Additional Hetero Ring Attached Directly Or Indirectly To The Quinazoline Ring System By Nonionic Bonding Patents (Class 514/266.2)
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Publication number: 20120077811Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.Type: ApplicationFiled: March 11, 2010Publication date: March 29, 2012Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
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Publication number: 20120077804Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.Type: ApplicationFiled: July 24, 2008Publication date: March 29, 2012Applicant: The Regents of the University of CaliforniaInventor: Shou-Wei Ding
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Publication number: 20120064025Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.Type: ApplicationFiled: September 28, 2011Publication date: March 15, 2012Applicant: EXELIXIS, INC.Inventors: Richard Martin, Jeffrey D. Kahl, Brenton T. Flatt, Ronald Griffith
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Publication number: 20120059002Abstract: Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: April 21, 2010Publication date: March 8, 2012Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
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Publication number: 20120058987Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).Type: ApplicationFiled: March 25, 2010Publication date: March 8, 2012Applicant: SANOFIInventors: Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
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Publication number: 20120052130Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: April 12, 2010Publication date: March 1, 2012Inventors: Etzer Darout, Michael Paul DeNinno, Kentaro Futatsugi, Cristiano Ruch Werneck Guimaraes, Bruce Allen Lefker, Vincent Mascitti, Kim Francis McClure, Michael John Munchhof, Ralph Pelton Robinson, JR.
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Publication number: 20120052061Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.Type: ApplicationFiled: September 23, 2008Publication date: March 1, 2012Applicant: Tragara Pharmaceuticals Inc.Inventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield, Tracy Lawhon
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Publication number: 20120053052Abstract: The present invention relates to the 3-arylquinazolin-4-one compounds of the formula I and the salts thereof, wherein n is 0, 1 or 2; X is O, S or N—R4; Y1 is N or CH; Y2 is N or C—R5; R1 is C1-C10-alkyl, C1-C10-haloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, C2-C10-alkynyl, C2-C10-haloalkynyl, C3-C12-cycloalkyl, C5-C12-cycloalkenyl, C3-C12-cycloalkyl-C1-C4-alkyl, C5-C12-cycloalkenyl-C1-C4-alkyl, where the cycloalkyl radical and the cycloalkenyl radical in the last four mentioned radicals are unsubstituted, partially or fully halogenated and/or carry 1, 2, 3, 4, or 5 C1-C4-alkyl radicals; R2 is hydrogen, halogen, CN, C(Z)NH2, C1-C4-alkyl or C1-C4-haloalkyl, wherein Z is O, S or NR6; and the variables k, R, R3, R4, R5 and R6 are as defined in the claims. The invention also relates to the use of novel compounds of formula I for combating invertebrate pests and to a method for controlling invertebrate pests.Type: ApplicationFiled: March 3, 2010Publication date: March 1, 2012Applicant: BASF SEInventors: Steffen Gross, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Matthias Pohlman, Michael Puhl, Sarah Thompson, Cecille Ebuenga, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20120046269Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: February 4, 2010Publication date: February 23, 2012Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Steiber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Publication number: 20120040954Abstract: Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.Type: ApplicationFiled: March 16, 2010Publication date: February 16, 2012Inventor: Henrik C. Hansen
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Publication number: 20120040980Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Penelope Jane Huggins, Jack Gordon Parsons
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Publication number: 20120040935Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: May 18, 2011Publication date: February 16, 2012Applicant: Vertex Pharmaceuticals, Inc.Inventors: Dean M. Wilson, Andreas P. Termin, Timothy D. Neubert, Jian Wang, Yulian Zhang, Jesus E. Gonzalez, III, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120022021Abstract: The present invention relates to mixtures comprising a) a compound of the formula I in which X, m, Q and a are as defined in the description and b) one or more ethylene modulators (II) selected from the group consisting of: inhibitors of ethylene biosynthesis which inhibit the conversion of S-adenosyl-L-methionine into 1-aminocyclopropane-1-carboxylic acid (ACC), inhibitors of ethylene biosynthesis which block the conversion of ACC into ethylene, or inhibitors of ethylene action, and also to compositions comprising them and to their use for controlling harmful fungi.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Applicant: BASF SEInventors: Wilhelm RADEMACHER, John S. HARDEN, Dan E. WESTBERG, Joseph E. ZAWIERUCHA, Thomas J. HOLT, Hendrik YPEMA, Ted R. BARDINELLI, Albert C. EVERSON, Edson BEGLIOMINI
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Publication number: 20120015905Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventor: Henrik C. Hansen
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Publication number: 20120009144Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: July 6, 2011Publication date: January 12, 2012Applicant: Roche Palo Alto LLCInventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
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Publication number: 20120004210Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.Type: ApplicationFiled: December 18, 2009Publication date: January 5, 2012Inventors: Caroline Leriche, Eric Auclair, Jacques Le Roux, David Middlemiss
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Patent number: 8088766Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.Type: GrantFiled: September 12, 2008Date of Patent: January 3, 2012Assignee: Array BioPharma Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Publication number: 20110319380Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: December 17, 2010Publication date: December 29, 2011Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
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Publication number: 20110306572Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.Type: ApplicationFiled: September 23, 2008Publication date: December 15, 2011Applicant: TRAGARA PHARMACEUTICALS, INCInventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield
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Publication number: 20110294807Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: January 8, 2010Publication date: December 1, 2011Inventor: Henrik C. Hansen
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Publication number: 20110294818Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 28, 2011Publication date: December 1, 2011Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Patent number: 8067436Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: May 24, 2007Date of Patent: November 29, 2011Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Publication number: 20110288082Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate.Type: ApplicationFiled: May 6, 2011Publication date: November 24, 2011Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
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Publication number: 20110280959Abstract: A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the following formula or its salt: wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2? is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2? is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2? and R2? optionally form a condensed ring containing an oxygen atom and (b) at least one other fungicide.Type: ApplicationFiled: May 26, 2011Publication date: November 17, 2011Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hisaya NISHIDE, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
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Publication number: 20110281896Abstract: Optical pure quinazoline compounds, especially compounds of the general formula (I), wherein R1 and Y are defined as the specification, preparation methods of them, pharmaceutical compositions containing them and their uses are provided. Compounds of the general formula (VII), which are intermediates in the synthesis of the compounds of the general formula (I), wherein Ar, R2, R3, m, n, T and carbon atom with * are defined as the specification, are also provided.Type: ApplicationFiled: January 7, 2010Publication date: November 17, 2011Inventors: Jiadeng Tang, Xuesong Wu
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Publication number: 20110269783Abstract: The present invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the derivatives for the manufacture of a medicament, to pharmaceutical compositions comprising the derivatives, and to methods of treating a disorder, disease or a condition responsive to activation of Kv7 channels.Type: ApplicationFiled: November 6, 2009Publication date: November 3, 2011Applicant: NEUROSEARCH A/SInventors: Carsten Jessen, William Dalby Brown, Dorte Strøbaek
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Patent number: 8048862Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: GrantFiled: April 14, 2009Date of Patent: November 1, 2011Assignee: InterMune, Inc.Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
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Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
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Publication number: 20110256240Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with a platinum anti-tumour agent; to a pharmaceutical composition comprising AZD2171 and a platinum anti-tumour agent; to a combination product comprising AZD2171 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and a platinum anti-tumour agent; to the use of AZD2171 and a platinum anti-tumour agent in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.Type: ApplicationFiled: November 22, 2010Publication date: October 20, 2011Inventor: Stephen Robert WEDGE
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Publication number: 20110245225Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R5 and X 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: November 12, 2009Publication date: October 6, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTINGInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
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Publication number: 20110245263Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: ApplicationFiled: June 15, 2011Publication date: October 6, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
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Publication number: 20110230505Abstract: Dihydroquinazoline compounds, compositions containing them, the use of the compounds and compositions for the treatment of Alzheimer's disease are described.Type: ApplicationFiled: November 20, 2009Publication date: September 22, 2011Applicant: PURDUE RESEARCH FOUNDATIONInventor: Arun K. Ghosh
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Publication number: 20110230465Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: September 16, 2010Publication date: September 22, 2011Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
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Publication number: 20110217300Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds.Type: ApplicationFiled: April 6, 2011Publication date: September 8, 2011Applicant: ARQULE, INC.Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
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Patent number: 8008311Abstract: Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: February 11, 2010Date of Patent: August 30, 2011Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustave Bergnes, Bainian Feng, Whitney W. Smith, John C. Chabala
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Publication number: 20110207756Abstract: The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and analogs thereof are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract.Type: ApplicationFiled: April 8, 2011Publication date: August 25, 2011Applicant: Eisai R&D Management Co., Ltd.Inventor: Junji Matsui
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Patent number: 8003659Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: February 3, 2009Date of Patent: August 23, 2011Assignee: Indenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
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Patent number: 8003658Abstract: The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells, a method for the preparation thereof and a pharmaceutical composition comprising same as an active ingredient.Type: GrantFiled: December 20, 2005Date of Patent: August 23, 2011Assignee: Hanmi Holdings Co., Ltd.Inventors: Young Jin Ham, Ji Hyeon Gong, Mi Young Cha, Jong Woo Kim, Maeng Sup Kim, Eun Young Kim, Ji Yeon Song, Chang In Kim, Se Young Kim, Gwan Sun Lee
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Publication number: 20110201592Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: October 23, 2008Publication date: August 18, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Jamieson Caldwell, Antony William Oliver, Tony Michael Raynham, Emma Jane Welsh, Cornelius Albertus Johannes Matijssen
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Patent number: 7994181Abstract: The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.Type: GrantFiled: August 3, 2006Date of Patent: August 9, 2011Assignee: Rottapharm S.p.A.Inventors: Antonio Giordani, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Francesca Tarchino, Gianfranco Caselli, Tiziana Piepoli, Silvio Mazzari, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20110190293Abstract: Quinazolinone compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Inventors: Weibo Wang, Liana M. Lagniton, Ryan N. Constantine, Manoj C. Desai
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Patent number: 7989461Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: December 20, 2006Date of Patent: August 2, 2011Assignee: Amgen Inc.Inventors: Frenel F. De Morin, Jian J. Chen, Stephen Hitchcock, Gang Liu, Nick A. Paras, Jeffrey Petkus, Adrian L. Smith, Andrew Tasker, Jiawang Zhu
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Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20110166135Abstract: The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity.Type: ApplicationFiled: September 9, 2009Publication date: July 7, 2011Inventors: Hiroshi Morimoto, Toshiaki Sakamoto, Toshiyuki Himiyama, Eiji Kawanishi, Takehiko Matsumura
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Patent number: 7972600Abstract: The present invention relates to a method of treating prostate cancer with androgen deprivation therapy and an insulin-like growth factor receptor (IGF-IR) antagonist. Although the response rate of prostate cancer to androgen deprivation therapy (ADT) is high, surviving cancer cells invariably become androgen independent (AI) and tumor growth follows. The invention inhibits or delays transition of androgen dependent cancer to androgen independent cancer, significantly decreases risk of recurrence, and improves treatment outcome.Type: GrantFiled: February 5, 2007Date of Patent: July 5, 2011Assignees: ImClone LLC, University of WashingtonInventors: Dale L. Ludwig, Stephen R. Plymate
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Patent number: 7968545Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 5, 2004Date of Patent: June 28, 2011Assignee: Vertex Pharmaceuticals Inc.Inventors: Dean M. Wilson, Andreas P. Termin, Timothy D. Neubert, Jian Wang, Yulian Zhang, Jesus E. Gonzalez, III, Esther Martinborough, Nicole Zimmerman
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Publication number: 20110136805Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: ApplicationFiled: November 3, 2007Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20110136806Abstract: The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, Rd, Re and X are as defined in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, in particular, the physiologically-acceptable salts thereof with inorganic and organic acids with useful pharmacological properties, in particular, an inhibitory effect on signal transduction brought about by tyrosine kinases, the use thereof for the treatment of diseases, in particular of tumour diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and airways and production thereof.Type: ApplicationFiled: February 15, 2011Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Birgit JUNG
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Patent number: 7951405Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and cisplatin combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and cisplatin combination in combination with a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as Tarceva™).Type: GrantFiled: June 3, 2005Date of Patent: May 31, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Brian Higgins, Kenneth Kolinsky
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Patent number: 7951955Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: May 1, 2008Date of Patent: May 31, 2011Assignee: Biota Scientific Management Pty LtdInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell