Patents Examined by F. Bernhardt
  • Patent number: 5217973
    Abstract: The present invention relates to the derivatives of formula: ##STR1## as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: June 8, 1993
    Assignee: Laboratoires UPSA
    Inventors: Nicole Bru-Magniez, Eric Nicolai, Jean-Marie Teulon
  • Patent number: 5185352
    Abstract: The invention concerns new derivatives of certain alkoxy -4(1H)-pyridones, processes for preparing them, and pharmaceutical compositions containing them. The compounds of the invention are useful in the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arteriosclerosis and hypertension, and of inflammatory processes, allergies, cancers, and certain degenerative damage of the central nervous system.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: February 9, 1993
    Assignee: Goedecke Aktiengesellschaft
    Inventors: Julian Aranda, Johannes Hartenstein, Reinhard Reck, Christopher Schachtele, Claus Rudolph, Hartmut Osswald, Gunter Weinheimer
  • Patent number: 5185446
    Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein n is 0,1 or 2 and X is --N.dbd.C--R.sub.9 or NR.sub.10 --C.dbd.Twhere R.sub.1, R.sub.2, R.sub.3, and R.sub.9 and R.sub.10 and X, Y, W and T are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdoes with benzodiazepine type drugs, and enhancement of alertness.
    Type: Grant
    Filed: September 4, 1990
    Date of Patent: February 9, 1993
    Assignee: Neurogen Corporation
    Inventors: Kenneth Shaw, Alan J. Hutchison
  • Patent number: 5175294
    Abstract: New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.
    Type: Grant
    Filed: August 5, 1991
    Date of Patent: December 29, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Wierzbicki, Frederic Sauveur, Jacqueline Bonnet, Martine Brisset, Charles Tordjman
  • Patent number: 5166155
    Abstract: 1-carboxyalkylquinoxaline-2,3(1H,4H)-dione compounds or tautomeric forms thereof of the formula ##STR1## wherein R represents hydrogen, C.sub.1-6 -alkyl, including branched chains, or aralkyl and n represents the number from 0 to 5;R.sup.4 represents hydrogen or hydroxy;R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen, nitro, halogen, alkoxy, aryloxy, aralkoxy, C.sub.1-6 -alkyl including branched chains, or aryl;R.sup.9 represents hydrogen, lower alkyl, or aryl;R.sup.10 represents hydrogen, or alkyl.The compounds are useful in the treatment of neurological and psychiatric diseases.
    Type: Grant
    Filed: March 12, 1991
    Date of Patent: November 24, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Anker S. Jorgensen, Carsten E. Stidsen, Peter Faarup, Frederik S. Gronvald
  • Patent number: 5158953
    Abstract: The present invention provides a novel series of 2-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-ones (-thiones) compounds. These compounds are found useful as an active ingredient for the prophylaxis and treatment of hypertension.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: October 27, 1992
    Assignee: National Science Council
    Inventors: Ji-wang Chern, Chia-Yang Shiau, Mao-Hsiung Yen, Guan-Yu Lu
  • Patent number: 5126353
    Abstract: Novel enantiomeric and diasteroisomeric forms of tetrahydropyridines of the formula ##STR1## wherein n.sub.1 is 0 or 2, A is selected from the group consisting of --(CH.sub.2).sub.n2 -- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms and n.sub.2 is 0 to 5, Z is selected from the group consisting of phenyl, naphthyl, indenyl, heteromonocycle of 5 to 6 ring members and heterobicycle, each optionally substituted with at least one substituent and their non-toxic, pharmaceutically acceptable acid addition salts and quarternary ammonium salts having central analgesic properties as well as diuretic, anti-arrhythmic, anti-cerebral-ischemia and hypotensive properties.
    Type: Grant
    Filed: March 6, 1990
    Date of Patent: June 30, 1992
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Daniel Frechet, Michel Fortin
  • Patent number: 5126340
    Abstract: Novel compounds of the formula ##STR1## wherein n is an integer from 1 to 4 inclusive; R.sub.1 represents a mono- or disubstituent of hydrogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy (C.sub.1 -C.sub.3), halogen, nitro or trifluoromethyl; R.sub.2 is cyano, carboxamido, ethyl carboxylate or halogen; R.sub.3 is hydrogen, straight or branched chain lower alkyl (C.sub.1 -C.sub.3), alkenyl (C.sub.2 -C.sub.3), alkynyl(C.sub.2 -C.sub.3), cycloalkyl(C.sub.3 -C.sub.6), hydroxyalkyl(C.sub.1 -C.sub.3), dimethylaminoalkyl(C.sub.1 -C.sub.3), ethylcarboxylate, alkyl(C.sub.1 -C.sub.13)carbonyl, 1-(methylethyl)acetamide, cyclohexylethyl, phenyl, mono- or disubstituted phenyl (wherein the phenyl substituent is halogen, trifluoromethyl, lower alkyl(C.sub.1 -C.sub.3) or lower alkoxy (C.sub.1 -C.sub.3)), benzyl, mono- or disubstituted benzyl (wherein the benzyl substituent is halogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.
    Type: Grant
    Filed: August 10, 1990
    Date of Patent: June 30, 1992
    Assignee: American Cyanamid Company
    Inventors: Shin S. Tseng, Herbert J. Brabander, Joseph W. Epstein
  • Patent number: 5116970
    Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: May 26, 1992
    Inventors: James S. New, William J. Christopher
  • Patent number: 5114464
    Abstract: Herbicidal methods utilizing compounds having the structure ##STR1## wherein: n is 0, 1, 2, or 3;R is H or alkyl; andR.sup.1 is halogen, nitro, methyl, halomethyl, methoxy, halomethoxy or ethoxyare disclosed which control the growth of undesirable weeds but are substantially innocuous to corn. Herbicidal compositions comprising the compounds and a carrier are also disclosed.
    Type: Grant
    Filed: September 27, 1990
    Date of Patent: May 19, 1992
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Robert G. Davis, Allyn R. Bell
  • Patent number: 5086186
    Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with trichloracetyl isocyanate to produce novel N-trichloroacetyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as analgesic and antiinflammatory agents and/or intermediates for such agents.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: February 4, 1992
    Assignee: Pfizer Inc.
    Inventor: Sarah E. Kelly
  • Patent number: 5071994
    Abstract: 2-aryl-4-halomethyl-4-isoxazolin-3-1-derivatives of formula (I), useful as intermediates for positive working compounds in silver halide photographic materials ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl having from 1 to 6 carbon atoms or a substituted or unsubstituted aryl having from 6 to 24 carbon atoms; R.sup.2, R.sup.3, and R.sup.4, are the same or different, each having up to 20 carbon atoms and each represents hydrogen, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aryloxy, a substituted or unsubstituted acyl, a substituted or unsubstituted alkoxycarbonyl, a substituted or unsubstituted aryloxycarbonyl, halogen, nitro, a substituted or unsubstituted carbamoyl, a substituted or unsubstituted sulfamoyl, a substituted or unsubstituted sulfonyl, cyano, trifluoromethyl, or carboxyl, with the proviso that at least one of said R.sup.2 and R.sup.
    Type: Grant
    Filed: January 23, 1991
    Date of Patent: December 10, 1991
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Koki Nakamura, Shigeru Nakamura
  • Patent number: 5030733
    Abstract: Novel hydroxy-, alkoxy- and benzyloxy-substituted phospholipids, a process for the preparation thereof, and methods for treating pain, phospholipase, A.sub.2 mediated inflammation and similar conditions utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: July 9, 1991
    Assignee: Hoechst-Roussel Pharmaceticals Incorporated
    Inventors: John J. Tegeler, Kirk D. Shoger
  • Patent number: 5026704
    Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substututed by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, Cl or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 - alkyl; orR.sup.7 and R.sup.
    Type: Grant
    Filed: December 26, 1989
    Date of Patent: June 25, 1991
    Assignee: Novo Nordisk A/S
    Inventors: Tage Honore, Poul Jacobsen, Flemming E. Nielsen, Lars Naerum
  • Patent number: 5010078
    Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 14, 1990
    Date of Patent: April 23, 1991
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
  • Patent number: 5010079
    Abstract: An indolone derivative is useful for the treatment of anxiety, depression and schizophrenia and is a 5HT.sub.1A agonist and 5HT.sub.2 antagonist, which is a compound of formula (I): ##STR1## in which R.sub.1 is a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical,R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical,R.sub.3 is a hydrogen atom, a (C.sub.1-4)alkyl radical or an S-(C.sub.1-4) alkyl radical; andR.sub.4 is a phenyl, chlorophenyl, naphthyl, 7-methoxy-1-naphthyl, 6-methoxy-1-indanyl, 2-methoxy-6-pyridyl, 3-methoxy-2-pyridyl, isoquinolyl, 7-methoxy-1-isoquinolyl, 7-methoxy-1,2,3,4-tetrahydro-1-naphthyl or 7-fluoro-1-naphthyl radical;or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: April 23, 1991
    Assignee: Synthelabo
    Inventors: Philippe Manoury, Jean Binet, Daniel Obitz, Gerard Defosse, Elisabeth Dewitte, Corinne Veronique
  • Patent number: 5000880
    Abstract: Glycero-phosphatidylcholine is acylated with a higher fatty acid anhydride in the presence of a special organic solvent in the absence of a catalyst.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: March 19, 1991
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Masami Ishihara, Hiroyoshi Nawa, Tsutomu Miyagawa
  • Patent number: 5001124
    Abstract: This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, -SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W where W is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 2, 1990
    Date of Patent: March 19, 1991
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, Bruce H. Devens
  • Patent number: 4997940
    Abstract: Novel compounds, e.g. 3-cyano-5,7-dimethyl-N-(2,6-dichlorophenyl)pyrazolo[1,5-a]pyrimidine-2-sul fonamide and their use as herbicides and/or for the suppression of nitrification of ammonium nitrogen in soil.
    Type: Grant
    Filed: July 27, 1988
    Date of Patent: March 5, 1991
    Assignee: The Dow Chemical Company
    Inventors: Anna P. Vinogradoff, William A. Kleschick
  • Patent number: 4994464
    Abstract: Certain piperazinylpyrimidines have pronounced .beta.-adrenergic blocking properties and some of the compounds are particularly useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: October 5, 1989
    Date of Patent: February 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Tolman, John J. Baldwin, Arthur F. Wagner, Adolph Pietruszkiewicz