Patents Examined by G. Thomas Todd
  • Patent number: 3982005
    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
  • Patent number: 3982001
    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
  • Patent number: 3982002
    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.
    Type: Grant
    Filed: February 5, 1975
    Date of Patent: September 21, 1976
    Assignee: Especialidades Latinas Medicamentos Universales S.A.
    Inventors: Fernando Montoro, Antonio Vila-Coro, Jose Calatayud
  • Patent number: 3981877
    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.
    Type: Grant
    Filed: June 5, 1974
    Date of Patent: September 21, 1976
    Assignee: Merck & Co., Inc.
    Inventor: John D. Prugh
  • Patent number: 3981874
    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
  • Patent number: 3981872
    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.
    Type: Grant
    Filed: December 6, 1974
    Date of Patent: September 21, 1976
    Assignee: A. Christiaens Societe Anonyme
    Inventors: Pierre M. Vanhoof, Pierre M. Clarebout
  • Patent number: 3980788
    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.
    Type: Grant
    Filed: September 15, 1975
    Date of Patent: September 14, 1976
    Assignee: SmithKline Corporation
    Inventors: Paul E. Bender, Bernard Loev
  • Patent number: 3980656
    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.
    Type: Grant
    Filed: May 16, 1974
    Date of Patent: September 14, 1976
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rudolf Kunstmann, Ernold Granzer
  • Patent number: 3980786
    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.
    Type: Grant
    Filed: July 15, 1975
    Date of Patent: September 14, 1976
    Assignee: American Hoechst Corporation
    Inventor: Brian J. Duffy
  • Patent number: 3980658
    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
  • Patent number: 3980787
    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.
  • Patent number: 3979395
    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.
    Type: Grant
    Filed: August 6, 1975
    Date of Patent: September 7, 1976
    Assignee: Buskine S.A.
    Inventor: Ida Taccone
  • Patent number: 3979444
    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.
    Type: Grant
    Filed: May 28, 1974
    Date of Patent: September 7, 1976
    Assignee: The Upjohn Company
    Inventor: Daniel Lednicer
  • Patent number: 3979391
    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.
    Type: Grant
    Filed: August 4, 1975
    Date of Patent: September 7, 1976
    Assignee: Sterling Drug Inc.
    Inventors: Ernest John Alexander, Aram Mooradian
  • Patent number: 3979390
    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.
    Type: Grant
    Filed: March 16, 1973
    Date of Patent: September 7, 1976
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kikuo Sasajima, Keiichi Ono, Masaru Nakao, Isamu Maruyama, Masaharu Takayama, Shigenari Katayama, Junki Katsube, Shigeho Inaba, Hisao Yamamoto
  • Patent number: 3978045
    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.
    Type: Grant
    Filed: August 13, 1974
    Date of Patent: August 31, 1976
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Shosuke Okamoto, Ryoji Kikumoto, Yoshikuni Tamao, Shinji Tonomura, Kazuo Ohkubo
  • Patent number: 3978059
    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.
    Type: Grant
    Filed: November 6, 1972
    Date of Patent: August 31, 1976
    Assignee: Sandoz, Inc.
    Inventor: Goetz E. Hardtmann
  • Patent number: 3976653
    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.
    Type: Grant
    Filed: December 16, 1974
    Date of Patent: August 24, 1976
    Assignee: Sterling Drug Inc.
    Inventors: Noel F. Albertson, William F. Michne
  • Patent number: 3974164
    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
    Inventor: Marguerite Severine Lucie LeRoche Navarron
  • Patent number: 3974284
    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.
    Type: Grant
    Filed: December 6, 1974
    Date of Patent: August 10, 1976
    Assignee: Ciba-Geigy Corporation
    Inventor: Herbert Schroter