1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 10973830
    Abstract: The present invention relates to Provided are compounds of Formula (I): wherein R1, R2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: April 13, 2021
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
  • Patent number: 10974081
    Abstract: The disclosure relates to methods for treating or preventing a sleep disorder by administering a compound of formula (1)(1), or a compound of formula (1A), (1B), (1C), (1D), (1E), or (1F) to an animal in need of such treatment. In certain embodiments, such compounds effectively treat or prevent a sleep disorder in the animal, while producing reduced side effects compared to previously available compounds.
    Type: Grant
    Filed: July 25, 2017
    Date of Patent: April 13, 2021
    Assignee: Purdue Pharma L.P.
    Inventors: Stephen C. Harris, Ram P. Kapil, Donald J. Kyle, Garth Whiteside
  • Patent number: 10968221
    Abstract: The present invention is directed to [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-a]pyrazine derivatives of Formula IIa, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: October 3, 2019
    Date of Patent: April 6, 2021
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
  • Patent number: 10953008
    Abstract: Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 18, 2020
    Date of Patent: March 23, 2021
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Yohei Ikuma, Kengo Tojo, Ryo Fukazawa, Shuji Masumoto
  • Patent number: 10946014
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: March 16, 2021
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Patent number: 10941149
    Abstract: Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: March 9, 2021
    Assignee: Enterprise Therapeutics Limited
    Inventors: Clive McCarthy, Jonathan David Hargrave, Duncan Alexander Hay, Thomas Beauregard Schofield, Naomi Went
  • Patent number: 10925877
    Abstract: Compositions comprising derivatives of biopterin, useful for the treatment of traumatic brain injury, non-traumatic brain injury, elevated cranial pressure, and secondary brain injury.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: February 23, 2021
    Assignee: VASOPHARM GMBH
    Inventors: Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
  • Patent number: 10912773
    Abstract: The present invention provides combination treatments comprising compounds of Formula (I): that are PDE1 enzyme inhibitors, and other compounds useful in the treatment of neurodegenerative disorders such as for example Alzheimer's Disease, Parkinson's Disease or Huntington's Disease. Separate aspects of the invention are directed to the combined use of said compounds for the treatment of neurodegenerative and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of neurodegenerative disorders.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: February 9, 2021
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl
  • Patent number: 10905688
    Abstract: The present invention provides combination treatments comprising compounds of Formula (I): that are PDE1 enzyme inhibitors and other compounds useful in the treatment of psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of psychiatric and/or cognitive disorders.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: February 2, 2021
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl
  • Patent number: 10906886
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa andor plasma kallikrein which may be used as medicaments.
    Type: Grant
    Filed: May 17, 2018
    Date of Patent: February 2, 2021
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, Indawati De Lucca
  • Patent number: 10899769
    Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: January 26, 2021
    Assignee: Board of Regents, The University of Texas System
    Inventors: Kang Le, Michael J. Soth, Gang Liu, Philip Jones, Jason Bryant Cross, Timothy Joseph Mcafoos, Christopher L. Carroll, Richard T. Lewis
  • Patent number: 10894794
    Abstract: Compounds for the treatment of hyperglycemia and/or diabetes are provided. The compounds, which inhibit the enzyme dipeptidyl peptidase (DPP-4), are based on the structure where n1=0-2 such as 0 or 1; R1 is i) a saturated or unsaturated, substituted or unsubstituted monocyclic aliphatic ring, alone or fused with cyclopropane or cyclobutene, optionally comprising one or more substituents attached to the ring; or ii) a substituted or unsubstituted monocyclic aromatic ring, optionally comprising one or more substituents attached to the ring; R2 is present or absent and if present is: C?O; (CH2)n where n=0-4; S; SO; SO2; NR where R?H, CH3 or CH2CH3; or NH(CH2)n where n=0-4; and R3 is present or absent and if present is (CH2)n where n=0-4; S; SO; SO2; NR where R?H, CH3 or CH2CH3; or NH(CH2)n where n=0-4; and salts and isomers thereof.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: January 19, 2021
    Assignee: King Abdulaziz University
    Inventors: Abdelsattar M. Omar, Mohamed A. El-Zahabi, Salah G. Atteiah, Ashraf B. Abdel-Naim, Moustafa E. El-Araby
  • Patent number: 10881706
    Abstract: A product containing plant derived exosome that may be used in cancer treatment and wound healing. The product enables to provide a low-cost product, which does not cause toxic effects in human body, does not cause damage in the healthy cells during the course of the cancer treatment, does not pose any infection risk since it does not require any procedure such as radiotherapy or surgery, and the side effects occurring in chemotherapy treatment are not experienced. Wheatgrass, garlic and ginger can be used alone or in combination in the product as the plant source.
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: January 5, 2021
    Assignee: YEDITEPE UNIVERSITESI
    Inventors: Fikrettin Sahin, Merve Yildirim, Polen Kocak, Burge Ulukan
  • Patent number: 10851086
    Abstract: A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: December 1, 2020
    Assignee: MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.
    Inventors: Wenbao Li, Shixiao Wang, Zhongpeng Ding, Yingwei Hou, Huashi Guan
  • Patent number: 10845622
    Abstract: A contact lens product includes a multifocal contact lens and a buffer solution. The multifocal contact lens is immersed in the buffer solution. The multifocal contact lens includes a central region and at least one annular region. The annular region concentrically surrounds the central region, and a diopter of the annular region is different from a diopter of the central region. The multifocal contact lens is made of silicone hydrogel or hydrogel. The annular region closest to a periphery of the multifocal contact lens is a first annular region.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: November 24, 2020
    Assignee: LARGAN MEDICAL CO., LTD.
    Inventors: En-Ping Lin, Wei-Yuan Chen, Chun-Hung Teng
  • Patent number: 10828299
    Abstract: The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: November 10, 2020
    Assignee: KRONOS BIO, 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: 10821260
    Abstract: A state control apparatus including: an acquiring unit configured to acquire a state index indicating a state of target feeling based on biological information corresponding to the target feeling which is feeling of a target to be guided, the biological information being detected from a guide target whose state of feeling is to be guided; and a state control unit configured to determine a feeling guiding medium to be used for guiding the state of the target feeling based on the acquired state index and pattern information which is associated with the feeling guiding medium for guiding the state of the target feeling and which indicates a pattern of temporal change of the state index so that the state of the target feeling becomes a predetermined set state, and control the state of the target feeling of the guide target by performing processing relating to the determined feeling guiding medium. The biological information includes information indicating a detection result of an enzyme.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: November 3, 2020
    Assignee: Sony Corporation
    Inventors: Nobuyuki Kuboi, Takashi Kinoshita, Shinya Yamakawa
  • Patent number: 10821110
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: November 3, 2020
    Assignee: HYUNDAI PHARM CO., LTD.
    Inventors: Jin Yang, Jin Woong Kim, Han Kyu Lee, Jae Hyun Kim, Chang Mo Son, Kyu Hwan Lee, Hyung-Ho Choi, Daehoon Kim, Tae-Young Ha, Jaekeol Rhee
  • Patent number: 10822306
    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: May 29, 2019
    Date of Patent: November 3, 2020
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Patent number: 10822340
    Abstract: Described herein, inter alia, are certain substituted imidazolopyrazines of formula (I) and methods of using the same for modulating the activity of Ire1.
    Type: Grant
    Filed: October 2, 2018
    Date of Patent: November 3, 2020
    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: 10815216
    Abstract: The present invention relates to an improved process for the preparation of Aripiprazole Lauroxil of Formula (I).
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: October 27, 2020
    Assignee: NEULAND PHARMA RESEARCH PRIVATE LIMITED
    Inventors: Ponnaiah Ravi, Neela Praveen Kumar, Batthini Guruswamy, Krishnaiah Pendem, Satya Nagendra Kumar Lakkadasu, Mahesh Gattikoppula
  • Patent number: 10800779
    Abstract: The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: October 13, 2020
    Assignee: Incyte Corporation
    Inventors: Chunhong He, Zhenwu Li, Liangxing Wu, Wenqing Yao, Fenglei Zhang
  • Patent number: 10787448
    Abstract: 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: Grant
    Filed: January 23, 2018
    Date of Patent: September 29, 2020
    Assignees: SEOUL NATIONAL UNIVERSITY R & DB FOUNDATION, INDUSTRY-ACADEMIC COOPERATION FOUNDATION YONSEI UNIVERSITY
    Inventors: Jeeyeon Lee, Ikyon Kim, Soonbum Kwon, Bumhee Lim
  • Patent number: 10781207
    Abstract: 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: Grant
    Filed: October 10, 2017
    Date of Patent: September 22, 2020
    Assignee: IsoCure Biosciences Inc.
    Inventors: Tinghu Zhang, Jianwei Che
  • Patent number: 10753947
    Abstract: 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: Grant
    Filed: August 29, 2014
    Date of Patent: August 25, 2020
    Assignee: D.E. SHAW RESEARCH, LLC
    Inventors: Morten Østergaard Jensen, David Wayne Borhani, Vishwanath Jogini
  • Patent number: 10723729
    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 16, 2019
    Date of Patent: July 28, 2020
    Assignee: Hoffmann-Le Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Patent number: 10716787
    Abstract: 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: Grant
    Filed: April 17, 2018
    Date of Patent: July 21, 2020
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Eleonora Jovcheva, Timothy Pietro Suren Perera
  • Patent number: 10710984
    Abstract: 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: Grant
    Filed: April 7, 2017
    Date of Patent: July 14, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer
  • Patent number: 10710996
    Abstract: 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: Grant
    Filed: May 23, 2016
    Date of Patent: July 14, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
  • Patent number: 10711004
    Abstract: 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: Grant
    Filed: September 3, 2019
    Date of Patent: July 14, 2020
    Assignee: 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
  • Patent number: 10689393
    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: March 4, 2019
    Date of Patent: June 23, 2020
    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: 10683300
    Abstract: The present disclosure relates to synthesis and characterization of novel polymorphic forms of Cyclo (-His-Pro) (“CHP”).
    Type: Grant
    Filed: June 21, 2019
    Date of Patent: June 16, 2020
    Assignee: NovMetaPharma Co., Ltd.
    Inventors: Kay Olmstead, David Pearson, Elaine McPherson
  • Patent number: 10683306
    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: April 17, 2019
    Date of Patent: June 16, 2020
    Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Kyle Hoehn, Brandon Kenwood
  • 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: 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: 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: 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