Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
  • Patent number: 12129267
    Abstract: The present application provides heteroaryl amide compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
    Type: Grant
    Filed: January 6, 2020
    Date of Patent: October 29, 2024
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Neil Lajkiewicz, Wenqing Yao
  • Patent number: 11993604
    Abstract: A 1H-pyrazolo[4,3-H]quinazoline compound represented by formula (I) can be used for treating cell proliferation dysfunction, and is an broad-spectrum and strongly-active inhibitor for a cell cyclin-dependent kinase (CDK).
    Type: Grant
    Filed: April 1, 2022
    Date of Patent: May 28, 2024
    Assignee: SHENGKE PHARMACEUTICALS (JIANGSU) LTD.
    Inventors: Bin Liu, Hang Cheng, Weiyan Xiong, Chenggang Zhang, Chengzhi Yu
  • Patent number: 11981679
    Abstract: The present disclosure relates to a series of tricyclic compounds, their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The disclosure also relates to process of preparation of these tricyclic compounds of Formula I. These compounds are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor. The disclosure also relates to the process of preparation of the tricyclic compounds, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 9, 2022
    Date of Patent: May 14, 2024
    Assignee: IMPETIS BIOSCIENCES LTD.
    Inventors: Sujay Basu, Sachin Thorat, Yogesh Shejul, Anil Panmand, Meena Patel, Goraksha Khose, Rajesh Bonagiri, Dinesh Barawkar, Bheemashankar Kulkarni, Kasim Mookhtiar
  • Patent number: 11964981
    Abstract: Pyrimido[4,5-b]indole compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrimido[4,5-b]indole compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
    Type: Grant
    Filed: September 18, 2023
    Date of Patent: April 23, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Michelyne Haroun, Christophe Tratrat
  • Patent number: 11939335
    Abstract: Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.
    Type: Grant
    Filed: May 19, 2023
    Date of Patent: March 26, 2024
    Assignee: 858 THERAPEUTICS, INC.
    Inventors: James M. Veal, Jeffrey A. Stafford, Donald S. Karanewsky, Shyama Herath
  • Patent number: 11759467
    Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: November 16, 2020
    Date of Patent: September 19, 2023
    Assignee: VERONA PHARMA PLC
    Inventors: Katharine Abbott-Banner, John Hanrahan, David Thomas
  • Patent number: 11518766
    Abstract: A compound represented by formula (I), an optical isomer thereof and a pharmaceutically acceptable salt thereof, as well as an application of said compound as an FXIa inhibitor.
    Type: Grant
    Filed: June 28, 2020
    Date of Patent: December 6, 2022
    Assignees: SHANGHAI JEMINCARE PHARMACEUTICALS CO., LTD., JIANGXI JEMINCARE GROUP CO., LTD.
    Inventors: Shuchun Guo, Jiangwei Wang, Shan Yao, Yong Zhang, Zhangping Kang, Qiong Zhang, Yan Ye, Jianbiao Peng, Haibing Guo
  • Patent number: 11465963
    Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: October 11, 2022
    Assignee: BIOGEN MA INC.
    Inventors: Andrew George Capacci, Edward Yin Shiang Lin, Brian Stuart Lucas
  • Patent number: 11447494
    Abstract: The present application provides tricyclic amine compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), of Formula (I): as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: September 20, 2022
    Assignee: Incyte Corporation
    Inventors: Qinda Ye, Ken Mukai, Liangxing Wu, Wenqing Yao
  • Patent number: 11440916
    Abstract: The present invention relates to a selective A2A receptor antagonist, and in particular to a selective A2A receptor antagonist of Formula (I), a pharmaceutical composition comprising the antagonist, use of the antagonist in manufacturing a medicament and in treatment of a disease: wherein the groups in Formula (I) are defined as in the specification.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: September 13, 2022
    Assignee: INXMED (NANJING) CO., LTD.
    Inventors: Zaiqi Wang, Lihu Yang
  • Patent number: 11407758
    Abstract: The present disclosure relates to a series of tricyclic compounds, their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The disclosure also relates to process of preparation of these tricyclic compounds of Formula I. These compounds are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor. The disclosure also relates to the process of preparation of the tricyclic compounds, and to pharmaceutical compositions containing them. Formula (I) wherein D represents a tricyclic ring system selected from: Formula (II) or Formula (III).
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: August 9, 2022
    Assignee: IMPETIS BIOSCIENCES LTD.
    Inventors: Sujay Basu, Sachin Thorat, Yogesh Shejul, Anil Panmand, Meena Patel, Goraksha Khose, Rajesh Bonagiri, Dinesh Barawkar, Bheemashankar Kulkarni, Kasim Mookhtiar
  • Patent number: 11384083
    Abstract: The present application provides pyrrolo[2,3-d]pyrimidinone inhibitors of cyclin-dependent kinase 2 (CDK2) of Formula (I): as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: July 12, 2022
    Assignee: Incyte Corporation
    Inventors: Alexander Sokolsky, Sarah Winterton, Liangxing Wu, Wenqing Yao
  • Patent number: 11319323
    Abstract: A 1H-pyrazolo[4,3-H]quinazoline compound represented by formula (I) can be used for treating cell proliferation dysfunction, and is an broad-spectrum and strongly-active inhibitor for a cell cyclin-dependent kinase (CDK).
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: May 3, 2022
    Inventors: Bin Liu, Hang Cheng, Weiyan Xiong, Chenggang Zhang, Chengzhi Yu
  • Patent number: 11266648
    Abstract: The present invention provides, inter alia, compounds of general formula (I) capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.
    Type: Grant
    Filed: April 27, 2020
    Date of Patent: March 8, 2022
    Assignee: ImmuneTarget, Inc.
    Inventors: Samedy Ouk, Hsiou-Chi Liou
  • Patent number: 11117901
    Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 3, 2018
    Date of Patent: September 14, 2021
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Alessandra Badari, Elena Casale, Marcella Nesi, Francesca Quartieri
  • Patent number: 11026948
    Abstract: A compound of formula I or a pharmaceutically acceptable salt or ester thereof is provided for the treatment of cancer wherein (i) the cancer is one that has the characteristic of being a type prone to being or becoming refractory or resistant to platinum drug based therapy and (ii) the treatment is with a dose of between 1 mg/m2 and 30 mg/m2 of compound per patient body surface area per administration. Method of treatment and novel dosage forms are also provided. Particularly treated arc ovarian cancers, particularly those expressing a-folate receptors, including epithelial ovarian, fallopian tube or peritoneal cancer.
    Type: Grant
    Filed: March 5, 2020
    Date of Patent: June 8, 2021
    Assignee: BTG INTERNATIONAL LIMITED
    Inventor: Udai Banerji
  • Patent number: 11001595
    Abstract: The present invention discloses a compound of the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: August 11, 2020
    Date of Patent: May 11, 2021
    Assignee: Duquesne University of The Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10961253
    Abstract: Disclosed herein are pyrido[3?,2?:4,5]thieno[3,2-d]pyrimidine and pyrimido[4?,5?:4,5]thieno[2,3-c]pyridazine compounds, which may be useful as positive allostenc modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: March 30, 2021
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, Darren W. Engers, P. Jeffrey Conn, Katrina A. Bollinger, Rory Capstick, Paul Spearing, Sean R. Bollinger
  • Patent number: 10864213
    Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: December 15, 2020
    Assignee: VERONA PHARMA PLC
    Inventors: Katharine Abbott-Banner, John Hanrahan, David Thomas
  • Patent number: 10861630
    Abstract: An inductor includes a body having a first magnetic portion above and below a coil, and a second magnetic portion above and below the first magnetic portion. The magnetic flux density of the magnetic substance in the first magnetic portion is higher than that of the magnetic substance in the second magnetic portion.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: December 8, 2020
    Assignee: SAMSUNG ELECTRO-MECHANICS CO., LTD.
    Inventors: Han Wool Ryu, Jung Hyuk Jung, Hyo Chan Oh, Yoon Hee Kim, Woon Chul Choi, Jin Ho Ku, Il Jin Park
  • Patent number: 10763438
    Abstract: There is provided a material comprising a n-doped electrically conductive polymer comprising at least one electron-deficient aromatic moiety, each electron-deficient aromatic moiety having a gas-phase electron affinity (EA) of 1-3 eV; and at least one counter-cation covalently bonded to the polymer or to a further polymer comprised in the material, the polymer being n-doped to a charge density of 0.1-1 electron per electron-deficient aromatic moiety, the polymer being capable of forming a layer having a vacuum workfunction (WF) of 2.5-4.5 eV, and wherein all the counter-cations comprised in the material are immobilised such that any electron in the polymer cannot significantly diffuse or migrate out of the polymer. There is also provided a method of preparing the material.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: September 1, 2020
    Assignee: National University of Singapore
    Inventors: Lay-Lay Chua, Peter Kian-Hoon Ho, Rui-Qi Png, Mervin Chun-Yi Ang, Kim-Kian Choo, Cindy Guan-Yu Tang
  • Patent number: 10696675
    Abstract: A novel imidazopyridine derivative compound and uses thereof are disclosed.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: June 30, 2020
    Assignee: HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Moon Sub Lee, Eun Young Byun, Ji Sook Kim, Won Jeoung Kim, Nam Du Kim, Seung Hyun Jung, Young Gil Ahn
  • Patent number: 10688191
    Abstract: A therapeutic method and composition which includes a cannabinoid chemically linked to a chemotherapy agent. The therapeutic composition is capable of crossing the blood-brain barrier, and delivery of the composition across the blood-brain barrier provides both chemotherapy for the treatment of brain cancer and alleviation of side effects caused by the chemotherapy agent. Once across the blood-brain barrier, the chemotherapy agent will be released to attack cancer cells, and the cannabinoid will be free to bind to cannabinoid receptors in the brain to alleviate side effects of chemotherapy such as nausea/vomiting, pain and decreased appetite.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: June 23, 2020
    Assignee: HR BIOMED, LLC
    Inventor: Heidi Rowles
  • Patent number: 10676483
    Abstract: A method of treating a patient having cancer is provided comprising administering a therapeutically effective amount of a tricyclic compound or a pharmaceutically acceptable salt of the tricyclic compound to a patient. A method of inhibiting the mitosis of a cancerous cell is also provided.
    Type: Grant
    Filed: September 25, 2019
    Date of Patent: June 9, 2020
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10654868
    Abstract: Provided is a dihydropyrazole azepine compound serving as an Akt inhibitor; specifically disclosed is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: May 19, 2020
    Assignee: HARBIN ZHENBAO PHARMACEUTICAL CO., LTD.
    Inventors: Lun Lu, Zhibo Zhang, Gang Li, Lihong Hu, Charles Z. Ding, Shuhui Chen
  • Patent number: 10611779
    Abstract: The invention relates to novel compounds of the formula (I) in which Q, Aa, Ab, Ac, Ad, R1 and n have the definitions given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: April 7, 2020
    Assignees: Bayer CropScience Aktiengesellschaft, Bayer Aktiengesellschaft
    Inventors: Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Nina Kausch-Busies, Marc Mosrin, David Wilcke, Matthieu Willot, Kerstin Ilg, Ulrich Goergens, Andreas Turberg
  • Patent number: 10487092
    Abstract: The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, inflammatory disease and disease associated with inflammatory pain, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: November 26, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Anja Giese, Ulrich Klar, Keith Graham, Georg Kettschau, Detlev Sülzle, Philip Lienau, Kirstin Petersen, Julien LeFranc, Nicole Schmidt
  • Patent number: 10471005
    Abstract: Present invention relates to a low dose pharmaceutical composition, preferably oral composition comprising therapeutically effective amount of [(2-hydroxy-4-oxo-6,7,8,9-tetrahydro-4H,5H-10-thia-1,4a-diaza-benzo[a]azulene-3-carbonyl)-amino]-acetic acid (compound A) in the range of 2.5 mg to 60 mg. Present invention also relates to a method of treating inflammatory bowel disease in a mammal by administrating said low dose pharmaceutical composition. Further, present invention relates to a use of the compound A for the preparation of low dose pharmaceutical composition for the treatment of inflammatory bowel disease in a mammal.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: November 12, 2019
    Assignee: Torrent Pharmaceuticals Limited
    Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ram Gupta, Shitalkumar Zambad, Shailesh Deshpande, Jignesh Kotecha, Ramesh Gupta, Sanjay Srivastava, Laxmikant Chhipa, Jaya Abraham
  • Patent number: 10414769
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups A, R and q are defined in claim 1, their use as inhibitors of IGF-1R, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: September 17, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Treu, Stephan Karl Zahn
  • Patent number: 10357508
    Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 23, 2019
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 10253044
    Abstract: The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: April 9, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Yujun Zhao, Bing Zhou, Angelo Aguilar, Liu Liu, Longchuan Bai, Donna McEachern, Duxin Sun, Bo Wen, Ruijuan Luo, Ting Zhao, Arul Chinnaiyan, Irfan A. Asangani, Jeanne Stuckey, Jennifer Lynn Meagher, Xu Ran, Yang Hu
  • Patent number: 10226464
    Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: March 12, 2019
    Assignee: ImmuneTarget, Inc.
    Inventors: Samedy Ouk, Hsiou-Chi Liou
  • Patent number: 10179790
    Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: January 15, 2019
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Sylvain Jacques, Evert Homan, Thomas Helleday
  • Patent number: 10166271
    Abstract: This disclosure reveals that cyclic corticotrophin releasing factor (CRF) antagonist peptides (such as astressin B, its functional fragments, and their derivatives) induce hair growth and prevent hair loss in vivo. This important discovery enables, for instance, methods of promoting hair growth, and methods of treating hair loss (such as the hair loss that occurs normally in some individuals or that is the result of a health disorder or therapeutic treatment). Exemplary cyclic CRF antagonist peptides useful in the disclosed methods are provided throughout the disclosure.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: January 1, 2019
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SALK INSTITUTE FOR BIOLOGICAL STUDIES
    Inventors: Million Mulugeta, Lixin Wang, Yvette Taché, Jean Rivier
  • Patent number: 10149852
    Abstract: The present disclosure describes the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogs/derivatives as well as their acceptable salts, for treating neuropathic pain resulting from chemotherapy. Methods, compositions, dose units and dose forms of tetrodotoxin related to the use are described.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: December 11, 2018
    Assignee: WEX PHARMACEUTICALS INC.
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens, Susan Lu, Donald Wong, Walter Korz
  • Patent number: 10085991
    Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 2, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lei Zhu, Yvonne Cegielnik, Qun Lu
  • Patent number: 10005789
    Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: June 26, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Patent number: 9981921
    Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: May 29, 2018
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, David P. Reed
  • Patent number: 9968574
    Abstract: The present invention provides, among other things, therapeutic compositions and methods that can effectively treat, slow or prevent a neurological disease (e.g., a neurodegenerative disease, e.g., mild cognitive impairment (MCI) or Alzheimer's disease (AD)), in particular, based on therapeutically effective amount of nifedipine, oxidized or nitroso nifedipine derivatives, lactam (e.g., a compound of formula (Ic) or (Ic-i), e.g., NFD-L1), thyroxine (T4), triiodothyronine (T3) and combinations thereof.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: May 15, 2018
    Assignee: The University of Kentucky Research Foundation
    Inventors: Mark Lovell, Bert Lynn
  • Patent number: 9896455
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Grant
    Filed: August 22, 2016
    Date of Patent: February 20, 2018
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9802955
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: October 31, 2017
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9790234
    Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: October 17, 2017
    Assignee: NIMBUS IRIS, INC.
    Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
  • Patent number: 9717903
    Abstract: Methods to restore and/or improve the libido, the sex drive, in males and females, without introducing any external unnatural drugs. The process utilizes a TENS/EMS (Transcutaneous Electrical Nerve Stimulation/Electronic Muscle Stimulation) machine to naturally generate the increased production by the human body's nerve fiber's neurotransmitters.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: August 1, 2017
    Inventor: Gary Barrett
  • Patent number: 9708332
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: July 18, 2017
    Assignee: MEDIVIR AB
    Inventors: Claudio Sturino, Teddy Halmos, Anne Decor, Martin Duplessis, Patrick Deroy, Araz Jakalian, Louis Morency, Cyrille Kuhn, Chantal Grand-Maitre, Martin Tremblay, Christian Brochu
  • Patent number: 9695135
    Abstract: The invention provides compounds of formula I: and salts thereof wherein R1-R4 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: July 4, 2017
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Eddy Arnold, Joseph D. Bauman, John E. Kerrigan, Ajit K. Parhi, Kalyan Das, Cody Kelley, Dishaben V. Patel
  • Patent number: 9649302
    Abstract: The present disclosure relates to pharmaceutical compositions useful for (and to a method of) treating autoimmune, respiratory and/or inflammatory diseases and conditions. The method involves administering to a subject in need thereof roflumilast N-oxide by inhalation. The present disclosure particularly relates to the treatment of asthma and chronic obstructive pulmonary disease (COPD) by administering roflumilast N-oxide by inhalation.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: May 16, 2017
    Assignee: INCOZEN THERAPEUTICS PVT. LTD.
    Inventor: Swaroop K. Vakkalanka
  • Patent number: 9636342
    Abstract: The invention provides a method for treating prostate cancer in a subject comprising administering to the subject an effective amount of a selective inhibitor of one or more of CDK8 and CDK19. In some embodiments the inhibitor inhibits CDK19. In some embodiments, the inhibitor inhibits CDK8 at a Kd of lower than 200 nM and/or inhibits CDK19 at a Kd of lower than 100 nM. In some embodiments, the prostate cancer is androgen independent. In some embodiments, the prostate cancer is androgen independent due to one or more of androgen receptor gene amplification, androgen receptor gene mutation, ligand-independent transactivation of androgen receptor and activation of intracellular androgen synthesis. In some embodiments, the inhibitor inhibits increased activity of NF-?B. In some embodiments, the inhibitor does not inhibit increased basal levels of NF-?B. In some embodiments, inhibition of one or more genes by AR is not inhibited.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: May 2, 2017
    Assignee: University of South Carolina
    Inventors: Mengqian Chen, Igor Roninson
  • Patent number: 9604937
    Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: March 28, 2017
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Thomas Helleday, Tobias Koolmeister, Sylvain Jacques
  • Patent number: 9585885
    Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 7, 2017
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Nishimura, Yasunori Ueno, Kiyoshi Kasai, Masako Yoshida
  • Patent number: RE49873
    Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).
    Type: Grant
    Filed: July 22, 2021
    Date of Patent: March 19, 2024
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen