Patents Represented by Attorney William G. Isgro

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  • Process of making 6-chloro-.alpha.-methyl-carbazole-2-acetic acid
    Patent number: 4264500
    Abstract: The aromatization of (6-chloro-1,2,3,4-tetrahydro-2-carbazolyl)-methyl-malonic acid dialkyl ester, utilizing chlorine and subsequent conversion of the resulting product to 6-chloro-.alpha.-methyl-carbazole-2-acetic acid by hydrolysis and decarboxylation are described.
    Type: Grant
    Filed: February 28, 1980
    Date of Patent: April 28, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Willy Zwahlen
  • Octahydro-1H-pyrrolo[2,3-g]isoquinolines
    Patent number: 4260762
    Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth,are described.
    Type: Grant
    Filed: September 10, 1979
    Date of Patent: April 7, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Process for the preparation of oxadiazolopyrimidine derivatives
    Patent number: 4256886
    Abstract: A process for preparing oxadiazolopyrimidines of the formula ##STR1## wherein R is alkyl or alkoxyalkyl, by reacting a compound of the formula ##STR2## wherein R is as set forth above, with phosgene, is described.
    Type: Grant
    Filed: February 21, 1980
    Date of Patent: March 17, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Imidazo[2,1-b]quinazolin-2(3H)-ones and pharmaceutical compositions for treatment and prophylaxis of cardiac insufficiency and cardiac failure
    Patent number: 4256748
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1,R.sup.2,R.sup.3 and R.sup.4 are as hereinafter described, tautomers and salts thereof, are disclosed. The foregoing compounds inhibit the aggregation of blood platelets which renders them useful as therapeutic agents in the prophylaxis of thromboses. Furthermore, they are useful for the treatment and prophylaxis of cardiac insufficiency and cardiac failure, due to their inotropic activity without substantial tachycardia.
    Type: Grant
    Filed: June 20, 1979
    Date of Patent: March 17, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Madhukar S. Chodnekar, Ado Kaiser
  • Process for preparing 2,4-diamino-pyrimidines
    Patent number: 4255574
    Abstract: A process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are lower alkoxy or taken together are methylenedioxy; R.sub.3 is lower alkyl or hydrogen, which comprises the step of reacting an aromatic compound of the formula ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as previously described, with a diamino-pyrimidine of the formula ##STR3## wherein R.sub.4 is lower alkoxy, benzyloxy, hydroxy or halogen, in the presence of an inorganic or organic acid selected from the group consisting of ortho-phosphoric acid, poly-phosphoric acid, hydrohalic acids and tri-haloacetic acids, at a temperature in the range of from about 50.degree. C. to about 110.degree. C., is described.
    Type: Grant
    Filed: December 8, 1978
    Date of Patent: March 10, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • Benzylpyrimidines
    Patent number: 4251454
    Abstract: Benzylpyrimidines of the formula ##STR1##wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter described, are prepared. The benzylpyrimidines are useful as potentiators of the activity of the sulfonamides.
    Type: Grant
    Filed: July 24, 1978
    Date of Patent: February 17, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Gerald Rey-Bellet, Guido Zanetti
  • Treatment of gastric ulcers with naphthimidazole derivatives
    Patent number: 4248880
    Abstract: Imidazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X and n are as hereinafter set forth,and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of gastric ulcers.
    Type: Grant
    Filed: July 2, 1979
    Date of Patent: February 3, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Ernst-Peter Krebs
  • 2-Imino-imidazolidine derivatives
    Patent number: 4244957
    Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.
    Type: Grant
    Filed: November 6, 1978
    Date of Patent: January 13, 1981
    Assignee: Hoffman-La Roche Inc.
    Inventor: Henri Ramuz
  • Phenyl-quinolizidines
    Patent number: 4236010
    Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
    Type: Grant
    Filed: October 15, 1979
    Date of Patent: November 25, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Process of making a carbazole acetic acid
    Patent number: 4234487
    Abstract: A process for preparing 6-chloro-.alpha.-methylcarbazole-2-acetic acid and esters thereof by the steps of:(a) reacting 6-chloro-1,2,3,4-tetrahydrocarbazole-2-one with a trialkyl-.alpha.-methylphosphonoacetate to yield corresponding 3,4-dihydro-.alpha.-methylcarbazole-2-acetic acid ester; and(b) aromatizing the reaction product of step (a), prior to or after saponification, to yield, respectively, 6-chloro-.alpha.-methylcarbazole-2-acetic acid or ester, is described. Additionally, there are described 6-chloro-1,2,3,4-tetrahydrocarbazole-2-one useful as an intermediate, and dihydrocarbazoles useful as intermediates and/or as anti-inflammatory and antirheumatic agents.
    Type: Grant
    Filed: May 3, 1979
    Date of Patent: November 18, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, John W. Scott
  • Carbazole melonates
    Patent number: 4226774
    Abstract: A process for the preparation of .alpha.-methyl-carbazole-2-acetic acids, which comprises reacting an .alpha.-methyl-3-oxocyclohexane malonic acid di-lower alkyl ester with a substituted phenylhydrazine, and thereafter sequentially oxidizing and hydrolyzing the reaction product to obtain the desired acid, is described.
    Type: Grant
    Filed: August 8, 1979
    Date of Patent: October 7, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harvey Gurien, Sidney Teitel
  • Halo-3-dibenzofuran alkanonitriles
    Patent number: 4222944
    Abstract: Dibenzofurans of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are as hereinafter described prepared, inter alia, from the correspondingly substituted phenol and haloketocyclohexane are described. The dibenzofurans of the invention are useful anti-inflammatory, analgesic and anti-rheumatic agents.
    Type: Grant
    Filed: July 31, 1978
    Date of Patent: September 16, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Robert A. Schmidt
  • Process for the preparation of oxadiazolopyrimidine derivatives
    Patent number: 4220772
    Abstract: A process for preparing oxadiazolopyrimidines of the formula ##STR1## wherein R is alkyl or alkoxyalkyl, by reacting a compound of the formula ##STR2## wherein R is as set forth above, with phosgene, is described.
    Type: Grant
    Filed: July 6, 1979
    Date of Patent: September 2, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Liquid crystal mixtures
    Patent number: 4198130
    Abstract: Liquid crystal mixtures having positive anisotropy of the dielectric constants comprising a nematogenic material having a clearing point above 60.degree. C., one or more compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or straight-chain alkyl, provided that at least one of R.sub.1 and R.sub.2 is other than hydrogen and that R.sub.1 and R.sub.2 together contain no more than 9 carbon atoms,and, if desired, one or more additional doping agents, are described.
    Type: Grant
    Filed: May 22, 1978
    Date of Patent: April 15, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Alfred Germann, Martin Schadt, Hanspeter Scherrer
  • Immunoassay for phencyclidine
    Patent number: 4196185
    Abstract: An improved immunoassay for detecting the drug of abuse phencyclidine is described. This immunoassay is characterized in utilizing as reagents (i) an antibody elicited with a novel immunogen comprising 4-[(1-piperidinyl)cyclohexyl] benzoic acid covalently bonded to an immunogenic carrier material through the carboxyl group and (ii) a novel radiolabeled derivative of phencyclidine, namely .sup.125 I N-(4-hydroxy-2-phenylethyl)-4-[1-(1-piperidinyl)cyclohexyl] benzamide.
    Type: Grant
    Filed: June 5, 1978
    Date of Patent: April 1, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Antonino Focella, John E. Heveran
  • 5-(Indol-3-ylmethylene)-1,3-dimethyl-2-methylamino-4-imidazolidinone
    Patent number: 4195179
    Abstract: 5-(Indol-3-ylmethylene)-1,3-dimethyl-2-methylimino-4-imidazolidinone and its geometric isomers, prepared, inter alia, from indole-3-aldehyde and 1,3-dimethyl-2-methylimino-4-imidazolidinone, are described. The end products are useful as antidepressants.
    Type: Grant
    Filed: September 2, 1977
    Date of Patent: March 25, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert J. Wells, Peter T. Murphy
  • Tetrahydro 2-carbazolyl methyl malonate derivatives
    Patent number: 4193923
    Abstract: A process for the preparation of .alpha.-methyl-carbazole-2-acetic acids, which comprises reacting an .alpha.-methyl-3-oxocyclohexane malonic acid di-lower alkyl ester with a substituted phenylhydrazine, and thereafter sequentially oxidizing and hydrolyzing the reaction product to obtain the desired acid, is described.
    Type: Grant
    Filed: March 23, 1979
    Date of Patent: March 18, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harvey Gurien, Sidney Teitel
  • Certain 8-halodibenzofuran-3-alkanols
    Patent number: 4192809
    Abstract: Dibenzofurans of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are as hereinafter described, prepared, inter alia, from the correspondingly substituted phenol and haloketocyclohexane are described. The dibenzofurans of the invention are useful antiinflammatory, analgesic and anti-rheumatic agents.
    Type: Grant
    Filed: April 7, 1978
    Date of Patent: March 11, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Robert A. Schmidt
  • 6-[3,6-Dihydro-1(2H)-pyridyl]-pyrimidine-3-oxides
    Patent number: 4182867
    Abstract: Alkyl or alkoxyalkyl 5-[3,6-dihydro-1(2H)-pyridyl]-2-oxo-2H-[1,2,4]-oxadiazolo-[2,3-a]pyrimidin e-7-carbamates, prepared, inter alia, from the corresponding 6-[3,6-dihydro-1(2H)-pyridyl]-2,4-pyrimidine-dicarbamate-3-oxide, are described. The end products are useful in the treatment of vascular-conditioned hypertension or as vasodilators in the case of peripheral blood supply disorders.
    Type: Grant
    Filed: December 22, 1978
    Date of Patent: January 8, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Naphth[2,3-d]imidazoles
    Patent number: 4182766
    Abstract: Imidazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 R.sub.4, R.sub.5, X and n are as hereinafter set forth,and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of gastric ulcers.
    Type: Grant
    Filed: September 11, 1978
    Date of Patent: January 8, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Ernst-Peter Krebs