1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 10640509
    Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: May 5, 2020
    Assignee: Acerta Pharma B.V.
    Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
  • Patent number: 10611760
    Abstract: The present invention relates to compounds that are inhibitors of the orexin-1 receptor. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: April 7, 2020
    Assignee: C4X Discovery Limited
    Inventors: Emma Louise Blaney, Barrie Phillip Martin, Thorsten Nowak, Martin John Watson
  • Patent number: 10610529
    Abstract: The present invention relates to a trabectedin-inclusive injectable pharmaceutical composition for gastrointestinal external use and a method for manufacturing the same. Specifically, the composition contains trabectedin and a first excipient, the first excipient being selected from one or more of monosaccharide or polylols. The preparation in the present invention has a stable quality, and can be applied to mass production.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: April 7, 2020
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Likun Wang, Qiong Sun, Chen Xu, Rong Yin, Kai Liu
  • Patent number: 10604512
    Abstract: The present disclosure relates to indazole compounds having the following structure: or a pharmaceutically acceptable salt thereof, for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: March 31, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10604520
    Abstract: The invention relates to compounds of formula (I): or a salt thereof, wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are ?v?1 integrin inhibitors that are useful for treating tissue specific fibrosis.
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: March 31, 2020
    Assignee: Pliant Therapeutics, Inc.
    Inventors: Lan Jiang, David John Morgans, Jr., Gustave Bergnes, Chun Chen, Hui Li, Patrick Andre, Randall L. Halcomb, Jacob Cha, Timothy Hom
  • Patent number: 10604536
    Abstract: Provided herein are substituted cyclopropane compounds, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorders.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: March 31, 2020
    Assignee: Sunovion Pharamaceuticals Inc.
    Inventors: John Emmerson Campbell, Philip G. Jones, Scott Malcolm
  • Patent number: 10584099
    Abstract: The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam-amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions.
    Type: Grant
    Filed: January 8, 2018
    Date of Patent: March 10, 2020
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Laura Cook Blumberg
  • Patent number: 10584124
    Abstract: Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: March 10, 2020
    Assignee: Array Biopharma Inc.
    Inventors: Andrew T. Metcalf, David Fry, Elizabeth A. McFaddin, Gabrielle R. Kolakowski, Julia Haas, Tony P. Tang, Yutong Jiang
  • Patent number: 10570144
    Abstract: The present invention describes compounds of Formula (I): or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of Formula (I) have activity as prostaglandin EP4 receptor antagonists, and are useful in the treatment or alleviation of pain and inflammation and other inflammation-associated disorders, such as arthritis, treating or preventing disorders or medical conditions selected from pain, inflammatory diseases and the like. Also described herein are methods of treating pain by administering the compounds of Formula (I), which are EP4 receptor antagonists.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: February 25, 2020
    Assignee: Avista Pharma Solutions, Inc.
    Inventor: Jason D. Speake
  • Patent number: 10562897
    Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: February 18, 2020
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: François Paul Bischoff, Adriana Ingrid Velter, Frederik Jan Rita Rombouts, Michel Anna Jozef De Cleyn, Sven Franciscus Anna Van Brandt, Henricus Jacobus Maria Gijsen, Chiara Zavattaro, Frans Alfons Maria Van den Keybus
  • Patent number: 10538511
    Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: January 21, 2020
    Assignee: Selenity Therapeutics (Bermuda), Ltd.
    Inventors: Steven Sparks, Christopher M. Yates, Sammy R. Shaver
  • Patent number: 10519162
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: May 10, 2018
    Date of Patent: December 31, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio-Alvar Alonso-de Diego, Michiel Luc Maria Van Gool, Maria Luz Martin-Martin, Susana Conde-Ceide, José Ignacio Andrés-Gil, Óscar Delgado-González, Gary John Tresadern, Andrés Avelino Trabanco-Suárez
  • Patent number: 10517870
    Abstract: Disclosed is a compound of Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein one R3 is H and the other R3 is an aryl group substituted with zero to 3 R3a; and R1, R2, and R3a are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors for the inhibition or prevention of platelet aggregation, and the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder. Also disclosed are methods of using such compounds for the treatment of human papillomavirus. Additionally, pharmaceutical compositions comprising at least one compound of Formula (I) are disclosed.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: December 31, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiaojun Zhang, Xiaofan Zheng, Louis S. Chupak
  • Patent number: 10513523
    Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of using compounds of Formula (I).
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: December 24, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Bradley M. Savall, Devin M. Swanson, Dongpei Wu
  • Patent number: 10479800
    Abstract: The present invention encompasses the use of compounds for a novel approach to treat and prevent diseases, conditions, and disorders such as diabetes and ischemic reperfusion injury. Compounds of the invention, including but not limited to BAM15 ((2-fluorophenyl){6-[(2-fluorophenyl)amino](1,2,5-oxadiazolo[3,4-e]pyrazin-5-yl)}amine), a mitochondrial uncoupler, can improve glucose tolerance, increases cellular oxygen consumption, treat or prevent kidney ischemia reperfusion injury reverse insulin resistance, reverse or treat hyperinsulinemia, and reverse or treat hyperlipidemia. The present invention further provides novel compounds as well as methods for identifying compounds with the same or similar properties as BAM15.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: November 19, 2019
    Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Kyle Hoehn, Brandon Kenwood
  • Patent number: 10438688
    Abstract: An in silico screening method generated compounds that are against laminin receptor 37LR and their anti-cancer functions in prostate cancer cell lines are disclosed herein. A group of derivatives based on the hit compound from the in silico screening are synthesized and tested with improved IC50 value that can have relevant clinical use for prostate cancer or osteoarthritis.
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: October 8, 2019
    Assignee: Purdue Research Foundation
    Inventors: Marxa L. Figueiredo, Charles Samuel Umbaugh, Herman O. Sintim, Adriana Diaz-Quinones
  • Patent number: 10426758
    Abstract: The present invention relates to a compound of the following general formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, for use as inhibitor of cellular necroptosis. The present invention also relates to a pharmaceutical composition comprising a compound of general formula (I), or a pharmaceutically acceptable salt and/or solvate thereof, for use for preventing and/or treating disorders associated with cellular necroptosis. The present invention also encompasses the use of a compound of the general formula (I) for organs preservation.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: October 1, 2019
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Centre National de la Recherche Scientifique (CNRS), Universite De Poitiers, Sorbonne Universite, Universite Claude Bernard Lyon 1
    Inventors: Marie-Thérèse Dimanche-Boitrel, Stéphane Bach, Claire Delehouze, Yvette Mettey, Peter Goekjian, Arnaud Comte
  • Patent number: 10399969
    Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: September 3, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Patent number: 10383819
    Abstract: A method to effect biphasic bioavailability of oral euphoric psychogenic cannabis. The method comprises the step of providing and ingesting a chambered, layered oral drug delivery arrangement, to achieve both a rapid systemic euphoric cannabis effect, and a delayed, but sustained, systemic cannabis euphoric effect.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: August 20, 2019
    Assignee: Callitas Therapeutics, Inc.
    Inventors: Ronald J. Thompson, James M. Thompson
  • Patent number: 10377729
    Abstract: The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: August 13, 2019
    Assignee: BSIM Therapeutics, S.A.
    Inventors: Carlos José Vieira Simões, Zaida Catarina Lourenço de Almeida, Teresa Margarida Vasconcelos Dias de Pinho e Melo, Rui Manuel Pontes Meireles Ferreira de Brito, Dora Cristina Silva Costa, Ana Lúcia Cabral Cardoso Lopes
  • Patent number: 10351529
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: July 16, 2019
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Patent number: 10344035
    Abstract: Disclosed is a salt of a quinoline derivative, polymorphic forms thereof, preparation methods thereof, a composition, and applications. The SPH1772 ditartrate or crystal form A thereof expresses the following excellent properties: high stability, great bioavailability, excellent pharmacokinetic properties, and better in vivo efficacy than SPH1772 free base.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: July 9, 2019
    Assignee: Shanghai Phaarmaceuticals Holding Co., Ltd.
    Inventors: Jianxin Yu, Yu Hao, Jing Zhang, Fei Zhao, Leduo Zhang, Zhenying Liu, Gongsheng Li, Yuji Wang, Na Chen, Rui Bai, Yi Fan
  • Patent number: 10342794
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: July 9, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Jennifer R. Lo, Scott A. Mitchell, Aaron C. Schmitt, Sundaramoorthi Swaminathan, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao
  • Patent number: 10272082
    Abstract: Provided is a method for treating ALS in a subject, comprising administering to the subject a therapeutically effective amount of riluzole and a therapeutically effective amount of CK-2017357. Also provided are methods of reducing the variability of riluzole exposure (e.g., Cmax and/or AUC24h) in a subject, methods of reducing the variability of riluzole exposure (e.g., Cmax and/or AUC24h) between two or more subjects, methods of decreasing the total daily dose of riluzole in a subject, methods of increasing the half-life of riluzole in a subject, methods for decreasing the frequency of riluzole dosing in the subject, and methods for reducing the incidence and/or severity of adverse events in a subject treated with riluzole.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: April 30, 2019
    Assignee: Cytokinetics, Inc.
    Inventors: Jesse Cedarbaum, John Mao, Fady Malik, Andrew A. Wolff
  • Patent number: 10259821
    Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: April 16, 2019
    Assignees: Astellas Pharma Inc., Cytokinetics, Incorporated
    Inventors: Ippei Sato, Takashi Kamikubo, Masanori Miura, Yuji Matsushima, Hiroaki Tanaka, Yasuhiro Shiina, Susumu Yamaki, Tomoyuki Saito, Hiroshi Kiyohara, Munemichi Ohe, Kayoko Mihara, Bradley Paul Morgan, Fady Malik, Scott Emile Collibee, Luke Ashcraft, Pu-Ping Lu, Jeffrey Michael Warrington, Marc Garard
  • Patent number: 10246454
    Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: April 2, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: François Paul Bischoff, Adriana Ingrid Velter, Frederik Jan Rita Rombouts, Michel Anna Jozef De Cleyn, Sven Franciscus Anna Van Brandt, Henricus Jacobus Maria Gijsen, Chiara Zavattaro, Frans Alfons Maria Van den Keybus
  • Patent number: 10245264
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: April 2, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joie Garfunkle, Olga Ornoski, Dann L. Parker, Jr., Subharekha Raghavan, Libo Xu
  • Patent number: 10239885
    Abstract: The present invention describes novel compounds, or veterinary or pharmaceutically acceptable salts thereof, veterinary or pharmaceutical compositions thereof, and medical uses thereof. The compounds of the invention have activity as prostaglandin EP4 receptor antagonists and are useful in the treatment or alleviation of pain, inflammation and inflammation-associated disorders. Also described herein are methods for treating pain by administering the compounds of the invention. For example, the invention describes 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-a]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyflurea of the formula: veterinary or pharmaceutical compositions thereof, and methods of treatment using the subject compound and compositions thereof.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: March 26, 2019
    Assignee: Avista Pharma Solutions, Inc.
    Inventor: Jason D. Speake
  • Patent number: 10231452
    Abstract: This disclosure relates to thiopicolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: March 19, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Kyle A. DeKorver, Kevin G. Meyer, Chenglin Yao, Karla Bravo-Altamirano, Ronald J. Heemstra, Brannon Sam, David M. Jones
  • Patent number: 10221186
    Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: March 5, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark W. Embrey, Thomas H. Graham, Izzat T. Raheem, John D. Schreier, Sherman T. Waddell, John S. Wai, Lihong Hu, Xuanjia Peng
  • Patent number: 10201623
    Abstract: The present invention provides new methods for cardiac imaging and related medical applications thereof. In some embodiments, the present invention provides a method for the diagnosis of cardiovascular diseases, conditions, or disorders. In some embodiments, the present invention provides a method for the treatment or prevention of cardiovascular diseases, conditions, or disorders. In some embodiments, the present invention provides methods for monitoring the effect of cancer treatment on the heart, and/or methods for monitoring a cancer treatment regimen. In some embodiments, the present invention provides a method for selecting subjects for a test or treatment. In some embodiments, the present invention provides a method for determining the dosage of a drug. In some embodiments, the present invention provides methods for determining the risk of a cardiovascular disease, for assessing risk of a cardiovascular disease, and/or for determining the risk of heart attack.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 12, 2019
    Assignee: Memorial Sloan Kettering Cancer Center
    Inventors: Mark Dunphy, H. William Strauss, Gabriela Chiosis
  • Patent number: 10196396
    Abstract: The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: February 5, 2019
    Assignee: HANDOK INC.
    Inventors: Jin-Hwa Lee, Seung-Yong Kim, Do-Ran Kim, Koo-Hyeon Ahn, Gwi-Bin Lee, Doo-Seop Kim, Hyun-Sook Hwang
  • Patent number: 10195150
    Abstract: In some aspects of the present invention is a formulation comprising a solid dispersion or intimate mixture of a poorly water soluble drug and an ionic polymer surprisingly exhibiting fast disintegration of tablet.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: February 5, 2019
    Assignee: Kashiv Pharma, LLC
    Inventors: Jelena Djordjevic, Murali Mohan Bommana, Wantanee Phuapradit, Navnit H. Shah, Christopher A. Pizzo
  • Patent number: 10189795
    Abstract: The present invention provides new compounds of formula I(a)-I(d) and II, The compounds can inhibit cancerous inhibitor of protein phosphate 2A (CIP2A), can be used as protein phosphate 2A (PP2A) accelerator and oncoprotein SET antagonist, and can treat cancers effectively.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: January 29, 2019
    Inventors: Kuen-Feng Chen, Chung-Wai Shiau
  • Patent number: 10188632
    Abstract: Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: January 29, 2019
    Assignee: Allergan Holdings Unlimited Company
    Inventors: Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
  • Patent number: 10172937
    Abstract: The present invention provides antibodies that bind FGFR2IIIb, wherein the antibodies are afucosylated. The present invention provides compositions comprising antibodies that bind FGFR2IIIb, wherein at least 95% of the antibodies in the composition are afucosylated. In some embodiments, methods of treating cancer comprising administering afucosylated anti-FGFR2IIIb antibodies are provided.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: January 8, 2019
    Assignee: Five Prime Therapeutics, Inc.
    Inventors: Thomas Harding, Kristen Pierce, Namrata Patil, Thomas Brennan, Julie Hambleton
  • Patent number: 10172856
    Abstract: The present invention relates to 2,4-diaminopyrimidines and pharmaceutically acceptable salts thereof, purification methods for the same, pharmaceutical compositions containing them, methods of obtaining and using them for the treatment of disease states, disorders, and conditions mediated by the histamine H4 receptor activity.
    Type: Grant
    Filed: April 6, 2018
    Date of Patent: January 8, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Wenying Chai, James P. Edwards, Russell C. Smith, Mark S. Tichenor, Jennifer D. Venable, Jianmei Wei
  • Patent number: 10167291
    Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: January 1, 2019
    Assignee: Acerta Pharma B.V.
    Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
  • Patent number: 10159667
    Abstract: The present invention relates to a composition for preventing or treating renal diseases. The composition of the present invention improves lipid metabolism, prevents histological damage including renal fibrosis, alleviates microalbuminuria, and maintains nephrons of renal glomeruli. Therefore, the composition is useful for treating renal diseases.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: December 25, 2018
    Assignee: DONG-A ST Co., Ltd
    Inventors: Dae Ryong Cha, Young Sun Kang, Jin Joo Cha, Ji Eun Lee, Hyun Wook Kim, Mi Hwa Lee, Jung Eun Kim, Mi-Kyung Kim, Moon-Ho Son, Soon Hoe Kim
  • Patent number: 10144724
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: December 4, 2018
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 10131668
    Abstract: Described herein, inter alia, are compositions and methods of using the same for modulating the activity of Ire1 using for example, substituted imidazopyrazine compounds.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: November 20, 2018
    Assignees: The Regents of the University of California, University of Washington Through Its Center For Commercialization
    Inventors: Bradley J. Backes, Dustin J. Maly, Scott A. Oakes, Feroz R. Papa, Gayani Perera, Likun Wang
  • Patent number: 10125114
    Abstract: The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: November 13, 2018
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: James Bradner, Dennis Buckley, Georg Winter
  • Patent number: 10122633
    Abstract: A method for selecting an access network in a terminal of a mobile communication system according to one embodiment of the present specification comprises the steps of: if traffic is generated in the terminal, selecting an access network according to the characteristics of the generated traffic and network selection policy information; and transmitting and receiving the generated traffic via the selected access network. According to the embodiment, the present invention adjusts priorities of accesses given to users and applications in a wireless communication system including heterogenerous networks, thereby reducing processes for reselecting an access network of a user terminal, and reducing the cases of unnecessarily accessing a network having a low priority or requiring high costs for a long time. Therefore, the present invention can enhance user convenience and improve communication efficiency.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: November 6, 2018
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Sangsoo Jeong, Songyean Cho, Beomsik Bae
  • Patent number: 10117875
    Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Grant
    Filed: April 3, 2017
    Date of Patent: November 6, 2018
    Assignee: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Patent number: 10112911
    Abstract: This disclosure relates to: (a) compounds and salts of formula (I), formula (II), formula (III), and formula (IV), that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: October 30, 2018
    Assignee: ABBVIE INC.
    Inventors: Artour Gomtsian, Tatyana Dekhtyar, Kristine E. Frank, Michael M. Friedman, Nathan Josephsohn, M-Akhteruzzaman Molla, Anil Vasudevan, Iok Chan Ng, Mikhail Chafeev
  • Patent number: 10112903
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: October 30, 2018
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Patent number: 10106544
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is one of the groups represented below wherein A is a bond, CH?CH or C?C; U is N or CH; V is N or CH; W represents N or CH; and R1A, R2A, R3A, R1B and R1C are as defined in the claims; and salts thereof.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: October 23, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Gaelle Chapoux, Jean-Christophe Gauvin, Azely Mirre, Philippe Panchaud, Christine Schmitt, Jean-Luc Specklin, Jean-Philippe Surivet
  • Patent number: 10106542
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”) useful for the treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved (e.g. mood disorder, schizophrenia, etc.). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: October 23, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio-Alvar Alonso-de Diego, José Maria Cid-Núñez, Óscar Delgado-González, Annelies Marie Antonius Decorte, Michiel Luc Maria Van Gool, Gregor James MacDonald, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Aránzazu Garcia-Molina, José Ignacio Andrés-Gil
  • Patent number: 10100040
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: October 16, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Qing Xu, Brian W. Metcalf, Stephen L. Gwaltney, II, Jason R. Harris, Calvin W. Yee
  • Patent number: 10098876
    Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: October 16, 2018
    Inventors: Franco Borsini, Kenneth Robert Evans