Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Patent number: 9376432Abstract: This invention is related to the use of inhibitors of vascular endothelial growth factor receptor 3 for treating hepatocellular carcinoma.Type: GrantFiled: July 16, 2013Date of Patent: June 28, 2016Assignee: SANOFIInventors: Antoine Alam, Isabelle Blanc
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Patent number: 9376434Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: GrantFiled: March 16, 2015Date of Patent: June 28, 2016Assignee: Merial Inc.Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
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Patent number: 9370533Abstract: Pharmaceutical or medical compositions for treating a wound are provided, the composition comprise microspheres as an active ingredient and water as a carrier for said microspheres. In some embodiments, compositions comprising a thickening agent dissolved within the water to form a solution having a specific gravity similar to that of the microspheres are provided.Type: GrantFiled: September 12, 2013Date of Patent: June 21, 2016Assignee: PolyHeal Ltd.Inventors: Vladimir Ritter, Mery Kleyman, Deborah Hanah Bartfeld, Eilon Asculai
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Patent number: 9364466Abstract: The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A? B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.Type: GrantFiled: February 13, 2015Date of Patent: June 14, 2016Assignee: Daiichi Sankyo Company, LimitedInventors: Ashwani Kumar Verma, Kumaragurubaran Nagaswamy, Lalima Sharma, Soma Ghosh, Balkrishna Ramchandra Kale, Aniruddha Mondal, Punit Kumar Srivastava, Sunanda Ghosh Dastidar, Rijwan Jaffer Momin, Pradip Balu Wagh, Sonali Nanasaheb Pansare, Pramod Raosaheb Markad, Yogesh Balasaheb Khairnar, Rie Miyauchi, Takeshi Murata, Masayuki Ishizaki, Masatoshi Nagamochi, Shin Iimura
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Patent number: 9359350Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: GrantFiled: February 11, 2015Date of Patent: June 7, 2016Assignee: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Patent number: 9358231Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: GrantFiled: November 24, 2014Date of Patent: June 7, 2016Assignees: Dana-Farber Cancer Institute, Inc., University of MiamiInventors: Nathanael Gray, Hwan Geun Choi, Xianming Deng, Jianming Zhang, Izidore Lossos
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Patent number: 9359275Abstract: Provided herein are pure and isolated natural products and analogs thereof of Formula (I), (II), (III), and (IV), pharmaceutical compositions thereof, and methods of use, for example, for treating a bacterial infection. Further provided are methods useful in identifying an inhibitor of bacterial sugar fermentation in a bacterial strain, such as a compound (inhibitor) of Formula (I), (II), (III), or (IV): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 25, 2013Date of Patent: June 7, 2016Assignees: Children's Medical Center Corporation, President and Fellows of Harvard CollegeInventors: Paula I. Watnick, Patrick Ymele-Leki, Jon Clardy, Shugeng Cao
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Patent number: 9328089Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.Type: GrantFiled: June 17, 2015Date of Patent: May 3, 2016Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao
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Patent number: 9314452Abstract: Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).Type: GrantFiled: February 24, 2014Date of Patent: April 19, 2016Assignee: MediciNova, Inc.Inventors: Michael E. Kalafer, Kenneth W. Locke, Kazuko Matsuda, Richard E. Gammans
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Patent number: 9309243Abstract: A series of imidazo[1,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: July 5, 2013Date of Patent: April 12, 2016Assignee: UCB Biopharma SPRLInventors: Jonathan Mark Bentley, Daniel Christopher Brookings, Julien Alistair Brown, Thomas Paul Cain, Praful Tulshi Chovatia, Anne Marie Foley, Ellen Olivia Gallimore, Laura Jane Gleave, Alexander Heifetz, Helen Tracey Horsley, Martin Clive Hutchings, Victoria Elizabeth Jackson, James Andrew Johnson, Craig Johnstone, Boris Kroeplien, Fabien Claude Lecomte, Deborah Leigh, Martin Alexander Lowe, James Madden, John Robert Porter, Joanna Rachel Quincey, Laura Claire Reed, James Thomas Reuberson, Anthony John Richardson, Sarah Emily Richardson, Matthew Duncan Selby, Michael Alan Shaw, Zhaoning Zhu
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Patent number: 9309245Abstract: The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3 and R4 are described herein.Type: GrantFiled: April 2, 2013Date of Patent: April 12, 2016Assignee: Entasis Therapeutics LimitedInventors: Helen McGuire, Shanta Bist, Neil Bifulco, Liang Zhao, Ye Wu, Hoan Huynh, Hui Xiong, Janelle Comita-Prevoir, Daemian Dussault, Bolin Geng, Brendan Chen, Thomas Durand-Reville, Satenig Guler
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Patent number: 9302987Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,Type: GrantFiled: March 13, 2015Date of Patent: April 5, 2016Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
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Patent number: 9295669Abstract: The present invention relates to a combination therapy of propane-1-sulfonic acid{3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl-2,4-difluoro-phenyl]-amide}, or a pharmaceutically acceptable salt thereof, and an interferon for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer. In particular, the present invention relates to such a therapy wherein the interferon is peginterferon alfa-2a and the disorder is melanoma containing the V600E b-Raf mutation.Type: GrantFiled: December 7, 2011Date of Patent: March 29, 2016Assignee: Hoffman La-Roche Inc.Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
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Patent number: 9289419Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compoundsType: GrantFiled: February 26, 2015Date of Patent: March 22, 2016Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ganesh Prabhu, Ashok Tehim, Vidyadhar Paradkar, Marahanakuli Prasanna Dattatreya, Nanjegowda Jagadeesh Mavinhalli
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Patent number: 9278968Abstract: [Problem] A pharmaceutical composition for treating or preventing various cardiovascular diseases, which have sGC activities based on improvement of cGMP signals, is provided. [Means for Solution] It was found that imidazo[1,2-a]pyridine compounds having a carbamoyl group at the 3-position and a particular cyclic group at the 8-position via a methyleneoxy group, or a salt thereof have sGC activation, and are useful as active ingredients of pharmaceutical compositions for treating or preventing various sGC-related cardiovascular diseases, in particular, peripheral arterial diseases, intermittent claudication, critical limb ischemia, hypertension, and pulmonary hypertension, thereby completing the present invention.Type: GrantFiled: November 28, 2013Date of Patent: March 8, 2016Assignee: Astellas Pharma Inc.Inventors: Toshio Kurosaki, Tsubasa Watanabe, Kazuhiko Ohne, Hiroki Ishioka, Eisuke Nozawa, Takeshi Hanazawa, Shunichiro Hachiya, Hiroshi Shibata, Yuji Koga, Ryo Mizoguchi
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Patent number: 9266884Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: GrantFiled: November 5, 2014Date of Patent: February 23, 2016Assignee: SciFluor Life Sciences, Inc.Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Patent number: 9241930Abstract: Substituted perhydro pyrrolopyridines and methods for their use in the treatment of HIV infections, AIDS, and AIDS-related diseases, and in the treatment of BVDV infections are described herein. Also, pharmaceutical compositions comprising the substituted perhydro pyrrolopyridines are useful for the treatment of HIV infections, AIDS, and AIDS-related diseases. The compositions include one or more carriers, diluents, or excipients, or a combination thereof.Type: GrantFiled: August 23, 2012Date of Patent: January 26, 2016Assignee: NovaDrug, LLCInventor: Eliezer Huberman
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Patent number: 9233104Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: GrantFiled: February 12, 2015Date of Patent: January 12, 2016Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 9206183Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: GrantFiled: February 18, 2011Date of Patent: December 8, 2015Assignee: ALMIRALL, S.A.Inventors: Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Paul Robert Eastwood, Jacob Gonzalez Rodrigues, Victor Giulio Matassa
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Patent number: 9199987Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: GrantFiled: January 7, 2014Date of Patent: December 1, 2015Assignees: Savira pharmaceuticals GmbH, European Molecular Biology Laboratory, F. Hoffmann-La Roche AGInventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
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Patent number: 9193723Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: GrantFiled: May 10, 2013Date of Patent: November 24, 2015Assignee: AbbVie Inc.Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
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Patent number: 9187472Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: GrantFiled: May 10, 2013Date of Patent: November 17, 2015Assignee: AbbVie Inc.Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
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Patent number: 9187474Abstract: This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.Type: GrantFiled: March 5, 2013Date of Patent: November 17, 2015Assignees: Deciphera Pharmaceuticals, LLC, Eli Lilly and CompanyInventors: Daniel L. Flynn, Michael D. Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, Timothy Malcolm Caldwell, William C. Patt, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
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Patent number: 9181247Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. The compounds include substituted pyrrolo [2,3b]pyridines having Formula IX Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: GrantFiled: October 7, 2014Date of Patent: November 10, 2015Assignee: The University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
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Patent number: 9163020Abstract: The invention provides compounds of formula (I) and methods of treating a Mycobacterium infection or tuberculosis, or inhibiting DprE1 with the same.Type: GrantFiled: July 10, 2014Date of Patent: October 20, 2015Assignees: Global Alliance for TB Drug Development, Foundation for Neglected Disease ResearchInventors: Pravin S. Shirude, Maruti N. Naik, Vikas Narayan Shinde, Shahul Hameed Peer Mohamed, Monalisa Chatterji, Radha K. Shindil
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Patent number: 9150570Abstract: Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.Type: GrantFiled: March 11, 2013Date of Patent: October 6, 2015Assignee: Plexxikon Inc.Inventor: Prabha N. Ibrahim
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Patent number: 9150548Abstract: The invention provides a combination of a) a compound of Formula Ia: [insert Formula Ia], or a pharmaceutically acceptable salt thereof, and b) vemurafenib or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer.Type: GrantFiled: March 30, 2012Date of Patent: October 6, 2015Assignee: Genentech, Inc.Inventors: Klaus Hoeflich, Mark Merchant
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Patent number: 9139604Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 19, 2014Date of Patent: September 22, 2015Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina E. Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten A. Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie O'Shea, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
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Patent number: 9133190Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.Type: GrantFiled: July 23, 2014Date of Patent: September 15, 2015Assignee: PFIZER INC.Inventors: Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Chakrapani Subramanyam, Lei Zhang
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Patent number: 9134300Abstract: The subject matter disclosed herein pertains to a method for screening drugs using second-harmonic generation microscopy. The tissue is scanned with a pulsed laser light which has an excitation wavelength. At least some of microtubules within the tissue produce generated light with a second-harmonic wavelength that is half the excitation wavelength. A microtubule pattern within the tissue is determined based on an analysis of the generated second-harmonic wavelength.Type: GrantFiled: June 17, 2014Date of Patent: September 15, 2015Assignees: Research Foundation of the City University of New York, Research Foundation of the State University of New YorkInventors: Ioannis Danias, Hyungsik Lim
