Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/288)
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Publication number: 20090054655Abstract: The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R1—X1—NY—R2, wherein: X1 represents —CO— or —SO2—; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R1 represents a substituted or unsubstituted hydrocarbon group, —NYR3 group or —OR3 group (in the formulae, R3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R2 represents a hydrogen atom or —CO—R4 group (in the formula, R4 represents a substituted or unsubstituted hydrocarbon group, —NYR5 group or —OR5 group (in the formulae, R5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R1 and R4 may bind to each other to form a further substiType: ApplicationFiled: April 5, 2007Publication date: February 26, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomomi Ikemoto, Naohiro Fukuda
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Publication number: 20090030010Abstract: This invention relates to compounds of general formula I in which R1 and R2 are described in this application, the use of the compounds of general formula I as inhibitors of protein tyrosine kinases for treatment of various diseases as well as the compounds of general formulas II and III as intermediate compounds for the production of compounds of general formula I, whereby X, R1a and R2a have the meaning that is described in general formulas II and III.Type: ApplicationFiled: December 14, 2005Publication date: January 29, 2009Inventors: Wolfgang Schwede, Hermann Kuenzer, Antonius Ter Laak, Benjamin Bader, Roman Hillig, Ursula Moenning, Arndt Schmitz, Dieter Zopf
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7332498Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.Type: GrantFiled: November 23, 2005Date of Patent: February 19, 2008Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
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Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7321043Abstract: Disclosed herein is a process for the preparation of a compound of the formula (II): or a salt thereof, wherein X is halogen; each Y, which may be the same or different, is halogen, haloalkyl, alkoxycarbonyl or alkylsulphonyl, and n is 0 to 3; which process comprises treating a compound of the formula (III): with a cyanide source and a catalyst selected from the group consisting of a tetraalkyl ammonium salt and a tetraalkyl phosphonium salt in an aqueous solvent or without solvent, wherein: X is halogen; each Y, which may be the same or different, is halogen, haloalkyl, alkoxycarbonyl or alkylsulphonyl: and n is 0 to 3; and wherein the cyanide source is hydrogen cyanide, an alkali metal cyanide, an alkaline earth metal cyanide or an optionally substituted ammonium cyanide.Type: GrantFiled: July 8, 2005Date of Patent: January 22, 2008Assignee: Bayer Cropscience S.A.Inventors: Norman Dann, Peter Dominic Riordan, Mehul Rasikchandra Amin, Michael Mellor
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Patent number: 7276528Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases.Type: GrantFiled: May 25, 2006Date of Patent: October 2, 2007Assignee: AstraZeneca ABInventors: Stephen Connolly, Glen Ernst
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Patent number: 7262252Abstract: There is provided a fluorine-containing resin composition which is used for nonlinear optical material and comprises (I) a fluorine-containing prepolymer and (II) an organic compound exhibiting a second- or higher-order nonlinear optical effect, in which the fluorine-containing prepolymer (I): (1) is a non-crystalline polymer having a fluorine content of not less than 25% and (2) has a carbon-carbon double bond in a polymer side chain or at an end of a polymer trunk chain and also there is provided a nonlinear optical waveguide device produced from the fluorine-containing resin composition. A suitable nonlinear optical material having a stable structure with a nonlinear substance is produced, and an excellent nonlinear optical waveguide device is produced by relatively simple steps while maintaining transparency in a near infrared region.Type: GrantFiled: November 12, 2003Date of Patent: August 28, 2007Assignee: Daikin Industries, Ltd.Inventors: Takayuki Araki, Yoshito Tanaka, Mihoko Ohashi, Yuzo Komatsu
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Patent number: 7262209Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: October 2, 2002Date of Patent: August 28, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Pierre Ducray
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Patent number: 7151182Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.Type: GrantFiled: September 3, 2004Date of Patent: December 19, 2006Assignee: Basilea Pharmaceutica AGInventors: Hiroshi Fukuda, Tadakatsu Hayase, Eisaku Mizuguchi, Nobuo Shimma, Jun Ohwada, Nobuhiro Oikawa, Masahiro Sakaitani, Masao Tsukazaki, Isao Umeda
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Patent number: 7132546Abstract: The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: [wherein A is CO or SO2; Cy is an aryl group or a heterocyclic group; each of R1 and R2 which are independent of each other, is a halogen atom, a cyano group, a nitro group, an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, a cycloalkyl group which may be substituted, a cycloalkenyl group which may be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an amino group which may be substituted or a —B-Q group; R3 is a -M1-M2-R5 group; R4 is a hydrogen atom or an alkyl group which may be substituted; x is an integer of from 0 to 5; y is an integer of from 0 to 4; and z is an integer of from 0 to 1].Type: GrantFiled: December 21, 2001Date of Patent: November 7, 2006Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Hirohiko Kimura, Shunji Yuki, Kazuhiro Yamamoto, Takashi Okada
