Asymmetrical (e.g., 1,2,4-triazine, Etc.) Patents (Class 514/242)
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Patent number: 11952366Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular in the treatment of diseases or disorders associated to increased relative to physiological or desired RhoJ/Cdc42 levels of expression or function.Type: GrantFiled: November 23, 2021Date of Patent: April 9, 2024Assignees: Fondazione Istituto Italiano Di TecnologiaInventors: Marco De Vivo, Anand Ganesan, Jose Antonio Ortega Martinez, Sohail Jahid
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Patent number: 11707466Abstract: Described herein, in part, are tablets, such as immediate release multi-layer or bilayer tablets for orally delivering olanzapine and samidorphan, methods of using said tablets in the treatment of disorders described herein, and kits comprising said tablets.Type: GrantFiled: June 30, 2022Date of Patent: July 25, 2023Assignee: Alkermes Pharma Ireland LimitedInventors: Renato A. Chiarella, Hector Guzman, Paul Hurley, David Manser, Kristopher Perkin
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Patent number: 11491120Abstract: Methods for prophylactically treating a stress-induced affective disorder or stress-induced psychopathology in a subject are provided. Also provided are methods for inducing and/or enhancing stress resilience in a subject. In certain embodiments, an effective amount of (R,S)-ketamine or (2R, 6R)-hydroxynorketamine ((2R, 6R)-HNK) is administered to a female or male subject prior to a stressor.Type: GrantFiled: November 9, 2018Date of Patent: November 8, 2022Assignees: The Trustees of Columbia University in the City of New York, The Research Foundation for Mental Hygiene, Inc.Inventors: Christine Ann Denny, Briana Kaying Chen
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Patent number: 11447456Abstract: The invention relates to a crystalline form of lamotrigine hydrate, a method for preparing the same and a composition comprising the same, and in particular, to a lamotrigine hydrate form A, a method for preparing the lamotrigine hydrate form A and a composition comprising the lamotrigine hydrate form A.Type: GrantFiled: July 2, 2021Date of Patent: September 20, 2022Assignee: SHANGHAI AUCTA PHARMACEUTICALS CO., LTD.Inventors: Shoufeng Li, Sr., Yong Wang
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Patent number: 11208389Abstract: 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: GrantFiled: April 29, 2019Date of Patent: December 28, 2021Assignee: GLAX LLCInventors: Rakesh K Srivastava, Sharmila Shankar, Sushant Kumar Shrivastava, Anupam G. Banerjee
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Patent number: 11034647Abstract: 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: GrantFiled: December 9, 2019Date of Patent: June 15, 2021Assignee: The Trustees of Columbia University in the City of New YorkInventors: Yan Feng, Mauro Fa, Ottavio Arancio, Shixian Deng, Donald W. Landry, Yitshak Francis
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Patent number: 10894050Abstract: 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: GrantFiled: July 1, 2019Date of Patent: January 19, 2021Assignees: 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
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Patent number: 10576086Abstract: 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: GrantFiled: June 10, 2016Date of Patent: March 3, 2020Assignee: UNIVERSITY OF GREENWICHInventors: Laurence Harbige, Michael Leach
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Patent number: 10456392Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: GrantFiled: February 6, 2018Date of Patent: October 29, 2019Assignee: Corcept Therapeutics, Inc.Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
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Patent number: 10112913Abstract: 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: GrantFiled: May 4, 2015Date of Patent: October 30, 2018Assignee: BASF SEInventors: 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
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Patent number: 9862712Abstract: 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: GrantFiled: November 20, 2015Date of Patent: January 9, 2018Assignee: Council of Scientific & Industrial ResearchInventors: Pradeep Kumar, Jignesh Kantilal Parikh, Eeshwaraiah Begari
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Patent number: 9826740Abstract: 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: GrantFiled: September 9, 2016Date of Patent: November 28, 2017Assignee: ZELAM LIMITEDInventors: Christopher Molloy, Peter James Hayward, Paul Garry Lobb, George William Mason, Stephen Millward, Wallace James Rae, Andre Frederik Siraa
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Patent number: 9751862Abstract: 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: GrantFiled: March 18, 2015Date of Patent: September 5, 2017Assignee: Syngenta Participations AGInventors: Andre Jeanguenat, Andrew Edmunds, Roger Graham Hall
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Patent number: 9732046Abstract: 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: GrantFiled: July 28, 2015Date of Patent: August 15, 2017Assignee: YM BIOSCIENCES AUSTRALIA PTY LTD.Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Patent number: 9635852Abstract: 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: GrantFiled: December 23, 2013Date of Patent: May 2, 2017Assignee: Dow Global Technologies LLCInventors: Jing Ji, Ling Zhong, Jianhai Mu
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Patent number: 9468643Abstract: The invention features methods and compositions featuring a PDE5 inhibitor for treating or preventing immunological-mediated disease in a subject.Type: GrantFiled: May 19, 2014Date of Patent: October 18, 2016Assignee: The Johns Hopkins UniversityInventors: Ivan M. Borrello, Paolo Serafini, Kimberly A. Noonan, Vincenzo Bronte
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Patent number: 9458195Abstract: 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: GrantFiled: March 29, 2011Date of Patent: October 4, 2016Assignee: Ipsen Pharma S.A.S.Inventors: Zheng Xin Dong, Jacques-Pierre Moreau
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Patent number: 9439429Abstract: 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: GrantFiled: June 22, 2011Date of Patent: September 13, 2016Assignee: ZELAM LIMITEDInventors: Christopher Molloy, Peter James Hayward, Paul Garry Lobb, George William Mason, Stephen Millward, Wallace James Rae, André Frederik Siraa
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Patent number: 9422253Abstract: 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: GrantFiled: February 6, 2014Date of Patent: August 23, 2016Assignee: UNIVERSITY OF GREENWICHInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Patent number: 9386769Abstract: 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: GrantFiled: October 11, 2012Date of Patent: July 12, 2016Assignee: 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
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Patent number: 9346807Abstract: 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: GrantFiled: September 14, 2011Date of Patent: May 24, 2016Assignee: Exelixis, Inc.Inventor: Patrick Kearney
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Patent number: 9340564Abstract: 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: GrantFiled: June 5, 2015Date of Patent: May 17, 2016Assignee: Zoetis Services LLCInventors: Richard A. Ewin, Timothy Allan Johnson, Susan M. K. Sheehan
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Patent number: 9340523Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: GrantFiled: January 3, 2014Date of Patent: May 17, 2016Assignee: FOCHON PHARMA, INC.Inventors: Weibo Wang, Tongshuang Li
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Patent number: 9139589Abstract: 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: GrantFiled: January 28, 2010Date of Patent: September 22, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Patent number: 9040530Abstract: 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: GrantFiled: March 15, 2013Date of Patent: May 26, 2015Assignee: PORTOLA PHARMACEUTICALS, INC.Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
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Publication number: 20150133441Abstract: 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: ApplicationFiled: June 6, 2014Publication date: May 14, 2015Inventor: Gerard M. Housey
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Publication number: 20150126474Abstract: 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: ApplicationFiled: February 20, 2013Publication date: May 7, 2015Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
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Patent number: 9024019Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 20, 2012Date of Patent: May 5, 2015Assignee: Syngenta Participations AGInventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
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Patent number: 9017735Abstract: 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: GrantFiled: June 3, 2010Date of Patent: April 28, 2015Assignee: Marquette UniversityInventor: Mohammadhossein Behnam Ghasemzadeh
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Publication number: 20150105385Abstract: 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: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: 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
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Publication number: 20150098978Abstract: 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: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Feng Gao, Diane L. Gee, Phillip M. Hulan, Shuzhong Zhuang, William J. Burke, Gerd Kobal
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Patent number: 9000155Abstract: 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: GrantFiled: April 30, 2014Date of Patent: April 7, 2015Assignee: University Of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20150094308Abstract: 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: ApplicationFiled: January 8, 2013Publication date: April 2, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Dieter Lang
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Patent number: 8993566Abstract: 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: GrantFiled: August 29, 2014Date of Patent: March 31, 2015Assignee: Wuhan Shengyun Biopharma Co., Ltd.Inventor: Hua Xu
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Patent number: 8987256Abstract: 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: GrantFiled: April 6, 2009Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: 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
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Publication number: 20150072986Abstract: 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: ApplicationFiled: June 11, 2014Publication date: March 12, 2015Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
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Patent number: 8969554Abstract: 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: GrantFiled: May 26, 2011Date of Patent: March 3, 2015Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
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Publication number: 20150050355Abstract: 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: ApplicationFiled: September 17, 2014Publication date: February 19, 2015Inventors: James D. Pipkin, Gerold L. Mosher, Douglas B. Hecker
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Publication number: 20150045331Abstract: 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: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Uma Santhanam, Permanan Raaj Khusial
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Publication number: 20150030704Abstract: 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: ApplicationFiled: August 21, 2012Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: William Farnaby, Charlotte Fieldhouse, Katherine Hazel, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller
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Patent number: 8940774Abstract: 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: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Patent number: 8940891Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: GrantFiled: December 7, 2009Date of Patent: January 27, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou -
Publication number: 20150017263Abstract: 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: ApplicationFiled: July 9, 2014Publication date: January 15, 2015Inventors: Nhan Tran, Nathalie Meurice, Harshil Dhruv
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Publication number: 20150005276Abstract: 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, whicType: ApplicationFiled: July 2, 2014Publication date: January 1, 2015Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Publication number: 20140378432Abstract: 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: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140371221Abstract: 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: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventor: Hua XU
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Publication number: 20140371223Abstract: 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: ApplicationFiled: June 16, 2014Publication date: December 18, 2014Applicant: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Patent number: 8906919Abstract: 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: GrantFiled: June 29, 2010Date of Patent: December 9, 2014Assignee: Ozteo Pty LtdInventors: Paul Nathaniel Smith, Steven Michael Weiss
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Publication number: 20140357599Abstract: 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: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING