Patents Examined by Mark L. Shibuya
  • Patent number: 10875883
    Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: December 29, 2020
    Inventors: Hong Liu, Jiang Wang, Shengbin Zhou, Panfeng Peng, Yong Nian, Shuni Wang, Shuangjie Shu, Hao Shen, Hualiang Jiang, Kaixian Chen
  • Patent number: 10870627
    Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 22, 2020
    Inventors: Guangxin Xia, Di Li, Ning Zhou, Ao Chen, Liang Zhao, Jiansheng Han, Yanjun Liu
  • Patent number: 10870626
    Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: December 22, 2020
    Assignees: F. Hoffman-La Roche AG, Genentech, Inc.
    Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
  • Patent number: 10865206
    Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: December 15, 2020
    Assignee: Syros Pharmaceuticals, Inc.
    Inventors: Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
  • Patent number: 10865188
    Abstract: The present disclosure provides crystalline Compound I and crystalline Compound II, pharmaceutical compositions comprising one of said crystalline compounds suitable for intratympanic administration, and methods for treating otic disorders using the crystalline compounds and the pharmaceutical compositions.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Thomas Jon Seiders, Catherine Yuling Lee, Yiwei Li
  • Patent number: 10865193
    Abstract: This invention relates to pyridone derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: December 15, 2020
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10858367
    Abstract: Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: December 8, 2020
    Inventors: Xiao Ding, Feng Ren, Yingxia Sang, Weiqiang Xing, Yang Zhan, Baowei Zhao
  • Patent number: 10849982
    Abstract: This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: December 1, 2020
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Kiel Lazarski, Gesine Kerstin Veits, Harit U. Vora
  • Patent number: 10844067
    Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X1, X2, X3, X4, integer a and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: November 24, 2020
    Assignee: Cancer Research Technology Limited
    Inventors: Allan Michael Jordan, Rebecca Newton, Bohdan Waszkowycz, Jonathan Mark Sutton, George Hynd, Silvia Paoletta, Euan Alexander Fraser Fordyce
  • Patent number: 10842794
    Abstract: Compositions and methods for the prevention, inhibition, and/or treatment of progressive fibrosis present in various fibroproliferative disorders. Embodiments relate to the use of Sigma-1 receptor agonists for use in the treatment of prevention of progressive fibrosis characterized by the over proliferation of ECM producing cells, e.g. myofibroblasts and by the excessive deposition of ECM components in a medical or disease condition. Preferred Sigma-1 agonists are disclosed.
    Type: Grant
    Filed: March 21, 2019
    Date of Patent: November 24, 2020
    Assignees: Támogatott Kutatócsoportok Irodája, Semmelweis Egyetem, SigmaDrugs Kft.
    Inventors: Andrea Fekete, Ádám Vannay, Endre Illés Kovács
  • Patent number: 10821127
    Abstract: The present invention relates to a method for inhibiting myeloid-derived suppressor cells or treating cancer comprising administering a pharmaceutical composition containing decitabine or its pharmaceutically acceptable salt as an active ingredient. The decitabine suppresses creation of a cell population of myeloid-derived suppressor cells (MDSC) created in spleen and bone marrow in tumorigenic mice and induces apoptosis of the MDSC cell population. Therefore, the decitabine may be useful as agents for treating MDSC-related diseases and anticancer immunotherapy, or an anticancer supplement.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: November 3, 2020
    Assignee: SHAPERON INC.
    Inventors: Seung-Yong Seong, Jung Ah Cho, Tae Joo Kim, Hyeon Park
  • Patent number: 10822325
    Abstract: The present invention relates to compounds which have been discovered to be potent ligands (inhibitors) of human GLUT5 (glucose transporter type 5), a facilitative glucose transporter that transports fructose, and their use as ligands assays which can uncover additional ligands of GLUT5, having the potential for being used as drugs. In addition, the present invention is directed to compounds, chemical compositions and methods for treating disease states and conditions which are mediated through GLUT5, including such disease states and conditions as GLUT5 deficiency syndrome, diabetes (type I and II), cancer, metabolic diseases including metabolic syndrome and fatty liver disease, among others.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: November 3, 2020
    Inventors: Tudor I. Oprea, Cristian George Bologa, Oleg Ursu, Jun-Yong Choe, Cristina Iancu
  • Patent number: 10822311
    Abstract: The present disclosure provides pyrimidine compounds and uses thereof, for example, for the treatment of diseases associated with P2X purinergic receptors. In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: November 3, 2020
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Ronald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
  • Patent number: 10815223
    Abstract: This invention provides for flow and batch synthesis processes for the production of Lamivudine and Emtricitabine, including flow and batch synthesis processes wherein at least of the synthesis steps are conducted in a solvent free environment.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: October 27, 2020
    Assignee: Nelson Mandela Metropolitan University
    Inventors: Devender Mandala, Paul Watts
  • Patent number: 10813927
    Abstract: The subject invention concerns a compound and compositions having activity as an inhibitor of Stat3 protein and methods of using the compound and compositions. In one embodiment, a compound of the invention has the structure shown in formula I, formula II, or formula III. The subject invention also concerns methods of using the compounds and compositions of the invention.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: October 27, 2020
    Inventors: Said M. Sebti, Nicholas J. Lawrence, James Turkson
  • Patent number: 10815232
    Abstract: The present disclosure relates to novel crystalline forms of VX-787, processes for preparation thereof and use thereof. VX-787 is a viral-protein inhibitor drug. The present disclosure provides crystalline form CS1, crystalline form CS2, crystalline form CS3, and crystalline form CS4 of compound (I) hydrochloride. The present disclosure also provides crystalline form CS3 and crystalline form CS9 of compound (I).free form.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: October 27, 2020
    Assignee: Crystal Pharmaceutical (Suzhou) Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Lie Chen, Chaohui Yang, Nan Xia, Xiaoyu Zhang, Chunxiang Huang
  • Patent number: 10807973
    Abstract: New compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, R1 is selected from the group consisting of fluoro, chloro and methoxy; B is selected from the group consisting of a residue of formula (II), (III) and (IV) wherein, “*” denotes the point of attachment to the remainder of the molecule, and R2, R2?, R2?, R3, R3?, R3?, R4, R4?, R4?, R5, R5? and R5? are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: October 20, 2020
    Inventors: Matthias Steger, Alex Mueller, Bernhard Fasching, Daphna Mokady
  • Patent number: 10807970
    Abstract: The present invention relates to tetrahydropyran and thiopyran derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: October 20, 2020
    Inventors: Monica Garcia-Lopez, Carmen Almansa-Rosales, Ana Virginia Llorente-Fernandez, Ute Christmann, Sergio Rodriguez Escrich
  • Patent number: 10792283
    Abstract: The present disclosure provides selective phosphoinositide 3-kinase inhibitors of formula (A), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more P13K isoforms, such as PI3K delta (PI3K?). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase inhibitors using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase activity.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: October 6, 2020
    Inventor: Xiaolin Hao
  • Patent number: 10786507
    Abstract: Provided in the present invention is a pharmaceutical composition containing a JAK kinase inhibitor or a pharmaceutically acceptable salt thereof. In particular, provided in the present invention is a pharmaceutical composition containing (3aR, 5s, 6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo [2,3-d] pyrimidin-4-yl) amino) hexahydrocyclopenta [c] pyrrol-2 (1H)-carboxamide, or a pharmaceutically acceptable salt thereof, and cellulose ether. The pharmaceutical composition of the present invention is characterized by a rapid dissolution rate and good stability.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: September 29, 2020
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Yun Lu, Hao Chen, Xiaochen Pan