Exactly Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/262.1)
  • Patent number: 11059850
    Abstract: The present invention relates to novel spirobicyclic analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: July 13, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jonas Verhoeven, Guido Alfons F. Verniest, Johannes Wilhelmus John F. Thuring, Tongfei Wu, Vineet Pande, Lieven Meerpoel, Dirk Brehmer, Weimei Sun, Scott E. Denmark
  • Patent number: 11046696
    Abstract: The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: May 13, 2020
    Date of Patent: June 29, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita, Satoru Iguchi
  • Patent number: 11040980
    Abstract: The present disclosure provides compounds of Formula (IA), such as, e.g., (R)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile having the chemical structure and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 9, 2019
    Date of Patent: June 22, 2021
    Assignee: Principia Biopharma Inc.
    Inventors: Tim Owens, Erik Verner
  • Patent number: 11028092
    Abstract: The present invention is directed to pyrazolopyrimidine compounds of the general structural formula I: which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: October 31, 2019
    Date of Patent: June 8, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ashok Arasappan, Jason M. Cox, John S. Debenham, Zahid Hussain, Derun Li, Dongfang Meng, Subharekha Raghavan
  • Patent number: 11008324
    Abstract: The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: May 13, 2020
    Date of Patent: May 18, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita, Satoru Iguchi
  • Patent number: 10975082
    Abstract: The present invention provides a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound of formula (I), as well as the use and method for preventing or treating FLT3-related conditions, especially conditions related to mutant FLT3 kinase (particularly, FLT3/ITD mutant kinase).
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: April 13, 2021
    Assignee: PRECEDO PHARMACEUTICALS CO., LTD
    Inventors: Qingsong Liu, Jing Liu, Xixiang Li, Aoli Wang, Ziping Qi, Hong Wu, Jiaxin Wu, Wenchao Wang, Chen Hu, Cheng Chen, Li Wang, Beilei Wang
  • Patent number: 10961251
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: November 18, 2020
    Date of Patent: March 30, 2021
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Patent number: 10947244
    Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: March 16, 2021
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventor: Swaroop K. Vakkalanka
  • Patent number: 10946008
    Abstract: The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
    Type: Grant
    Filed: October 4, 2019
    Date of Patent: March 16, 2021
    Assignee: Principia Biopharma Inc.
    Inventor: Steven Gourlay
  • Patent number: 10934299
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5? and R6 are described herein.
    Type: Grant
    Filed: July 19, 2019
    Date of Patent: March 2, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, Darby Rye Schmidt, David Joseph Guerin, Justin Andrew Caravella, R. Bruce Diebold, Anna Ericsson, David R. Lancia, Jr.
  • Patent number: 10927130
    Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, X1, X2, X3, n, and m are described herein.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: February 23, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
  • Patent number: 10870652
    Abstract: Provided herein, inter alia, are compounds and methods for modulating Bruton's Tyrosine Kinase.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: December 22, 2020
    Assignee: CORVUS PHARMACEUTICALS, INC.
    Inventors: Ryan Hudson, Anne-Marie Beausoleil, Richard A. Miller, Erik Verner
  • Patent number: 10851109
    Abstract: The disclosure is directed to compounds and pharmaceutically acceptable salts thereof for the treatment and/or prevention of neurodegenerative and/or mitochondrial diseases, such as Parkinson's disease and Leigh's disease. The compounds and pharmaceutically acceptable salts thereof are of the class of nitrogenous bases, for example, pyrimidines, purines, pteridines, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: December 1, 2020
    Assignee: Mitokinin LLC
    Inventors: Daniel de Roulet, Robert Devita
  • Patent number: 10828307
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: November 10, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Patent number: 10828259
    Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: April 10, 2020
    Date of Patent: November 10, 2020
    Assignee: Pharmacyclics LLC
    Inventors: Ching W. Chong, Robert Kuehl, Heow Tan, Harisha Atluri
  • Patent number: 10807986
    Abstract: The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: October 20, 2020
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita, Satoru Iguchi
  • Patent number: 10766902
    Abstract: The present invention relates to pyrazolopyrimidinone derivatives, such as those of Formula (I), that are useful as inhibitors of the activity of Wee-1 kinase.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: September 8, 2020
    Assignee: ALMAC DISCOVERY LIMITED
    Inventors: Frank Burkamp, James Samuel Shane Rountree, Adam Piotr Treder
  • Patent number: 10752634
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: April 1, 2020
    Date of Patent: August 25, 2020
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Patent number: 10711006
    Abstract: The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug. The compound of the present invention has a structure of Formula II or Formula II?: or their optical isomers, or pharmaceutically acceptable salts or solvates; where each Rg is independently H, halogen, —CF2H, —CF3, —CN, C1-C3 alkyl, or C1-C3 alkoxy; n is selected from 0, 1 and 2; Rd is selected from Re is selected from H, CH3, C2-C6 alkyl, C1-C6 azaalkyl, and C1-C6 oxaalkyl, wherein CH3, C2-C6 alkyl, C1-C6 azaalkyl and C1-C6 oxaalkyl are further substituted with amino, hydroxyl, and C1-C3 alkyl; Y1, Y2, Y3 and Y4 are independently selected from C(Rf) and N, and at least one of Y1, Y2, Y3 and Y4 is N, wherein Rf is selected from H, halogen, C1-C3 alkyl, —CF3, and —CF2H.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: July 14, 2020
    Assignee: HANGZHOU HERTZ PHARMACEUTICAL CO., LTD.
    Inventors: Xinglu Zhou, Xingguo Liu, Miao Hu
  • Patent number: 10695350
    Abstract: Described herein are methods for treating and preventing graft versus host disease using ACK inhibitors. The methods include administering to an individual in need thereof an ACK inhibitor such as ibrutinib for treating and preventing graft versus host disease.
    Type: Grant
    Filed: September 25, 2019
    Date of Patent: June 30, 2020
    Assignee: Pharmacyclics LLC
    Inventors: John C. Byrd, Jason A. Dubovsky, Natarajan Muthusamy, Amy J. Johnson, David Miklos
  • Patent number: 10676487
    Abstract: The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.
    Type: Grant
    Filed: September 6, 2016
    Date of Patent: June 9, 2020
    Assignee: On Target Laboratories, LLC
    Inventors: Sumith A. Kularatne, Pravin Gagare, Carrie H. Myers
  • Patent number: 10676436
    Abstract: Provided are compounds that target the nucleotide-binding oligomerization domain, leucine rich repeat containing X1 (NLRX1) pathway. The compounds can be used to treat multiple conditions, including inflammatory, immune-mediated, and/or chronic inflammatory gastrointestinal diseases; systemic immune-mediated diseases; cancers; and infectious diseases.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: June 9, 2020
    Assignee: LANDOS BIOPHARMA, INC.
    Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas
  • Patent number: 10675400
    Abstract: The present disclosure relates, in part, to a kit including at least two prefilled syringes. The first prefilled syringe includes a dose of a hazardous agent in a first volume of a pharmaceutical composition comprising a pharmaceutically acceptable solvent.
    Type: Grant
    Filed: June 27, 2016
    Date of Patent: June 9, 2020
    Assignee: Antares Pharma, Inc.
    Inventors: Paul K. Wotton, Peter L. Sadowski, Kaushik J. Dave, Dominic P. Capone
  • Patent number: 10647727
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: May 12, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Ashley Forster, Richard Berger, Kausik K. Nanda, William D. Shipe
  • Patent number: 10626117
    Abstract: The present invention relates to an improved process for the preparation of Ibrutinib with high purity and high yields. The present process is cost effective and feasible in large scale production also. The present process avoids the mitsunobu reagent conditions also. The present Invention also relates to a process for the preparation of Crystalline form A and Crystalline form C of Ibrutinib.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: April 21, 2020
    Assignee: NATCO PHARMA LIMITED
    Inventors: Pulla Reddy Muddasani, Shankar Reddy Budideti, Veerababu Madalapu, Anitha Gattu, Bala Ankireddy Konda, Venkaiah Chowdary Nannapaneni
  • Patent number: 10610531
    Abstract: Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml.
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: April 7, 2020
    Assignee: MEDAC GESELLSCHAFT FUER KLINISCHE SPEZIALPRAEPARARATE MBH
    Inventor: Heiner Will
  • Patent number: 10562912
    Abstract: A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: February 18, 2020
    Assignee: C&C Research Laboratories
    Inventors: Chan Hee Park, Sang Hwi Lee, Junhwan Im, Soon Ok Lee, Hoe Moon Kim, Sung Hyun Moon, Seunghee Kim, Jongmin Kim, Kwang Seok Ko, Bu Young Choi, Byungho Kim
  • Patent number: 10538513
    Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: January 21, 2020
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Robert Murray McKinnell, Erik Fenster, Tom M. Lam, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
  • Patent number: 10533013
    Abstract: The present disclosure provides compounds of Formula (IA), such as, e.g., (R)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile having the chemical structure ?and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: January 14, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Tim Owens, Erik Verner
  • Patent number: 10485797
    Abstract: The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: November 26, 2019
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventor: Steven Gourlay
  • Patent number: 10456403
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: October 29, 2019
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Patent number: 10434103
    Abstract: An object of the present invention is to provide a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one, which is useful as an antitumor agent, the crystal being stable, excellent in oral absorbability, highly chemically pure, and suitable for mass production. The present invention provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least three characteristic peaks at diffraction angles (2?±0.2°) selected from 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, and 25.2°. The present invention also provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least seven characteristic peaks at diffraction angles (2?±0.2°) selected from 13.5°, 17.9°, 19.5°, 20.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: October 8, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Kosuke Egami
  • Patent number: 10413546
    Abstract: A medicament for prophylactic and/or therapeutic treatment of dementia, which comprises a compound represented by the formula (I) having a xanthine oxidase inhibitory action as an active ingredient.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: September 17, 2019
    Assignees: NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, NIPPON MEDICAL SCHOOL FOUNDATION, NIPPON CHEMIPHAR CO., LTD.
    Inventors: Takeshi Nishino, Shinsuke Kato, Masako Kato, Hidenori Suzuki, Ken Okamoto
  • Patent number: 10414773
    Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: September 17, 2019
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventor: Swaroop K. Vakkalanka
  • Patent number: 10391052
    Abstract: Provided are an injection preparation which includes: an aqueous composition containing pemetrexed or a salt thereof, at least one antioxidant agent A which is selected from the group consisting of cysteine and a salt thereof, and of which the content is 0.001 mass % to 0.1 mass % with respect to the total mass of the aqueous composition, thioglycerol of which the content is 0.001 mass % to 0.1 mass % with respect to the total mass of the aqueous composition, and an aqueous solvent of which the content is greater than or equal to 50 mass % with respect to the total mass of the aqueous composition, and a container which seals the aqueous composition, in which the concentration of oxygen in gas within the container which seals the aqueous composition is less than or equal to 2.0 volume %, and a method for producing the injection preparation.
    Type: Grant
    Filed: September 20, 2016
    Date of Patent: August 27, 2019
    Assignee: FUJIFILM CORPORATION
    Inventors: Shinichi Hashimoto, Shigetomo Tsujihata, Yasuyuki Izumi
  • Patent number: 10377760
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5 and R6 are described herein.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: August 13, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, Darby Rye Schmidt, David Joseph Guerin, Justin Andrew Caravella, R. Bruce Diebold, Anna Ericsson, David R. Lancia, Jr.
  • Patent number: 10363263
    Abstract: The invention generally relates to anti-aging compositions and methods for using the anti-aging compositions. In one aspect, the invention provides a method for preventing cellular aging in a cell of a subject, the method comprising the step of providing to the cell an effective amount of at least one lithium compound or a pharmaceutically acceptable salt thereof, and an effective amount of at least one glycyrrhizie triterpenoid compound or a pharmaceutically acceptable salt thereof, thereby preventing the cell from aging. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: July 30, 2019
    Assignee: Prescient Pharma, LLC
    Inventors: Pavel Idelevich, Anna Idelevich
  • Patent number: 10358424
    Abstract: Provided are a sodium salt of a uric acid transporter inhibitor and a crystalline form thereof, In particular, provided are a uric acid transporter (URAT1) inhibitor 1-((6-bromo-quinoline-4-yl)thio)cyclobutyl sodium formate (the compound of formula (I)), a crystal form I, and preparation method thereof. The obtained crystal form I of the compound of formula (I) has a good crystal form stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, and can be better used in clinical treatment.
    Type: Grant
    Filed: October 11, 2018
    Date of Patent: July 23, 2019
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Zhenjun Qiu, Yunpeng Su, Xi Lu
  • Patent number: 10335453
    Abstract: The embodiments include methods of improving sexual function in a male with benign prostatic hyperplasia (BPH), using compositions containing compounds based on small peptides and a pharmaceutically acceptable carrier. The method includes, but is not limited to, administering the compounds intramuscularly, orally, intravenously, intraprostatically, intrathecally, intratumorally, intranasally, topically, transdermally, etc., either alone or conjugated to a carrier to a male in need thereof.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: July 2, 2019
    Assignee: Nymox Corporation
    Inventor: Paul Averback
  • Patent number: 10329304
    Abstract: Compounds and compositions, and methods of use thereof, are provided and have utility in inhibiting hedgehog signaling and/or phosphodiesterase-4 activity.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: June 25, 2019
    Assignee: Vanderbilt University
    Inventors: Charles C. Hong, Charles H. Williams, Jonathan Hempel, T K Feaster, Don H. Rubin, Gary Sulikowski, Jijun Hao, Audrey Frist
  • Patent number: 10329300
    Abstract: To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect. The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, Z3, Z4, W, n, R1, R2, and R3 have meanings as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 25, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yuichi Kawai, Hiroki Irie, Takeshi Sagara, Kazutaka Miyadera
  • Patent number: 10322129
    Abstract: A method comprising: (a) identifying a subject in need of treatment for cataract and/or nevus and/or tumor lesion; and (b) topically administering to the eye an amount of dipyridamole which is physiologically effective in treatment of cataract and/or nevus and/or melanoma.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: June 18, 2019
    Assignee: O.D. Ocular Discovery Ltd.
    Inventor: Moshe Rogosnitzky
  • Patent number: 10322127
    Abstract: Methods of tests that assess the expression of DPC4 (SMAD4) to identify subjects with pancreatic cancer that are likely or unlikely to respond to treatment with BTK inhibitors; methods of treating subjects based on identification of the subjects as likely to respond to treatment with BTK inhibitors; therapeutic targets for cancers, particularly cancers with inactivated DPC4 gene or protein; methods of screening of new therapeutic agents using the target; pharmaceutical composition comprising BTK inhibitors, such as PCI-32765 or derivatives thereof, for cancer treatment; and kits that facilitate the performance of the methods are disclosed.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: June 18, 2019
    Assignee: The Translational Genomics Research Institute
    Inventors: Haiyong Han, Daniel Von Hoff, Caroline H. Diep, Hongwei Yin
  • Patent number: 10300063
    Abstract: Provided are a composition containing an unstable drug against oxidation like pemetrexed with improved stability and a preparation method thereof, by removing oxygen during the preparation without use of an antioxidant. The method is readily applicable for manufacturing by freezing and degassing in a sealed chamber, and can provide formulations with significantly increased stability for the unstable drug against oxidation.
    Type: Grant
    Filed: December 26, 2014
    Date of Patent: May 28, 2019
    Assignee: SAMYANG BIOPHARMACEUTICALS CORPORATION
    Inventors: Joong-Woong Cho, Gyeong-Hae Kim, Min-Hyo Seo, Sa-Won Lee
  • Patent number: 10300068
    Abstract: Methods for treating insomnia are disclosed. The methods are directed to administering a pharmaceutically effective amount of phosphodiesterase 5 (PDE5) inhibitor to a male individual suffering from insomnia. In addition, due to the PDE5 inhibitor positive effects on addressing erectile dysfunction (ED) in males, the present methods are directed to treating insomnia in patients that also suffer from ED by administering a pharmaceutically effective amount of a PDE5 inhibitor.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: May 28, 2019
    Inventor: Leon I. Rosenberg
  • Patent number: 10300066
    Abstract: Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: May 28, 2019
    Assignee: Zhejiang DTRM Biopharma Co. Ltd.
    Inventor: Wei He
  • Patent number: 10280173
    Abstract: Provided are ibrutinib polymorphs, e.g., crystalline ibrutinib Forms III, IV, V, VI, VII, VIII and Form IX and processes for producing these crystalline forms, stable amorphous ibrutinib and processes for preparing stable amorphous ibrutinib, pharmaceutical compositions comprising these forms and methods of using these crystalline and amorphous forms.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: May 7, 2019
    Assignee: WAVELENGTH ENTERPRISES LTD
    Inventors: Itai Adin, Sonia Krivonos, Yevgeny Rozenblat, Alex Weisman, Ana Fernandez Casares, Gloria Ten Figas, Revital Ben-Daniel
  • Patent number: 10272083
    Abstract: Therapeutic methods of treating chronic lymphocytic leukemia (CLL) and small lymphocytic leukemia (SLL) are described. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating subtypes of CLL and SLL using a BTK inhibitor, including subtypes of CLL in patients sensitive to thrombosis and subtypes of CLL that increase monocytes and NK cells in peripheral blood after treatment with a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a combination of a BTK inhibitor and an anti-CD20 antibody.
    Type: Grant
    Filed: January 21, 2015
    Date of Patent: April 30, 2019
    Assignee: ACERTA PHARMA B.V.
    Inventors: Ahmed Hamdy, Wayne Rothbaum, Raquel Izumi, Brian Lannutti, Todd Covey, Roger Ulrich, Dave Johnson, Tjeerd Barf, Allard Kaptein
  • Patent number: 10259818
    Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: April 16, 2019
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
  • Patent number: RE48175
    Abstract: Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: August 25, 2020
    Assignees: Dana-Farber Cancer Institute, Inc., Yale University
    Inventors: Nathanael Gray, Ting Xie, Sang Min Lim, Pasi A. Janne, Craig M. Crews