The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/252.03)
  • Patent number: 10336684
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: July 2, 2019
    Assignee: Bristol=Myers Squibb Company
    Inventors: Peter T. W. Cheng, David S. Yoon
  • Patent number: 10328075
    Abstract: The present invention relates generally to a method of therapeutically or prophylactically treating ischaemia-induced myocardial tissue damage, in particular ischaemia-reperfusion-induced myocardial tissue damage. More particularly, the present invention relates to a method of reducing the extent of ischaemia-induced myocardial tissue damage in a mammal by selectively upregulating FPR1-mediated ERK signalling. The method of the present invention is useful, inter alia, in reducing the extent and/or severity of myocardial tissue damage associated with conditions characterized by myocardial ischaemia or myocardial ischaemia and reperfusion, such as acute myocardial infarction caused by atherosclerotic artery occlusion or blood clot-induced artery occlusion.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: June 25, 2019
    Assignees: Baker Heart and Diabetes Institute, Monash University
    Inventors: Rebecca Helen Ritchie, Cheng Xue Qin, Arthur Christopoulos, Patrick Michael Sexton, Jonathan Bayldon Baell
  • Patent number: 10278968
    Abstract: The invention relates to methods of treating cancer or myeloproliferative diseases with a combination of a glutaminase inhibitor and an anticancer agent selected from cabozantinib, crizotinib, and axitinib. The invention further relates to methods of treating cancer or myeloproliferative diseases that are resistant to one or more anticancer agents.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: May 7, 2019
    Assignee: Calithera Biosciences, Inc.
    Inventors: Francesco Parlati, Keith Orford, Sam H. Whiting
  • Patent number: 10052208
    Abstract: A unicompartmental knee prosthesis for implantation in a knee joint between a femoral condyle and a corresponding tibia plateau is provided including a generally elliptical body having opposed femoral and tibial face, the body having an anterior end and a posterior end. A keel is provided on the tibial face having a generally anterior-posterior orientation, the keel having an anterior end and a posterior end, where the keel posterior end includes a distal posterior portion that extends farther toward the body posterior end compared with a proximal posterior portion of the keel posterior end.
    Type: Grant
    Filed: August 18, 2016
    Date of Patent: August 21, 2018
    Inventor: Barry M. Fell
  • Patent number: 10053446
    Abstract: It is an object of the present invention to provide a compound having an excellent antibacterial activity against tuberculosis bacteria, multidrug-resistant tuberculosis bacteria and/or non-tuberculous mycobacteria. Disclosed is a compound of the general formula (1): wherein each symbol is defined as described in the attached specification, or a salt thereof.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: August 21, 2018
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Shimizu, Yoshikazu Kawano, Shunpei Ishikawa, Yukitaka Uematsu, Toshio Shinohara, Motohiro Itotani, Yoshikazu Haraguchi, Isao Takemura, Atsunori Kaneshige, Yuya Nakai, Norimitsu Hariguchi, Yohei Hayashi, Makoto Matsumoto
  • Patent number: 9890137
    Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: February 13, 2018
    Assignee: Georgetown University
    Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
  • Patent number: 9822058
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 21, 2017
    Assignee: CHDI Foundation, Inc.
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Patent number: 9815814
    Abstract: The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: November 14, 2017
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 9809586
    Abstract: Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R1 and R2 independently are —OR7, or —NHSO2R8, where R7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R?—CO—R?, —R?—CO—O—R?, —CO—R?, —R?—O—CO—R?, —R?—CO—NR?, —CO—NR?, or —R?—O—CO—NR?, and R8 is selected from hydrogen, alkyl, aryl, arylalkyl; R3, R4 and R6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, haloalkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R?— is a divalent straight chain or branched alkylene, and —R? is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.
    Type: Grant
    Filed: March 28, 2016
    Date of Patent: November 7, 2017
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Ronald T. Raines, James Vasta
  • Patent number: 9789079
    Abstract: The invention provides compositions and methods for treatment of epilepsy in an animal. In one embodiment, a dietary regime suitable for enhancing the effect of an anti-epileptic drug (AED) in an animal can comprise a food composition comprising a medium chain triglyceride (MCT) and the AED, wherein the MCT is present in the food composition in an effective amount for enhancing the effect of the AED when the food composition and the AED are administered to the animal.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: October 17, 2017
    Assignee: Nestec S.A.
    Inventors: Yuanlong Pan, Brian Michael Zanghi, Jean-Christophe Bouthegourd
  • Patent number: 9751860
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds of the invention can be administered to a patient in need thereof to treat or prevent psychosis including, but not limited to, schizophrenia, schizophreniform disorder and schizoaffective disorder. Compounds of the present invention include those encompassed by Formula I.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: September 5, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 9469631
    Abstract: The present invention relates to compounds of general formula (I), wherein R1, LP, LQ, (Het)Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR1 19 receptor and modulate its activity.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: October 18, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Andreas Blum, Armin Heckel, Frank Himmelsbach, Neil J. Ashweek, Nicole Harriott
  • Patent number: 9468640
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: October 18, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 9440990
    Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: September 13, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tatsuki Koike, Masato Yoshikawa, Haruhi Ando, William John Farnaby, Toshiya Nishi
  • Patent number: 9296735
    Abstract: The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: March 29, 2016
    Assignee: Amgen Inc.
    Inventors: Eric A. Bercot, Matthew Bio, Johann Chan, John Colyer, Yuanqing Fang, Steven Mennen, Robert R. Milburn, Jason Tedrow, Babak Riahi
  • Patent number: 9265758
    Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: February 23, 2016
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Daniel J. Rader
  • Patent number: 9139613
    Abstract: There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: September 22, 2015
    Assignee: NEUROVIVE PHARMACEUTICAL AB
    Inventors: Steven James Moss, Matthew Alan Gregory, Barrie Wilkinson
  • Patent number: 9133160
    Abstract: Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 15, 2015
    Assignee: Bristol-Meyers Squibb Company
    Inventor: Audris Huang
  • Patent number: 9061012
    Abstract: The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: June 23, 2015
    Assignee: Novartis AG
    Inventors: Charles Meyers, Michael H. Serrano-Wu, Tom Thuren
  • Patent number: 9045461
    Abstract: The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: June 2, 2015
    Assignee: TransTech Pharma, LLC
    Inventors: Devi R. Gohimukkula, David Jones, Ghassan Qabaja, Jeff J. Zhu, Jeremy T. Cooper, William K. Banner, Kurt Sundermann, Muralidhar Bondlela, Mohan Rao, Pingzhen Wang, Raju B. Gowda, Robert C. Andrews, Suparna Gupta, Anitha Hari, Rongyuan Xie
  • Publication number: 20150141398
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 21, 2015
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • Publication number: 20150141432
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: Marcel Frans, Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond, Josephine Kennis, Xavier Jean, Michel Langlois, Frans Alfons, Maria Van den Keybus, Yves Emiel, Maria Van Roosbroeck
  • Patent number: 9034873
    Abstract: The present disclosure describes compounds of the following formula in which: the groups A, which may be identical or different, represent a group n is an integer equal to 1 or 2, Y represents an oxygen or sulfur atom, a methylene, hydroxymethylene, carbonyl or thiocarbonyl group, or a group of formula the groups R, which may be identical or different, represent a hydrogen, an alkyl, alkylamine, hydroxyl-alkyl or alkyloxy chain containing from 1 to 6 carbons, or a —COOH, —CONH2, —COOR2 or —CONHR2 group in which R2 is an alkyl chain containing from 1 to 6 carbons, or, when the substituents R are identical in the 2-pyridinyl groups, the substituents R2 may together form an ethereal cyclic alkyl chain, with the exception of the compounds: 2,6-di[5-(2-pyridyl)pyrrol-2-yl]pyridine and bis[5-(6-methyl-2-pyridyl)pyrrol-2-yl]methane.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: May 19, 2015
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Didier Max Dubreuil, Muriel Genevieve Pipelier, Jean-Paul Pradere, Hicham Bakkali, Patrice Lepape, Thierry Delaunay, Alexandra Tabatchnik
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • Patent number: 9023872
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Ixchelsis Limited
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Patent number: 9018212
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: April 28, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Patent number: 9012451
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: April 21, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
  • Publication number: 20150105393
    Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases 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 in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
  • Publication number: 20150065517
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20150065516
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: October 29, 2014
    Publication date: March 5, 2015
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
  • Publication number: 20150057288
    Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Masaaki MITOMI
  • Publication number: 20150045218
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Publication number: 20150030704
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 21, 2012
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: William Farnaby, Charlotte Fieldhouse, Katherine Hazel, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller
  • Publication number: 20150030563
    Abstract: The present invention relates to the treatment, alleviation, prevention or reduction in the incidence of symptoms, diseases or conditions resulting from or associated with enteroviruses, more particularly the enteroviral infections they cause.
    Type: Application
    Filed: August 5, 2014
    Publication date: January 29, 2015
    Inventors: Johan NEYTS, Armando De Palma, Hendrik Jan Thibaut, Pieter Leyssen, Simon Tucker
  • Publication number: 20150031681
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: April 9, 2013
    Publication date: January 29, 2015
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Patent number: 8940743
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 8933080
    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 Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: January 13, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Publication number: 20150011534
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 8, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter DORSCH, Frank STIEBER, Oliver SCHADT, Andree BLAUKAT
  • Patent number: 8927540
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Publication number: 20150004134
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: December 3, 2013
    Publication date: January 1, 2015
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Publication number: 20150005313
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.
    Type: Application
    Filed: June 23, 2014
    Publication date: January 1, 2015
    Inventors: MICHAEL AARON BRODNEY, JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, MICHAEL ERIC GREEN, JACLYN LOUISE HENDERSON, CHEWAH LEE, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, LEI ZHANG
  • Publication number: 20150005303
    Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: George W. MULLER, Roger Shen-Chu CHEN, Alexander L. RUCHELMAN
  • Publication number: 20140371220
    Abstract: The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
    Type: Application
    Filed: December 5, 2012
    Publication date: December 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
  • Patent number: 8912183
    Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: December 16, 2014
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • Patent number: 8912192
    Abstract: Disclosed is a sustained release preparation which releases a poorly soluble medicinal agent in a pH-independent manner. Also disclosed is a sustained release preparation which is capable of controlling the Cmax of a medicinal agent to an adequate amount and is thus capable of maintaining the level of the medicinal agent in the blood to a level at which medicinal effects can be expected for a long period of time. Specifically disclosed is a sustained release preparation which is characterized by containing a pharmaceutically acceptable salt of 4-bromo-6-[3-(4-chlorophenyl)propoxy]-5-(3-pyridylmethylamino)-3(2H)-pyridazinone, and hypromellose. An organic acid is blended in the sustained release preparation in an amount of less than 1% by mass.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: December 16, 2014
    Assignees: Taisho Pharmaceutical Co., Ltd, Nissan Chemical Industries, Ltd.
    Inventors: Noriyuki Hirasawa, Nobuyoshi Kamikido, Akihiko Tasaki, Shusei Ito
  • Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • Patent number: 8901127
    Abstract: The present invention relates to the compounds of general formula I wherein R1 and R2 are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: December 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Norbert Hauel, Raimund Kuelzer
  • 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: 8877780
    Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: November 4, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Ehab M. Khalil