hydrogen or C.sub.1-7 alkyl,stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.