Benzene Ring Bonded Directly To The Diazole Ring Patents (Class 548/377.1)
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Publication number: 20110038835Abstract: Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: February 17, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Xingang Fang, Yen ting Chen, Yan Yin, Michael P. Smolinski, Lei Yao, Bo Wang, Hampton Sessions
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Publication number: 20110040094Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.Type: ApplicationFiled: September 15, 2008Publication date: February 17, 2011Applicant: ENVIVO PHARMACEUTICALS, INC.Inventors: Gideon Shapiro, Richard Chesworth
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Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
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Publication number: 20110028485Abstract: 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: September 16, 2010Publication date: February 3, 2011Inventors: Hans-Michael EGGENWEILER, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Patent number: 7879897Abstract: The invention relates to 5-sub-stituted-oxyalkylaminopyrazole derivatives of the formula or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests including arthropods and helminths.Type: GrantFiled: August 21, 2004Date of Patent: February 1, 2011Assignee: Merial LimitedInventors: David Teh-Wei Chou, Stefan Schnatterer, Werner Knauf, Karl Seeger
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Publication number: 20110021592Abstract: The present invention provides a process for preparing a redispersible powder of nanoparticles of a water-insoluble organic compound, the process including the steps of: (i) preparing an oil-in-water microemulsion comprising a water-insoluble organic compound, a volatile water-immiscible organic solvent, water, and at least one surfactant; and (ii) removing the volatile water-immiscible organic solvent and the water so as to form the redispersible powder comprising said nanoparticles, wherein the nanoparticle are in a particulate form, and wherein the solubility of the water-insoluble organic compound is at least about 5 times greater than the solubility of the water-insoluble organic compound in unprocessed form. Step (i) can further include the addition of co-solvent or polymer.Type: ApplicationFiled: September 16, 2007Publication date: January 27, 2011Inventors: Shlomo Magdassi, Hadas Netivi, Katrin Goshen
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Publication number: 20110003817Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc forms a saturated or unsaturated 5- or 6-membered hetero ring; and B is a substituted or unsubstituted pyrazole, imidazole, pyridine, or piperidine; with the proviso that at least one of R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1?X2?Y1?N and X3?CR2.Type: ApplicationFiled: February 6, 2009Publication date: January 6, 2011Applicant: SHISEIDO COMPANY LTD.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Patent number: 7863313Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.Type: GrantFiled: April 7, 2004Date of Patent: January 4, 2011Assignee: Cortical PTY LTDInventors: Eric Francis Morand, Magdy Naguib Iskander, Colin Edward Skene
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Publication number: 20100331540Abstract: A method for producing a compound having a deuterated aromatic ring or heterocyclic ring according to the invention includes heating a compound having an aromatic ring or heterocyclic ring in the presence of heavy water, a transition metal and a metal which generates deuterium. As the metal which generates deuterium, at least one metal selected from the group consisting of aluminum, magnesium, zinc, iron, lead and tin is preferred. As the transition metal, at least one metal selected from the group consisting of platinum, palladium, ruthenium and rhodium is preferred. The heating is preferably carried out by microwave irradiation.Type: ApplicationFiled: January 30, 2009Publication date: December 30, 2010Inventors: Haruki Shimodaira, Toshifumi Abe, Akira Miyazawa, Yuji Kawanishi, Taichi Abe
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Publication number: 20100331295Abstract: Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: June 26, 2006Publication date: December 30, 2010Applicant: EXELIXIS, INC.Inventors: Brett B Busch, Brenton T. Flatt, Xiao Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin Schweiger, William C. Stevens, JR., Tie Lin Wang, Yinong Xie
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Publication number: 20100324001Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.Type: ApplicationFiled: June 30, 2010Publication date: December 23, 2010Applicant: Cortical Pty LTDInventors: Eric Francis Morand, Magdy Naguib Iskander, Colin Edward Skene
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Publication number: 20100305181Abstract: In accordance with the present invention, there are provided novel compounds that have a variety of properties, i.e., antioxidant, anti-inflammatory, antiviral, antibacterial, and antifungal properties. Invention compounds, therefore, have the ability to impart a variety of beneficial physiological effects, e.g., to protect neurons and/or to promote neuroregeneration and/or to promote memory formation and/or to act as protein phosphatase or kinase inhibitors and/or to act as lipoxygenase inhibitors. Such compounds are useful for treatment of a variety of indications, including neurodegenerative diseases and conditions, diabetes, ischemia associated with heart disease, and memory deficit. In another aspect of the present invention, there are also provided formulations containing one or more of the above-described compounds, optionally further containing additional neurologically active compound(s) and/or adjuvants to facilitate delivery thereof across the blood/brain barrier.Type: ApplicationFiled: October 14, 2008Publication date: December 2, 2010Inventor: David R. Schubert
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Publication number: 20100298569Abstract: The invention relates to the use of cyclovinyl phosphine compounds in the form of complexes with copper, as catalysts for reactions leading to the formation of carbon-carbon and carbon-heteroatom bonds. The invention also relates to complexes of copper with at least one cyclovinyl phosphine, as well as to the method for creating a carbon-carbon or a carbon-heteroatom bond catalysed by a cyclovinyl phosphine/copper complex.Type: ApplicationFiled: September 26, 2008Publication date: November 25, 2010Inventors: Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani
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Publication number: 20100267964Abstract: The invention relates to novel intermediates for the preparation of N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure.Type: ApplicationFiled: May 27, 2010Publication date: October 21, 2010Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Stefan Lehr, Klaus Kunz, Jorg Konze, Olga Malsam, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi, Guido Bojack, Thomas Auler, Martin Hills, Heinz Kehne
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Publication number: 20100261772Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.Type: ApplicationFiled: May 24, 2010Publication date: October 14, 2010Inventors: Jing Fang, Dennis Heyer, Subba Reddy Katamreddy, Kenneth William Batchelor, Richard Dana Caldwell
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Patent number: 7812176Abstract: 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: GrantFiled: July 21, 2004Date of Patent: October 12, 2010Assignee: Arena Pharmaceuticals, Inc.Inventors: John Robert Fritch, Fiona M. Carleton, Edward A. Lally, Hongmei Li, Bradley Teegarden
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Publication number: 20100249135Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting ofType: ApplicationFiled: December 11, 2007Publication date: September 30, 2010Applicant: THE GENETICS COMPANY, INC.Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Jaschinskin Frank, Guy Lemaillet, Cornelia Marty-Ernest, Elena Marzi, Leonardo Scapozza
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Patent number: 7799818Abstract: Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 17, 2009Date of Patent: September 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Emma R. Parmee, Yusheng Xiong, Jian Guo, Rui Liang, Linda Brockunier
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Publication number: 20100234380Abstract: The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.Type: ApplicationFiled: May 17, 2007Publication date: September 16, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Tawfik Gharbaoui, Dipanjan Sengupta, Ashwin M. Krishnan, Nainesh Shah, Ryan M. Hart, Mark Macias
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Patent number: 7795294Abstract: This invention is directed to a tetrahydro-2H-indazole pyrazole cannabinoid modulator compound of formula (I): or a form thereof, wherein p, R1, R2 and Ar are as herein described and * represents a chiral center, and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: February 13, 2007Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Fina Liotta, Huajun Lu, Michael P. Wachter, Mingde Xia
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Publication number: 20100227846Abstract: The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I?) wherein R1 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R2 is a phenyl group having cyano (the phenyl group may further have substituent(s) other than cyano); R3 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R4 is a cyclic group optionally having substituent(s); and X is methylene optionally having substituent(s), or CO, or a salt thereof.Type: ApplicationFiled: August 27, 2008Publication date: September 9, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Mitsuhiro Ito, Tomohiko Suzaki, Satoshi Tamamoto
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Publication number: 20100227902Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: ApplicationFiled: May 14, 2010Publication date: September 9, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Publication number: 20100210617Abstract: The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two caType: ApplicationFiled: June 21, 2006Publication date: August 19, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Steven John Woodhead, Robert Downham, Christopher Hamlett, Steven Howard, Hannah Fiona Sore, Marinus Leendert Verdonk, David Winter Walker, Richard William Arthur Luke
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Patent number: 7776902Abstract: New compounds able to release COX-2 inhibitors and NO having formula (I): M-T-YA—NO2??(I) for the treatment and/or prophylaxis of inflammatory processes.Type: GrantFiled: June 20, 2003Date of Patent: August 17, 2010Assignee: Nicox S.A.Inventors: Piero Del Soldato, Giancarlo Santus
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Publication number: 20100204206Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 3, 2009Publication date: August 12, 2010Applicant: SANOFI-AVENTISInventors: Thomas BOHME, Uwe GERLACH, Dirk GRETZKE, Heinz-Werner KLEEMANN, Stefania PFEIFFER-MAREK, Henning VOLLERT, Jean-Michel ALTENBURGER, Sergio MALLART
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Publication number: 20100197924Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.Type: ApplicationFiled: December 16, 2009Publication date: August 5, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
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Publication number: 20100184995Abstract: The present invention relates to a process for the production of crystalline particles of a glucagon receptor antagonist compound. The process includes the steps of generating microseeds and subjecting the microseeds to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 mm. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.Type: ApplicationFiled: September 8, 2008Publication date: July 22, 2010Inventors: Benjamin M. Cohen, Daniel J. Kumke, Lushi Tan, Aaron S. Cote
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Patent number: 7759497Abstract: A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.Type: GrantFiled: September 7, 2006Date of Patent: July 20, 2010Assignee: Pfizer Inc.Inventors: Leo J. Letendre, William D. McGhee, Cynthia Snoddy, George Klemm, Henry T. Gaud
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Patent number: 7759291Abstract: The present invention provides a pyrazole compound of formula (a): a noxious arthropod pests controlling composition containing the compound shown by the formula (a) as an active ingredient; and a method for controlling noxious arthropod pests comprising applying an effective amount of the compound shown by the formula (a).Type: GrantFiled: January 25, 2005Date of Patent: July 20, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Hayato Takyo, Masaya Hashizume, Noriyasu Sakamoto
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Publication number: 20100152252Abstract: The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I), wherein K-L-M-N, Z and R1, R2, R3, R4 are as described in the claims methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: December 21, 2007Publication date: June 17, 2010Applicant: LABORATORIOS DEL DR. ESTEVE,S.A.Inventors: Mónica Garcia-López, Antonio Torrens-Jover, Luz Romero-Alonso, Helmut H. Buschmann
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Publication number: 20100152098Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: November 5, 2009Publication date: June 17, 2010Applicant: Mpex Pharmaceuticals, Inc.Inventors: Tomasz Glinka, Olga Rodny, Keith A. Bostian, David M. Wallace, Robert I. Higuchi, Chun Chow, Chi Ching Mak, Gavin Hirst, Brian Eastman
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Publication number: 20100144818Abstract: The present invention relates to compounds corresponding to formula (I): in which Y, R1, R2, R3, R4, R5 and R6 are as defined herein. The present invention also relates to the methods of preparation and the therapeutic applications of the compounds of formula (I).Type: ApplicationFiled: December 3, 2009Publication date: June 10, 2010Applicant: SANOFI-AVENTISInventors: Francis BARTH, Laurent BOULU, Joseph MILLAN, Murielle RINALDI-CARMONA
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Publication number: 20100137338Abstract: Invented are novel pyrazole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: March 28, 2008Publication date: June 3, 2010Inventor: Mark Andrew Seefeld
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NOVEL ORGANOMETALLIC COMPLEXES WHICH EMIT IN THE RED TO GREEN SPECTRAL REGION AND THEIR USE IN OLEDS
Publication number: 20100127215Abstract: Organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm?1, a process for preparing the organometallic complexes, a mixture comprising at least one inventive organometallic complex, the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and specific nitrogen- or phosphorus-substituted triphenylene derivatives and a process for their preparation.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Applicant: BASF SEInventors: Herbert Friedrich Boerner, Hans-Peter Loebl, Josef Salbeck, Elena Popova -
Publication number: 20100120714Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 4, 2008Publication date: May 13, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Bruce Lawrence Finkelstein, Andrew Edmund Taggi, Jefrey Keith Long, Paula Louise Sharpe, Chi-ping Tseng, Stephen Frederick Mccann, Amy X. Ding, Steven Lewis Swann, JR.
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Publication number: 20100121076Abstract: The present invention relates to a method for preparing phosphine butadiene-type ligands, and their use, particularly as catalytic metal ligands used in the reactions leading to the formation of carbon-carbon and carbon-heteroatom bonds.Type: ApplicationFiled: April 21, 2008Publication date: May 13, 2010Applicants: Centre National De La Recherche Scientifique (C.N.R.S.), Ecole Nationale Superieure De Chimie De Montpellier, Universite Sidi Mohammed Ben AbdellahInventors: Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani, Armelle Ouali
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Publication number: 20100113551Abstract: The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.Type: ApplicationFiled: March 14, 2008Publication date: May 6, 2010Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Steven John Woodhead, David Charles Rees, Martyn Frederickson, Kyla Merriom Grimshaw
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Patent number: 7709658Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: July 21, 2006Date of Patent: May 4, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
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Publication number: 20100105684Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.Type: ApplicationFiled: March 28, 2008Publication date: April 29, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut Buschmann
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Patent number: 7700786Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.Type: GrantFiled: February 19, 2002Date of Patent: April 20, 2010Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.Inventors: Kenji Hirai, Atsushi Uchida, Atsuko Watanabe, Taeko Abe, Takuya Ueda, Hiroshi Sakurai
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Publication number: 20100093820Abstract: The present invention relates to crystal forms of 4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonamide and methods for preparation, interconversion, and isolation of such crystals.Type: ApplicationFiled: December 18, 2009Publication date: April 15, 2010Applicant: PHARMACIA & UPJOHN COMPANY LLCInventors: Changquan Sun, Garry O'Connor
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Publication number: 20100035936Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I), methods for their preparation, and compositions comprising these compounds as well as their use for the treatment or prophylaxis of various disorders in humans or animals.Type: ApplicationFiled: February 6, 2008Publication date: February 11, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut Buschmann
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Publication number: 20100010054Abstract: A novel therapeutic agent for amyotrophic lateral sclerosis. A therapeutic agent for amyotrophic lateral sclerosis, including a compound having xanthine dehydrogenase inhibitory action and not acting as a substrate for the purine salvage pathway.Type: ApplicationFiled: July 13, 2007Publication date: January 14, 2010Applicants: NIPPON MEDICAL SCHOOL FOUNDATION, NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITYInventors: Takeshi Nishino, Yasuko Abe, Shinsuke Kato
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Patent number: 7645786Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: December 14, 2006Date of Patent: January 12, 2010Assignee: Pfizer Inc.Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Publication number: 20090326240Abstract: The present invention relates to a process for creating a Carbon-Carbon bond (C—C) or a Carbon-Heteroatom bond (C—HE) by reacting a compound carrying a leaving group with a nucleophilic compound carrying a carbon atom or a heteroatom (HE) that can substitute for the leaving group, creating a C—C or C—HE bond, wherein the reaction takes place in the presence of an effective quantity of a catalytic system comprising iron and copper.Type: ApplicationFiled: July 4, 2007Publication date: December 31, 2009Applicants: Centre National de la Recherche Scientifique (C.N.R.S.), Ecole Nationale Superieure de Chimie de MontpellierInventors: Marc Taillefer, Ning Xia, Armelle Ouali
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Publication number: 20090325974Abstract: 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: April 20, 2007Publication date: December 31, 2009Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Publication number: 20090324569Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: December 31, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20090306055Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a): X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.Type: ApplicationFiled: May 15, 2009Publication date: December 10, 2009Applicant: NIPPON SODA CO., LTD.Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Mitsumasa Takada, Seiichi Ikeyama, Shiro Tsubokura, Yasuyuki Shiinoki, Fumie Shirato, Hiroko Moroe
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Patent number: 7618969Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consistingType: GrantFiled: August 5, 2005Date of Patent: November 17, 2009Assignee: Glaxo Group LimitedInventors: Daniel Marcus Bradley, Kevin Michael Thewlis, Simon Edward Ward
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Publication number: 20090281328Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof; and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.Type: ApplicationFiled: June 2, 2009Publication date: November 12, 2009Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventor: Ching-Shih Chen