Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/376.1)
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Publication number: 20080207853Abstract: Compounds are provided that are useful as precatlysts in the polymerization of olefins such as ethylene and propylene. Other compounds are useful as intermediates in the production of such precatalysts.Type: ApplicationFiled: February 23, 2007Publication date: August 28, 2008Inventors: Omofolami Tesileem Ladipo, Richard Eaves, Alexey Zazybin, Sean Parkin
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Patent number: 7396850Abstract: The present invention is directed to a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.Type: GrantFiled: December 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Daniel Ray Mayhugh, Guoxin Zhu
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Publication number: 20080085904Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: July 14, 2005Publication date: April 10, 2008Inventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7342037Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: June 9, 2006Date of Patent: March 11, 2008Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20080045511Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: August 15, 2007Publication date: February 21, 2008Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
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Patent number: 7312350Abstract: The invention relates to a process for preparing arylvinyl halides and sulphonates and arylalkynes by reacting haloaromatics or aryl sulphonates with vinyl halides or sulphonates in the presence of a palladium catalyst and a base and, if appropriate, subsequent elimination.Type: GrantFiled: January 5, 2004Date of Patent: December 25, 2007Assignee: LANXESS Deutschland GmbHInventors: Wolfgang Ebenbeck, Florian Rampf
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Patent number: 7309712Abstract: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.Type: GrantFiled: November 3, 2006Date of Patent: December 18, 2007Assignee: Pfizer LimitedInventors: Paul Anthony Bradley, Kevin Neil Dack, Patrick Stephen Johnson, Sarah Elizabeth Skerratt
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Patent number: 7244753Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, 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 therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: GrantFiled: July 29, 2003Date of Patent: July 17, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder
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Patent number: 7220867Abstract: The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention.Type: GrantFiled: July 26, 2005Date of Patent: May 22, 2007Assignee: Pharmacia Corporation (of Pfizer, Inc.)Inventors: Michael J. Hageman, Xiaorong He, Tugrul T. Kararli, Lesley A. MacKin, Patricia J. Miyake, Brian R. Rohrs, Kevin J. Stefanski
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Patent number: 7183306Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.Type: GrantFiled: November 14, 2003Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
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Patent number: 7153330Abstract: The present invention relates to a composition for the oxidation dyeing of keratin fibers, in particular of human keratin fibers such as the hair, comprising at least one oxidation base chosen from 4,5- or 3,4-diaminopyrazoles and triaminopyrazoles, in combination with at least one selected mineral compound, and also to the dyeing process using this composition with an oxidizing agent.Type: GrantFiled: November 26, 2001Date of Patent: December 26, 2006Assignee: L'OrealInventor: Jean Cotteret
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Patent number: 7144911Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: December 24, 2003Date of Patent: December 5, 2006Assignee: Deciphera Pharmaceuticals LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 7141585Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.Type: GrantFiled: April 26, 2004Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
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Patent number: 7115575Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.Type: GrantFiled: July 28, 2005Date of Patent: October 3, 2006Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
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Patent number: 7112601Abstract: Compounds of Formula I are disclosed which inhibit hepatitis C NS5B RNA-dependent RNA polymerase and are useful for treating hepatitis C.Type: GrantFiled: August 19, 2004Date of Patent: September 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Brent D. Douty, Scott W. Martin, Jeffrey Romine
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Patent number: 7094906Abstract: The present invention relates to processes for the preparation of a compound of the formula wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen or halogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2; and processes for using a compound of the formula (I) in the synthesis of compounds of the formulaType: GrantFiled: November 10, 2003Date of Patent: August 22, 2006Assignee: Basf Agro B.V. Arnthem (NL) Wädenswil-BranchInventor: Jean-Erick Ancel
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Patent number: 7074867Abstract: A compound having the general formula (I): ?O3S—R1—V1—R2—V2 wherein R1 is a hydrocarbon radical comprising C1 to C10 main chain carbon atoms, wherein hydrogen atoms bonded to the main chain carbon atoms are optionally substituted; R2 is a hydrocarbon radical comprising 6 to 20 main chain carbon atoms, wherein hydrogen atoms bonded to the main chain carbon atoms are optionally substituted; V1 is a saturated or unsaturated, monocyclic or bicyclic ring system comprising 5 to 9 ring atoms, wherein at least 2 ring atoms are nitrogen atoms forming the same cyclic moiety; and V2 is a moiety comprising a carboxyl group and an unsaturated carbon-carbon bond.Type: GrantFiled: November 21, 2003Date of Patent: July 11, 2006Assignee: Agency for Science, Technology and ResearchInventors: Leong Ming Gan, Pei Yong Chow
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Patent number: 7056892Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.Type: GrantFiled: July 27, 2005Date of Patent: June 6, 2006Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
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Patent number: 7037931Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators.Type: GrantFiled: July 2, 2003Date of Patent: May 2, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Terrance D. Barrett, J. Guy Breitenbucher, Laurent Gomez, Michael D. Hack, Liming Huang, Kelly J. McClure, Magda F. Morton, Clark A. Sehon, Nigel P. Shankley
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Patent number: 7026346Abstract: Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-smalll cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including hormone-refractory prostate cancer. Further provided are methods of treating cancer in a subject in need of such treatment using the compounds of the present invention. Further provided are methods for using the compounds of the present invention to treat, inhibit, or delay the onset of cancer in a subject. Further provided are methods of inducing apoptosis in rapidly proliferating cells, particularly, though not necessarily cancer cells, using the compounds of the present invention.Type: GrantFiled: April 8, 2003Date of Patent: April 11, 2006Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Xueqin Song, Ho-Pi Lin
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Patent number: 7009056Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.Type: GrantFiled: February 5, 2001Date of Patent: March 7, 2006Assignee: University College LondonInventors: Giti Garthwaite, David Selwood, Marcel Kling, Grant Wishart
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Patent number: 6972283Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.Type: GrantFiled: January 20, 2004Date of Patent: December 6, 2005Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
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Patent number: 6964978Abstract: The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention.Type: GrantFiled: December 6, 2000Date of Patent: November 15, 2005Assignee: Pharmacia CorporationInventors: Michael J. Hageman, Xiaorong He, Tugrul T. Kararli, Lesley A. Mackin, Patricia J. Miyake, Brian R. Rohrs, Kevin J. Stefanski
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Patent number: 6949578Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.Type: GrantFiled: July 14, 2004Date of Patent: September 27, 2005Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
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Patent number: 6927232Abstract: This invention relates to the treatment of mGluR5 receptor mediated disorders, which comprises administering to a person in need of treatment a compound having the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH?CH— or —C?C—; and B signifies wherein R6 to R26, X and Y are as defined herein.Type: GrantFiled: April 4, 2003Date of Patent: August 9, 2005Assignee: Hoffman-La Roche Inc.Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 6906196Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted arylType: GrantFiled: September 18, 2002Date of Patent: June 14, 2005Assignee: Onconova Therapeutics, Inc.Inventors: M. V. Ramana Reddy, Stanley C. Bell
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6872741Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).Type: GrantFiled: September 11, 2003Date of Patent: March 29, 2005Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
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Publication number: 20040192930Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.Type: ApplicationFiled: November 3, 2003Publication date: September 30, 2004Applicant: G.D. Searle & Co.Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter, Stephen H. Docter, Stella S. Yu
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Patent number: 6797723Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.Type: GrantFiled: April 24, 2002Date of Patent: September 28, 2004Assignee: Eli Lilly and CompanyInventors: Jason Scott Sawyer, Douglas Wade Beight, Edward C R Smith, William Thomas McMillen
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Publication number: 20040171781Abstract: A compound having the general formula (I):Type: ApplicationFiled: November 21, 2003Publication date: September 2, 2004Inventors: Leong Ming Gan, Pei Yong Chow
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Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
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Patent number: 6750230Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.Type: GrantFiled: July 5, 2001Date of Patent: June 15, 2004Assignee: Pfizer, Inc.Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
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Publication number: 20040053985Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, 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 therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: ApplicationFiled: June 25, 2003Publication date: March 18, 2004Applicant: NitroMed, Inc.Inventors: Upul K. Bandarage, Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunga, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 6696477Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation. Compounds of particular interest are defined by Formula I wherein A, Y, R1, R2, R3, R4 and R5 are as defined in the specification.Type: GrantFiled: November 29, 2001Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas
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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: 6673818Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: April 16, 2002Date of Patent: January 6, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Patent number: 6610726Abstract: The invention is directed to pharmaceutical compositions containing small organic molecules having the ability to mimic or agonize hepatocyte growth factor/scatter factor (HGF/SF) activity, useful for promoting, for example, vascularization of tissues or organs for promoting wound or tissue healing, or augmenting or restoring blood flow to ischemic tissues such as the heart following myocardial infarction.Type: GrantFiled: December 19, 2001Date of Patent: August 26, 2003Assignee: North Shore-Long Island Jewish Research InstituteInventors: Sivaram Pillarisetti, Itzhak D. Goldberg
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Patent number: 6603012Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.Type: GrantFiled: April 23, 2001Date of Patent: August 5, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6596752Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: July 12, 2002Date of Patent: July 22, 2003Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Patent number: 6596879Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.Type: GrantFiled: June 11, 2002Date of Patent: July 22, 2003Assignee: Warner-Lambert CompanyInventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6548529Abstract: aP2 inhibiting compounds are provided having the formula wherein R1, R2, R3, R4, X-Z and are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: March 6, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Richard B. Sulsky, David R. Magnin
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Publication number: 20030022925Abstract: Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two substituents, and their physiologically acceptable salts; are useful as drugs in human and/or veterinary therapeutics to treat urinary incontinence in mammals, including man.Type: ApplicationFiled: July 3, 2002Publication date: January 30, 2003Applicant: Laboratorios del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 6500950Abstract: Benzylidenepyrazolones of the formula I, where the substituents and the index n have the following meanings: R1 is unsubstituted or substituted C1-C6-alkyl; R2 is unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, halogen, nitro, cyano; R3 is hydrogen, halogen, nitro, cyano, a group NR5R6, OCOR5, NR5COR6, CO2R5, —COSR5, —CONR5R6, C1-C4-alkoxyiminoalkyl, C1-C6-alkylcarbonyl, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, unsubstituted or substituted C1-C6-alkylthio, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, an unsubstituted or substituted 5- or 6-membered saturated or unsaturated heterocycle which may contain up to 4 nitrogen atoms and/or up to 2 oxygen or sulfur atoms as ring members; R4 is C1-C6-alkyl, C1-C4-haloalkyl; R3 and R4 form an optionally substituted saturated or unsaturatedType: GrantFiled: January 22, 2001Date of Patent: December 31, 2002Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Matthias Witschel, Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20020173662Abstract: Compounds of formula (I): 1Type: ApplicationFiled: April 29, 2002Publication date: November 21, 2002Inventor: Bernard Joseph Banks
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Patent number: 6458803Abstract: 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: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: 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: 6444612Abstract: A method of controlling a plant disease caused by a fungus comprising applying a 5-amino-pyrazole of the formula wherein, R1, R2, R3, R4, R5 and Y are as defined in the specification.Type: GrantFiled: February 20, 2001Date of Patent: September 3, 2002Assignee: Bayer AktiengesellschaftInventors: Markus Heil, Thomas Bretschneider, Hans-Christian Militzer, Astrid Mauler-Machnik, Klaus Stenzel
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Patent number: 6436967Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.Type: GrantFiled: September 14, 2000Date of Patent: August 20, 2002Assignee: Pharmacia CorporationInventors: John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier