Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/301)
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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: 20080262238Abstract: A dendron or dendrimer, which has, as a recurring unit of each branch, a structure of formula (I): wherein TC designates a linkage to a former generation in the direction to a focal point of the dendron or a core of the dendrimer; TT designates a linkage to a next generation in the direction to a terminal; X is a divalent group comprised of at least one heteroatom; L1 and L2 each are a divalent linking group; R is a hydrogen atom or a substituent; and a method of producing a dendron or a dendrimer; and a method of producing a thioacetal compound.Type: ApplicationFiled: March 28, 2005Publication date: October 23, 2008Inventor: Koki Nakamura
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Publication number: 20080255155Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds, compositions and methods for the inhibition of kinase activity. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: October 18, 2007Publication date: October 16, 2008Inventors: Stephane Raeppel, Oscar Saavedra, Stephen Claridge, Arkadii Vaisburg, Frederic Gaudette, Ljubomir Isakovic, Robert Deziel
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Publication number: 20080221127Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: March 5, 2008Publication date: September 11, 2008Inventors: Jack Lin, Patrick Womack, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang
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Publication number: 20080188477Abstract: The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.Type: ApplicationFiled: December 12, 2007Publication date: August 7, 2008Applicant: SANOFI-AVENTISInventors: Joachim BRENDEL, Heinrich Christian ENGLERT, Klaus WIRTH, Michael WAGNER, Jean-Marie RUXER, Fabienne PILORGE
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Publication number: 20080161351Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.Type: ApplicationFiled: August 20, 2004Publication date: July 3, 2008Inventors: Hiroyuki Abe, Jonathan Houze, Hisashi Kawasaki, Frank Kayser, Rajiv Sharma, Samuel Sperry
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Publication number: 20080071084Abstract: Method for preparing compounds of the formula (III) by reacting compounds of the formula (II) with a) an alcoholate or b) an alcohol R1-OH and a base in the presence of a Cu-containing catalyst and of a ligand, where X1-5 are independently of one another either carbon or nitrogen, or in each case two adjacent X1R1, with i=1?6, linked by a formal double bond together O, S, NRH or Nrl. The ligands preferably employed are acyclic and/or cyclic oligo- and polyglycols, oligo- and polyamides or oligo- and polyamine glycols of the general formula (IV) k is an integer >0 and n is an integer >1; X and Y are independently of one another O, NH or NR1.Type: ApplicationFiled: May 30, 2007Publication date: March 20, 2008Inventors: Andreas MEUDT, Bernhard J. Rausch
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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: 7253178Abstract: The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them.Type: GrantFiled: March 27, 2002Date of Patent: August 7, 2007Assignee: Eisai Co., Ltd.Inventors: Hitoshi Harada, Masanobu Shinoda, Richard Clark, Fumiyoshi Matsuura, Eita Emori, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
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Patent number: 7232821Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: GrantFiled: April 7, 2003Date of Patent: June 19, 2007Assignee: Glaxo Group LimitedInventors: Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Xiao Qing Lewell, Alan Naylor, Riccardo Novelli
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Patent number: 7214710Abstract: The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof.Type: GrantFiled: May 24, 2004Date of Patent: May 8, 2007Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Tadeusz Cynkowski, Grazyna Cynkowska, Hong Guo, Paul Ashton
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Patent number: 7211591Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: July 12, 2005Date of Patent: May 1, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 7208500Abstract: The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X1–X5 and R1–R5 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).Type: GrantFiled: August 26, 2004Date of Patent: April 24, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Jihong Lou, Robert Steven Kania, Mingying He
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Patent number: 7205302Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: April 25, 2002Date of Patent: April 17, 2007Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
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Patent number: 7129246Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for, and intermediates used in, their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: November 12, 2002Date of Patent: October 31, 2006Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Timothy Johnson, Michael Stocks
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Patent number: 7115608Abstract: The present invention is concerned among others with compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Q is halo, C1-6 alkyl or C2-6 alkenyl; X is (a-2) with q and r being O and Z being O, S or SO; R1 is aryl; R2 is selected from formyl; C1-6alkyloxycarbonylalkyl; Het2; Het2C1-6alkyl, C1-6alkylthio; C1-6alkyl optionally substituted with one or two substituents each independently selected from hydroxy, and halo; R3 is selected from formyl; C1-6alkyl optionally substituted with one or two C1-6alkyloxy; R4 is hydrogen, with HTV inhibiting propertiesType: GrantFiled: September 18, 2001Date of Patent: October 3, 2006Assignees: Centre National de la Recherche Schentifique, Institute CurieInventors: Jérôme Guillemont, Abdellah Benjahad, Dominique Mabire, Chi Hung N'Guyen, David Grierson, Claude Monneret, Emile Bisagni, Gérard Sanz, Laurence Decrane
