Polycyclo Ring System Having The Additional Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.06)
  • Patent number: 10329303
    Abstract: The invention provides compounds that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 25, 2019
    Assignee: The Scripps Research Institute
    Inventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
  • Patent number: 10214544
    Abstract: The present invention provides imidazopyridazine compounds or imidazothiadiazole compounds of Formula I having the structure: (I) wherein X1, X2, X3, X4, X5, Y, W, R1, R2, R3, R4, R5 and (II) are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: February 26, 2019
    Assignee: Universite De Montreal
    Inventor: Jacques Banville
  • Patent number: 9616134
    Abstract: A liquid preparation includes an etherified cyclodextrin derivative and a substituted benzimidazol, where the etherified cyclodextrin derivative is one of alpha-, beta, and gamma-cyclodextrin ether.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: April 11, 2017
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin Folger, Stefan Lehner
  • Patent number: 9521850
    Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: December 20, 2016
    Assignee: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INCORPORATED
    Inventors: Nian Wang, Nagaraju Akula
  • Patent number: 9242991
    Abstract: This invention relates to certain novel fused quinazoline derivatives (Formula I) as c-Met inhibitors which is shown as formula I, their synthesis and their use for treating a c-Met mediated disorder.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 26, 2016
    Assignee: BETTA PHARMACEUTICALS CO., LTD
    Inventors: Shaojing Hu, Fei Wang, Wei Long, Xiaoyan Shen, Fenlai Tan, Yinxiang Wang
  • Publication number: 20150148335
    Abstract: The invention relates to a liquid formulation comprising propylene glycol and an effective amount of an inodilator, an angiotensin converting enzyme inhibitor, or a combination of an inodilator and an angiotensin converting enzyme inhibitor and to use of the formulation for treating cardiac disease and/or hypertension.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 28, 2015
    Inventors: Nicholas Bova, Stephen Page, Giuseppe Pippia
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150119402
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Inventor: Derk Hogenkamp
  • Patent number: 9012445
    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: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8987273
    Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacture and their use for the treatment of benign and malignant neoplasia.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
  • Patent number: 8987250
    Abstract: 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: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: 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
  • Patent number: 8980894
    Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patients having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having symptomatic or asymptomatic (occult) heart failure.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: March 17, 2015
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann, Christian Troetschel, Andrea Vollmar
  • Patent number: 8975260
    Abstract: Pyridazinone 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: Grant
    Filed: August 31, 2011
    Date of Patent: March 10, 2015
    Assignees: Genetech, Inc, Gilead Connecticut, Inc.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
  • Patent number: 8962580
    Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: February 24, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
  • Publication number: 20150025082
    Abstract: The present invention is directed to a preserved liquid aqueous pharmaceutical composition comprising one or more etherified cyclodextrin derivatives; one or more water-soluble preservatives; preferably selected from the group consisting of sorbic acid or salts thereof, preferably sodium sorbate, potassium sorbate, calcium sorbate; benzoic acid or salts thereof, preferably sodium benzoate; benzalkonium chloride; benzethonium chloride; cetylpyridinium chloride; sodium metabisulfite; sodium acetate; parabenes and salts thereof, preferably methylparabene, ethylparabene, propylparabene, butylparabene, butylparabene sodium; or combinations thereof; and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Michael AVEN, Tim LUKAS
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Publication number: 20140363510
    Abstract: A solid formulation includes pimobendan or a pharmaceutically acceptable salt thereof, which is homogenously dispersed with a polyvalent acid and a flavor suitable to animals.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Martin A. Folger, Bernhard Hassel, Stefan Henke, Jens Lehmann
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Publication number: 20140349990
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Patent number: 8883788
    Abstract: Provided is a compound having a PDE10A inhibitory action, and useful as a medicament for the prophylaxis or treatment of mental diseases such as schizophrenia and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: November 11, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomoaki Hasui, Makoto Fushimi, Hironori Kokubo, Takenori Hitaka, Shotaro Miura, Takahiko Taniguchi
  • Publication number: 20140315856
    Abstract: A method for treating cancer that includes administering a pharmaceutically effective amount of a composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.
    Type: Application
    Filed: June 6, 2014
    Publication date: October 23, 2014
    Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
  • Patent number: 8865719
    Abstract: The present invention is related to heterocycles represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs and/or GABAA receptors. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs and negative allosteric modulation of GABAA receptors in a mammal by administering an effective amount of a compound of Formula I.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 21, 2014
    Assignee: The Regents of the University of California
    Inventors: Timothy B. C. Johnstone, Derk J. Hogenkamp, Kelvin W. Gee
  • Patent number: 8859554
    Abstract: A packaging assembly or kit includes packaging material containing a solid formulation including pimobendan dispersed in a polyvalent acid. The kit may also include a package leaflet or user instruction including the information concerning use of the solid formulation, for example, via the oral route for the prevention and/or treatment of congestive heart failure in a mammal in need of such prevention or treatment, preferably in a dog, cat or rodent.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin A. Folger, Bernhard Hassel, Stefan Henke, Jens Lehmann
  • Publication number: 20140296246
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Ruben Martinez, Samuel E. Metobo, Michael R. Mish, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8846679
    Abstract: The invention relates to novel solid formulations comprising as pharmaceutically active compound pimobendan and to processes for producing such solid formulations. The invention furthermore relates to a method for manufacturing a medicament for the prevention and/or treatment of congestive heart failure, wherein the solid formulations according to the invention are used.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin A. Folger, Bernhard Hassel, Stefan Henke, Jens Schmalz
  • Patent number: 8846680
    Abstract: The invention relates to novel solid formulations comprising as pharmaceutically active compound pimobendan and to processes for producing such solid formulations. The invention furthermore relates to a method for manufacturing a medicament for the prevention and/or treatment of congestive heart failure, wherein the solid formulations according to the invention are used.
    Type: Grant
    Filed: February 22, 2012
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin A. Folger, Bernhard Hassel, Stefan Henke, Jens Schmalz
  • Publication number: 20140288050
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 25, 2014
    Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
  • Patent number: 8841302
    Abstract: The present invention is directed to a combination product for treating or ameliorating hepatitis C virus (HCV) infection or disorders or symptoms associated therewith in a subject in need thereof comprising, a HCV inhibitor and one or more therapeutic agents selected from either or both a HCV protease inhibitor and one or more different therapeutic agents administered in combination in an effective amount to the subject.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: September 23, 2014
    Assignee: PTC Therapeutics, Inc.
    Inventors: Frederick C. Lahser, Zhengxian Gu
  • Patent number: 8841310
    Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen R & D Ireland
    Inventor: Paul Stoffels
  • Publication number: 20140235648
    Abstract: A liquid preparation includes an etherified cyclodextrin derivative and a substituted benzimidazol, where the etherified cyclodextrin derivative is one of alpha-, beta, and gamma-cyclodextrin ether.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin FOLGER, Stefan LEHNER
  • Publication number: 20140221376
    Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Application
    Filed: April 9, 2014
    Publication date: August 7, 2014
    Applicant: Xcovery Holding Company, LLC
    Inventors: Congxin Liang, Zhigang Li
  • 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
  • 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
  • Publication number: 20140194407
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: February 25, 2014
    Publication date: July 10, 2014
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hiroshi SATO, Kazutoshi YOKOYAMA, Kazushi SATO
  • 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
  • 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
  • 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
  • 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
  • Publication number: 20140155338
    Abstract: A phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof is provided for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Juergen DAEMMGEN, Olaf JOENS, Rainer KLEEMANN
  • 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
  • Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Patent number: 8703760
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • Publication number: 20140107057
    Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8697869
    Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: April 15, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
  • Publication number: 20140088112
    Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 27, 2014
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 8680101
    Abstract: The invention relates to a pharmaceutical composition containing pimobendan as an active ingredient. The invention also relates to a crystalline form of pimobendan, as well as to a combination of said crystalline form with at least one other therapeutically active ingredient. Moreover, the invention relates to uses of said crystalline form, as well as to a pharmaceutical composition containing it. Finally, the invention relates to a process for preparing a crystalline form of pimobendan.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: March 25, 2014
    Assignee: Eurovet Animal Health B.V.
    Inventors: Marinus Maria Martinus Boeren, Rudolf Johannes Paridaans, Sanita Petkune, Viesturs Lusis, Dzintra Muceniece