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Patent number: 9132133Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: January 30, 2015Date of Patent: September 15, 2015Assignee: Wockhardt Ltd.Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Patent number: 9127003Abstract: Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.Type: GrantFiled: July 26, 2012Date of Patent: September 8, 2015Assignee: Glaxo Group LimitedInventors: Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Robert John Sheppard, Ann Louise Walker, Christopher Wellaway, David Matthew Wilson
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2-amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors
Patent number: 9126972Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.Type: GrantFiled: May 16, 2012Date of Patent: September 8, 2015Assignee: SANOFIInventors: Alain Braun, Olivier Duclos, Gilbert Lassalle, Franz Lorge, Valerie Martin, Olaf Ritzeler, Aurelie Strub -
Patent number: 9114136Abstract: Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).Type: GrantFiled: December 21, 2012Date of Patent: August 25, 2015Assignee: MEDICINOVA, INC.Inventors: Michael E. Kalafer, Kenneth W. Locke, Kazuko Matsuda, Richard E. Gammans
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Patent number: 9115131Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: GrantFiled: January 21, 2015Date of Patent: August 25, 2015Assignee: Wockhardt Ltd.Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
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Patent number: 9108951Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: GrantFiled: October 12, 2012Date of Patent: August 18, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Patent number: 9090616Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: GrantFiled: January 16, 2015Date of Patent: July 28, 2015Assignee: Wockhardt Ltd.Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
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Patent number: 9090615Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 22, 2014Date of Patent: July 28, 2015Assignee: HOFFMANN-LA ROCHE INC.Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
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Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as janus kinase inhibitors
Patent number: 9090611Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: GrantFiled: April 17, 2014Date of Patent: July 28, 2015Assignee: Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Patent number: 9067887Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: GrantFiled: February 28, 2014Date of Patent: June 30, 2015Assignee: OTSUKA PHARMACEUTICAL CO., LTDInventors: Mamuti Abudusaimi, Fangguo Ye, Jiangqin Sun, Hisashi Miyamoto, Jay-Fei Cheng, Daisuke Oka
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Patent number: 9056099Abstract: Substituted perhydro pyrrolopyridines and methods for their use in the treatment of viral diseases including hepatitis C viral infections are described herein.Type: GrantFiled: February 25, 2011Date of Patent: June 16, 2015Assignee: NovaDrug, LLCInventor: Eliezer Huberman
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Publication number: 20150148372Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: November 26, 2014Publication date: May 28, 2015Applicant: INCYTE CORPORATIONInventors: Eddy W. Yue, Andrew P. Combs
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Publication number: 20150148375Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: November 26, 2014Publication date: May 28, 2015Applicant: Incyte CorporationInventors: Eddy W. Yue, Andrew P. Combs, Andrew W. Buesking
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Publication number: 20150148342Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: November 26, 2014Publication date: May 28, 2015Applicant: INCYTE CORPORATIONInventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
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Publication number: 20150148334Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: June 27, 2014Publication date: May 28, 2015Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Patent number: 9040555Abstract: The present invention provides compounds having the general structural formula (I), and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.Type: GrantFiled: January 26, 2013Date of Patent: May 26, 2015Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
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Patent number: 9040554Abstract: Disclosed are solid forms of 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)-imidazo[1,2-a]pyridine-2-carboxamide (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are nematocidal compositions comprising a nematocidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematicide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant from nematodes comprising applying to the plant, or portion, or seed thereof, or to the growing medium of the plant, a nematocidally effective amount of Compound 1 comprising the polymorph Form A.Type: GrantFiled: October 5, 2012Date of Patent: May 26, 2015Assignee: E I DU PONT DE NEMOURS AND COMPANYInventors: Christian Hoffmann, William J Marshall, Rafael Shapiro, Richard A Berger
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Patent number: 9040551Abstract: The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.Type: GrantFiled: June 4, 2010Date of Patent: May 26, 2015Assignees: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA, ALBERTA HEALTH SERVICESInventors: Michael Weinfeld, Dennis G. Hall, Feridoun Karimi-Busheri, Gary Kenneth Freschauf, Todd Randall Mereniuk
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Publication number: 20150140093Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.Type: ApplicationFiled: November 6, 2014Publication date: May 21, 2015Inventors: Cory J. Berkland, Lianjun Shi, Nashwa El Gendy, Carl Plumley, Mark Bailey
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Publication number: 20150140082Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier