Asymmetrical (e.g., 1,2,4-triazine, Etc.) Patents (Class 514/242)
  • Patent number: 11208389
    Abstract: This invention is directed to compositions, methods and kits that can be used for reducing cell viability, inducing cell apoptosis, and inhibiting cell proliferation, such as for the treatment of cancer. The invention is also directed to compositions, methods and kits that can be used for treating inflammatory conditions, such as by modulating inflammatory cytokines.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: December 28, 2021
    Assignee: GLAX LLC
    Inventors: Rakesh K Srivastava, Sharmila Shankar, Sushant Kumar Shrivastava, Anupam G. Banerjee
  • Patent number: 11034647
    Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
    Type: Grant
    Filed: December 9, 2019
    Date of Patent: June 15, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Yan Feng, Mauro Fa, Ottavio Arancio, Shixian Deng, Donald W. Landry, Yitshak Francis
  • Patent number: 10894050
    Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: January 19, 2021
    Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.
    Inventors: D. Keith Hester, II, Robert J. Duguid, Martha J. Kelly, Anna Chasnoff, Gang Dong, Edwin L. Crow, Lianhe Shu, Ping Wang, Duk Soon Choi
  • Patent number: 10576086
    Abstract: The present invention relates to interferon-gamma (IFN-?) inhibitors, and their utility in treating or controlling diseases that can be treated or controlled through inhibition of IFN-? production, such as Alzheimer's disease, prion diseases, multiple sclerosis, epilepsy, rheumatoid arthritis, inflammatory bowel disease, uveitis, autoimmune skin diseases, psoriasis, Sjögren's syndrome, Crohn's disease, and type 1 diabetes mellitus. The compounds are of Formula 1, 2 3, or are solvates, tautomers, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: March 3, 2020
    Assignee: UNIVERSITY OF GREENWICH
    Inventors: Laurence Harbige, Michael Leach
  • Patent number: 10456392
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: October 29, 2019
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Patent number: 10112913
    Abstract: The present invention relates to compounds of the formula I wherein the variables are defined in the claims and the specification, to their preparation and their use as fungicides.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: October 30, 2018
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Nadege Boudet, Bernd Mueller, Maria Angelica Quintero Palomar, Ana Escribano Cuesta, Erica May Lauterwasser Cambeis, Jan Klaas Lohmann, Thomas Grote, Manuel Kretschmer, Ian Robert Craig
  • Patent number: 9862712
    Abstract: The present invention disclosed a novel EGFR inhibitor compound of formula (I), process for preparation thereof and methods of treating abnormal cell growth in mammals by administering the compounds of formula (I). Wherein, R?—H, 3-CH3, 4-NO2, 4-Cl, 2-CH3, 4-CH3, 4-Br, 4-F R1?—H, -4-OCH3, -4-NO2,-2-NO2, -4-Cl, -2,4,6-CH3, -4-CH3, -2-F,4-Br, -4-CF3, -4-S—CH3, -4-Cl,-3-CF3, -3-S—CH3, -3,5-CF3, -2-S—CH3, -3-CF3,-4-OCF3, —Si—(CH3)3, —Si—(C2H5)3, (CH3)2—Si— C2H5.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: January 9, 2018
    Assignee: Council of Scientific & Industrial Research
    Inventors: Pradeep Kumar, Jignesh Kantilal Parikh, Eeshwaraiah Begari
  • Patent number: 9826740
    Abstract: Described is a broad spectrum, synergistic fungicidal composition when used for the preservation of a glued wood product comprising as active ingredients: (A) triadimefon, and (B) cyproconazole characterised in that the weight ratio of (A):(B) is from about 20:1 to about 1:1, the composition being further characterised in that the application rate for the composition is from about 10 gai/m3 to about 6,000 gai/m3.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: November 28, 2017
    Assignee: ZELAM LIMITED
    Inventors: Christopher Molloy, Peter James Hayward, Paul Garry Lobb, George William Mason, Stephen Millward, Wallace James Rae, Andre Frederik Siraa
  • Patent number: 9751862
    Abstract: Compounds of formula (I) wherein m is 0 or 1; Z is methine or nitrogen; X is oxygen or sulfur, R1 is C1-C6-alkyl, halo-C1-C6-alkyl, C3-C6-cycloalkyl or C2-C6-alkynyl; R2 is C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, halo-C3-C6-cycloalkyl, fluoro, chloro or bromo; R3 is C1-C3-alkyl; R4 is hydrogen, C1-C6-alkyl, fluoro, chloro, bromo or cyano; Y is CN, COOR9 or CONHR6; n is 0, 1 or 2; R5 is hydrogen, fluoro, chloro or bromo; R6 is C1-C4-alkyl; R9 is C1-C4-alkyl; R10 and R11 are, independently from each other, hydrogen, C1-C3-alkyl or C1-C3-alkoxy; or R10 and R11 taken together form with the carbon atom to which they are bonded a C3-C6-carbocyclic ring; or R10 and R11 taken together form a ketone or a ?NOR12 group; and R12 is hydrogen or C1-C4-alkyl; and agrochemically acceptable salts and enantiomers of those compounds can be used as insecticides an can be prepared in a manner known per se.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: September 5, 2017
    Assignee: Syngenta Participations AG
    Inventors: Andre Jeanguenat, Andrew Edmunds, Roger Graham Hall
  • Patent number: 9732046
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: August 15, 2017
    Assignee: YM BIOSCIENCES AUSTRALIA PTY LTD.
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Patent number: 9635852
    Abstract: The present disclosure relates generally to insecticide formulations. The present disclosure relates more particularly to aqueous pymetrozine formulations that can be provided in concentrate form and methods for making them. In one aspect, the disclosure provides a composition including pymetrozine in particulate form; a first polymeric dispersing agent, the first polymeric dispersing agent being a copolymer of (a) a maleic acid monomer and (b) a hydrophobic monomer; and a second polymeric dispersing agent, the second polymeric dispersing agent being a copolymer of (a) a (meth)acrylic acid monomer, an ethylenically unsaturated dicarboxylic acid monomer or a combination thereof, (b) a (meth)acrylamido alkyl or aryl sulfonate monomer; and (c) a third monomer selected from one or more of vinylic compounds, (meth)acrylic esters, vinyl acetate, and substituted (meth)acrylamides.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 2, 2017
    Assignee: Dow Global Technologies LLC
    Inventors: Jing Ji, Ling Zhong, Jianhai Mu
  • Patent number: 9468643
    Abstract: The invention features methods and compositions featuring a PDE5 inhibitor for treating or preventing immunological-mediated disease in a subject.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: October 18, 2016
    Assignee: The Johns Hopkins University
    Inventors: Ivan M. Borrello, Paolo Serafini, Kimberly A. Noonan, Vincenzo Bronte
  • Patent number: 9458195
    Abstract: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: October 4, 2016
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, Jacques-Pierre Moreau
  • Patent number: 9439429
    Abstract: Described is a broad spectrum, synergistic fungicidal composition when used for the preservation of a glued wood product comprising as active ingredients: (A) triadimefon, and (B) cyproconazole characterized in that the weight ratio of (A):(B) is from about 20:1 to about 1:1, the composition being further characterized in that the application rate for the composition is from about 10 gai/m3 to about 6,000 gai/m3.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: September 13, 2016
    Assignee: ZELAM LIMITED
    Inventors: Christopher Molloy, Peter James Hayward, Paul Garry Lobb, George William Mason, Stephen Millward, Wallace James Rae, André Frederik Siraa
  • Patent number: 9422253
    Abstract: A method of treating a disorder such as epilepsy, multiple sclerosis, glaucoma and uveitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia, or trigeminal autonomic cephalalgias. The method includes administering to a subject in need thereof substituted 1,2,4-triazine compounds of formula (I): Each of A, N*, X, Y, Z, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: August 23, 2016
    Assignee: UNIVERSITY OF GREENWICH
    Inventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
  • Patent number: 9386769
    Abstract: Disclosed are thiazole methylamino pyridine compounds represented by the general formula (I) having fungicidal, insecticidal/acaricidal, and herbicidal activity, the preparation method thereof, the fungicidal, insecticidal/acaricidal, and herbicidal compositions containing the compounds of the present invention, and the use and the method for controlling fungi, insects/acari and weeds of the compounds of the present invention.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: July 12, 2016
    Assignee: HUNAN RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD.
    Inventors: Aiping Liu, Xiaoguang Wang, Lian He, Xiaoming Ou, Minhua Liu, Ming Chen, Xingping Liu, Ming Tang, Yeguo Ren, Haobin Chen
  • Patent number: 9346807
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: May 24, 2016
    Assignee: Exelixis, Inc.
    Inventor: Patrick Kearney
  • Patent number: 9340564
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: May 17, 2016
    Assignee: Zoetis Services LLC
    Inventors: Richard A. Ewin, Timothy Allan Johnson, Susan M. K. Sheehan
  • Patent number: 9340523
    Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: May 17, 2016
    Assignee: FOCHON PHARMA, INC.
    Inventors: Weibo Wang, Tongshuang Li
  • Patent number: 9139589
    Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: September 22, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Publication number: 20150133441
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: June 6, 2014
    Publication date: May 14, 2015
    Inventor: Gerard M. Housey
  • Publication number: 20150126474
    Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.
    Type: Application
    Filed: February 20, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
  • Patent number: 9024019
    Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: May 5, 2015
    Assignee: Syngenta Participations AG
    Inventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150105385
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Publication number: 20150098978
    Abstract: A tablet that includes a solid solution of soluble fiber and one or more sugar alcohols, the solid solution having a glass transition temperature of less than 40° C., and one or more additives dispersed in the solid solution such that at least one additive is released from the tablet when the tablet is chewed or dissolved within an oral cavity.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Feng Gao, Diane L. Gee, Phillip M. Hulan, Shuzhong Zhuang, William J. Burke, Gerd Kobal
  • Patent number: 9000155
    Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: in which R1 is a halo-alkyl group and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: April 7, 2015
    Assignee: University Of Greenwich
    Inventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
  • Publication number: 20150094308
    Abstract: The present application relates to novel substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: January 8, 2013
    Publication date: April 2, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Dieter Lang
  • Patent number: 8993566
    Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: March 31, 2015
    Assignee: Wuhan Shengyun Biopharma Co., Ltd.
    Inventor: Hua Xu
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Patent number: 8969554
    Abstract: Disclosed are compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. The compounds are triazine derivatives represented by following Formula 1 or salts thereof, and the herbicides containing them: [Chem. 28] wherein in the formula, R1 represents a hydrogen atom; a C1-C12 alkyl group; a C2-C6 alkenyl group, etc., R2 represents a C1-C12 alkyl group, etc., Y and Z represent an oxygen atom or a sulfur atom, and A represents a 5- or 6-membered cyclic group which may contain a nitrogen atom, an oxygen atom, or a sulfur atom.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: March 3, 2015
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
  • Publication number: 20150050355
    Abstract: A particulate SAE-CD composition is provided. The SAE-CD composition has an advantageous combination of physical properties not found in known solid forms of SAECD. In particular, the SAE-CD composition possesses an advantageous physicochemical and morphological property profile such that it can be tailored to particular uses. The SAE-CD composition of the invention has improved flow and dissolution performance as compared to known compositions of SAE-CD.
    Type: Application
    Filed: September 17, 2014
    Publication date: February 19, 2015
    Inventors: James D. Pipkin, Gerold L. Mosher, Douglas B. Hecker
  • Publication number: 20150045331
    Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Uma Santhanam, Permanan Raaj Khusial
  • Publication number: 20150030704
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 21, 2012
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: William Farnaby, Charlotte Fieldhouse, Katherine Hazel, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller
  • Patent number: 8940891
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 27, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Patent number: 8940774
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 27, 2015
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20150017263
    Abstract: The present disclosure is directed to methods of using fibroblast growth factor-inducible 14 (Fn14) antagonists to modulate activity at a TNF-like weak inducer of apoptosis (TWEAK) binding site on a cysteine-rich domain (CRD) of Fn14. The present disclosure also provides pharmaceutical compositions comprising synergistic combinations Fn14 antagonists and chemotherapeutic agents.
    Type: Application
    Filed: July 9, 2014
    Publication date: January 15, 2015
    Inventors: Nhan Tran, Nathalie Meurice, Harshil Dhruv
  • Publication number: 20150005276
    Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whic
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
  • Publication number: 20140378432
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140371223
    Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.
    Type: Application
    Filed: June 16, 2014
    Publication date: December 18, 2014
    Applicant: Addex Pharma S.A.
    Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
  • Publication number: 20140371221
    Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventor: Hua XU
  • Patent number: 8906919
    Abstract: The present invention relates to a method for slowing the development of mammalian organ, tissue and cellular damage and death by using a persistent sodium current blocker (or a pharmaceutically acceptable salt or derivative thereof). The present invention further relates to a method for preventing damage and death in mammalian organs, tissues and cells or reducing the extent of damage and death in mammalian organs, tissues and cells. In particular the invention relates to a method for the treatment, amelioration or prevention of non-neuronal and non-myocardial cell or tissue damage or death and for reducing the pain associated with non-neuronal and non-myocardial cell or tissue damage.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: December 9, 2014
    Assignee: Ozteo Pty Ltd
    Inventors: Paul Nathaniel Smith, Steven Michael Weiss
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8901170
    Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: December 2, 2014
    Assignee: BASF SE
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
  • Patent number: 8901122
    Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: December 2, 2014
    Assignee: Avon Products, Inc.
    Inventors: Uma Santhanam, Permanan Raaj Khusial
  • Patent number: 8895553
    Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: November 25, 2014
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Publication number: 20140343038
    Abstract: The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally substituted C1-C8 alkyl group, an optionally substituted C2-C6 alkenyl group, an optionally substituted C2-C6 alkynyl group, an optionally substituted C3-C10 cycloalkyl group, an optionally substituted C6-C14 aromatic hydrocarbon group, an optionally substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally substituted 4- to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; and B represents an optionally substituted unsaturated heterocyclic group).
    Type: Application
    Filed: September 28, 2012
    Publication date: November 20, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Sakamoto, Takashi Mita, Kazuaki Shibata, Yoshio Ogino, Hideya Komatani