Patents Examined by Jeffrey H Murray
  • Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor
    Patent number: 10829492
    Abstract: Provided is an amino pyrazolopyrimidine compound as represented by the following structural formula used as a neurotrophic factor tyrosine kinase receptor inhibitor. The compound can inhibit the activity of Trk kinase and can treat diseases mediated by a Trk tyrosine kinase receptor in mammals.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: November 10, 2020
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., CENTAURUS BIOPHARMA CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.
    Inventors: Li Zhu, Yuandong Hu, Wei Wu, Liguang Dai, Xiaowei Duan, Yanqing Yang, Yinghui Sun, Yongxin Han, Yong Peng, Fansheng Kong, Hong Luo, Ling Yang, Hongjiang Xu, Meng Guo, Zhaobai Zhong, Shanchun Wang
  • Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
    Patent number: 10829487
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: November 10, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Ramharter, Christiane Kofink, Heinz Stadtmueller, Tobias Wunberg
  • Nitrogenous heterocyclic compound, preparation method, intermediate, composition and use
    Patent number: 10828305
    Abstract: Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: November 10, 2020
    Assignee: Shanghai Pharmaceuticals Holding Co., Ltd.
    Inventors: Guangxin Xia, Di Li, Hongjian Zuo, Guangsheng Wu, Lingjun Duan, Jing Zhang, Yu Mao, Yanjun Liu
  • Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor
    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
  • Thieno[3,2-d]pyrimidines derivatives for the treatment of viral infections
    Patent number: 10822347
    Abstract: This invention relates to thieno[3,2-d]pyrimidines derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: November 3, 2020
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • ErbB receptor inhibitors
    Patent number: 10822334
    Abstract: Disclosed are compounds inhibiting ErbBs (e.g. HER2), pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat diseases associated ErbBs (especially HER2), including cancer.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: November 3, 2020
    Inventors: Zhengtao Li, Wei Zhong, Jiabing Wang, Qingbei Zeng, Honchung Tsui, Zhenfan Yang, Xiaolin Zhang
  • Manufacturing process and intermediates for a pyrrolo[2,3-d]pyrimidine compound and use thereof
    Patent number: 10815240
    Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: October 27, 2020
    Assignee: Pfizer Inc.
    Inventors: Kapildev Kashmirilal Arora, Jacob Cole DeForest, Andrew Kevern Hills, Brian Patrick Jones, Kris Nicole Jones, Chad Arthur Lewis, Anil Mahadeo Rane
  • Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-YL)-pyrazolo[1,5-A]pyrimidin-3-YL)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
    Patent number: 10813936
    Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: March 27, 2019
    Date of Patent: October 27, 2020
    Assignee: Array BioPharma, Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Fused pyrimidine compound or salt thereof
    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
  • Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
    Patent number: 10799505
    Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: October 13, 2020
    Assignee: Array BioPharma, Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Bicyclic inhibitors of histone deacetylase
    Patent number: 10793567
    Abstract: Provided are compounds of the formula and pharmaceutically acceptable salts and composition thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g. HDAC2).
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: October 6, 2020
    Assignee: Rodin Therapeutics, Inc.
    Inventors: Nathan Oliver Fuller, John A. Lowe, III
  • First-in-class of SHMT2 and MTHFD2 inhibitors as antitumor agents
    Patent number: 10793573
    Abstract: A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer ranging from 1 to 4; X is one selected from the group consisting of —CH2—, O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2?-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: October 6, 2020
    Assignees: Duquesne University of The Holy Spirit, Wayne State University
    Inventors: Aleem Gangjee, Larry H. Matherly
  • Hepatitis C virus inhibitors
    Patent number: 10787441
    Abstract: A compound of Formula (I) or (II), for treating or preventing an HCV infection in a subject.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: September 29, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang, Zhixin Lei
  • Pyrimidone compounds used as Lp-PLAinhibitors and pharmaceutical compositions thereof
    Patent number: 10787422
    Abstract: The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: September 29, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Jianhua Shen, Yiping Wang, Xinde Chen, Wenwei Xu, Kai Wang
  • Enantiomers of the 1?,6?-isomer of neplanocin A
    Patent number: 10787478
    Abstract: Enantiomers of 1?,6?-isoneplanocin, including derivatives of the enantiomers of 1?,6?-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1?,6?-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1?,6?-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: September 29, 2020
    Assignee: Auburn University
    Inventors: Stewart W. Schneller, Chong Liu, Qi Chen, Wei Ye
  • Substituted inhibitors of menin-MLL and methods of use
    Patent number: 10781218
    Abstract: The present disclosure provides compounds of Formula (II-A), which inhibit the interaction of menin with one or more of MLL1, MLL2 and MLL-fusion oncoproteins. Also disclosed are methods for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: September 22, 2020
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
  • 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
    Patent number: 10774070
    Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 15, 2020
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Natasja Brooijmans, Lucian V. DiPietro, Paul E. Fleming, Joseph L. Kim, Steven Mark Wenglowsky, Yulian Zhang
  • GSK-3 inhibitors
    Patent number: 10774086
    Abstract: The disclosure generally relates to compounds of formula (I), including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: September 15, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, Prasanna Sivaprakasam, Gene M. Dubowchik, John E. Macor
  • Indazole derivatives useful as glucagon receptor antagonists
    Patent number: 10774048
    Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
    Type: Grant
    Filed: January 8, 2019
    Date of Patent: September 15, 2020
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Guozhang Xu, Micheal Gaul, Shyh-Ming Yang, Tianbao Lu, Rui Zhang, Fengbin Song
  • Wee-1 inhibiting pyrazolopyrimidinone compounds
    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