Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
  • 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 9718771
    Abstract: A compound having an S1P1 receptor antagonistic activity. A compound represented by general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds have an excellent S1P1 receptor antagonistic activity and are useful for the treatment or prevention of autoimmune diseases.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: August 1, 2017
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Hitoshi Inoue, Kohsuke Ohno, Tetsuya Nakamura, Yusuke Ohsawa
  • Patent number: 9718802
    Abstract: The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2? diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2? diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: August 1, 2017
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Liang Zhang, Chuan Liu, Jinyi Xu, Zhaozhao Zhang, Zhi Chen, Jian Chai, Zhiqing Yang, Hairong Luo, Xiangyang Zhang
  • Patent number: 9688794
    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: October 15, 2013
    Date of Patent: June 27, 2017
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Jason Shih-Hao Chen, Michael Richard Kessler, Michael Dennis Zenner
  • Patent number: 9670223
    Abstract: A compound having the structural formula (I) and pharmaceutically acceptable salt and/or hydrates thereof, (I) wherein Y is an arylester or an C1-C8 alkylaryl ester, selected from the group consisting of: benzene, toluene, xylene, benzoic acid, benzoate, nicotinate, isonicotinate and halobenzene, which can be unsubstituted or substituted with at least one nitric oxide releasing group; and/or at least one of hydroxide, —Cl, —Br, a C1-C8 alkyl, benzyl, a C1-C8 alkoxy, benzyloxy, —NHC(O)R, —NH2, —NO2, —ONO2, —(CH2)nONO2, —OC(O)[(CH2)m], cyclic ONO2, —OCOArONO2, —OCOAr(CH2)nONO2 or a C1-C5 haloalkyl ester, wherein R is a C1-C8 alkyl or a C1-C8 alkoxy group, n=1-8 and m=3-10, to produce a super-aspirin effect.
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: June 6, 2017
    Assignee: SOLVOTRIN THERAPEUTICS LTD.
    Inventors: John Francis Gilmer, Mark Ledwidge, Pat O'Flynn, Shona Harmon, Marek Radomski, Carlos Medina Martin
  • Patent number: 9598370
    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: September 15, 2015
    Date of Patent: March 21, 2017
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Patent number: 9573963
    Abstract: A fused heterocyclic compound represented by formula (1) or an N-oxide thereof has an excellent control effect on pests: wherein A1 represents N or the like, A2 represents NR6 or the like, A3 represents CR12 or the like, R1 represents a C1 to C6 chain hydrocarbon group or the like, R2, R4 and R5 are the same or different and represent a C1 to C3 alkyl group optionally having one or more halogen atoms or the like, R3 represents a C1 to C6 chain hydrocarbon group or the like, R6 represents a C1 to C6 chain hydrocarbon group or the like, any one set of R9 and R10, R10 and R11, and R11 and R12 in R9, R10, R11 and R12, together with the carbon atoms to which they are bound, forms a ring, and n represents 0, 1 or 2.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: February 21, 2017
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takamasa Tanabe, Mai Ito, Chie Shimizu, Yoshihiko Nokura
  • Patent number: 9567328
    Abstract: The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: February 14, 2017
    Assignee: ALLERGAN, INC.
    Inventors: William R. Carling, Jose L. Martos, Jussi J. Kangasmetsa, Jenny W. Wang, David F. Woodward
  • Patent number: 9463186
    Abstract: The present invention provides systems, compositions and methods for treatment of dopaminergic disorders (e.g., Parkinson's disease) using the combination of a first compound that inhibits a voltage-gated calcium channel of the type Cav1.3 (e.g., a dihydropyridine such as isradipine), and a second compound that is monoamine oxidase inhibitor and/or is a nitric oxide synthase inhibitor (e.g., rasagiline or derivative thereof).
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: October 11, 2016
    Assignee: Northwestern University
    Inventors: Dalton J. Surmeier, Javier Sanchez, Jaime Guzman, Enrico Zampese, Daniel Galtieri, Ema Ilijic
  • Patent number: 9402835
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: August 2, 2016
    Assignee: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David Rock, Mark Ridall
  • Patent number: 9381177
    Abstract: The present invention relates to: combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino)aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and a kit comprising such a combination.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: July 5, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Florian Pühler, Marion Hitchcock
  • Patent number: 9370184
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: June 21, 2016
    Assignee: Bayer Cropscience AG
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Patent number: 9365554
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: June 14, 2016
    Assignee: AVIRAGEN THERAPEUTICS, INC.
    Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
  • Patent number: 9327031
    Abstract: Buffer solutions for pharmaceutical preparations that have bactericidal activity preferentially against gram negative bacteria are provided. The buffers have a pH of greater than about 10 or less than about 4.5 with low buffer capacity. Methods of their use in reducing the occurrence of blood stream infections in a mammal is also provided.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: May 3, 2016
    Assignee: United Therapeutics Corporation
    Inventors: Roger Andrew Jeffs, David Zaccardelli
  • Patent number: 9278983
    Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: March 8, 2016
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
  • Patent number: 9273055
    Abstract: The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.
    Type: Grant
    Filed: June 18, 2014
    Date of Patent: March 1, 2016
    Assignee: CHEMBRIDGE CORPORATION
    Inventor: Vlad Edward Gregor
  • Patent number: 9238029
    Abstract: Herein provided are dosage forms (variously referred to as “formulations”) comprising a PPI that is released from the dosage form as a first and a second dose. Each dose of PPI is present in an amount sufficient to raise the plasma levels of the PPI to at least 100 ng/ml.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: January 19, 2016
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventors: Rajneesh Taneja, Majid Vakilynejad
  • Patent number: 9221764
    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: May 7, 2014
    Date of Patent: December 29, 2015
    Assignee: University of Virginia Patent Foundation
    Inventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Dixon
  • Patent number: 9205078
    Abstract: The present invention relates to a method of treating chronic myelogenous leukemia in a subject comprising administering to the subject a compound, such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: December 8, 2015
    Assignee: PFIZER INC.
    Inventor: Brion William Murray
  • Patent number: 9192606
    Abstract: The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: November 24, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Christopher Young
  • Patent number: 9181234
    Abstract: The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: November 10, 2015
    Assignee: Biota Europe Ltd.
    Inventors: James T Palmer, Christopher James Lunnis, Daniel A Offermann, Lorraine Claire Axford, Michael Blair, Dale Mitchell, Nicholas Palmer, Christopher Steele, John Atherall, David Watson, David Haydon, Lloyd Czaplewski, David Davies, Ian Collins, Edward Malcolm Tyndall, Laura Andrau, Gary Robert William Pitt
  • Patent number: 9156834
    Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
    Type: Grant
    Filed: August 15, 2014
    Date of Patent: October 13, 2015
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
  • Patent number: 9145389
    Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: September 29, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akira Fujishima, Isao Aoki
  • Patent number: 9138426
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Patent number: 9115118
    Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dehydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: August 25, 2015
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna, Voggu Ramesh Reddy
  • Patent number: 9095578
    Abstract: The present invention relates to a method of preventing or treating a disease caused by infection by a eukaryotic pathogen, wherein the method comprises administering an effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of a eukaryotic pathogen's adenylyl cyclase that do not substantially modulate an adenylyl cyclase of the subject. The invention also provides methods for culturing eukaryotic pathogens and methods for inducing the pathogenic state in vitro.
    Type: Grant
    Filed: January 11, 2008
    Date of Patent: August 4, 2015
    Assignee: CORNELL RESEARCH FOUNDATION, INC.
    Inventors: Lonny Levin, Jochen Buck, Leo Brizuela, Michael Pinnisi
  • 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