1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • SUBSTITUTED 4-(1H-PYRAZOL-4-YL)BENZYL ANALOGUES AS POSITIVE ALLOSTERIC MODULATORS OF MACHR M1 RECEPTORS
    Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • (1-AZINONE)-SUBSTITUTED PYRIDOINDOLES
    Publication number: 20140206696
    Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark HADDEN, James GRABOWSKI, Alexander USYATINSKY
  • CYCLIC PROTEIN TYROSINE KINASE INHIBITORS
    Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
    Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • 7-phenoxychroman carboxylic acid derivatives
    Patent number: 8785445
    Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 22, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
  • HETEROCYCLIC-SUBSTITUTED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20140199263
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
    Publication number: 20140200207
    Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 17, 2014
    Applicant: Signal Pharmaceutical LLC
    Inventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
  • SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
    Publication number: 20140200206
    Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 17, 2014
    Applicant: Signal Pharmaceutical LLC
    Inventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
  • NOVEL POLYMORPHIC FORMS OF 3-(1--6-OXO-1,6-DIHYDRO-PYRIDAZIN-3-YL)-BENZONITRILE HYDROCHLORIDE SALT AND PROCESSES OF MANUFACTURING THEREOF
    Publication number: 20140200221
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 17, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Axel BECKER, Clemens KUEHN, Christoph SAAL, Oliver SCHADT, Dieter DORSCH, Heinz-Hermann BOKEL, Frank STIEBER, Cristina DONINI
  • N-LINKED QUINOLINEAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20140200222
    Abstract: The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: July 17, 2014
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Zhi-Qiang Yang
  • Pyridazinone compounds
    Patent number: 8778944
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: July 15, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Akira Kawada, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
  • Arylalkylamine compound and process for preparing the same
    Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • HETEROCYCLIC GLUTAMINASE INHIBITORS
    Publication number: 20140194421
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: November 15, 2013
    Publication date: July 10, 2014
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • HETEROARYLMETHYL AMIDES
    Publication number: 20140194436
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: February 24, 2014
    Publication date: July 10, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Multicyclic compounds and methods of their use
    Patent number: 8772291
    Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
  • Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
    Patent number: 8772323
    Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM
    Publication number: 20140187543
    Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
    Type: Application
    Filed: September 25, 2013
    Publication date: July 3, 2014
    Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
  • PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
    Publication number: 20140179673
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: GILEAD CALISTOGA LLC
    Inventors: Jerry EVARTS, Leena PATEL, Jennifer A. TREIBERG, Stephane PERREAULT, Arthur YEUNG, Lafe J. PURVIS, II, Musong KIM
  • RADIOLABELED COMPOUNDS AND THEIR USE AS RADIOTRACERS FOR QUANTITATIVE IMAGING OF PHOSPHODIESTERASE (PDE10A) IN MAMMALS
    Publication number: 20140178304
    Abstract: The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.
    Type: Application
    Filed: August 21, 2012
    Publication date: June 26, 2014
    Inventors: Takahiko Taniguchi, Shotaro Miura, Tomoaki Hasui, Christer Halldin, Vladimir Stepanov, Akihiro Takano
  • BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
    Publication number: 20140179666
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 26, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Novel Heterocyclic Compounds as Bromodomain Inhibitors
    Publication number: 20140179648
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • Use of 4-(pyrrolidin-1-yl)quinoline compounds to kill clinically latent microorganisms
    Patent number: 8759348
    Abstract: There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: June 24, 2014
    Assignee: Helperby Therapeutics Limited
    Inventors: Mandy Christine Beswick, Susan Mary Cramp, Yanmin Hu, Thomas David Pallin, Hazel Joan Dyke, Anthony Coates
  • Substituted bicyclic amines for the treatment of diabetes
    Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20140171408
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum MacLeod, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang
  • TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
    Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • HISTONE DEMETHYLASE INHIBITORS
    Publication number: 20140171432
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 19, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • PYRIDIN-2(1H)-ONE DERIVATIVES USEFUL AS MEDICAMENTS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS, TRANSPLANT REJECTION, IMMUNE-MEDIATED AND INFLAMMATORY DISEASES
    Publication number: 20140170110
    Abstract: Compounds having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: May 21, 2012
    Publication date: June 19, 2014
    Applicant: ALMIRALL, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
  • Indazole derivatives or pharmaceutically acceptable salts thereof as protein kinase inhibitors for proliferative diseases treatment, and a pharmaceutical composition containing the same as an active ingredient
    Patent number: 8754209
    Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: June 17, 2014
    Assignees: Korea Institute of Science and Technology, Korea Research Institute of Chemical Technology, Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
  • Carbamate/urea derivatives
    Publication number: 20140163036
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: July 17, 2013
    Publication date: June 12, 2014
    Inventors: Yves AUBERSON, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT
    Publication number: 20140163226
    Abstract: The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.
    Type: Application
    Filed: June 29, 2012
    Publication date: June 12, 2014
    Applicant: HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Chul Hyun Park, Won Jeoung Kim, Young Hee Jung, Nam Du Kim, Young Kil Chang, Maeng Sup Kim
  • PYRIDO-/AZEPINO-BENZOFURAN AND PYRIDO-/AZEPINO-BENZOTHIOPHENE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
    Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Inhibitors of diacylglycerol acyl transferase
    Patent number: 8748426
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: June 10, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Microbicidal heterocycles
    Patent number: 8748431
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Syngenta Participations AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • NOVEL COMPOUNDS
    Publication number: 20140155375
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 5, 2014
    Applicant: GlaxoSmithKline Interllectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • AMIDINE COMPOUND OR SALT THEREOF
    Publication number: 20140155597
    Abstract: The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori
  • SELECTIVE CYP11B1 INHIBITORS FOR THE TREATMENT OF CORTISOL DEPENDENT DISEASES
    Publication number: 20140155407
    Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.
    Type: Application
    Filed: October 21, 2011
    Publication date: June 5, 2014
    Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
  • Arlethynyl Derivatives
    Publication number: 20140155602
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: November 20, 2013
    Publication date: June 5, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • NOVEL SUBSTITUTED BIPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE RECEPTOR LIGANDS
    Publication number: 20140155401
    Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
  • 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS
    Publication number: 20140155385
    Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 11, 2012
    Publication date: June 5, 2014
    Inventors: Tjeerd A. Barf, Christian Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C.A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C.H.M. Wijkmans
  • PYRAZOLO[1,5-A]PYRIMIDINES FOR ANTIVIRAL TREATMENT
    Publication number: 20140154240
    Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: May 30, 2013
    Publication date: June 5, 2014
    Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
  • HETEROCYCLE AMINES AND USES THEREOF
    Publication number: 20140155379
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 5, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • Triazole compounds I
    Patent number: 8742097
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Maria-Clemencia Hernandez, Matthew C. Lucas, Andrew Thomas
  • INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
    Publication number: 20140148462
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 25, 2013
    Publication date: May 29, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
  • Pyrazole Compounds for Controlling Invertebrate Pests
    Publication number: 20140142111
    Abstract: The present invention relates to pyrazole compounds of formulae I or II and the salts and N-oxides thereof, wherein A is a pyrazole radical of formulae A1, A2 or A3, wherein # denotes the binding site: R1, W, V, U, T, R41, R42, R43, R51, R52, R53, R61, R62, R63, X1, X2 are as defined herein. The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.
    Type: Application
    Filed: November 14, 2013
    Publication date: May 22, 2014
    Applicant: BASF SE
    Inventors: Steffen GROSS, Karsten KOERBER, Wolfgang von DEYN, Florian KAISER, Prashant DESHMUKH, Joachim DICKHAUT, Ronan LE VEZOUET, Sebastian SOERGEL, Matthias POHLMAN, Douglas D. ANSPAUGH, Deborah L. CULBERTSON, Hassan OLOUMI-SADEGHI
  • PYRIDINE-AND PYRAZINE DERIVATIVES
    Publication number: 20140142097
    Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
    Type: Application
    Filed: April 11, 2012
    Publication date: May 22, 2014
    Applicant: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
  • TRIAZOLOPYRAZINE
    Publication number: 20140142098
    Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Christian SMETHURST
  • SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
    Publication number: 20140142108
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 22, 2014
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20140142088
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
    Type: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
  • COMPOUNDS FOR THE TREATMENT OF HIV
    Publication number: 20140142085
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: July 5, 2012
    Publication date: May 22, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • COMPOUNDS AND THEIR METHODS OF USE
    Publication number: 20140142081
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 22, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen