Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
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Publication number: 20150133422Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.Type: ApplicationFiled: November 8, 2013Publication date: May 14, 2015Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
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Publication number: 20150126487Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH? or —N?, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.Type: ApplicationFiled: February 28, 2013Publication date: May 7, 2015Inventors: Hiroki Sakamoto, Takahiro Sugimoto
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Patent number: 9023848Abstract: The present invention provides compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful in treating central nervous system disorders, such as anxiety disorders or depression.Type: GrantFiled: March 2, 2012Date of Patent: May 5, 2015Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Dharam Paul, Andrew John Harvey, Damian Wojciech Grobelny, Sue O'Connor, Jonathan Bayldon Baell, Brad Sleebs, Ian Phillip Street
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Publication number: 20150119394Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.Type: ApplicationFiled: March 14, 2013Publication date: April 30, 2015Inventors: Abhijit Roychowdhury, Rajiv Sharma, Malcolm Mascarenhas, Chandrika B-Rao, Shashikant M. Patil, Sambhaji Chavan, Nitin Lad, Smriti Khanna, Christopher J. Dinsmore
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Publication number: 20150119383Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: June 5, 2014Publication date: April 30, 2015Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
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Publication number: 20150111885Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Publication number: 20150111886Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
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Publication number: 20150111890Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: April 19, 2013Publication date: April 23, 2015Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
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Publication number: 20150111870Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 14, 2014Publication date: April 23, 2015Applicant: JOHNSON & JOHNSONInventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS, KELLY MCCLURE, VIRGINIA TANIS
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Patent number: 9012443Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 6, 2012Date of Patent: April 21, 2015Assignee: Amgen Inc.Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
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Publication number: 20150105370Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
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Publication number: 20150105366Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
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Publication number: 20150105384Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 9, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Simon Stewart Jones, Min Yang, David Lee Tamang
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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: 20150105376Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Patent number: 9006241Abstract: The invention provides novel pyrimidine derivatives of formula (I), methods of preparing such compounds, pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer; wherein R1-R11, Z, and Y are as defined in the specification.Type: GrantFiled: March 23, 2012Date of Patent: April 14, 2015Assignee: Noviga Research ABInventors: Marita Högberg, Emma Dahlstedt, Olof Smitt, Tommy Johansson
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Patent number: 9006276Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: September 23, 2011Date of Patent: April 14, 2015Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20150099732Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: ApplicationFiled: March 7, 2013Publication date: April 9, 2015Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
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Publication number: 20150099736Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituType: ApplicationFiled: November 10, 2014Publication date: April 9, 2015Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
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Publication number: 20150099746Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: October 16, 2014Publication date: April 9, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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FORMULATIONS OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE
Publication number: 20150099745Abstract: Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and/or an immune-related disorder.Type: ApplicationFiled: October 7, 2014Publication date: April 9, 2015Inventors: Darshan Parikh, Anil Menon -
Patent number: 8999982Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 26, 2011Date of Patent: April 7, 2015Assignees: Lead Discovery Center GmbH, Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
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Patent number: 8993565Abstract: The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.Type: GrantFiled: June 23, 2014Date of Patent: March 31, 2015Assignee: SanofiInventors: Jean-Christophe Carry, Victor Certal, Frank Halley, Karl Andreas Karlsson, Laurent Schio, Fabienne Thompson
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Patent number: 8993554Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.Type: GrantFiled: April 19, 2012Date of Patent: March 31, 2015Assignee: GlaxoSmithKline LLCInventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
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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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Publication number: 20150087645Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: ApplicationFiled: October 7, 2014Publication date: March 26, 2015Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Publication number: 20150086629Abstract: Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.Type: ApplicationFiled: April 25, 2014Publication date: March 26, 2015Applicant: Supernus Pharmaceuticals, Inc.Inventors: Rong-Kun Chang, Michael L. Vieira, Likan LIANG, Padmanabh P. BHATT, Austin B. HUANG, Sachin V. PATEL
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Publication number: 20150087617Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.Type: ApplicationFiled: April 2, 2013Publication date: March 26, 2015Inventors: Abraham Nudelman, Marta Weinstock-Rosin
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Publication number: 20150080395Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R and R6 are each independently (LQ)mY; R4 is H, halogen, optionally substituted aryl or optionally substituted alkyl; and; each X is independently CR7 or N. The compounds are PI3K inhibitors and therefore have potential utility in therapy.Type: ApplicationFiled: March 8, 2013Publication date: March 19, 2015Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva
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Publication number: 20150080394Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: ApplicationFiled: March 25, 2014Publication date: March 19, 2015Applicant: COLUMBIA UNIVERSITYInventors: Yan FENG, Ottavio ARANCIO, Shixian DENG, Donald W. LANDRY
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Publication number: 20150080381Abstract: Method of treating alopecia and acne with are disclosed.Type: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Inventors: Mark G. Currie, Yueh-tyng Chien
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Publication number: 20150072955Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: October 14, 2014Publication date: March 12, 2015Applicant: Resverlogix Corp.Inventor: Henrik C. Hansen
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Publication number: 20150071919Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Patients to be treated include those that have been treated with Tarceva or other therapeutic compounds and relapsed or are resistant to treatment. The compounds described herein may exhibit a synergistic effect when administered with another agent.Type: ApplicationFiled: September 9, 2014Publication date: March 12, 2015Inventors: Thomas F. WHITE, Dan HOTH
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Publication number: 20150065489Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: October 30, 2014Publication date: March 5, 2015Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Publication number: 20150065502Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: ApplicationFiled: April 26, 2013Publication date: March 5, 2015Inventors: Jerome Emile Georges Guillemont, Magali Madeleine Simone Motte, David Francis Alain Lançois, Wendy Mia Albert Balemans
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Publication number: 20150057278Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: September 10, 2012Publication date: February 26, 2015Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Patent number: 8957070Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.Type: GrantFiled: April 20, 2006Date of Patent: February 17, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Osamu Ujikawa
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Publication number: 20150045362Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: ApplicationFiled: August 25, 2014Publication date: February 12, 2015Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
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Publication number: 20150045354Abstract: The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Inventors: Ian Hugh Gilbert, Neil Norcross, Beatriz Baragana Ruibal, Achim Porzelle
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Patent number: 8952007Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.Type: GrantFiled: December 10, 2013Date of Patent: February 10, 2015Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
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Publication number: 20150038511Abstract: Provided herein are methods of using compounds and compositions for modulating leukocytic activity, including activity of B cells and/or T cells monocytes, macrophages, and other lymphoid or myeloid-derived cell types, in immune-related diseases or inflammatory diseases. Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.Type: ApplicationFiled: May 19, 2014Publication date: February 5, 2015Inventors: PETER H. SCHAFER, YING YE, DONNA J. SUTHERLAND, RAJESH CHOPRA, ANITA GANDHI
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Publication number: 20150031696Abstract: The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions.Type: ApplicationFiled: May 28, 2014Publication date: January 29, 2015Applicant: FIBROGEN, INC.Inventors: Michael Arend, Lee A. Flippin, Min Wu, Eric D. Turtle, Wen-Bin Ho, Shaojiang Deng
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Publication number: 20150031672Abstract: 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: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150031673Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
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Patent number: 8940737Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: October 11, 2012Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
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Patent number: 8940724Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: GrantFiled: June 25, 2010Date of Patent: January 27, 2015Assignee: Amgen Inc.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Patent number: 8940784Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: GrantFiled: February 2, 2007Date of Patent: January 27, 2015Assignee: Syntarga B.V.Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus de Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
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Publication number: 20150018310Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: September 29, 2014Publication date: January 15, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster