Patents Examined by F. Bernhardt
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Patent number: 5217973Abstract: 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: GrantFiled: August 7, 1991Date of Patent: June 8, 1993Assignee: Laboratoires UPSAInventors: Nicole Bru-Magniez, Eric Nicolai, Jean-Marie Teulon
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Patent number: 5185352Abstract: 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: GrantFiled: January 28, 1991Date of Patent: February 9, 1993Assignee: Goedecke AktiengesellschaftInventors: Julian Aranda, Johannes Hartenstein, Reinhard Reck, Christopher Schachtele, Claus Rudolph, Hartmut Osswald, Gunter Weinheimer
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Patent number: 5185446Abstract: 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: GrantFiled: September 4, 1990Date of Patent: February 9, 1993Assignee: Neurogen CorporationInventors: Kenneth Shaw, Alan J. Hutchison
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Patent number: 5175294Abstract: 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: GrantFiled: August 5, 1991Date of Patent: December 29, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Frederic Sauveur, Jacqueline Bonnet, Martine Brisset, Charles Tordjman
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Patent number: 5166155Abstract: 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: GrantFiled: March 12, 1991Date of Patent: November 24, 1992Assignee: Novo Nordisk A/SInventors: Anker S. Jorgensen, Carsten E. Stidsen, Peter Faarup, Frederik S. Gronvald
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Patent number: 5158953Abstract: 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: GrantFiled: August 13, 1991Date of Patent: October 27, 1992Assignee: National Science CouncilInventors: Ji-wang Chern, Chia-Yang Shiau, Mao-Hsiung Yen, Guan-Yu Lu
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Patent number: 5126353Abstract: 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: GrantFiled: March 6, 1990Date of Patent: June 30, 1992Assignee: Roussel UclafInventors: Francois Clemence, Daniel Frechet, Michel Fortin
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Patent number: 5126340Abstract: 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: GrantFiled: August 10, 1990Date of Patent: June 30, 1992Assignee: American Cyanamid CompanyInventors: Shin S. Tseng, Herbert J. Brabander, Joseph W. Epstein
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Patent number: 5116970Abstract: 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: GrantFiled: December 20, 1990Date of Patent: May 26, 1992Inventors: James S. New, William J. Christopher
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Patent number: 5114464Abstract: 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: GrantFiled: September 27, 1990Date of Patent: May 19, 1992Assignee: Uniroyal Chemical Company, Inc.Inventors: Robert G. Davis, Allyn R. Bell
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Patent number: 5086186Abstract: 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: GrantFiled: May 31, 1990Date of Patent: February 4, 1992Assignee: Pfizer Inc.Inventor: Sarah E. Kelly
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Patent number: 5071994Abstract: 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: GrantFiled: January 23, 1991Date of Patent: December 10, 1991Assignee: Fuji Photo Film Co., Ltd.Inventors: Koki Nakamura, Shigeru Nakamura
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Patent number: 5030733Abstract: 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: GrantFiled: June 15, 1989Date of Patent: July 9, 1991Assignee: Hoechst-Roussel Pharmaceticals IncorporatedInventors: John J. Tegeler, Kirk D. Shoger
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Patent number: 5026704Abstract: 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: GrantFiled: December 26, 1989Date of Patent: June 25, 1991Assignee: Novo Nordisk A/SInventors: Tage Honore, Poul Jacobsen, Flemming E. Nielsen, Lars Naerum
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Patent number: 5010078Abstract: 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: GrantFiled: March 14, 1990Date of Patent: April 23, 1991Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 5010079Abstract: 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: GrantFiled: August 2, 1989Date of Patent: April 23, 1991Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Daniel Obitz, Gerard Defosse, Elisabeth Dewitte, Corinne Veronique
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Patent number: 5000880Abstract: 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: GrantFiled: June 1, 1989Date of Patent: March 19, 1991Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Masami Ishihara, Hiroyoshi Nawa, Tsutomu Miyagawa
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Patent number: 5001124Abstract: 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: GrantFiled: February 2, 1990Date of Patent: March 19, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, Bruce H. Devens
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Patent number: 4997940Abstract: 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: GrantFiled: July 27, 1988Date of Patent: March 5, 1991Assignee: The Dow Chemical CompanyInventors: Anna P. Vinogradoff, William A. Kleschick
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Patent number: 4994464Abstract: 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: GrantFiled: October 5, 1989Date of Patent: February 19, 1991Assignee: Merck & Co., Inc.Inventors: Richard L. Tolman, John J. Baldwin, Arthur F. Wagner, Adolph Pietruszkiewicz