Patents Examined by Alan L. Rothman
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Patent number: 6500844Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: December 31, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Bryan Oates
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Patent number: 6130227Abstract: 20S-Camptothecin derivatives in which the 7-position bears as a substituent --CN, --CH(CN)R.sub.4, --CH.dbd.C(CN)R.sub.4, --C(.dbd.NOH)NH.sub.2, --C(.dbd.NH)NH.sub.2, --CH.dbd.C(NO.sub.2)R.sub.4, --CH(CN)R.sub.5, --CH(CH.sub.2 NO.sub.2)R.sub.5, tetrazol-5-yl, 4,5-dihydrooxazol-2-yl, or 1,2,4-oxadiazolin-3-yl-5-one. These compounds are active as topoisomerase I inhibitors, and can be used as antitumor drugs.Type: GrantFiled: August 20, 1998Date of Patent: October 10, 2000Assignee: Istituto Nazional per Lo Studio e la Cura Dei TumoriInventors: Lucio Merlini, Sergio Penco, Franco Zunino
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Patent number: 5756480Abstract: The invention concerns the treatment of hyperandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5.alpha.-reductase enzymes from 3-oxo-4-oxa end 4-thiasteroids having a 1,2-double bond and the pyridine-nucleotide cofactor of the 5.alpha.-reductase enzyme, NADPH. The invention further relates to the isolated inhibitor-cofactor complex.Type: GrantFiled: October 24, 1996Date of Patent: May 26, 1998Assignee: Merck & Co., Inc.Inventors: Herb G. Bull, Georgianna Harris, Robert W. Myers
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Patent number: 5545740Type: GrantFiled: August 11, 1994Date of Patent: August 13, 1996Assignee: SmithKLine Beecham, p.l.c.Inventors: Mark J. Hughes, John Kitteringham
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Patent number: 5493027Abstract: Coupled to the N-methyl-D-aspartate (NMDA) receptor-channel complex is a strychnine-insensitive binding site for glycine. Pharmacological antagonism of glycine binding at this site can produce anticonvulsant activity. Derivatives of kynurenic acid, pyridine and 2-carboxy-indole were synthesized and evaluated as antagonists of glycine binding and for anticonvulsant effects. Compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole, and in the rotorod assay for neurologic deficit. The derivatives were also assayed for binding at the NMDA-associated glycine site. The most potent anticonvulsant was ethyl 4-methylamino-5,7-dichloro-2-quinoline carboxylate. This compound provided protection against maximal electroshock (MES) induced seizures at a dose of 30 mg/kg. Other compounds were active at 100 mg/kg dose level, including 5-fluoro-2-indole carboxylic acid and the diethyl ester of 2,6-pyridine dicarboxylic acid.Type: GrantFiled: January 22, 1993Date of Patent: February 20, 1996Assignee: Board of Regents, the University of Texas SystemInventors: Alfred C. Nichols, K. Lemone Yielding
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Patent number: 5475012Abstract: Antiinfluenza A activity was found in compounds of the formula: ##STR1## wherein: X is 2-phenylethyl, 2-furanylmethyl, or ##STR2## where one of R.sup.1 and R.sup.2 is H and the other is phenylamino; Z is --SCH.sub.3 when X is ##STR3## or ##STR4## when X is 2-phenylethyl or 2-furanylmethyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 13, 1994Date of Patent: December 12, 1995Assignee: American Home Products CorporationInventors: Kuo-Hom L. Hsu, Daniel M. Teller, Alan R. Davis, Michael D. Lubeck, Harry R. Munson, Jr., Gunnar E. Jagdmann, Ibrahim M. Uwaydah
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Patent number: 5183910Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.Type: GrantFiled: October 3, 1991Date of Patent: February 2, 1993Assignee: Eli Lilly and CompanyInventor: Leland O. Weigel
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Patent number: 5118696Abstract: Novel 5-acyl-2-(1H)pyrdinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.Type: GrantFiled: November 9, 1990Date of Patent: June 2, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Winton D. Jones, Richard A. Schnettler, Richard C. Dage
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Patent number: 4959362Abstract: An ascorbic acid derivative of the formula: ##STR1## wherein R.sup.1 is organic residue having molecular weight of from 15 to 700, R.sup.2 is hydrogen or hydroxyl, R.sup.3 is hydrogen, acyl, optionally substituted phosphono or sulfo, and R.sup.3 and hydroxyl or R.sup.2 may form acetal residue or ketal residue, and a salt thereof are provided.The compound [I] and salts thereof have antioxidant activity and excellent prophylactic and improving actions on disorders of circulatory functions, and they are usefule as antioxidant agent for food and as agents of prophylaxis and improvement of circulatory functional disorders.Type: GrantFiled: September 19, 1988Date of Patent: September 25, 1990Assignee: Takeda Chemical Industries, Inc.Inventors: Shinji Terao, Minoru Hirata
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Patent number: 4786317Abstract: Compounds of the formula ##STR1## wherein W and X, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, iodine, nitro, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms or chloro-substituted alkyl of 1 to 4 carbon atoms;Y is hydrogen, fluorine, chlorine, bromine, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms or chloro-substituted alkyl of 1 to 4 carbon atoms;Z is fluorine, chlorine, bromine, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms, chloro-substituted alkyl of 1 to 4 carbon atoms, --COOH or --COO-(alkyl of 1 to 4 carbon atoms); andn is 0 or 1;and, when Z is COOH, salts thereof, especially their alkali metal salts. The compunds as well as the salts are useful as selective herbicides.Type: GrantFiled: September 5, 1986Date of Patent: November 22, 1988Assignee: Celamerck GmbH & Co. KGInventors: Rudolf Mengel, Ludwig Schroder, Werner Stransky, Gerbert Linden, Sigmund Lust
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Patent number: 4752610Abstract: There are disclosed novel compounds of the formula ##STR1## where R is H, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)r.sub.1, --C(OH)r.sub.1 r.sub.2 or --CH.sub.2 Or.sub.2, where r.sub.1 is H, loweralkyl, arylloweralkyl or aryl and r.sub.2 is loweralkyl; R.sub.1 is H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl or alkynoyl; and R.sub.2 is H, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl, or R.sub.Type: GrantFiled: December 4, 1985Date of Patent: June 21, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 4681941Abstract: An improved method of preparing aryloxyphenoxy propanoic acid esters is disclosed. Low-water levels and low temperatures increase the yield and decrease by-product formation. A hindered non-nucleophilic phenol, which is converted in situ to the phenate form, is added to the reaction mixture to drive the reaction to 99+% conversion.Type: GrantFiled: April 11, 1985Date of Patent: July 21, 1987Assignee: The Dow Chemical CompanyInventor: Timothy J. Adaway
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Patent number: 4663323Abstract: Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.Type: GrantFiled: May 11, 1984Date of Patent: May 5, 1987Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru Uchida, Takao Nishi, Kazuyuki Nakagawa
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Patent number: 4657577Abstract: Novel substituted pyridyl-phenyl ethers of the formula ##STR1## in which X represents trifluoromethyl or chlorine,Y represents hydrogen or chlorine,R.sup.1 represents hydrogen or methyl andR.sup.2 represents formyl or the radicals of the formulae ##STR2## in which R.sup.3 represents alkyl with 1 to 4 carbon atoms, or the two radicals R.sup.3 together represent an alkylene chain with 2 or 3 carbon atoms,R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen or alkyl with 1 to 4 carbon atoms,m represents 1 or 2,n represents 0 or 1 andZ represents trimethylsilyl, optionally substituted azolyl which is bonded via nitrogen or the radicals of the formulae ##STR3## in which R.sup.8 represents alkyl with 1 to 4 carbon atoms,or the two radicals R.sup.8 together represent an alkylene chain with 2 or 3 carbon atoms,R.sup.9 represents alkyl with 1 to 4 carbon atoms,X.sup.1 represents oxygen or sulphur andR.sup.10 and R.sup.Type: GrantFiled: March 28, 1985Date of Patent: April 14, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Erich Klauke, Uwe Priesnitz, Hans-Jochem Riebel, Ludwig Eue, Robert R. Schmidt
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Patent number: 4499277Abstract: 2(6)-(Trichloromethyl)pyridines are reduced to the corresponding 2(6)-(dichloromethyl)pyridines by treatment with a strong base and an anionic reductant derived from a reductant source material selected from the group consisting of dialkylphosphite and trialkylphosphite said treatment taking place in the presence of a polar, non-hydroxylic solvent and/or a phase transfer catalyst.Type: GrantFiled: March 14, 1983Date of Patent: February 12, 1985Assignee: The Dow Chemical CompanyInventors: Sudarhshan K. Malhotra, Jon A. Orvik
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Patent number: 4493931Abstract: The present invention provides a multistep process for the preparation of .beta.-cyclo-substituted ethylamines of the general formula:-Ar--CH.sub.2 --CH.sub.2 --NH.sub.2 (I)in which AR is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly- substituted, wherein said compounds represent a class of intermediates which can be converted to 4,5,6,7-tetrahydro[3,2-C] or [2,3-C]pyridines wherein the latter are useful for anti-inflammatory, vasodilator or blood platelet aggregation inhibition activities.Type: GrantFiled: June 29, 1982Date of Patent: January 15, 1985Assignee: SanofiInventors: Isaac Chekroun, Alain Heymes
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Patent number: 4189588Abstract: Novel triazolo- or imidazo-benzotriazepines are prepared from 1,3,4-benzotriazepine-2-thiones which in turn are prepared from a 2-aminobenzophenone.Type: GrantFiled: October 16, 1978Date of Patent: February 19, 1980Assignee: The Dow Chemical CompanyInventors: Thomas C. Britton, Donald L. Trepanier
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Patent number: 4154838Abstract: The compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N"-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitroeth ylene.Type: GrantFiled: January 13, 1978Date of Patent: May 15, 1979Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
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Patent number: 4065459Abstract: This invention relates to a process for the preparation of compounds having the formula: ##STR1## in which R.sub.1 is H or lower alkyl and R.sub.2 is H or lower alkyl, or phenyl or benzyl optionally substituted with at least one halogen or a lower alkyl, lower alkoxy, trifluoromethyl or nitro group.According to this method, a compound of the formula: ##STR2## in which R.sub.1 and R.sub.2 are as defined above and R.sub.3 is H or optionally substituted alkyl or benzyl, is reacted with a derivative Hal--SO.sub.2 --R (III) in which Hal is halogen and R is optionally substituted alkyl, aryl or aralkyl, to give a derivative of the formula: ##STR3## in which the various symbols have the above-defined meanings, and the sulfonated derivative of the formula (IV) is heated in the presence of an acid, to give the compound of the formula (I).Type: GrantFiled: February 6, 1976Date of Patent: December 27, 1977Assignee: ParcorInventors: Alan Heymes, Jean-Pierre Maffrand