Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/256)
  • Patent number: 4861881
    Abstract: The polyglycidamides are epoxy derivatives of cyclic ureas such as glycouril and aminotriazines such as melamine and guanamines. They are prepared from cyclic ureas and aminotriazines by methylolating with formaldehyde, etherifying with an alcohol, transetheramidizing with acrylamide and epoxidizing with hydrogen peroxide. They are used with polyamines and other epoxy reactive oligomers to provide crosslinkable coating systems which possess solvent, chemical and water resistance and UV stability.
    Type: Grant
    Filed: May 2, 1984
    Date of Patent: August 29, 1989
    Assignee: Monsanto Company
    Inventor: William F. Pfohl
  • Patent number: 4845081
    Abstract: N-methylamino derivatives of biologically active substances which have enhanced delivery across topical membranes and pharmaceutical compositions adapted for topical administration containing same.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: July 4, 1989
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4838925
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: June 13, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4735957
    Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.
    Type: Grant
    Filed: November 18, 1986
    Date of Patent: April 5, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi
  • Patent number: 4714698
    Abstract: The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: December 22, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Josef Roch, Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Rainer Zimmermann, Johannes Weisenberger
  • Patent number: 4659824
    Abstract: A process for the selective production of defined, partial reaction products of polyfunctional N-glycidyl compounds with hydrohalic acids, pseudohydrohalic acids or acids of phosphorus; mono- or di-ring opening products are obtainable as required. The process is carried out at a pH of from about 2 to 10 which is kept constant within a band of at most 2 units on the pH-scale. N,N'-diglycidyl-N"-(halohydroxypropyl)-urazoles and N-glycidyl-N,N"-bis(halohydroxypropyl) urazoles having pharmaceutical utility are produced in good yield.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: April 21, 1987
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventor: Hinrich Moller
  • Patent number: 4649146
    Abstract: The invention relates to novel pharmaceutical compounds for treatment for ulcer of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl or hydroxyiminomethyl,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino or guanidino optionally substituted with dimethylaminomethylene,R.sup.3 is dihydroisoquinolyl which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino or guanidino,Q is --CO--, andn is an integer of 0 or 1, andpharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 27, 1984
    Date of Patent: March 10, 1987
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi
  • Patent number: 4636457
    Abstract: Direct positive photographic elements are disclosed employing internal latent image silver halide emulsions associated with developer autoxidation promoter agents constituted by 5 or 6 membered nucleus-containing heterocyclic compounds comprising an azomethine group, whose methine group is substituted with a 5-amino-1,2,4-triazolyl group, and/or copper complex compounds thereof.Preferably said direct positive photographic elements are multi-layer elements comprising internal latent image type type silver halide emulsion layers sensitized to different regions of the visible light and associated with image-dye providing compounds (photographic color couplers).
    Type: Grant
    Filed: July 15, 1985
    Date of Patent: January 13, 1987
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Luigi Valbusa, Enzo Coraluppi, Andrea Quaglia, Mario Tavella
  • Patent number: 4614800
    Abstract: A new one-step synthesis of cyclic 1,3 dinitramines is disclosed. This syesis utilizes a solution of N.sub.2 O.sub.5 in 100% nitric acid as the nitrolyzing media. The polynitramines thus produced find utility as explosive and propellant ingredients, gas generants and in other ordnance applications.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: September 30, 1986
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Rodney L. Willer, Ronald L. Atkins
  • Patent number: 4603203
    Abstract: Novel 3-aminopyrazolo[3,4-d]pyrimidine derivatives represented by the general formula (I) ##STR1## wherein R.sub.1 and R.sub.2 each represents an aliphatic hydrocarbon group; R.sub.3 and R.sub.4 each represents hydrogen, alkyl or acyl; R.sub.5 is alkyl, alkoxycarbonyl or formyl; and the dotted line designates the presence of two double bonds on the pyrazole ring, to which R.sub.5 is linked at either the 1- or 2-position and their salts, are useful for antiinflammatory, analgesic and antipyretic agents.
    Type: Grant
    Filed: December 5, 1984
    Date of Patent: July 29, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiyasu Furukawa, Yoshitaka Maki
  • Patent number: 4591375
    Abstract: A process for the preparation of neutralized, clear, stable solutions by acid catalyzed reaction of urea and aldehydes where the aldehydes are either acetaldehyde or mixtures of not more than 3 moles of propionaldehyde to 1 mole of acetaldehyde, at reaction pH's of from about 3.1 to 4.5 at temperatures from about 30.degree. C. to 75.degree. C. and the mole ratio of urea to aldehydes is about 1.3:1 to 2.5:1. The products of the process are useful as sprayable sources of nitrogen which are non phytotoxic and have prolonged fertilizer activity.
    Type: Grant
    Filed: September 30, 1985
    Date of Patent: May 27, 1986
    Assignee: W. A. Cleary Chemical Corporation
    Inventor: Paul Sartoretto
  • Patent number: 4478833
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted alkyl;R.sub.2 is hydrogen or optionally substituted alkyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form an optionally substituted cyclic imino group;R.sub.3 is an optionally substituted cyclic imino group; andR.sub.4 is substituted hydroxyl, mercapto or amino;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
    Type: Grant
    Filed: December 16, 1981
    Date of Patent: October 23, 1984
    Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter Haftung
    Inventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
  • Patent number: 4460590
    Abstract: Diclycidyl substituted heterocyclic compounds of the formula: ##STR1## wherein X and Y can be the same or different and are either nitrogen or the radical C-R, where R is a hydrogen, or a hydrocarbon group, e.g., a straight or branched chain saturated or unsaturated hydrocarbon group, a substituted or unsubstituted cycloaliphatic group, an aromatic hydrocarbon-substituted alkyl group, a cycloaliphatic hydrocarbon-substituted alkyl group, an aromatic hydrocarbon group, a heterocyclic group, or a hetero-cyclic-substituted alkyl group, and where the glycidyl group in the five-membered ring is attached to a ring nitrogen atom; processes for their preparation; and compositions and methods for their use as cytostatic agents.
    Type: Grant
    Filed: June 23, 1982
    Date of Patent: July 17, 1984
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventor: Hinrich Moller
  • Patent number: 4329459
    Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: May 11, 1982
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4323679
    Abstract: The present invention provides pyrimido(4,5-c)pyridazines, to methods for preparing them, formulations containing them and the preparation of such formulation and the use of such compounds in human therapy. These pyrimido(4,5-c)pyridazines of this invention are useful due to their activity as inhibitors of dihydropteroic and biosynthesis.
    Type: Grant
    Filed: May 27, 1980
    Date of Patent: April 6, 1982
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4315932
    Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.
    Type: Grant
    Filed: September 17, 1979
    Date of Patent: February 16, 1982
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4303790
    Abstract: The present invention provides pyrimido(4,5-c)pyridazines, to methods for preparing them, formulations containing them and the preparation of such formulation and the use of such compounds in human therapy. These pyrimido(4,5-c)pyridazines of this invention are useful due to their activity as inhibitors of dihydropteroic and biosynthesis.
    Type: Grant
    Filed: May 27, 1980
    Date of Patent: December 1, 1981
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4288365
    Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.
    Type: Grant
    Filed: September 17, 1979
    Date of Patent: September 8, 1981
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4269980
    Abstract: This disclosure describes novel 5-, 7-, and 8-(substituted-phenyl)-1,2,4-triazolo[4,3-c]pyrimidines and 5-, 7-, and 8-(substituted-phenyl)-1,2,4-triazolo[1,5-c]pyrimidines and their use as anxiolytic agents.
    Type: Grant
    Filed: December 17, 1979
    Date of Patent: May 26, 1981
    Assignee: American Cyanamid Company
    Inventors: Robert A. Hardy, Jr., Jannie S. Baker, Nicanor Q. Quinones
  • Patent number: 4260758
    Abstract: Novel compounds of the general formula (XIX) ##STR1## where R.sup.9 is selected from lower alkyl, phenyl, phenyl substituted by one or more hydroxy or lower alkoxy, or pyridyl, are disclosed.A method of making the compounds of Formula (XIX) is disclosed, which comprises heating in aqueous acid a compound of formula (XX) ##STR2## wherein R.sup.10 is selected from lower alkyl, phenyl, phenyl substituted by one or more hyroxy or lower alkoxy or pyridyl and R.sup.11 is selected from lower alkyl, phenyl, substituted by one or more hydroxy or lower alkoxy, pyridyl or --CO.sub.2 R where R is lower alkyl.
    Type: Grant
    Filed: September 17, 1979
    Date of Patent: April 7, 1981
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4252946
    Abstract: 8-Substituted pyrido[2,3-d]pyrimidines having activity against microorganisms which utilize de novo synthesis of riboflavin.
    Type: Grant
    Filed: March 30, 1978
    Date of Patent: February 24, 1981
    Assignee: Burroughs Wellcome Co.
    Inventors: Hamish C. S. Wood, Thomas Paterson
  • Patent number: 4237289
    Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.
    Type: Grant
    Filed: September 17, 1979
    Date of Patent: December 2, 1980
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4235905
    Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.
    Type: Grant
    Filed: September 17, 1979
    Date of Patent: November 25, 1980
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert W. Morrison, Jr., William R. Mallory, Virgil L. Styles
  • Patent number: 4174442
    Abstract: Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.
    Type: Grant
    Filed: February 3, 1978
    Date of Patent: November 13, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter C. Wade, Thomas P. Kissick
  • Patent number: 4139364
    Abstract: Triazolone herbicides of the formula: ##STR1## where V is hydrogen, fluorine, chlorine, bromine, methyl or OR where R is alkyl of 1-4 carbon atoms;X is hydrogen, fluorine, chlorine, bromine, cyano, methyl, methoxy, or nitro;Y is hydrogen, fluorine, chlorine, bromine, or methyl;N, m is 0, 1, 2, 3 or 4;Q is oxygen or sulfur;Z is oxygen, S(O).sub.p or NR';p is 0, 1 or 2 andR' is alkyl of 1-3 carbon atomsWith the provisos that(1) n + m = 2, 3, or 4; and(2) if n + m = 2 or 4 then Y, X .noteq. Hand when Z is S(O).sub.p, n is 1, 2, 3 or 4.
    Type: Grant
    Filed: August 9, 1977
    Date of Patent: February 13, 1979
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anthony D. Wolf
  • Patent number: 4113867
    Abstract: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.
    Type: Grant
    Filed: November 15, 1976
    Date of Patent: September 12, 1978
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Seubert, Herbert Thomas, Peter Andrews