1,2-diazoles (including Hydrogenated) Patents (Class 548/356.1)
  • Patent number: 8114899
    Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: February 14, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Patent number: 8088810
    Abstract: A metal extractant comprising Formula (1) wherein R5, R6, R7 and R8 each independently are hydrogen, an optionally substituted hydrocarbyl group, an electron withdrawing group, an electron donating group, or one or more of R5 & R6, R6 & R7, R7 & R8 are linked in such way as to form an optionally substituted ring; Y is N or CR9 wherein R9 is hydrogen, an optionally substituted hydrocarbyl, optionally substituted hydrocarbyloxy, optionally substituted hydrocarbyloxycarbonyl, optionally substituted hydrocarbylcarbonyloxy group, optionally substituted optionally substituted mono or dihydrocarbylaminocarbonyl group; Z is N or CR10 wherein R10 is hydrogen, an optionally substituted hydrocarbyl, optionally substituted hydrocarbyloxy, optionally substituted hydrocarbyloxycarbonyl, optionally substituted hydrocarbylcarbonyloxy group, optionally substituted optionally substituted mono or dihydrocarbylaminocarbonyl group; and tautomers or salts thereof, with the proviso that both Y and Z could be N provided
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: January 3, 2012
    Assignee: Cytec Technology Corp.
    Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
  • Patent number: 8063229
    Abstract: The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against various pathogens.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: November 22, 2011
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han
  • Patent number: 8062767
    Abstract: An organic light emitting diode with Ir complex is disclosed in this specification, wherein the Ir complex is used as the phosphorous emitter. The chemical containing pyridyl triazole or pyridyl imidazole functional group is used as the auxiliary monoanionic bidentate ligand in the mentioned Ir complex, so that the CIE coordinate of the mentioned Ir complex is adjustable and the light emitting performance of the Ir complex is improved.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: November 22, 2011
    Inventors: Chien-Hong Cheng, Wei-Hsien Liao, Hung-Hsin Shih, Min-Jie Huang, Ting-Wei Tang
  • Publication number: 20110281875
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Application
    Filed: July 8, 2011
    Publication date: November 17, 2011
    Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
  • Publication number: 20110263626
    Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Application
    Filed: August 28, 2008
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
  • Patent number: 8034124
    Abstract: The subject of the present invention is azo derivatives containing a pyrazolinone unit having the following formula (I), their mesomeric forms, their addition salts with an acid and their solvates and their use for dyeing keratin fibers. The subject of the invention is also a composition for dying keratin fibers comprising at least one azo derivative containing a pyrazolinone unit of formula (I) as direct dye, and the method for dyeing keratin fibers using this composition. The present invention makes it possible in particular to obtain chromatic colors that are resistant to the various attacks to which the hair may be subjected, in particular to shampoos and to light.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: October 11, 2011
    Assignee: L'Oreal S.A.
    Inventors: Aziz Fadli, Eric Metais
  • Patent number: 8026260
    Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
  • Patent number: 8017635
    Abstract: Certain novel phenylalkyl substituted azole derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B, D, E, G, a, b, c, d, and R through R11, inclusively, are folly described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: September 13, 2011
    Assignee: FMC Corporation
    Inventors: John W. Lyga, Frank Zawacki, Larry Y. Zhang
  • Patent number: 8003801
    Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: August 23, 2011
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
  • Patent number: 7968579
    Abstract: Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection.
    Type: Grant
    Filed: October 31, 2006
    Date of Patent: June 28, 2011
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Kyung A Yu, Sun Young Kim, Yeon Jung Song, Kang-Pil Kim, Yun Soo Yoon, Mi Ryeong Han
  • Patent number: 7947726
    Abstract: The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: May 24, 2011
    Assignee: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Nilesh Shah
  • Patent number: 7947685
    Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: May 24, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7943653
    Abstract: This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: May 17, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Mingde Xia, Meng Pan, Michael P. Wachter
  • Patent number: 7906656
    Abstract: This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, and to the preparation of such intermediates.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 15, 2011
    Assignee: Bayer CropScience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
  • Patent number: 7902248
    Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
  • Patent number: 7888289
    Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: February 15, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Darren Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Alain Villier, Pierre Genix, Marie-Claire Grosjean-Cournoyer
  • Patent number: 7888365
    Abstract: Cannabinoid derivatives according to formula (I) are disclosed wherein, X, Y, R1, R2, and W can have the definitions provided herein. Without limitation, use of such compounds, their salts or pro-drug, or compositions containing the compounds, salts, or pro-drug, to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.
    Type: Grant
    Filed: March 3, 2008
    Date of Patent: February 15, 2011
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Himanshu Bhattacharjee, Charles R. Yates, Leslie Stuart
  • Patent number: 7884216
    Abstract: The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same. A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like. The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: February 8, 2011
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
  • Patent number: 7879761
    Abstract: The present invention relates to heteroaroyl-substituted serineamides of the formula I in which the variables A and R1 to R6 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of the compositions comprising these compounds for controlling unwanted plants.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: February 1, 2011
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Rack, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt
  • Patent number: 7868204
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: January 11, 2011
    Assignee: MethylGene Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Patent number: 7867949
    Abstract: A hydrazide compound represented by the formula (1): has excellent pesticidal activity.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: January 11, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
  • Patent number: 7855222
    Abstract: A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy, substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: December 21, 2010
    Assignees: UBE Industries, Ltd., Santen Pharmaceutical Co., Ltd.
    Inventors: Masahiko Hagihara, Ken-ichi Komori, Hidetoshi Sunamoto, Hiroshi Nishida, Takeshi Matsugi, Tadashi Nakajima, Masakazu Hatano, Kazutaka Kido, Hideaki Hara
  • Patent number: 7851638
    Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • Publication number: 20100292239
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: July 24, 2008
    Publication date: November 18, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, Antoine Daina, Harald Walter, Hans Tobler, Ramya Rajan
  • Patent number: 7834186
    Abstract: A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II) wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: November 16, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 7834192
    Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: November 16, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
  • Patent number: 7816522
    Abstract: A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: October 19, 2010
    Assignee: Eisai Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Kazunobu Kira, Shinsuke Hirota, Hiroshi Azuma, Tadashi Nagakura, Tatsuo Horizoe, Kimiyo Tabata, Kazutomi Kusano, Takao Omae, Atsushi Inoue
  • Patent number: 7816562
    Abstract: The invention is amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate anion wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms, and a cationic counter ion.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: October 19, 2010
    Assignee: Dow Global Technologies Inc.
    Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
  • Patent number: 7812045
    Abstract: Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: October 12, 2010
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Kyung A Yu, Il Yeong Jeong
  • Patent number: 7803831
    Abstract: Compounds of formula (IA) or (IB) or salts, N-oxides, hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: September 28, 2010
    Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute Of Cancer Research
    Inventors: Mandy Christine Beswick, Paul Andrew Brough, Martin James Drysdale, Brian William Dymock
  • Patent number: 7786144
    Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: August 31, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
  • Patent number: 7776910
    Abstract: Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: August 17, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan
  • Patent number: 7759382
    Abstract: This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity, and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: July 20, 2010
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jay S. Tung, Lee H. Latimer, Jing Wu, Albert Garofalo, Michael A. Pleiss, Darren Dressen, Ashley Guinn, Scott A. Jenkins, Jennifer Sealy, John Tucker, David W. G. Wone
  • Patent number: 7745477
    Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 29, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
  • Patent number: 7737241
    Abstract: The invention is a system for initiating free radical polymerization comprising: a) in one part, one or more amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms and optionally containing one or more heteroatoms or heteroatom containing functional moieties, and one or more cationic counter ions and b) in a second part, a liberating compound which reacts with the nitrogen atom(s) bound to the boron atom(s) upon contact with the amido-borate to form an organoborane radical.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: June 15, 2010
    Assignee: Dow Global Technologies Inc.
    Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
  • Patent number: 7728030
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: June 1, 2010
    Assignees: AstraZeneca AB, Bayer Schering Pharma Aktiengesellschaft
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Patent number: 7718687
    Abstract: The present invention relates to prodrugs of dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.,
    Inventors: Paul J. Coleman, Christopher D. Cox, George D. Hartman
  • Patent number: 7705029
    Abstract: What is claimed is a compound represented by the following structural formula: or a pharmaceutically acceptable salt, solvate or clathrate thereof. The variables for Structural Formula (I) are as described herein.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: April 27, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Weiwen Ying, Jun Jiang, Mitsunori Ono, Lijun Sun
  • Patent number: 7678818
    Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 19, 2007
    Date of Patent: March 16, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
  • Patent number: 7662844
    Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: February 16, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Vanessa Smith, Anthony Nigro, Mark Mulvihill, Cara Cesario, Patricia Anne Beck, Arlindo L. Castelhano
  • Patent number: 7659298
    Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: February 9, 2010
    Assignee: sanofi-aventis
    Inventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
  • Patent number: 7659300
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Patent number: 7652057
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: August 29, 2006
    Date of Patent: January 26, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V Mayweg, Werner Neidhart
  • Patent number: 7649009
    Abstract: Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: January 19, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
  • Patent number: 7645786
    Abstract: 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: Grant
    Filed: December 14, 2006
    Date of Patent: January 12, 2010
    Assignee: Pfizer Inc.
    Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
  • Patent number: 7625938
    Abstract: 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: Grant
    Filed: July 19, 2005
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Linda Brockunier, Jian Guo, Rui Liang, Emma R. Parmee, Subharekha Raghavan, George Scott Tria, Yusheng Xiong
  • Patent number: 7622491
    Abstract: The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.
    Type: Grant
    Filed: August 11, 2005
    Date of Patent: November 24, 2009
    Assignee: Metabolex Inc.
    Inventors: Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
  • Patent number: 7605266
    Abstract: The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: October 20, 2009
    Assignee: SmithKline Beecham
    Inventors: Dashyant Dhanak, Kenneth Allen Newlander
  • Publication number: 20090253905
    Abstract: The invention relates to a method for producing onium salts comprising alkyl anions or aryl sulfonate anions or alkyl carboxylate anions or acryl carboxylate anions by reacting an onium halide with an alkyl silyl ester or trialkyl silyl ester of an alkyl sulfonic acid or aryl sulfonic acid or an alkyl carboxylic acid or aryl carboxylic acid or the anhydrides thereof.
    Type: Application
    Filed: November 18, 2005
    Publication date: October 8, 2009
    Inventors: Nikolai (Mykola) Ignatyev, Urs Weiz-Biermann, Andriy Kucheryna, Helge Willner