1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 11318166
    Abstract: Described herein are methods and compositions using PTH and mesenchymal stem cells (MSCs) for treatment of osteoporosis, bone fractures, and related conditions. Administration of both PTH and MSCs leads to increased homing of MSCs to sites of vertebral bone and rib fracture. The described methods and compositions provide therapeutic approaches that rely, in-part, on stem cell capacity for regeneration and repair. The potential for enhanced bone formation and fracture repair may allow for both preventative and palliative treatments in osteoporotic patients, with combined PTH+MSC therapy producing bone regeneration capacity that is significantly superior to either treatment alone.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: May 3, 2022
    Assignee: Cedars-Sinai Medical Center
    Inventors: Dan Gazit, Edward M. Schwarz, Hyun Bae, Gadi Pelled, Zulma Gazit, Dmitriy Sheyn, Wafa Tawackoli
  • Patent number: 11312715
    Abstract: Disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an application of the compound or slat in preparation of drugs for treating diseases related to an A2A receptor.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: April 26, 2022
    Assignees: CSTONE PHARMACEUTICALS (SUZHOU) CO., LTD., CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD., CSTONE PHARMACEUTICALS
    Inventors: Kevin X Chen, Kai Zhou, Boyu Hu, Minliang Xiao, Shuhui Chen
  • Patent number: 11306086
    Abstract: The present invention is related to crystalline salts of N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide, a RAF kinase Inhibitor, useful in the treatment of cancer and other diseases.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: April 19, 2022
    Assignee: Xynomic Pharmaceuticals, Inc.
    Inventors: Ulrike Werthmann, Gerd-Michael Maier, Bodo Betzemeier, Otmar Schaaf
  • Patent number: 11306077
    Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or prodrug thereof, and methods of making and using thereof.
    Type: Grant
    Filed: May 28, 2021
    Date of Patent: April 19, 2022
    Assignee: Denali Therapeutics Inc.
    Inventors: Robert A. Craig, II, Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian M. Fox, Maksim Osipov, Arun Thottumkara
  • Patent number: 11292802
    Abstract: The disclosure relates to compounds of formula I: Formula I which inhibit ?V-containing integrins, and includes pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?V-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: April 5, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guohua Zhao, James Mignone
  • Patent number: 11274093
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, isotopic form, stereoisomer or prodrug thereof, wherein A, B, X, R1, R2a, R2b, R2c, L, 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: January 24, 2018
    Date of Patent: March 15, 2022
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 11261190
    Abstract: A dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B, specifically, is a compound having Formula (I) or (Ia), or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification; and also includes the use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: March 1, 2022
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Xinchang Liu, Qingyun Ren, Guanghua Yan, Siegfried Goldmann, Yingjun Zhang
  • Patent number: 11247998
    Abstract: The present invention relates to a piperazine heteroaryl derivative, a preparation method therefor and the use of same in medicine. In particular, the present invention relates to the piperazine heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and the use of same as a capsid protein inhibitor, in particular in the prevention and/or treatment of diseases such as hepatitis B, influenza, herpes, AIDS, etc. The definitions of each group in the general formula (I) are the same as those defined in the description.
    Type: Grant
    Filed: July 26, 2018
    Date of Patent: February 15, 2022
    Assignees: JIANGSU HENGRUI MEDICINE CO., LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.
    Inventors: Xin Li, Wei He, Yang Chen, Feng He, Weikang Tao
  • Patent number: 11229627
    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: October 21, 2021
    Date of Patent: January 25, 2022
    Assignee: Allergan Holdings Unlimited Company
    Inventors: Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
  • Patent number: 11229656
    Abstract: A method for manufacturing a hyaluronan conjugate comprises providing hyaluronan in solution or gel form, reacting the hyaluronan in solution or gel form with anhydride reagent to provide a hyaluronan hemi-ester with a chain of length L between the hyaluronan and the ester group, and subsequently binding the hyaluronan hemi-ester to a pharmaceutically active compound. A hyaluronan conjugate comprises hyaluronan having free hemi-ester-groups and a pharmaceutically active compound bound to the hyaluronan via hemi-ester groups, wherein the hemi-ester groups have a chain length of 2-9 atoms. The hyaluronan conjugate is suitable for use in various methods of treatment in human or veterinary medicine and for preparation of a medicament for use in human or veterinary medicine.
