Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/375.1)
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Publication number: 20090062552Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.Type: ApplicationFiled: May 6, 2006Publication date: March 5, 2009Inventors: Thierry Eynard, Cecile Franc
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Patent number: 7491748Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: GrantFiled: August 8, 2002Date of Patent: February 17, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20090036510Abstract: The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2—COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.Type: ApplicationFiled: July 27, 2006Publication date: February 5, 2009Inventors: Janos Fischer, Istvanne Kis-Varga, Gyorgy Szabo, Janos Leibinger
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7476744Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a therapeutically effective amount, wherein the compound is present in the form of solid particles, about 25% to 100% by weight of which are smaller than 1 micrometer. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired. The novel Form I and Form II crystalline forms of celecoxib are described. The crystalline forms have unique chemical and physical properties relative to other solid state forms of celecoxib and are characterized by their powder x-ray diffraction (PXRD) patterns, differential scanning calorimetric (DSC) thermograms, and other physical characterizations.Type: GrantFiled: December 1, 2000Date of Patent: January 13, 2009Assignee: Pfizer Inc.Inventors: Leonard J. Ferro, Patricia S. Miyake
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Publication number: 20080280915Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: November 13, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Publication number: 20080275062Abstract: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consistinType: ApplicationFiled: January 28, 2005Publication date: November 6, 2008Inventors: David Harold Drewry, David Kendall Jung, James Andrew Linn, Robert Neil Hunter, Dennis Lee, Robert A. Stavenger, Clark Sehon
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Patent number: 7442802Abstract: 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: May 5, 2006Date of Patent: October 28, 2008Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20080249150Abstract: Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.Type: ApplicationFiled: June 19, 2008Publication date: October 9, 2008Applicant: WyethInventors: Lynn Resnick, Donna M. Huryn, Joan E. Sabalski, Joshua D. Berkowitz, Anthony Frank Kreft, Dennis Martin Kubrak, Thomas Joseph Caggiano, Koi Michele Morris
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Patent number: 7432285Abstract: The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) 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 optionally, at least one therapeutic agent. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent.Type: GrantFiled: November 15, 2006Date of Patent: October 7, 2008Assignee: NitroMed, Inc.Inventors: Ramani R. Bandarage, Upul K. Bandarage, Xinqin Fang, David S. Garvey, L. Gordon Letts, Joseph D. Schroeder, Sang W. Tam
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Publication number: 20080234491Abstract: There is provided a process for preparation of celecoxib by reacting 4,4,4-trifluoro-1-[4-(methyl)phenyl]butane-1,3-dione with 4-sulphonamidophenylhydrazine or its salt in a solvent medium that contains an alkyl ester. There is also provided a process for the purification of celecoxib using aromatic hydrocarbon solvents.Type: ApplicationFiled: March 19, 2008Publication date: September 25, 2008Inventors: Raghupathi Reddy Anumula, Goverdhan Gilla, Sampath Alla, Thirupathi Reddy Akki, Yakambram Bojja
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Publication number: 20080200693Abstract: The present invention refers to the use of derivatives of aryl (or heteroaryl) azolylcarbinol of general formula (I), and their physiologically acceptable salts, as medicinal products for human and/or animal therapeutics for the treatment of the symptoms of opioid addiction. The preferred compound is cizolirtin citrate.Type: ApplicationFiled: September 7, 2005Publication date: August 21, 2008Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventor: Antonio Jose Farre Gomis
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Publication number: 20080194836Abstract: The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.Type: ApplicationFiled: January 25, 2006Publication date: August 14, 2008Inventors: Tawfik Gharbaoui, Claudia Averbuj, Marlony Carlos, Edward A. Lally, Dipanjan Sengupta, John Robert Fritch
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Publication number: 20080194650Abstract: The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.Type: ApplicationFiled: December 5, 2007Publication date: August 14, 2008Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080119658Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20080114037Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 15, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20080114175Abstract: The present invention is directed to a process for preparing certain cysteine protease inhibitors.Type: ApplicationFiled: September 16, 2005Publication date: May 15, 2008Inventor: Jiayao Li
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Patent number: 7361769Abstract: The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 14, 2005Date of Patent: April 22, 2008Assignee: Schering CorporationInventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7358371Abstract: The present invention comprises a process for the preparation of compounds that possess an affinity for the cannabinoid receptor in the human brain. These compounds are useful as immunomodulators and psychotropic agents in the treatment of thymic disorders, vomiting, myo-relaxation, various types of neuropathy, memory disorders, dyskinesia, migraine, asthma, epilepsy, glaucoma, anticancer chemotherapy, in ischemia and angina, in orthostatic hypotension and in cardiac distress. More specifically, the present invention comprises a process for the preparation of a series of compounds of formula (I): in which R1-R7 and W represent various alkyl groups and the derivatives thereof and are more specifically are defined herein.Type: GrantFiled: October 10, 2006Date of Patent: April 15, 2008Assignee: Sanofi-AventisInventors: Marc Daumas, Philippe Vayron
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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: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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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: 7332608Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: November 9, 2006Date of Patent: February 19, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 7297710Abstract: The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.Type: GrantFiled: July 12, 2006Date of Patent: November 20, 2007Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Philippe Pointeau, Murielle Rinaldi-Carmona
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Patent number: 7294645Abstract: The invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 are as defined herein. The invention also relates to the preparation method thereof and to the use of same in therapeutics.Type: GrantFiled: July 6, 2006Date of Patent: November 13, 2007Assignee: Sanofi-AventisInventors: Francis Barth, Serge Martinez, Murielle Rinaldi-Carmona, Christian Congy
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Patent number: 7271191Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.Type: GrantFiled: April 1, 2004Date of Patent: September 18, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Mark Stuart Chambers, Peter Alan Hunt, Philip Jones, Angus Murray MacLeod, Helen Jane Szekeres, Martin Richard Teall
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Patent number: 7253170Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: June 28, 2006Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Patent number: 7247628Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein.Type: GrantFiled: November 4, 2003Date of Patent: July 24, 2007Assignees: Pfizer, Inc., Pfizer Products, Inc.Inventors: Robert L. Dow, Marlys Hammond
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Patent number: 7241793Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:Type: GrantFiled: June 18, 2003Date of Patent: July 10, 2007Assignee: SmithKline Beecham CorporationInventors: Nerina Dodic, Bernard André Dumaître, Francoise Jeanne Gellibert, Michael Lawrence Sierra
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Patent number: 7235690Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: April 26, 2002Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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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: 7211598Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone 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 therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, 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 having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated.Type: GrantFiled: June 30, 2003Date of Patent: May 1, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, Ramani R. Ranatunge, Stewart K. Richardson
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Patent number: 7208528Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: September 15, 1999Date of Patent: April 24, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7192906Abstract: Substituted pyrazole compounds of the formula (1). The compounds are synthesized from a pyrazole derivative and a haloalkyleneoxime ester derivative, and have excellent herbicidal effects.Type: GrantFiled: December 18, 2002Date of Patent: March 20, 2007Assignee: SDS Biotech K.K.Inventors: Yoji Hirohara, Eiji Ikuta, Sayo Osanai, Hideki Nakashima, Teruhiko Ishii
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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: 7179825Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aType: GrantFiled: March 16, 2005Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 7151113Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: May 3, 2004Date of Patent: December 19, 2006Assignee: Bristol Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7138414Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.Type: GrantFiled: July 11, 2003Date of Patent: November 21, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
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Patent number: 7122547Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2006Assignees: Schering AG, Novartis AGInventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
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Patent number: 7109349Abstract: A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers. The process involves the asymmetric addition of a metalated phenyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield Cizolirtine or its enantiomers.Type: GrantFiled: January 24, 2005Date of Patent: September 19, 2006Assignee: Laboratorios Del Dr. Esteve, S/AInventors: Antoni Torrens Jover, Helmut H. Buschmann, Stefan Dahmen, Matthias Lormann
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7045532Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.Type: GrantFiled: October 31, 2001Date of Patent: May 16, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
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Patent number: 7041833Abstract: A process and intermediate useful for forming a 1H-Pyrazolo[1,5-b][1,2,4]triazole compounds comprise the step of reacting a 1,5-diaminopyrazole bearing a substituent, bonded to one and only one of the amine nitrogens by an acyl or thioacyl group, with a dehydrating agent in the presence of an aprotic solvent.Type: GrantFiled: April 23, 2004Date of Patent: May 9, 2006Assignee: Eastman Kodak CompanyInventor: Catherine Mineur
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Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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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: 7001917Abstract: This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglandin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: April 9, 2003Date of Patent: February 21, 2006Assignee: Warner Lambert Company LLCInventors: Misato Hirano, Kazunari Nakao, Seiji Nukui, Tatsuya Yamagishi