Abstract: This invention relates to indole-7-carboxamide derivatives of the formula ##STR1## where R.sub.1 through R.sub.6 are independently H, loweralkyl, aryl, and aralkyl; and in addition R.sub.3 and R.sub.5 can be joined together to form a piperazine ring of the formula ##STR2## where R.sub.7 is H, loweralkyl, aryl, arylloweralkyl, pyrimidyl; and R.sub.4 and R.sub.5 can be joined together to form a pyrrolidine ring of the formula ##STR3## where R.sub.8 is H, loweralkyl, aryl, arylloweralkyl; X is H, loweralkyl, halogen, NO.sub.2, CF.sub.3, NH.sub.2, and OR.sub.9 ; where R.sub.9 is loweralkyl, arylloweralkyl and n is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and the optical isomers thereof where such isomers exist.

Abstract: 2-R.sub.2 -R.sub.4 -substitutea-3-R.sub.3 -CO-1-[(C-attached-N-heteryl)(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is carboxy or pharmaceutically acceptable salts and esters thereof;R.sup.2 is hydrogen, lower alkyl or halogen;R.sup.3 is phenyl, naphthyl, phenyl or naphthyl each substituted by from one to three C.sub.1-6 alkyl groups, mono-, di- or triphenyl (C.sub.1-6)alkyl; or substituted mono-, di- or triphenyl (C.sub.1-6) alkyl;A is lower alkylene which may be substituted by oxo or lower alkenylene,Q is carbonyl or lower alkylene,X is ##STR2## in which R.sup.4 is hydrogen or C.sub.1-6 alkyl, andR.sup.5 is hydrogen, C.sub.1-6 alkyl or Y--Z--R.sup.3,Y is a bond or lower alkylene,Z is lower alkylene ##STR3## in which R.sup.6 is hydrogen, (C.sub.1 -C.sub.6) alkyl, mono-, di- or triphenyl(C.sub.1-10) alkyl, C.sub.1-6 alkyl or lower alkoxycarbonyl substituted mono-, di- or triphenyl(C.sub.1-6)alkyl or pharmaceutically acceptable carboxylic acid acyl, and pharmaceutically acceptable salts thereof. The compound is useful as a testosterone 5.alpha.-reductase inhibitor.

Abstract: The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic acids or ester amides, or 2-acylsulfonamides thereof; and including also as 3-substituents unsaturated acids and their further ester and amide derivatives. These 2-carboxyindoles are useful as pharmaceutical agents, therefore, the present invention is also pharmaceutical compositions and pharmaceutical methods of treatment therefor. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.

Abstract: Indole derivatives of the following formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.2 is hydrogen, lower alkyl or halogen,R.sup.3 and R.sup.4 are each hydrogen or lower alkyl,R.sup.5 is ar(lower)alkyl which may have suitable substituent(s), andA is carbonyl, sulfonyl or lower alkylene, or a pharmaceutically acceptable salt thereof, which are useful as a testosterone 5.alpha.-reductase inhibitor.

Abstract: Novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds, intermediates and processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.

Abstract: Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.

Abstract: The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: ##STR1## in which: Het represents one of the groups: ##STR2## in which T,T' and T"represent particularly a group: ##STR3## R and R.sub.a, identical or different, represent X represent --O-- or --S--Y represents a radical ##STR4## These compounds are useful as medecines particularly for the treatment of pathological syndroms of the cardio-vascular system.

Abstract: Non-peptidyl compounds characterized generally as indolyl/indolylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein X is selected from ##STR3## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.

Abstract: Indole derivatives of the formula ##STR1## and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia, acnes and prostatism.

Abstract: A novel compound--ethyl 6-bromo-5-hydroxy-4-dimethylaminomethyl-1-methyl-2-phenylthiomethylindole- 3- carboxylate hydrochloride monohydrate having the following formula: ##STR1## A process for preparing the compound according to the invention, characterized in that it comprises treating ethyl 5-acetoxy-1,2-dimethylindole-3-carboxylate with a brominating agent in an inert organic solvent under reflux, reacting the resultant ethyl 5-acetoxy-6-bromo-2-bromomethyl-1-methylindole-3-carboxylate with thiophenol in the presence of an alkali metal hydroxide or its alcoholate in an organic solvent, reacting the resultant ethyl 6-bromo-5-hydroxy-1-methyl-2-phenylthiomethylindole-3-carboxylate with an aminomethylating agent in an organic solvent at a temperature of from 65.degree. C. to a temperature of refluxing the reaction mixture. The end product is then isolated from the resultant base--ethyl 6-bromo-5-hydroxy-4-dimethylaminomethyl-1-methyl-2-phenylthiomethylindole- 3- carboxylate.

Abstract: Compounds of general formula: ##STR1## in which A and R are defined in the description.

Abstract: The invention concerns novel, pharmaceutically useful, benzheterocyclyl sulphones of the formula I: ##STR1## in which ring A may bear optional halogeno, (1-4C)alkyl or fluoro(1-4C)alkyl substituents; X is oxygen, or a group of the formula --S(O).sub.n -- or --NR.sup.1 -- in which n is zero, 1 or 2 and R.sup.1 is hydrogen, (1-4C)alkyl, (1-6C)alkanoyl, benzoyl or phenyl(1-4C)alkyl, the last two optionally substituted; Y is various linking groups defined hereinafter, such as ethylene or trimethylene; and in which the group --SO.sub.2 CH.sub.2 NO.sub.2 is located at position a, b or c in ring A; together with the non-toxic thereof. Other aspects of the invention include the production of the novel compounds by analogy processes and pharmaceutical compositions of the novel compounds for use in the treatment of diabetic complications.

Abstract: The present invention relates to 2-substituted-1-hydroxyindoles of the following formula: ##STR1## wherein, R.sup.1 is an electron withdrawing group,R.sup.2 is an alkenyl having 2-10 carbon atoms, and N-substituted .alpha.-iminobenzyl group wherein the substituents are selected from the group consisting of phenyl, anilino and dimethylamino, an unsubstituted aromatic group, and an aromatic group having meta or para substituents which are nitro, trifluoromethyl, fluoro, formyl, hydroxyiminomethyl and carbamoyl,R.sup.3 is a halogen atom, andn is 0, 1, or 2,provided that when R.sup.2 is either phenyl or nitro substituted phenyl and n is 0, then R.sup.1 is not cyano.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl,R.sup.4 is imidazolyl, which may have alkyl or imino-protective group as substituents, or pyridyl,A is lower alkylene, andis single bond or double bond, and pharmaceutically acceptable salts thereof, having 5-HT antagonism.

Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.

Abstract: Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is selected from methyl and ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is selected from isobutyl and ethyl; wherein X is selected from ##STR3## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; and wherein n is a number selected from zero through four, inclusive; or a pharmaceutically-acceptable salt thereof.

Abstract: The present invention relates to novel compounds, which are derivatives of ureas, thioureas, carbamates, sulfonylureas, sulfonamides, amides, and thioamides of 2-carboxyindoles as illustrated by the formula ##STR1## The invention also relates to methods for the preparation of the novel compounds, as well as to pharmaceutical compositions or methods of use for the novel compounds. More specifically, the compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders as well as in the treatment of schizophrenia or epilepsy; and as analgesics and anxiolytics.

Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.

Abstract: Disclosed are compounds of formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, benzyl or an indolyl carbonyl group, R.sub.2 is a saturated or unsaturated 5- or 8-membered heterocyclic group containing as a hetero atom one or more nitrogen atoms, the heterocyclic group is optionally substituted at an N or C atom by a C.sub.1 -C.sub.6 alkyl or aralkyl group, n is an integer of 1 to 5 and one or more hydrogen atoms, in an alkylene chain --(CH.sub.2).sub.n -- are optionally substituted by a C.sub.1 -C.sub.6 alkyl, phenyl and/or hydroxyl group, physiologically acceptable salts and quaternary ammonium salts thereof. The compounds are selective antagonists of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, neurotic diseases, gastric stasis symptoms, gastrointestinal disorders, nausea and vomiting.

Abstract: 1-Hydroxyindoles of the following formula are useful in controlling fungi: ##STR1## wherein: R.sup.1 is hydrogen or an electron withdrawing group;R.sup.2 is selected from the group consisting of alkenyl having 2-10 carbon atoms, N-substituted-.alpha.-iminobenzyl, an unsubstituted or substituted aromatic group and acyl of 2-16 carbon atoms,R.sup.3 is selected from the group consisting of halogen atoms, andn is 0 to 4.

Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.

Abstract: The present invention is directed a new group of indole derivatives that are NMDA antagonists.

Abstract: Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.

Abstract: Indole-2-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, inflammation, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dismenorrhea and as cytoprotective agents.

Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: A process for the preparation of aromatic carboxylic acids or their salts comprises heating carboxyl-free aromatic compounds and aromatic carboxylic acid salts whose basic structures differ from those of the aromatic compounds, or heating polycyclic aromatic compounds with three or more rings and monocyclic or bicyclic aromatic carboxylic acid salts, under carbon dioxide pressure in the presence of one or more metal compounds selected from group (a) of compounds of zinc, cadmium, and thallium and one or more compounds selected from group (b) of compounds of cesium, Group II metals, And Group IIIa metals to effect the intermolecular transfer of the carboxyl groups.

Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.

Abstract: All possible isomeric forms and mixtures thereof of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of indolyl, pyridyl, piperidinyl, quinolyl, thiazolyl and aryl of 6 to 14 carbon atoms and aralkyl of 7 to 18 carbon atoms with the latter two being unsubstituted or substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2, R.sub.2 is selected from the group consisting of ##STR2## Ar' are selected from the group consisting of pyridyl, indolyl, thiazolyl and aryl of 6 to 14 carbon atoms with the latter and the phenyl ring of b) being substituted or substrituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2 and R.sub.3 is hydrogen or R.sub.2 and R.sub.

Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy;R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.

Abstract: .beta.-Alkylmelatonins are useful as ovulation inhibitors.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is selected from C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-4 alkyl, COR.sub.8 where R.sub.8 is hydroxy, C.sub.1-6 alkoxy or NR.sub.9 R.sub.10 where R.sub.9 and R.sub.10 are independently hydrogen or C.sub.1-4 alkyl and CH.sub.2 OR.sub.11 and R.sub.11 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkanoyl;R.sub.5 is hydrogen, C.sub.1-6 alkyl or phenyl C.sub.1-4 alkyl;R.sub.6 is phenyl C.sub.1-7 alkyl in which the phenyl moiety is optionally substituted by one or two of halogen, ortho-nitro, meta- or para-methoxy, methyl or NR.sub.12 R.sub.13 wherein R.sub.12 and R.sub.13 are independently hydrogen or C.sub.1-6 alkyl or R.sub.12 and R.sub.13 together are C.sub.2-6 polymethylene or the phenyl moiety is 3,4-disubstituted by methylenedioxy or ethylenedioxy; andR.sub.7 is hydrogen or C.sub.

Abstract: A method of preparing indole carboxylic acid derivatives from aniline derivatives is described which can be carried out in a single reaction vessel without any isolation of intermediate products. The method involes reacting an aniline derivative with a soluble nitrite in an acid medium, reducing the resulting nitrosamine by treating the acidic nitrosamine containing reaction solution with zinc in the presence of sufficient acid, optionally with addition of additional acid and/or a solvent such as a lower alcohol, reacting the resulting hydrazine derivative containing solution with a lower alkyl ester of pyruvic acid to obtain a corresponding hydrazone which cyclizes to yield an indole carboxylic acid ester, and if desired, hydrolyzing the ester to obtain the corresponding carboxylic acid.

Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.

Abstract: Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.

Abstract: New Sulphonamides of the formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or halogen atoms, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl or trifluoromethyl radicals or hydroxyl or cyano groups, R.sub.3 and R.sub.8, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 -alkyl, benzyl or C.sub.1 -C.sub.6 -alkanoyl radicals, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.6 -alkyl radicals, R.sub.6 and R.sub.7 are both hydrogen atoms or together form a valency bind, X is an oxygen or sulphur atom or an .dbd.NOH or .dbd.NR.sub.8 group and n is a whole number of from 1 to 4; and the physiologically acceptable salts thereof with inorganic and organic bases.

Abstract: Simple amides and derivatives thereof useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.

Abstract: Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring.The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.

Abstract: New original derivatives are described of 5-pentylamino -5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

Abstract: Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.

Abstract: A process for the asymmetric preparation of a compound of the formula ##STR1## wherein the hydrogen at 3a and 7a are of cis or trans configuration and their non-toxic, pharmaceutically acceptable acid addition salts comprising submitting a compound of the formula ##STR2## to a Hoffman reaction and reacting the resulting product with formaldehyde in the presence of cyanide ions and acid halide of benzoic acid or an aliphatic carboxylic acid of 1 to 5 carbon atoms to obtain a compound of the formula ##STR3## wherein R is acyl of benzoic acid or aliphatic carboxylic acid of 1 to 5 carbon atoms, cyclizing the latter to form a compound of the formula ##STR4## selectively hydrolyzing the latter with a dilute aqueous mineral acid to obtain a compound of the formula ##STR5## subjecting the latter to hydrolysis with a concentrated aqueous mineral acid to form the acid addition salt of a compound of claim 1 and optionally forming the free base.

Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.

Abstract: The invention relates to a process for preparing compounds of the formula I ##STR1## in which R stands for hydrogen, alkyl or aralkyl and R.sup.1 to R.sup.5 are identical or different radicals, (substituted) alkyl, cycloalkyl or (substituted) aryl or in which the pairs of radicals R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5 together with the carbon atom(s) supporting them form a mono- or bicyclic ring system and the other radicals are hydrogen, by treating a compound of the formula II ##STR2## in which R and R.sup.1 and R.sup.5 have the abovementioned meaning and R.sup.6 and R.sup.7 denote alkyl or aralkyl or together with the nitrogen atom supporting them form a heterocycle which can additionally contain an oxygen atom, with a reducing agent.

Abstract: Indole derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, or benzylR.sub.2 is hydrogen, alkyl of up to 4 carbon atoms, free or esterified hydroxyalkyl of up to 4 carbon atoms, or free, amidated or esterified carboxy or carboxyalkyl,R.sub.3 is hydrogen or alkyl containing 1-6 carbon atoms,R.sub.4 is hydrogen or alkyl containing 1-6 carbon atoms andR.sub.5 is hydrogen, or alkyl, alkenyl, or cycloalkyl, all of which per se contain up to 6 carbon atoms, and all of which are optionally substituted by a free or esterified carboxy group or by an optionally substituted phenyl group; or a polymethylene group of up to 8 carbon atoms linking the first indole residue to a second indole residue of Formula Ia ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined above,and the physiologically acceptable salts thereof with acids and, optionally, their alkali metal and alkaline earth metal salts,possess valuable pharmacological properties, such as stimulating .beta.

Abstract: New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutasnoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

Abstract: A resolving agent for N-acetylindoline-2-carboxylic acid, comprising an optically active .alpha.-amino-.epsilon.-caprolactam gives an optically active N-acetylindoline-2-carboxylic acid in both high yield and high optical purity.

Abstract: The present invention provides a process for the preparation of 4-hydroxyindole derivatives of the general formula: ##STR1## in which R.sub.1 is a hydrogen atom or an alkyl radical containing up to 6 carbon atoms and R.sub.2 is a hydrogen atom or an alkyl radical containing up to 6 carbon atoms, wherein a compound of the general formula: ##STR2## in which R.sub.2 has the same meaning as above, is reacted with a compound of the general formula:R.sub.3 --CH.sub.2 --CO--COOR.sub.1 (III)in which R.sub.1 has the same meaning as above and R.sub.3 is a reactive residue, to give a 2-(2-imino-6-oxocyclohexylidene)-propionic acid derivative of the general formula: ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, which is then cyclized in known manner to give a compound of the general formula: in which R.sub.1 and R.sub.2 have the same meanings as above, which is subsequently dehydrated.

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.