    Type: Grant
    Filed: April 16, 2020
    Date of Patent: January 25, 2022
    Assignee: SYNARTRO AB
    Inventors: Bengt Lindqvist, Rune Ringom
  • Patent number: 11213527
    Abstract: A novel therapeutic drug for malignant tumors, cancer stem cells, or fibrosis is obtained. A therapeutic drug for malignant tumors or cancer stem cells is used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof. Alternatively, a therapeutic drug for fibrosis can be used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: January 4, 2022
    Assignees: National University Corporation Tottori University, KanonCure, Inc.
    Inventors: Goshi Shiota, Noriko Itaba, Keita Kanki, Kenzo Seto, Hiroki Shimizu, Yohei Kouno, Shinya Kunita, Zyunya Adumi, Tomohiko Sakabe, Kenichiro Abe, Minoru Morimoto, Hiroyuki Oka
  • Patent number: 11207431
    Abstract: Provided herein are compounds useful for binding to one or more histone deacetylase enzymes (HDACs). The present application further provides radiolabeled compounds useful as a radiotracer for position emission tomography imaging of HDAC. Methods for prepared unlabeled and labeled compounds, diagnostic methods, and methods of treating diseases associated HDAC are also provided.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: December 28, 2021
    Assignee: The General Hospital Corporation
    Inventors: Jacob Hooker, Changning Wang, Martin Georg Strebl-Bantillo
  • Patent number: 11185536
    Abstract: Methods for treating hearing loss that include administering an inhibitor, e.g., a small molecule inhibitor, of casein kinase 1, preferably in combination with a treatment that stimulates Atoh1 gene expression, e.g., a gamma-secretase inhibitor, an Atoh1 stimulatory compound, or a GSK-3-beta inhibitor.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: November 30, 2021
    Assignee: Massachusetts Eye and Ear Infirmary
    Inventors: Albert Edge, Yenfu Cheng
  • Patent number: 11180466
    Abstract: The invention relates to a compound of general formula (I): wherein R1, R2, R3, R4, Q, m and n are as defined herein. The compounds are inhibitors of Bcl-3 and are useful for the treatment of cancer, particularly metastatic cancer.
    Type: Grant
    Filed: October 4, 2019
    Date of Patent: November 23, 2021
    Assignee: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Andrew David Westwell, Andrea Brancale, Richard William Ernest Clarkson, Jitka Soukupova
  • Patent number: 11173158
    Abstract: Disclosed is a means for improving the symptoms of a cerebral dysfunction. The present inventors made a new discovery that the activity of brain aromatic monoamines increases when sepiapterin is administered peripherally. Disclosed, therefore, is a medicinal agent, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Also disclosed is a beverage/food, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Unlike tetrahydrobiopterin and the like, sepiapterin can control reductions in the brain neuron levels of brain aromatic monoamines (serotonin, dopamine, noradrenaline, and the like) and increase the activity thereof even when administered peripherally.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: November 16, 2021
    Assignees: PTC Therapeutics MP, Inc., Shiratori Pharmaceuticals Co., Ltd.
    Inventors: Hiroyuki Hasegawa, Shin Aizawa
  • Patent number: 11174254
    Abstract: The present invention relates to a 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative substituted by N-(3-aminophenyl)acrylamide and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound of formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application of the same. The definition of each substituent in the formula is described in detail in the specification and claims.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: November 16, 2021
    Assignees: YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD., SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Shuchun Guo, Fusheng Zhou, Xiang Chen, Jinzhu Zhao, Dong Huang, Jing Xie, Changjiang Qiao, Wan He, Kai Zhang, Xi Chen, Jiong Lan
  • Patent number: 11168090
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: November 9, 2021
    Assignee: Array BioPharma Inc.
    Inventors: Steven W Andrews, James F Blake, Julia Haas, Yutong Jiang, Gabrielle R Kolakowski, David A Moreno, Li Ren, Shane M Walls
  • Patent number: 11147812
    Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are tyrosine analogues derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: October 19, 2021
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Alessandro Accetta, Anna Maria Capelli, Fabio Rancati, Gurdip Bhalay, Arnaud Jean Francois Auguste Cheguillaume, Christine Edwards, Patrizia Tisselli
  • Patent number: 11142527
    Abstract: A dihydropyrimidine compound and a pharmaceutical application thereof, especially the application used for treating and preventing HBV diseases. Specifically, a compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also, use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicine, especially for treating and preventing HBV diseases.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: October 12, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Qingyun Ren, Xinchang Liu, Jianzhou Huang, Yingjun Zhang, Siegfried Goldmann
  • Patent number: 11135202
    Abstract: Thiazolide compounds, such as nitazoxanide and/or tizoxanide, may be used against viruses belonging to the Picornaviridae family or the Paramyxoviridae family.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: October 5, 2021
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, Maria Gabriella Santoro
  • Patent number: 11104691
    Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: August 31, 2021
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, John Wityak, Jonathan Bard, Alex Kiselyov, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Daniel Clark-Frew
  • Patent number: 11078203
    Abstract: Deuterated fezolinetant (R)-(4-fluorophenyl)-(8-methyl-3-(3-(methyl-d3)-1,2,4-thiadiazol-5-yl)-5,6-dihydro-[1,2,4]trizolo[4,3-a]pyrazin-7(8H)-yl)methanone: or a pharmaceutically acceptable salt or solvate thereof, as an NK-3 antagonist. Also, methods of modulating NK-3 receptor activity including administering an effective amount of the compound or pharmaceutically acceptable salt or solvate thereof. Additionally, a process for manufacturing the compound or pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: August 3, 2021
    Assignee: Ogeda SA
    Inventor: Hamid Hoveyda
  • Patent number: 11077111
    Abstract: The present application relates to the use of fused heteroaromatic pyrrolidones for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals and to the use thereof for production of medicaments for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals, especially of atopic dermatitis and/or Flea Allergy Dermatitis, and especially in domestic animals, particularly in dogs.
    Type: Grant
    Filed: October 15, 2018
    Date of Patent: August 3, 2021
    Assignee: Bayer Animal Health GmbH
    Inventors: Nils Griebenow, Maria De Lourdes Mottier, Gerald Beddies, Jörg Cramer, Ulf Bömer, Iring Heisler
  • Patent number: 11059829
    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: April 30, 2020
    Date of Patent: July 13, 2021
    Assignee: Acerta Pharma B.V.
    Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
  • Patent number: 11059819
    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 A, W, X, Y, Z, and 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: January 25, 2018
    Date of Patent: July 13, 2021
    Assignees: Janssen Biotech, Inc., Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 11046700
    Abstract: The present invention relates to compounds of formula (1a), formula (1b), formula (1c) or formula (1d): or, or a pharmaceutically acceptable salt thereof, which have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such compounds, salts or solvates and to the use of such compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
    Type: Grant
    Filed: January 15, 2018
    Date of Patent: June 29, 2021
    Assignee: Merck Patent GmbH
    Inventors: John Mark Francis Gardner, Andrew Simon Bell
  • Patent number: 11034687
    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: June 17, 2020
    Date of Patent: June 15, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Patent number: 11026884
    Abstract: The present invention is directed to methods for improving night vision and visual performance in low light conditions comprising ophthalmological administration of compositions comprising low dose brimonidine and a vehicle for improved performance.
    Type: Grant
    Filed: January 22, 2019
    Date of Patent: June 8, 2021
    Assignee: Eye Therapies LLC
    Inventor: Gerald Horn
  • Patent number: 11026913
    Abstract: This disclosure relates to nutritional formulas and uses for treating or preventing a gastrointestinal condition and/or motor-planning speech and/or coordinator difficulties. In certain embodiments, this disclosure relates to a nutritional formula comprising medium 5 chain fatty acids, or esters thereof (such as and tri-, di-, mono-glycerides, or alkyl esters), unsaturated fatty acids, and a vitamin E and optionally other nutrients. In certain embodiments, any of the compounds or nutrients may be in alternative salt forms.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: June 8, 2021
    Assignees: Emory University, Children's Healthcare of Atlanta, Inc.
    Inventor: Claudia R. Morris
  • Patent number: 11020382
    Abstract: Provided herein are methods for treating sickle cell disease, comprising administering to a subject 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)-methoxy)benzaldehyde (Compound 1), or a polymorph thereof, in certain dosing regimens.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: June 1, 2021
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Eleanor L. Ramos, Joshua Eli Lehrer-Graiwer, Athiwat Hutchaleelaha
  • Patent number: 11014931
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds, such as the compound: and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: May 25, 2021
    Assignee: Praxis Precision Medicines, Inc.
    Inventors: Andrew Mark Griffin, Brian Edward Marron, Gabriel Martinez Botella
  • Patent number: 11013734
    Abstract: Methods of treating patients diagnosed with AML or MDS harboring mutant IDH-1 include detecting an IDH1 mutation and the therapeutic administration of an inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA) or cytarabine.
    Type: Grant
    Filed: July 30, 2019
    Date of Patent: May 25, 2021
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
  • 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: 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: 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: 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: 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: 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