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Patent number: 7071175Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds: to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: May 3, 2000Date of Patent: July 4, 2006Assignee: Astrazeneca ABInventors: Marcel Linschoten, Magnus Polla
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Patent number: 7038058Abstract: The present invention relates to a process for continuously preparing 5-alkoxy-substituted oxazoles, in particular for continuously preparing 4-methyl-5-alkoxy-substituted oxazoles and also a process for preparing pyridoxine derivatives.Type: GrantFiled: December 3, 2003Date of Patent: May 2, 2006Assignee: BASF AktiengesellschaftInventors: Harald Rust, Kirsten Burkart, Tillmann Faust, Jochem Henkelmann, Alois Kindler, Christian Knoll, Andre Mohry
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Patent number: 7015320Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrL+X? wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected fromType: GrantFiled: March 18, 2003Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: William A. Nugent, Tai Yue
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Patent number: 6987189Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2–C6 alkyl, and R5 and R6 are each independently H or C1–C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: September 28, 2004Date of Patent: January 17, 2006Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6972294Abstract: Disclosed are novel compounds of formula (I) wherein A1, A2, Ar, R5, R6, R8, M, Q, Y, Z, k, m and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). Such conditions include diabetes and obesity.Type: GrantFiled: April 18, 2000Date of Patent: December 6, 2005Assignee: Novo Nordisk, A/SInventors: Anthony Murray, Per Sauerberg, Lone Jeppesen, Ingrid Pettersson, Paul Stanley Bury
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Patent number: 6949680Abstract: A compound of formula wherein Y represents a pyridyl group, or a phenyl group of formula wherein R3 represents a hydrogen atom, a CF3 group or an alkoxy group, R4 represents a hydrogen atom, an alkyl group, or a CF3 group, R5 represents a hydrogen atom, an alkyl group, a CF3 group or an alkoxy group, and R1 and R2 are the substituents of a terminal alkene of formula wherein R1 represents an alkyl or alkylene group, a mono- or poly-cycloalkyl group, or a phenyl group that optionally includes one or several hetero-atoms of oxygen, nitrogen, phosphorous or sulfur; R2 represents a hydrogen atom, an alkyl or alkylene group, a mono- or poly-cycloalkyl group, or a phenyl group that optionally includes one or several hetero-atoms of oxygen, nitrogen, phosphorous and sulfur.Type: GrantFiled: October 15, 2002Date of Patent: September 27, 2005Assignee: Firmenich SAInventor: Andreas Herrmann
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Patent number: 6939875Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.Type: GrantFiled: November 2, 2004Date of Patent: September 6, 2005Assignee: Warner-Lambert CompanyInventors: Bruce J. Auerbach, Larry D. Bratton, Gary F. Filzen, Andrew G. Geyer, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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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: 6881845Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.Type: GrantFiled: January 4, 2001Date of Patent: April 19, 2005Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
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Patent number: 6878704Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.Type: GrantFiled: August 2, 2001Date of Patent: April 12, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Steven Aitken, Gerald Brooks, Steven Dabbs, Colin Henry Frydrych, Steven Howard, Eric Hunt
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Patent number: 6875780Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.Type: GrantFiled: January 22, 2003Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: Bruce J. Auerbach, Larry D. Bratton, Gary F. Filzen, Andrew G. Geyer, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 6872690Abstract: The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I): wherein R1, R3, A, X, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to novel compounds of formula I as well as to herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: March 1, 2002Date of Patent: March 29, 2005Assignee: WYETHInventor: Thomas Maier
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Patent number: 6846830Abstract: Use of compounds of the formula (I) where A, E, R1, R2, p and q have the meanings given in the specification are GluR6 antagonists useful for the treatment of disorders of the central nervous system.Type: GrantFiled: March 19, 2001Date of Patent: January 25, 2005Assignee: Eli Lilly and CompanyInventors: Stephen Richard Baker, David Bleakman, Carlos Lamas-Peteira
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Patent number: 6806371Abstract: A process for preparing substituted pyridine N-oxide compounds of the formula in which R1, R2, R3 and R4 are each H, a carboxyl group or a C1-C12-alkyl radical which may contain atoms from the group of N, O and S, or R1 and R2 and/or R3 and R4 together may each form an optionally substituted C4-C20-alkylene radical which may contain atoms from the group of N, O and S, A is benzyl or a (CH2)m group where m may be an integer from 1 to 12, Z1 and Z2 are each independently O or S, and Y is H, a C1-C12-alkyl radical which may optionally contain atoms from the group of N, O and S, a C6-C20-aryl radical or a C5-C20-heterocycle, and the radicals may optionally be substituted, or Z2 and Y together form an optionally substituted ring or ring system, in which case the ring or ring system may contain atoms from the group of N, O and S, from the corresponding 4-halopyridine N-oxide of the formula in which X is chlorine, bromine or iodine, by reacting the compound of the formula (II)Type: GrantFiled: October 1, 2003Date of Patent: October 19, 2004Assignee: DSM Fine Chemicals Austria Nfg GmbH & Co KGInventors: Thomas Zich, Wolfgang Schiek, Markus Rössler, Christian Seifter
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Patent number: 6794396Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.Type: GrantFiled: March 31, 2003Date of Patent: September 21, 2004Assignee: Pharmacia CorporationInventors: Len F. Lee, Kevin C. Glenn, Daniel T. Connolly, David G. Corley, Daniel L. Flynn, Ashton T. Hamme, Shridhar G. Hegde, Michele A. Melton, Roger J. Schilling, James A. Sikorski, Nancy N. Wall, Jeffery A. Zablocki
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Publication number: 20040176605Abstract: 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: October 10, 2003Publication date: September 9, 2004Applicant: 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: 6787562Abstract: Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R1, X and D are as defined in the specification, methods of making such compounds, methods of using such compounds and pharmaceutical compositions containing such compounds.Type: GrantFiled: October 31, 2002Date of Patent: September 7, 2004Assignee: Zeneca Ltd.Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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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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Patent number: 6765019Abstract: The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof.Type: GrantFiled: May 4, 2000Date of Patent: July 20, 2004Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Tadeusz Cynkowski, Grazyna Cynkowska, Hong Guo, Paul Ashton
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Publication number: 20040106652Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.Type: ApplicationFiled: July 10, 2003Publication date: June 3, 2004Applicant: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li
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Patent number: 6723853Abstract: A method of synthesizing a compound having the formula: from a compound having the formula: wherein R1 is hydrogen, fluorine, chlorine or SiR5R6R7, wherein R5, R6, and R7 are independently the same or different an alkyl group or an aryl group, R2 is an alkyl group, R3 is a protecting group, R4 is an alkyl group, an allyl group, a propargyl group —CO2H, or a benzyl group, R8 is —CO2R10, wherein R10 is an alkyl group or an aryl group, X1 is OH and X2 is H, includes the step of exposing compound (III) to at least one of an organic acid or an inorganic acid. A compound has the general formula (III).Type: GrantFiled: August 27, 2001Date of Patent: April 20, 2004Assignee: University of PittsburghInventors: Dennis P. Curran, Ana E. Gabarda
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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
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Patent number: 6646130Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonistsType: GrantFiled: July 17, 2002Date of Patent: November 11, 2003Assignee: Merck & Co., Inc.Inventors: Nelo R. Rivera, Christopher J. Welch, Yi Xiao, Nobuyoshi Yasuda
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Publication number: 20030208072Abstract: A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.Type: ApplicationFiled: January 24, 2003Publication date: November 6, 2003Inventors: Guang-Pei Chen, Prasad Koteswara Kapa, Eric M. Loeser, Ulrich Beutler, Werner Zaugg, Michael John Girgis
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Patent number: 6635766Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.Type: GrantFiled: March 28, 1997Date of Patent: October 21, 2003Assignee: Lonza AGInventors: Jean-Paul Roduit, Georges Kalbermatten
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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: 6632946Abstract: The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino[1,2-b]quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.Type: GrantFiled: December 12, 2000Date of Patent: October 14, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Alain Rolland, Christophe Lanco, Gerard Ulibarri
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Patent number: 6624142Abstract: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.Type: GrantFiled: May 9, 2001Date of Patent: September 23, 2003Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Hong Zhao
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Patent number: 6620939Abstract: This disclosure relates to a method for producing and using catalysts in the production of bisphenols, and in particular to a method for producing catalysts which contain poly-sulfur mercaptan promoters, and using these catalysts in the production of bisphenol-A and its derivatives.Type: GrantFiled: September 18, 2001Date of Patent: September 16, 2003Assignee: General Electric CompanyInventors: Jimmy Lynn Webb, James Lawrence Spivack
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Publication number: 20030166941Abstract: A method of making a compound of Formula VI: 1Type: ApplicationFiled: December 16, 2002Publication date: September 4, 2003Inventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6608060Abstract: 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: June 14, 1999Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Patent number: RE39916Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds of their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of suppressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.Type: GrantFiled: November 28, 2005Date of Patent: November 6, 2007Assignee: Warner Lambert CompanyInventors: Bruce J. Auerbach, Larry D. Bratton, Gary Filzen, Andrew G. Geyer, Bharat K. Trivedi, Paul C. Unangst