Patents Issued in August 1, 2017
  • Patent number: 9718777
    Abstract: A process for the preparation and isolation of crystalline miglustat without the use of a column chromatography or ion exchange purification. The crystalline miglustat has a high purity and a melting point of 128° C. and an endothermic peak is 133° C.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: August 1, 2017
    Assignee: Navinta, LLC
    Inventors: Shrenik K. Shah, Raju Mahadev Kharatkar, Chiragkumar Anilkumar Bhatt, Jitendra Bhagwandas Kevat
  • Patent number: 9718778
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to mixed disulfide conjugates of thienopyridine compounds, and their use as therapeutics for the treatment, amelioration, and prevention of cardiovascular diseases.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: August 1, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Haoming Zhang, Paul Hollenberg
  • Patent number: 9718779
    Abstract: The present invention provides a novel intermediate as well as novel polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula-1 and processes for their preparation.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: August 1, 2017
    Assignee: MSN Laboratories Limited
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Mummadi Venkatesh
  • Patent number: 9718780
    Abstract: The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1, R2a, R2b, A1, A2, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: August 1, 2017
    Inventors: Laykea Tafesse, Jiangchao Yao
  • Patent number: 9718781
    Abstract: The invention generally relates to methods and compounds for treating proliferative disorders, viral infections, or both. In some embodiments, the invention provides an anticancer or antiviral compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating a proliferative disorder or a viral infection including administering an anticancer or antiviral compound that binds to a thromboxane receptor, has preferential binding for either TPalpha (TP?) or TPbeta (TP?) receptor subtype.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: August 1, 2017
    Assignee: UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN
    Inventors: B. Therese Kinsella, Helen Reid
  • Patent number: 9718782
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • Patent number: 9718783
    Abstract: 4,6-Dibromo-3-hydroxypicolinonitrile may be prepared from furfural in a series of chemical steps selected from cyano-amination, amine salt formation and bromination-rearrangement. 4-Alkoxy-3-hydroxypicolinic acids may be conveniently prepared from 4,6-dibromo-3-hydroxypicolinonitrile in a series of chemical steps selected from bromo substitution, nitrile hydrolysis and halogen reduction.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: August 1, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: James M. Renga, Yuanming Zhu, Gregory T. Whiteker, Nakyen Choy, Kenneth E. Stockman
  • Patent number: 9718784
    Abstract: The present invention relates to substituted pyrazole compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof) and pharmaceutical formulations thereof.
    Type: Grant
    Filed: April 18, 2016
    Date of Patent: August 1, 2017
    Assignees: DUKE UNIVERSITY, CHAPERONE THERAPEUTICS, INC.
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose Serafin Mendoza
  • Patent number: 9718785
    Abstract: Compounds of the formula I in which R, Y, R1, X1, X2, X3 and q have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: August 1, 2017
    Assignee: MERCK PATENT GMBH
    Inventors: Christos Tsaklakidis, Wolfgang Staehle, Birgitta Leuthner, Thomas Fuchss
  • Patent number: 9718786
    Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: August 1, 2017
    Assignee: Lantheus Medical Imaging, Inc.
    Inventors: David S. Casebier, Ajay Purohit, Heike S. Radeke
  • Patent number: 9718787
    Abstract: Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: August 1, 2017
    Assignee: CHENGDU DI'AO PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Jianxin Ji, Na Guo, Ting Xue, Bingqiang Kang, Xinfa Ye, Xin Chen, Tao Zhang
  • Patent number: 9718788
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: August 1, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil
  • Patent number: 9718789
    Abstract: Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure: wherein R1, R2, R3 and n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: August 1, 2017
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Neil J. Ashweek, John P. Williams, Deborah Slee, Manisha Moorjani
  • Patent number: 9718790
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Ri are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstjtuted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: August 1, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Tohru Horiguchi, Kentaro Asahi, Yasuhiko Fujii
  • Patent number: 9718791
    Abstract: Described are methods for preparing salts of 5-nitrotetrazolate that include reacting aqueous solutions of 5-aminotetrazole, an acid, and sodium nitrite in a continuous flow system at an ambient temperature.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: August 1, 2017
    Assignee: Pacific Scientific Energetic Materials Company
    Inventors: Jon G. Bragg, Jason B. Pattison, John W. Fronabarger, Michael D. Williams
  • Patent number: 9718792
    Abstract: This invention pertains generally to compounds of Formula I and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention pertains to methods and compositions for treating infections caused by Gram-negative bacteria.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: August 1, 2017
    Assignee: Novartis AG
    Inventors: Jiping Fu, Xianming Jin, Subramanian Karur, Guillaume LaPointe, Patrick Lee, Zachary Kevin Sweeney
  • Patent number: 9718793
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: August 1, 2017
    Assignees: Vernalis (R&D) Ltd., Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Patent number: 9718794
    Abstract: The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 1, 2017
    Assignee: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 9718795
    Abstract: The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms associated to schizophrenia, with the following structural formula: (A) The invention further relates to the synthesis of intermediates useful in the preparation of Cariprazine.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: August 1, 2017
    Assignee: CHEMO RESEARCH, S.L.
    Inventors: Maurizio Taddei, Elena Cini, Marcello Rasparini
  • Patent number: 9718796
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: August 1, 2017
    Assignees: VENTIRX PHARMACEUTICALS, INC., ARRAY BIOPHARMA, INC.
    Inventors: James Jeffry Howbert, Robert Hershberg, Laurence E. Burgess, Hong Woon Yang
  • Patent number: 9718797
    Abstract: Disclosed are methods for preparing a mixture of eight diasteromers of vittatalactone Also disclosed are mixtures of eight diasteromers of vittatalactone produced by the methods described herein. In addition there are described compositions comprising a mixture of eight diasteromers of vittatalactone and optionally (2E,6Z)-nona-2,6-dienal and optionally cucurbitacin B or cucurbitacin B, and optionally a carrier. Furthermore, there are describe methods of attracting Acalymma vittatum to an object or area, involving treating said object or area with a Acalymma vittatum attracting composition containing a Acalymma vittatum attracting effective amount of the compositions described herein.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: August 1, 2017
    Assignees: The United States of America, as Represented by the Secretary of Agirculture, Chemveda Life Sciences, Inc.
    Inventors: Kamlesh R. Chauhan, Bheema R. Paraselli
  • Patent number: 9718798
    Abstract: Provided are solid forms of 5-(halomethyl)furfural, including a crystalline form of 5-(chloromethyl)furfural. Provided are also methods for preparing solid forms of 5-(halomethyl)furfural by crystallization using certain solvents.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: August 1, 2017
    Assignee: MICROMIDAS, INC.
    Inventors: Shawn M. Browning, Makoto N. Masuno, John Bissell, II, Benjamin F. Nicholson
  • Patent number: 9718799
    Abstract: Isoflavonoids or pharmaceutically acceptable salts thereof or pharmaceutically acceptable compositions thereof for the treatment of prostate cancer or for the treatment or inhibition of prostate cancer metastasis in a patient in need thereof are disclosed.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: August 1, 2017
    Assignee: University of Kentucky Research Foundation
    Inventors: Svitlana P. Bondarenko, Mykhaylo S. Frasinyuk, Chunming Liu, David S. Watt
  • Patent number: 9718800
    Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: August 1, 2017
    Assignee: ASTRAZENECA AB
    Inventors: Bernard Christophe Barlaam, Sebastien Louis Degorce, Christine Marie Paul Lambert-Van Der Brempt, Remy Robert Morgentin, Patrick Ple
  • Patent number: 9718801
    Abstract: The present invention is directed to a method and device to isolate compounds from plant material using vibrational pulsing, vibrational decanting, vibrational sieving and vibrational rinsing. A susceptible liquid is generated by vibrational agitation, decanted when in a vibrating container and then collected by passing over a series of vibrating screens and then rinsed with water while collected on the vibrating screens and the residue collected. The isolated compound can either be collected in the decant or retained on the screens. In an embodiment of the invention, the vibrational rinsing step reduces unwanted impurities isolated.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: August 1, 2017
    Assignee: JP LOVE
    Inventor: J P Love
  • Patent number: 9718802
    Abstract: The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2? diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2? diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: August 1, 2017
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Liang Zhang, Chuan Liu, Jinyi Xu, Zhaozhao Zhang, Zhi Chen, Jian Chai, Zhiqing Yang, Hairong Luo, Xiangyang Zhang
  • Patent number: 9718803
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: August 1, 2017
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu Harrington, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Patent number: 9718804
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: August 1, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Ling Chen, Gene M. Dubowchik, Swanee E. Jacutin-Porte, Vivekananda M. Vrudhula, Senliang Pan, Prasanna Sivaprakasam, John E. Macor
  • Patent number: 9718805
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of A?-related diseases.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: August 1, 2017
    Assignee: Acturum Life Science AB
    Inventors: Yevgeni Besidski, Ulrika Yngve, Kim Paulsen, Christian Erik Linde, Jonas Malmborg
  • Patent number: 9718806
    Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: August 1, 2017
    Assignee: AstraZeneca AB
    Inventors: David Yunzhi Li, Jiabing Wang, Zhenfan Yang, Qingbei Zeng, Xiaolin Zhang
  • Patent number: 9718807
    Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: August 1, 2017
    Assignee: GILEAD PHARMASSET LLC
    Inventors: Robert William Scott, Justin Philip Vitale, Kenneth Stanley Matthews, Martin Gerald Teresk, Alexandra Formella, Jared Wayne Evans
  • Patent number: 9718808
    Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dipshikha Biswas, Fa-Xiang Ding, Shuzhi Dong, Xin Gu, Jinlong Jiang, Alexander Pasternak, Takao Suzuki, Joseph Vacca, Shouning Xu
  • Patent number: 9718809
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: August 1, 2017
    Assignee: Kancera AB
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Patent number: 9718810
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: August 1, 2017
    Assignee: IGNYTA, INC.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Patent number: 9718811
    Abstract: The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)-mepazine and one of its intermediates.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: August 1, 2017
    Assignees: Helmholtz Zentrum München—Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH), Ludwig-Maximilians—Universität München
    Inventors: Daniel Krappmann, Daniel Nagel, Florian Schlauderer, Katja Lammens, Karl-Peter Hopfner, Robert A. Chrusciel, Dale L. Kling
  • Patent number: 9718812
    Abstract: The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: August 1, 2017
    Assignee: Axxam S.P.A.
    Inventors: Paolo Pevarello, Stefan Lohmer, Chiara Llberati, Pierfausto Seneci, Cristina Pesenti, Adolfo Prandi
  • Patent number: 9718813
    Abstract: The present invention is directed to imidazolin-5-one derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, and are defined herein.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: August 1, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J Connolly, Tianbao Lu
  • Patent number: 9718814
    Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: August 1, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shigemitsu Matsumoto, Yasushi Hattori, Masashi Toyofuku, Shinji Morimoto, Takuto Kojima, Tomohiro Kaku, Mitsuhiro Ito
  • Patent number: 9718815
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: January 8, 2015
    Date of Patent: August 1, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 9718816
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1-R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 1, 2017
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Kenneth W. Duncan, Lorna Helen Mitchell, Lei Jin, Robert E. Babine
  • Patent number: 9718817
    Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein Ring A, Ring B, R, R2, R3, n, and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (ROR?t). These compounds prevent, inhibit, or suppress the action of ROR?t and are therefore useful in the treatment of ROR?t mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: August 1, 2017
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sachin S. Chaudhari, Abraham Thomas, Ashok B. Kadam, Sachin V. Dhone, Bharat G. Adik, Neelima Khairatkar-Joshi, Daisy M. Shah, Malini Bajpai
  • Patent number: 9718818
    Abstract: The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane DeMong, Thomas J. Greshock, Ronald K. Chang, Xing Dai, Hong Liu, John A. McCauley, Wei Li, Kallol Basu, Jack D. Scott, Michael Miller
  • Patent number: 9718819
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment 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: Grant
    Filed: February 1, 2016
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yunfu Luo, Zhiyu Lei
  • Patent number: 9718820
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: August 1, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel J. Parks, William J. Parsons, Scott Ballentine, Shawn Branum
  • Patent number: 9718821
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: August 1, 2017
    Assignee: AbbVie Inc.
    Inventors: Keith W. Woods, Anthony Mastracchio, Chunqiu Lai, Viraj B. Gandhi, Thomas D. Penning
  • Patent number: 9718822
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: August 1, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
  • Patent number: 9718823
    Abstract: The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability.
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: August 1, 2017
    Assignee: ZHEJIANG MEDICINE CO., LTD. XINCHANG PHARMACEUTICAL FACTORY
    Inventors: Guofeng Wu, Yongmei Xu, Wei Mao, Chunlin Chen, Zhanggui Wu, Xiaoqin Lin, Jun Wang, Jinna Cai, Sen Xiao, Lili Lv
  • Patent number: 9718824
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: August 1, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventor: Kevin Klopfer
  • Patent number: 9718825
    Abstract: The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: August 1, 2017
    Assignee: SANOFI
    Inventors: Marc Nazare, Nis Halland, Friedemann Schmidt, Heinz-Werner Kleemann, Tilo Weiss, Joachim Saas, Carsten Struebing
  • Patent number: 9718826
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: August 1, 2017
    Assignee: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Dieter Dorsch