Nitrogen Attached Directly To The Triazole Ring By Nonionic Bonding Patents (Class 548/264.8)
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Patent number: 7888380Abstract: 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.Type: GrantFiled: October 6, 2005Date of Patent: February 15, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Shenlin Huang, Ronghui Lin, Peter J. Connolly, Stuart L. Emanuel, Steven A. Middleton, Robert H. Gruninger, Steven K. Wetter
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Patent number: 7872036Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.Type: GrantFiled: October 20, 2005Date of Patent: January 18, 2011Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Keiji Toriyabe, Mikio Yamaguchi, Yoshihiro Ito, Shiori Kinpara, Hiroyuki Yano, Satoru Takahashi, Norihisa Yonekura, Ryuji Hamaguchi
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Publication number: 20100330069Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20100324053Abstract: The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: March 18, 2009Publication date: December 23, 2010Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Pauline Carol Stanislawski, Wei Zhuang, Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van Den Keybus
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Patent number: 7851495Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.Type: GrantFiled: May 22, 2007Date of Patent: December 14, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
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Patent number: 7825278Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.Type: GrantFiled: May 5, 2005Date of Patent: November 2, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Patent number: 7776898Abstract: The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.Type: GrantFiled: September 18, 2007Date of Patent: August 17, 2010Assignee: The Curators of the University of MissouriInventors: William J. Welsh, Seong Jae Yu, Anil Nair
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Publication number: 20100196357Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: January 21, 2010Publication date: August 5, 2010Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Patent number: 7745472Abstract: There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C?O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.Type: GrantFiled: March 27, 2008Date of Patent: June 29, 2010Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Lok Wai Lawrence Woo, Atul Purohit, Michael John Reed, Oliver Brook Sutcliffe, Christian Bubert
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Publication number: 20100120874Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: ApplicationFiled: November 4, 2009Publication date: May 13, 2010Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Patent number: 7709469Abstract: The invention is directed to compounds that are P2X7 antagonist and have the formula (I) or (II) or a pharmaceutically acceptable salt, prodrug, salt of a prodrug or a combination thereof, wherein R1, R2, and R3 are defined in the specification. The invention is also directed to a method of selectively inhibiting P2X7 activity comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (III), (IV) or (V) wherein R6, R7, R8, R9, R10, and R11 are defined in the specification.Type: GrantFiled: November 6, 2006Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: William A. Carroll, Alan S. Florjancic, Arturo Perez-Medrano, Sridhar Peddi
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Publication number: 20100004298Abstract: Provided are 5-membered heterocycle-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: ApplicationFiled: September 11, 2009Publication date: January 7, 2010Inventors: Qing Dong, Fabrice Pierre, Jianqiang Wang
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Publication number: 20090312352Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.Type: ApplicationFiled: October 19, 2005Publication date: December 17, 2009Inventors: Tomas Mikael Mustelin, Maurizio Pellecchia, Lutz Tautz
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Publication number: 20090253691Abstract: The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: April 19, 2007Publication date: October 8, 2009Applicants: JANSSEN PHARMACEUTICA N.V., BIOFOCUS DPI LIMITEDInventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Anne Simone Josephine Lesage, Wei Zhuang, Marcel Frans Leopold De Bruyn, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck, Theodorus Dinklo
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Patent number: 7598245Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: April 13, 2007Date of Patent: October 6, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang
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Publication number: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Publication number: 20090215759Abstract: The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: February 16, 2009Publication date: August 27, 2009Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
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Publication number: 20090186895Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: May 17, 2007Publication date: July 23, 2009Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jingdong Xu
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Publication number: 20090076282Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.Type: ApplicationFiled: October 20, 2005Publication date: March 19, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD, IHARA CHEMICAL INDUSTRY CO., LTDInventors: Keiji Toriyabe, Mikio Yamaguchi, Yoshihiro Ito, Shiori Kinpara, Hiroyuki Yano, Satoru Takahashi, Norihisa Yonekura, Ryuji Hamaguchi
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Publication number: 20090049622Abstract: Provided is a hair dye composition containing a dissociative direct dye (1): (wherein Ar represents an aromatic group or heterocyclic aromatic group which may have a substituent, Ar? represents an aromatic group which may be substituted by an alkyl group or an electron drawing group, or a specific heterocyclic aromatic group, and W represents an electron drawing group); or salt thereof.Type: ApplicationFiled: February 3, 2006Publication date: February 26, 2009Applicants: Kao Corporation, Fujifilm CorporationInventors: Kenichi Matsunaga, Hiromi Saimiya, Dominic Pratt, Yasuhiro Ishiwata
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Publication number: 20090018150Abstract: Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.Type: ApplicationFiled: July 23, 2004Publication date: January 15, 2009Applicant: ASTERAND UK LIMITEDInventors: Richard Anthony Borman, Robert Alexander Coleman, Kenneth Lyle Clark, Alexander William Oxford, George Hynd, Janet Ann Archer, Amanda Aley, Neil Victor Harris
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Publication number: 20080286607Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20080287681Abstract: The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.Type: ApplicationFiled: July 16, 2008Publication date: November 20, 2008Inventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Sudhir Srivastava, Goutam Saha
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Publication number: 20080249115Abstract: This invention relates, e.g., to methods for inhibiting or stimulating an activity of an adrenomedullin (AM) or gastrin releasing peptide (GRP) peptide hormone, comprising contacting the peptide with a small molecule, non-peptide, modulatory agent of the invention. Complexes of these modulatory agents with other components, such as the peptides or blocking antibodies specific for the peptides, are also described, as are pharmaceutical compositions comprising the modulatory agents, and methods for using the modulatory agents to diagnose or treat patients.Type: ApplicationFiled: September 8, 2004Publication date: October 9, 2008Applicant: THE GOVERNMENT OF THE UNITED STATES OF AMERICA, ASInventors: Frank Cuttitta, Alfredo Martinez
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Publication number: 20080234252Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2.Type: ApplicationFiled: May 8, 2006Publication date: September 25, 2008Inventors: Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
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Patent number: 7423157Abstract: The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.Type: GrantFiled: August 9, 2006Date of Patent: September 9, 2008Assignee: Basilea Pharmaceutica AGInventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Sudhir Srivastava, Goutam Saha
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Publication number: 20080176840Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: May 25, 2007Publication date: July 24, 2008Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Przewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
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Patent number: 7361677Abstract: There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C?O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.Type: GrantFiled: August 22, 2005Date of Patent: April 22, 2008Assignee: Sterix, Ltd.Inventors: Barry Victor Lloyd Potter, Lok Wai Lawrence Woo, Atul Purohit, Michael John Reed, Oliver Brook Sutcliffe, Christian Bubert
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Patent number: 7329652Abstract: The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 19, 2005Date of Patent: February 12, 2008Assignee: Vertex Pharamaceuticals IncorporatedInventors: Francesco Salituro, Mark Ledeboer, Brian Ledford, Jian Wang, Albert Pierce, John Duffy, David Messersmith
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Patent number: 7317024Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 12, 2006Date of Patent: January 8, 2008Assignee: Bristol-Myers Squibb Co.Inventor: Bingwei V. Yang
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Patent number: 7294720Abstract: The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.Type: GrantFiled: January 23, 2006Date of Patent: November 13, 2007Assignee: The Curators of the University of MissouriInventors: William J. Welsh, Seong Jae Yu, Anil Nair
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Publication number: 20070238710Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Applicant: ARDEA BIOSCIENCESInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
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Patent number: 7279469Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: November 17, 2003Date of Patent: October 9, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Albert C. Pierce, Michael Amost, Robert J. Davies, Cornelia J. Forster, Vincent Galullo, Ronald Grey, Jr., Mark Ledeboer, Shi-Kai Tian, Jinwang Xu, Hayley Binch, Brian Ledford, David Messersmith, Suganthi Nanthakumar, Andrew Jayaraj, Greg Henkel, Francesco G. Salituro, Jian Wang
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Patent number: 7226920Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 6, 2004Date of Patent: June 5, 2007Assignee: Vertex Pharmaceuticals Inc.Inventors: Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang
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Patent number: 7220883Abstract: Process for the preparation of primary amines of formula (I): where R3 represents an alkyl, cycloalkyl or aralkyl group, by reaction of a triazolium salt of formula (II): where R1 and R2 represent hydrogen or an alkyl, aralkyl or aryl group, R4 represents an alkyl or aralkyl group or a residue of an organic polymer functionalized by an alkylating group, and A? represents a halogen, alkylsulphonate, arylsulphonate, alkyl sulphate, hydrogensulphate, hemisulphate, perchlorate or hydroxide, with a hydride, in order to obtain an amine of formula (I), which is isolated, if desired, and intermediates.Type: GrantFiled: July 28, 2003Date of Patent: May 22, 2007Assignee: Clariant (France)Inventors: Muriel Serradeil Albalat, Jean-Claude Vallejos, Christian Roussel, Didier Wilhelm
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Patent number: 7098343Abstract: There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C?O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.Type: GrantFiled: November 20, 2002Date of Patent: August 29, 2006Assignee: Sterix, LimitedInventors: Barry Victor Lloyd Potter, Lok Wai Lawrence Woo, Atul Purohit, Michael John Reed, Oliver Brook Sutcliffe, Christian Bubert
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Patent number: 7045635Abstract: An improved process for synthesizing 4-amino-1,2,4-triazole. Hydrazine hydrate solution is mixed into ethyl formate, ethanol, and an acidic ion exchange resin in a condenser. The solution is held at 75 degrees Celsius until no more liquid exits the condenser. The solution is then heated to between 130 and 133 degrees Celsius and kept at this temperature long enough to remove water and ethanol and to complete the synthesis. The solution is then cooled to 60 degrees Celsius and filtered to remove the ion-exchange resin. The filtered liquid is then cooled to ambient temperature.Type: GrantFiled: January 27, 2004Date of Patent: May 16, 2006Assignee: BWXT Pantex, LLCInventors: William T. Quinlin, Dillard M. Cates
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Patent number: 7045520Abstract: The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.Type: GrantFiled: February 7, 2003Date of Patent: May 16, 2006Assignee: The Curators of the University of MissouriInventors: William J. Welsh, Seong Jae Yu, Anil Nair
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Patent number: 6962936Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: April 26, 2002Date of Patent: November 8, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Francois Maltais
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Patent number: 6946562Abstract: Disclosed is a process for the preparation of a peptoid substituted azole compound comprising reacting an amino functionalized azole compound with a resin bound peptoid oligomer bearing a terminal halogen substituent followed by cleavage of the resultant product from the resin surface using a fluorinated organic acid in an inert solvent.Type: GrantFiled: December 12, 2001Date of Patent: September 20, 2005Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Robert J. Niger, Hans F. Schmitthenner, William J. Sonnefeld, Richard P. Dunlap
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Patent number: 6933390Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.Type: GrantFiled: July 15, 2004Date of Patent: August 23, 2005Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
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Patent number: 6919363Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R8 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: June 9, 2003Date of Patent: July 19, 2005Assignee: Euro-Celtique S.A.Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
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Patent number: 6846838Abstract: Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.Type: GrantFiled: June 17, 2003Date of Patent: January 25, 2005Assignee: Bristol-Myers Squibb CompanyInventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
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Publication number: 20040249150Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: June 29, 2004Publication date: December 9, 2004Applicant: Pfizer IncInventors: David W. Piotrowski, Bruce N. Rogers, William W. McWhorter, Daniel Patrick Walker, Jeffrey W. Corbett, Vincent E. Groppi, Daniel G. Rudmann
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Publication number: 20040214817Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 17, 2003Publication date: October 28, 2004Inventors: Albert C. Pierce, Michael Amost, Robert J. Davies, Cornelia J. Forster, Vincent Galullo, Ronald Grey, Mark Ledeboer, Shi-Kai Tian, Jinwang Xu, Hayley Binch, Brian Ledford, David Messersmith, Suganthi Nanthakumar, Andrew Jayaraj, Greg Henkel, Francesco G. Salituro, Jian Wang
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Patent number: 6806282Abstract: The present invention relates to novel branched substituted amino derivatives of 3-amino-1-phenyl-1H-[1,2,4]triazole, processes for their preparation and pharmaceutical compositions comprising them.Type: GrantFiled: June 12, 2002Date of Patent: October 19, 2004Assignee: Sanofi-SynthelaboInventors: Michel Geslin, Danielle Gully, Jean-Pierre Maffrand, Pierre Roger
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Publication number: 20040142985Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: ApplicationFiled: May 15, 2003Publication date: July 22, 2004Inventors: Rajinder Singh, Dane Goff, John Partridge
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Publication number: 20040142995Abstract: Disclosed are thermally-stable, anthraquinone colorant compounds (dyes) which contain one or more vinyl groups which render the compounds copolymerizable with reactive vinyl monomers to produce colored, polymeric compositions such as acrylate and methacrylate polymeric materials. The compounds possess good fastness (stability) to ultraviolet (UV) light, good solubility in vinyl monomers, good color strength and excellent thermal stability. Also disclosed are (1) coating composition comprising (i) one or more polymerizable vinyl compounds, (ii) one or more of the dye compounds described above, and (iii) a photoinitiator and (2) polymeric materials, i.e., polymers derived from one or more acrylic acid esters, one or more methacrylic acid esters, one or more other polymerizable vinyl compounds or mixtures of any two or more thereof, having copolymerized therein one or more of the anthraquinone colorant compounds.Type: ApplicationFiled: December 12, 2003Publication date: July 22, 2004Inventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook, Jos Simon De Wit, Larry Keith Johnson
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Publication number: 20040106607Abstract: The present invention relates to new compounds of formula I, 1Type: ApplicationFiled: August 8, 2003Publication date: June 3, 2004Applicant: AstraZeneca AB and NPS Pharmaceuticals, Inc.Inventors: Jalaj Arora, Louise Edwards, Methvin Isaac, Abdelmalik Slassi, Tomislav Stefanac, David Wensbo, Tao Xin
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Publication number: 20040106795Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: September 29, 2003Publication date: June 3, 2004Inventors: Ajita Bhat, Siegfried B. Christensen IV, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li