Patents Examined by Jose Tovar
  • Patent number: 4327213
    Abstract: Pharmaceutical compositions having anti-ulcer activity, containing as an active ingredient a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Het is a heteroaromatic group (substituted or unsubstituted), containing one or more nitrogen atoms as hetero atoms and no more than two rings;X is a hydrogen atom or a cyano, trifluoromethyl or an amido group with the formula--C(A)NR.sup.1 R.sup.2, wherein A is oxygen or sulphur, R.sup.1 is hydrogen or a C.sub.1-4 alkyl group, R.sup.2 is hydrogen or a C.sub.1-4 alkyl group, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 5- to 6-membered heterocyclic ring in which another hetero atom may be present; andR is C.sub.1-6 alkyl, C.sub.5-6 cycloalkyl, C.sub.5-8 cycloalkylalkyl, C.sub.3-6 alkenyl, C.sub.3-4 alkynyl, phenyl C.sub.1-3 alkyl, the phenyl group being optionally substituted by one or more C.sub.1-6 alkyl, halogen, C.sub.
    Type: Grant
    Filed: December 29, 1977
    Date of Patent: April 27, 1982
    Assignee: ACF Chemiefarma VA
    Inventor: Jacob A. van Zorge
  • Patent number: 4322417
    Abstract: Polyfluorohydroxyisopropyl tricyclic carbostyrils, such as 2,3-dihydro-7-methyl-9-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl ]-5H-[1,4]thiazino[2,3,4-ij]-quinolin-5-one, useful as antihypertensive agents.
    Type: Grant
    Filed: December 22, 1977
    Date of Patent: March 30, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Paul E. Aldrich, Gilbert H. Berezin
  • Patent number: 4271161
    Abstract: Compounds of the formula: ##STR1## in which R represents an ethyl or isopropyl group, and their addition salts with acids or quaternary ammonium salts can be prepared from the compounds: ##STR2## in which R has the same meaning as above, and are valuable as analgesics.
    Type: Grant
    Filed: July 9, 1979
    Date of Patent: June 2, 1981
    Assignee: Hexachimie
    Inventor: Jean M. Teulon
  • Patent number: 4267178
    Abstract: Disubstituted piperazines of the formula ##STR1## in which n is 1 or 2,m is 0 or 1, andHet is pyridyl, pyrimidinyl, pyrazinyl, thiazolyl or thiadiazolyl each optionally substituted by one or more alkyl having from 1 to 5 carbon atoms inclusive.These compounds and their physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of hypertension.
    Type: Grant
    Filed: February 26, 1979
    Date of Patent: May 12, 1981
    Assignee: Science Union et Cie, Societe Francaise de Recherche Med.
    Inventors: Gilbert Regnier, Michel Laubie, Jean-Claude Poignant
  • Patent number: 4267327
    Abstract: 2-Hydroxymethyl-pyrazine derivatives are disclosed, such as, for instance, the compound 2-hydroxymethyl-5-methylpyrazine-4-oxide. The compounds exhibit an elevated lipid lowering activity, and can be used to control triglyceride and cholesterol levels.
    Type: Grant
    Filed: February 26, 1979
    Date of Patent: May 12, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Cozzi, Osvaldo Magni, Leone Bertone, Romano Angelucci, Pier P. Lovisolo
  • Patent number: 4261998
    Abstract: 2-(2-Chlorobenzyl)-1,2,3,4-tetrahydroisoquinoline of the formula ##STR1## and its pharmaceutically acceptable addition salts, are useful for the treatment of arterial or venous thrombosis. They can be prepared by reducing the amide 2-(2-chlorobenzoyl)-1,2,3,4-tetrahydroisoquinoline, for example with boron hydride in an inert organic solvent, and optionally converting a free amine thereby produced into a salt.
    Type: Grant
    Filed: November 13, 1979
    Date of Patent: April 14, 1981
    Assignee: Synthelabo
    Inventor: Henry Najer
  • Patent number: 4256758
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: March 17, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4255426
    Abstract: 1-(2-Hydroxy-3-n-alkoxypropyl)-4-substituted-piperazines and piperidines and derivatives thereof useful as immune regulants are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds and a method of regulating the immune response of a subject by administration of the novel compounds.
    Type: Grant
    Filed: July 9, 1979
    Date of Patent: March 10, 1981
    Assignee: Pfizer Inc.
    Inventor: Allen R. Kraska
  • Patent number: 4255334
    Abstract: 3-Azabicyclo(3.1.0)hexane-2-carboxylic acid, a plant gametocide, is prepared by effecting reaction between cis 2-aminomethylcyclopropyl-1,1-dimethyl acetal and a cyanide in the presence of a liquid lower-alkanecarboxylic acid; treating the resulting N-alkanoyl-3-azabicyclo(2.1.0)hexane-2-carbonitrile with a strong acid; treating the resulting 3-alkanoyl-3-azabicyclo(3.1.0)hexane-2-carboxylic acid with strong acid to form the desired 3-azabicyclo(3.1.0)hexane-2-carboxylic acid.
    Type: Grant
    Filed: June 18, 1979
    Date of Patent: March 10, 1981
    Assignee: Shell Oil Company
    Inventors: Janet A. Day, Barry R. J. Devlin, Robert J. G. Searle
  • Patent number: 4255575
    Abstract: Derivatives of 2-hydroxy-5-(1-hydroxy-2-piperazinylethyl)benzoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful as spasmolytic and antihypertensive agents.
    Type: Grant
    Filed: May 4, 1979
    Date of Patent: March 10, 1981
    Assignee: Richardson-Merrell Inc.
    Inventors: J. Martin Grisar, George P. Claxton
  • Patent number: 4255333
    Abstract: A process for the preparation of an indolenine of the formula ##STR1## where R, X and Y are conventional substituents, by thermal rearrangement of a compound of the formula ##STR2## to give a compound of the formula ##STR3## and cyclization of this compound in the presence of an acid catalyst.
    Type: Grant
    Filed: January 30, 1979
    Date of Patent: March 10, 1981
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Joachim Opgenorth, Horst Scheuermann, Harald Laas, Axel Nissen
  • Patent number: 4254124
    Abstract: 2-[3-[4-[3-(Trifluoromethyl)phenyl]-1-piperazinyl]propyl]-1,2,4-triazolo[4, 3-a]pyridin-3(2H)-one and its pharmaceutically acceptable acid addition salts are antidepressant agents.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: March 3, 1981
    Assignee: Mead Johnson & Company
    Inventor: Duane F. Morrow
  • Patent number: 4252721
    Abstract: Compounds of the general formula: ##STR1## in which alk and alk' represent the bivalent radicals; aliphatic alkyl chains; and R and R' represent the alkyl, halogen, hydrogen, alkyloxy, --OH, --CF.sub.3 or --SCH.sub.3 radicals. Said compounds of the formula I are effective and useful as antiglaucomic and antipsychotic agents and also as additive agents in the withdrawal treatment of various addictive conditions. Methods for their preparation are also disclosed.
    Type: Grant
    Filed: March 29, 1979
    Date of Patent: February 24, 1981
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Bruno Silvestrini, Leandro Baiocchi
  • Patent number: 4252949
    Abstract: Previously unknown and undescribed long chain (C-12 to C-18) monoesters of pyrazinetetracarboxylic acid have been prepared and shown to be effective surface active agents useful as detergents, sequestrants, and chelating agents for extractive metallurgy.
    Type: Grant
    Filed: August 31, 1979
    Date of Patent: February 24, 1981
    Inventor: Richard H. Wiley
  • Patent number: 4252806
    Abstract: 2-[3-[4-Arylpiperazin-1-yl]propyl]-1,2,4-triazolo[4,3-a]-quinolin-3(2H)-one s are antidepressant agents.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: February 24, 1981
    Assignee: Mead Johnson & Company
    Inventor: Duane F. Morrow
  • Patent number: 4251525
    Abstract: 3-Allyl-7,8-dihydroxy-6-halo-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-be nzazepine derivatives are prepared by N-allylation of 7,8-dimethoxy-6-halo-1-(4-methoxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi ne using an allyl halide in acetonitrile in the presence of base followed by O-demethylation. These compounds have a unique cardiovascular effect in that they are potent renal vasodilators and also induce bradycardia.
    Type: Grant
    Filed: May 25, 1979
    Date of Patent: February 17, 1981
    Assignee: SmithKline Corporation
    Inventor: Joseph Weinstock
  • Patent number: 4251660
    Abstract: A method for preparing 1,2,3,4-tetrahydroisoquinolines comprising heating N-halo or hydroxyethyl-N-benzylamines in an aluminum chloride melt at 160.degree.-210.degree..
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: February 17, 1981
    Assignee: SmithKline Corporation
    Inventors: Bing L. Lam, Wilford L. Mendelson, Charles B. Spainhour, Jr.
  • Patent number: 4251659
    Abstract: Polyfluorohydroxyisopropyl: -indolines, -tetrahydroquinolines, and -benzazepines, such a .alpha.,.alpha.-bis(trifluoromethyl)-1,2,3,4-tetrahydroquinoline-6-methano l, useful as intermediates for antihypertensives.
    Type: Grant
    Filed: December 22, 1977
    Date of Patent: February 17, 1981
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Paul E. Aldrich, Gilbert H. Berezin
  • Patent number: 4251534
    Abstract: Polyfluorohydroxyisopropyl bicyclic and tricyclic carbostyrils, such as 2,3-dihydro-7-methyl-9-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl ]-5H-pyrido[1,2,3-de]-1,4-benzoxazin-5-one, useful as antihypertensive agents.
    Type: Grant
    Filed: December 22, 1977
    Date of Patent: February 17, 1981
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Aldrich Paul E., Gilbert H. Berezin
  • Patent number: RE30563
    Abstract: Benzoylureas are prepared from a benzamide, an alkyllithium, a phenyl chloroformate, and an amine. Two reaction sequences are described. The benzoylureas obtained by the process are useful as insecticides.
    Type: Grant
    Filed: November 2, 1979
    Date of Patent: March 31, 1981
    Assignee: Eli Lilly and Company
    Inventors: Riaz F. Abdulla, Norman H. Terando