The Nitrogen Is Multiply Bonded To Carbon Patents (Class 548/336.1)
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7026339Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.Type: GrantFiled: November 3, 2004Date of Patent: April 11, 2006Inventors: Fan Yang, Bo Zhang, Nancy Anne Wicnienski, Jeffrey Allen Pfefferkorn, Meredith L. Greene, Ke Chen, Richard A. Nugent, Matthew Todd Reding, Robert Charles Kelly, Mark A. Mitchell, Lee A. Funk, Richard Frederick Heier, III, Rebecca Merry Anderson
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Patent number: 7026345Abstract: The present invention relates to chiral N-acetyl-alpha-amino acid salts of optically active ?-amino alkylnitriles, and also to a process for preparing optically active ?-amino alkylnitriles by resolving racemic ?-amino alkylnitriles using chiral N-acetyl-alpha-amino acids as resolving agent.Type: GrantFiled: September 17, 2004Date of Patent: April 11, 2006Assignee: Pfizer Inc.Inventors: Juan Colberg, Samuela Zambelli Franz, Riccardo Motterle, Mariano Stivanello
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Patent number: 6951948Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) wherein X, R2 and the ring components are as described herein, novel intermediates useful for synthesizing such substituted azole compounds and methods for identifying and isolating the compounds.Type: GrantFiled: May 22, 2001Date of Patent: October 4, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Yijun Deng, Dennis Hlasta
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Patent number: 6936627Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.Type: GrantFiled: October 29, 2002Date of Patent: August 30, 2005Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
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Patent number: 6878829Abstract: ?-alaninamides of the general formula Wherein R1 is hydrogen or C1-6 alkyl which is unsubstituted or substituted with hyroxy, amino, carboxy, carbamoyl, methylmercapto, guanidino, unsubstituted or substituted aryl or heteroaryl, and R2 is hydrogen, or R1 and R2 together form a group of the formula —(CH2)n— where n is 3 or 4, and R3 is hydrogen, a negative charge compensated by an equivalent of an inorganic or organic cation or is C1-6 alkyl, are prepared, without using an amino-protective group, by reacting the corresponding ?-amino acid or the corresponding ?-amino acid ester with a cyanoacetic ester to give a cyanoacetamide and by subsequent catalytic hydrogenation. The method is particularly suitable for preparing carnosine (?-alanyl-L-histidine, R1=imidazol-4-yl-methyl, R2=R3=H), a naturally occurring dipeptide which used as a dietary supplement with antioxidative action.Type: GrantFiled: March 2, 2001Date of Patent: April 12, 2005Assignee: Lonza AGInventors: Stefan Hildbrand, Thomas Ruppen, Dario Veghini
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Publication number: 20040158062Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds are useful in the treatment of benign prostatic hyperplasia.Type: ApplicationFiled: February 9, 2004Publication date: August 12, 2004Applicant: Pfizer IncInventors: Jens Bertil Ahman, Paul Blaise Hodgson, Sarah Jane Lewandowski, Robert Walton
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Publication number: 20040092495Abstract: The present invention relates to biguanide derivatives of formula (I), wherein R1, R2, R3 and R4 have the meanings as given in claim (1). Compounds are useful in the treatment of pathologies associated with hyperglycaemia, such as diabetes.Type: ApplicationFiled: September 22, 2003Publication date: May 13, 2004Inventors: Gerard Moinet, Daniel Cravo
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Patent number: 6720452Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: June 10, 2002Date of Patent: April 13, 2004Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
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Patent number: 6709824Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: September 24, 2001Date of Patent: March 23, 2004Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Patent number: 6703411Abstract: Benzoylguanidines of the formula (I) in which R1 to R4 have the meanings given in the specification and claims are suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. The compounds of the invention also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the triggering of ischemically induced cardiac arrhythmias.Type: GrantFiled: January 17, 2001Date of Patent: March 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Andreas Weichert, Udo Albus, Hans-Willi Jansen, Heinz-Werner Kleemann, Hans Jochen Lang
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Patent number: 6649643Abstract: Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.Type: GrantFiled: April 12, 2002Date of Patent: November 18, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6638962Abstract: Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing tType: GrantFiled: January 16, 2002Date of Patent: October 28, 2003Assignee: Les Laboratoires ServierInventors: Patrick Casara, Thierry Le Diguarher, Gilbert Dorey, John Hickman, Alain Pierre, Gordon Tucker, Nicolas Guilbaud
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Patent number: 6610716Abstract: Provided, among other things, is a compound of the formula:Type: GrantFiled: July 13, 2001Date of Patent: August 26, 2003Assignee: Alteon IncorporatedInventors: Dilip R. Wagle, Sheng Ding Fang
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Publication number: 20030153559Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: ApplicationFiled: November 20, 2002Publication date: August 14, 2003Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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Patent number: 6593473Abstract: Improved process for the preparation of granular N-alkylammoniumacetonitrile salts I R2R3N+R1—CR4R5—CN Y− (I) where R1 to R5 are hydrogen or organic radicals, and Y− is a sulfate or hydrogensulfate anion, from an aqueous solution of the compound II R2R3N+R1—CR4R5—CN R6O—SO2—O− (II) where R6 is C1- to C4-alkyl, which comprises evaporating this aqueous solution at a temperature of from 80° C. to 250° C. and a pressure of from 10 mbar to 2 bar to give a melt, then allowing the melt to solidify, where, during or following the evaporation, customary carrier materials and/or auxiliaries can be added, and the resulting solidified compound I is converted into the desired granular form.Type: GrantFiled: September 25, 2001Date of Patent: July 15, 2003Assignee: BASF AktiegesellschaftInventors: Michael Schönherr, Hans-Jürgen Kinder, Klaus Mundinger, Gregor Schürmann
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Publication number: 20030130520Abstract: A method of producing a compound of formula 1Type: ApplicationFiled: August 22, 2002Publication date: July 10, 2003Inventor: Peter Maienfisch
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Publication number: 20030125561Abstract: The present invention is directed to salts of the formula: 1Type: ApplicationFiled: May 21, 2002Publication date: July 3, 2003Inventors: Louis A. Carpino, Hideko Imazumi, Ayman El-Faham
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Patent number: 6562846Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.Type: GrantFiled: April 23, 2002Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, Kai Xie
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Publication number: 20030045726Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: ApplicationFiled: September 13, 2002Publication date: March 6, 2003Inventors: George W. Muller, Mary Shire
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Patent number: 6518257Abstract: To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.Type: GrantFiled: April 18, 2002Date of Patent: February 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Tomohiro Kaku, Masami Kusaka
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Publication number: 20030004358Abstract: 1 The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their prepration and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.Type: ApplicationFiled: June 11, 2002Publication date: January 2, 2003Inventors: Wolf- Rudiger Ulrich, Christian Scheufler, Thomas Fuchss, Jorg Senn-Bilfinger
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Patent number: 6495580Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.Type: GrantFiled: October 18, 1999Date of Patent: December 17, 2002Assignee: ViroPharma IncorporatedInventors: Theodore J. Nitz, Daniel C. Pevear
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Patent number: 6495699Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R5, X, Y, and are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.Type: GrantFiled: August 6, 2001Date of Patent: December 17, 2002Assignee: Agouron Pharmaceuticals Inc.Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
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Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6384068Abstract: In one embodiment, the invention provides a polymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions. G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The polymers formed by at least two of the cyclic imidazole units. In another embodiment, the invention provides new imidazole compounds usable as monomers to form the polymers. In still another embodiment, the invention provides a method for using the polymers as a coupling/activator for synthon synthesis.Type: GrantFiled: July 26, 2001Date of Patent: May 7, 2002Assignee: The Regents of the University of MichiganInventors: Paul G. Rasmussen, Sarah E. Reybuck, David M. Johnson, Richard G. Lawton
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Patent number: 6358987Abstract: A compound of formula (I) wherein X is —COOH or —CONHOH Y is a group of formula (ID) or (IE) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.Type: GrantFiled: March 5, 2001Date of Patent: March 19, 2002Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
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Patent number: 6359061Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.Type: GrantFiled: March 19, 1999Date of Patent: March 19, 2002Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Edward Swayze, Peter William Davis
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Publication number: 20020032227Abstract: A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as the active ingredient wherein R1 represent optionally substituted aryl, optionally substituted heterocycle, mono- or di-substituted methyleneamino, optionally substituted (substituted imino)methyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, substituted carbonyl or substituted sulfonyl; R2 represents alkyl, alkenyl, alkynyl or cycloalkyl; R3 represents optionally substituted heterocycle; R4 represents hydrogen, alkyl, alkoxy, halogen, nitro, cyano or haloalkyl; M represents oxygen, S(O)i (i being 0, 1 or 2), NR16 (R16 being hydrogen, alkyl or acyl) or a single bond; n represents 0 or 1, provided n represent 1 when R3 represents imidazol-1-yl or 1H-1,2,4-triazol-1-yl; and the symbol˜represents the E form, Z form or a mixture thereof.Type: ApplicationFiled: December 4, 2000Publication date: March 14, 2002Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Tsuneo Iwakawa, Kazuo Ueda, Michio Masuko
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Publication number: 20020028952Abstract: In one embodiment, the invention provides a polymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions. G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The polymers formed by at least two of the cyclic imidazole units. In another embodiment, the invention provides new imidazole compounds usable as monomers to form the polymers. In still another embodiment, the invention provides a method for using the polymers as a coupling/activator for synthon synthesis.Type: ApplicationFiled: July 26, 2001Publication date: March 7, 2002Inventors: Paul G. Rasmussen, Sarah E. Reybuck, David M. Johnson, Richard G. Lawton
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Publication number: 20020022728Abstract: Novel nitrophenyl-sulphonyl-imidazoles of the formula 1Type: ApplicationFiled: January 30, 2001Publication date: February 21, 2002Inventors: Lutz Assmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Peter Wachtler
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Publication number: 20010056107Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: ApplicationFiled: July 16, 2001Publication date: December 27, 2001Inventors: George W. Muller, Mary Shire
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Patent number: 6326500Abstract: Compounds of formula (I) and salts thereof, wherein R1 is hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, —NR13R14, —N(R15)SO2R16, haloalkoxy, haloalkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, —SOnR7, alkoxycarbonylalkyl, carboxylalkyl, —CONR11R12, carbamoylvinyl, —O—SO2R21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl, —NR60R61 or —(O)z—L3—G (G=−NR22R23, —SOmR26, CONR27R28 or —OR29); R2 and R3 are independently hydrogen halo, alkyl, alkoxy, —NR13R14, haloalkoxy, haloalkyl, hydroxy, —SOnR7 or —NR60R61; L1 is a bond, alkylene, cycloalkylene or cycloalkylidene; T is a bond, O, S, SO, SO2, CO or 1,3-dioxolan-2-ylidene; L2 is alkylene, cycloalkylene or cycloalkylidene; R6 is hydrogen or alkyl; Q is alkylene; and Y is imidazolyl, which are antiinflammatory, antiallergic and immunodulant agents.Type: GrantFiled: December 27, 2000Date of Patent: December 4, 2001Assignee: Abbott LaboratoriesInventors: David John Calderwood, Adrian John Fisher, James Edward Jeffery, Colin Gerhart Pryce Jones, Paul Rafferty
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Patent number: 6323227Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: February 26, 1999Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
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Patent number: 6316616Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: April 22, 1998Date of Patent: November 13, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Patent number: 6310067Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.Type: GrantFiled: August 3, 2000Date of Patent: October 30, 2001Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Kazuhiko Ito, Takahiro Sakaue, Sachiko Inoue, Shinya Ogino
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Patent number: 6303782Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventor: Stéphane Caron
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Patent number: 6297239Abstract: The present invention is directed to compounds which inhibit a prenyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting a prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: October 6, 1998Date of Patent: October 2, 2001Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, John H. Hutchinson, Anthony W. Shaw, Samuel L. Graham, Terrence M. Ciccarone
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6215001Abstract: Compounds of the formula I and pharmaceutically acceptable salts thereof in which R1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, —NR13R14, —N(R15)SO2R16, halogenated alkoxy, halogenated alkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, —S(O)nR7, alkoxycarbonylalkyl, carboxyalkyl, —CONR13R12 carbamoylvinyl, —OSO2R21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl or —NR60R61; or R1 represents a group of formula —(O)z—L3G wherein z equals 0 or 1, L3 represents a C1-4 alkylene chain, G represents a group of formula a), b), c), or d): a) —NR22R23; b) —S(O)mR26; c) CONR27R28; d) —OR29; R2 and R3 independently represent hydrogen, halo, alkyl, alkoxy, —NR13R14, halogenated alkoxy, halogenated alkyl, hydroxy, —S(O)nR7 or —NR60R61; L1 represents e) a bond, or f) alkylene, cycloalkylene or cycloalkylidene; T represents a bond or O, S, SO, SO2, a carboType: GrantFiled: October 7, 1999Date of Patent: April 10, 2001Assignee: Knoll AktiengesellschaftInventors: David John Calderwood, Adrian John Fisher, James Edward Jeffery, Colin Gerhart Pryce Jones, Paul Rafferty
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Patent number: 6197973Abstract: 3-phenylpyrazoles of formula I wherein R1 is cyano, alkyl or haloalkyl; R2 is cyano or is optionally halogenated alkyl, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl; R3 is hydrogen, cyano, halogen, alkyl or haloalkyl; R4 is hydrogen or halogen; R5 is cyano, halogen, or is optionally halogenated alkyl or alkoxy; R6, R7 independently of one another are optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl or phenyl, optionally substituted alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or optionally halogenated alkylsulfonyl; X is a chemical bond, —C≡C—, —CH2—CH(R8)— or —CH═C(R8)—, wherein R8 is hydrogen, cyano, nitro, halogen, alkyl or haloalkyl; Y is oxygen or sulfur; their preparation and their use for controlling undesirable vegetation.Type: GrantFiled: February 1, 1999Date of Patent: March 6, 2001Assignee: BASF AktiengesellschaftInventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Peter Schäfer, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6184244Abstract: This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.Type: GrantFiled: June 30, 1999Date of Patent: February 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Xu Bai