Patents Examined by Erich Leeser
  • Patent number: 10497878
    Abstract: A compound represented by formula (I) or formula (1I): in formula (I), R3 represents an electron donating group, R4 represents a hydrogen atom, a substituted or unsubstituted aryl group or an electron donating group, L3 represents a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L4 represents a single bond, a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L3 and L4 may bond together to form a ring with the carbon atoms to which they are bonded, in formula (II), R5 represents an electron donating group, R6 represents a hydrogen atom, a substituted or unsubstituted aryl group or an electron donating group, L5 represents a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L6 represents a single bond, a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group.
    Type: Grant
    Filed: January 29, 2019
    Date of Patent: December 3, 2019
    Assignees: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, NIPPON SODA CO., LTD.
    Inventors: Takuma Yasuda, In Seob Park, Yu Seok Yang, Hiroshi Sumiya, Yukio Fukushima
  • Patent number: 10494348
    Abstract: The invention relates to novel methods of preparing cell-binding agent-cytotoxic agent conjugates, wherein the cytotoxic agent is an imine-containing cytotoxic agent bearing a maleimide group. In some embodiments, the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides conjugates prepared by the methods of the present invention, compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.
    Type: Grant
    Filed: March 26, 2019
    Date of Patent: December 3, 2019
    Assignee: IMMUNOGEN, INC.
    Inventors: Scott A. Hilderbrand, Benjamin M. Hutchins
  • Patent number: 10478424
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: November 19, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Laxman Pasunoori, Sreekantha Ratna Kumar
  • Patent number: 10479791
    Abstract: Disclosed herein is a compound of formula I and/or a pharmaceutically acceptable salt thereof that can serve as Erk inhibitors: They are potentially useful in the treatment of diseases treatable by inhibition of Erk, such as cancers. Also disclosed herein is a pharmaceutical composition comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: November 19, 2019
    Assignees: CHANGZHOU JIEKAI PHARMATECH CO. LTD, JS INNOPHARM (SHANGHAI) LTD
    Inventors: Jintao Zhang, Wen Xu, Shanzhong Jian
  • Patent number: 10471023
    Abstract: Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, L1, L2, L3, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: November 12, 2019
    Assignees: British Columbia Cancer Agency Branch, The University of British Columbia
    Inventors: Raymond John Andersen, Kunzhong Jian, Marianne Dorothy Sadar, Nasrin R. Mawji, Carmen Adriana Banuelos
  • Patent number: 10472369
    Abstract: The present disclosure relates to novel crystalline form I, form II and form III of 6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo [1,2-a]pyrazin-8-amine mesylate, and preparation methods and use thereof. Crystalline form I is a dimesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 5.9°±0.2°, 13.5°±0.2° and 21.8°±0.2°. Crystalline form II is a dimesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 15.8°±±0.2°, 17.2°±0.2° and 19.5°±0.2°. Crystalline form III is a monomesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 7.4°±0.2°, 12.9°±0.2° and 19.2°±0.2°. The crystalline forms are more suitable for drug development than prior crystalline forms, and the preparation methods for the crystalline forms are simple and repeatable and have significant value for future drug optimization and development.
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: November 12, 2019
    Assignee: Crystal Pharmatech Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Po Zou, Xiaoyu Zhang
  • Patent number: 10472372
    Abstract: Various embodiments relate to a compound of the formula (I): wherein X, X1, R1—R4 and R7 are defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I), or a pharmaceutical compositions comprising compounds of the formula (I), to a patient in need thereof.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: November 12, 2019
    Assignees: Purdue Research Foundation, National University Corporation Kumamoto University
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya
  • Patent number: 10464944
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: May 31, 2018
    Date of Patent: November 5, 2019
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10464902
    Abstract: The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: November 5, 2019
    Assignee: Ontogenesis, LLC
    Inventor: Gerald Horn
  • Patent number: 10457673
    Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions in a method of treating cancer. The dUTPase inhibitors disclosed contain a uracil isostere in the molecule represented by a 2,6-diketopiperazine moiety. Thioanalogs of the uracil isostere where a thione replaces each of the ketone are also disclosed.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: October 29, 2019
    Assignee: University of Southern California
    Inventors: Robert D. Ladner, Bruno Giethlen
  • Patent number: 10456394
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: October 29, 2019
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Sida Shen, Joel Bergman, Irina Gaisina
  • Patent number: 10456397
    Abstract: The disclosure includes compounds of Formula (I) wherein R0, R1, R2, R3, R4, R5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: October 29, 2019
    Assignee: Newave Pharmaceutical Inc.
    Inventors: Yi Chen, Yan Lou
  • Patent number: 10441588
    Abstract: The present disclosure relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present disclosure provides compounds as therapeutic agents against bacterial infections (e.g., biofilms). The present disclosure also provides topical formulations for use in methods for treating bacterial infections.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: October 15, 2019
    Assignees: Curators of the University of Missouri, Nanova, Inc.
    Inventors: Hongmin Sun, David W. Anderson, Feng Qi
  • Patent number: 10428061
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4a, R4b, R4c, R4d, L, A, Q, W and HET are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. 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 (e.g. fibrosis) in which ATX activity is implicated.
    Type: Grant
    Filed: October 25, 2018
    Date of Patent: October 1, 2019
    Assignee: Cancer Research Technology Limited
    Inventors: Francesca Blum, James Lindsay Carr, Pritom Shah, Maria Del Mar Jimenez Quesada, Irene Farre Gutierrez
  • Patent number: 10428076
    Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: October 1, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Yi-Heng Chen, Guoqing Li, Joie Garfunkle, Hong-Dong Li, Shouwu Miao, Subharekha Raghavan, Cameron J. Smith, John Stelmach, Alan Whitehead, Rui Zhang, Yong Zhang, Jianmin Fu, Gang Ji, Falong Jiang
  • Patent number: 10428067
    Abstract: Disclosed are compounds having a compound of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, compositions thereof, and uses thereof.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: October 1, 2019
    Assignee: Plexxikon Inc.
    Inventors: Chao Zhang, Guoxian Wu, Wayne Spevak, Zuojun Guo, Ying Zhang
  • Patent number: 10420772
    Abstract: Provided herein are Aminopurine compounds of Formula I: or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: September 24, 2019
    Assignee: Celgene Corporation
    Inventors: Stacie S. Canan, Natalie Anne Hawryluk, Michael John Witty
  • Patent number: 10420771
    Abstract: Provided herein are Purine Compounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologs, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: September 24, 2019
    Assignee: Celgene Corporation
    Inventors: Stacie S. Canan, Natalie Anne Hawryluk
  • Patent number: 10421750
    Abstract: The present invention relates to substituted morpholine derivatives having pharmacological activity towards the sigma (?) 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: October 21, 2016
    Date of Patent: September 24, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Marina Virgili-Bernado, Carlos Alegret-Molina
  • Patent number: 10414777
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: September 17, 2019
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee