Three Or More Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/236.2)
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Publication number: 20150072977Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Inventors: David Alexander LEARMONTH, Laszlo Erno KISS, Pedro Nuno LEAL PALMA, Humberto DOS SANTOS FERREIRA, Patricio Manuel Vieira ARAUJO SOARES DA SILVA
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Publication number: 20150065506Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 13, 2014Publication date: March 5, 2015Applicant: ROCHE PALO ALTO LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8962574Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 10, 2009Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventor: Paul Anthony Reilly
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Publication number: 20150045359Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.Type: ApplicationFiled: January 8, 2013Publication date: February 12, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
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Publication number: 20150045365Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.Type: ApplicationFiled: August 6, 2014Publication date: February 12, 2015Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
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Publication number: 20150045347Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: February 12, 2015Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
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Patent number: 8951536Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.Type: GrantFiled: February 28, 2013Date of Patent: February 10, 2015Assignee: Incyte CorporationInventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
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Patent number: 8940738Abstract: A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: August 11, 2010Date of Patent: January 27, 2015Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Daiki Sakai, Kazuki Nakayama, Kazutoshi Watanabe
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Publication number: 20150025057Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.Type: ApplicationFiled: October 8, 2014Publication date: January 22, 2015Applicant: NOVARTIS AGInventors: Oliver BARKER, Jonathan Mark BENTLY, Mark Gary BOCK, Thomas CAIN, Praful CHOVATIA, Jennifer Ruth DOD, Florence EUSTACHE, Laura GLEAVE, Jonathan HARGRAVE, Alexander HEIFETZ, Richard LAW, Ali RAOOF, David WILLOWS
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Publication number: 20150018328Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Applicant: AGIOS PHARMACEUTICALS, INCInventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
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Publication number: 20150018331Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: March 24, 2014Publication date: January 15, 2015Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Publication number: 20150018344Abstract: Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 15, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Publication number: 20150011532Abstract: Compounds having the following formula: wherein A is, or; and X is N or C—R7, or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banejee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Patent number: 8927548Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: GrantFiled: January 13, 2012Date of Patent: January 6, 2015Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Kowalczyk-Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
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Publication number: 20150005292Abstract: There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.Type: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Applicant: CHASE PHARMACEUTICALS CORPORATIONInventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
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Publication number: 20150005276Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whicType: ApplicationFiled: July 2, 2014Publication date: January 1, 2015Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Publication number: 20140377292Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20140378438Abstract: The invention relates to compounds of formula (I) wherein m, n, R1, T0 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds as well as methods of treating mTOR related diseases.Type: ApplicationFiled: September 21, 2012Publication date: December 25, 2014Applicant: CELLZOME LIMITEDInventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
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Publication number: 20140378443Abstract: The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.Type: ApplicationFiled: June 20, 2014Publication date: December 25, 2014Inventors: William L. Jorgensen, Karen S. Anderson
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Publication number: 20140371222Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
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Publication number: 20140369961Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
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Publication number: 20140357599Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
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Patent number: 8901121Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: December 2, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
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Publication number: 20140349973Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 10, 2012Publication date: November 27, 2014Applicant: Viamet Pharmaceuticals, IncInventors: William J. Hoekstra, Christopher M. Yates
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Publication number: 20140350003Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20140343060Abstract: Aprepitant L-proline solvate compositions and aprepitant L-proline solvate cocrystals are disclosed as well as pharmaceutical compositions containing them. The compositions and cocrystals of the invention are: 1:1:1 aprepitant L-proline methanol composition; a 1:1:1 aprepitant L-proline methanol cocrystal; a 1:1:1:1 aprepitant L-proline ethanol composition; a 1:1:1 aprepitant L-proline ethanol cocrystal; l 1:1:1 aprepitant L-proline n-propanol composition; and a 1:1:1 aprepitant L-proline n-propanol cocrystal: The aprepitant L-proline solvate compositions or cocrystals may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch a respiratory disease, or an addiction.Type: ApplicationFiled: November 21, 2012Publication date: November 20, 2014Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
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Publication number: 20140343061Abstract: The present invention relates to compounds corresponding to formula (I) in which: —R1 represents a substituted phenyl; —R2 represents: —a substituted phenyl; —a heteroaromatic group, the said group being unsubstituted or substituted one or more times; —R3 represents a group Alk; —R4 represents a hydrogen atom or a (C1-C4)alkyl; —R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; —or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; —R6 represents a group —COOAlk, a group —CONH2 or a group —NHSO2Alk; —Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use.Type: ApplicationFiled: December 11, 2012Publication date: November 20, 2014Inventors: Joelle Arnaud, Martine Artiaga, Francis Barth, Laurent Hortala, Serge Martinez, Pascale Roux
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Publication number: 20140343041Abstract: The present invention provides topical ophthalmic formulations comprising a combination of one or more antihistamine agents and optionally one or more vasculature modifying agents such as a ? adrenergic receptor antagonist. Also provided are methods of using the formulations of the invention for treating and/or preventing symptoms associated with migraine headache, and for reducing the frequency, severity and duration of migraine attacks.Type: ApplicationFiled: March 13, 2014Publication date: November 20, 2014Inventors: Matthew J. Chapin, Richard Abelson
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Patent number: 8889677Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8889668Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: December 12, 2012Date of Patent: November 18, 2014Assignee: Merck Serono SAInventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
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Publication number: 20140329797Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 16, 2012Publication date: November 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
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Publication number: 20140329812Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.Type: ApplicationFiled: December 13, 2011Publication date: November 6, 2014Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Loredana Vesci, Maria Luisa Cervoni, Claudio Pisano, Maurizio Taddei, Serena Ferrini
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Publication number: 20140329816Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 26, 2012Publication date: November 6, 2014Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
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Publication number: 20140322247Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.Type: ApplicationFiled: March 13, 2014Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
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Publication number: 20140309209Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: November 23, 2012Publication date: October 16, 2014Inventors: Yonghong Song, Qing Xu, Zhaozhong J. Jia, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Publication number: 20140303166Abstract: The current application is directed to cosmetic methods for changing the appearance of eyes by causing a retraction of the eyelids so that the eyes appear to be more open and have a wider appearance. Various methods involve application of one or more prostaglandins, synthetic prostaglandins, including synthetic prostaglandin F, and synthetic prostaglandin analogues, to eyelids, which results in contraction of eyelid muscles and a wider, more open appearance of the eyes.Type: ApplicationFiled: April 8, 2013Publication date: October 9, 2014Inventor: Gordon C. Tang
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Publication number: 20140301978Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: ApplicationFiled: June 18, 2014Publication date: October 9, 2014Applicant: PTC Therapeutics Inc.Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
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Publication number: 20140303167Abstract: The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.Type: ApplicationFiled: August 22, 2012Publication date: October 9, 2014Applicant: LEAD DISCOVERY CENTER GMBHInventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
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Publication number: 20140302988Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.Type: ApplicationFiled: August 10, 2012Publication date: October 9, 2014Applicant: Bayer Intellectual Property GMBHInventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
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Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Patent number: 8846674Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: GrantFiled: October 18, 2011Date of Patent: September 30, 2014Assignee: Nicox, S.A.Inventor: David S. Garvey
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140271923Abstract: Patients inflicted with various clustering chronic diseases require treatment with multiple drugs having distinct mechanisms of action. Accordingly, patients with multiple conditions suffer from cumulative side effects of multiple drugs as well as drug-drug interactions. Embodiments, agents, compounds or drugs of the present invention, such as sesquiterpenes, e.g., Zerumbone, replace an equal or larger number of approved drugs during patient treatment. Examples of disorders prevented or ameliorated by administration of the formulations of this invention include but are not limited to inflammatory diseases that may be, oncological, genetic, ischemic, infectious, neurological, hematological, ophthalmological, rheumatoid, orthopedic, neurological, hematological, kidney, vascular, dermatological, gynecological, or obstetric.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventor: Christopher Brian Reid
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Publication number: 20140255386Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: July 24, 2012Publication date: September 11, 2014Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTEInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20140256726Abstract: The present invention is directed to preservative-free solutions of bimatoprost and timolol for lowering intra-ocular pressure and treatment of glaucoma.Type: ApplicationFiled: March 5, 2013Publication date: September 11, 2014Applicant: ALLERGAN, INC.Inventors: Sukhon Likitlersuang, Ajay Parashar, Chetan P. Pujara, William F. Kelly, Jie Shen, Marina Bejanian, Rhett Schiffman
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Publication number: 20140249128Abstract: The present disclosure provides substituted triazine carboxamides of Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, E, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: February 26, 2014Publication date: September 4, 2014Applicant: Purdue Pharma L.P.Inventors: Dawit Tadesse, Jianming Yu
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Publication number: 20140248239Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: April 23, 2014Publication date: September 4, 2014Applicant: WYETH LLCInventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
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Patent number: 8822465Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.Type: GrantFiled: March 14, 2013Date of Patent: September 2, 2014Assignee: Wuhan Shengyun Biopharma Co., Ltd.Inventor: Hua Xu
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Publication number: 20140235586Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: PTC Therapeutics, Inc.Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch