Patents Examined by Jose Tovar
  • Patent number: 4211709
    Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, and R.sub.2 and R.sub.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: July 8, 1980
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giorgio Tarzia, Gianbattista Panzone
  • Patent number: 4211708
    Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, R.sub.2 and R.sub.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: July 8, 1980
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giorgio Tarzia, Gianbattista Panzone
  • Patent number: 4211870
    Abstract: Preparation of substituted 2-aminopyrazines by reaction of an .alpha.-chloro or .alpha.-bromo oxime with an aminoacetonitrile in the presence of an acid-uptake agent, followed by separation of the intermediate novel hydroxyimino-substituted aminoacetonitrile, and cyclization thereof with acid.
    Type: Grant
    Filed: April 6, 1979
    Date of Patent: July 8, 1980
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas L. Emmick, Richard C. Hoying
  • Patent number: 4209624
    Abstract: A process is disclosed for preparing substituted bis-(amidinoureas) by reacting a 1-substituted-4-alkyl-4-isothiobiuret with a compound containing two aliphatic amino groups.
    Type: Grant
    Filed: July 19, 1977
    Date of Patent: June 24, 1980
    Assignee: Cooper Laboratories, Inc.
    Inventor: Ronald A. Wohl
  • Patent number: 4209628
    Abstract: Process for preparing 2-oxazolidone and its derivatives by reacting react carbon dioxide with aziridine compound, preferably, in the presence of Lewis acid as a catalyst.
    Type: Grant
    Filed: April 26, 1978
    Date of Patent: June 24, 1980
    Assignee: Tokyo Institute of Technology
    Inventors: Sakuji Ikeda, Kazuo Soga
  • Patent number: 4208522
    Abstract: Substituted piperazine diones are stabilizers for synthetic polymeric materials normally subject to deterioration caused by ultraviolet light. The compounds are prepared by the alkylation reaction between a substituted piperazine dione and an organic halide. Polymeric compositions containing these stabilizers may also contain a hindered phenolic compound. A typical embodiment is 15,15'-dodecamethylenebis(7,15-diazadispiro[5,1,5,3]hexadecane-14,16-dione ).
    Type: Grant
    Filed: October 6, 1978
    Date of Patent: June 17, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Chester E. Ramey, John J. Luzzi
  • Patent number: 4208340
    Abstract: Ortho-quinones with alkyl, olefin polymer, or halogen substituents and a process for the preparation of these compounds comprising a base catalyzed halogen oxidation of alkylated phenol.
    Type: Grant
    Filed: October 30, 1978
    Date of Patent: June 17, 1980
    Assignee: Standard Oil Company (Indiana)
    Inventor: Richard J. Lee
  • Patent number: 4203986
    Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 represents a hydrogen or fluorine atom, and R.sub.2 represents an alkyl group containing 2 to 6 carbon atoms, or a cycloalkyl or cycloalkyl-alkyl group containing 5 to 8 carbon atoms, each of these groups being substituted by one or two hydroxy groups or an oxo group and, if desired, also by a 4-(m-trifluoromethylphenyl)-piperazino or 4-(3-trifluoromethyl-4-fluoro-phenyl)-piperazino group with the proviso that, when R.sub.1 represents a hydrogen atom, R.sub.2 does not represent a monohydroxyalkyl group, and their pharmaceutically acceptable acid addition salts are novel and have therapeutic use, notably in the region of the central nervous system and in the cardiovascular region.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: May 20, 1980
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin, Yves R. A. Pascal
  • Patent number: 4203901
    Abstract: This invention relates to a process for making N-(N'-methylenepyrrolidonyl)-2-substituted anilines in high yield. The products are useful intermediates in the synthesis of herbicides.The process comprises reacting substantially equivalent molar concentrations of a 2-substituted aniline, as defined herein, with N-methylolpyrrolidone in an aromatic hydrocarbon solvent in the absence of an acid or base catalyst at a reflux temperature of 80.degree.-140.degree. C. while simultaneously and continuously distilling out from the reaction mixture an azeotrope consisting essentially of water and solvent until substantially all the water produced during the reaction has been removed thereby, and, thereafter, crystallizing the product from the remaining solution.
    Type: Grant
    Filed: November 20, 1978
    Date of Patent: May 20, 1980
    Assignee: GAF Corporation
    Inventors: Louis Schneider, David E. Graham
  • Patent number: 4202896
    Abstract: Piperazine derivatives of the general formula ##STR1## wherein R.sub.1 -R.sub.9 are the same or different and each represents a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, n is 2 or 3 and X represents a group (CH.sub.2).sub.m (in which m is 1, 2, 3 or 4) or a group --CH.sub.2 --CH.dbd.CH--, having methylene linked to the piperazine group, and acid addition and quaternary ammonium salts thereof, are described.The compounds exhibit a strong specific dopaminergic activity.Also described are methods for their preparation and use as therapeutic agents in the form of therapeutic compositions.
    Type: Grant
    Filed: December 14, 1977
    Date of Patent: May 13, 1980
    Assignee: Gist-Brocades N.V.
    Inventor: Johan Gootjes
  • Patent number: 4200642
    Abstract: Novel spiro-oxazolidindiones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.
    Type: Grant
    Filed: August 21, 1978
    Date of Patent: April 29, 1980
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4199519
    Abstract: Polyprenyl derivatives having the formula ##STR1## [wherein A and B individually represent a group of the formula --CH.sub.2 OR.sup.1 (wherein R.sup.1 is hydrogen atom, an alkyl group having an intervening hetero atom in the carbon chain, carboxyl group on its salt or an aliphatic acyl group optionally having an intervening hetero atom in the carbon chain, an aromatic acyl group, a heterocyclic acyl group, an araliphatic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt) or where one of A and B represents the group --CH.sub.2 OR.sup.1, the other represents a group of the formula --COOR.sup.2 (wherein R.sup.2 represents hydrogen atom, a metal atom capable of forming a salt, an organic base or an akyl group), a group of the formula ##STR2## or a group of the formula ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen atom, an alkyl group optionally having a heterocyclic substituent, an aryl group or an aralkyl group or R.
    Type: Grant
    Filed: August 31, 1978
    Date of Patent: April 22, 1980
    Assignee: Sankyo Company Limited
    Inventors: Hiroshi Mishima, Akira Ogiso, Shinsaku Kobayashi
  • Patent number: 4199507
    Abstract: Disclosed are degradation products of the antibiotics rubradirin and rubradirin B and processes for their preparation. Some of these products have antibacterial activity, and, thus, can be used in various environments to inhibit susceptible bacteria. Also, some of these products can be used as intermediates to make useful antibacterials.
    Type: Grant
    Filed: August 31, 1978
    Date of Patent: April 22, 1980
    Assignee: The Upjohn Company
    Inventor: Herman Hoeksema
  • Patent number: 4198509
    Abstract: The mercaptoacylpiperazine carboxylic acid compounds which have the formula ##STR1## wherein R, R.sub.3 and R.sub.4 each is hydrogen or lower alkyl;R.sub.1 is lower alkyl;R.sub.2 is hydrogen, lower alkanoyl, benzoyl or ##STR2## m is 0, 1 or 2; n is 1, 2 or 3, the sum of m+n being equal to 1, 2 or 3and salts thereof, are useful as hypotensive agents.
    Type: Grant
    Filed: October 30, 1978
    Date of Patent: April 15, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Kathryn A. Losee, Jack Bernstein
  • Patent number: 4198424
    Abstract: Selected substituted 1-phenyl-2-pyrrolidin-2-yl-ethanols and their pharmacologically-acceptable acid-addition salts are useful as analgesics in human and veterinary medicine. Such compounds are prepared by reducing corresponding substituted 1-phenyl-2-pyrrolidin-2-yl ethanones and are formulated into medicinal compositions suitable for administration.
    Type: Grant
    Filed: November 30, 1978
    Date of Patent: April 15, 1980
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Klaus Eistetter, Hans-Peter Kley
  • Patent number: 4196291
    Abstract: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof. This is a division, or application Ser. No. 742,133, filed on Nov. 15, 1976, which in turn is a divisional of Ser. No. 533,467, filed on Dec. 16, 1974, now U.S. Pat. No. 4,001,411.
    Type: Grant
    Filed: December 18, 1978
    Date of Patent: April 1, 1980
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Jurgen Seubert, Herbert Thomas, Peter Andrews
  • Patent number: 4193925
    Abstract: An improved process for the preparation of 2-pyrrolidone by the liquid phase hydrogenation of succinonitrile in the presence of a hydrogenation catalyst and ammonia, whereafter the resulting hydrogenation product is hydrolyzed with water. A hydrogenation catalyst in the form of a fixed bed is used, and a liquid phase of succinonitrile and liquid ammonia is passed over the catalyst at a temperature of between 50.degree. and 130.degree. C.
    Type: Grant
    Filed: January 18, 1979
    Date of Patent: March 18, 1980
    Assignee: Stamicarbon, B.V.
    Inventors: Peter J. N. Meijer, Johannes G. M. Nieuwkamp
  • Patent number: 4193922
    Abstract: Herbicidal and fungicidal compounds of the formula ##STR1## wherein R.sub.1 is substituted or unsubstituted phenyl or naphthyl and R.sub.2 and R.sub.3 are the same or different and are C.sub.1 -C.sub.5 alkyl or from a five- or six-membered ring.
    Type: Grant
    Filed: June 8, 1976
    Date of Patent: March 18, 1980
    Assignee: Eszakmagyarorszagi Vegyimuvek
    Inventors: Pal Agocs, Istvan Fabian, Andras Gajdacsi, Sandor Nagy, Zoltan Pinter
  • Patent number: 4192803
    Abstract: This disclosure describes substituted 11-piperazinyl-5H-pyrrolo[2,1-c][1,4]benzodiazepines useful as anti-psychotic or neuroleptic agents.
    Type: Grant
    Filed: September 15, 1978
    Date of Patent: March 11, 1980
    Assignee: American Cyanamid Company
    Inventors: William B. Wright, Jr., Robert A. Hardy, Jr.
  • Patent number: 4192867
    Abstract: 2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
    Type: Grant
    Filed: December 21, 1977
    Date of Patent: March 11, 1980
    Assignee: Abbott Laboratories
    Inventors: Jerry R. Martin, John S. Tadanier, Paulette Collum