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: A compound of the formula ##STR1## wherein R.sub.1 and R.sub.6 independently represent hydroxy, C.sub.1 -C.sub.4 -alkoxy, substituted C.sub.1 -C.sub.4 - alkoxy, amino, or substituted amino, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, or C.sub.2 -C.sub.4 -alkenyl, R.sub.3 represents cyclo-C.sub.3 -C.sub.6 -alkyl, phenyl, phenyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, nitro, or C.sub.1 -C.sub.4 -alkoxy, or cyclo-C.sub.3 -C.sub.6 -alkyl fused with benzene, or wherein R.sub.2 and R.sub.3 are connected and together with the adjacent --CH-group and the adjacent N-atom form a saturated or partially saturated, monocyclic, five- or six-membered heterocyclic group or form a saturated or partially saturated, bicyclic heterocyclic group containing five or six atoms per ring, R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sub.5 represents an acyl group, are useful as antihypertensive and cardioactive agents.

Abstract: The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinol ine derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hdyroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is alky having from 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an optionally substiutted heterocyclic group,and acid addition and quaternary salts thereof.Compounds of the formula (I) are pharmaceutically active, in particular show spasmolytic, analgesic, antipyretic activity and have a protecting effect in acute alcoholic intoxication.

Abstract: New chemical compounds having the generic formula: ##STR1## where n is 3 to 16 carbon atoms and where X is one equivalent of a monovnt or polyvalent anion, and having utility as toxic agents.

Abstract: The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof.

Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.

Abstract: The invention relates to new bis(substituted methyl)-methyl-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a ##STR2## group, in which R.sup.4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or --NH--phenyl,X is oxygen or sulfur,R.sup.7 is hydroxyl, halogen or an ##STR3## group, R.sup.8 is halogen, alkoxy from 1 to 4 carbon atoms or an ##STR4## group, in which X has the same meaning as defined above, andR.sup.9 independently from R.sup.4 may have the same meanings as defined for R.sup.4, or is an --NH(C.sub.1-4 -alkyl) or C.sub.3-6 -cycloalkyl group,and salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds and pharmaceutical compositions containing them.

Abstract: The invention relates to novel pharmaceutical compounds for treatment for ulcer of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl or hydroxyiminomethyl,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino or guanidino optionally substituted with dimethylaminomethylene,R.sup.3 is dihydroisoquinolyl which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino or guanidino,Q is --CO--, andn is an integer of 0 or 1, andpharmaceutically acceptable salts thereof.

Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: There are disclosed aza analogs of carboxyalkyl dipeptide derivatives and related compounds which are useful as converting enzyme inhibitors and as antihypertensives said compounds being represented by the general formula: ##STR1## wherein A and B can be joined together to form various ring structures.

Abstract: Compounds of the formula: ##STR1## where R.sup.3 is ##STR2## where n is 1-3 and the R.sup.a 's and R.sup.b 's are independently hydrogen or loweralkyl; and pharmaceutically acceptable salts thereof; are inhibitors or angiotensin I converting enzyme useful as antihypertensive agents.

Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.

Abstract: What are disclosed are indole, quinoline and isoquinoline compounds of the formula ##STR1## in which n denotes 0 or 1, m denotes 1 or 2, but (n+m).ltoreq.2, A together with the bridgehead carbon atoms denotes a benzene or a cyclohexane ring, Y.sub.1 denotes hydrogen, lower alkanoyl or lower cycloalkanoyl, benzoyl nicotinoyl or a radical of the formula II, and Y.sub.2 denotes methyl, amino, lower alkanoylamino, lower cycloalkanoylamino, benzoylamino or nicotinoylamino, and salts thereof, useful as hypotensive agents, and methods for making the same.

Abstract: Oxacycloalkane-alpha-(thio)carboxylic acid derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are H or optionally-substituted alkyl; n is 0 or 1; X is O or S and Y is NR.sup.4 R.sup.5 or when X is O then Y is also OH or OR.sup.3 in which R.sup.3, R.sup.4 and R.sup.5 is H or an optionally-substituted hydrocarbyl group; and W is an optionally-substituted unsaturated, cycloalkyl, secondary alkyl, aromatic or heterocyclic group, are useful as plant growth regulators, herbicides, intermediates and the like.

Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.

Abstract: 4-[(4-Isoquinolinylmethyl)amino]benzoic acid derivatives useful as selective thromboxane synthetase inhibitors are described herein. The compounds are obtained from the appropriate 4-isoquinolinecarboxylic acid derivative and an aminobenzoic acid derivative. This gives the corresponding Schiff base which is then reduced to give the desired compounds.

Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.

Abstract: New derivatives of the general formula (I) in which:R=H or Cl and either R.sub.1 and R.sub.2 form a tetrahydroquinoxaline, tetrahydroquinoline, tetrahydroisoquinoline, dihydrobenzoxazine, tetrahydro-1H-benzazepine or isoindoline ring, it being possible for all these rings to be substituted by one or more halogen, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano, nitro, alkoxy, alkylthio or alkyl, substituted by carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, hydroxyl, amino, alkylamino or dialkylamino, or R.sub.1 =alkyl and R.sub.2 =alkyl substituted by phenyl which is itself unsubstituted or substituted by one or more halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano or nitro, all the alkyls having 1 to 4 C in a straight or branched chain.These new products are used as antirheumatics.

Abstract: Compounds of the formula ##STR1## wherein X is various imino or amino acids or esters are disclosed. These compounds possess angiotensin converting enzyme inhibition activity and depending upon the definition of X also possess enkephalinase inhibition activity.

Abstract: Compounds of the general formula: ##STR1## wherein: the ring A is saturated and n=0 or 1, orthe ring A is a benzene ring and n=1,R.sub.1 represents a lower alkyl group which can carry an amino group,R.sub.2 represents a hydrogen atom or a lower alkyl group,R.sub.3 represents a straight or branched alkyl group, a mono- or di-cycloalkylalkyl or phenylalkyl group having no more than a total of 9 carbon atoms, or a substituted alkyl group, and also the salts thereof.These compounds are useful as therapeutic drugs.

Abstract: Quaternary ammonium compounds containing an anhydride groups are prepared by halogenating dimethylmaleic anhydride and reacting the halogenated product with a tertiary amine. The products are useful as surfactants, biocides and as cosurfactants in enhanced oil recovery.

Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is a lower alkoxy, n is the integer zero or 1, andA is ##STR2## wherein R.sub.1 is phenyl halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

Abstract: A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.

Abstract: Acyloxyketone substituted imino and amino acids of the formula ##STR1## are disclosed. These compounds are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.

Abstract: 2-Acyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino-[2,1-a]-4-isoquinoleinones having anthelmintic activity of the formula ##STR1## are prepared from 4-acyl-2,6-dioxopierazines by reaction with a phenethyl halide, selective reduction of one of the oxo groups and cyclization, by the novel intermediates of formula ##STR2## in which Y represents O or H, OH.

Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.

Abstract: Serine derivatives are synthesized by the condensation of an alkali metal salt of a glycine derivative and a carbonyl compound in the presence of a phase transfer catalyst.

Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.

Abstract: This invention provides the neuromuscular blocking agents of formula (I): ##STR1## where B and C are each a group of formula (II) and are meta or para to one another: ##STR2## wherein D is CH.sub.2 CH.sub.2 or CH.dbd.CH (preferably trans); Y is alkyl of 1-4 carbon atoms (methyl, ethyl, propyl or butyl); E and F and H or OCH.sub.3 ; X.sup.- is an anion, preferably pharmaceutically acceptable; and the substituted benzyl and substituted propyl groups are in a trans relationship relative to each other in the nitrogen-containing ring.Methods for preparing the compounds, pharmaceutical formulations containing the compounds, and their use are also described.

Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group:R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group;R.sub.4 is benzofuryl, benzothienyl, indolyl, quinolyl, isoquinolyl,2,3-dihydrobenzofuryl, 2,3-dihydrobenzylthienyl or 2,3-dihydroindolyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or acyloxy, trifluoromethyl, halogen or nitro; andA is a bond or C.sub.1-6 alkylene,a process for their preparation, and pharmaceutical compositions containing them.

Abstract: Compounds of the formula: ##STR1## wherein R is H or ##STR2## and n is 0 or 1 are useful as angiotensin I converting enzyme inhibitors.

Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.

Abstract: Bicyclic imino acids, particularly 2-carboxylic acid derivatives of azabicycloalkanes and process for preparing them.These compounds have therapeutical activity and may be used as medicines, particularly as cardiovascular and antihypertensive drugs in human or veterinary medicine.

Abstract: The invention relates to urea compounds which are useful as antihypertensives.

Abstract: A process for preparing imidazoleacetic acid derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl, a heterocyclic group, amino, or amino substituted by alkyl, cycloalkyl, aralkyl, or aryl,R.sub.2 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl, or a heterocyclic group,R.sub.1 and R.sub.2 together form a ring, andR.sub.3 is alkoxy, aralkoxy, amino, mono- or dialkylamino, pyrrolidino, piperidino, morpholino, or arylamino or heteroarylamino, each optionally substituted in the aryl portion,comprises reacting the corresponding amidine or guanidine of Formula II ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and(HY) represents an optional inorganic mineral acid or an organic acid,with the corresponding acetoacetic acid derivative of Formula III ##STR3## wherein R.sub.3 is as defined above,X is a halogen, andR.sub.4 is trialkyl- or triaralkylsilyl, alkyl, or aralkyl.

Abstract: Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.

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: In a process for the preparation of an aromatic chloroformic acid ester by contacting a phenol and phosgene, the improvement wherein the reaction is carried out in a homogeneous liquid phase at a temperature of 60.degree. to 180.degree. C. in the presence of organic phosphorus compound of the formulaR.sup.1 R.sup.2 R.sup.3 PR.sup.4.sub.n X.sub.nin whichR.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, alkyl, alkenyl, aralkyl, aryl or halogen and two of the said radicals together with the phosphorus atom can form a 5-membered or 6-membered phosphorus-containing saturated or unsaturated heterocyclic radical,X represents OH, homopolar-bonded halogen or an inorganic or organic acid anion,R.sup.4 denotes hydrogen or alkyl or, if X denotes halogen, can also denote halogen and n denotes 0 or 1,and in which, furthermore,R.sup.4 and X together can represent oxygen or sulfur.

Abstract: Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.

Abstract: Substituted acyl derivatives of octahydro-1H-indole-2-carboxylic acid and the pharmaceutically acceptable salts thereof are produced by acylating a suitably substituted octahydro-1H-indole with a suitably activated substituted carboxylic acid and when desired hydrolyzing the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.

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: Novel isoquinoline derivatives of the general formula ##STR1## wherein R represents a lower alkyl group, a lower cycloalkyl group, or a group of the formula ##STR2##in which R.sup.2 represents a hydrogen atom, a halogen atom, a methyl group, a trifluoromethyl group, a methoxy group, a methylamino group or a dimethylami no group;R.sup.1 represents a hydrogen atom or a lower alkyl group; andY represents a carboxyl group, a cyano group, a carbamoyl group, a lower alkoxycarbonyl group or a lower alkylaminocarbonyl group;or a salt thereof; a process for the production thereof.The above compound is useful as an anti-inflammatory and analgesic agent.