1,3-diazines (e.g., Pyrimidines, Etc.) Patents (Class 514/256)
  • Patent number: 11357777
    Abstract: The present disclosure relates to methods, uses, pharmaceutical compositions and kits comprising an sGC stimulator or a pharmaceutically acceptable salt thereof, alone or in combination with one or more additional therapeutic agents, for the treatment of Nonalcoholic Steatohepatitis (NASH).
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: June 14, 2022
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: G-Yoon Jamie Im, Mark G. Currie, James Edward Sheppeck, Paul Allan Renhowe, Pei Ge, Jaime L. Masferrer
  • Patent number: 11345678
    Abstract: The invention relates to a benzopyrazole compound used as RHO kinase inhibitor, a pharmaceutical composition and uses thereof for preparing an RHO kinase inhibiting drug, and more specifically to said compound of formula (I-1), a pharmaceutically acceptable salt and isomer thereof.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: May 31, 2022
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Lingyun Wu, Jun Yin, Cailin Wang, Zheming Xiao, Jian Li, Shuhui Chen
  • Patent number: 11331311
    Abstract: The object of the present invention is to find a new application of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof. Isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl) aminometh yl}pyridin-2-ylamino) acetate or a salt thereof is useful as a therapeutic agent for a disease involving a greatly elevated intraocular pressure.
    Type: Grant
    Filed: March 11, 2020
    Date of Patent: May 17, 2022
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Tomoko Kirihara, Atsushi Shimazaki, Najam A. Sharif
  • Patent number: 11299473
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: April 12, 2022
    Assignee: Incyte Corporation
    Inventors: Joshua Hummel, Minh Nguyen, Alexander Sokolsky, Oleg Vechorkin, Qinda Ye, Wenqing Yao
  • Patent number: 11285134
    Abstract: Described herein are methods and compositions for the treatment of ocular conditions and for the improvement of vision parameters using pharmaceutically acceptable ophthalmic pilocarpine formulations. A nonlimiting example of an ocular condition that may be treated with the methods and compositions disclosed herein is presbyopia.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: March 29, 2022
    Assignee: ALLERGAN, INC.
    Inventors: Michael R. Robinson, Mohammed Dibas, Jaya Giyanani, Anuradha Gore, Sungwook Lee, Haixia Liu, Aileen Morgan, Jihao Zhou
  • Patent number: 11278545
    Abstract: The present disclosure describes compositions which improve visual acuity and to methods for their use.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: March 22, 2022
    Assignee: PRESBYOPIA TREATMENTS LIMITED
    Inventor: Anant Sharma
  • Patent number: 11279728
    Abstract: Compounds and methods for treating viral infections and reducing viral multiplication, including flaviviruses. Provided is a derivative of a compound or a pharmaceutical salt thereof, wherein the compound comprises a 3?,4-didehydroribose.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: March 22, 2022
    Assignees: Albert Einstein College of Medicine, The Penn State Research Foundation
    Inventors: Steven C. Almo, Tyler Grove, Anthony Gizzi, Craig E. Cameron, James J. Arnold
  • Patent number: 11273160
    Abstract: Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: March 15, 2022
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Erica Evans Raab, Beni B. Wolf
  • Patent number: 11236080
    Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: February 1, 2022
    Assignee: Princeton Drug Discovery, Inc
    Inventor: Kan He
  • Patent number: 11198682
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular in the treatment of diseases or disorders associated to increased relative to physiological or desired RhoJ/Cdc42 levels of expression or function.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: December 14, 2021
    Assignees: Fondazione Istituto Italiano Di Tecnologia, The Regents of the University of California
    Inventors: Marco De Vivo, Anand Ganesan, Jose Antonio Ortega Martinez, Sohail Jahid
  • Patent number: 11197855
    Abstract: A use of of ligustrazine nitrone derivatives and a pharmaceutical composition thereof in the preparation of medicine for preventing and treating diabetic complication diseases. The ligustrazine nitrone derivatives can be prepared into various dose forms together with drug carriers.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: December 14, 2021
    Inventors: Yuqiang Wang, Yewei Sun, Lipeng Xu, Mei Jing, Zaijun Zhang, Gaoxiao Zhang, Pei Yu, Peng Yi
  • Patent number: 11191758
    Abstract: The present invention relates to the reduction of the side-effects induced by tetrabenazine or other inhibitors of vesicular monoamine transporter (VMAT), in the treatment of central nervous system disorders such as Huntington's disease, L-DOPA-induced dyskinesias in Parkinson's disease, Tourette's syndrome or tardive dyskinesia. The invention comprises administering to a patient in need thereof an effective amount of activates selective serotonin 5-HT1A receptors agonist, whereby the side-effects of depression or Parkinsonism induced by tetrabenazine or other VMAT inhibitors are minimized.
    Type: Grant
    Filed: July 20, 2018
    Date of Patent: December 7, 2021
    Assignees: Neurolixis, Uniwersytet Jagiellonski Collegium Medicum
    Inventors: Anna Wesolowska, Magdalena Jastrzebska-Wiesek, Adrian Newman-Tancredi, Mark Andrew Varney
  • Patent number: 11178871
    Abstract: The present invention relates to the use of pyrimidine compounds of formula (I), or their agriculturally acceptable salts or derivatives as herbicides, wherein the variables are defined according to the description, specific pyrimidine compounds of formula (I), compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one pyrimidine compounds of the formula (I) to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: November 23, 2021
    Assignee: BASF SE
    Inventors: Florian Vogt, Matthias Witschel, Tobias Seiser, Veronica Lopez Carrillo, Thomas Seitz, Gerd Kraemer, Klaus Kreuz, Trevor William Newton, Klaus Reinhard, Doreen Schachtschabel
  • Patent number: 11147814
    Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.
    Type: Grant
    Filed: February 11, 2020
    Date of Patent: October 19, 2021
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Markus Ostermeier, Ulrike Werthmann
  • Patent number: 11149021
    Abstract: An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
    Type: Grant
    Filed: May 22, 2018
    Date of Patent: October 19, 2021
    Assignee: ABBISKO THERAPEUTICS CO., LTD.
    Inventors: Baowei Zhao, Mingming Zhang, Hongping Yu, Shuqun Yang, Zhui Chen, Yaochang Xu
  • Patent number: 11142505
    Abstract: Selected compounds, compositions, and methods for inhibiting BACE are presented that have relatively high selectivity towards APP via interaction of the inhibitor with both BACE and APP.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: October 12, 2021
    Assignee: The Regents of the University of California
    Inventors: Varghese John, Patricia Spilman, Barbara Jagodzinska
  • Patent number: 11129813
    Abstract: Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
    Type: Grant
    Filed: September 3, 2020
    Date of Patent: September 28, 2021
    Assignee: Frost Biologic, Inc.
    Inventor: Adam Siddiqui-Jain
  • Patent number: 11124520
    Abstract: The present invention provides a compound of Formula III, and salts thereof, and a pharmaceutical composition comprising a compound of Formula III: wherein R1 is selected from the group consisting of: wherein R2 is H or an alkyl group having from one to ten carbon atoms; R3 is H or an alkyl group having from one to ten carbon atoms; and R4 is H or an alkyl group having from one to ten carbon atoms. Methods of treating a patient with cancer with these compounds are also provided.
    Type: Grant
    Filed: December 4, 2019
    Date of Patent: September 21, 2021
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 11124495
    Abstract: The present invention provides novel compounds having the general formula (I): wherein R1, R2, R3, U, V, W, X and Y are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: September 21, 2021
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Zhanling Cheng, Jianhua Wang, Min Wang, Song Yang
  • Patent number: 11071731
    Abstract: Disclosed herein are compounds, of the class of amine-bearing heterocycles, which act as positive allosteric modulators and silent allosteric modulators of the mu opioid receptor. These compounds are useful for the treatment of pain, drug addiction, and other CNS derived maladies that are controlled directly or indirectly by activation of the mu opioid receptor. Methods for making and using the allosteric modulators disclosed herein are also provided.
    Type: Grant
    Filed: February 26, 2020
    Date of Patent: July 27, 2021
    Assignee: Chiromics, LLC
    Inventors: Joel Francis Austin, Michael David VanHeyst, James S. Harvey, Elizabeth Gerig Rowley, Christophe Lamarque-Lacoste
  • Patent number: 11053221
    Abstract: Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: July 6, 2021
    Assignee: ARRIEN PHARMACEUTICALS LLC
    Inventor: Hariprasad Vankayalapati
  • Patent number: 11053235
    Abstract: The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: July 6, 2021
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Gang Deng, Yimin Jiang, Qian Liu, Chao Liang, Zhao-Kui Wan, Wing Shun Cheung, Zhanling Cheng, Yanping Xu
  • Patent number: 11046680
    Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: June 29, 2021
    Assignee: AMGEN INC.
    Inventors: Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, James S. Harvey, Julie Anne Heath, Lars V. Heumann, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Frank Kayser, Aarif Yusuf Khakoo, David J. Kopecky, Su-Jen Lai, Zhihua Ma, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Malgorzata Wanska, Kevin Yang, Wen-Chen Yeh
  • Patent number: 11034678
    Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: June 15, 2021
    Assignee: Pfizer Inc.
    Inventors: Markus Boehm, Shawn Cabral, Matthew S. Dowling, Kentaro Futatsugi, Kim Huard, Esther Cheng Yin Lee, Allyn T. Londregan, Jana Polivkova, David A. Price, Qifang Li
  • Patent number: 11008339
    Abstract: Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.
    Type: Grant
    Filed: May 17, 2016
    Date of Patent: May 18, 2021
    Assignee: Shenyang Sinochem Agrochemicals R&D Co., Ltd.
    Inventors: Changling Liu, Aiying Guan, Junfeng Wang, Xufeng Sun, Zhinian Li, Jinbo Zhang, Lanfeng Ban, Sen Ma, Jie Lan, Xiaoli Xia, Jinlong Yang
  • Patent number: 10968172
    Abstract: The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: April 6, 2021
    Assignee: Mitobridge, Inc.
    Inventors: Arthur Kluge, Bharat Lagu, Pranab Maiti, Sunil Kumar Panigrahi
  • Patent number: 10954221
    Abstract: The present disclosure provides compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
    Type: Grant
    Filed: June 16, 2020
    Date of Patent: March 23, 2021
    Assignee: QILU REGOR THERAPEUTICS INC.
    Inventors: Wenge Zhong, Wei Guo
  • Patent number: 10946019
    Abstract: The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the symptoms of such diseases and therefore represent a new treatment modality for ameliorating chronic and acute conditions. The compounds of the invention are capable of selectively potentiating the activity of the Nurr1:RXR? heterodimer, and are able to treat diseases or conditions associated with aberrant Nurr1:RXR? function. The invention further provides methods for treating neurodegenerative disorders by administration of Nurr1:RXR? activating agents.
    Type: Grant
    Filed: October 20, 2016
    Date of Patent: March 16, 2021
    Inventor: Demetrios K. Vassilatis
  • Patent number: 10940144
    Abstract: The present invention aims to find a novel pharmaceutical use of omidenepag, esters thereof, or salts thereof. The present inventors have made intensive studies to find a novel pharmaceutical use of omidenepag, an ester thereof, or a salt thereof, and have found as a result that omidenepag, an ester thereof, or a salt thereof significantly dilates retinal blood vessels, and significantly increases blood flow. Therefore, omidenepag, an ester thereof, or a salt thereof is expected to protect retinal nerve cells and be useful for prevention and/or treatment of ophthalmic diseases involving retinal nerve cell disorder.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: March 9, 2021
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takazumi Taniguchi, Takahiro Akaishi, Hitoshi Nakazawa
  • Patent number: 10933064
    Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: March 2, 2021
    Assignees: Novartis AG, Palobiofarma S.L.
    Inventors: Kai Cui, Julio Cesar Castro-Palomino Laria, Weiyong Kong
  • Patent number: 10934284
    Abstract: Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: March 2, 2021
    Assignee: Wellstat Therapeutics Corporation
    Inventors: David M. Simpson, Dennis Bryan Zerby, Ming Lu, Reid W. Von Borstel, Rui Li, Julian Reading, Stephen Wolpe
  • Patent number: 10927136
    Abstract: The present patent application discloses the compounds according to Formula (I) shown below, or pharmaceutically acceptable salts thereof wherein JB, n, R1, R2, R3, R4, R5, m and X as defined herein.
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: February 23, 2021
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: James Edward Sheppeck, Paul Allan Renhowe, Ara Mermerian, Timothy Claude Barden, Glen Robert Rennie, Rajesh R. Iyengar, Takashi Nakai
  • Patent number: 10912763
    Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6?-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: February 9, 2021
    Assignee: Grünenthal GmbH
    Inventors: Nadja Gruening, Marc Schiller, Ashish Hemani, Chris Kirby, Ingo Friedrich, John Bothmer, Andreas Scholz
  • Patent number: 10912774
    Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
    Type: Grant
    Filed: December 17, 2019
    Date of Patent: February 9, 2021
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
  • Patent number: 10874673
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: December 29, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 10800775
    Abstract: The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: October 13, 2020
    Assignee: ACLARIS THERAPEUTICS, INC.
    Inventors: David Randolph Anderson, Susan Landis Hockerman, James Robert Blinn, Eric Jon Jacobsen
  • Patent number: 10787430
    Abstract: Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: September 29, 2020
    Assignee: FRONTHERA U.S. PHARMACEUTICALS LLC
    Inventors: Bohan Jin, Qing Dong, Gene Hung
  • Patent number: 10780091
    Abstract: The present invention relates to a maleate salt of a compound represented by formula I, a method for preparing the salt, a pharmaceutical composition containing the salt, and the use of the salt. The present invention also relates to crystalline forms C, D and E of the maleate salt of the compound represented by formula I, methods for preparing the crystalline forms, crystalline compositions and pharmaceutical compositions containing the crystalline forms, and uses thereof.
    Type: Grant
    Filed: February 4, 2017
    Date of Patent: September 22, 2020
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Zheng Wang, Ling Yang
  • Patent number: 10774070
    Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 15, 2020
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Natasja Brooijmans, Lucian V. DiPietro, Paul E. Fleming, Joseph L. Kim, Steven Mark Wenglowsky, Yulian Zhang
  • Patent number: 10759782
    Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: September 1, 2020
    Assignees: Jiangsu Hansoh Pharmaceutical Group Co., Ltd., Shanhgai Hansoh Biomecial Co., Ltd.
    Inventors: Zhongke Chen, Fuping Liu, Lei Liu, Rudi Bao
  • Patent number: 10752596
    Abstract: The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: August 25, 2020
    Assignee: JAPAN TOBACCO INC.
    Inventors: Hironobu Nagamori, Tatsuya Nishimaru, Masaki Takagi, Ikuo Mitani, Yuichi Nakagawa
  • Patent number: 10744138
    Abstract: A hair growth formulation includes minoxidil and foeniculum vulgare, atriplex nummularia extract, or a combination of foeniculum vulgare and atriplex nummularia extract. A method for increasing hair growth includes applying a hair growth formulation to a subject.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: August 18, 2020
    Assignee: GARUHDA LLC
    Inventor: David Ben Kunin
  • Patent number: 10736896
    Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: August 11, 2020
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
  • Patent number: 10716788
    Abstract: The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: July 21, 2020
    Assignee: Merck Patent GmbH
    Inventor: Tammy Dellovade
  • Patent number: 10709707
    Abstract: Described herein are methods and pharmaceutical formulations for treating ocular conditions.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: July 14, 2020
    Assignee: Oyster Point Pharma, Inc.
    Inventors: Douglas Michael Ackermann, James Loudin, Kenneth J. Mandell
  • Patent number: 10702525
    Abstract: The pyrimidine derivatives as anti-diabetic agents are chloropyrimidinyl derivatives having the general formula of compound 81, wherein R1 is —N(CH3)CH2CH2OH (compound 81c) or —N(H)CH2CH2OH (compound 81f) or the general formula of compound 82, wherein R2 is —N(CH3)CH2CH2OH (compound 82c) or —N(CH2CH2)2O (compound 82d), as follows: The derivatives may be used for treating diabetes in humans or animals and have demonstrated efficacy, specifically in treating type 2 diabetes. Two methods of synthesizing the pyrimidine derivatives are described herein. The method using microwaves (Method B) is a green method that can provide high yields in a short time and with high purity. The compounds act as GLP-1 receptor agonists and are more potent than conventional drugs. As such, the compounds may be used in lower doses, and, hence, have fewer side effects.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 7, 2020
    Assignee: United Arab Emirates University
    Inventors: Abdu Adem, Shaikha S. Al Neyadi, Ibrahim M. Abdu, Alaa A. Salem, Naheed Amir
  • Patent number: 10702589
    Abstract: The present disclosure provides the use of Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10 in methods and compositions for the treatment of neurological disorders and stress-induced conditions. Methods of increasing the levels of 5Thr3a on neuronal cells is also provided by contacting the neuronal cells with Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 7, 2020
    Assignee: ANN AND ROBERT H. LURIE CHILDREN'S HOSPITAL OF CHICAGO
    Inventor: Jhumku D. Kohtz
  • Patent number: 10702524
    Abstract: The present invention falls within the field of medical technology, and in particular relates to the use of a compound as shown in formula (I). In particular, the present invention relates to the use of the compound as shown in formula (I) in the preparation of a pharmaceutical composition for preventing and/or treating a nerve injury, or relieving a nerve injury-associated symptom, and further relates to the use thereof in the preparation of a healthcare product for protecting an injured nerve and/or improving motor function. After a nerve injury has occurred, the compound can reduce the production of pro-inflammatory cytokine, decrease the level of apoptosis, promote the survival of neuron, inhibit the formation of glial scar, and has a significant effect in promoting the recovery of motor function.
    Type: Grant
    Filed: October 10, 2017
    Date of Patent: July 7, 2020
    Inventors: Shiqing Feng, Xue Yao
  • Patent number: 10696666
    Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.
    Type: Grant
    Filed: October 18, 2017
    Date of Patent: June 30, 2020
    Assignee: CELLCENTRIC LIMITED
    Inventors: Neil Anthony Pegg, Stuart Thomas Onions, David Michel Adrien Taddei, Jonathan Shannon, Silvia Paoletta, Richard James Brown, Don Smyth, Gareth Harbottle
  • Patent number: RE48687
    Abstract: The present invention relates to pyridinylaminopyrimidine derivatives represented by the following formula (I), and pharmaceutically acceptable salts, preparation process and use thereof, wherein R1, R2, R3, R4, R5, m and A are defined as in the description. Pyridinylaminopyrimidine derivatives of the present invention can selectively inhibit the activity of mutant-type epidermal growth factor receptor (EGFR), have a good inhibition for the cancer cell proliferation, and therefore can be used as a therapeutic agent for treating tumors and relevant diseases.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: August 17, 2021
    Assignee: Shanghai Allist Pharmaceuticals Co., Ltd.
    Inventors: Huibing Luo, Huayong Zhou, Shuhui Wang, Yong Wu