Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
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Patent number: 11319303Abstract: It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.Type: GrantFiled: May 18, 2018Date of Patent: May 3, 2022Assignee: WIGEN BIOMEDICINE TECHNOLOGY (SHANGHAI) CO., LTD.Inventors: Cheng Luo, Yuli Xie, Bing Zhou, Zhiyi Yao, Liyan Yue, Wei Wan, Bidong Zhang, Yuanyuan Zhang, Hualiang Jiang, Kaixian Chen
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Patent number: 11311527Abstract: Patients diagnosed with a cancer harboring an IDH-1 mutation can be treated by the administration of a therapeutically effective amount of a pharmaceutical composition comprising Compound 1, a selective inhibitor of 2-HG production from mIDH-1 enzymes including the R132 mutations R132C, R132H, R132L, R132G, and R132S.Type: GrantFiled: June 4, 2020Date of Patent: April 26, 2022Assignee: FORMA Therapeutics, Inc.Inventors: Patrick F. Kelly, Susan Ashwell, Blythe Thomson, Alan Collis, Jeff Davis, Duncan Walker, Wei Lu
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Patent number: 11291662Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: December 5, 2019Date of Patent: April 5, 2022Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Patent number: 11273154Abstract: Method and compounds for treating cancer by, for example, modulating immune system activity, are provided.Type: GrantFiled: March 2, 2018Date of Patent: March 15, 2022Assignee: PROGENRA, INC.Inventors: Hui Wang, Jian Wu, Suresh Kumar Kizhakkethil-George, Feng Wang, Joseph Weinstock
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Patent number: 11161818Abstract: A novel quinolone derivative and methods of its preparation are described in which the novel derivative comprises a diphenyl ether substituent on the nitrogen atom at the 1-position of the main quinolone ring. The novel derivative is shown to have antibacterial and anti-tumor cell activity.Type: GrantFiled: March 24, 2020Date of Patent: November 2, 2021Assignee: HANGZHOU NORMAL UNIVERSITYInventors: Pengfei Zhang, Wanmei Li, Weiming Xu, Haifeng Wu
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Patent number: 11147807Abstract: The present invention relates to a pharmaceutical composition comprising a DUSP1 inhibitor. The pharmaceutical composition comprising the DUSP1 inhibitor according to the present invention can solve the problems of inhibitors that target the active site because it inhibits DUSP1 by an allosteric inhibitory mechanism, and is effective for preventing or treating diseases involving DUSP1 enzymes, for example, a cancer such as a liver cancer, a breast cancer and a pancreatic cancer, a hepatitis C, and a depression. In particular, the DUSP1 inhibitor according to the present invention is very effective in treating a depression because it directly acts on neuronal growth.Type: GrantFiled: February 28, 2018Date of Patent: October 19, 2021Assignees: INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Seong Eon Ryu, Tae Hyun Park, Kwang Hwan Lee, Ju Seop Kang, Shin Hee Kim, Kyoung Tae Nam, Hyeon Kyu Lee
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Patent number: 11141413Abstract: The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.Type: GrantFiled: April 17, 2017Date of Patent: October 12, 2021Assignee: Exelixis, Inc.Inventors: Dana T. Aftab, Gisela Schwab, Colin Hessel, Christian Scheffold, Steven Lacy, Dale Miles, Alan Arroyo, Mark Dean
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Patent number: 11130737Abstract: Aminoquinoline compounds useful for treating chronic pain, addiction, and other conditions are provided. The aminoquinoline compound is represented by Formula (I): in which the substituents thereof are defined as set forth in the specification.Type: GrantFiled: October 7, 2019Date of Patent: September 28, 2021Assignee: LOHOCLA RESEARCH CORPORATIONInventor: Boris Tabakoff
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Patent number: 11123338Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.Type: GrantFiled: December 20, 2019Date of Patent: September 21, 2021Assignee: Exelixis, Inc.Inventors: Jo Ann Wilson, Khalid Shah
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Patent number: 11098015Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.Type: GrantFiled: February 9, 2021Date of Patent: August 24, 2021Assignee: Exelixis, Inc.Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
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Patent number: 11083743Abstract: The present invention relates to a method of treating and/or preventing cancer comprising administering a combination of an effective amount of a DNA hypomethylating agent and an effective amount of at least one immunomodulatory agent and/or optionally an effective amount of at least one targeted therapy agent.Type: GrantFiled: February 21, 2014Date of Patent: August 10, 2021Inventors: Michele Maio, Sandra Coral, Alessia Covre
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Patent number: 11058676Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.Type: GrantFiled: August 27, 2019Date of Patent: July 13, 2021Assignee: PHARMAKEA, INC.Inventors: Martin W. Rowbottom, John Howard Hutchinson
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Patent number: 11026937Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.Type: GrantFiled: September 11, 2017Date of Patent: June 8, 2021Assignee: Padlock Therapeutics, Inc.Inventors: Rajesh Devraj, Gnanasambandam Kumaravel, Cristina Lecci, Pui Leng Loke, Mirco Meniconi, Nathaniel Julius Thomas Monck, Carl Leslie North, Mark Peter Ridgill, Heather Tye
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Patent number: 11016085Abstract: The present invention describes methods of identifying drugs for the treatment or prevention of diabetes by measuring the activity of the human zinc transporter ZnT8 and pharmaceutical compositions.Type: GrantFiled: April 25, 2017Date of Patent: May 25, 2021Assignee: The Johns Hopkins UniversityInventor: Dax Fu
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Patent number: 10988478Abstract: Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.Type: GrantFiled: January 29, 2020Date of Patent: April 27, 2021Assignee: Genentech, Inc.Inventors: Marian C. Bryan, Alberto Gobbi, James Richard Kiefer, Jr., Aleksandr Kolesnikov, Alan G. Olivero, Joy Drobnick, Jun Liang, Naomi Rajapaksa, Chudi Ndubaku, Jianwen Feng
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Patent number: 10980793Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.Type: GrantFiled: August 14, 2019Date of Patent: April 20, 2021Assignee: KURA ONCOLOGY, INC.Inventors: Antonio Gualberto, Catherine Rose Scholz
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Patent number: 10954210Abstract: The present invention relates to novel crystal forms of tipifarnib. Compared with the prior art, the crystal forms of tipifarnib have advantages in crystallinity, hygroscopicity, morphology, form stability and chemical stability. The present invention also relates to the preparation methods of crystal forms of tipifarnib, pharmaceutical composition thereof and their use in preparation for treating and/or preventing abnormal cell growth diseases.Type: GrantFiled: December 8, 2016Date of Patent: March 23, 2021Assignee: Hangzhou SoliPharma Co., Ltd.Inventors: Xiaohong Sheng, Xiaoxia Sheng, Yanli Dai
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Patent number: 10881655Abstract: The present disclosure relates generally to compositions and methods of treating neoplastic diseases or cancers, such as glioblastoma and non-Hodgkin's lymphomas, or other cancers in which the subject suffers from an advanced solid tumor, comprising a combination of, or administering a combination of, a bromodomain and extra-terminal protein (BET) inhibitor and at least one chemotherapeutic agent, which does not inhibit BET directly. The BET inhibitor/chemotherapeutic agent combination, or combination therapy, can yield synergistic effects, thereby increasing the effectiveness of the cancer treatment as compared with the administration of either the BET inhibitor or the chemotherapeutic agent alone.Type: GrantFiled: January 23, 2020Date of Patent: January 5, 2021Assignee: Celgene Quanticel Research, Inc.Inventors: Robert Cho, Jeffrey Alan Stafford
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Patent number: 10875831Abstract: A method for preparing an alkyl 5,7-dihalo-1,4-dihydro-4-oxoquinoline-2-carboxylate ester is described herein. The method comprises cyclizing a compound of Formula III with Eaton's reagent in heated continuous flow reactor to form a compound of Formula IV wherein in Formula III and Formula IV, each X independently is a halogen atom; and each R independently is C1 to C4 alkyl. Optionally, a cosolvent such as dichloromethane can be included with the Eaton's reagent. A method of preparing a diphenylureido-dihalokynurenic acid alkyl ester of Formula VI from the compound of Formula IV also is described.Type: GrantFiled: August 12, 2019Date of Patent: December 29, 2020Assignee: Lohocla Research CorporationInventors: Sergiy Krasutsky, Scott Tweedie, Gurusankar Ramamoorthy
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Patent number: 10865206Abstract: 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: GrantFiled: May 15, 2019Date of Patent: December 15, 2020Assignee: 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
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Patent number: 10851061Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.Type: GrantFiled: November 1, 2019Date of Patent: December 1, 2020Assignee: Exelixis, Inc.Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
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Patent number: 10844416Abstract: The present invention pertains to a cell culture medium comprising manganese as a media supplement, which was shown to control recombinant protein glycosylation and methods of using thereof. The present invention further pertains to a method of controlling or manipulating glycosylation of a recombinant protein of interest in a large scale cell culture.Type: GrantFiled: June 1, 2016Date of Patent: November 24, 2020Assignee: Biogen MA Inc.Inventors: Lia Tescione, Thomas Ryll, Alan Gilbert
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Patent number: 10772865Abstract: The present invention relates to methods for treating a disease associated with insulin resistance selected from a nonalcoholic fatty liver disease (NAFLD) and its sequelae, a lipodystrophic syndrome or a combination thereof with the selective PPAR? agonist, INT131 and optionally vitamin E or compositions thereof. NAFLDs that may be treated with methods and compositions of the present invention include, but are not limited to, simple nonalcoholic fatty liver and nonalcoholic steatohepatitis (NASH). Lipodystrophic syndromes that may be treated with the methods and compositions of the present invention include, but are not limited to, generalized lipodystrophy including congenital generalized lipodystrophy and acquired generalized lipodystrophy and/or partial lipodystrophy, including congenital partial lipodystrophy and acquired partial lipodystrophy, all of which may or may not include hyperlipidemia and/or hyperglycemia and may or may not include NAFLD.Type: GrantFiled: January 16, 2020Date of Patent: September 15, 2020Assignee: Coherus Biosciences, Inc.Inventor: Christos Mantzoros
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Patent number: 10744127Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.Type: GrantFiled: April 5, 2017Date of Patent: August 18, 2020Assignee: Magyar Tudományos Akadémia Természettudományi KutatóközpontInventors: Gergely Szakács, Tibor Soós, Roberta Ferenczi-Palkó, András Füredi, Szilárd Tóth, Dóra Türk, Veronika Pape, Ferenc Fülöp, István Szatmári, György Dormán
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Patent number: 10745390Abstract: Methods for improving mitochondrial function, decreasing iron accumulation, and/or decreasing oxidative stress by exposing cells or treating a subject to compounds or compositions of the general formula are described that are beneficial in treating, for example, diseases and conditions such as Friedreich's ataxia, normal aging, and various neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. Furthermore, such compounds are useful as probes for identifying defects in mitochondrial metabolism, mitochondrial iron accumulation, cellular stress among other mitochondrial diseases and helping to identify compounds active in overcoming such defects.Type: GrantFiled: June 2, 2017Date of Patent: August 18, 2020Assignee: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Robert B. Wilson, Maria Grazia Cotticelli, Phillip A. Benedetti, Amos Smith, Jason E. Melvin, Donna M Huryn
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Patent number: 10736886Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.Type: GrantFiled: January 18, 2019Date of Patent: August 11, 2020Assignee: Exelixis, Inc.Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
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Patent number: 10683274Abstract: The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: wherein X is an oxygen atom and the like; Y is —CO—, —SO2— and the like; R1 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.Type: GrantFiled: November 29, 2018Date of Patent: June 16, 2020Assignee: Boston Biomedical, Inc.Inventors: Toshihiko Sone, Wataru Hirose, Naoaki Shimada, Chiang Li, Wei Li, David Leggett
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Patent number: 10675366Abstract: The present disclosure provides a positron emission tomography (PET)-detectable 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) probe that can selectively bind to the pyruvate kinase variant M2 (PKM2) found in cancer cells, such as of human glioma. Given the importance of PKM2 in the regulation of tumor metabolism, there is an on-going need to non-invasively measure its expression through the development of PKM2-specific radiopharmaceuticals. Precursors useful for the synthesis of the radiolabeled [18F]DASA-23-PKM2-specific probe and related compounds, and their methods of synthesis, are provided. Since the half-life of the 18F isotope is approximately 110 min, it is advantageous for a practitioner to attach the radionuclide to the precursor shortly before administration. Therefore, a precursor compound suitable for receiving the radionuclide and capable of specifically binding to the PKM2 variant can be provided.Type: GrantFiled: August 11, 2017Date of Patent: June 9, 2020Assignee: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Corrine Gaye Beinat, Israt Shamima Alam, Michelle L. James, Sanjiv S. Gambhir, Ananth Srinivasan
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Patent number: 10662207Abstract: The present disclosure is directed to disclosed compounds that modulate e.g., address underlying defects in cellular processing of CFTR activity.Type: GrantFiled: April 7, 2017Date of Patent: May 26, 2020Assignee: Proteostasis Therapeutics, Inc.Inventors: Benito Munoz, Daniel Parks, Cecilia M. Bastos
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Patent number: 10654807Abstract: Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR8 agonist is useful. The pharmaceutical compositions can include any ingredients, such as carries, diluents, excipients, fillers or the like that are common in pharmaceutical compositions. The compounds can be those illustrated or described herein as well as derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combinations thereof. As such, the compounds can be used as adjuvants in vaccines as well as for other therapeutic purposes described herein. The compounds can have any one of the formulae described herein or derivative thereof.Type: GrantFiled: December 19, 2014Date of Patent: May 19, 2020Assignee: The University of KansasInventors: Sunil Abraham David, Hari Prasad Kokatla, Diptesh Sil, Subbalakshmi Malladi, Lauren Miranda Fox
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Patent number: 10639299Abstract: Described herein are compounds that can bind CaSR and/or a CaSR extracellular domain and formulations thereof. Also described herein are methods of inhibiting CaSR and/or treating a disease or disorder associated with a mutation in CaSR by administering a compound or formulation thereof described herein. Also described herein are assays that can be used to identify compounds that can bind an extracellular domain of CaSR.Type: GrantFiled: March 29, 2017Date of Patent: May 5, 2020Assignees: Georgia State University Research Foundation, Inc., University of Georgia Research Foundation, Inc., Board of Trustees of Michigan State UniversityInventors: Jenny Jie Yang, Jian Hu, Edward Brown, Kelley Moremen
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Patent number: 10588900Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.Type: GrantFiled: February 7, 2017Date of Patent: March 17, 2020Assignee: PHARMAKEA, INC.Inventors: Martin W. Rowbottom, John Howard Hutchinson
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Patent number: 10583133Abstract: The present invention relates to a pharmaceutical composition comprising lenvatinib mesylate and a stabilizer in an amount of about 10% to about 20% based on the total weight of the composition, wherein the stabilizer is selected from the group consisting of calcium hydroxide and potassium hydroxide; and its process for preparation thereof.Type: GrantFiled: March 1, 2019Date of Patent: March 10, 2020Assignee: SHILPA MEDICARE LIMITEDInventors: Nijaguni Revansiddayya Rudraswamy Math, Sreenivas Reddy, Ravi Vamsi Peri, Krishnamurthy Toppaladoddi, Shivakumar Pradeep
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Patent number: 10556883Abstract: Compounds having formula (I) are described. Also described, are methods of using these compounds to treat diseases, conditions, and disorders.Type: GrantFiled: February 1, 2017Date of Patent: February 11, 2020Assignee: GALDERMA RESEARCH & DEVELOPMENTInventors: Gilles Ouvry, Craig Steven Harris, Yushma Bhurruth-Alcor
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Patent number: 10548888Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.Type: GrantFiled: July 3, 2018Date of Patent: February 4, 2020Assignee: EXELIXISInventors: Jo Ann Wilson, Khalid Shah
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Patent number: 10508097Abstract: The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.Type: GrantFiled: March 7, 2017Date of Patent: December 17, 2019Assignees: The Global Alliance for TB Drug Development, Inc., Janssen Pharmaceutica NVInventors: Anna Marie Upton, Christopher Blair Cooper, Koenraad Jozef Lodewijk Marcel Andries, Jerome Emile Georges Guillemont, Walter Marcel Mathilde Van den Broeck, Brian Desmond Palmer, Zhenkun Ma
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Patent number: 10501418Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.Type: GrantFiled: February 16, 2015Date of Patent: December 10, 2019Assignee: Exelixis, Inc.Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
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Patent number: 10501438Abstract: This application relates to aryl-substituted dihydroquinolinones of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to aryl-substituted dihydroquinolinones and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.Type: GrantFiled: August 11, 2016Date of Patent: December 10, 2019Assignee: Neomed InstituteInventors: Guillaume Jacquemot, Malken Bayrakdarian, Shawn Johnstone, Jeffrey S. Albert, Andrew Griffin
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Patent number: 10472342Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.Type: GrantFiled: April 12, 2019Date of Patent: November 12, 2019Assignee: FORMA THERAPEUTICS, INC.Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
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Patent number: 10450286Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.Type: GrantFiled: April 19, 2019Date of Patent: October 22, 2019Assignee: FORMA THERAPEUTICS, INC.Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
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Patent number: 10449189Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.Type: GrantFiled: June 24, 2016Date of Patent: October 22, 2019Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventor: Akio Fujioka
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Patent number: 10442817Abstract: The present invention includes novel RAD52 inhibitors for preventing or treating cancers in a subject in need thereof. The present invention further includes a method of preventing or treating cancers in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent.Type: GrantFiled: June 3, 2016Date of Patent: October 15, 2019Assignee: Drexel UniversityInventor: Alexander V. Mazin
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Patent number: 10435389Abstract: The present invention relates to compounds 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: GrantFiled: September 11, 2018Date of Patent: October 8, 2019Assignee: Krouzon Pharmaccuticals, Inc.Inventors: Robert Volkmann, Anthony Marfat, Frederick Nelson, Panayiotis Zagouras
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Patent number: 10426767Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.Type: GrantFiled: April 5, 2018Date of Patent: October 1, 2019Assignee: Kura Oncolofy, Inc.Inventors: Antonio Gualberto, Catherine Rose Scholz
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Patent number: 10426780Abstract: The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: GrantFiled: December 1, 2016Date of Patent: October 1, 2019Assignee: ViiV Healthcare CompanyInventor: Mark Richard Underwood
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Patent number: 10406149Abstract: A novel technique with which it is possible to suppress chemical degradation of a compound represented by general formula (1) or a salt thereof in an aqueous liquid formulation containing a compound represented by general formula (1) or a salt thereof. A method for suppressing the generation of a compound represented by general formula (2) or a salt thereof including containing a compound represented by general formula (1) or a salt thereof and a magnesium compound in an aqueous liquid formulation.Type: GrantFiled: June 2, 2016Date of Patent: September 10, 2019Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Wataru Minagawa, Hitoshi Kozuka, Mizuho Shibata, Takahiro Goto, Chifuyu Toriumi, Norihiro Kanayama
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Patent number: 10407435Abstract: The present invention is a compound having the following formula: (Formula (I)) or a pharmaceutically acceptable salt thereof, wherein e.g. X is C or N; n is 1 to 10; each L is independently a 5- to 12-membered heteroaryl containing at least two nitrogen atoms; and W is a zinc-binding group. The compounds are useful as histone deacetylase (HDAC) inhibitors.Type: GrantFiled: October 29, 2015Date of Patent: September 10, 2019Assignee: Karus Therapeutics LimitedInventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Somhairle MacCormick, William John Nodes, Cyrille Davy Tomassi
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Patent number: 10399951Abstract: The present invention relates to compounds and compositions for inhibition of FASN, their synthesis, applications, and antidotes.Type: GrantFiled: August 31, 2018Date of Patent: September 3, 2019Assignee: FORMA THERAPEUTICS, INC.Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
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Patent number: 10376504Abstract: The present invention is directed to azacyanoquinolinone compounds of the general structural formula: (wherein R5 and R6 are defined herein) which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: July 27, 2016Date of Patent: August 13, 2019Assignee: Merck, Sharp & Dohme Corp.Inventors: Antonella Converso, Kevin Rodzinak
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Patent number: 10351527Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.Type: GrantFiled: April 9, 2015Date of Patent: July 16, 2019Assignees: THE UNIVERSITY OF BRITISH COLUMBIA, SIMON FRASER UNIVERSITYInventors: Paul Rennie, Artem Tcherkassov, Robert N. Young, Christophe M. Andre