Abstract: Compounds of the formula ##SPC1##Wherein R.sub.1 is methyl or phenyl, andR.sub.2 is hydrogen, methyl or acetyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as analgesics.
Type:
Grant
Filed:
July 30, 1975
Date of Patent:
September 21, 1976
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Herbert Merz, Adolf Langbein, Gerhard Walther, Klaus Stockhaus
Abstract: This invention provides new compounds of formula I, ##SPC1##wherein R.sub.1 and R.sub.2 are the same or different and are in each case hydrogen, halogen, lower alkyl, hydroxy or lower alkoxy R.sub.3 is hydrogen or lower acyl and A stands for groups of formula ##EQU1## wherein R.sub.5 and R.sub.6 are independently, hydrogen or methyl and n is 0, 1 or 2, useful as analgesic agents.
Type:
Grant
Filed:
September 19, 1974
Date of Patent:
September 21, 1976
Assignee:
Sandoz, Inc.
Inventors:
Wilhelm Heffe, Fritz Hunziker, Klaus Thoma
Abstract: The new compound vincamine 2-ketoglutarate of the formula: ##SPC1##Is disclosed and is prepared by mixing 2-ketoglutaric acid and vincamine or a salt thereof in a solvent and recovering the resulting vincamine 2-ketoglutarate which has interesting properties as a vasodilator and brain oxygenator. The vincamine may be prepared by allowing a mixture of a solution of 16-epivincamine and a quaternary ammonium hydroxide to stand whereafter the vincamine is recovered.
Abstract: The new 1-alkyl-4-(1, 2, or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-one by reaction with a Grignard reagent prepared from a 1-alkyl-4-halo piperidine to form an intermediate carbinol, or a 1, 2 or 3-carboxy-5-(1-alkyl-4-piperidyl)-5H-dibenzo[a,d]cyclohepten-5-ol which is then dehydrated to produce the desired 1-alkyl-4-(1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine, or alternatively by hydrolysis of a 1-alkyl-4-(1, 2 or 3-cyano-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compound to form the corresponding 1-alkyl-4-(1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compound.
Abstract: Compound of the formula ##SPC1##WhereinR.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms,R.sub.3 is hydrogen or methyl,R.sub.4 is ##SPC2##R.sub.5 is hydrogen, methyl or acetyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics.
Type:
Grant
Filed:
October 15, 1974
Date of Patent:
September 21, 1976
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Herbert Merz, Adolf Langbein, Gerhard Walther, Klaus Stockhaus
Abstract: This invention relates to new derivatives of 2-amino-(1,2,3,4-tetrahydronaphthalene), namely 2-[N-phenyl-N-(R.sub.1,R.sub.2 -aminoalkyl or alkanoyl)]-amino-(1,2,3,4-tetrahydronaphthalenes), in which R.sub.1 and R.sub.2 represent a lower alkyl group or form together with the attached nitrogen atom a nitrogenous heterocyclic ring, with the proviso that R.sub.1 may also represent hydrogen, as well as to the acid addition salts of these new derivatives.These new derivatives are active for the treatment of heart arrhythmy.
Abstract: Pharmaceutical compositions and methods of inhibiting gastric acid secretion by administering 1-(9-xanthenyl) amino-substituted-piperidines and pyrrolidines and new 1-(9-xanthenyl) amino-piperidine compounds.
Abstract: Partially hydrogenated 1H-indeno[1,2-b]-pyridine derivatives of the general formula I ##SPC1##in whichR.sup.1 and R.sup.2, which may be identical or different, represent hydrogen, halogen or alkoxy of 1 to 4 carbon atoms,R.sup.3 represents pyridyl, phenyl, or phenyl mono- or di-substituted by halogen, nitro, amino, acylamino, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, or amino substituted by 1 or 2 aliphatic or aromatic hydrocarbon groups having 2 to 18 carbon atoms or substituted amino wherein the amino-nitrogen is included in a heterocycle,A represents a single or double bond, andX represents oxygen or sulfur,And their physiologically tolerated salts, process for preparing them and pharmaceutical preparations containing them.
Abstract: Novel 1,3-dihydro-3-phenyl-1'-(2-propynyl)spiro[isobenzofuran]s and methods of preparing the same are described. These compounds are useful as antidepressants.
Abstract: Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, chlorine, methyl, methoxy or trifluoromethyl,R.sub.2 is hydrogen or methyl,R.sub.3 is methyl or phenyl, andR.sub.4 and R.sub.5 together form a double bond or, in caseR.sub.1 is chloro, methyl or trifluoromethyl, are also hydrogen atoms,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as sedatives and tranquilizers.
Type:
Grant
Filed:
May 6, 1974
Date of Patent:
September 14, 1976
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Genus Possanza, Kurt Freter, Sven Luttke
Abstract: Novel 3-phenylspiro[isobenzofuran-1,4'-piperidine]sulfenamides and derivatives and a method of preparing the same are described. These compounds are useful as diuretic and antihypertensive agents.
Type:
Grant
Filed:
August 25, 1975
Date of Patent:
September 14, 1976
Assignee:
American Hoechst Corporation
Inventors:
Solomon S. Klioze, William J. Novick, Jr.
Abstract: The invention relates to the preparation of vincamine and similar indole alkaloids, capable of being easily converted to vincamine, by oxydating a starting alkaloid selected between tabersonine and vincadifformine with oxygen, the reaction mixture being added with an essential amount of an inorganic or organic salt of a metal selected among Cu, Fe and Co.
Abstract: The invention relates to novel 4-hydroxymethyl(acyloxymethyl and methyl)-4-arylcyclohexylamines embraced by the formula ##SPC1##Wherein Ar is an aromatic ring selected from the group consisting of phenyl and naphthyl, each of which has from zero through three substituents independently selected from the group consisting of fluorine, chlorine, bromine, lower alkyl of one through three carbon atoms, lower alkoxy of one through three carbon atoms, and lower alkylthio of one through three carbon atoms; Z is selected from the group consisting of hydrogen, hydroxy and lower acyloxy of one through four carbon atoms; .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof, with the proviso that when the stereoconfiguration of the linkage connecting the cyclohexane ring and CH.sub.2 Z is cis to the amino group, the linkage connecting the cyclohexane and Ar rings is trans, and vice versa; R.sup.
Abstract: Novel 4-R.sub.1 R.sub.2 NCH.sub.2 -9-benzyl-6-R.sub.3 -7-R.sub.4 -1,2,3,4-tetrahydrocarbazoles having antibacterial activity are disclosed. The compounds are prepared by the chemical reduction of the corresponding 4-R.sub.1 R.sub.2 NCO-9-benzyl-6-R.sub.3 -7-R.sub.4 -1,2,3,4-tetrahydrocarbazoles.
Abstract: A process for producing butyrophenone derivatives of the formula: ##EQU1## which comprises reacting a compound of the formula: ##SPC1##With an amine of the formulaH-W(wherein Ar represents a group of either one of the formulas: ##SPC2##Z is a secondary amino group and W is the residue of an amine excluding a hydrogen atom therefrom). The said butyrophenone derivatives and their salts exhibit a variety of beneficial pharmacological activities including a central and autonomic nervous system depressing activity.
Abstract: N.sup.2 -dansyl-L-arginine esters and amides having the formula ##SPC1##Or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the group consisting of(1) alkoxy, alkenyloxy, alkynyloxy, and cycloalkoxy, respectively, containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, tetrahydrofurfuryloxy, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms, halogen or nitro; ##EQU1## wherein R.sub.1 and R.sub.
Abstract: The compounds are biologically active tricyclic quinazolinones of the class of imidazo[2,1-b]quinazolin-5-ones, pyrimido[2,1-b]quinazolin-6-ones and diazepino[2,1-b]quinazolin-7-ones substituted by a thienyl or furyl group, e.g., 10-(2-thienylmethyl)-2,3-dihydro-imidazo[2,1-b] quinazolin-5(10)-one, and useful, for example, as broncho-dilator agents. Processes for preparation of said compounds include the reaction of a N-carboxy anthranilic anhydride (an isatoic anhydride) with a cyclic pseudothiourea such as 2-organomercapto-4,5-dihydroimidazole or 2-organomercapto-3,4,5,6-tetrahydropyrimidine.
Abstract: 1,2,3,4,4a,5,10,10a-octahydro-5-(Y.sup.3)-5-(Y.sup.4)-benzo[g]quinolines and 1,2,3,4,4a,9b-hexahydro-5-(Y.sup.3)-5-(Y.sup.4)-5H-indeno[1,2,b]pyridi nes wherein Y.sup.3 and Y.sup.4 are hydrogen, alkyl or phenyl, which are useful as antagonists of strong analgesics, are obtained by cyclizing derivatives of 2-(phenyl or benzyl)-.alpha.-(Y.sup.3)-.alpha.-(Y.sup.4)-3-piperidinemethanols. The latter are obtained from corresponding 3-piperidinecarboxylic acids.
Abstract: The invention relates to compounds having the formula: ##SPC1##In which R is a group --NHR.sub.1, --NH--COOR.sub.2, --NH--CO--R.sub.3, -CONH--Ar, --NH--CS--NH--Ar or --N=CH--Ar,R.sub.1 being hydrogen, R.sub.2 being lower alkyl or phenyl, R.sub.3 being optionally substituted phenyl and Ar being optionally substituted phenyl, and their pharmaceutically acceptable acid addition salts.Said compounds possess an anti-hypertensive activity.
Type:
Grant
Filed:
July 22, 1974
Date of Patent:
August 10, 1976
Assignee:
Serdex-Societe d'Etudes, de Recherches, de Diffusion et d'Exploitation
Abstract: Compounds of the class of 1,1a,6,10b-tetrahydro-1,6-methano-dibenzo[a,e]cyclopropa[c]cycloheptene derivatives and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an antidepressive and stimulating action.