Ring Nitrogen In The Additional Hetero Ring Patents (Class 514/235.5)
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Patent number: 8835648Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: GrantFiled: June 9, 2010Date of Patent: September 16, 2014Assignee: Siena Biotech S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
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Patent number: 8828996Abstract: The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: March 13, 2012Date of Patent: September 9, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Hayley Marie Binch, Michael Paul DeNinno, Lev Tyler Dewey Fanning, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Nicole Hilgraf, Pramod Joshi, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Alina Silina, Urvi Jagdishbhai Sheth, Dennis James Hurley, Vijayalaksmi Arumugam
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Publication number: 20140249149Abstract: The present invention relates to the use of known pyridyl carboxamide derivatives and novel pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.Type: ApplicationFiled: October 29, 2012Publication date: September 4, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Nico Greul, Darren Mansfield, Martin Fusslein, Heiko Rieck, Matthias Riedrich, Lars Rodefeld, Kristian Kather, Olga Malsam, Peter Losel, Arnd Voerste, Hans-Georg Schwarz, Kerstin Ilg, Ulrich Gorgens, Lionel Carles, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse
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Patent number: 8822449Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: GrantFiled: August 25, 2009Date of Patent: September 2, 2014Assignee: SanofiInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 8822463Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: GrantFiled: September 28, 2011Date of Patent: September 2, 2014Assignee: Sk Biopharmaceuticals Co., Ltd.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Publication number: 20140243335Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Publication number: 20140243337Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140243336Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
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Patent number: 8815855Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: GrantFiled: December 1, 2009Date of Patent: August 26, 2014Assignee: 4SC AGInventors: Thomas Maier, Thomas Bär, Thomas Beckers, Astrid Zimmermann, Siegfried Schneider, Volker Gekeler
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Publication number: 20140235637Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: InterMune, Inc.Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Publication number: 20140235636Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20140235608Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140235635Abstract: An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.Type: ApplicationFiled: August 7, 2013Publication date: August 21, 2014Applicant: PONIARD PHARMACEUTICALS, INCInventors: Yixiong Lei, Carl Henry Behrens, Hui-Yin Li, Connie L. Sun
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Publication number: 20140228340Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: August 13, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
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Publication number: 20140228363Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Patent number: 8802666Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140221361Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
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Publication number: 20140221373Abstract: The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A1, A2, A3, L1, L2 and D are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the Compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 17, 2012Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alexander Heim-Riether, Anil Kumar Padyana, Shuang Liang, Steven John Taylor, Qiang Zhang
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Publication number: 20140221374Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.Type: ApplicationFiled: March 16, 2012Publication date: August 7, 2014Applicant: Ruga CorporationInventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
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Patent number: 8796254Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: GrantFiled: March 31, 2011Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
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Patent number: 8796267Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.Type: GrantFiled: June 17, 2008Date of Patent: August 5, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Roger Tung, Scott Harbeson
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Publication number: 20140213587Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: December 2, 2013Publication date: July 31, 2014Applicant: KINEX PHARMACEUTICALS, LLCInventor: David G. Hangauer, Jr.
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Publication number: 20140213569Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: March 31, 2014Publication date: July 31, 2014Applicant: GRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER, Simon LUCAS
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Publication number: 20140213588Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.Type: ApplicationFiled: September 26, 2012Publication date: July 31, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140206690Abstract: The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.Type: ApplicationFiled: April 2, 2012Publication date: July 24, 2014Applicants: SOCIETE SPLICOS, UNIVERSITE DE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Didier Scherrer, Jamal Tazi, Romain Najman, Florence Mahuteau, Pierre Roux
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Publication number: 20140200197Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 9, 2013Publication date: July 17, 2014Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
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Publication number: 20140200217Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.Type: ApplicationFiled: January 24, 2014Publication date: July 17, 2014Inventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Patent number: 8778927Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Novartis AGInventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
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Patent number: 8778628Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 17, 2013Date of Patent: July 15, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140194424Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.Type: ApplicationFiled: December 12, 2013Publication date: July 10, 2014Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20140187555Abstract: The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.Type: ApplicationFiled: August 9, 2012Publication date: July 3, 2014Applicant: AMAKEM NVInventors: Dirk Leysen, Olivier Defert, Sandro Boland
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Publication number: 20140187554Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: ApplicationFiled: May 16, 2012Publication date: July 3, 2014Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Publication number: 20140187539Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
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Patent number: 8765739Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.Type: GrantFiled: May 14, 2010Date of Patent: July 1, 2014Assignee: Japan Tobacco Inc.Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
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Patent number: 8765730Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: July 12, 2011Date of Patent: July 1, 2014Assignee: Hoffmann-La Roche IncInventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Patent number: 8765732Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: December 20, 2012Date of Patent: July 1, 2014Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Patent number: 8765751Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.Type: GrantFiled: September 28, 2012Date of Patent: July 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
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Publication number: 20140179687Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: February 21, 2014Publication date: June 26, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Patent number: 8754107Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: November 16, 2007Date of Patent: June 17, 2014Assignee: AbbVie Inc.Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Patent number: 8754081Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.Type: GrantFiled: March 31, 2009Date of Patent: June 17, 2014Assignee: The United States of America as represented by the Secretary, Departmnet of Health and Human ServicesInventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Terrence Burke, Jr., Gagani Athauda, Sarah Choyke, Alessio Giubellino, Nelly Tan, Zhen-Dan Shi
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Publication number: 20140163017Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: ApplicationFiled: June 19, 2013Publication date: June 12, 2014Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Publication number: 20140155391Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.Type: ApplicationFiled: December 5, 2013Publication date: June 5, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Oriana Esposito, Laura Carzaniga, Carmelida Capaldi
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Publication number: 20140155400Abstract: Immunohistochemical methods and compositions for the typing of molecular subgroups of medulloblastomas are provided. The methods comprise determining a protein expression profile for a sample obtained from a medulloblastoma by detecting expression of GAB 1, filamin A, or at least two biomarker proteins selected from the group consisting of ?-catenin, YAP1, GAB1, and filamin A, and typing the medulloblastoma as a WNT pathway tumor, a SHH pathway tumor, or a non-WNT/non-SHH tumor based on this protein expression profile. Kits for typing a medulloblastoma according to these three molecular subgroups are provided. The kits comprise at least two antibodies, wherein each of said antibodies specifically binds to a distinct biomarker protein selected from the group consisting of ?-catenin, YAP1, GAB1, and filamin A, and can optionally comprise one or more of instructions for use, reagents for detecting antibody binding to one or more of said biomarker proteins, and one or more positive control samples.Type: ApplicationFiled: September 30, 2011Publication date: June 5, 2014Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventor: David Ellison
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Publication number: 20140155401Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
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Publication number: 20140148453Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: July 25, 2011Publication date: May 29, 2014Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
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Publication number: 20140148454Abstract: The invention relates to amino-arylcarboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: November 27, 2013Publication date: May 29, 2014Applicant: GRÜNENTHAL GMBHInventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder