Abstract: The invention relates to a process for the preparation of 1-alkyl-1,2,3,4-tetrahydroisoquinoline derivatives of the general formula ##STR1## The compounds can be used for the preparation of tetrahydroisoquinolines of the reticuline type, or of the norreticuline type, by reductive removal of the OH groups or, if they carry an acyl protective group on the nitrogen, for the preparation of isoquinolines of the papaverine type by acid-catalyzed hydrolysis with removal of the acyl groups and simultaneous removal of the hydroxyl groups.These 1-alkyl-1,2-dihydroisoquinoline derivatives can then be used for the preparation of isoquinolines of the papaverine type by aromatization by means of acids or hydrazine.

Abstract: Carbonate esters with rapamycin at position 42 or positions 31 and 42 have been shown to have immunosuppressant properties and are useful in the treatment of transplant rejections and autoimmune diseases. These esters are represented by the formula below: ##STR1## wherein: R.sup.1 and R.sup.2 are independently H or --COOR.sup.3 but both R.sup.1 and R.sup.2 cannot be H, andR.sup.3 is C.sub.1 -C.sub.6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, or Ar--(CH.sub.2).sub.n -- where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; pyridinyl, indolyl, quinolyl or furanyl;or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.t may be H, loweralkyl, loweralkoxy, or halo: R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

Abstract: Tetrahydroisoquinoline amides having the general structure ##STR1## are disclosed, the substituents defined hereinbelow, which amides are useful in inhibiting human leukocyte and neutrophil elastaes.

Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O--or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl,andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereofand their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

Abstract: The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ;R.sup.2 is hydrogen or --SiR.sup.3 R.sup.4 R.sup.5 ; andR.sup.3, R.sup.4, and R.sup.5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-3 alkoxy, n-botoxy, i-botoxy, sec-butoxy, R.sup.7 R.sup.8 N-- (wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-3 alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.l OR.sup.19 (wherein R.sup.19 is hydrogen or C.sub.1-3 alkyl, and l is 1,2 or 3); or when located at the ortho position to each other, R.sup.1 and R.sup.2, or R.sup.3 and R.sup.4 together form --CH.dbd.CH--CH.dbd.CH--; or when located at the ortho position to each other, R.sup.1 and R.sup.2 together form --OC(R.sup.15) (R.sup.16)O--(wherein R.sup.15 and R.sup.16 are independently hydrogen or C.sub.1-3 alkyl); Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --CH.dbd.CH-- or -- CH.dbd.CH--CH.sub.

Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O-- or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl, andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereof and their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.

Abstract: Novel compounds represented by the formula: ##STR1## wherein R.sub.1 represents an alkyl group having 1 to 3 carbon atoms, R.sub.2 represents an amino group or a group of formula ##STR2## in which R.sub.4 represents an alkyl group having 1 to 3 carbon atoms, R.sub.5 represents an alkyl group having 1 to 3 carbon atoms or may combine with R.sub.6 to form a five or six membered ring containing 4 to 5 carbon atoms, R.sub.6 represents a hydrogen atom or may combine with R.sub.5 to form a five or six membered ring containing 4 to 5 carbon atoms, R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms or a halogen atom, X represents a carbonyl group or a methylene group, Y represents a sulfur atom or a vinylene group and pharmaceutically acceptable salts thereof which exhibit a vasodilating activity and inhibitory activity for platelet aggregation. Thus, they are useful as therapeutic agents for treatment of angina pectoris, hypertension, throbosis and the like.

Abstract: Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.

Abstract: A derivative of rapamycin in which the 27-position has the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl, or --CH.sub.2 Ar;Ar is ##STR2## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;X is N, O, or S;or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: This invention provides an oxidized derivative of rapamycin in which the hydroxyl at the 42-position has been oxidized to the corresponding ketone or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive and antifungal activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, and fungal infections and a process for the preparation of this oxidized derivative of rapamycin.

Abstract: A derivative of rapamycin where one, two, or three of the double bonds at the 1-,3-, or 5-positions of rapamycin have been reduced to the corresponding alkane, or a pharmaceutically acceptable salt thereof, which by virtue of its antifungal activity is useful in treating fungal infections.

Abstract: Compounds of the formula ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group--(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar wherein Z represents O, S or --CH.sub.2 --and Ar is phenyl, optionally substituted by one or two groups selected from the group consisting of hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2, CF.sub.3, CN, R.sup.6 -S(O).sub.x, R.sup.7 --CO--,(R.sup.8 R.sup.9)NCO-and phenyl, wherein x is 0, 1 or 2, and each R.sup.6, R.sup.7, R.sup.8 and R.sup.9 is independently C.sub.1 to C.sub.6 alkyl or two adjacent groups on Ar may form together an additional fused benzenoid ring; n and m independently represent integers of from 1 to 8; and ring Q represents one of the rings Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 below: ##STR2## X is N or C--R.sup.1 ; Y is N or C--R.sup.4 ;W represents O or S;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.

Abstract: A process for preparing cotarnine is provided which comprises oxidizing the amino group of a tetrahydroisoquinoline compound represented by the following formula (I): ##STR1## to convert said compound into a dihydroisoquinolinium salt represented by the following formula (II): ##STR2## wherein A.sup.- represents an anion, and then hydrolyzing said dihydroisoquinolinium salt.

Abstract: Halogenated hydroxyquinoline compounds such as 5-chloro-7-bromomethyl-8-hydroxyquinoline are prepared by contacting a 5-halo-8-hydroxyquinoline with formaldehyde to produce a cyclic dioxane and then contacting with concentrated hydrobromic acid to form the desired halogenated hydroxyquinoline compound.The compounds of this invention are usefual as intermediates in the production of ion-exchange resins.

Abstract: Derivatives of 2-(2-aminobenzyl or 2-nitrobenzyl)-1,2,3,4-tetrahydroisoquinoline of the formula ##STR1## in which each of substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 or R.sub.8 may represent either a hydrogen atom, a straight or branched chain alkyl group, a straight or branched chain alkoxy group, a hydroxy group or corresponding esters, a phenoxy group, a benzyloxy group, a methylenedioxy bridge (--O--CH.sub.2 --O--) when this substituent is connected with an adjacent carbon, a halogen, a nitro group, an amine function corresponding to primary or secondary or tertiary amine, or quarternary ammonium;each of substituents R.sub.9 or R.sub.10 may represent either a hydrogen atom, a straight or branched chain alkyl group, an arylalkyl group, an amine function corresponding to primary or secondary or tertiary amine or quarternary ammonium, or may each be oxygen atoms;each of substituents R.sub.11 or R.sub.

Abstract: The instant invention relates to optically pure, L-(S)forms of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid compounds and their method of preparation from optionally pure L-phenylalanine precursor compounds and their preparation utilizing novel in situ cationic catalyst systems.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.

Abstract: A compound of the formula: ##STR1## (wherein R is hydrogen, hydroxy, methoxy, acetoxy, acetoxymethyl or trifluoromethyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each is hydrogen, hydroxy, optionally substituted C.sub.1 -C.sub.5 alkoxy, acetoxy, propynyloxy, allyloxy or benzyloxy; or R.sup.2 and R.sup.3 taken together form methylenedioxy;R.sup.5 is hydrogen, hydroxymethyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.5 acyloxymethyl or phthalidyl; and n is 0 or 1 except for the case in which R is methoxy and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each is hydrogen) or its pharmaceutically acceptable acid addition salt, being useful as anti-ulcer agents is provided through several routes.

Abstract: The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.

Abstract: Isoquinoline derivatives of compounds of the general formula ##STR1## that exhibit cardiotonic and/or phosphodiesterase fraction III inhibiting properties and/or renal vasodilating are pharmacologically active in the treatment of cardiac conditions. Methods for synthesizing and using the compounds are described.

Abstract: Substituted 3-isoquinolinol compounds of the general formula ##STR1## that exhibit cardiotonic, renal vasodilating and phosphodiesterase fraction III properties are pharmacologically active in the treatment of cardiac conditions. Methods for synthesizing and using those compounds are described.

Abstract: This invention relates to new 3-(hydroxymethyl)-isoquinoline derivatives of the general formula (I), their acid addition salts, and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R and R.sup.1 are identical or different and stand for a hydrogen or halogen atom, a nitro or a C.sub.1-4 alkoxy group,R.sup.2 stands for a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.3 and R.sup.4 are identical or different and stand for a hydrogen atom or a C.sub.1-4 alkyl group, or R.sup.3 and R.sup.4 combined denote a methylene group,with the proviso that when R stands for 3-methoxy, R.sup.1 for 4-methoxy, R.sup.3 and R.sup.4 are identical and represent methyl or ethyl groups, R.sup.2 is other than hydrogen atom.

Abstract: The present invention relates to novel antibacterial agents, corresponding to the following general formula I ##STR1## in which: Q represents an aromatic ring,X represents a hydrogen atom or a linear or branched alkyl group,Y represents a linkage or an alkyl group,Z represents a hydrogen atom, an alkyl, aralkyl or heteroalkyl group.These compounds constitute anti-bacterial agents with multiple pharmacological activity.

Abstract: A tetrahydroisoquinoline derivative represented by formula: ##STR1## wherein R.sup.1 represents hydrogen or methyl and X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are defined as follows:(1) X.sup.1 represents --OH, ##STR2## or OR.sup.2 wherein R.sup.2 represents lower alkyl when X.sup.2, Y.sup.1 and Y.sup.2 represent hydrogen(2) X.sup.1 and X.sup.2 together form oxo (.dbd.O), when Y.sup.1 and Y.sup.2 represent hydrogen or(3) Y.sup.1 and Y.sup.2 together form oxo (.dbd.O), when X.sup.1 and X.sup.2 represent hydrogen which is useful as an intermediate in preparation of Cotarnine.

Abstract: There is provided a novel anisole derivative represented by the following formula (I): ##STR1## wherein A to D are defined as follows: (1) A, B and C are each a hydrogen atom, and D represents --OH, a halogen atom, --CO.sub.2 R.sup.1 of which R.sup.1 represents a lower alkyl group, --SO.sub.2 R.sup.2 of which R.sup.2 represents a lower alkyl group, or ##STR2## or (2) A and C are each a hydrogen atom, B is --OH, and D represents --CO.sub.2 R.sup.3 of which R.sup.3 represents a lower alkyl group; or(3) A is a hydrogen atom, B and C form an oxo group .dbd.O together, and D represents --CO.sub.2 R.sup.4 of which R.sup.4 represents a lower alkyl group; or(4) B and C are each a hydrogen atom, D is a halogen atom, and A represents --CHO.

Abstract: This invention relates to novel heterocyclic carboxamides which increase the activity of the immune system and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds and methods of treatment therewith.

Abstract: Disclosed herein is an improved process for preparing 1RS-3'RS epimer of aminated phthalideisoquinolines represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen atom or a lower alkoxy group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen atom, amino group or a lower alkoxy group with at least one of R.sup.3 -R.sup.6 being amino group, and R.sup.7 is a lower alkyl group. The improvement comprises, after having reduced a mixture of epimers of corresponding nitro compounds of the general formula (I) wherein the amino group is replaced by nitro group into the amino compounds (I), treating said amino compound at a temperature in the range of 20.degree.-100.degree. C. in an aliphatic lower alcohol in the presence of an alkali to epimerize 1RS-3'SR epimer of said amino compound into said 1RS-3'RS epimer thereof.

Abstract: Disclosed herein is a process for preparing phthalide derivatives represented by the general formula (IV): ##STR1## wherein R.sup.1 to R.sup.7 are herein defined, comprising (i) reacting a nitrophthalide of the general formula (I) defined herein with an isoquinoline of the general formula (II) defined herein, and (ii) reducing the resultant phthalideisoquinoline of the general formula (III) defined herein. The process is characterized in (A) that the reaction defined in (i) is carried out in methanol, and/or (B) that the nitrophthalide of the general formula (I) is a nitrophthalide obtained by a reaction of a phthalide of the general formula (V) defined herein with copper nitrate or zinc nitrate.

Abstract: Water soluble prodrugs of rapamycin are disclosed which are useful as components in injectable pharmaceutical formulations for the treatment of tumors in mammals.

Abstract: There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally interrupted by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is phenyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or together are a group X; SO.sub.2 NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X or S(O).sub.m R.sub.13 wherein m is 1 or 2 and R.sub.13 is C.sub.

Abstract: Circulation-active novel ring-bridged 1,4-dihydropyridines of the formula ##STR1## in which ##STR2## is an aryl or heterocyclic radical, X is an alkyl or alkoxy radical, andZ is a carboxylic or sulphonic acid ester radical,or pharmaceutically acceptable acid addition salts thereof, which affect the circulatory system.

Abstract: 1-Phenylisoquinoline derivatives of the general formula I ##STR1## and a process for their preparation are described. They act on the central nervous system, in particular as antidepressants.

Abstract: This invention relates to novel heterocyclic carboxamides which increase the activity of the immune system and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds and methods of treatment therewith.

Abstract: New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bri

Abstract: Novel 5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acids substituted in the 5-position by lower-alkylamino or di-lower-alkylamino, useful as antibacterial agents, are prepared from 8-hydroxy-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid or a lower-alkyl ester thereof via a series of novel intermediates.

Abstract: A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl, R.sub.3 is phenyl having substituents selected from the group consisting of lower alkenyloxy, mercapto, lower alkylthio, sulfamoyl and mono or disubstituted sulfamoyl, or a heterocyclic group, R.sub.4 and R.sub.5 are each hydroxy or protected hydroxy and X is --O-- or--S--.

Abstract: Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof are produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and when desired hydrolyzing or removing protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.

Abstract: This invention relates to substituted 1-(.alpha.-aminocarbonyl-benzyl)-3,4-dihydro-isoquinolines in the racemic or optically active form and the non-toxic pharmacologically acceptable salts thereof. These compounds are useful in the promotion of blood circulation in warm-blooded animals.