Patents Examined by Venkataraman Balasubramanian
  • Patent number: 10913737
    Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: February 9, 2021
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Marvin J. Miller, Garrett C. Moraski, Lowell D. Markley, George E. Davis
  • Patent number: 10913735
    Abstract: The present invention relates to bis-heteroaryl compounds of formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: February 9, 2021
    Assignee: UCB Biopharma SRL
    Inventor: Adrian Hall
  • Patent number: 10913742
    Abstract: The invention relates to 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 respiratory disorders or pain.
    Type: Grant
    Filed: May 23, 2019
    Date of Patent: February 9, 2021
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Daniel Shore, Elisia Villemure, Matthew Volgraf, Baihua Hu, Aijun Lu, Andrew Cridland, Stuart Ward, Francis Beaumier, Martin Dery, Robin Larouche-Gauthier
  • Patent number: 10899762
    Abstract: This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
    Type: Grant
    Filed: February 10, 2020
    Date of Patent: January 26, 2021
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Sharon Mates, Peng Li, Lawrence P. Wennogle, Robert Davis
  • Patent number: 10899767
    Abstract: Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and/or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: January 26, 2021
    Assignee: Hangzhou SoliPharma Co., Ltd.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Tao Zhu
  • Patent number: 10899766
    Abstract: The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; -( ) m-is —(CH2)m— or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-in-farct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: January 26, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Jérôme Charles Sarie, Greta Vastakaite
  • Patent number: 10899764
    Abstract: The present invention relates to an imidazo isoindole derivative, a preparation method therefor and a medical use thereof. In particular, the present invention relates to the imidazo isoindole derivative as shown in the formula (I), a preparation method and pharmaceutical composition containing the derivative, and a use thereof for treating diseases with a pathological characteristic of the IDO-mediated tryptophan metabolic pathways. The diseases comprise cancers, Alzheimer's disease, autoimmune diseases, depression, anxiety disorders, cataracts, psychological disorders and AIDS, wherein the substituents in the formula (I) are the same as those defined in the specification.
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: January 26, 2021
    Assignees: JIANGSU HENGRUI MEDICINE CO., LTD., SHANGHAI HENGRUI PHRMACEUTICAL CO., LTD.
    Inventors: Wangyang Tu, Guoji Xu, Haitang Zhang, Jiangtao Chi, Qing Dong
  • Patent number: 10899734
    Abstract: The present disclosure relates to chemical compounds that modulate pantothenate kinase (PanK) activity for the treatment of metabolic disorders (such as diabetes mellitus type II), neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: January 26, 2021
    Assignee: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, INC.
    Inventors: Lalit Kumar Sharma, Richard E. Lee, Charles O. Rock, Suzanne Jackowski, Mi Kyung Yun, Chitra Subramanian, Jiuyu Liu
  • Patent number: 10894050
    Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: January 19, 2021
    Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.
    Inventors: D. Keith Hester, II, Robert J. Duguid, Martha J. Kelly, Anna Chasnoff, Gang Dong, Edwin L. Crow, Lianhe Shu, Ping Wang, Duk Soon Choi
  • Patent number: 10889584
    Abstract: The present invention relates to certain bicyclic bis-heteroaryl compounds of Formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: January 12, 2021
    Assignee: UCB Biopharma SRL
    Inventors: Adrian Hall, Laurent Provins, Malcolm Maccoss
  • Patent number: 10882866
    Abstract: The present invention encompasses intermediates for preparing compounds of formula (I) wherein the groups R1 to R4, R7, A, D, E, F, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.
    Type: Grant
    Filed: April 9, 2020
    Date of Patent: January 5, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Gollner, Joachim Broeker, Nina Kerres, Christiane Kofink, Juergen Ramharter, Harald Weinstabl, Annika Gille, Stefan Goepper, Manuel Henry, Guenther Huchler
  • Patent number: 10875840
    Abstract: A method for catalytically converting a dihydrotetrazine 1 into a tetrazine 2, wherein one R group on the dihydrotetrazine 1 is a substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl, or heteroatom-containing group, and the other R group is selected from the group consisting of H and substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl,- or heteroatom-containing groups; 1, 2 wherein the method comprises oxidizing dihydrotetrazine 1 in a reaction medium in the presence of a catalyst and a stoichiometric oxidant.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: December 29, 2020
    Assignee: UNIVERSITY OF DELAWARE
    Inventors: Joseph Fox, Xinqiao Jia, Will Trout, Joel Rosenthal, Han Zhang, Yinzhi Fang, Colin Thorpe, Shuang Liu, Yixin Xie
  • Patent number: 10865209
    Abstract: The present invention relates to an efficient and industrially advantageous process for preparing temozolomide and the carbamoyl-AICA intermediate through the use of N-methyl carbamoylimidazole in a good overall yield and high purity.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: December 15, 2020
    Assignee: CRISTÁLIA PRODUTOS QUÍMICOS FARMACÊUTICOS LTDA
    Inventors: Ogari Pacheco, Vincenzo De Sio, Murilo Massoni, Leandro Camargo
  • Patent number: 10849899
    Abstract: In one aspect the present disclosure provides a method of sensitizing a cancer patient to chemotherapy by administering a combination therapy comprising; a) a therapeutically effective amount of a compound of formula (I) an enantiomer thereof or a pharmaceutically acceptable salts of any one of the same, and b) a chemotherapeutic agent or a combination of chemotherapeutic agents.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: December 1, 2020
    Assignee: ASLAN Pharmaceuticals PTE LTD
    Inventors: Bertil Lindmark, Lisa Ooi
  • Patent number: 10851100
    Abstract: Disclosed are an intermediate of a pyrrolo six-membered heteroaromatic ring derivative as a JAK inhibitor and a preparation method therefor, and a method for preparing a pyrrolo six-membered heteroaromatic ring derivative using the intermediate. The method improves the reaction yield, is simple and easy to operate and control, and is conducive to expanded industrial production.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: December 1, 2020
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Bing Liu, Lin Bian, Xiaohui Gao
  • Patent number: 10851069
    Abstract: The present invention provides, in certain embodiments, compositions comprising a uniform population of free, single crystals of a hydrophobic compound. Methods of administering, and processes for preparing, compositions comprising a uniform population of free, single crystals of a hydrophobic compound are also provided.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: December 1, 2020
    Assignee: Massachusetts Institute of Technology
    Inventors: Shady Farah, Joshua C. Doloff, Robert S. Langer, Daniel G. Anderson
  • Patent number: 10851068
    Abstract: A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.
    Type: Grant
    Filed: July 3, 2018
    Date of Patent: December 1, 2020
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Runfeng Lin, Xiaojun Wang, Jihua Lin, Liang Chen, Yingjun Zhang, Jiancun Zhang
  • Patent number: 10844069
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: November 24, 2020
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Xiaozhao Wang, Chunhong He
  • Patent number: 10844076
    Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: November 24, 2020
    Assignee: Nektar therapeutics
    Inventors: Pankaj Sharma, Vijay Kumar Khatri, Xuyuan Gu, Yuan Song, Michael Lixin Shen, Jennifer Riggs-Sauthier, Neel K. Anand, Antoni Kozlowski, Aleksandrs Odinecs, Timothy A. Riley, Zhongxu Ren, YongQi Mu, Xiaoming Shen, Xuejun Yuan, Natalia Aurrecoechea, Donogh John Roger O'Mahony, Bo-Liang Deng
  • Patent number: 10836730
    Abstract: The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
    Type: Grant
    Filed: February 21, 2018
    Date of Patent: November 17, 2020
    Assignee: UNICHEM LABORATORIES LTD.
    Inventors: Dhananjay G. Sathe, Arijit Das, Vishal Kulkarni, Tushar Patil, Yogesh Patil, Prafulla Nagawade