Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.3)
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Publication number: 20120046307Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: ApplicationFiled: October 16, 2009Publication date: February 23, 2012Applicant: UNIVERSITAET DES SAARLANDESInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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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: 20120034315Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.Type: ApplicationFiled: April 19, 2010Publication date: February 9, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Mary Ann Hanagan, Matthew Richard Oberholzer, Robert James Pasteris, Rafael Shapiro
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Publication number: 20120035050Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.Type: ApplicationFiled: March 25, 2009Publication date: February 9, 2012Applicant: BAYER CROPSCIENCE AGInventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
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Patent number: 8101624Abstract: The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) in the formula, R1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1-3 substituents selected from halogen, C1-6 alkyl, C1-6 haloalkyl containing 1-6 halogen atoms and C1-6 alkoxy; and n is an integer of 1-3.Type: GrantFiled: July 24, 2007Date of Patent: January 24, 2012Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Akira Asagarasu, Shuichiro Sato, Makoto Okada
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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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Patent number: 8084459Abstract: Compounds of the formula or salts, tautomers or isomers thereof, are useful for treating neurological conditions, especially neurodegenerative disorders, such as Alzheimer's disease.Type: GrantFiled: April 1, 2005Date of Patent: December 27, 2011Assignee: Prana Biotechnology LtdInventors: Gaik Beng Kok, Brenda Kwan Yi Leung
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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: 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: 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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Publication number: 20110268775Abstract: The present invention is directed to methods of preparing nanoparticles of aqueous-insoluble compounds, particularly aqueous-insoluble bioactive (drug) compounds, and to compositions and medicaments obtained by these methods. These methods, compositions, and other inventive aspects of the present invention are based particularly on the use of bile acid compound(s) to prepare nanoparticles of aqueous-insoluble compounds.Type: ApplicationFiled: January 5, 2010Publication date: November 3, 2011Applicant: PHARMANOVA, INC.Inventors: Kris Holt, Deepak Thassu, Michael R. Violante
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Patent number: 8030320Abstract: The present invention relates to compounds of formula I, to the preparation thereof and to the therapeutic use thereof.Type: GrantFiled: January 26, 2010Date of Patent: October 4, 2011Assignee: Sanofi-AventisInventors: Michel Evers, Arielle Genevois-Borella, Andreas Karlsson, Jean-Luc Malleron
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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: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110218206Abstract: Disclosed are pharmaceutical compositions comprising mdivi-1 and nutlin-3, individually and in combination, for topical or intravitreal ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma, optic neuropathies including Leber Hereditary Optic Neuropathy, arteritic or non-arteritic Ischemic Optic Neuropathy, and retinal artery and vein occlusions.Type: ApplicationFiled: March 2, 2010Publication date: September 8, 2011Inventor: Ian H Chan
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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: 8012988Abstract: 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: GrantFiled: September 29, 2009Date of Patent: September 6, 2011Assignee: Novartis AGInventors: 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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Publication number: 20110212974Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.Type: ApplicationFiled: August 18, 2009Publication date: September 1, 2011Inventor: Anne Blangy
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Publication number: 20110212980Abstract: The present invention relates to novel combinations suitable for the treatment of migraine of various genesis or aetiology, which comprise, as active ingredients, at least one 5-HT1 B/1 D receptor agonist and at least one selective, competitive AMPA receptor antagonist being a 1 H-quinazoline-2,4-dione of formula (I) as defined in the claims; to their preparation; to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: October 21, 2009Publication date: September 1, 2011Inventors: Graeme Bilbe, Baltazar Gomez-Mancilla, Daniel Hoyer, Donald Johns, Hans O. Kalkman, Kevin Hall Mcallister
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Patent number: 7994182Abstract: The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.Type: GrantFiled: April 30, 2004Date of Patent: August 9, 2011Assignee: Pecsi TudomanyegyetemInventors: Balázs Sümegi, Kálmán Hideg, Tamás Kálai
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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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Publication number: 20110172254Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.Type: ApplicationFiled: September 17, 2009Publication date: July 14, 2011Applicant: ENDOCYTE, INC.Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Philip Stewart Low
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Publication number: 20110160231Abstract: A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: June 30, 2011Inventors: Jason David Oliver, John Leslie Thain, Michael John Bromley, Graham Edward Morris Sibley, Michael Birch
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Publication number: 20110159107Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one isoxazoline compound I of the formula I wherein R1, R2, R3, R4, R5 and A are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: July 2, 2009Publication date: June 30, 2011Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Egon Haden
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Publication number: 20110136813Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 27, 2009Publication date: June 9, 2011Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20110129463Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: Proteologics, Ltd.Inventors: Omri EREZ, Philippe NAKACHE
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Patent number: 7951814Abstract: The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: GrantFiled: June 16, 2009Date of Patent: May 31, 2011Assignee: Glenmark Pharmaceuticals, S.A.Inventors: Meyyappan Muthuppalniappan, Abraham Thomas, Sukeerthi Kumar, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Srinivas Gullapalli
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Patent number: 7951813Abstract: Disclosed are novel quinazolinone derivatives of formula: wherein: R1 is optionally substituted phenyl or optionally substituted heteroaryl; R2 is 3-hydroxy, 4-hydroxy, 3-NHR4 or 4-NHR4, in which R4 is hydrogen, —C(O)R5, —C(O)NHR6, or —SO2R6; in which R5 is optionally substituted lower alkyl or optionally substituted lower alkoxy; and R6 is optionally substituted lower alkyl; R3 is hydrogen, lower alkyl, lower alkoxy, or halo; V is oxygen, sulfur, or —NH—; and W is lower alkylene of 1-3 carbon atoms, which are useful as ALDH-2 inhibitors for treating mammals for various disease states, such as treatment for cocaine dependency and alcohol dependency.Type: GrantFiled: April 3, 2008Date of Patent: May 31, 2011Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Michael Organ, Jeff Zablocki, Wing Ming Keung, Guoxin Tao
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Publication number: 20110118245Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.Type: ApplicationFiled: March 17, 2009Publication date: May 19, 2011Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
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Publication number: 20110112073Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
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Patent number: 7939539Abstract: 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: GrantFiled: November 24, 2004Date of Patent: May 10, 2011Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Weibo Wang, Liana M. Lagniton, Ryan N. Constantine, Manoj C. Desai
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Patent number: 7935709Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein s, T, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of p38 mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: July 16, 2007Date of Patent: May 3, 2011Assignee: Amgen Inc.Inventors: Fang-Tsao Hong, Kelvin K. C. Sham, Seifu Tadesse, Andrew Tasker
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Publication number: 20110098255Abstract: The primary subject of the invention is the use of a PARP inhibitor and an Akt kinase activating compound in combination in the treatment of pathological conditions related to PARP activation and/or that could benefit from Akt activation. A further subject of the invention is the use of a PARP inhibitor and an Akt kinase activating compound in combination for the preparation of pharmaceutical composition or kit for the treatment of a pathological condition related to PARP activation. The invention also relates to pharmaceutical composition, which contains a PARP-inhibitor and an Akt kinase activating compound together with auxiliaries generally used in pharmacy.Type: ApplicationFiled: July 1, 2009Publication date: April 28, 2011Inventors: Ferenc Gallyas, Balázs Sümegi, Sára Vetö, Péter Ács, Sámuel Komoly, Zsolt Illés
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Patent number: 7928114Abstract: Crystalline Forms of erlotinib are made. The crystalline materials are useful as pharmaceutical active agents in treating various cancers as well as in forming erlotinib salts.Type: GrantFiled: July 27, 2007Date of Patent: April 19, 2011Assignee: Synthon BVInventor: Raymond J. H. Westheim
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Publication number: 20110077256Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.Type: ApplicationFiled: April 28, 2010Publication date: March 31, 2011Inventors: Oivin M. Guicherit, Lee Rubin
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Publication number: 20110071148Abstract: The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of SciencesInventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
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Publication number: 20110065671Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Joel M. Harris, Santhosh Francis, Bernard R. Neustadt, Craig D. Boyle, Hong Liu, Jinsong Hao, Andrew Starnford, Samuel Chackalamannil, William J. Greenlee
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Publication number: 20110053932Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, p38, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 18, 2008Publication date: March 3, 2011Inventors: Taebo Sim, Truc Ngoc Nguyen, Baogen Wu, Yun He, Yongping Xie, Xing Wang, Guobao Zhang, Nathanael Schiander Gray
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Patent number: 7893071Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: GrantFiled: April 22, 2002Date of Patent: February 22, 2011Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Publication number: 20110028420Abstract: A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Inventors: Hamid A. Boulares, Chetan P. Hans, Amarjit S. Naura
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Publication number: 20110028433Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.Type: ApplicationFiled: March 26, 2009Publication date: February 3, 2011Applicants: JANSSEN PHARMACEUTICA NV, JANSSEN-CILAGInventors: Eddy Jean Edgard Freyne, Laurence Anne Mevellec, Jorge Eduardo Vialard, Christophe Meyer, Elisabeth Thérèse Jeanne Pasquier, Xavier Marc Bourdrez, Patrick René Angibaud
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Publication number: 20110020217Abstract: There is described a pharmaceutical composition comprising dexanabinol, or a derivative thereof, in combination with a second therapeutic agent that targets BRAF or MEK, and a pharmaceutically acceptable adjuvant, diluent or carrier. There is also described a method of treating a patient suffering from melanoma and uses related thereto.Type: ApplicationFiled: October 10, 2008Publication date: January 27, 2011Applicant: E-THERAPEUTICS PLCInventors: Malcolm Philip Young, Catherine Mary Thomas, Olusola Clement Idowu
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Publication number: 20110008333Abstract: The present application is directed to compositions and methods for inhibiting angiogenesis and treating or preventing unwanted cell proliferation, including tumors, by inhibiting the hedgehog pathway, e.g., with an antagonist of the hedgehog pathway such as those disclosed herein.Type: ApplicationFiled: April 8, 2010Publication date: January 13, 2011Applicant: CURIS, INC.Inventors: HENRYK DUDEK, IRINA KARAVANOV, CARMEN PEPICELLI, KAREN KOTKOW, LEE L. RUBIN
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Publication number: 20110009434Abstract: Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as ?4 integrin inhibitors.Type: ApplicationFiled: September 20, 2010Publication date: January 13, 2011Applicant: AJINOMOTO CO., INC.Inventors: Koichi FUJITA, Shinichiro Takahashi, Tatsuya Okuzumi, Tatsuhiro Yamada, Kotaro Okado, Noriyasu Kataoka, Haruko Hirashima, Hideyuki Yamaguchi
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Patent number: 7863283Abstract: The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.Type: GrantFiled: June 13, 2008Date of Patent: January 4, 2011Assignee: Bayer Schering Pharma AGInventors: Duy Nguyen, Arne von Bonin, Michael Haerter, Hartmut Schirok, Anne Mengel, Martina Schaefer, Oliver von Ahsen
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Publication number: 20100311769Abstract: The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease.Type: ApplicationFiled: January 8, 2009Publication date: December 9, 2010Applicant: SHIN POONG PHARMACEUTICAL CO., LTD.Inventors: Hwan Cho, II, Eun Bang Lee, Sin Cheol Kang, Won Seok Kim, Chul Kyu Lee
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Patent number: 7842700Abstract: Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as ?4 integrin inhibitors.Type: GrantFiled: December 21, 2007Date of Patent: November 30, 2010Assignee: Ajinomoto Co., Inc.Inventors: Koichi Fujita, Shinichiro Takahashi, Tatsuya Okuzumi, Tatsuhiro Yamada, Kotaro Okado, Noriyasu Kataoka, Haruko Hirashima, Hideyuki Yamaguchi
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Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors
Publication number: 20100298358Abstract: Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicant: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping LU, Zhibin Li, Song Shan, Jindi Yu, Zhiqiang Ning