Patents Represented by Attorney William G. Isgro

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  • Tricyclic compounds
    Patent number: 4136116
    Abstract: 1-Methyl(or acetyl)-5H-dibenzo[a,d]cycloheptenes and 1-methyl(or acetyl)-10,11-dihydro-5H-dibenzo[a,d]cycloheptenes bearing a basic side chain at the 5-position, such as a 3-mono- or dimethylaminopropylidene, a 3-mono- or dimethylaminopropyl or a 3-dimethylaminopropylidene(or propyl)-N-oxide, intermediates and processes for their preparation, are described. The end products are useful antidepressants.
    Type: Grant
    Filed: March 14, 1975
    Date of Patent: January 23, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emilio Kyburz, Hans Spiegelberg
  • Process and intermediates for isoindole derivatives
    Patent number: 4130717
    Abstract: A process for the preparation of isoindole derivatives which comprises heating a compound of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as hereinafter set forth, in the presence of a suitable imidazole, is described.
    Type: Grant
    Filed: February 17, 1978
    Date of Patent: December 19, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Derivatives of 3-phenylisoindole-1-carboxylic acid
    Patent number: 4122265
    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: April 22, 1977
    Date of Patent: October 24, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Dibenz(b,f)oxepin derivatives
    Patent number: 4118572
    Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described, are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
    Type: Grant
    Filed: March 18, 1977
    Date of Patent: October 3, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
  • Process for preparing 2,4-diamino-5-(substituted benzyl)-pyrimidines
    Patent number: 4115650
    Abstract: 2,4-Diaminopyrimidines bearing a substituted benzyl group in position-1 are prepared from the correspondingly substituted .alpha.-alkoxymethylcinnamonitrile by treatment of the latter with an alkali metal alkoxide in mono-methyl ether of ethylene glycol and subsequently reacting the resulting reaction mixture with guanidine.
    Type: Grant
    Filed: November 17, 1976
    Date of Patent: September 19, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Percy Manchand
  • Ribofuranosyl-imidazole derivatives
    Patent number: 4115641
    Abstract: Ribofuranoysl-imidazole derivatives of the formula ##STR1## wherein R, X, Y and Z have one of the meanings set forth hereinafter, are described. The ribofuranosyl-imidazole derivatives have cardiac and circulatory-dynamic properties and are useful in the treatment of angina pectoris.
    Type: Grant
    Filed: August 1, 1977
    Date of Patent: September 19, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Pierre-Charles Wyss
  • 1-(2-Aminoethyl)-3-(2,6-dihalophenyl)guanidines
    Patent number: 4113776
    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: October 25, 1977
    Date of Patent: September 12, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Robert Cohen, Richard Wightman Kierstead, Jefferson Wright Tilley
  • Process for preparing cyano-enol ethers
    Patent number: 4108888
    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: February 18, 1977
    Date of Patent: August 22, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • Dibenz[b,f]oxepin derivatives
    Patent number: 4105664
    Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
    Type: Grant
    Filed: March 18, 1977
    Date of Patent: August 8, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
  • Dibenz[b,f]oxepin derivatives
    Patent number: 4100173
    Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described,Are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
    Type: Grant
    Filed: March 18, 1977
    Date of Patent: July 11, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
  • Amides of 2-(3-dibenzofuran) alkanoic acids
    Patent number: 4097497
    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: January 27, 1977
    Date of Patent: June 27, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Robert August Schmidt
  • Thiourea derivatives for treating hypertension
    Patent number: 4096276
    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: January 27, 1977
    Date of Patent: June 20, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Robert Cohen, Richard Wightman Kierstead, Jefferson Wright Tilley
  • 4-[5(R)-Alkyl(or alkenyl)-4(S)-quinuclidin-2(S) or 2(R)-ylcarbonyl]-quinolines, antipodes or racemates thereof and processes for their preparation
    Patent number: 4096146
    Abstract: Quinine, quinidine, their antipodes or racemates and derivatives thereof, are prepared by (a) cyclizing the correspondingly substituted 4-[3-(1-chloro-3(R)-alkyl(or alkenyl)-4-(R)-piperidyl)-1-oxopropyl]quinolines, antipodes or racemates thereof, to the corresponding 4-[5(R)-alkyl(or alkenyl)-4-(S)-quinuclidin-2(S) or 2(R)-ylcarbonyl]quinolines, antipodes or racemates thereof; and (b) stereoselectively reducing the products of step (a) to .sup.a (S)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(R)-yl]-4-quinoline-methanols, antipodes or racemates thereof, and .alpha.(R)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(S)-yl]-4-quinolinemethanols, antipodes or racemates thereof. Various intermediates and the end products are useful antimalarial and antiarrhythmic agents.
    Type: Grant
    Filed: August 20, 1975
    Date of Patent: June 20, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Juerg Albert Walter Gutzwiller, Milan Radoje Uskokovic
  • Dibenz[b,f]oxepin derivatives
    Patent number: 4091023
    Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described, are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
    Type: Grant
    Filed: March 18, 1977
    Date of Patent: May 23, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
  • Thienothiazine derivatives
    Patent number: 4090020
    Abstract: Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,Prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.
    Type: Grant
    Filed: February 9, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dieter Binder, Otto Hromatka, Rudolf Pfister, Paul Zeller
  • Isoindole derivatives
    Patent number: 4090027
    Abstract: Isoindole derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.6, A and Z are as hereinafter described. The isoindole derivatives are useful as appetite suppressants.
    Type: Grant
    Filed: August 25, 1976
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • (+)-(S)-Enantiomer of 3-{2-[4-(8-fluoro-10,11-dihydro-2-methyl-dibenzo[b,f]thiepin-10-yl)-1-pi perazinyl]-ethyl}-2-oxazolidinone
    Patent number: 4089861
    Abstract: (+)-(S)-enantiomer of 3-{2-[4-(8-fluoro-10,11-dihydro-2-methyldibenzo[b,f]thiepin-10-yl)-1-piper azinyl]-ethyl} -2-oxazolidinone, active as a neuroleptic agent, is described.
    Type: Grant
    Filed: May 26, 1976
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Emilio Kyburz
  • Antibacterial compositions
    Patent number: 4089950
    Abstract: Compositions comprising N-sulfanilyl-1-ethylcytosine and a sulfonamide potentiator, which are useful as antibacterial agents, are described.
    Type: Grant
    Filed: May 6, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erika Bohni, Marc Montavon
  • Process and intermediates for isoindole derivatives
    Patent number: 4089875
    Abstract: A process for the preparation of isoindole derivatives which comprises heating a compound of the formula ##STR1## wherein R,R.sub.1,R.sub.2,R.sub.3,R.sub.4 and R.sub.5 are hereinafter set forth, in the presence of a suitable imidazole, is described.
    Type: Grant
    Filed: July 7, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Isoindole derivatives
    Patent number: 4077978
    Abstract: Isoindole derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.6, A and Z are as hereinafter described. The isoindole derivatives are useful as appetite suppressants.
    Type: Grant
    Filed: August 25, 1976
    Date of Patent: March 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin