Exactly Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/262.1)
  • Patent number: 11518764
    Abstract: The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
    Type: Grant
    Filed: February 6, 2019
    Date of Patent: December 6, 2022
    Assignee: ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR)
    Inventors: Rima Al-awar, Methvin Isaac, Anh My Chau, Ahmed Mamai, Iain Watson, Gennady Poda, Pandiaraju Subramanian, Brian Wilson, David Uehling, Michael Prakesch, Babu Joseph, Justin-Alexander Morin
  • Patent number: 11512085
    Abstract: The present invention provides a class of novel compounds having Btk selective inhibitory activity, better metabolic stability and the like.
    Type: Grant
    Filed: December 22, 2019
    Date of Patent: November 29, 2022
    Assignee: SHANGHAI DUDE MEDICAL TECHNOLOGY CO., LTD
    Inventors: Xin Liu, Zhedong Yuan, Rui Kong, Shan Chen
  • Patent number: 11406713
    Abstract: Disclosed herein are methods and compositions for involving a xanthine oxidase inhibitor that has enhanced solubility. The compositions described herein include a xanthine oxidase inhibitor combined with an organic base. The compositions can be used to treat a disease or medical condition that involves elevated uric acid levels.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: August 9, 2022
    Assignee: XORTX THERAPEUTICS, INC.
    Inventor: Allen Davidoff
  • Patent number: 11407754
    Abstract: The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, and the compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions: wherein, X1 is —NR1—, —O—, or —S—, X2 is CH or N, R1 is C1-5 alkyl, C3-6 cycloalkyl, CH2CHF2, or CH2CF3, wherein the C1-5 alkyl is optionally substituted with one NHC(O)OC(CH3)3 substituent, R2 is H, C1-5 alkyl, or halogen, and R3 is H or C1-5 alkyl.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: August 9, 2022
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Nam Youn Kim, Seung Hwarn Jeong, Bo-Kyoung Kim, Jun Hee Lee
  • Patent number: 11369613
    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 5, 2020
    Date of Patent: June 28, 2022
    Assignee: Principia Biopharma Inc.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Patent number: 11364242
    Abstract: Methods are provided for treating HIV and cancer in a subject in need thereof by administering to the subject therapeutically effective amounts of an mTOR inhibitor. Other methods are provided for treating subjects infected with HIV by administering to the subject therapeutically effective amounts of the mTOR inhibitor INK128, GSK2126458, AZD2014 or Torin-2.
    Type: Grant
    Filed: September 24, 2019
    Date of Patent: June 21, 2022
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Robert R. Redfield, Alonso Heredia, Charles Davis, Ronald Gartenhaus, Edward A. Sausville
  • Patent number: 11352359
    Abstract: The present disclosure provides novel compounds useful as PI3K protein kinase modulators, in particular as PI3K delta (?) and/or gamma (?) protein kinase modulators. The present disclosure also provides methods for preparing PI3K protein kinase modulators, pharmaceutical compositions containing them, and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: June 7, 2022
    Assignee: RHIZEN PHARMACEUTICALS AG
    Inventors: Prashant Kashinath Bhavar, Swaroop Kumar Venkata Satya Vakkalanka, Govindarajulu Babu
  • Patent number: 11332473
    Abstract: This invention provides for substituted pyrazolo[3,4-d]pyrimidine compounds of the Formula (I): as Wee1 inhibitors. The substituted pyrazolo[3,4-d]pyrimidine compounds may find use as therapeutic agents for the treatment of diseases. The substituted pyrazolo[3,4-d]pyrimidine compounds may also find particular use in oncology.
    Type: Grant
    Filed: April 8, 2020
    Date of Patent: May 17, 2022
    Assignee: NUVATION BIO INC.
    Inventors: Sarvajit Chakravarty, Son Minh Pham, Jayakanth Kankanala, Brahmam Pujala, Sanjeev Soni, Puja Jaiswal, Deepak Palve, Varun Kumar
  • Patent number: 11291666
    Abstract: The disclosure provides the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment and prophylaxis of diseases or disorders characterized by inflammation, e.g., neuroinflammation, including methods of treatment and pharmaceutical compositions for use therein.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: April 5, 2022
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Gretchen Snyder, Lawrence P. Wennogle, Jennifer O'Brien, Joseph Hendrick
  • Patent number: 11274074
    Abstract: The present disclosure relates to a novel anticancer pharmaceutical composition. The present disclosure achieves an anticancer effect using a compound effective in inhibiting the expression of ANO1 (TMEM16A). In addition, the present disclosure provides an ANO1 (TMEM16A) antagonist using the compound inhibiting the expression of ANO1 (TMEM16A).
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: March 15, 2022
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION YONSEI UNIVERSITY
    Inventors: Wan Namkung, Ik Yon Kim, Yohan Seo, Jin Hwang Kim
  • Patent number: 11241435
    Abstract: The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI).
    Type: Grant
    Filed: September 16, 2017
    Date of Patent: February 8, 2022
    Assignees: The General Hospital Corporation, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Marc Wein, Henry Kronenberg, Thomas Sundberg, Ramnik Xavier, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi, Alykhan Shamji
  • Patent number: 11234981
    Abstract: A pharmaceutical composition is provided comprising combination of antiretroviral drugs optionally in combination of pharmacokinetic boosters. The formulation is used for the treatment of diseases caused by retroviruses. The process of preparation of the formulation is also provided.
    Type: Grant
    Filed: April 18, 2018
    Date of Patent: February 1, 2022
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Kalpana Joshi, Preeti Raut
  • Patent number: 11198696
    Abstract: The present invention relates to compounds of formula I a process for their manufacture, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels. R1, R2, R3, R4 and R5 have meanings given in the description.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: December 14, 2021
    Assignees: Boehringer Ingelheim International GmbH, Hydra Biosciences, LLC
    Inventor: Kai Gerlach
  • Patent number: 11185545
    Abstract: The present invention is directed to a crystalline sodium salt of 5-methyl-(6S)-tetrahydrofolic acid wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to sodium is from 1:0.5 to 1:1.5 (in mol/mol) and/or hydrates and/or solvates thereof, as well as, a processes of obtaining the same.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: November 30, 2021
    Assignee: Merck Patent GmbH
    Inventors: Rudolf Moser, Viola Groehn, Fritz Blatter, Martin Szelagiewicz, Ruth Boehni Stamm, Markus Ruettimann, Giuseppe Lapadula
  • Patent number: 11186578
    Abstract: A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation, compositions, and uses thereof are disclosed. In particular, compounds of formula (I) and (II), or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a polymorph, a prodrug or an isotopic variation thereof, as well as a pharmaceutical composition including the same are disclosed. Compounds disclosed herein are substituted pyrrolo[3,2-d]pyrimidines and are selective irreversible inhibitors of Bruton's tyrosine kinase. The described compounds can therefore be used for preventing or treating diseases such as inflammation, autoimmune diseases (such as rheumatoid arthritis), xenogeneic immune diseases and cancers.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: November 30, 2021
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Qingfeng Xing
  • Patent number: 11180498
    Abstract: The present technology provides compounds according to Formula I expected to be useful in inhibiting an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus in a cell and/or treating subjects suffering from an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: November 23, 2021
    Assignee: The Regents of the University of California
    Inventors: Paul Krogstad, Michael E. Jung, Jun Zuo, Yanpeng Xing
  • Patent number: 11147817
    Abstract: The present invention relates to pharmaceutical composition comprising pemetrexed, a ready to use injection comprising pemetrexed. Liquid composition of pemetrexed comprises head space oxygen less than 5%, dissolved oxygen less than 2 ppm and individual impurity level less than 0.2%.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: October 19, 2021
    Assignee: FTF PHARMA PRIVATE LIMITED
    Inventors: Jayanta Kumar Mandal, Sandip Pareshbhai Mehta
  • Patent number: 11103602
    Abstract: A method for producing a solution including a positron emitting zinc cation of 63Zn, and the method comprises bombarding a solution target including 63Cu with high energy protons to produce a solution including a positron emitting zinc cation. A method for detecting or ruling out Alzheimer's disease in a patient comprises administering to a patient a detectable amount of a compound including a positron emitting zinc cation, wherein the zinc cation is targeted to ?-amyloid in the patient, and acquiring an image to detect the presence or absence of ?-amyloid in the patient. A method for detecting or ruling out cancer in a patient comprises administering to a patient a detectable amount of a compound including a positron emitting zinc cation, wherein the zinc cation is targeted to tissue in the patient; and acquiring an image using a medical imaging technique to detect zinc distribution in tissue in the patient.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: August 31, 2021
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Timothy R. Degrado, Mukesh K. Pandey, Hendrik Petrus Engelbrecht, Val J. Lowe
  • Patent number: 11090302
    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: March 11, 2019
    Date of Patent: August 17, 2021
    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: 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: 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: 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: 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: 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