Patents Examined by Erich A. Leeser
  • Patent number: 10851084
    Abstract: The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: December 1, 2020
    Assignee: Lysoway Therapeutics, Inc.
    Inventor: Congxin Liang
  • Patent number: 10851064
    Abstract: The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and drug resistant cancer of various types.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: December 1, 2020
    Assignee: METABOMED LTD.
    Inventors: Philippe Nakache, Omri Erez, Simone Botti, Andreas Goutopoulos
  • Patent number: 10851098
    Abstract: The present invention provides compounds of Formula (I): (Formula (I)), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?v-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: December 1, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, Wei Wang
  • Patent number: 10844079
    Abstract: Provided is a compound of formula I or a pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, isotopic substituent, polymorph, prodrug, or metabolite thereof. Also provided is a method for preparing the compound of formula I. The compound of formula I has higher inhibitory activity against SHP2, and thus can be used to prevent or treat a disease related to SHP2.
    Type: Grant
    Filed: June 22, 2020
    Date of Patent: November 24, 2020
    Assignee: Etern Biopharma (Shanghai) Co., Ltd.
    Inventors: Qiangang Zheng, Ming Xu, Qinglong Zeng, Jing Li, Hao Zhuge
  • Patent number: 10822333
    Abstract: The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): or pharmaceutically acceptable salts thereof, or their mixtures (in any ratio), a pharmaceutical composition containing them, a method for using the new pyridopyrimidine derivatives compounds as inhibitor of the cyclic nucleotide synthesis or as inhibitor of the cAMP and cGMP synthesis, and their uses in the prophylactic and/or curative treatment of diarrhea, colitis and irritable bowel syndrome.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: November 3, 2020
    Assignee: Biolab Sanus Farmaceutica LTDA
    Inventor: Gilberto De Nucci
  • Patent number: 10822348
    Abstract: The present disclosure is directed to compounds of formula I? and methods of their use and preparation, as well as compositions comprising compounds of formula I?.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: November 3, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nidhi Arora, Genesis M. Bacani, Joseph Kent Barbay, Scott D. Bembenek, Min Cai, Wei Chen, Charlotte Pooley Deckhut, James P. Edwards, Brahmananda Ghosh, Baoyu Hao, Kevin D. Kreutter, Gang Li, Mark S. Tichenor, Jennifer D. Venable, Jianmei Wei, John J. M. Wiener, Yao Wu, Yaoping Zhu, Feihuang Zhang, Zheng Zhang, Kun Xiao
  • Patent number: 10821188
    Abstract: The present teachings relate generally to conjugates and methods for imaging a tumor microenvironment in a patient, and to conjugates and methods for treating LHRH-R expressing cancer in a patient. The present teachings relate generally to method of making conjugates comprising an LHRH-R antagonist.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: November 3, 2020
    Assignee: Purdue Research Foundation
    Inventors: Philip Stewart Low, Jyoti Roy
  • Patent number: 10822344
    Abstract: A method of preparing neosaxitoxin in quantities of a purity sufficient to allow the compound to be used as an active pharmaceutical ingredient (API) is described. The method includes the reductive desulfonation of an unresolved mixture of gonyautoxin 1 (GTX1) and gonyautoxin 4 (GTX4).
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: November 3, 2020
    Inventors: Andrew Ian Selwood, Roelof Van Ginkel, Craig Alan Waugh
  • Patent number: 10822313
    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: October 30, 2019
    Date of Patent: November 3, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Scott A. Hilderbrand, Benjamin M. Hutchins
  • Patent number: 10815218
    Abstract: Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: October 27, 2020
    Inventors: Dominique Amans, Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Jessica Fanny Renaux, Robert John Sheppard, Ann Louise Walker, Christopher Roland Wellaway, David Matthew Wilson
  • Patent number: 10815226
    Abstract: The present disclosure provides heteroaryl compounds of formulas I, Ia and Ib, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to necrosis.
    Type: Grant
    Filed: July 15, 2017
    Date of Patent: October 27, 2020
    Inventors: Xiaohu Zhang, Haikuo Ma, Jiyue Zheng, Sudan He
  • Patent number: 10815233
    Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: October 27, 2020
    Inventors: Motoyuki Tanaka, Takashi Kondo, Yasuo Hirooka, Taihei Nishiyama, Atsushi Hiramatsu, Tomoyuki Koda, Sho Kouyama
  • Patent number: 10806719
    Abstract: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: October 20, 2020
    Inventors: Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He
  • Patent number: 10800758
    Abstract: The present invention provides a novel pyrimidine compound represented by Formula [I] and a salt thereof: [in the formula, the symbols are as defined in the specification], which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
    Type: Grant
    Filed: May 31, 2018
    Date of Patent: October 13, 2020
    Inventors: Tomoichi Shinohara, Shin Iwata, Kenta Arai, Nobuaki Ito, Masaki Suzuki
  • Patent number: 10787424
    Abstract: The present invention relates to oxopiperazines that mimic helix ?B of the C-terminal transactivation domain of HIF1?. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
    Type: Grant
    Filed: May 20, 2015
    Date of Patent: September 29, 2020
    Inventors: Paramjit S. Arora, Brooke Bullock Lao, Richard Bonneau, Kevin Drew
  • Patent number: 10786512
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: February 21, 2019
    Date of Patent: September 29, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
  • Patent number: 10787451
    Abstract: Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxy urea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: September 29, 2020
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Suncadia Pharmaceuticals Co., Ltd.
    Inventors: Quanliang Zhang, Junlei Jia, Lin Bian, Xiaohui Gao
  • Patent number: 10780180
    Abstract: The present invention relates to compounds for targeted immunotherapy, as well as compositions comprising the same. Further, the present invention relates to the use of the compounds in the treatment of diseases such as cancer.
    Type: Grant
    Filed: May 2, 2019
    Date of Patent: September 22, 2020
    Assignee: Birdie Biopharmaceuticals, Inc.
    Inventor: Lixin Li
  • Patent number: 10774065
    Abstract: The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: September 15, 2020
    Assignee: NOVARTIS AG
    Inventors: Christine Hiu-Tung Chen, Zhuoliang Chen, Jorge Garcia Fortanet, Denise Grunenfelder, Rajesh Karki, Mitsunori Kato, Matthew J. LaMarche, Lawrence Blas Perez, Travis Matthew Stams, Sarah Williams
  • Patent number: 10766878
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
    Type: Grant
    Filed: January 15, 2019
    Date of Patent: September 8, 2020
    Assignee: Genentech, Inc.
    Inventors: Baihua Hu, Vishal Verma, Matthew Volgraf, Anthony Estrada, Joseph Lyssikatos