Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
  • Patent number: 11096940
    Abstract: Provided herein are methods for treating and/or preventing hepatocellular carcinoma (HCC) characterized by hepatitis B virus (HBV) infection in a patient, comprising administering an effective amount of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one or a pharmaceutically acceptable salt or tautomer thereof (collectively referred to herein as “Compound 1”) to the patient having HCC characterized by HBV infection.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: August 24, 2021
    Assignee: Celgene Corporation
    Inventors: Ellen Filvaroff, Kristen M. Hege, Shaoyi Li
  • Patent number: 11098016
    Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
    Type: Grant
    Filed: August 12, 2020
    Date of Patent: August 24, 2021
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Guozhang Xu, Micheal Gaul, Shyh-Ming Yang, Tianbao Lu, Rui Zhang, Fengbin Song
  • Patent number: 11091421
    Abstract: The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is —CH2—, —CH(OH)—, or —C(O)—; G is C or N; X is —CH2—, O, or —C(O)—; Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, —NRy1Ry2, —ORy1, —Ry1C(O)Ry3, —C(O)Ry1, —C(O)ORy2, —C(O)ORy2Ry3, —NRy1C(O)Ry2, —NRy1C(O)NRy2Ry3, —NRy1C(O)ORy2Ry3, —NRy1C(O)Ry2ORy3, C(O)NRy1(Ry2Ry3), —C(O)NRy1(Ry2ORy1), —ORy2Ry3, and —ORy2ORy3, wherein each of Ry1 and Ry2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and Ry3 is aryl optionally substituted with at least one halogen; Z is —NRz1Rz2, —NRz1Rz3, —ORz1, —ORz1Rz3, —C(O)Rz1Rz3, —C(O)ORz1Rz3, —NRz1C(O)Rz2Rz3, —NRz1C(O)ORz2Rz3, —C(O)NRz1Rz3, or ORz2ORz3, wherein each of Rz1 and Rz2 is independently sel
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: August 17, 2021
    Assignee: TAIWANJ PHARMACEUTICALS CO., LTD.
    Inventors: Syaulan S. Yang, Kuang Yuan Lee, Meng Hsien Liu, Yan-Feng Jiang, Yu-Shiou Fan, Chi-Han Chen, Sheng Hung Liu
  • Patent number: 11084789
    Abstract: Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders associated with mast cells. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more diseases and disorders associated with mast cells.
    Type: Grant
    Filed: January 9, 2020
    Date of Patent: August 10, 2021
    Assignee: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Lijun Sun, Aristidis Veves
  • Patent number: 11084825
    Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL inter-action; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 31, 2019
    Date of Patent: August 10, 2021
    Assignee: BIOMEA FUSION, LLC
    Inventors: Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
  • Patent number: 11083721
    Abstract: The present invention provides an oral pharmaceutical composition and a usage thereof, comprising a pharmaceutically acceptable acidic medicinal auxiliary material whose surface is modified and dabigatran etexilate or pharmaceutically acceptable salts or aquo-complexes thereof. The present invention further provides a surface modification method for a medicinal auxiliary material.
    Type: Grant
    Filed: December 26, 2019
    Date of Patent: August 10, 2021
    Assignee: Shenzhen Pharmacin Co., Ltd.
    Inventors: Zeren Wang, Yulan Zhao, Lijiang Wang, Xiao Zhang, Jun Xu, Shunqin Chen, Meili Sun, Guisheng Jiang
  • Patent number: 11045450
    Abstract: Described herein are pharmaceutical compositions including a proton pump inhibitor and an antiparasitic drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: June 29, 2021
    Assignee: Adamis Pharmaceuticals Corporation
    Inventors: David Clayton Sutherland, James Kyle Zorn, Dennis J. Carlo
  • Patent number: 11013729
    Abstract: Compositions comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts, polymorphs, solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid, use of said compositions in the reduction of the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and/or in the prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery and processes for the preparation of said compositions.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: May 25, 2021
    Assignee: TOWA Pharmaceutical Europe, S.L. Unipersonal
    Inventors: Pratibha S. Pilgaonkar, Maharukh T. Rustomjee, Anilkumar S. Gandhi
  • Patent number: 11000540
    Abstract: This disclosure relates to treatments for reducing the side effects associated with treatment of a medication or drug, such as a chemotherapy medication, being experienced by a patient. This may be accomplished by administering to a patient taking the medication, a buffered aqueous liquid having a pH of about 10 to about 11.5.
    Type: Grant
    Filed: June 3, 2020
    Date of Patent: May 11, 2021
    Inventor: Al Siamon
  • Patent number: 11001588
    Abstract: The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).
    Type: Grant
    Filed: September 19, 2019
    Date of Patent: May 11, 2021
    Assignee: Forma Therapeutics, Inc.
    Inventors: David R. Lancia, Jr., Gary Gustafson, Neal Green, Lorna Mitchell, Anna Ericsson, David Richard
  • Patent number: 10961249
    Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: March 30, 2021
    Assignee: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Benjamin E. Blass, Daniel J. Canney, Kevin M. Blattner
  • Patent number: 10881615
    Abstract: A pharmaceutical composition comprising dabigatran etexilate, and preparation method and use thereof, and solid preparation comprising the pharmaceutical composition; the pharmaceutical composition comprises a vitamin C layer and a dabigatran etexilate layer separated by a semipermeable film layer, and the semipermeable film layer comprises a water-soluble compound, a water-insoluble compound and an optional anti-sticking agent and/or plasticizer.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: January 5, 2021
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Xiongxiong He, Ping Dong, Jiahui Cai, Xin Huang, Xiquan Zhang
  • Patent number: 10874646
    Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: December 29, 2020
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C Nicolaou, Derek Rhoades, Yanping Wang, Sotirios Totokotsopoulos
  • Patent number: 10864204
    Abstract: The present invention provides an oral pharmaceutical composition and a usage thereof, comprising a pharmaceutically acceptable acidic medicinal auxiliary material whose surface is modified and dabigatran etexilate or pharmaceutically acceptable salts or aquo-complexes thereof. The present invention further provides a surface modification method for a medicinal auxiliary material.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: December 15, 2020
    Assignee: SHENZHEN PHARMACIN CO., LTD.
    Inventors: Zeren Wang, Yulan Zhao, Lijiang Wang, Xiao Zhang, Jun Xu, Shunqin Chen, Meili Sun, Guisheng Jiang
  • Patent number: 10858346
    Abstract: The present invention provides a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-I, a co-crystal of Lumacaftor and nicotinamide, compositions including this crystalline form, and processes for the preparation of this crystalline form.
    Type: Grant
    Filed: October 15, 2018
    Date of Patent: December 8, 2020
    Assignee: Apotex Inc.
    Inventors: Fabio E. S. Souza, Bahareh Khalili, Katherine A. Rantanen
  • Patent number: 10851095
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: December 1, 2020
    Assignee: ANGION BIOMEDICA CORP.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen
  • Patent number: 10774048
    Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
    Type: Grant
    Filed: January 8, 2019
    Date of Patent: September 15, 2020
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Guozhang Xu, Micheal Gaul, Shyh-Ming Yang, Tianbao Lu, Rui Zhang, Fengbin Song
  • Patent number: 10696687
    Abstract: Disclosed herein is a compound of formula (I) and/or a pharmaceutically acceptable salt thereof that can serve as Erk inhibitors. They are potentially useful in the treatment of diseases treatable by inhibition of Erk, such as cancers. Also disclosed herein is a pharmaceutical composition, comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: June 30, 2020
    Assignee: Changzhou Jiekai Pharmatech Co., LTD.
    Inventors: Jintao Zhang, Wen Xu, Shanzhong Jian
  • Patent number: 10689358
    Abstract: An object of the invention is to provide a novel method for producing an indazole compound, by which an indazole compound can be produced without using a reaction reagent that exhibits strong toxicity, and a novel indazole compound. According to the invention, a method for producing an indazole compound, including obtaining an indazole compound or a salt thereof from a diazonium salt prepared from an aniline compound in the presence of a compound represented by the following General Formula (1), is provided. In the formula, R1 represents a hydrogen atom or an alkali metal; R2 represents a hydrogen atom, a hydroxyl group, or the like; and R3 represents a hydrogen atom, a C1-30 alkylcarbonyl group which may have a substituent, or a C6-20 arylcarbonyl group which may have a substituent.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: June 23, 2020
    Assignee: FUJIFILM Corporation
    Inventor: Motomasa Takahashi
  • Patent number: 10611720
    Abstract: Provided are a compound represented by the following Formula I, or a solvate, stereoisomer, or pharmaceutically acceptable salt thereof, and a composition for preventing or treating hair loss, the compound including the compound as an active ingredient:
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: April 7, 2020
    Assignees: UNIST (ULSAN NATIONAL INSTITUTE OF SCIENCE AND TECHNOLOGY), Seoul National University Hospital
    Inventors: Mi Hee Lim, Sang Tae Kim, Ho Seong Han
  • Patent number: 10597384
    Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methypyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: March 24, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Patent number: 10591481
    Abstract: Methods of measuring the activity of Factor D, the key driver in the activation of the alternative complement pathway, methods of determining the potency of Factor D inhibitors, and methods of screening for Factor D inhibitors are provided.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: March 17, 2020
    Assignee: Genentech, Inc.
    Inventors: Linda Orren, Aaron Miller, Xiaoqing Jia, Pin Yee Wong
  • Patent number: 10513529
    Abstract: Derivatives of 1,2,4-Triazolo-[3,4-b]-1,3,4-thiadiazoles according to formula (I), as set forth below: processes for production thereof, pharmaceutical compositions containing the same and the use thereof in treatment of cancer.
    Type: Grant
    Filed: July 14, 2017
    Date of Patent: December 24, 2019
    Assignees: GALENICA S.A., ENERGONBIO TECHNOLOGIES S.A.
    Inventor: Dimitrios Trafalis
  • Patent number: 10479782
    Abstract: The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: November 19, 2019
    Assignee: Mylan Laboratories Limited
    Inventors: Ramakoteswara Rao Jetti, Hemant Malhari Mande, AnJaneyaraju Indukuri, Bommareddy Aggiramireddy, Neelima Bhagavatula, Amit Singh, Soumyajit Ghosh, Attanti Veera Venkata Srinivasarao, Umasankara Sastry Tummalapalli, Veera Venkata Satya Surya Appala Gosula
  • Patent number: 10441575
    Abstract: Described herein are pharmaceutical compositions including a proton pump inhibitor and an antiparasitic drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: October 15, 2019
    Assignee: Adamis Pharmaceuticals Corporation
    Inventors: David Clayton Sutherland, James Kyle Zorn, Dennis J. Carlo
  • Patent number: 10342841
    Abstract: Liquid antacid compositions containing citrus extract are disclosed. The liquid antacid compositions possess superior resistance to microbial attack.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: July 9, 2019
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Javier Barraza, Renata Muniz
  • Patent number: 10280241
    Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R?C(O)R2)1-8. At each occurrence R? is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R? is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R?C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: May 7, 2019
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Jason Shih-Hao Chen, Michael Richard Kessler, Michael Dennis Zenner
  • Patent number: 10221171
    Abstract: Provided herein are compounds of formula (I) which are, inter alia, useful allosteric inhibitors of Hsp70. The compounds and methods provided are useful for the treatment of cancer, infectious and neurodegenerative diseases.
    Type: Grant
    Filed: January 11, 2016
    Date of Patent: March 5, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Jason E. Gestwicki, Xiaokai Li
  • Patent number: 10221185
    Abstract: The present invention relates to a crystal form of a substituted aminopyran compound, and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes. In particular, the present invention relates to a crystal form IV of a compound as shown by formula (I) and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: March 5, 2019
    Assignee: Sichuan Haisco Pharmaceutical Co., Ltd.
    Inventors: Chen Zhang, Jianmin Wang
  • Patent number: 10214493
    Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: February 26, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Micheal Gaul, Guozhang Xu, Shyh-Ming Yang, Tianbao Lu, Rui Zhang, Fengbin Song
  • Patent number: 10159664
    Abstract: The present invention provides an oral pharmaceutical composition and a usage thereof, comprising a pharmaceutically acceptable acidic medicinal auxiliary material whose surface is modified and dabigatran etexilate or pharmaceutically acceptable salts or aquo-complexes thereof. The present invention further provides a surface modification method for a medicinal auxiliary material.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: December 25, 2018
    Assignee: Shenzhen Pharmacin Co., Ltd.
    Inventors: Zeren Wang, Yulan Zhao, Lijiang Wang, Xiao Zhang, Jun Xu, Shunqin Chen, Meili Sun, Guisheng Jiang
  • Patent number: 10160753
    Abstract: The present invention provides indazole compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein Z1, Z2, R1, R2, R3, ‘m’ and ‘n’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of the compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: December 25, 2018
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Venkateshwar Rao Gummadi, Susanta Samajdar, Ajay Gupta
  • Patent number: 10137116
    Abstract: The present invention relates to the use of benzimidazole sulfide derivatives and prodrugs thereof in the treatment and/or prevention of tuberculosis.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: November 27, 2018
    Assignee: École Polytechnique Fédérale de Lausanne (EPFL)
    Inventors: Stewart Cole, Jan Lars Rybniker
  • Patent number: 10137111
    Abstract: Described herein are pharmaceutical compositions including a proton pump inhibitor and an antiparasitic drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: November 27, 2018
    Assignee: Adamis Pharmaceuticals Corporation
    Inventors: David Clayton Sutherland, James Kyle Zorn, Dennis J. Carlo
  • Patent number: 10130618
    Abstract: This invention is a novel pharmaceutical composition comprising dabigatran or a pharmaceutically acceptable salt thereof in combination with a proton pump inhibitor for use in the antithrombotic treatment with preventing or reducing the risk of a gastrointestinal disorder.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: November 20, 2018
    Assignee: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETI
    Inventors: Ali Türkyilmaz, Mehtap Saydam, Yildiz Gülkok, Nur Kirat Uzunogullari, Sevgi Gökcek
  • Patent number: 10117840
    Abstract: This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: November 6, 2018
    Assignee: The Scripps Research Institute
    Inventors: Jiajia Dong, K. Barry Sharpless, Jeffery W. Kelly, Wentao Chen
  • Patent number: 10065962
    Abstract: The present disclosure relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: September 4, 2018
    Assignee: SICHUAN HAISCO PHARMACEUTICAL CO., LTD
    Inventors: Chen Zhang, Jianmin Wang, Caihu Li, Yonggang Wei
  • Patent number: 10045973
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent and to use of such compositions in treating nocturnal acid breakthrough.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: August 14, 2018
    Assignee: THE CURATORS OF THE UNIVERSITY OF MISSOURI
    Inventor: Jeffrey Owen Phillips
  • Patent number: 9970938
    Abstract: Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a compound of general formula I wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C?Y, wherein Y stands for ox
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: May 15, 2018
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann, Madlaina Breuleux, Michael Boutros, Daniel Gilbert, Xian Zhang
  • Patent number: 9969710
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: May 15, 2018
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-Lebrun, Ruoxi Lan, Austin Chen, Ryan C. Clark
  • Patent number: 9938270
    Abstract: The present invention relates to crystalline and amorphous forms of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2-a]pyridine mono-phosphate salt and methods of making these solid forms thereof. The invention compounds are modulators of mGlu5 which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGlu5 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGlu5 is involved.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: April 10, 2018
    Assignee: Addex Pharma S.A.
    Inventors: Béatrice Bonnet, Sonia Maria Poli
  • Patent number: 9924712
    Abstract: The present invention relates to a liquid concentrate formulation comprising a pyripyropene pesticide of the formula I as defined below and an alkoxylated aliphatic alcohol as an adjuvant. Moreover, the invention relates to the use of the formulations for the treatment of plants and seed and to corresponding methods.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: March 27, 2018
    Assignee: BASF SE
    Inventors: Wen Xu, Matthias Pohlman
  • Patent number: 9926290
    Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: March 27, 2018
    Assignee: University of Virginia Patent Foundation
    Inventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Mishra
  • Patent number: 9920145
    Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R?C(O)R2)1-8. At each occurrence R? is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R? is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R?C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: March 20, 2018
    Assignee: IOWA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Jason Shih-Hao Chen, Michael Richard Kessler, Michael Dennis Zenner
  • Patent number: 9907751
    Abstract: Oral liquid colchicine formulations are described herein. Methods of using the oral liquid colchicine formulations are also provided.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: March 6, 2018
    Assignee: RxOMEG Therapeutics LLC
    Inventors: Indu Muni, Naomi Vishnupad
  • Patent number: 9834527
    Abstract: The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: December 5, 2017
    Assignee: SANOFI
    Inventors: Andreas Evers, Christopher Kallus, Michael Wagner, Hermut Wehlan
  • Patent number: 9820977
    Abstract: Pharmaceutically acceptable single parasiticidal agent compositions of imidacloprid for oral delivery to mammals to systemically control targeted blood-sucking or blood-consuming parasites, such as fleas, ticks and certain species of helminthes and scabies.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: November 21, 2017
    Assignee: BAYER HEALTHCARE LLC
    Inventors: Roland H. Johnson, Douglas I. Hepler, Kathleen G. Palma, William R. Campbell
  • Patent number: 9751890
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: October 19, 2016
    Date of Patent: September 5, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Patent number: 9737510
    Abstract: The patent discloses novel indazole compounds of general formula 1 and analogues thereof, use thereof for the treatment of diabetes, diabetic complications, cardiovascular dysfuntion or related diseases, pharmaceutical compositions comprising them and processes for their preparation.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: August 22, 2017
    Assignees: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH, SHANTANI PROTEOME ANALYTICS PVT. LTD
    Inventors: Dumbala Srinivasa Reddy, Chaitanya Saxena, Kashinath Komirishetty
  • Patent number: RE47437
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: June 18, 2019
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon