The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
  • Publication number: 20130131342
    Abstract: The present invention relates to the field of chemical-pharmaceutical industry and medicine. An agent, exhibiting the properties of a cognitive function promoter, was selected from 1,3-dimethyl-5-[(4-pyridylamino)methylene]barbituric acid and 4-amino-1-(3 -nitro-2-oxo-1-pheny-1 ,2-dihydro-1 ,6-naphthyridin-5-yl)pyridinium chloride. The compounds, that are proposed as agents, exhibit potent biological activity.
    Type: Application
    Filed: April 28, 2011
    Publication date: May 23, 2013
    Applicant: UNIKORM
    Inventors: Valery Aleksandrovich Parshin, Tatyana Vasilyevna Golovko, Nelya Zarifovna Tugusheva, Marina Igorevna Medvedeva, Vladimir Vladimirovich Granik
  • Publication number: 20130123244
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: July 26, 2011
    Publication date: May 16, 2013
    Applicant: JANSSEN R&D IRELAND
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Publication number: 20130115193
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: November 8, 2012
    Publication date: May 9, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8436011
    Abstract: The present invention relates to pyridopyridone derivatives of formula (I): in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the kinase activity of PDGF (platelet-derived growth factor) ligand receptors and possibly of FLT3 (fms-like tyrosine kinase receptor) ligand receptors.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: May 7, 2013
    Assignee: Sanofi
    Inventors: Patrice Bellevergue, Gilbert Lassalle, Gary McCort, Valerie Martin, Pierre Savi, Cecile Volle-Challier
  • Patent number: 8436180
    Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: May 7, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, Elke Hartmann
  • Patent number: 8431039
    Abstract: The present invention relates to compounds represented by the following Formula Ia, in which each R1-R6 can in each case be independently selected from hydrogen or hydrocarbyl (e.g., methyl); R7 is a multivalent linking group, such as L1 is a divalent linking group, such as a bond or divalent optionally substituted hydrocarbyl; each L2 independently represents a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 independently represents a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t is from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; and E can be hydrogen or optionally substituted hydrocarbyl. The present invention also relates to compositions, such as liquid crystal compositions, and articles, such as optical elements, that include the compound represented by Formula Ia.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: April 30, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Xiao-Man Dai, Ruisong Xu, Meng He, Anil Kumar, Rachael L. Yoest, Chenguang Li
  • Patent number: 8431594
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: April 30, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Publication number: 20130102603
    Abstract: The present invention relates to novel [1,8]naphthyridine 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: Application
    Filed: May 31, 2011
    Publication date: April 25, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Publication number: 20130102611
    Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.
    Type: Application
    Filed: July 14, 2011
    Publication date: April 25, 2013
    Applicant: Novartis AG
    Inventors: Steven John Charlton, Catherine Leblanc, Stephen Carl McKeown
  • Publication number: 20130096122
    Abstract: 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: Application
    Filed: December 6, 2012
    Publication date: April 18, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8415333
    Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 9, 2013
    Assignee: Respiratorious AB
    Inventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
  • Patent number: 8415375
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: April 9, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 8410273
    Abstract: Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: April 2, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Satoru Naito
  • Patent number: 8410109
    Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: April 2, 2013
    Assignee: Resverlogix Corp.
    Inventors: Norman C. W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
  • Publication number: 20130079365
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 A3 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 28, 2013
    Inventors: Johannes Aebi, Kurt Amrein, Serena Maria Fantasia, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Michelangelo Scalone, Xuefei Tan, Mingwei Zhou
  • Publication number: 20130072494
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 21, 2013
    Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • Publication number: 20130072679
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Henner Knust, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Mingwei Zhou
  • Publication number: 20130065760
    Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.
    Type: Application
    Filed: March 22, 2011
    Publication date: March 14, 2013
    Applicant: BASF SE
    Inventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Hans Wolfgang Hoeffken, Thomas Mietzner, William Karl Moberg
  • Publication number: 20130053348
    Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
    Type: Application
    Filed: September 12, 2012
    Publication date: February 28, 2013
    Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
  • Publication number: 20130040984
    Abstract: The present invention relates to 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 and/or basophil 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, chronic spontaneous urticaria and autoimmune conditions.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Francis Louis Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander George Steven Preston, David Matthew Wilson
  • Publication number: 20130035326
    Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 18, 2010
    Publication date: February 7, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
  • Publication number: 20130029994
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: July 20, 2012
    Publication date: January 31, 2013
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Publication number: 20130029982
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: July 18, 2012
    Publication date: January 31, 2013
    Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 8357688
    Abstract: Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: January 22, 2013
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
  • Patent number: 8357684
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 22, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
  • Publication number: 20130018046
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
  • Patent number: 8349830
    Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
  • Publication number: 20130005724
    Abstract: The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases.
    Type: Application
    Filed: May 22, 2012
    Publication date: January 3, 2013
    Applicant: SANOFI
    Inventors: Gilbert LASSALLE, Valérie MARTIN, Gary MCCORT, Cécile VOLLE-CHALLIER
  • Publication number: 20130005760
    Abstract: A heterocyclic compound of formula (I) or a salt thereof: wherein R1 is an optionally protected amino group or an optionally substituted C1-6 alkyl group; R2 and R3 are each independently a C1-2 alkyl group; X is a hydrogen atom or a halogen atom; Z1 is N or C—R4; Z2 is N or C—R5; Z3 is N or C—R6; Z4 is N or C—R7; R4, R5, R6, and R7 are each independently a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group; Z is CH or N; and A is a methylene group or a bond, which has an excellent anti-HIV activity and is useful as an anti-HIV agent.
    Type: Application
    Filed: January 20, 2011
    Publication date: January 3, 2013
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Yuji Oonishi, Kenichiro Awasaguchi, Nobuhiko Nomura, Keisuke Tohdo, Hyouei Kawai, Tomomi Wakatsuki
  • Patent number: 8343996
    Abstract: The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: January 1, 2013
    Assignee: AstraZeneca AB
    Inventor: Mark E. Duggan
  • Patent number: 8338605
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: December 25, 2012
    Assignee: Abbott Laboratories
    Inventors: Todd W. Rockway, David A. Betebenner, Allan C. Krueger, Nobuhiko Iwasaki, Curt S. Cooper, David D. Anderson, Dale J. Kempf, Darold L. Madigan, Christopher E. Motter, Jason P. Shanley, Michael D. Tufano, Rolf Wagner, Rong Zhang, Akteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V. L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
  • Publication number: 20120322785
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Application
    Filed: December 14, 2011
    Publication date: December 20, 2012
    Applicant: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
  • Patent number: 8334294
    Abstract: New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: December 18, 2012
    Assignee: Almirall, S.A.
    Inventors: Wenceslao Lumeras Amador, Paul Robert Eastwood
  • Publication number: 20120316166
    Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: January 10, 2011
    Publication date: December 13, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
  • Publication number: 20120302576
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.
    Type: Application
    Filed: August 9, 2012
    Publication date: November 29, 2012
    Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
  • Publication number: 20120295902
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: December 17, 2010
    Publication date: November 22, 2012
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Publication number: 20120289702
    Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.
    Type: Application
    Filed: December 28, 2010
    Publication date: November 15, 2012
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
  • Patent number: 8309734
    Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: November 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
  • Publication number: 20120258957
    Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 11, 2012
    Inventors: Matilda Jane Bingham, Andrew Dunbar, Margaret Jean Laats, Grant Wishart
  • Publication number: 20120258947
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2012
    Publication date: October 11, 2012
    Applicant: Grunenthal GmbH
    Inventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Publication number: 20120252809
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 24, 2012
    Publication date: October 4, 2012
    Applicant: SANOFI
    Inventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
  • Publication number: 20120252814
    Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: March 21, 2012
    Publication date: October 4, 2012
    Applicant: TAKEDA CALIFORNIA, INC.
    Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
  • Publication number: 20120252780
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 29, 2010
    Publication date: October 4, 2012
    Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
  • Publication number: 20120252806
    Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: December 9, 2010
    Publication date: October 4, 2012
    Inventors: Michael J. Kelly, III, Mark E. Layton
  • Patent number: 8278452
    Abstract: The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR? and PDGFR? kinases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: October 2, 2012
    Assignee: IRM LLC
    Inventors: Donatella Chianelli, Xiaolin Li, Xiaodong Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Vince Yeh
  • Patent number: 8278337
    Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme
    Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
  • Publication number: 20120245152
    Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
    Type: Application
    Filed: August 27, 2010
    Publication date: September 27, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Shinagawa-ku, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
  • Patent number: 8268803
    Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
  • Publication number: 20120232052
    Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.
    Type: Application
    Filed: November 16, 2010
    Publication date: September 13, 2012
    Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
  • Publication number: 20120226035
    Abstract: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.
    Type: Application
    Filed: May 10, 2012
    Publication date: September 6, 2012
    Applicants: Taisho Pharmaceutical Co., Ltd., Toyama Chemical Co., Ltd.
    Inventors: Taro KIYOTO, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri