Patents Examined by G. Thomas Todd
  • Patent number: 3974280
    Abstract: The invention relates to a process for the production of new benzo[b]thiophenes of formula I ##SPC1##whereinPH is optionally substituted o-phenylene, one of the radicals R.sub.1 and R.sub.2 is hydrogen or lower alkyl, and the other of the radicals R.sub.1 and R.sub.2 is optionally C-substituted piperidyl which optionally carries hydroxy on the ring-C-atom bound to the benzo[b]thienyl radical, or which optionally contains a C-C-double bond emanating from this C-atom, and which optionally carries on the N-atom a hydrocarbon radical of aliphatic character, which radical is optionally substituted in a position higher than the 1-position, and of their acid addition salts.These new compounds possess valuable pharmacological properties. In particular they inhibit mono-amine oxidase and further inhibit the absorption of noradrenaline and serotonine in the brain. They are useful as active substances for pharmaceutical preparations for the treatment of mental depressions and psychoses.
    Type: Grant
    Filed: December 3, 1974
    Date of Patent: August 10, 1976
    Assignee: Ciba-Geigy Corporation
    Inventor: Raymond Bernasconi
  • Patent number: 3971792
    Abstract: The new compound 4-amino-3-aminomethylpiperidine is manufactured by hydrogenating 4-amino-3-cyano-1,2,5,6-tetrahydropyridine under pressure and in the presence of ammonia and a hydrogenation catalyst. The 4-amino-3-cyano-1,2,5,6-tetrahydropyridine used as the starting substance can be obtained by cyclization of bis-cyanoethylenated ammonia. The new compound 4-amino-3-aminomethylpiperidine represents a valuable curing agent for epoxide resins, and advantageously 0.5 to 1.3 equivalents of nitrogen-bonded active hydrogen atoms of the 4-amino-3-aminomethylpiperidine are used per 1 equivalent of epoxide groups of the polyepoxide compound.
    Type: Grant
    Filed: June 10, 1974
    Date of Patent: July 27, 1976
    Assignee: Ciba-Geigy AG
    Inventors: Helmut Zondler, Wolfgang Pfleiderer
  • Patent number: 3968114
    Abstract: N-Alkylated-8-aminated-2,6-methano-3-benzazocines, useful as strong analgesics, are prepared by one route comprising reduction of 8-nitro intermediates or by another route comprising Birch type reduction of 8-methoxy intermediates followed by dehydration-rearrangement of the oximes of the resulting 8-oxo intermediates.
    Type: Grant
    Filed: September 20, 1974
    Date of Patent: July 6, 1976
    Assignee: Sterling Drug Inc.
    Inventor: Noel F. Albertson
  • Patent number: 3966747
    Abstract: N-substituted-9-hydroxy-6,7-benzomorphans have been found to possess potent narcotic agonist and/or antagonist activity. In particular, the compound 2'-hydroxy-2-cyclobutylmethyl-5-allyl-9.beta.-hydroxy-9.alpha.-methyl-6,7- benzomorphan has been found to possess potent narcotic agonist and antagonist activity. These compounds are prepared by total synthesis and are not derived from opium alkaloids.
    Type: Grant
    Filed: July 9, 1974
    Date of Patent: June 29, 1976
    Assignee: Bristol-Myers Company
    Inventors: Ivo Monkovic, Michel Saucier, Yvon Lambert, Thomas Alfred Montzka
  • Patent number: 3965106
    Abstract: A 3-phenoxypropylamine derivative of the formula: ##SPC1##Wherein Y is ##SPC2##(wherein R.sub.1 is a halogen atom or a trifluoromethyl group) or ##SPC3##(wherein R.sub.2 is a lower alkyl group) and its pharmaceutically acceptable salts which are useful as central nervous system depressing agents.
    Type: Grant
    Filed: December 12, 1973
    Date of Patent: June 22, 1976
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Isamu Maruyama, Masaru Nakao, Kikuo Sasajima, Shigeho Inaba, Hisao Yamamoto
  • Patent number: 3965113
    Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SR.sup.5 or --OR.sup.5 ; and R.sup.5 is aryl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
    Type: Grant
    Filed: November 21, 1973
    Date of Patent: June 22, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Colin C. Beard, John A. Edwards, John H. Fried
  • Patent number: 3965103
    Abstract: Compounds of the formula v,2/12Wherein R.sub.1 is H, lower-alkyl, hydroxyalkyl, phenyl, aralkyl, or --(CH.sub.2) .sub.n --X wherein n is 0-4 and X is --COO-lower-alkyl, C.tbd.N or --COOH and R.sub.2 is H, lower-alkyl or aralkyl, produced by condensing a diamine of the formula ##SPC1##With a nitro compound of the formula R.sub.1 --CH.sub.2 --NO.sub.2 in the presence of formalin or paraformaldehyde, or with the R.sub.1 -- C(CH.sub.2 OH).sub.2 NO.sub.2 reaction product of the above nitro compound and formalin or paraformaldehyde, or with formalin or paraformaldehyde followed by reaction with the above nitro compound, and their acid addition salts, possess antimicrobial activity against both gram-positive and gram-negative bacteria and also against dermatophytes, yeasts and other fungi.
    Type: Grant
    Filed: September 20, 1974
    Date of Patent: June 22, 1976
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Biere, Hermann Ulbrich, Hans-Joachim Kessler, Ulrich Redmann
  • Patent number: 3963730
    Abstract: A process for preparing triacetonamine, characterized in that acetonine is reacted with acetone in the presence of at least 12.5 mol % based on acetonine of an acid catalyst under anhydrous conditions. Triacetonamine is used as an intermediate for light stabilizer for synthetic polymers.
    Type: Grant
    Filed: June 21, 1974
    Date of Patent: June 15, 1976
    Assignee: Sankyo Company Limited
    Inventors: Keisuke Murayama, Syoji Morimura, Takao Yoshioka, Tomoyuki Kurumada
  • Patent number: 3963727
    Abstract: A compound having the formula: ##SPC1##Wherein R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom; or the acid-addition salt thereof having a distinctive neuroleptic activity.
    Type: Grant
    Filed: June 6, 1975
    Date of Patent: June 15, 1976
    Assignee: Daiichi Seiyaku Co., Ltd.
    Inventors: Katsujiro Ueno, Makoto Sato, Masahiro Arimoto, Hiroshi Kojima, Terukiyo Yamasaki, Takeo Sakurai
  • Patent number: 3962258
    Abstract: The invention provides indolo[2,3-a]quinolizine derivatives which are active as hypotensive and anti-histamine agents. The invention also provides a pharmaceutical composition comprising an indolo[2,3-a]quinolizine derivative together with a pharmaceutical carrier.
    Type: Grant
    Filed: May 17, 1974
    Date of Patent: June 8, 1976
    Assignee: John Wyeth & Brother Limited
    Inventors: John Leheup Archibald, John Lambert Jackson, Brian John Bushell
  • Patent number: 3962269
    Abstract: Certain m-dioxane-5-methylamines are useful analgesic agents and intermediate 2-substituted-1,3-propanediols are useful in the preparation of such compounds.
    Type: Grant
    Filed: May 8, 1975
    Date of Patent: June 8, 1976
    Assignee: Eli Lilly and Company
    Inventor: Richard N. Booher
  • Patent number: 3962259
    Abstract: Novel substituted 1,3-dihydrospiro[isobenzofuran]s and methods of preparing the same are described. These compounds are useful as tranquilizers, analgetic agents and intermediates therefor.
    Type: Grant
    Filed: December 12, 1973
    Date of Patent: June 8, 1976
    Assignee: American Hoechst Corporation
    Inventors: Victor J. Bauer, Raymond W. Kosley, Jr.
  • Patent number: 3962263
    Abstract: N-(2,2-Difluoroalkanoyl)-2,3-pyridinediamine compounds useful as herbicides.
    Type: Grant
    Filed: December 9, 1971
    Date of Patent: June 8, 1976
    Assignee: Eli Lilly and Company
    Inventor: George O. P. Doherty
  • Patent number: 3962256
    Abstract: Compounds having the formula ##EQU1## WHEREIN Ar is phenyl optionally substituted by one or more halogens, alkyl having 1 to 4 carbons or alkoxy containing up to 4 carbons, and R.sub.1 and R.sub.2 each is alkyl having one to 4 carbons or ##EQU2## is piperidino, pyrrolidino, morpholino and hexamethyleneimino. The compounds are prepared by reacting the corresponding 2-chloromethyl benzimidazole with ##EQU3## The compounds possess analgesic, antihypertensive, gastric antisecretory, antiinflammatory, antibronchoconstrictive, anticholinergic, spasmolytic, sedative, antiulcerous, vasodilatatory, central nervous system stimulant, antiarythmic, diuretic and antihistaminic properties.
    Type: Grant
    Filed: June 20, 1974
    Date of Patent: June 8, 1976
    Assignee: Delalande S.A.
    Inventors: Claude P. Fauran, Jeannine A. Eberle, Guy M. Raynaud, Nicole A. M. Dorme
  • Patent number: 3962449
    Abstract: Cardioactive bispidones and bispidines of the formula ##SPC1##Wherein R is =C=O or --CH.sub.2 -- and R' and R" are alkyl mono- or di-substituted by phenyl, made by a Mannich reaction from formaldehyde, piperidones of the formula ##SPC2##And amines of the formula R"--NH.sub.2.
    Type: Grant
    Filed: June 10, 1975
    Date of Patent: June 8, 1976
    Assignee: Knoll A.G. Chemische Fabriken
    Inventors: Fritz Binnig, Manfred Raschack, Hans-Joerg Treiber
  • Patent number: 3960857
    Abstract: Ureas such as 1,3-bis(morpholinothio)-imidazolidinone are used to affect the vulcanization characteristics of sulfur vulcanizable polymers by increasing the state of vulcanization and improving scorch resistance and/or increasing the rate of vulcanization.
    Type: Grant
    Filed: June 26, 1972
    Date of Patent: June 1, 1976
    Assignee: The Goodyear Tire & Rubber Company
    Inventor: John P. Lawrence
  • Patent number: 3960874
    Abstract: .alpha.-(Cyclic tert. aminophenoxy)-alkanoic acids, e.g., those of the formula ##EQU1## AND FUNCTIONAL DERIVATIVES THEREOF ARE ANTI-INFLAMMATORY AND HYPOLIPIDEMIC AGENTS.
    Type: Grant
    Filed: June 20, 1974
    Date of Patent: June 1, 1976
    Assignee: Ciba-Geigy Corporation
    Inventor: Richard William James Carney
  • Patent number: 3960875
    Abstract: 2,2,6,6-Tetramethyl-4-oxopiperidine is prepared from 2,2,4,4,6-pentamethyl-2,3,4,5-tetramethylpyrimidine (acetonine) by heating in the presence of acetone, diacetone alcohol or water. These regents may be used in excess or an organic solvent is added. The preferred modification is the heating of acetonine hydrate in an excess of acetone or in an acetone-methanol mixture to about 40.degree. to 65.degree.C for several hours. The use of diacetone alcohol permits higher reaction temperatures leading to shorter reaction times.
    Type: Grant
    Filed: June 21, 1974
    Date of Patent: June 1, 1976
    Assignee: Ciba-Geigy Corporation
    Inventors: Ivan Orban, Hanns Lind, Heimo Brunetti, Jean Rody
  • Patent number: 3960870
    Abstract: The compounds are alkanesulfonic acid salts of decinine. These salts are water soluble. Decinine and the salts thereof have glucocorticoid-like water diuretic and anti-inflammatory activity.
    Type: Grant
    Filed: August 2, 1974
    Date of Patent: June 1, 1976
    Assignee: SmithKline Corporation
    Inventors: Dale W. Blackburn, Henry Cecil Caldwell
  • Patent number: 3960886
    Abstract: N-Arylanilines, further substituted on nitrogen by aroyl, aralkanoyl or aralkyl groups, and wherein one of the aryl groups has a 3- or 4-(aminoalkoxy)substituent, having hypocholesteremic activity, are prepared by a series of O-alkylation, N-acylation or -alkylation, and reduction reactions starting from the appropriate hydroxydiarylamines or benzyl ethers thereof.
    Type: Grant
    Filed: November 20, 1970
    Date of Patent: June 1, 1976
    Assignee: Sterling Drug Inc.
    Inventor: John W. Schulenberg