1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Patent number: 10815216Abstract: The present invention relates to an improved process for the preparation of Aripiprazole Lauroxil of Formula (I).Type: GrantFiled: October 27, 2017Date of Patent: October 27, 2020Assignee: NEULAND PHARMA RESEARCH PRIVATE LIMITEDInventors: Ponnaiah Ravi, Neela Praveen Kumar, Batthini Guruswamy, Krishnaiah Pendem, Satya Nagendra Kumar Lakkadasu, Mahesh Gattikoppula
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Patent number: 10800779Abstract: The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: March 7, 2018Date of Patent: October 13, 2020Assignee: Incyte CorporationInventors: Chunhong He, Zhenwu Li, Liangxing Wu, Wenqing Yao, Fenglei Zhang
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Patent number: 10787448Abstract: Provided is a fluorescent probe composition including an indolizino[3,2-c]quinoline-based compound, and a nucleic acid/protein/cell imaging method using the same. Since the compound of the present invention demonstrates excellent environmental sensitivity, fluorescence intensity, photostability, nucleic acid/protein binding, intracellular permeability, etc., the compound may be effectively used for various studies of protein/cell functions and imaging technologies, such as nucleic acid/protein kinetics, drug-protein interactions, and intracellular protein imaging.Type: GrantFiled: January 23, 2018Date of Patent: September 29, 2020Assignees: SEOUL NATIONAL UNIVERSITY R & DB FOUNDATION, INDUSTRY-ACADEMIC COOPERATION FOUNDATION YONSEI UNIVERSITYInventors: Jeeyeon Lee, Ikyon Kim, Soonbum Kwon, Bumhee Lim
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Patent number: 10781207Abstract: The invention provides novel chemical compounds useful for treating cancer, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.Type: GrantFiled: October 10, 2017Date of Patent: September 22, 2020Assignee: IsoCure Biosciences Inc.Inventors: Tinghu Zhang, Jianwei Che
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Patent number: 10753947Abstract: In one aspect, the invention relates to a method for identifying a compound which modulates the activity of a voltage-gated protein. In certain embodiments, the voltage gate protein is a voltage-gated ion channel. In certain embodiments, the voltage-gated protein is a voltage sensitive phosphatase. In certain embodiments, the voltage-gated protein used in conjunction with the methods of the invention is modified to altered permeability or voltage sensitivity.Type: GrantFiled: August 29, 2014Date of Patent: August 25, 2020Assignee: D.E. SHAW RESEARCH, LLCInventors: Morten Østergaard Jensen, David Wayne Borhani, Vishwanath Jogini
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Patent number: 10723729Abstract: 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: GrantFiled: July 16, 2019Date of Patent: July 28, 2020Assignee: Hoffmann-Le Roche Inc.Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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Patent number: 10716787Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.Type: GrantFiled: April 17, 2018Date of Patent: July 21, 2020Assignee: ASTEX THERAPEUTICS LTDInventors: Eleonora Jovcheva, Timothy Pietro Suren Perera
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Patent number: 10710996Abstract: The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.Type: GrantFiled: May 23, 2016Date of Patent: July 14, 2020Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
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Patent number: 10711004Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.Type: GrantFiled: September 3, 2019Date of Patent: July 14, 2020Assignee: Genentech, Inc.Inventors: Huifen Chen, Brian Safina, Daniel Shore, Jack Terrett, Elisia Villemure, Matthew Volgraf, Stuart Ward, Aijun Lu, Robin Larouche-Gauthier, Francis Beaumier, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Luce Lepissier
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Patent number: 10710984Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.Type: GrantFiled: April 7, 2017Date of Patent: July 14, 2020Assignee: Boehringer Ingelheim International GmbHInventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer
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Patent number: 10689393Abstract: 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: GrantFiled: March 4, 2019Date of Patent: June 23, 2020Assignees: Astellas Pharma Inc., Cytokinetics, IncorporatedInventors: 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
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Patent number: 10683300Abstract: The present disclosure relates to synthesis and characterization of novel polymorphic forms of Cyclo (-His-Pro) (“CHP”).Type: GrantFiled: June 21, 2019Date of Patent: June 16, 2020Assignee: NovMetaPharma Co., Ltd.Inventors: Kay Olmstead, David Pearson, Elaine McPherson
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Patent number: 10683306Abstract: 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: GrantFiled: April 17, 2019Date of Patent: June 16, 2020Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Kyle Hoehn, Brandon Kenwood
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Patent number: 10640509Abstract: 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: GrantFiled: November 1, 2018Date of Patent: May 5, 2020Assignee: Acerta Pharma B.V.Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
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Patent number: 10611760Abstract: 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: GrantFiled: September 3, 2015Date of Patent: April 7, 2020Assignee: C4X Discovery LimitedInventors: Emma Louise Blaney, Barrie Phillip Martin, Thorsten Nowak, Martin John Watson
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Patent number: 10610529Abstract: 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: GrantFiled: January 23, 2017Date of Patent: April 7, 2020Assignee: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Likun Wang, Qiong Sun, Chen Xu, Rong Yin, Kai Liu
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Patent number: 10604536Abstract: 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: GrantFiled: May 11, 2018Date of Patent: March 31, 2020Assignee: Sunovion Pharamaceuticals Inc.Inventors: John Emmerson Campbell, Philip G. Jones, Scott Malcolm
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Patent number: 10604512Abstract: 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: GrantFiled: August 3, 2016Date of Patent: March 31, 2020Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 10604520Abstract: 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: GrantFiled: September 7, 2017Date of Patent: March 31, 2020Assignee: 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
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Patent number: 10584099Abstract: 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: GrantFiled: January 8, 2018Date of Patent: March 10, 2020Assignee: Alkermes Pharma Ireland LimitedInventors: Tarek A. Zeidan, Laura Cook Blumberg
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Patent number: 10584124Abstract: 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: GrantFiled: October 10, 2018Date of Patent: March 10, 2020Assignee: Array Biopharma Inc.Inventors: Andrew T. Metcalf, David Fry, Elizabeth A. McFaddin, Gabrielle R. Kolakowski, Julia Haas, Tony P. Tang, Yutong Jiang
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Patent number: 10570144Abstract: 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: GrantFiled: January 31, 2019Date of Patent: February 25, 2020Assignee: Avista Pharma Solutions, Inc.Inventor: Jason D. Speake
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Patent number: 10562897Abstract: 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: GrantFiled: July 18, 2018Date of Patent: February 18, 2020Assignee: JANSSEN PHARMACEUTICA NVInventors: 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
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Patent number: 10538511Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: December 29, 2017Date of Patent: January 21, 2020Assignee: Selenity Therapeutics (Bermuda), Ltd.Inventors: Steven Sparks, Christopher M. Yates, Sammy R. Shaver
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Patent number: 10517870Abstract: 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: GrantFiled: July 28, 2016Date of Patent: December 31, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Xiaofan Zheng, Louis S. Chupak
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Patent number: 10519162Abstract: 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: GrantFiled: May 10, 2018Date of Patent: December 31, 2019Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 10513523Abstract: 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: GrantFiled: April 28, 2016Date of Patent: December 24, 2019Assignee: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Bradley M. Savall, Devin M. Swanson, Dongpei Wu
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Patent number: 10479800Abstract: 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: GrantFiled: November 2, 2016Date of Patent: November 19, 2019Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Kyle Hoehn, Brandon Kenwood
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Patent number: 10438688Abstract: 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: GrantFiled: August 27, 2018Date of Patent: October 8, 2019Assignee: Purdue Research FoundationInventors: Marxa L. Figueiredo, Charles Samuel Umbaugh, Herman O. Sintim, Adriana Diaz-Quinones
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Patent number: 10426758Abstract: 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: GrantFiled: October 13, 2016Date of Patent: October 1, 2019Assignees: 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 1Inventors: Marie-Thérèse Dimanche-Boitrel, Stéphane Bach, Claire Delehouze, Yvette Mettey, Peter Goekjian, Arnaud Comte
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Patent number: 10399969Abstract: 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: GrantFiled: July 12, 2018Date of Patent: September 3, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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Patent number: 10383819Abstract: 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: GrantFiled: November 5, 2018Date of Patent: August 20, 2019Assignee: Callitas Therapeutics, Inc.Inventors: Ronald J. Thompson, James M. Thompson
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Patent number: 10377729Abstract: 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: GrantFiled: June 15, 2016Date of Patent: August 13, 2019Assignee: 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
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Patent number: 10351529Abstract: 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: GrantFiled: September 14, 2018Date of Patent: July 16, 2019Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Patent number: 10344035Abstract: 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: GrantFiled: December 29, 2016Date of Patent: July 9, 2019Assignee: 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
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Patent number: 10342794Abstract: 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: GrantFiled: April 4, 2018Date of Patent: July 9, 2019Assignee: 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
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Patent number: 10272082Abstract: 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: GrantFiled: July 12, 2012Date of Patent: April 30, 2019Assignee: Cytokinetics, Inc.Inventors: Jesse Cedarbaum, John Mao, Fady Malik, Andrew A. Wolff
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Patent number: 10259821Abstract: 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: GrantFiled: January 17, 2018Date of Patent: April 16, 2019Assignees: Astellas Pharma Inc., Cytokinetics, IncorporatedInventors: 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
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Patent number: 10246454Abstract: 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: GrantFiled: January 16, 2014Date of Patent: April 2, 2019Assignee: JANSSEN PHARMACEUTICA NVInventors: 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
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Patent number: 10245264Abstract: 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: GrantFiled: May 23, 2016Date of Patent: April 2, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Joie Garfunkle, Olga Ornoski, Dann L. Parker, Jr., Subharekha Raghavan, Libo Xu
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Patent number: 10239885Abstract: 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: GrantFiled: August 10, 2018Date of Patent: March 26, 2019Assignee: Avista Pharma Solutions, Inc.Inventor: Jason D. Speake
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Patent number: 10231452Abstract: This disclosure relates to thiopicolinamides of Formula I and their use as fungicides.Type: GrantFiled: August 30, 2017Date of Patent: March 19, 2019Assignee: Dow AgroSciences LLCInventors: Kyle A. DeKorver, Kevin G. Meyer, Chenglin Yao, Karla Bravo-Altamirano, Ronald J. Heemstra, Brannon Sam, David M. Jones
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Patent number: 10221186Abstract: 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: GrantFiled: December 4, 2015Date of Patent: March 5, 2019Assignee: 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
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Patent number: 10201623Abstract: 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: GrantFiled: March 14, 2014Date of Patent: February 12, 2019Assignee: Memorial Sloan Kettering Cancer CenterInventors: Mark Dunphy, H. William Strauss, Gabriela Chiosis
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Patent number: 10196396Abstract: 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: GrantFiled: January 13, 2017Date of Patent: February 5, 2019Assignee: HANDOK INC.Inventors: Jin-Hwa Lee, Seung-Yong Kim, Do-Ran Kim, Koo-Hyeon Ahn, Gwi-Bin Lee, Doo-Seop Kim, Hyun-Sook Hwang
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Patent number: 10195150Abstract: 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: GrantFiled: December 19, 2013Date of Patent: February 5, 2019Assignee: Kashiv Pharma, LLCInventors: Jelena Djordjevic, Murali Mohan Bommana, Wantanee Phuapradit, Navnit H. Shah, Christopher A. Pizzo
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Patent number: 10188632Abstract: 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: GrantFiled: May 5, 2017Date of Patent: January 29, 2019Assignee: Allergan Holdings Unlimited CompanyInventors: Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
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Patent number: 10189795Abstract: 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: GrantFiled: July 7, 2015Date of Patent: January 29, 2019Inventors: Kuen-Feng Chen, Chung-Wai Shiau
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Patent number: 10172856Abstract: 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: GrantFiled: April 6, 2018Date of Patent: January 8, 2019Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Wenying Chai, James P. Edwards, Russell C. Smith, Mark S. Tichenor, Jennifer D. Venable, Jianmei Wei
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Patent number: 10172937Abstract: 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: GrantFiled: May 27, 2016Date of Patent: January 8, 2019Assignee: Five Prime Therapeutics, Inc.Inventors: Thomas Harding, Kristen Pierce, Namrata Patil, Thomas Brennan, Julie Hambleton