Plural Ring Chalcogens In The Hetero Ring Patents (Class 514/360)
  • Patent number: 5238950
    Abstract: A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed.Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: August 24, 1993
    Assignee: Schering Corporation
    Inventors: John W. Clader, Harry R. Davis, Deborra Mullins, Stuart Rosenblum, Jay Weinstein
  • Patent number: 5156665
    Abstract: A synergistic antimicrobial composition comprising 2-alkyl-3-isothiazolones, preferably 4,5-dichloro-2-n-octyl-3-isothiazolone or 2-n-octyl-3-isothiazolone, and certain iodopropargyl compounds, in a ratio to each other which exhibits synergism is disclosed.
    Type: Grant
    Filed: January 3, 1991
    Date of Patent: October 20, 1992
    Assignee: Rohm and Haas Company
    Inventors: Samuel E. Sherba, Raj J. Mehta
  • Patent number: 5140018
    Abstract: Novel 1,3,2-benzodithiazole-1-oxides of formula (I) ##STR1## and their pharmaceutically acceptable salts are disclosed, wherein R.sup.1 is a substituent on the 4-, 5-, 6- or 7-position of the benzodithiazole nucleus selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl, halogen, halo(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, and nitro; andR.sup.2 is selected from the group consisting of (C.sub.1 -C.sub.12)alkyl; substituted (C.sub.1 -C.sub.12)alkyl; (C.sub.2 -C.sub.16)alkenyl; (C.sub.2 -C.sub.16)alkynyl; (C.sub.3 -C.sub.10)cycloalkyl; (C.sub.6 -C.sub.10)aryl; mono- or di-substituted (C.sub.6 -C.sub.10)aryl; (C.sub.6 -C.sub.10)aryl-(C.sub.1 -C.sub.4)alkyl; mono- or di-substituted (C.sub.6 -C.sub.10)aryl-(C.sub.1 -C.sub.4)alkyl; heterocycle-(C.sub.1 -C.sub.4)alkyl; and mono- or di-substituted heterocycle-(C.sub.1 -C.sub.4)alkyl.Also disclosed are the antifungal use and method of preparation of such compounds, as well as their formulation as pharmaceutical compositions.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: August 18, 1992
    Assignee: Abbott Laboratories
    Inventors: Larry L. Klein, Clinton M. Yeung
  • Patent number: 5106861
    Abstract: This invention relates to novel derivatives of tetralin, to the processes for their preparation, to their use as amino-peptidase inhibitors and to their end-use application as immunomodulators and as analgesic agents.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: April 21, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Hugues d'Orchymont, Celine Tarnus
  • Patent number: 5087631
    Abstract: The present invention relates to the compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.5-8 cycloalkyl, aryl-C.sub.1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, amino or C.sub.1-4 alkyl mono or disubstituted amino, pharmaceutical formulations containing these compounds and their use as vasodilators in the treatment of cardiovascular disorders.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: February 11, 1992
    Assignee: Glaxo Inc.
    Inventors: Joel E. Shaffer, Stephen A. Thomson
  • Patent number: 5034392
    Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.5 and R.sub.6 taken together with the nitrogen atom to which they are attached are ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, amino, cyano, trifluoromethyl or methoxy; and m is 0, 1 or 2; the pharmaceutically acceptable acid addition salts thereof and where applicable the optical and geometrical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesic and antihypertensive agents.
    Type: Grant
    Filed: April 16, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Nicholas J. Hrib
  • Patent number: 5010092
    Abstract: Drug treatment therapies and kits for use therewith are disclosed. They involve the use of methimazole and/or its pro-drug carbimazole to reduce nephrotoxic effects of chemical exposure. In one embodiment, a patient receives cisplatin and then is treated with methimazole. The time delay in providing methimazole prevents the methimazole from being substantially expelled by the kidney prior to cisplatin reaching the kidney.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: April 23, 1991
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Adnan A. Elfarra
  • Patent number: 5001115
    Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: March 19, 1991
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4970224
    Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: November 13, 1990
    Assignee: Rohm and Haas Company
    Inventors: Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
  • Patent number: 4910019
    Abstract: The compounds: ##STR1## in which the dotted line represents optional unsaturation; R.sup.1 is hydrogen, halo or alkoxy; R.sup.2 is hydrogen or alkoxy and X is methylene, ethylene, ethylidene, 1,2-propylene or propylene; or a biologically acceptable salt thereof are growth promoting agents which rapidly lead to increased lean body mass in domestic animals and humans.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: March 20, 1990
    Assignee: American Home Products Corporation
    Inventor: Michael L. McCaleb
  • Patent number: 4897405
    Abstract: This invention relates to novel [(substituted naphthalenyl)alkyl]-3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: January 30, 1990
    Assignee: American Home Products Corporation
    Inventors: Thomas R. Alessi, Terence M. Dolak, John W. Ellingboe, Louis J. Lombardo
  • Patent number: 4895862
    Abstract: This invention relates to novel benzyl-3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: January 23, 1990
    Assignee: American Home Products Corp.
    Inventors: Thomas R. Alessi, Terence M. Dolak
  • Patent number: 4895860
    Abstract: This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: January 23, 1990
    Assignee: American Home Products Corporation
    Inventors: Thomas R. Alessi, John W. Ellingboe
  • Patent number: 4895861
    Abstract: This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: January 23, 1990
    Assignee: American Home Products Corporation
    Inventors: Louis J. Lombardo, Thomas R. Alessi
  • Patent number: 4742060
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: May 3, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4737507
    Abstract: The invention provides a method of combating a microorganism which comprises allowing a heterocyclic pentalene derivative of general formula I ##STR1## wherein X represents an oxygen atom, a sulphur atom or an --SO-- moiety; Y represents a sulphur, selenium or tellurium atom, provided that when Y represents a selenium or tellurium atom X is an oxygen atom; and R.sup.1 and R.sup.2 together represent a --CH.sub.2 --C(CH.sub.3).sub.2 --CCl(CONH.sub.2)-- or --CH.sub.2 --A--CH.sub.2 -- linkage where A is a --CH.sub.2 --, --CH(CH.sub.3)-- or --S(O).sub.n -- moiety, where n is 0, 1 or 2; provided that when X is an oxygen atom and Y is a sulphur atom R.sup.1 and R.sup.2 together represent a --CH.sub.2 --S(O).sub.n --CH.sub.2 -- linkage and when X is an --SO-- moiety and A is a S(O).sub.n --, n is 2; to act on the microorganism or its environment; and such derivatives for use as a therapeutic substance.
    Type: Grant
    Filed: July 9, 1986
    Date of Patent: April 12, 1988
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventors: Susan J. Turner, Michael T. Clark
  • Patent number: 4562185
    Abstract: The present invention relates to combating pests with five-membered nitrogen-containing heterocyclic compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in the description. Many of the compounds are new.
    Type: Grant
    Filed: March 15, 1984
    Date of Patent: December 31, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Jager, Rudolf Fauss, Kurt Findeisen, Benedikt Becker, Bernhard Homeyer