Patents Represented by Attorney Joseph I. Hirsch
  • Patent number: 3966820
    Abstract: 2-Substituted-5-oxo-5H-dibenzo [a,d]cycloheptenes represented by the following formula: ##SPC1##Where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; the dotted line represents an optional, additional bond between the carbon atoms at the 10- and 11-positions; and the pharmaceutically acceptable esters and ethers thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
    Type: Grant
    Filed: May 30, 1975
    Date of Patent: June 29, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Karl G. Untch
  • Patent number: 3964483
    Abstract: An inhalation device having an elongate housing having one or more passageways for the passage of air therethrough. The passageway, of relatively small diameter, opens into an emptying chamber, of relatively greater diameter, adjacent that end of the housing which is adapted for insertion into the mouth or nose of a user. Adjacent that end of the emptying chamber closest to the passageway(s), the housing has means to hold a medicament-holding container so it is tilted toward the passageway (i.e., away from the output end of the housing). During inhalation, the powdered medicament in the container is entrained in the air stream being inhaled and is carried into the nose, throat, or lungs of the user where beneficial or therapeutic action of the medicament occurs.
    Type: Grant
    Filed: January 13, 1975
    Date of Patent: June 22, 1976
    Assignee: Syntex Puerto Rico, Inc.
    Inventor: Stanley Mathes
  • Patent number: 3965113
    Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SR.sup.5 or --OR.sup.5 ; and R.sup.5 is aryl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
    Type: Grant
    Filed: November 21, 1973
    Date of Patent: June 22, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Colin C. Beard, John A. Edwards, John H. Fried
  • Patent number: 3962437
    Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; and R.sup.1 is a fused, bicyclic heterocyclic ring moiety. The R.sup.1 S-substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
    Type: Grant
    Filed: April 7, 1975
    Date of Patent: June 8, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Colin C. Beard
  • Patent number: 3960936
    Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
    Type: Grant
    Filed: April 25, 1974
    Date of Patent: June 1, 1976
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 3960957
    Abstract: New compounds, 2-(6'-methoxynaphth-2'-yl)propylene oxide, 2-(6'-methoxynaphth-2'-yl)propionaldoxime, 2-hydroxy-2-(6'-methoxynaphth-2'-yl)-propionitrile, 2-(6'methoxynaphth-2'-yl)acrylonitrile, 2-(6'-methoxynaphth-2'-yl)acrylic acid, the corresponding 5'-halo compounds and 2-(5'-halo-6'-methoxynaphth-2'-yl)propionaldehyde are useful intermediates in producing 2-(6'-methoxynaphth-2'-yl)propionic acid and the corresponding 5'-halo acids from 6-methoxy-2-acetylnaphthalene and the corresponding 5-halo compounds. The 2-propionic acids are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. The 2-propionaldehydes, obtained from the 2-acetyl compounds by way of the 2-propylene oxide, can be converted directly to the 2-propionic acids by way of the 2-propionaldoximes and the 2-propionitriles or more directly by Jones oxidation.
    Type: Grant
    Filed: January 10, 1975
    Date of Patent: June 1, 1976
    Assignee: Syntex Corporation
    Inventor: Francisco Sanchez Alvarez
  • Patent number: 3958012
    Abstract: The d 2-(6-substituted-2-naphthyl)propanals of this invention are prepared by oxidizing the corresponding 2-(6-substituted-2-naphthyl)-1-propanols or by reducing d 2-(6-substituted-2-naphthyl)propionic acids, the 6-substituent being a methyl, ethyl, isopropyl, cyclopropyl, trifluoromethyl, vinyl, ethynyl, fluoro, chloro, methoxy, methoxymethyloxy, difluoromethoxy, methylthio, methoxymethylthio or difluoromethylthio group. The products have anti-inflammatory, analgesic and antipyretic activities.
    Type: Grant
    Filed: March 27, 1975
    Date of Patent: May 18, 1976
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 3947479
    Abstract: A method for lowering elevated serum lipid concentrations comprising administering a composition containing, as the active ingredient, a 3.beta. -substituted-16.alpha.-cyanopreg-5-en-20-one wherein the substituent at the 3.beta.-position is selected from the group consisting of hydroxy, alkoxy having 1 to 6 carbon atoms, cycloalkoxy having 3 to 6 carbon atoms, acyloxy wherein the acyl moiety has 2 to 7 carbon atoms, tetrahydrofuran-2'-yloxy, tetrahydropyran-2'-yloxy, and 4'-alkoxytetrahydropyran-4'-yloxy where the alkoxy moiety has 1 to 6 carbon atoms. Representative active ingredients are 3.beta.-acetoxy-16.alpha.-cyanopreg-5-en-20-one and 3.beta.-cyclopentyloxy-16.alpha.-cyanopregn-5-en-20-one. These representative agents are also useful in the therapeutic method of protecting and regenerating damaged hepatic tissue.
    Type: Grant
    Filed: November 21, 1973
    Date of Patent: March 30, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Wendell H. Rooks, II
  • Patent number: 3947472
    Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
    Type: Grant
    Filed: July 29, 1974
    Date of Patent: March 30, 1976
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 3942641
    Abstract: This invention relates to a method of fertility control by use of novel cyclic progestogen-interrupted estrogen oral contraceptive regimens. Considering the first day of menstrual flow as day one of a 28 day medication administration cycle, a combined formulation of estrogen and progestogen substances is administered on the 3rd, 4th, 5th or 6th day of the cycle and every second or third day thereafter through, and including, the 23rd, 24th, 25th, 26th, 27th or 28th day of the cycle, and a formulation having only a progestogen substance as the active component is administered on the 4th, 5th, 6th, or 7th day of the cycle and every day thereafter on which a combination formulation is not administered, through, and including, the 22nd, 23rd, 24th, 25th, 26th, 27th or 28th day of the cycle.
    Type: Grant
    Filed: March 24, 1975
    Date of Patent: March 9, 1976
    Assignee: Syntex Corporation
    Inventor: Eugene J. Segre
  • Patent number: 3938516
    Abstract: An inhalation device having an elongate housing having one or more passageways for the passage of air therethrough. Each passageway, of relatively small diameter, opens into an emptying chamber, of relatively greater diameter, adjacent that end of the housing which is adapted for insertion into the mouth or nose of a user. Adjacent that end of the emptying chamber closest to the passageway(s), the housing has means for receiving or presenting a unit dose of powdered medicament for administration. During inhalation, the air stream passing over and directed into the powdered medicament holder entrains the powdered medicament which is then carried into the nose, throat or lungs of the user where beneficial or therapeutic action of the medicament occurs.
    Type: Grant
    Filed: January 13, 1975
    Date of Patent: February 17, 1976
    Assignee: Syntex Puerto Rico, Inc.
    Inventor: Stanley Mathes
  • Patent number: 3936528
    Abstract: This application describes analgesic formulations including d 2-(6-methoxy-2-naphthyl)propionic acid, or a pharmaceutically acceptable salt or ester thereof, in combination with at least one central nervous system active analgesic compound. Analgesic activity of the combination is greater than that obtained with either of the components alone, thus demonstrating enhanced analgesia which can be obtained therewith.
    Type: Grant
    Filed: February 13, 1974
    Date of Patent: February 3, 1976
    Assignee: Syntex Corporation
    Inventor: Martin Katz
  • Patent number: 3935273
    Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
    Type: Grant
    Filed: April 25, 1974
    Date of Patent: January 27, 1976
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 3935209
    Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is a heterocyclic ring having 1-4 hetero atoms; and M is O, S, or ##EQU1## The R.sup.1 M-substitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
    Type: Grant
    Filed: February 11, 1974
    Date of Patent: January 27, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Colin C. Beard, John A. Edwards, John H. Fried
  • Patent number: 3932635
    Abstract: This invention relates to a method of fertility control by use of novel cyclic progestogen-interrupted estrogen oral contraceptive regimens. Considering the first day of menstrual flow as day one of a 28 day medication administration cycle, a combined formulation of estrogen and progestogen substances is administered on the 3rd, 4th, 5th or 6th day of the cycle and every second or third day thereafter through, and including, the 23rd, 24th, 25th, 26th, 27th or 28th day of the cycle, and a formulation having only a progestogen substance as the active component is administered on the 4th, 5th, 6th, or 7th day of the cycle and every day thereafter on which a combination formulation is not administered, through, and including, the 22nd, 23rd, 24th, 25th, 26th, 27th or 28th day of the cycle.
    Type: Grant
    Filed: May 5, 1972
    Date of Patent: January 13, 1976
    Assignee: Syntex Corporation
    Inventor: Eugene J. Segre