1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • MODULATORS OF HEC1 ACTIVITY AND METHODS THEREFOR
    Publication number: 20130190312
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.
    Type: Application
    Filed: November 29, 2012
    Publication date: July 25, 2013
    Inventors: Jiann-Jyh HUANG, Shih-Hsien CHUANG, Ying-Shuan Eda LEE, Yu-Ling HUANG, Johnson LAU
  • PYRIDAZINE DERIVATIVES AND USE THEREOF AS MEDICAMENTS FOR TREATING MICRORNA VIRAL INFECTION
    Publication number: 20130190319
    Abstract: Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification.
    Type: Application
    Filed: August 2, 2011
    Publication date: July 25, 2013
    Applicant: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES
    Inventors: Song Li, Hongliang Wang, Junhai Xiao, Xian Zhang, Lili Wang, Zhibing Zheng, Wu Zhong, Yunde Xie, Xingzhou Li, Xinbo Zhou, Guoming Zhao, Xiaokui Wang
  • Arylalkylamine compound and process for preparing the same
    Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF
    Publication number: 20130184284
    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 agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Application
    Filed: July 16, 2012
    Publication date: July 18, 2013
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
  • NOVEL COMPOUNDS
    Publication number: 20130184248
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Application
    Filed: January 11, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
  • PYRROLIDINE DERIVATIVES
    Publication number: 20130184249
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 18, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Protein Kinase Inhibitors and Methods of Treatment
    Publication number: 20130184274
    Abstract: The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
    Type: Application
    Filed: July 8, 2011
    Publication date: July 18, 2013
    Inventors: Guillaume Laurent Lessene, Jonathan Bayldon Baell, Antony Wilks Burgess, Hiroshi Maruta
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20130184260
    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: March 5, 2013
    Publication date: July 18, 2013
    Inventor: Merck Patent Gesellschaft Mit Beschrankter Haftung
  • 1,2,4 oxadiazole compounds and methods of use thereof
    Patent number: 8486979
    Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: July 16, 2013
    Assignee: AbbVie Inc.
    Inventors: Jianguo Ji, Chih-Hung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20130178461
    Abstract: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • PYRIDAZINE AMIDE COMPOUNDS
    Publication number: 20130178478
    Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Application
    Filed: January 10, 2013
    Publication date: July 11, 2013
    Applicant: Hoffman-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Crystals of hydrochloride of pyridazin-3(2H)-one compound and process for production of same
    Patent number: 8481727
    Abstract: Provided are novel crystals of 4-bromo-6-(3-(4-chloro-phenyl)propoxy)-5-(pyridin-3-ylmethylamino)pyridazin-3(2H)-one monohydrochloride, and a process for production of same. A-form crystals of 4-bromo-6-(3-(4-chlorophenyl)propoxy)-5-(pyridin-3-ylmethylamino)pyridazin-3(2H)-one monohydro-chloride represented by formula (1), which exhibit a powder X-ray diffraction pattern with characteristic peaks at diffraction angles (2?) of 8.24, 11.24, 11.76, 16.48, 17.16, 17.80, 18.24, 19.80, 21.64, 22.56, 22.96, 23.68, 24.52, 25.92, 26.32, 27.12, 27.40, 28.00, 28.64, 29.28, 31.84 and 34.80°.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: July 9, 2013
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shiro Kawahara, Junichi Nishitani
  • Pyridazinyl derivatives as smo inhibitors
    Patent number: 8481542
    Abstract: The present invention relates to compounds of formula I: in which R11 and R12 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: July 9, 2013
    Assignee: Novartis AG
    Inventors: Feng He, Stefan Peukert, Karen Miller-Moslin, Naeem Yusuff, Zhuoliang Chen, Bharat Lagu
  • Caspase inhibitors based of pyridazinone scaffold
    Patent number: 8481537
    Abstract: The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: July 9, 2013
    Assignee: LG Life Sciences Ltd.
    Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang
  • Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
    Patent number: 8481539
    Abstract: The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: July 9, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulf Bömer
  • Derivatives of 6,7-dihydro-5-imidazo[1,2-?]imidazole-3-carboxylic acid amides
    Patent number: 8481750
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 9, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. Kowalski, Matt Aaron Tschantz
  • New azetidine derivatives, pharmaceutical compositions and uses thereof
    Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20130172335
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • METHOD FOR PRODUCING PYRIDAZINONE COMPOUNDS AND INTERMEDIATE THEREOF
    Publication number: 20130172556
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Application
    Filed: September 7, 2011
    Publication date: July 4, 2013
    Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
  • PYRIDAZINONES AS GPR119 AGONISTS
    Publication number: 20130172323
    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: Application
    Filed: May 6, 2011
    Publication date: July 4, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • HETEROCYCLIC FLAVIVIRIDAE VIRUS INHIBITORS
    Publication number: 20130171102
    Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 4, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
  • Indole, indazole and benzimidazole arylamides as P2Xand P2Xantagonists
    Patent number: 8476457
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: July 2, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Nancy Elisabeth Krauss
  • INHIBITORS OF SYK AND JAK PROTEIN KINASES
    Publication number: 20130165431
    Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: October 23, 2012
    Publication date: June 27, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • 1,4-SUBSTITUTED PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20130164259
    Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 27, 2013
    Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
  • HETEROCYCLIC INHIBITORS OF GLUTAMINASE
    Publication number: 20130157998
    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 19, 2012
    Publication date: June 20, 2013
    Applicant: CALITHERA BIOSCIENCES INC.
    Inventor: Calithera Biosciences Inc.
  • AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
    Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • PYRIMIDINE DERIVATIVES AS FAK INHIBITORS
    Publication number: 20130158005
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: July 19, 2011
    Publication date: June 20, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
  • HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
    Publication number: 20130157981
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: December 18, 2012
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Armin HECKEL, Andreas BLUM, Dieter HAMPRECHT, Joerg KLEY
  • TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
    Publication number: 20130157996
    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: June 21, 2012
    Publication date: June 20, 2013
    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
  • Tyrosine Kinase Inhibitors
    Publication number: 20130158041
    Abstract: The present invention relates to pyridazinthione derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: August 26, 2011
    Publication date: June 20, 2013
    Inventors: Kevin Wilson, Matthew Daniels
  • NOVEL COMPOUNDS
    Publication number: 20130158038
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS
    Publication number: 20130158009
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Application
    Filed: May 13, 2011
    Publication date: June 20, 2013
    Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, Steven Armen Boyd
  • 1,2-disubstituted heterocyclic compounds
    Patent number: 8466148
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: June 18, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Piperidinylamino-pyridazines and their use as fast dissociating dopamine 2 receptor antagonists
    Patent number: 8466153
    Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as 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: December 5, 2007
    Date of Patent: June 18, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gregor James MacDonald, José Ignacio Andrés-Gil, Frans Alfons Maria Van Den Keybus, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • Compounds and method for treatment of cancer
    Patent number: 8466151
    Abstract: The invention relates to a compound of Formula (I) and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein X is selected from S or O; R5 is selected from a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, or (Formula II) and the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: June 18, 2013
    Assignee: Critical Outcome Technologies, Inc.
    Inventors: Wayne R Danter, Cheuk Kun Kun Lau
  • HETEROCYCLIC COMPOUND
    Publication number: 20130150344
    Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 13, 2013
    Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
  • NOVEL COMPOUNDS
    Publication number: 20130150341
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Application
    Filed: December 3, 2012
    Publication date: June 13, 2013
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
  • NICOTINIC RECEPTOR COMPOUNDS
    Publication number: 20130150373
    Abstract: Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.
    Type: Application
    Filed: August 19, 2011
    Publication date: June 13, 2013
    Applicant: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Pauline Wanjiku Ondachi
  • NOVEL COMPOUNDS
    Publication number: 20130150355
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • AUTOTAXIN INHIBITORS AND USES THEREOF
    Publication number: 20130150326
    Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.
    Type: Application
    Filed: August 19, 2011
    Publication date: June 13, 2013
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
  • Isoquinoline derivative
    Patent number: 8461329
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: June 11, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
  • Dihydropyrimidinones
    Patent number: 8461160
    Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: June 11, 2013
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
  • CERTAIN AMINO-PYRIDAZINES, COMPOSITIONS THEREOF, AND METHODS OF THEIR USE
    Publication number: 20130143862
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 22, 2011
    Publication date: June 6, 2013
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Jeffrey M. Warrington, Zhe Yang, Pu-Ping Lu, Antonio Romero
  • NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES
    Publication number: 20130143863
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20130143892
    Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: June 6, 2012
    Publication date: June 6, 2013
    Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Armin HECKEL, Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE, Neil J. ASHWEEK, Nicole HARRIOTT
  • DEUTERATED COMPOUNDS FOR ELECTRONIC APPLICATIONS
    Publication number: 20130140544
    Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
    Type: Application
    Filed: January 24, 2013
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: E I DU PONT DE NEMOURS AND COMPANY
  • Therapeutic compounds
    Patent number: 8455477
    Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: June 4, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • HETEROCYCLIC COMPOUND AND USE THEREOF
    Publication number: 20130137675
    Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: May 30, 2013
    Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
  • FUSED HETEROCYCLIC RING COMPOUND
    Publication number: 20130137700
    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: Application
    Filed: August 3, 2011
    Publication date: May 30, 2013
    Inventors: Tomoaki Hasui, Makoto Fushimi, Hironori Kokubo, Takenori Hitaka, Shotaro Miura, Jun Kunitomo, Takahiko Taniguchi
  • 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES
    Publication number: 20130137685
    Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2 and R3 are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.
    Type: Application
    Filed: January 12, 2011
    Publication date: May 30, 2013
    Applicant: SANOFI
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss