Nitrogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/205)
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Patent number: 6987112Abstract: The present invention is directed to compounds represented by Formula (1); wherein A, R, X, Y and n are as defined in the description, the salts thereof, and insecticide/acaricide compositions characterized by comprising one or more of said compounds and/or said salts as the active ingredients.Type: GrantFiled: November 1, 2001Date of Patent: January 17, 2006Assignee: Nippon Soda Co., Ltd.Inventors: Yasushi Shibata, Renpei Hatano, Takao Iwasa, Satoru Makita, Daisuke Hanai, Masao Yamaguchi, Naomi Ichikawa
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Patent number: 6949536Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.Type: GrantFiled: February 3, 2004Date of Patent: September 27, 2005Assignee: Pfizer, Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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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: 6933309Abstract: A halogenobenzylaminopropionic acid derivative represented by the following formula (1): or a pharmaceutically acceptable salt of the derivative, and a drug containing the same as an active ingredient for treating diabetes, hyperlipidemia, or similar pathological conditions.Type: GrantFiled: December 26, 2002Date of Patent: August 23, 2005Assignee: Toaeiyo Ltd.Inventors: Koichi Takayanagi, Hideki Yamada, Shin-ichi Kazayama, Shin-ya Ohnuma
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Patent number: 6921769Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: March 28, 2003Date of Patent: July 26, 2005Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexy Rivkin, Fumikiko Yoshimura, Ting-Chao Chou, Ana E. Gabarda
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Patent number: 6916956Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.Type: GrantFiled: August 10, 2001Date of Patent: July 12, 2005Assignee: Japan Tobacco, Inc.Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
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Patent number: 6908938Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and, in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, RY, Xb, A,B,Z, R3, R4, R4a, R5 and R5a are as defined herein.Type: GrantFiled: October 28, 2002Date of Patent: June 21, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6875873Abstract: 1,4-Diamino-2-(thiazol-2-yl)benzene derivatives of general formula (I) and the physiologically tolerated, water-soluble salts thereof: and agents containing these compounds, for oxidative dyeing of keratin fibers.Type: GrantFiled: September 10, 2001Date of Patent: April 5, 2005Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6864270Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.Type: GrantFiled: August 8, 2002Date of Patent: March 8, 2005Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 6861522Abstract: A process for the preparation of a compound of the formula in which Q is CH or N; Y is NO2 or CN; Z is CHR3, O, NR3 or S; R1 and R2 are, for example, together an alkylene bridge which optionally contains an O; R3 is H or unsubstituted or R4-substituted C1-C12alkyl, R4 is unsubstituted or substituted aryl or heteroaryl; wherein said compound has pesticidal activity.Type: GrantFiled: October 25, 2001Date of Patent: March 1, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Rapold, Gottfried Seifert, Marcel Senn
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Patent number: 6828341Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.Type: GrantFiled: March 27, 2002Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer
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Publication number: 20040224945Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) 1Type: ApplicationFiled: May 28, 2004Publication date: November 11, 2004Applicant: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hutter, Klaus Dembowsky, Elke Stahl
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Patent number: 6812238Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.Type: GrantFiled: October 31, 2000Date of Patent: November 2, 2004Assignee: 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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Publication number: 20040204406Abstract: The present invention is directed to a compound of formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: October 14, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20040186151Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.Type: ApplicationFiled: February 12, 2004Publication date: September 23, 2004Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ravindra R. Yarragunta, Rongyuan Xie, Tan Ren, Govindan Subramanian, James C. Quada
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Patent number: 6784167Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
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Publication number: 20040157892Abstract: Disclosed herein are fluoroethyl pyrazole compounds of the formula: 1Type: ApplicationFiled: February 12, 2003Publication date: August 12, 2004Applicants: CROMPTON CO./Cie, UNIROYAL CHEMICAL CO., INC.Inventors: Sheldon B. Park, Mark A. Dekeyser, Paul T. McDonald
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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: 20040116616Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.Type: ApplicationFiled: December 11, 2002Publication date: June 17, 2004Applicant: 3M Innovative Properties CompanyInventors: Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann, Larry R. Krepski, Stephen B. Roscoe, Michael S. Wendland
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Publication number: 20040116424Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula 1Type: ApplicationFiled: March 28, 2003Publication date: June 17, 2004Applicant: Neurogen CorporationInventors: George P. Luke, George D. Maynard, Scott Mitchell, Andrew Thurkauf, Linghong Xie, LuYan Zhang, Suoming Zhang, He Zhao, Bertrand L. Chenard, Yang Gao, Bingsong Han, Xiao Shu He
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Patent number: 6747146Abstract: Method of producing compounds of formula wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C8-alkyl, C3-C6-cycloalkyl, or a radical —N(R3)R4; or R2 and R6 together are —CH2—CH2—S—; R3 and R4 are hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or a radical —CH2B; R6 is hydrogen, C1-C8-alkyl, aryl or benzyl; or R3 and R6 together are —CH2—CH2—, —CH2—CH2—CH2—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—N(R5)—CH2—; X is CH—CN; CH—NO2 or N—NO2; A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and B is optionally substituted phenyl, 3-pyridyl or thiazolyl; characterised in that a compound of formula wherein R2, R6 and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of fType: GrantFiled: December 20, 2002Date of Patent: June 8, 2004Assignee: Syngenta Crop Protection, Inc.Inventors: Gottfried Seifert, Thomas Rapold, Verena Gisin
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Patent number: 6737418Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is 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: April 30, 2002Date of Patent: May 18, 2004Assignee: Euro-Celtique S.A.Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
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Patent number: 6727238Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 oType: GrantFiled: June 18, 2003Date of Patent: April 27, 2004Assignee: Pfizer Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Publication number: 20040054189Abstract: A process for the preparation of a compound of the formula (I) in which Q, Y, Z, R1, R2 are as defined in claim 1; in which a) a compound of the formula (II), in which X is a leaving group, is reacted with a halogenating agent to give a compound of the formula (III), in which W is a halogen atom; and b) the resulting compound of the formula (III) is reacted with a compound of the formula (IV), in which R1, R2, Y, Z and Q are as defined in claim 1; wherein the preparation of the compound of the formula (III) according to process stage a) involves a purification step in which the reaction mass which has formed is treated with water in the acidic pH range; a process for the preparation of a compound of the formula (III) according to the abovementioned process a), and the use of the compounds of the formulae (II), (III) and (IV) in a process as detailed above are described.Type: ApplicationFiled: September 17, 2003Publication date: March 18, 2004Inventors: Thomas Rapold, Gottfried Seifert, Marcel Senn
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Patent number: 6703403Abstract: A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.Type: GrantFiled: September 20, 2001Date of Patent: March 9, 2004Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Dale J. Kempf, John M. Leonard, Richard J. Bertz
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Patent number: 6699896Abstract: This invention provides compounds having the structure wherein A is OR5, or R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, R2 is H, alkyl, or aryl; R3 and R4 are halo, H, alkyl, aryl, trifluoromethyl, alkoxyaryl, nitro, amino, carboalkoxy, carbamide, carbamate, urea, alkylsulfonamide, —NR7(CH2)mCO2H, arylsulfonamide, cycloalkyl, or a heterocycle; R5 is H, alkyl, —CH(R8)R9, —CH2(CH2)nCO2R10, —C(CH3)2CO2R10, —CH(R8)(CH2)nCO2R10, —CH(R8)C6H4CO2R10, or —CH2-tetrazole; R6 is H, alkyl, halo, alkoxy, trifluoroalkyl or trifluoroalkoxy; R7 is H or alkyl; R8 is H, alkyl, aryl, arylalkyl, cycloalkyl, phthalic acid, R9 is CO2R12, CONHR12, tetrazole, or PO3R12; R10 is H, alkyl, aryl, or aralkyl; R11 is alkyl; R12 is H, alkyl, aryl, or aralkyl; X is O, or S; Y is O, N, or S; Z is C, or N; Q is O, N, or S; m=1-3; n=1-6, or a pharmaceutically acceptable salt thereof, whichType: GrantFiled: May 10, 1999Date of Patent: March 2, 2004Assignee: WyethInventor: Michael S. Malamas
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Patent number: 6699898Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.Type: GrantFiled: May 23, 2002Date of Patent: March 2, 2004Assignee: Pharmacia COrporation Global Patent DepartmentInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040039033Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: December 10, 2002Publication date: February 26, 2004Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
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Publication number: 20040029883Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.Type: ApplicationFiled: November 19, 2002Publication date: February 12, 2004Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
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Publication number: 20040030149Abstract: There are described a process for the preparation of a compound of formula 1Type: ApplicationFiled: June 12, 2003Publication date: February 12, 2004Inventors: Dominik Faber, Oliver Desponds, Thomas Rapold, Marco Passafaro
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Publication number: 20040019090Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: 1Type: ApplicationFiled: May 7, 2003Publication date: January 29, 2004Applicants: Eli Lilly & Company, Ligand Pharmaceuticals, Inc.Inventors: Dawn A. Brooks, Christopher J. Rito, Anthony J. Shuker, Samuel J. Dominianni, Alan M. Warshawsky, Lynn S. Gossett, Donald P. Matthews, David A. Hay, Robert J. Ardecky, Pierre-Yves Michellys, John S. Tyhonas
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6673927Abstract: The present invention is directed to compounds of the wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.Type: GrantFiled: November 20, 1996Date of Patent: January 6, 2004Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S.Inventors: Thomas D. Gordon, Barry A. Morgan
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Patent number: 6667404Abstract: A retroviral protease inhibiting compound of the formula: is disclosed.Type: GrantFiled: February 7, 2003Date of Patent: December 23, 2003Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing Leung Sham, Chen Zhao, Thomas J. Sowin, Daniel S. Reno, Anthony R. Haight
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Publication number: 20030208067Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: May 28, 2002Publication date: November 6, 2003Inventors: Sheldon Xiaodong Cao, David Paul Dumas, Xiaohua Chen, Jae Young Yang
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Patent number: 6642379Abstract: Benzamide derivatives represented by the general formula (I): and insecticides for agricultural and horticultural use and usage thereof, wherein Z1 is O or S; R is H, (substituted) alkyl, or alkoxycarbonyl; X is halogeno, cyano, nitro, C3-C6(halo)cycloalkyl, (substituted) phenyl, a (substituted) heterocyclic group, or —A1—R1 [wherein A1 is —O—, —S—, —SO—, —SO2—, —C(═O)—, or —C(═NOR2)— (wherein R2 is H, C1-C6(halo)alkyl, (substituted) phenylated C1-C4 alkyl, or the like); and R1 is halogeno, C3-C6 cycloalkyl, C3-C6 halocycloalkenyl, (substituted) phenyl, or the like]; n is 0 to 4; Y is halogeno, cyano, nitro, C3-C6 halocycloalkyl, (substituted) phenyl, or the like; m is 1 to 5; Q is a heterocycle such as oxazoline; and B1 to B4 are each CH or N.Type: GrantFiled: April 4, 2002Date of Patent: November 4, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
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Patent number: 6620799Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, m, p, R1, R2, R3, and R4 are as defined in the specification.Type: GrantFiled: September 27, 2001Date of Patent: September 16, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Publication number: 20030171349Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.Type: ApplicationFiled: February 28, 2003Publication date: September 11, 2003Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
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Publication number: 20030166689Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme.Type: ApplicationFiled: April 1, 2003Publication date: September 4, 2003Inventors: Guido Kurz, Marianne Nilsson
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Publication number: 20030162771Abstract: The present invention relates to compounds of formula: 1Type: ApplicationFiled: June 12, 2002Publication date: August 28, 2003Inventors: Michel Geslin, Danielle Gully, Jean-Pierre Maffrand, Pierre Roger
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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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Patent number: 6608095Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 orType: GrantFiled: April 24, 2001Date of Patent: August 19, 2003Assignee: Pfizer Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Publication number: 20030153567Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: ApplicationFiled: January 29, 2003Publication date: August 14, 2003Applicant: SmithKline Beecham CorporationInventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
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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: 20030130520Abstract: A method of producing a compound of formula 1Type: ApplicationFiled: August 22, 2002Publication date: July 10, 2003Inventor: Peter Maienfisch
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Patent number: 6583163Abstract: The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula: [wherein R1 is a phenyl group which may have a lower alkoxy group(s) as a substituent(s) on the phenyl ring, and R2 is a group represented by the following general formula: (wherein R3's, which may be the same or different, are each a carboxyl group, a lower alkoxy group or the like) or the like] and salts thereof.Type: GrantFiled: June 25, 2001Date of Patent: June 24, 2003Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masatoshi Chihiro, Takayuki Matsuzaki, Hisashi Nagamoto, Goro Miyakoda, Shinobu Sueyoshi, Toyoki Mori, Kazuyoshi Kitano, Isao Takemura, Hiroshi Yamashita, Muneaki Kurimura, Fujio Tabusa
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Patent number: 6579892Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.Type: GrantFiled: July 11, 2001Date of Patent: June 17, 2003Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
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Patent number: RE38330Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: August 12, 1999Date of Patent: November 25, 2003Assignee: Alteon Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan