Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/233.2)
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Publication number: 20140148431Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: August 24, 2012Publication date: May 29, 2014Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Patent number: 8729082Abstract: The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.Type: GrantFiled: April 24, 2010Date of Patent: May 20, 2014Assignee: Bayer Intellectual Property GmbHInventors: Marcus Koppitz, Benjamin Bader, Ulf Bömer, Bertolt Kreft, Philip Lienau, Tobias Marquardt, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
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Patent number: 8729074Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: March 19, 2010Date of Patent: May 20, 2014Assignee: Amgen Inc.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Publication number: 20140135323Abstract: The invention relates to novel inhibitors of kinases of the general formula (I): in which Q and R1 are defined in the claims, method for preparing such inhibitors, intermediates for preparing such inhibitors and uses of such inhibitors.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: Bayer Intellectual Property GmbHInventors: Olaf PRIEN, Knut EIS, Benjamin BADER, Judith GUENTHER, Arne VON BONIN
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Publication number: 20140128386Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Ingo HARTUNG, Markus FOLLMANN, Rolf JAUTELAT, Alexander STRAUB, Jorma HAßFELD, Niels LINDNER, Dirk SCHNEIDER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
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Publication number: 20140128372Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: March 7, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva-Maria BECKER, Andreas KNORR
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Publication number: 20140128385Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.Type: ApplicationFiled: January 13, 2012Publication date: May 8, 2014Inventor: Heinrich Ruegger
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Patent number: 8716282Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: GrantFiled: April 28, 2011Date of Patent: May 6, 2014Assignee: Janssen Pharmaceutica NVInventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
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Publication number: 20140121204Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: GALAPAGOS NVInventors: Frédéric Gilbert Labéguère, Gregory John Robert NEWSOME, Luke Jonathan ALVEY, Laurent Raymond Maurice Sanière, Stephen Robert FLETCHER
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Publication number: 20140121203Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).Type: ApplicationFiled: January 3, 2014Publication date: May 1, 2014Applicant: MEI Pharma, Inc.Inventors: Ken Chi Lik Lee, Eric T. Sun, Haishan Wang
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Publication number: 20140113896Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: November 8, 2011Publication date: April 24, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: William Johnston Scott, Orlin Pertov, Manfred Möwes, Ningshu Liu, Ulf Bömer
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Patent number: 8703759Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 30, 2011Date of Patent: April 22, 2014Assignee: Gilead Sciences, Inc.Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Publication number: 20140107073Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: ApplicationFiled: October 4, 2013Publication date: April 17, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Publication number: 20140107099Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Genentech, Inc.Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
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Patent number: 8697691Abstract: In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 21, 2010Date of Patent: April 15, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood, Rocco D. Gogliotti, Colleen M. Niswender, Bruce J. Melancon, Evan P. Lebois
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Publication number: 20140094448Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: September 13, 2013Publication date: April 3, 2014Applicant: SENHWA BIOSCIENCES, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas Raffaele, Suchitra Ravula, David M. Ryckman
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Patent number: 8685967Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.Type: GrantFiled: April 5, 2010Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
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Publication number: 20140088068Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: August 24, 2012Publication date: March 27, 2014Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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Publication number: 20140088097Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: September 23, 2013Publication date: March 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
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Publication number: 20140088098Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, and are defined herein.Type: ApplicationFiled: November 25, 2013Publication date: March 27, 2014Applicant: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, Mingde Xia, James J. McNally, Jay M. Matthews
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Publication number: 20140088096Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.Type: ApplicationFiled: February 14, 2013Publication date: March 27, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Mario Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
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Patent number: 8680096Abstract: The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.Type: GrantFiled: December 3, 2010Date of Patent: March 25, 2014Assignee: Sanofi-AventisInventors: Florian Auger, Luc Even
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Publication number: 20140080810Abstract: The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.Type: ApplicationFiled: November 15, 2011Publication date: March 20, 2014Applicant: Exelixis, Inc.Inventors: Kenneth D. Rice, David Markby
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Patent number: 8673905Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.Type: GrantFiled: March 9, 2012Date of Patent: March 18, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Michael Soth
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Publication number: 20140073638Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: ApplicationFiled: October 16, 2013Publication date: March 13, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20140072529Abstract: The present invention relates:—to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II): or a tautomer, solvate or hydrate thereof;—to methods of preparing said dihydrochloride salt;—to said dihydrochloride salt for the treatment and/or prophylaxis of a disease;—to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer;—to a pharmaceutical composition comprising said dihydrochloride salt; and to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agentType: ApplicationFiled: March 29, 2012Publication date: March 13, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jan-Georg Peters, Hans-Christian Militzer, Hartwig Müller
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Publication number: 20140066434Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: April 6, 2012Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: William C. Shakespeare
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Publication number: 20140057896Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: October 22, 2013Publication date: February 27, 2014Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
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Publication number: 20140057894Abstract: Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.Type: ApplicationFiled: January 26, 2012Publication date: February 27, 2014Applicant: Universite De MontrealInventors: Michel Bouvier, Anne Marinier, Rejean Ruel, Patricia René, Yves Chantigny, Philippe Dagneau, Stéphane Gingras
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Patent number: 8658641Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: GrantFiled: October 13, 2009Date of Patent: February 25, 2014Assignee: AstraZeneca ABInventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Publication number: 20140051696Abstract: Provided herein are methods that relate to a novel therapeutic strategy for treatment of cancer, including hematological malignancies such as leukemia, lymphoma, and multiple myeloma. In particular, the method includes administration of a PI3K? inhibitor and a Syk inhibitor.Type: ApplicationFiled: August 14, 2013Publication date: February 20, 2014Applicant: GILEAD CALISTOGA LLCInventors: Brian J. LANNUTTI, Julie DI PAOLO, Heather WEBB, Adam KASHISHIAN
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Publication number: 20140051689Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: ApplicationFiled: October 24, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
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Publication number: 20140051697Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Helen Anderson
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Publication number: 20140045835Abstract: Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification.Type: ApplicationFiled: October 15, 2013Publication date: February 13, 2014Applicant: Array BioPharma Inc.Inventors: Shelley Allen, Robert Kirk DeLisle, Julie Marie Hicks, Erik James Hicken, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, John E. Robinson, Qian Zhao
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Publication number: 20140045836Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: October 16, 2013Publication date: February 13, 2014Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
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Publication number: 20140045826Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: April 6, 2012Publication date: February 13, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: William C. Shakespeare, Frank G. Haluska
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Publication number: 20140045817Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Applicant: Array BioPharma Inc.Inventors: Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Hicks, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
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Patent number: 8648067Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: GrantFiled: December 22, 2011Date of Patent: February 11, 2014Assignees: Cephalon, Inc., Teva SanteInventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
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Publication number: 20140038955Abstract: Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: H. Lundbeck A/SInventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
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Publication number: 20140038920Abstract: The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases.Type: ApplicationFiled: March 7, 2012Publication date: February 6, 2014Applicant: FONDAZIONE TELETHONInventors: Andrea Ballabio, Carmine Settembre, Diego Luis Medina Sanabria
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Publication number: 20140038953Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to reduce circulating levels of ApoB-100 or LDL. These compounds may also be used to treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.Type: ApplicationFiled: January 20, 2012Publication date: February 6, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Paul B. Yu, Matthias Derwall, Kenneth D. Bloch, Rajeev Malhotra
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Publication number: 20140038939Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.Type: ApplicationFiled: October 9, 2013Publication date: February 6, 2014Applicant: Genentech, Inc.Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Christopher Hurley, Jun Liang, Wendy Liu, Joseph P. Lyssikatos
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Publication number: 20140038954Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: AMGEN INC.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Human
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Publication number: 20140031351Abstract: The present invention provides compounds of Formula I or a pharmaceutically acceptable salt forms thereof, wherein R1, R2, R3, R4, R5, A and X are as defined herein, methods of treatment and uses thereof.Type: ApplicationFiled: September 13, 2013Publication date: January 30, 2014Applicant: Cephalon, Inc.Inventors: Henry J. Breslin, Bruce D. Dorsey, Gregory R. Ott
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Publication number: 20140030191Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.Type: ApplicationFiled: April 20, 2012Publication date: January 30, 2014Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
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Publication number: 20140031333Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as 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 c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: September 19, 2013Publication date: January 30, 2014Applicant: IRM LLCInventors: Valentina MOLENTI, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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Publication number: 20140024643Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: David T. HUNG, Andrew Asher PROTTER, Sarvajit CHAKRAVARTY, Rajendra Parasmal JAIN
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Publication number: 20140018345Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.Type: ApplicationFiled: July 12, 2013Publication date: January 16, 2014Applicant: CHIESI FARMACEUTICI S.p.AInventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton
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Publication number: 20140018319Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: July 12, 2013Publication date: January 16, 2014Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann