Patents Represented by Attorney William G. Isgro

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  • 6-Chloro-1,2,3,4-tetrahydrocarbazole-2-one
    Patent number: 4179443
    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 the 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: December 21, 1978
    Date of Patent: December 18, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, John W. Scott
  • Carbazole acetic acid derivatives
    Patent number: 4178289
    Abstract: A process for the preparation of 6-chloro-.alpha.-methylcarbazole-2-acetic acid from 6-chloro-.alpha.-hydroxy-.alpha.-methylcarbazole-2-acetic acid and/or 6-chloro-.alpha.-methylene-2-carboxylic acid, is described. The preparation of intermediates, such as, 6-chloro-.alpha.-hydroxy-.alpha.-methylcarbazole-2-acetic acid and lower alkyl carbazole-2-oxalate, inter alia, is also described.
    Type: Grant
    Filed: January 11, 1979
    Date of Patent: December 11, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Alfred J. Corraz, David R. Parrish, John W. Scott
  • 2,4-Pyrimidine-dicarbamate-3-oxides
    Patent number: 4176119
    Abstract: Oxadiazolopyrimidine derivatives of the formula ##STR1## wherein R and R.sub.1 are as hereinafter described, prepared, inter alia, by cyclizing a compound of the formula ##STR2## wherein R and R.sub.1 are as hereinafter 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 26, 1978
    Date of Patent: November 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • 5-(6-Alkylindol-3-ylmethylene)-1,3-dimethyl-2-(methylimino)- 4-imidazolidinones
    Patent number: 4176230
    Abstract: 5-(6-alkylindol-3-ylmethylene)-1,3-dimethyl-2-(methylimino)-4-imidazolidino nes, prepared, inter alia, from the corresponding substituted indole-3-carboxaldehyde and dimethylcreatinine, are described. The imidazolidinones are useful as antidepressants.
    Type: Grant
    Filed: August 4, 1977
    Date of Patent: November 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Andrew D. Batcho
  • 6-Chloro-2,4-pyrimidine-dicarbamate-3-oxides
    Patent number: 4175190
    Abstract: Oxadiazolopyrimidine derivatives of the formula ##STR1## wherein R and R.sub.1 are as hereinafter described, prepared, inter alia, by cyclizing a compound of the formula ##STR2## wherein R and R.sub.1 are as hereinafter 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 26, 1978
    Date of Patent: November 20, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • 6-Chloro-2,4-pyrimidine-dicarbamate-3-oxides
    Patent number: 4175189
    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: November 20, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Method of treating depression with thiourea derivatives
    Patent number: 4169154
    Abstract: A method of utilizing thiourea derivatives of the formulas ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and X are as hereinafter described, as agents in the treatment of depression, is described.
    Type: Grant
    Filed: September 25, 1978
    Date of Patent: September 25, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael R. Cohen, Richard W. Kierstead, Jefferson W. Tilley
  • 7-Methoxy-5-oxo-5H-thiazolo[2,3-b]quinazoline-2-carboxylic acid
    Patent number: 4168380
    Abstract: 7-Methoxy-5-oxo-5H-thiazolo[2,3-b]quinazoline-2-carboxylic acid, useful as an antiallergic agent, and prepared by reaction of 5-methoxyanthranilic acid with methyl 2-chlorothiazole-5-carboxylate, and subsequent hydrolysis, is described.
    Type: Grant
    Filed: April 21, 1978
    Date of Patent: September 18, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ronald A. LeMahieu
  • Derivatives of 3-phenylisoindole-1-carboxylic acid
    Patent number: 4167632
    Abstract: Isoindole derivatives of the formula ##STR1## wherein A, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and n are as hereinafter set forth, as well as intermediates, are described. The end products of formula I are useful as appetite-suppressants.
    Type: Grant
    Filed: July 26, 1978
    Date of Patent: September 11, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Carbazole methyl malonates
    Patent number: 4158007
    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 21, 1978
    Date of Patent: June 12, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harvey Gurien, Sidney Teitel
  • Cyano-enol ethers
    Patent number: 4151196
    Abstract: The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: April 24, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • Oxadiazolopyrimidine derivatives
    Patent number: 4150132
    Abstract: Alkyl or alkoxyalkyl 5-[3,6-dihydro-1(2H)-pyridyl]-2-oxo-2H-[1,2,4]-oxadiazolo-[2,3-a]primidine -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: January 27, 1978
    Date of Patent: April 17, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Hydroxy methyl carbazole acetic acid and esters
    Patent number: 4150031
    Abstract: A process for the preparation of 6-chloro-.alpha.-methylcarbazole-2-acetic acid from 6-chloro-.alpha.-hydroxy-.alpha.-methylcarbazole-2-acetic acid and/or 6-chloro-.alpha.-methylene-2-carboxylic acid, is described. The preparation of intermediates, such as, 6-chloro-.alpha.-hydroxy-.alpha.-methylcarbazole-2-acetic acid and lower alkyl carbazole-2-oxalate, inter alia, is also described.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: April 17, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Alfred J. Corraz, David R. Parrish, John W. Scott
  • Substituted oxadiazolopyrimidines
    Patent number: 4150131
    Abstract: Oxadiazolopyrimidine derivatives of the formula ##STR1## wherein R and R.sub.1 are as hereinafter described, prepared, inter alia, by cyclizing a compound of the formula ##STR2## wherein R and R.sub.1 are as hereinafter 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: January 27, 1978
    Date of Patent: April 17, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Method of reducing blood pressure with thiourea derivatives and guanidine derivatives
    Patent number: 4150138
    Abstract: Antihypertensively active thiourea derivatives of the formulas ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and X are as hereinafter described, as well as a method of using a compound of the formula ##STR2## wherein R.sub.1 ', R.sub.2 ', R.sub.3 and X are as previously described, or a compound of formula II as an anti-hypertensive agent, is described.
    Type: Grant
    Filed: March 6, 1978
    Date of Patent: April 17, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael R. Cohen, Richard W. Kierstead, Jefferson W. Tilley
  • Antibacterial compositions
    Patent number: 4146620
    Abstract: Compositions comprising N-sulfanilyl-1-ethylcytosine and a sulfonamide potentiator, which are useful as antibacterial agents, are described.
    Type: Grant
    Filed: March 2, 1978
    Date of Patent: March 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erika Bohni, Marc Montavon
  • Dihydrocarbazole acetic acid and esters thereof
    Patent number: 4146542
    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 the 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: June 12, 1978
    Date of Patent: March 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, John W. Scott
  • Process for substituted 5-benzyl-2,4-diamino-pyrimidines
    Patent number: 4143227
    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: June 10, 1977
    Date of Patent: March 6, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • 3-Cyano-N-(N,N-dimethylaminopropyl)-iminodibenzyl and salts thereof
    Patent number: 4138482
    Abstract: 3-Cyano-N-(N,N-dimethylaminopropyl)-iminodibenzyl, and its salts, prepared, inter alia, by heating 3-cyano-iminodibenzyl-5-carboxylic acid (N,N-dimethylaminopropyl ester) are described. The end product and its salts are useful as antidepressants.
    Type: Grant
    Filed: October 11, 1977
    Date of Patent: February 6, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Philippe Dostert
  • Preparation of 2,4-diamino-5-(4-amino-3,5-substituted-benzyl)-pyrimidines
    Patent number: 4137411
    Abstract: A benzylpyrimidines of the formula ##STR1## wherein r.sup.1 and R.sup.2 independently are C.sub.1-3 -alkyl or C.sub.1-3 -alkoxy, and R is hydrogen or lower alkyl, is treated with hydroxylamine or a salt thereof in polyphosphoric acid or alternatively, when R is hydrogen, is treated with sodium azide in polyphosphoric acid, to yield the corresponding 4-amino benzylpyrimidine.
    Type: Grant
    Filed: February 1, 1978
    Date of Patent: January 30, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Alexander E. Wick