Patents Examined by Paul V. Ward
  • Patent number: 10894038
    Abstract: Provided are certain URAT1 inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Grant
    Filed: December 26, 2016
    Date of Patent: January 19, 2021
    Assignees: SHANGHAI FOCHON PHARMACEUTICAL CO. LTD., FOCHON PHARMACEUTICALS, LTD.
    Inventors: Tongshuang Li, Xingdong Zhao, Chuiliang Yu, Haohan Tan, Xianlong Wang, Rui Tan, Bin Liu, Weipeng Zhang, Huajie Zhang, Qihong Liu, Zuwen Zhou, Zhifu Li, Yue Rong, Jing Sun, Weibo Wang
  • Patent number: 10894785
    Abstract: The present invention relates to novel piperidine derivatives having better cell growth inhibitory activities toward cancer cell cultures and, more particularly, PANC-1 cancer cell cultures than FK866. Accordingly, the present invention relates to compounds of formula I, wherein Ar1 is aryl or heteroaryl, which are optionally substituted by one, two or three substituents selected from lower alkyl; lower alkoxy; formyl; hydroxyl; lower alkyl substituted by lower alkoxy or hydroxyl; A is CnH2n, CnH2n-2 or CnH2n-4, wherein n=4,5,6,7; B is ?N—CN, oxo (?O), thio (?S); D is NH, —CH?CH—; Ar2 is aryl or heteroaryl which are optionally substituted by one, two or three halogen substituents; wherein, if B is oxo (?O), Ar1 and Ar2 are not simultaneously phenyl and pyridine-3-yl; B and D are not simultaneously ?N—CN and —CH?CH—, or a pharmaceutically acceptable salt, a racemic mixture or its corresponding enantiomers and/or optical isomers.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: January 19, 2021
    Inventors: Pierre Vogel, Michel Duchosal, Nahimana Aimable, Inmaculada Robina, Faustino Mollinedo, Alessio Nencioni
  • Patent number: 10889573
    Abstract: The present invention covers new quinoline compounds of general formula (I) in which A, R1, R2, R3, R4, R5, R6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 6, 2017
    Date of Patent: January 12, 2021
    Assignee: Bayer Animal Health GMBH
    Inventors: Walter Hübsch, Johannes Köbberling, Adeline Köhler, Hans-Georg Schwarz, Daniel Kulke, Claudia Welz, Thomas Ilg, Kirsten Börngen, Wei Zhuang, Nils Griebenow, Claudia Böhm, Niels Lindner, Maike Hink, Ulrich Görgens
  • Patent number: 10882864
    Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: January 5, 2021
    Assignee: Genentech, Inc.
    Inventors: Danial Beaudry, Theresa Cravillion, Francis Gosselin, Ngiap-Kie Lim, Sushant Malhotra, Qingping Tian, Haiming Zhang, Alexander Gmehling, Alec Fettes, Stephan Bachmann
  • Patent number: 10882863
    Abstract: The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to administration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: January 5, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Changchun Deng, Mark Lipstein, Owen O'Connor, Donald W. Landry, Xiaoming Xu, Shi-Xian Deng
  • Patent number: 10882833
    Abstract: The present invention discloses a phenylate derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to phenylate derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: January 5, 2021
    Assignees: Institute of Materia Medica, Chinese Academy of Medical Sciences, Tianjin Chase Sun Pharmaceutical Co., LTD
    Inventors: Zhiqiang Feng, Xiaoguang Chen, Yang Yang, Chuan Zhou, Fangfang Lai, Ming Ji, Xiaofeng Jin, Nina Xue, Yi Zheng, Hao Chen, Ling Li
  • Patent number: 10875843
    Abstract: Disclosed is a process for preparing Compound 8: (8) comprising the step of reacting Compound of 7: (7) wherein R is C1-8 alkyl or benzyl in the presence of a base. Also disclosed are intermediates and processes for preparing the intermediates.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: December 29, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald Carrasquillo, Peng Geng, Eric C. Huang, Kishta Katipally, Andrew Lee, Boguslaw Mudryk, Xinhua Qian, Thomas M. Razler, Jianji Wang, Carolyn S. Wei, Steven R. Wisniewski, Ye Zhu
  • Patent number: 10870650
    Abstract: The present invention relates to a process for the preparation of stable and 5 pure amorphous form of Idelalisib. Further, the present process is simple, more economical, cost effective and efficient method of manufacturing that is suitable for industrial scale-up having a high degree of chromatographic purity.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: December 22, 2020
    Assignee: NATCO PHARMA LIMITED
    Inventors: Amala Kompella, Sreenivas Rachakonda, Venugopala Krishna Gampa, Subhash Kusumba, Durga Prasad Konakanchi, Pulla Reddy Muddasani, Venkaiah Chowdary Nannapaneni
  • Patent number: 10870663
    Abstract: The invention relates a compound of the formula: a pharmaceutically acceptable salt thereof, compositions thereof, and methods of therapeutic treatment using the same.
    Type: Grant
    Filed: June 10, 2020
    Date of Patent: December 22, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Richard M Dunham, David Margolis, Vincent Wing-Fai Tai, Jun Tang
  • Patent number: 10865214
    Abstract: The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
    Type: Grant
    Filed: July 5, 2018
    Date of Patent: December 15, 2020
    Assignees: The Trustees of Columbia University in they City of New York, NY State Psychiatric Institute
    Inventors: Kirsten Alison Rinderspacher, Wai Yu, Karen Duff, Donald Landry, Shi-Xian Deng
  • Patent number: 10865198
    Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.
    Type: Grant
    Filed: May 3, 2019
    Date of Patent: December 15, 2020
    Assignee: Alexion Pharmaceuticals, Inc.
    Inventors: Anjali Pandey, Julian Scott Northen, Philippe Fernandes, Ying Chen, Yuelie Lu, Sami Karaborni, Gus Kodersha
  • Patent number: 10849980
    Abstract: The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: December 1, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: James Bradner, Dennis Buckley, Georg Winter
  • Patent number: 10844045
    Abstract: Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: November 24, 2020
    Assignee: BETA PHARMA, INC.
    Inventors: Michael N. Greco, Michael J. Costanzo, Michael A. Green, Jirong Peng, Victoria Lynn Wilde, Don Zhang
  • Patent number: 10842878
    Abstract: The present application provides bifunctional compounds of Formula (I): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: November 24, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang
  • Patent number: 10836741
    Abstract: The present 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, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: November 17, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • Patent number: 10836773
    Abstract: The present invention provides a compound of Formula I: wherein R is hydrogen or methyl; and Z is: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating neurodegenerative diseases, such as Alzheimer's disease.
    Type: Grant
    Filed: July 28, 2020
    Date of Patent: November 17, 2020
    Assignee: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Jose Eduardo Lopez, Leonard Larry Winneroski, Jr., Eric Michael Woerly
  • Patent number: 10836731
    Abstract: A method for precipitating as particles 2,6-diamino-3,5-dinitropyrazine-1-oxide (or ANPZO) present in an acid medium, which comprises adding the acid medium to an aqueous solution and which is characterized in that the aqueous solution comprises a nitrate salt. Further disclosed is a method for synthesizing ANPZO implementing this precipitation method. The synthesis method comprises converting 2,6-diaminopyrazine-1-oxide (or DAPO) into ANPZO by nitration in an acid medium, and then precipitating as particles the ANPZO by adding the acid medium to an aqueous solution, and is characterized in that the aqueous solution comprises a nitrate salt.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: November 17, 2020
    Assignee: COMMISSARIAT A L'ÉNERGIE ATOMIQUE ET AUX ÉNERGIES ALTERNATIVES
    Inventors: Eric Pasquinet, Anne Wuillaume, Nicolas Pin, Arnaud Beaucamp, Christelle Barthet
  • Patent number: 10836778
    Abstract: Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates.
    Type: Grant
    Filed: January 15, 2018
    Date of Patent: November 17, 2020
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Pierluigi Padovan, Kexia Lou
  • Patent number: 10829458
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have one of the following structures (I), (II) or (III): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, B, G1, G2, L1, L2, m1, m2, n, x, y, X and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: February 21, 2019
    Date of Patent: November 10, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 10829464
    Abstract: Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: November 10, 2020
    Assignee: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Jian Li, Lefu Lan, Baoli Li, Feifei Chen, Shuaishuai Ni, Yifu Liu, Hanwen Wei, Fei Mao, Jin Zhu