At 2-position Patents (Class 544/315)
-
Patent number: 6867210Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: March 12, 2001Date of Patent: March 15, 2005Assignee: Euro-Celtique S.A.Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
-
Patent number: 6855716Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.Type: GrantFiled: December 26, 2001Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
-
Patent number: 6818648Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 17, 2003Date of Patent: November 16, 2004Assignee: Bristol-Myers Squibb PharmaInventors: Robert John Chorvat, Parthasarathi Rajagopalan
-
Patent number: 6818631Abstract: Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).Type: GrantFiled: August 15, 2003Date of Patent: November 16, 2004Assignee: Nippon Soda Co. Ltd.Inventors: Yuki Nakagawa, Sergey Bobrov, Charles R. Semer, IV, Thomas A. Kucharek, Masahiro Haramoto
-
Patent number: 6806230Abstract: Pyrimidine derivatives having excellent herbicidal activities for crop plants and selectivity between crop plants and weeds, are presented. Pyrimidine derivatives represented by the following formula (I): wherein R1 is a hydrogen atom, an alkyl group, a haloalkyl group or the like; R2 is an alkyl group, a phenyl group which may be substituted, or the like; R3 is a hydrogen atom, an alkyl group, an alkynyl group or the like; R7 is a hydrogen atom, a halogen atom, an alkyl group or the like; R8 is a hydrogen atom, an alkyl group or the like, W is a —C(═Q) Z— group or a —SO2— group; Q is O or S; Z is O, S, a —C(R4)R5—, a —NR6 group or the like; each of R4 and R5 is a hydrogen atom, an alkyl group, an alkoxy group or the like; R6 is a hydrogen atom or an alkyl group; and Ar is a phenyl group which may be substituted, a pyridyl group which may be substituted, or the like, and herbicides containing such pyrimidine derivatives as active ingredients.Type: GrantFiled: March 11, 2002Date of Patent: October 19, 2004Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Atsushi Yasuda, Fumiaki Takabe, Ikumi Urushibata, Mikio Yamaguchi, Yoshihiro Yamaji, Makoto Fujinami, Takeshige Miyazawa
-
Publication number: 20040198728Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.Type: ApplicationFiled: September 22, 2003Publication date: October 7, 2004Applicant: Cell Therapeutics, Inc.Inventors: Feng Hong, J. Peter Klein
-
Patent number: 6794378Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: December 31, 2001Date of Patent: September 21, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Koichi Fujita, Ariko Kodaira, Toshihiro Hatanaka, Kenji Takehana, Tsuyoshi Kobayashi, Atsushi Konishi, Takashi Yamamoto
-
Patent number: 6790846Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.Type: GrantFiled: May 7, 2002Date of Patent: September 14, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
-
Patent number: 6787544Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: February 20, 2001Date of Patent: September 7, 2004Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura
-
Patent number: 6780868Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: February 20, 2003Date of Patent: August 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
-
Publication number: 20040147761Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1Type: ApplicationFiled: December 15, 2003Publication date: July 29, 2004Inventors: Jean-Michel Paul, Bernard Dupont
-
Patent number: 6762197Abstract: A triazolone compound of the formula [I]: wherein; R1 represents optionally substituted phenyl or the like, T represents m-phenylene optionally substituted by methyl or the like; and a fungicidal composition containing it as an active ingredient.Type: GrantFiled: June 6, 2002Date of Patent: July 13, 2004Assignee: Sumitomo Chemical Company, LimitedInventors: Tomohiro Araki, Yoshiharu Kinoshita, Hiroshi Sakaguchi, Akio Manabe
-
Publication number: 20040132752Abstract: This invention discloses and claims diary heterocycles of formula (I) 1Type: ApplicationFiled: July 24, 2003Publication date: July 8, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Gerard Rosse, Armin Walser
-
Publication number: 20040087581Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: October 14, 2003Publication date: May 6, 2004Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
-
Publication number: 20040077641Abstract: Novel pyridylpyrimidines of the formula 1Type: ApplicationFiled: August 19, 2003Publication date: April 22, 2004Inventors: Thomas Bretschneider, Mazen Es-Sayed, Rudiger Fischer, Fritz Maurer, Christoph Erdelen, Peter Losel
-
Publication number: 20040063659Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.Type: ApplicationFiled: September 18, 2003Publication date: April 1, 2004Applicant: Merrell Pharmaceuticals Inc.Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
-
Patent number: 6710045Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.Type: GrantFiled: May 12, 2003Date of Patent: March 23, 2004Assignee: Bayer CropScience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
-
Patent number: 6686369Abstract: The present invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.Type: GrantFiled: October 8, 1998Date of Patent: February 3, 2004Assignee: Abbott GmbH & Co., KGInventors: Dagmar Klinge, Wilhelm Amberg, Ernst Baumann, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenröder, Sabine Schult
-
Patent number: 6664247Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: December 16, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
-
Patent number: 6653295Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: December 12, 2001Date of Patent: November 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Peter William Glunz, Brent Dale Douty, Wei Han
-
Patent number: 6653258Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.Type: GrantFiled: March 27, 1995Date of Patent: November 25, 2003Assignee: Syngenta LimitedInventors: John M Clough, Christopher R A Godfrey, Paul J de Fraine, Michael G Hutchings, Vivienne M Anthony
-
Patent number: 6653300Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
-
Patent number: 6649622Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: January 26, 2001Date of Patent: November 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard Sulsky, Jeffrey A. Robl
-
Patent number: 6632817Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.Type: GrantFiled: August 20, 2001Date of Patent: October 14, 2003Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Reinhard Lantzsch, Ralf Tiemann, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann, Martin Kugler, Hans-Ulrich Buschhaus
-
Publication number: 20030187259Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1Type: ApplicationFiled: May 12, 2003Publication date: October 2, 2003Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrim, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
-
Patent number: 6610691Abstract: The invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings defined in the description, to the preparation of these compounds and to their use as drugs.Type: GrantFiled: October 8, 1998Date of Patent: August 26, 2003Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Heinz Hillen, Liliane Unger, Bernd Elger
-
Patent number: 6608072Abstract: Compounds of formula (I) and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: April 22, 2002Date of Patent: August 19, 2003Assignee: Novartis AGInventor: Lászlo Révész
-
Patent number: 6605611Abstract: Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.Type: GrantFiled: September 3, 2002Date of Patent: August 12, 2003Assignee: Nycomed Amersham PLCInventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
-
Publication number: 20030119835Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: July 3, 2002Publication date: June 26, 2003Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
-
Publication number: 20030114472Abstract: This invention concerns the use of compounds of formula 1Type: ApplicationFiled: November 1, 1999Publication date: June 19, 2003Inventors: BART DE CORTE, MARC RENE DE JONGE, JAN HEERES, CHIH YUNG HO, PAUL ADRIAAN JAN JANSSEN, ROBERT W. KAVASH, LUCIEN MARIA HENRICUS KOYMANS, MICHAEL JOSEPH KUKLA, DONALD WILLIAM LUDOVICI, KOEN JEANNE ALFONS VAN AKEN
-
Patent number: 6579874Abstract: Compounds of formula I wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: October 12, 2001Date of Patent: June 17, 2003Assignee: Novartis AGInventors: Lászlo Révész, Achim Schlapbach
-
Publication number: 20030109484Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.Type: ApplicationFiled: June 6, 2002Publication date: June 12, 2003Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
-
Publication number: 20030105084Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1Type: ApplicationFiled: September 18, 2002Publication date: June 5, 2003Applicant: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Biswanath De
-
Publication number: 20030096931Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1Type: ApplicationFiled: August 22, 2002Publication date: May 22, 2003Inventors: Jean-Michel Paul, Bernard Dupont
-
Patent number: 6566357Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 uniType: GrantFiled: September 18, 2002Date of Patent: May 20, 2003Assignee: The Procter & Gamble Co.Inventors: Matthew John Laufersweiler, Michael Philip Clark, Jane Far-Jine Djung, Adam Golebiowski, Todd Andrew Brugel, Biswanath De
-
Publication number: 20030092678Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: May 15, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
-
Patent number: 6562832Abstract: Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: December 15, 1999Date of Patent: May 13, 2003Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm, Timothy Francis Gallagher
-
Patent number: 6554966Abstract: The invention relates to a process for preparing essentially formic acid-free N-alkyl-N′-methylalkyleneureas of the formula with R1=H or CH3, R2=CnH2n+1 with n=1-4 and x=0 or 1, from the corresponding alkyleneureas by reaction with monomeric or polymerized formaldehyde in the presence of formic acid. This entails feeding the mixture, obtained in the reaction, of N-alkyl-N′-methylalkyleneurea and formic acid to the upper region of a distillation column, distilling without further additions and removing essentially formic acid-free N-alkyl-N′-methylalkyleneurea in the lower region of the column.Type: GrantFiled: June 26, 2000Date of Patent: April 29, 2003Assignee: BASF AktiengesellschaftInventors: Andreas Kramer, Johann-Peter Melder, Heinz RĂĽtter, GĂĽnter Riewe, Wolfgang Siegel, Hans-JĂĽrgen Weyer
-
Publication number: 20030069242Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): 1Type: ApplicationFiled: April 15, 2002Publication date: April 10, 2003Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
-
Publication number: 20030064980Abstract: Compound represented by the structural formula 1Type: ApplicationFiled: June 6, 2002Publication date: April 3, 2003Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
-
Patent number: 6534492Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.Type: GrantFiled: May 4, 2001Date of Patent: March 18, 2003Assignee: BASF AktiengesellschaftInventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
-
Patent number: 6528510Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.Type: GrantFiled: November 2, 2000Date of Patent: March 4, 2003Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
-
Patent number: 6525025Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.Type: GrantFiled: September 7, 2001Date of Patent: February 25, 2003Assignee: Merck Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich L. Grimm, Renee Aspiotis, Cameron Black
-
Publication number: 20030036543Abstract: This invention describes novel pyrazole compounds of formula IIIa: 1Type: ApplicationFiled: December 19, 2001Publication date: February 20, 2003Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
-
Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
-
Patent number: 6509341Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.Type: GrantFiled: April 20, 2000Date of Patent: January 21, 2003Assignee: Abbott LaboratoriesInventors: Wilhelm Amberg, Rolf Jansen, Stefan Hergenröder, Manfred Raschack, Liliane Unger
-
Patent number: 6506763Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: July 30, 2001Date of Patent: January 14, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Publication number: 20020193375Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).Type: ApplicationFiled: June 27, 2002Publication date: December 19, 2002Applicant: ZENECA LIMITEDInventors: Peter Warner, Roger James, Thorsten Nowak
-
Patent number: 6492366Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;): wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.Type: GrantFiled: October 11, 2000Date of Patent: December 10, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
-
Patent number: 6489325Abstract: The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.Type: GrantFiled: March 30, 2000Date of Patent: December 3, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ralph F. Hall