Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Patent number: 8623869Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: GrantFiled: June 23, 2011Date of Patent: January 7, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Joanne Pinder, Ronald Marcellus Alphonsus Knegtel, Steven John Durrant, Damien Fraysse, Somhairle MacCormick, Anisa Nizarali Virani, Philip Michael Reaper
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Patent number: 8623862Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: GrantFiled: September 13, 2011Date of Patent: January 7, 2014Assignee: SanofiInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Publication number: 20140005200Abstract: The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.Type: ApplicationFiled: February 9, 2012Publication date: January 2, 2014Applicant: Janssen Pharmaceutica NVInventors: Andrés Avelino Trabanco-Suárez, Henricus Jacobus Maria Gijsen, Michiel Luc Maria Van Gool, Juan Antonio Vega Ramiro, Francisca Delgado-Jiménez
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Publication number: 20140005201Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgård
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Publication number: 20140005103Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.Type: ApplicationFiled: June 25, 2013Publication date: January 2, 2014Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
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Publication number: 20140005188Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.Type: ApplicationFiled: March 8, 2012Publication date: January 2, 2014Applicant: GLAXO GROUP LIMITEDInventors: Francis Louis Atkinson, Stephen John Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander G. Preston, Tracy Jane Shipley, David Matthew Wilson, Robert J. Watson
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Publication number: 20140005193Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Frances Meredith Hocutt, BARRY EASTMAN LEONARD, JR., HILLARY M. PELTIER, VICTOR K. PHUONG, MICHAEL H. RABINOWITZ, MARK D. ROSEN, KYLE T. TARANTINO, HARIHARAN VENKATESAN, LUCY XIUMIN ZHAO
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Publication number: 20140005394Abstract: The present invention provides a method which enables the simple, economical and high-yield production which is a key intermediate of antidiabetic drug Januvia.Type: ApplicationFiled: January 18, 2012Publication date: January 2, 2014Applicant: ST PHARM CO., LTDInventors: Geun Gho Lim, Sun Ki Chang, Chang Ho Byeon
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Patent number: 8618103Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 9, 2010Date of Patent: December 31, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
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Publication number: 20130345206Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Publication number: 20130345227Abstract: The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: February 13, 2012Publication date: December 26, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20130345205Abstract: In one aspect, the invention relates to substituted bicyclic aralkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
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Publication number: 20130345226Abstract: There are provided compounds of the formula wherein R1 and R2 are as described herein. The compounds are useful as anticancer agents.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Johannes Hermann, Ann Catherine Petersen, Jutta Wanner, Lin Yi
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Publication number: 20130345203Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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SUBSTITUTED BICYCLIC CYCLOALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
Publication number: 20130345204Abstract: In one aspect, the invention relates to substituted bicyclic cycloalkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong -
Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Patent number: 8609689Abstract: The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: GrantFiled: September 13, 2012Date of Patent: December 17, 2013Assignee: Merck Patent GmbHInventors: Gerard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
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Patent number: 8604196Abstract: A method of modulating one or more of ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and SAPK signal transduction pathway with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2,3-b]pyrazine-6-yl]thiourea, its geometric isomer, or its tautomer.Type: GrantFiled: July 5, 2012Date of Patent: December 10, 2013Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Publication number: 20130324527Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: December 16, 2011Publication date: December 5, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdella Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Publication number: 20130317213Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
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Patent number: 8592423Abstract: PDE10 inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit PDE10 are also disclosed.Type: GrantFiled: June 18, 2012Date of Patent: November 26, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, S. Roy Kimura
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Patent number: 8592422Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 16, 2011Date of Patent: November 26, 2013Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
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Publication number: 20130310391Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: January 9, 2012Publication date: November 21, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J.J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20130303507Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Applicant: Novartis AGInventors: William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
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Publication number: 20130303511Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Applicant: AbbVie Inc.Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
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Publication number: 20130303517Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Christopher W. Boyce, Sylvia Joanna Degrado, Xiao Chen, Jun Qin, Robert D. Mazzola, JR., Younong Yu, Kevin D. McCormick, Anandan Palani, Dong Xiao, Robert George Aslanian, Jie Wu, Ashwin Umesh Rao, Phieng Siliphaivanh, Joey L. Methot, Hongjun Zhang, Elizabeth Helen Kelley, William Colby Brown, Qin Jiang, Jolicia Polivina Gauuan, Andrew J. Leyhane, Purakkattle Johny Biju, Pawan K. Dhondi, Li Dong, Salem Fevrier, Xianhai Huang, Henry M. Vaccaro
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Publication number: 20130303370Abstract: The present invention provides a compound of formula (I) wherein R4 is of sub-formula (a) or (b) and wherein the other substituents are as defined in the specification. The compounds of formula (I) are potentially useful as herbicides.Type: ApplicationFiled: October 14, 2011Publication date: November 14, 2013Applicants: SYNGENTA LIMITED, SYNGENTA PARTICIPATIONS AGInventors: Alaric James Avery, Alain De Mesmaeker, Nicholas Phillip Mulholland, Nigel James Willetts, Paul Anthony Worthington
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Publication number: 20130303532Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 13, 2011Publication date: November 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Publication number: 20130296320Abstract: Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.Type: ApplicationFiled: January 6, 2012Publication date: November 7, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Publication number: 20130296565Abstract: A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: H. Scott WILKINSON, Richard HSIA, Tushar MISRA, Kostas SARANTEAS, Patrick MOUSAW
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Publication number: 20130296557Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animalsType: ApplicationFiled: January 23, 2012Publication date: November 7, 2013Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
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Patent number: 8575337Abstract: The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: June 23, 2009Date of Patent: November 5, 2013Assignee: Research Foundation Itsuu LaboratoryInventors: Issei Katoh, Toshiaki Aoki, Hideyuki Suzuki, Iwao Utsunomiya, Norikazu Kuroda, Tsutomu Iwaki
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Publication number: 20130289271Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: June 26, 2013Publication date: October 31, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Elizabeth Fultz, Rama Narla, Sabita Sankar, Jan Elsner
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Publication number: 20130287687Abstract: The present disclosure relates to organic chemistry and in particular to a series of corticotropin releasing factor type-1 (CRF1) receptor ligand compounds and compositions, as well as methods of preparation and treatment.Type: ApplicationFiled: April 30, 2013Publication date: October 31, 2013Inventor: EMORY UNIVERSITY
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Publication number: 20130289276Abstract: The invention provides a process for preparing 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (Formula I), into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms comprising: a) reacting 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-one of formula (III) with a suitable oxidoreductase enzymes or its suitable variants in the presence of suitable conditions and co-factor; and b) isolating 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one, into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms.Type: ApplicationFiled: October 10, 2011Publication date: October 31, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Sanjeev Kumar Mendirata, Bipin Pandey, Rupal Joshi, Umang Trivedi, Mayank G. Dave, Himanshu M. Kothari, Bhavin Shukla
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Patent number: 8569301Abstract: The present invention relates to 6,6-dioxo-6-thia-1,4-diaza-naphthalene derivatives of formula (I) where R1, R2, R3a, R3b, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to control plant growth.Type: GrantFiled: May 6, 2010Date of Patent: October 29, 2013Assignee: Syngenta LimitedInventors: Nigel James Willetts, Nicholas Phillip Mulholland, Paul Anthony Worthington, Alaric James Avery
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Patent number: 8569300Abstract: The present invention relates to substituted tetrazolo[1,5-a]pyrazine compounds for Formula IX: as well as pharmaceutical compositions thereof, which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: GrantFiled: March 10, 2011Date of Patent: October 29, 2013Assignee: Kalypsys Inc.Inventors: Allen Borchardt, Robert Davis, Stewart A. Noble
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Patent number: 8569494Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: GrantFiled: October 25, 2010Date of Patent: October 29, 2013Assignee: Signal Pharmaceuticals, LLCInventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip James Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
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Publication number: 20130281460Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): (I) in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 13, 2011Publication date: October 24, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130281690Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 24, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130281695Abstract: Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.Type: ApplicationFiled: December 1, 2011Publication date: October 24, 2013Applicant: ZHEJIANG HISOAR PHARMACEUTICAL CO., LTD.Inventors: Xianhua Pan, Weijin Li, Qunhui Zhang, Libo Ruan, Wansheng Yu, Fei Deng, Tianhua Ma, Mingwang Huang, Minhuan He
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Publication number: 20130281432Abstract: Pyridone and pyrazinone compounds of Formula I 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 compounds of Formula I 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: August 31, 2011Publication date: October 24, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
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Patent number: 8563554Abstract: This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel, such as compounds of formula (I): or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.Type: GrantFiled: March 16, 2010Date of Patent: October 22, 2013Assignee: Concert Pharmaceuticals, Inc.Inventors: Julie F. Liu, Scott L. Harbeson, Roger Tung
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Publication number: 20130274109Abstract: The present invention provides substituted pyrazine compounds of the formula I or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula I are defined as in the description. Substituted pyrazines of formula I are useful as herbicides.Type: ApplicationFiled: December 23, 2011Publication date: October 17, 2013Applicant: BASF SEInventors: Ruediger Reingruber, Helmut Kraus, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Gilbert Besong, Michael Rack, Andree Van Der Kloet, Thomas Seitz, Jens Lerchl, Klaus Kreuz, Klaus Grossmann, Richard Roger Evans
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Publication number: 20130274469Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130274239Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: May 8, 2013Publication date: October 17, 2013Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. A. Kiryanov
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Publication number: 20130274266Abstract: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.Type: ApplicationFiled: December 21, 2011Publication date: October 17, 2013Applicant: Janssen Pharmaceutica NVInventors: Andres Avelino Trabanco-Suárez, Francisca Delgado-Jiménez, Juan Antonio Vega Ramiro, Gary John Tresadern, Henricus Jacobus Maria Gijsen, Daniel Oehlrich