Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbon Atoms (e.g., Pyridazines, Etc.) Patents (Class 514/247)
  • Patent number: 10238657
    Abstract: Disclosed herein is a method of treating psoriasis involving the use of compound of formula I and/or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: March 26, 2019
    Assignee: JS INNOPHARM (SHANHAI) LTD.
    Inventors: Jintao Zhang, Quanhai Liu, Minyu Liu, Xiaoling Huang, Yifang Deng, Pengxia Yu
  • Patent number: 10202361
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, (N-oxides), and salts thereof, wherein A, R1, R2 Q and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: February 12, 2019
    Assignee: FMC Corporation
    Inventors: Thomas Martin Stevenson, Matthew James Campbell
  • Patent number: 10167250
    Abstract: The present invention relates to a process for preparation of 2-(trihalomethyl) benzamide.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: January 1, 2019
    Assignee: SRF Limited
    Inventors: Surender Dhingra, Kundan Singh Shekhawat, Satish Kumar, Kapil Kumar, Rajdeep Anand
  • Patent number: 10138210
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: November 27, 2018
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Patent number: 10112928
    Abstract: The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: October 30, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Niala Bhagirath, Joshua Kennedy-Smith, Nam T. Le, Matthew C. Lucas, Fernando Padilla, Michael Soth
  • Patent number: 10093656
    Abstract: Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: October 9, 2018
    Assignee: NANJING SANHOME PHARMACEUTICAL CO., LTD
    Inventors: Charles Z. Ding, Shuhui Chen, Baoping Zhao, Xile Liu, Linxia Xiao, Chao Ding, Fei Wang, Jian Li
  • Patent number: 10076519
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: September 18, 2018
    Assignee: CYTOKINETICS, INC.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang, Pu-Ping Lu, Antonio Romero
  • Patent number: 10047066
    Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: August 14, 2018
    Assignee: NEWLINK GENETICS CORPORATION
    Inventors: Mario Mautino, Firoz Jaipuri, Agnieszka Marcinowicz-Flick, Tanay Kesharwani, Jesse Waldo
  • Patent number: 10016420
    Abstract: The invention provides compounds of formula I, wherein: R1 represents a cyclic group selected from phenyl, heteroaryl1, heterocyclyl1 and C3-6 cycloalkyl; wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C1-6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C1-6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl1a and heterocyclyl1a; and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 6-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl1 and heterocyclyl1a may additionally be substituted with ?O; X represents a bond or C1-6 alkylene (which may be straight or branched); R2 represents H or C1-6 alkyl; R3 represents H or C1-6 alkyl; Y represents a bond or C1-6 alkylene (which may be straight
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: July 10, 2018
    Assignee: INHIBITAXIN LIMITED
    Inventors: Karl Richard Gibson, Dafydd Rhys Owen
  • Patent number: 10005767
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: June 26, 2018
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 9920016
    Abstract: Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3 -hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one(13, RX-3117) and its intermediates are described.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: March 20, 2018
    Assignee: REXAHN PHARMACEUTICALS, INC.
    Inventors: Deog Joong Kim, Haifeng Yin, Eliezer Falb, Leigh Andre Pearcey, Jonathan Cummins, Petra Dieterich, Jean-Francois Carniaux, Yi Wang, Vikram Chandrakant Purohit
  • Patent number: 9889148
    Abstract: A phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof is provided for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: February 13, 2018
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann
  • Patent number: 9840519
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: November 14, 2016
    Date of Patent: December 12, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
  • Patent number: 9732073
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Patent number: 9730933
    Abstract: The invention relates to medicine, in particular to gastroenterology, and lies in the field of treatment of liver diseases of various origins. For this purpose, the hepatoprotective agent that is introduced to the patient is embodied as derivatives of bis(2-thio-4,6-dioxo-1,2,3,4,5,6-hexahydropyrimidine-5-yl)arylmethanes. The method provides reduction of the manifestations of cytolysis under the influence of damaging agents and a statistically significant reduction of dysproteinemia, it accelerates restoration of detoxifying processes of the liver, increases induction of endogenic interferon alfa and, consequently, makes the protection of liver cells during hepatitides of various origins more effective.
    Type: Grant
    Filed: May 13, 2016
    Date of Patent: August 15, 2017
    Assignee: Viktor Veniaminovich Tets
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets
  • Patent number: 9718822
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: August 1, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
  • Patent number: 9708348
    Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: July 18, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
  • Patent number: 9701689
    Abstract: The present invention provides a heterocyclic compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof, in which XA, R1, YA, R2, R3A, and R4A are as defined herein. The compound of formula (I) inhibits a C-C chemokine receptor type 10 (CCR10) receptor and is useful as a prophylactic and/or therapeutic agent for skin diseases.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: July 11, 2017
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Kenji Uchida, Toshimi Kanai, Masakazu Homma, Seiji Aratake, Tatsuya Ishimori
  • Patent number: 9663493
    Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: May 30, 2017
    Assignees: Northwestern University, Universite De Strasbourg, Centre National De La Recherche Scientifique (CNRS)
    Inventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
  • Patent number: 9629855
    Abstract: The present invention relates to a pharmaceutical composition for the treatment of eye pain, containing a PGE2 synthesis inhibitor. The use of the pharmaceutical composition for the prevention or treatment of eye pain according to the present invention, which contains the PGE2 synthesis inhibitor as an active ingredient, makes it possible to alleviate the symptoms of eye pain by selectively inhibiting the PGE2 expression level, and also has the advantages of treating and preventing xerophthalmia and of overcoming and preventing eye discomfort caused by various inflammation-inducing circumstances including following surgery. Also, by using a kit for detecting the amount of PGE2, PGD2 and COX2, the present invention makes it possible to easily diagnose eye-pain symptoms in clinical practice, and can be widely used in checking the state not only of patients having xerophthalmia but also patients following eye surgery.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: April 25, 2017
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Hyung Keun Lee, Jong Woo Shim
  • Patent number: 9603803
    Abstract: This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: March 28, 2017
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: Filip Rene Irene Kiekens, Jody Firmin Marceline Voorspoels, Lieven Elvire Colette Baert
  • Patent number: 9604965
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 12, 2015
    Date of Patent: March 28, 2017
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang, Pu-Ping Lu, Antonio Romero
  • Patent number: 9573966
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, Formulas (I), (II), (III) and (IV) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent proliferative disorders and their use to manufacture a medicine to treat or prevent proliferative disorders, particularly cancer such as leukemia. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent proliferative disorders. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of proliferative disorders and pathologic conditions such as, but not limited to, cancer such as leukemia.
    Type: Grant
    Filed: September 8, 2011
    Date of Patent: February 21, 2017
    Assignee: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Jean Herman, Thierry Louat
  • Patent number: 9566283
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: February 14, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 9533958
    Abstract: Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: January 3, 2017
    Assignee: Rexahn Pharmaceuticals, Inc.
    Inventors: Haifeng Yin, Deog Joong Kim, Eliezer Falb, Leigh Andre Pearcey, Jonathan Cummins, Petra Dieterich, Jean-Francois Carniaux, Yi Wang, Vikram Chandrakant Purohit
  • Patent number: 9517237
    Abstract: The invention described herein pertains to the treatment of multiple sclerosis. In particular, the invention described herein pertains to the treatment of multiple sclerosis using compounds that modulate the action of acrolein.
    Type: Grant
    Filed: May 7, 2015
    Date of Patent: December 13, 2016
    Assignee: Purdue Research Foundation
    Inventor: Riyi Shi
  • Patent number: 9499548
    Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: November 22, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Christine E. Brotherton-Pleiss, Ramona Hilgenkamp, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou
  • Patent number: 9499560
    Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: November 22, 2016
    Assignee: YM BIOSCIENCES AUSTRALIA PTY LTD
    Inventors: David G. Bourke, Christopher J. Burns, Anthony N. Cuzzupe, John T. Feutrill, Marcel R. Kling, Tracy L. Nero
  • Patent number: 9408845
    Abstract: The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I wherein R1, R4, R5, R6, R7, R8, R9, R12, R13 ET R14 are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioallyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfonyl, sulfinyl, sulfonyl, sultanate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, ?O, ?S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: August 9, 2016
    Assignee: Northwestern University
    Inventors: D. Martin Watterson, Linda Van Eldik, Wenhui Hu
  • Patent number: 9376426
    Abstract: Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: June 28, 2016
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Patent number: 9333203
    Abstract: The invention relates to the field of female sexual dysfunction. It specifically relates to the influence of the combination of testosterone or an analog thereof and tadalafil on sexual health in female subjects with Female Sexual Dysfunction (such as Female Sexual Arousal Disorder (FSAD) or Female Sexual Desire Disorder (FSDD)). It further relates to the influence of the combination of testosterone or an analog thereof and a compound capable of at least in part inhibiting smooth muscle constriction, for example a compound capable of at least in part inhibiting the adrenergic tone. The invention further discloses other combinatorial therapies in the treatment of Female Sexual Dysfunction.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: May 10, 2016
    Assignee: EB IP LYBRIDO B.V.
    Inventors: Jan J. A. Tuiten, Johannes M. M. Bloemers
  • Patent number: 9273011
    Abstract: The invention provides compounds of formula I, (I) wherein: R represents a cyclic group selected from phenyl, heteroaryl, heterocyclyl and C 3-6 cycloalkyl; 10 wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C -6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl 1a and heterocyclyl 1a; and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 16-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl and heterocyclyl 1a may additionally be substituted with ?O; 20 X represents a bond or C -6 alkylene (which may be straight or branched); R 2 represents H or C -6 alkyl; R 3 represents H or C -6 alkyl; Y represents a bond or C -6 alkylene (which may be stra
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: March 1, 2016
    Assignee: Inhibitaxin Limited
    Inventors: Karl Richard Gibson, Dafydd Rhys Owen
  • Patent number: 9238019
    Abstract: The antitussive and bronchodilator use for an enaminone ester relates to the use of ethyl 4-[(4-chlorophenyl)amino]-6-methyl-2-oxocyclohex-3-en-1-oate (also referred to as “enaminone E121”) for treatment of respiratory conditions, and particularly to use of the ester as the active ingredient in a cough suppressant for nonproductive cough. The ester may be used to achieve an antitussive effect, a bronchodilator effect, or both in a patient in need thereof. The ester may be formulated in any desired delivery form (such as a tablet, a capsule, a time-release capsule, a syrup, a liquid, an injection, a spray, or an inhalant), and be combined with any suitable pharmaceutical carrier, vehicles, binders, fillers, disintegrators, lubricants, solubilizers, emulsifiers, surfactants, and other excipients.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: January 19, 2016
    Assignee: UNIVERSITY OF KUWAIT
    Inventors: Ahmed Z. El-Hashim, Ivan O. Edafiogho, Samuel B. Kombian, Mariam H. Yousif
  • Patent number: 9238643
    Abstract: A compound represented by formula (I) and the pharmaceutical acceptable salt thereof are disclosed, wherein, R1, R2, R3, R4, R5 and Ar are defined as those in the specification.
    Type: Grant
    Filed: September 6, 2010
    Date of Patent: January 19, 2016
    Assignee: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Wenhui Hu, Guifa Zhong, Ling Yang, Hongjiang Xu
  • Patent number: 9221806
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: December 29, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
  • Patent number: 9192623
    Abstract: The present invention discloses ophthalmic and otic compositions of facially amphiphilic antimicrobial polymers and oligomers and their uses, including their use in methods for treating and preventing ophthalmic infections and otic infections in humans and animals.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: November 24, 2015
    Assignee: Cellceutix Corporation
    Inventor: Richard W. Scott
  • Patent number: 9150588
    Abstract: A compound having PDE inhibitory represented by formula (1), W1-W2 (1), wherein (i) W1 is and W2 is (ii) W1 is and W2 is or (iii) W1 is and W2 is or a pharmaceutically acceptable salt thereof; and a method of treating or preventing schizophrenia.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: October 6, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takahiko Taniguchi, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
  • Patent number: 9150520
    Abstract: Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: October 6, 2015
    Assignee: Rexahn Pharmaceuticals, Inc.
    Inventors: Haifeng Yin, Deog J. Kim, Eliezer Falb, Leigh A. Pearcey, Jonathan Cummins, Petra Dieterich, Jean-Francois Carniaux, Yi Wang, Vikram Chandrakant Purohit
  • Patent number: 9056109
    Abstract: The invention described herein pertains to the treatment of multiple sclerosis. In particular, the invention described herein pertains to the treatment of multiple sclerosis using compounds that modulate the action of acrolein.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: June 16, 2015
    Assignee: Purdue Research Foundation
    Inventor: Riyi Shi
  • Patent number: 9040457
    Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: May 26, 2015
    Assignee: ISAGRO S.P.A.
    Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 9018207
    Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: April 28, 2015
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Maree Therese Smith, Bruce Douglas Wyse
  • Patent number: 9006431
    Abstract: There is provided a hemihydrate form of the sodium salt of pemirolast.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: April 14, 2015
    Assignee: RSPR Pharma AB
    Inventors: Anett Perlberg, Martin Viertelhaus, Ulrika Rosenström, Karol Horvath
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8999984
    Abstract: Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: April 7, 2015
    Assignee: University of Louisville Research Foundation, Inc.
    Inventors: Robert A. Mitchell, John O. Trent, Jason B. Meier
  • Patent number: 9000031
    Abstract: The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone-based autophagy inhibitor and a radiotherapy.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: April 7, 2015
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: Steffan Nawrocki, Jennifer Carew, Guru Reddy
  • Patent number: 8993595
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
  • Patent number: 8993569
    Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 31, 2015
    Assignee: Pierre Fabre Medicament
    Inventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
  • Patent number: RE46024
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: June 7, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nancy-Ellen Haynes, Denis J. Kertesz, Sherrie Lynn Pietranico-Cole, Yimin Qian, Nathan Robert Scott, Sung-Sau So, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley