Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
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Patent number: 10793551Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, Y1, Y2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification. The inventive Formula I and Formula II compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.Type: GrantFiled: October 17, 2018Date of Patent: October 6, 2020Assignee: eFFECTOR Therapeutics Inc.Inventors: Justin T. Ernst, Siegfried H. Reich, Paul A. Sprengeler, Alan X. Xiang
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Patent number: 10774080Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.Type: GrantFiled: January 8, 2020Date of Patent: September 15, 2020Assignee: Theravance Biopharma R&D IP, LLCInventors: Jennifer Kozak, Ryan Hudson
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Patent number: 10765677Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.Type: GrantFiled: June 7, 2019Date of Patent: September 8, 2020Assignee: ForSight Vision4, Inc.Inventors: Judit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
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Patent number: 10738035Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y—Z-L-R1??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: May 12, 2016Date of Patent: August 11, 2020Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Wei Li, Hui Cao, Meizhong Jin, Xuri Gao, Xiaowen Peng, Jorden Kass, Yat Sun Or
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Patent number: 10730859Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.Type: GrantFiled: November 5, 2014Date of Patent: August 4, 2020Assignee: Laurus Labs LimitedInventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Durga Prasad Kuchipudi
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Patent number: 10722512Abstract: The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatment of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.Type: GrantFiled: June 22, 2016Date of Patent: July 28, 2020Assignee: Acetylon Pharmaceuticals, Inc.Inventors: David Lee Tamang, Min Yang, Simon S. Jones
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Patent number: 10717725Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: GrantFiled: December 6, 2018Date of Patent: July 21, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Elizabeth Anne Jurica, Zhenqiu Hong
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Patent number: 10709705Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.Type: GrantFiled: August 28, 2017Date of Patent: July 14, 2020Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Jianyong Chen
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Patent number: 10710979Abstract: The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.Type: GrantFiled: July 11, 2016Date of Patent: July 14, 2020Assignee: ZHEJIANG BOSSAN PHARMACEUTICAL CO. LTD.Inventors: Dawei Ma, Qiang Yu, Junying Yuan, Hongguang Xia, Dongpo Cai, Kailiang Wang, Chen Zhang, Shanghua Xia
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Patent number: 10710983Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.Type: GrantFiled: June 26, 2017Date of Patent: July 14, 2020Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
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Patent number: 10702527Abstract: The present disclosure provides combination therapy of a transcription inhibitor and a kinase inhibitor. The combination of the transcription inhibitor and the kinase inhibitor may be useful in treating and/or preventing in a subject a proliferative disease, such as proliferative a disease that is resistant to the transcription inhibitor alone or the kinase inhibitor alone. In certain embodiments, the proliferative disease is a cancer. The combination of the transcription inhibitor and the kinase inhibitor is expected to be synergistic.Type: GrantFiled: June 10, 2016Date of Patent: July 7, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Peter Hammerman, Kwok-kin Wong, Nathanael S. Gray
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Patent number: 10682352Abstract: Provided in the present invention are a compound having the effects of preventing and treating diseases related to IDH mutation, and a preparation method and use thereof.Type: GrantFiled: March 21, 2017Date of Patent: June 16, 2020Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Lei Jiang, Meiyu Geng, Qiangang Zheng, Min Huang, Huixin Wan, Shuai Tang, Xianlei Fu, Xiaojing Lan, Jianhua Cao, Feifei Liu, Jian Ding
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Patent number: 10662186Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.Type: GrantFiled: December 30, 2016Date of Patent: May 26, 2020Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
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Patent number: 10647686Abstract: The present invention relates to compounds represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is chloro or methyl; R2 is hydrogen or chloro; R3 is hydrogen, fluoro, chloro, bromo, methyl, ethyl, isopropyl, pentyl, hexyl, octyl, methoxy, phenoxy, (4-nitrophenyl)sulfonyl, piperidin-4-yl, or piperazin-1-yl; R4 is hydrogen, chloro, methyl or trifluoromethyl, phenoxy, (4-nitrophenyl)sulfonyl or piperidin-4-yl; or R3 and R4, together with the carbons to which they are attached, form a fused ring selected form the group consisting of: n is 1 or 2. These compounds according to the present invention remarkably inhibits activity of DRAK that inhibits signal systems of TGF-?, which is known to suppress cancer growth, and thus the novel pyrimidine compounds can be used as a pharmaceutical composition for preventing or treating cancer and can be used as a pharmaceutical composition for preventing or treating inflammatory disease.Type: GrantFiled: November 1, 2017Date of Patent: May 12, 2020Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Kwangho Lee, Gildon Choi, Na Ri Lee, Sang Jun Park, Myoung Eun Jung, Seong Jin Kim, Kyung-Min Yang, Jihee Lee
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Patent number: 10633413Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminosterol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.Type: GrantFiled: July 13, 2018Date of Patent: April 28, 2020Assignee: ENTERIN, INC.Inventor: Michael Zasloff
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Patent number: 10632192Abstract: The present invention provides a compound of the formula (1): wherein X, R1, R2, R3, R4, R5, R6, Y1, Y2, L, and m are as defined in the description, and a pharmaceutically acceptable salt thereof, which are useful as a vaccine adjuvant.Type: GrantFiled: October 6, 2016Date of Patent: April 28, 2020Assignee: Sumitomo Dainippon Pharma Co., Ltd.Inventors: Hidenori Kimura, Hitoshi Ban, Yoshiaki Isobe, Hitoshi Watanabe
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Patent number: 10632120Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.Type: GrantFiled: August 26, 2019Date of Patent: April 28, 2020Assignee: Emory UniversityInventors: Michael G. Natchus, Richard Arrendale, Dennis Liotta, Ketan Desai, Hyunsuk Shim
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Patent number: 10618887Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.Type: GrantFiled: March 5, 2018Date of Patent: April 14, 2020Assignees: Sunesis Pharmaceuticals, Inc., Biogen MA Inc.Inventors: Brian T. Hopkins, Timothy R. Chan, Tracy J. Jenkins, Patrick Conlon, Xiongwei Cai, Michael Humora, Xianglin Shi, Ross A. Miller, Andrew Thompson
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Patent number: 10570122Abstract: The present invention relates to compounds of general formula (I). wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.Type: GrantFiled: February 5, 2016Date of Patent: February 25, 2020Assignee: AB ScienceInventors: Alain Moussy, Abdellah Benjahad, Didier Pez, Franck Sandrinelli, Jason Martin, Willy Picoul, Emmanuel Chevenier
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Patent number: 10562894Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.Type: GrantFiled: April 22, 2019Date of Patent: February 18, 2020Assignee: Theravance Biopharma R&D IP, LLCInventors: Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell
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Patent number: 10537574Abstract: This disclosure relates to the use of kinase inhibitor to treat or prevent infectious diseases such as tuberculosis. In certain embodiments, this disclosure relates to treating or preventing an infectious disease comprising administering an effective amount of a kinase inhibitor or other compound disclosed herein to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing tuberculosis comprising administering a kinase inhibitor to a subject in need thereof. In certain embodiments, the subject is diagnosed with Mycobacterium tuberculosis (Mtb) that is resistant to multiple antibiotic agents.Type: GrantFiled: September 16, 2016Date of Patent: January 21, 2020Assignee: Emory UniversityInventor: Daniel Kalman
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Patent number: 10527633Abstract: Use of prostacyclin or an analogue thereof for treatment of a new medical indication in acute critically ill patients, in particular acute critically ill patients with systemic endothelial damage, a biomarker for identifying individuals that have a new medical indication, and a method for identifying a new medical indication.Type: GrantFiled: March 22, 2016Date of Patent: January 7, 2020Assignee: ENDOTHEL PHARMA APSInventors: Sisse Rye Ostrowski, Pär Ingemar Johansson
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Patent number: 10526345Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.Type: GrantFiled: April 4, 2017Date of Patent: January 7, 2020Assignee: MANKIND PHARMA LTD.Inventors: Rakesh Ishwar Patil, Jeevan Verma, Dharmesh Shah, Sazid Ali, Srinivasa Reddy Bapuram, Santosh Kumar Rai, Anil Kumar
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Patent number: 10519107Abstract: The present disclosure relates to compounds having the Formula (Formula (I)) which are inhibitors of STAT5.Type: GrantFiled: May 29, 2015Date of Patent: December 31, 2019Assignee: The Governing Council of the University of TorontoInventors: Patrick Thomas Gunning, Abbarna A. Cumaraswamy, Andrew Martin Lewis, Mulu Geletu-Heye
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Patent number: 10519135Abstract: The present invention provides novel compounds of Formula (I) and Formula (II) 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 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.Type: GrantFiled: July 10, 2018Date of Patent: December 31, 2019Assignee: Syros Pharmaceuticals, Inc.Inventors: Kevin Sprott, Jason J. Marineau, Darby Schmidt, Michael Bradley, Stephane Ciblat, M. Arshad Siddiqui, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Stephanie Roy, Dana K. Winter, Tom Miller, Amy Ripka, Dansu Li
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Patent number: 10519169Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: August 3, 2016Date of Patent: December 31, 2019Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 10501461Abstract: Tyrosine amide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).Type: GrantFiled: January 30, 2018Date of Patent: December 10, 2019Assignee: CHIESI FARMACEUTICI S.P.A.Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay, Arnaud Jean Francois Auguste Cheguillaume
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Patent number: 10494378Abstract: Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.Type: GrantFiled: July 21, 2016Date of Patent: December 3, 2019Assignee: GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.Inventors: Zusheng Xu, Nong Zhang, Tinghan Wang, Qingrui Sun, Yuguang Wang
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Patent number: 10479785Abstract: A novel class of inhibitors of protein kinases that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of CDK4, CDK6 and/or cyclin D, including certain cancers of lung, breast, brain, central nervous system, colorectal cancer and leukaemias.Type: GrantFiled: August 4, 2016Date of Patent: November 19, 2019Assignee: AUCENTRA THERAPEUTICS PTY LTDInventors: Shudong Wang, Solomon Tadesse Zeleke, Mingfeng Yu
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Patent number: 10463641Abstract: The disclosure includes a method of inducing direct reprogramming (transdifferentiation) into non-oncogenic cells accompanied by tumor cell apoptosis in human tumor cells using a small molecule composition, based on the mechanism of chemical-induction of direct cellular reprogramming. The disclosure also includes a small molecule composition used for the method, and culture media and agents prepared from the composition.Type: GrantFiled: November 30, 2016Date of Patent: November 5, 2019Assignee: Transcend Cytotherapy Co., LtdInventors: Pei-Lin Zhang, Hong-Yang Wang
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Patent number: 10464927Abstract: The present disclosure relates to a 2,4-disubstituted pyrimidine derivative and the use thereof as a therapeutically effective cyclin-dependent kinase (CDK) inhibitor. In particular, the present disclosure relates to the use of a new 2,4-disubstituted pyrimidine derivatives shown in formula (I) and a pharmaceutical composition thereof as a selective CDK4/6 inhibitor in preventing or treating diseases related to CDK4/6.Type: GrantFiled: October 9, 2018Date of Patent: November 5, 2019Assignee: Shanghai Xunhe Pharmaceutical Technology Co. Ltd.Inventors: Yongyong Zheng, Hua Jin, Feng Zhou, Meihua Huang, Xin Meng
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Geminal substituted aminobenzisoxazole compounds as agonists of ?7-nicotinic acetylcholine receptors
Patent number: 10428062Abstract: The present invention relates to novel geminal substituted aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ?7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.Type: GrantFiled: August 10, 2016Date of Patent: October 1, 2019Assignee: Axovant Sciences GmbHInventors: Raksha Acharya, Duane A. Burnett, Matthew Gregory Bursavich, Andrew Simon Cook, Bryce Alden Harrison, Andrew J. McRiner -
Patent number: 10420761Abstract: The current invention is directed to a class of compounds that inhibit the function of Thymidylate synthase. Thymidylate synthase inhibition was noted to result in inhibition of tumor cell grow and killing of tumor cells. Thymidylate synthase inhibition is, thus, useful for treatment of various types of cancers, including but not limited to, acute lymphoblatic leukemia (ALL), acute myelogenous leukemia (AML), acute promyelocytic leukemia, chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML), acute monocytic leukemia (AMOL), hairy cell leukemia, large cell immunoblastic lymphoma, plasmacytoma, multiple myeloma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, leukemia, brain cancer, lung cancer, central nervous system (CNS) cancer, melanoma, renal cancer, prostate cancer, colon cancer, ovarian cancer and breast cancer. The compounds disclosed herein can be used alone or in combination with other cancer treatment regimens (e.g.Type: GrantFiled: March 17, 2014Date of Patent: September 24, 2019Assignee: University of Florida Research Foundation, Inc.Inventors: Maria Zajac-Kaye, Lidia Kulemina
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Patent number: 10385342Abstract: The present invention relates to oligomeric compounds and conjugates thereof that target Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) PCSK9 mRNA in a cell, leading to reduced expression of PCSK9. Reduction of PCSK9 expression is beneficial for a range of medical disorders, such as hypercholesterolemia and related disorders.Type: GrantFiled: May 4, 2018Date of Patent: August 20, 2019Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Nanna Albæk, Maj Hedtjärn, Marie Wickstrom Lindholm, Niels Fisker Nielsen, Andreas Petri, Jacob Ravn
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Patent number: 10370341Abstract: The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.Type: GrantFiled: September 28, 2018Date of Patent: August 6, 2019Assignee: NEOCULI PTY LTDInventors: Stephen Page, Sanjay Garg, Martine Keenan, Adam McCluskey, Andrew Stevens
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Patent number: 10369129Abstract: Disclosed herein is a long acting pharmaceutical composition for treating or preventing human immunodeficiency virus (HIV) infection. The pharmaceutical composition comprises a suspension of a lysine-based aspartyl protease inhibitor or salt thereof, a surface modifier, and a pharmaceutically acceptable carrier; wherein the lysine-based aspartyl protease inhibitor or salt thereof has an average effective particle size of less than about 500 nm. A method for treating or preventing HIV infection with the pharmaceutical composition is also disclosed.Type: GrantFiled: May 31, 2016Date of Patent: August 6, 2019Assignee: TaiMed Biologics, Inc.Inventors: James Nienyuan Chang, Hsiang-Fa Liang, Meng-Hsin Chen, Kuei-Ling Kuo, An-Chieh Li
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Patent number: 10363255Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.Type: GrantFiled: January 25, 2018Date of Patent: July 30, 2019Assignee: FORSIGHT VISION4, INC.Inventors: Judit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
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Patent number: 10350195Abstract: Compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, disclosed are combined therapies that modulate synapse function for treating the disease.Type: GrantFiled: November 30, 2015Date of Patent: July 16, 2019Assignee: PharnextInventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Nathalie Cholet
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Patent number: 10351560Abstract: The invention relates to a crystalline form of (S)-2-(8-((5-chloropyrimidin-2-yl)(methyl)amino)-2-fluoro-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as CRTH2 receptor modulators.Type: GrantFiled: September 14, 2016Date of Patent: July 16, 2019Assignee: IDORSIA PHARMACEUTICALS LTDInventors: Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist, Markus Von Raumer
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Patent number: 10342766Abstract: Derivatives of 6-shogaol are described herein. Also described herein are methods of preparing the derivatives, as well as methods of using the derivatives to activate Nrf2 and to treat diseases associated with inflammation and/or oxidative stress.Type: GrantFiled: March 23, 2018Date of Patent: July 9, 2019Assignees: North Carolina Agricultural and Technical State University, North Carolina Central UniversityInventors: Shengmin Sang, Yingdong Zhu, TinChung Leung
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Patent number: 10329261Abstract: A method of preparing 6-chloro-5-nitro-2,4-diaminopyrimidine includes: reacting guanidine hydrochloride with ethyl carbamoylacetate and sodium hypochlorite in the presence of a metal nitrate salt and acetate anhydride in an organic solvent.Type: GrantFiled: July 18, 2018Date of Patent: June 25, 2019Assignee: XI'AN TAIKOMED PHARMACEUTICAL TECHNOLOGY CO., LTD.Inventors: Yonghong Tang, Minghui Chang, Chengyuan Liang, Danni Tian, Juan Xia, Kaiqi Shi, Han Li, Xuechuan Wang
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Patent number: 10329278Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.Type: GrantFiled: June 18, 2018Date of Patent: June 25, 2019Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Benjamin Gerald Tehan, Barry John Teobald
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Patent number: 10308646Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.Type: GrantFiled: October 26, 2018Date of Patent: June 4, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell, Marta Dabros, Jerry Nzerem
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Patent number: 10301260Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: GrantFiled: May 6, 2015Date of Patent: May 28, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Bruce A. Ellsworth, Elizabeth A. Jurica
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Patent number: 10287253Abstract: The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of viral infections and cancers.Type: GrantFiled: December 4, 2017Date of Patent: May 14, 2019Assignee: APROS THERAPEUTICS, INC.Inventor: Tom Yao-Hsiang Wu
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Patent number: 10280154Abstract: Provided are a pyrimidine compound represented by Formula 1, a method of preparing the same, and a pharmaceutical use of the pyrimidine compound for the prevention or treatment of cancer.Type: GrantFiled: September 11, 2018Date of Patent: May 7, 2019Assignee: HANMI PHARM. CO., LTD.Inventors: Young Jin Ham, Seok Jong Kang, Jae Yul Choi, Seo Hee Kim, Tae Woo Kim, In Hwan Bae, Young Gil Ahn, Kwee Hyun Suh
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Patent number: 10272084Abstract: Disclosed are methods for treating cisplatin-induced peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a histone deacetylase 6 selective inhibitor.Type: GrantFiled: June 1, 2016Date of Patent: April 30, 2019Assignees: Regenacy Pharmaceuticals, LLC, Board of Regents, The University of Texas SystemInventors: Annemieke Kavelaars, Cobi J. Heijnen, Karen Krukowski, Matthew B. Jarpe
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Patent number: 10266521Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.Type: GrantFiled: January 4, 2018Date of Patent: April 23, 2019Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
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Patent number: 10233178Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: GrantFiled: June 15, 2017Date of Patent: March 19, 2019Assignee: Oryzon Genomics, S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez De La Cuesta, Maria de los Ángeles Estiarte Martinez
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Patent number: 10213511Abstract: The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.Type: GrantFiled: March 2, 2017Date of Patent: February 26, 2019Assignee: Frequency Therapeutics, Inc.Inventors: Christopher Loose, Will McLean, Megan Harrison, Michael R. Jirousek