Patents by Inventor Harold Zinnes

Harold Zinnes has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5919780
    Abstract: Compounds of formula I ##STR1## wherein X is N or C--R.sup.9, Y is N--R.sup.10, CH.sub.2, O, S, SO, SO.sub.2, C.dbd.O or CH--OH,R is H or alkyl,R.sup.1 is heteroaryl,n is 1-5, andR.sup.2 -R.sup.10 are H or various substituents,are useful as inhibitors of protein farnesyl transferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.
    Type: Grant
    Filed: December 11, 1997
    Date of Patent: July 6, 1999
    Assignee: Warner Lambert Company
    Inventors: Gary L. Bolton, Annette M Doherty, James S. Kaltenbronn, John Quin, III, Jeffrey D. Scholten, Judith Sebolt-Leopold, Harold Zinnes
  • Patent number: 4188482
    Abstract: 3,4-Dihydro-10-[2-(dialkylamino)ethyl]-1-phenyl-1H-thiazino[4,3-a]indol-4-o l compounds having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups. The compounds of this invention exhibit anti-allergy properties and are indicated in the management of allergy.
    Type: Grant
    Filed: May 4, 1978
    Date of Patent: February 12, 1980
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Martin L. Schwartz
  • Patent number: 4154735
    Abstract: 3,3'-Thiodimethylenebis 2-[(dialkylamino)methyl]indole compounds having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups. The compounds of this invention exhibit antifungal and CNS depressant properties and can be used as antifungal agents or CNS depressant agents.
    Type: Grant
    Filed: May 8, 1978
    Date of Patent: May 15, 1979
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Neil A. Lindo
  • Patent number: 4154734
    Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
    Type: Grant
    Filed: December 27, 1977
    Date of Patent: May 15, 1979
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4153711
    Abstract: .beta.-[2-[(DIALKYLAMINO)METHYL]-1H-indol-3-yl]-.alpha.,.alpha.-diphenylpro pionitriles and 4-[[2-[(dialkylamino)methyl]-1H-indol-3-yl]methyl]-2,4-dihydro-5-lower alkyl-2-phenyl-3H-pyrazol-3-ones and acid addition salts thereof which are useful pharmacological agents, especially as central nervous system depressants, are disclosed. The compounds can be produced by reacting an anion of an acetonitrile or a pyrazol-3-one with the appropriate quatenary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.
    Type: Grant
    Filed: December 19, 1977
    Date of Patent: May 8, 1979
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Neil A. Lindo
  • Patent number: 4148922
    Abstract: 3-[2-(Dialkylamino)ethyl]-2-(benzyl)indoles having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups and R.sub.3 is a phenyl, carboalkoxymethyl, lower alkyl or hydroxyethyl group. The compounds of the invention exhibit anti-aggression and anti-secretory properties and are indicated in the management of aggression and gastric hypersecretion.
    Type: Grant
    Filed: May 4, 1978
    Date of Patent: April 10, 1979
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Martin L. Schwartz
  • Patent number: 4140858
    Abstract: N,N-dialkyl-3-[(phenylthio)methyl]-1H-indole-2-methanamines or 3-(1H-imidazol-1-ylmethyl)-N,N,-dimethyl-1H-indole-2-methanamines and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a thiophenols or imidazoles with the appropriate 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.
    Type: Grant
    Filed: December 19, 1977
    Date of Patent: February 20, 1979
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Neil A. Lindo
  • Patent number: 4134897
    Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
    Type: Grant
    Filed: December 27, 1977
    Date of Patent: January 16, 1979
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4134900
    Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-theino[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: January 16, 1979
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4134896
    Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: January 16, 1979
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4134894
    Abstract: Pyrrolo[1,2-a]indole compounds having in free base form the formulas ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are lower alkyl; R.sub.4 is lower alkyl, phenyl, lower alkoxy or ##STR2## in which R.sub.8 and R.sub.9 are hydrogen, lower alkyl, phenyl or benzyl; R.sub.5 is hydrogen or lower alkyl; A is O or NH; and R.sub.6 and R.sub.7 are lower alkyl, phenyl, or carbo(lower)alkoxy.
    Type: Grant
    Filed: May 4, 1978
    Date of Patent: January 16, 1979
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Martin L. Schwartz
  • Patent number: 4132792
    Abstract: Bis(2-[(disubstitutedamino)methyl]-1H-indole) compounds wherein said 2-[(disubstitutedamino)methyl]-1H-indol-3-ylmethylene moieties are linked together through a piperazine or 1,3-dihydro-2H-indol-2-one fragment and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a piperazine or 1,3-dihydro-2H-indole-2-one compound with the appropriate quaternary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo-[3,4-b]indole.
    Type: Grant
    Filed: December 19, 1977
    Date of Patent: January 2, 1979
    Assignee: Warner-Lambert
    Inventors: Harold Zinnes, Neil A. Lindo
  • Patent number: 4127585
    Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
    Type: Grant
    Filed: December 27, 1977
    Date of Patent: November 28, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4116964
    Abstract: A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediates in the preparation of known anti-inflammatory agents.
    Type: Grant
    Filed: August 16, 1977
    Date of Patent: September 26, 1978
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Neil A. Lindo, John Shavel, Jr.
  • Patent number: 4098794
    Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
    Type: Grant
    Filed: December 7, 1977
    Date of Patent: July 4, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4097441
    Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno?2,3-b!thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
    Type: Grant
    Filed: December 7, 1977
    Date of Patent: June 27, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4092325
    Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
    Type: Grant
    Filed: December 10, 1976
    Date of Patent: May 30, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4082757
    Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
    Type: Grant
    Filed: December 10, 1976
    Date of Patent: April 4, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4076722
    Abstract: This invention relates to a process for the preparation of 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (III), a novel intermediate useful in the preparation of the known anti-inflammatory agent, 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (IV). According to the process of this invention, the saccharin compound, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (I) is reacted with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures below 30.degree. C. to form the benzenesulfonylglycineamide, alkyl 2-{[({[(5-methyl-3-isoxazolyl)amino]carbonyl}methyl)amino]sulfonyl}benzoat e (II), which is ring closed and rearranged by reaction with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures of from 60.degree. to 70.degree. C. to form the desired oxadiazole compound III.
    Type: Grant
    Filed: February 10, 1976
    Date of Patent: February 28, 1978
    Assignee: Warner-Lambert Company
    Inventors: Arthur C. Fabian, Jerome D. Genzer, Charles Francis Kasulanis, John Shavel, Jr., Harold Zinnes
  • Patent number: RE29836
    Abstract: Compounds having the following structural formula are disclosed: ##STR1## wherein R.sub.1 is hydrogen or methyl and R.sub.2, and R.sub.3 are hydrogen or alkyl. These compounds are useful as anti-inflammatory agents, antipyretics, analgesics.
    Type: Grant
    Filed: October 11, 1977
    Date of Patent: November 14, 1978
    Assignee: Warner-Lambert Company
    Inventors: Harold Zinnes, Martin L. Schwartz, John Shavel, Jr.