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Patent number: 7119109Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease, CNS disorders and pain.Type: GrantFiled: July 26, 2002Date of Patent: October 10, 2006Assignee: Astrazeneca ABInventors: Deborah Chen, David Cheshire, Stephen Connolly, Antonio Mete
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Patent number: 7115637Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: August 8, 2003Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Patent number: 7015237Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.Type: GrantFiled: May 10, 2004Date of Patent: March 21, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Michael William Wilson
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Patent number: 6946479Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: GrantFiled: November 6, 2003Date of Patent: September 20, 2005Assignee: The Procter & Gamble CompanyInventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Patent number: 6930117Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: GrantFiled: November 6, 2003Date of Patent: August 16, 2005Assignee: The Procter & Gamble CompanyInventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Patent number: 6911451Abstract: Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.Type: GrantFiled: June 4, 1999Date of Patent: June 28, 2005Assignee: Celltech R&D LimitedInventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
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Patent number: 6864267Abstract: Novel calcilytic compounds and methods of using them are provided.Type: GrantFiled: July 16, 2001Date of Patent: March 8, 2005Assignee: SmithKline Beecham CorporationInventors: Pradip K. Bhatnagar, James F. Callahan, Amparo M. Lago
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Publication number: 20040248913Abstract: The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions forType: ApplicationFiled: May 26, 2004Publication date: December 9, 2004Inventors: Timothy Alan Grese, Kevin M Gardinier, Marcus F Boehm
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Patent number: 6828276Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.Type: GrantFiled: August 30, 2001Date of Patent: December 7, 2004Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
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Publication number: 20040230055Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.Type: ApplicationFiled: April 6, 2004Publication date: November 18, 2004Inventors: Christopher J. Woltermann, Douglas E. Sutton
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Patent number: 6809109Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: June 25, 2003Date of Patent: October 26, 2004Assignee: Bristol-Myers Squibb CompanyInventors: James D. Rodgers, Haisheng Wang
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Publication number: 20040176422Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R3, Q, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: ApplicationFiled: January 8, 2004Publication date: September 9, 2004Inventors: Timothy Birkinshaw, David Cheshire, Stephen Connolly, Timothy Luker, Antonio Mete
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Patent number: 6765095Abstract: A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.Type: GrantFiled: March 10, 2003Date of Patent: July 20, 2004Assignee: Dainippon Pharmaceutical Company, LimitedInventors: Motoji Kawasaki, Tomohiro Nigo
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Publication number: 20040102325Abstract: Compounds of formula (I) wherein the substituents R1, R2, R3 and R4, and the suffixes n and m are as defined in claim 1, and agrochemically acceptable salts and all stereoisomers and tautomers of such compounds are suitable for use as herbicides.Type: ApplicationFiled: March 25, 2003Publication date: May 27, 2004Inventors: J?uuml;rgen Schaetzer, Peter Renold, Gerald Wayne Craig, Martin Eberle, Roger Graham Hall
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Publication number: 20040072878Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C independently represents a hydrogen atom or a monovalent substituent; and X and X′ independently represents a hydrogen atom or a monovalent substituent.Type: ApplicationFiled: August 19, 2003Publication date: April 15, 2004Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
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Publication number: 20040058964Abstract: Disclosed are compounds Formula I 1Type: ApplicationFiled: February 14, 2003Publication date: March 25, 2004Inventors: Balekudru Devadas, John Walker, Shaun R. Selness, Terri L. Boehm, Richard C. Durley, Rajesh Devraj, Brian S. Hickory, Paul V. Rucker, Kevin D. Jerome, Heather M. Madsen, Edgardo Alvira, Michele A. Promo, Radhika M. Blevis-Bal, Laura D. Marruto, Jeff Hitchcock, Thomas Owen, Win Naing, Li Xing, Huey S. Shieh, Aruna Sambandam, Shuang Liu, Ian L. Scott, Kevin F. McGee
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Publication number: 20040029921Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.Type: ApplicationFiled: March 24, 2003Publication date: February 12, 2004Applicant: Merck Frosst Canada & Co.Inventors: Daniel Dube, Rejean Fortin, Richard Friesen
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Publication number: 20040006082Abstract: The present invention provides 2-aminopyridine compound having an excellent adenosine receptor (A1, A2a, A2b receptors) antagonism, which is represented by the following formula: 1Type: ApplicationFiled: January 23, 2003Publication date: January 8, 2004Inventors: Hitoshi Harada, Osamu Asano, Shuhei Miyazawa, Masato Ueda, Masahiro Yasuda, Nobuyuki Yasuda
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Publication number: 20030229125Abstract: The present invention relates to a compound of the formula (I) or salt thereof 1Type: ApplicationFiled: June 21, 2002Publication date: December 11, 2003Inventors: Klaus Haaf, Lothar Willms, Thomas Auler, Hubert Menne, Hermann Bieringer
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Patent number: 6653331Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.Type: GrantFiled: March 17, 1999Date of Patent: November 25, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Zhiyang Zhao, Alfredo G. Tomasselli, Kenneth A. Koeplinger, Tillie Peterson
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Patent number: 6653310Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: October 7, 2002Date of Patent: November 25, 2003Assignee: SmithKline Beecham CorporationInventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Publication number: 20030216257Abstract: The use of 1-aryl-4-haloalkyl-2-[1H]-pyridones of the formula I 1Type: ApplicationFiled: January 14, 2003Publication date: November 20, 2003Inventors: Ingo Sagasser, Olaf Menke, Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Matthias Witschel, Cyrill Zagar, Helmut Walter
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Patent number: 6632823Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: December 22, 1997Date of Patent: October 14, 2003Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
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Patent number: 6632945Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: December 21, 2000Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Publication number: 20030162972Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: August 5, 2002Publication date: August 28, 2003Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Patent number: 6599924Abstract: The invention relates to novel 2-hetaryl-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Hetaryl represents substituted heterocyclyls and Ar represents substituted phenyl, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: April 5, 2001Date of Patent: July 29, 2003Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Bernd Alig, Alan Graff, Udo Kraatz, Wolfgang Krämer, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Publication number: 20030139418Abstract: Compounds of the formula I; 1Type: ApplicationFiled: October 31, 2002Publication date: July 24, 2003Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 6583161Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: December 12, 2000Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Julio C. Medina
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Publication number: 20030109555Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO 2-pyridinylsulfonyl groups, or p-NO 2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Gluthathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.Type: ApplicationFiled: March 17, 1999Publication date: June 12, 2003Inventors: ZHIYANG ZHAO, ALFREDO G. TOMASSELLI, KENNETH A. KOEPLINGER, TILLIE PETERSON
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Publication number: 20030109711Abstract: 4-Haloalkylnicotinonitriles having the formula (I) 1Type: ApplicationFiled: December 30, 2002Publication date: June 12, 2003Inventors: Sergiy Pazenok, Henricus Maria Martinus Bastiaans
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Publication number: 20030078235Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: ApplicationFiled: June 21, 2002Publication date: April 24, 2003Inventors: Yong-Moon Choi, Ki-Ho Lee
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Publication number: 20030050314Abstract: There are described cycloalkyl derivatives of the formula (I)Type: ApplicationFiled: May 10, 2002Publication date: March 13, 2003Applicant: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Publication number: 20020156285Abstract: Compounds of formula 1 1Type: ApplicationFiled: January 31, 2002Publication date: October 24, 2002Inventors: Walter Kunz, Kurt Nebel
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Patent number: 6444675Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.Type: GrantFiled: April 24, 2001Date of Patent: September 3, 2002Assignee: Bristol-Myers Squibb CompanyInventor: Sing-Yuen Sit
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Patent number: 6440933Abstract: The invention provides peptide derivatives designed to deliver peptides having growth factor inhibitory activity, especially somatostatin analogs, to the retina by sequential metabolism. The peptide derivatives, which comprise a dihydropyridinepyridinium salt-type redox targetor moiety, a bulky lipophilic function and an amino acid/dipeptide/tripeptide spacer, are used in the prevention and treatment of diabetic retinopathy.Type: GrantFiled: September 1, 1998Date of Patent: August 27, 2002Assignee: University of FloridaInventors: Nicholas Stephen Bodor, Maria Bartolomeo Grant
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Patent number: 6420314Abstract: Substituted 2-phenylpyridines of the formula I in which the substituents and the index m are defined in the specification.Type: GrantFiled: November 17, 1999Date of Patent: July 16, 2002Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Peter Schäfer, Markus Menges, Olaf Menke, Robert Reinhard, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Publication number: 20020035257Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: ApplicationFiled: August 30, 2001Publication date: March 21, 2002Inventors: Emily J. Canada, Robert P. Gajewski, Christopher S. Galka, Neil V. Kirby, Irene M. Morrison, Jeannie R. Philips, Mary E. Pieczko, Brent J. Rieder, Chrislyn M. Carson, Zhengyu Huang