1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • CONTINUOUS ARYCYCLIC COMPOUND
    Publication number: 20130261128
    Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Osamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro
  • N-(hetero)aryl, 2-(hetero)aryl—substituted acetamides for use as Wnt signaling modulators
    Patent number: 8546396
    Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: October 1, 2013
    Assignee: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • 6-triazolopyridazine sulfanyl benzothiazole derivatives as MET inhibitors
    Patent number: 8546393
    Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: October 1, 2013
    Assignee: Sanofi
    Inventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
  • Viral polymerase inhibitors
    Patent number: 8546389
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: October 1, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
  • NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
    Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS
    Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASE OR CONDITIONS MEDIATED BY LP-PLA2
    Publication number: 20130252963
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130252934
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 26, 2013
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • PYRAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20130252941
    Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.
    Type: Application
    Filed: May 16, 2013
    Publication date: September 26, 2013
    Applicant: F. Hoffmann-La Roche AG
    Inventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
  • Pyridazinone compound and use thereof as herbicides
    Patent number: 8541414
    Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.
    Type: Grant
    Filed: March 13, 2007
    Date of Patent: September 24, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toshiyuki Kiji, Takafumi Fusaka
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20130245010
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
    Publication number: 20130244994
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 15, 2013
    Publication date: September 19, 2013
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • 3-HETARYL-SUBSTITUTED PYRROLO[2,3 B]PYRIDINE DERIVATIVES AS PDK1 INHIBITORS
    Publication number: 20130245355
    Abstract: Compounds of the formula I in which Q, R1, R2, R3 and R4 have the meanings indicated in Claim 1, are PDK1 inhibitors and can be employed for the treatment of tumours.
    Type: Application
    Filed: November 17, 2011
    Publication date: September 19, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Margarita Wucherer-Plietker, Timo Heinrich
  • AMIDE COMPOUNDS
    Publication number: 20130245033
    Abstract: A compound represented by formula (I) and the pharmaceutical acceptable salt thereof are disclosed, wherein, R1, R2, R3, R4, R5 and Ar are defined as those in the specification.
    Type: Application
    Filed: September 6, 2010
    Publication date: September 19, 2013
    Applicant: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Wenhui Hu, Guifa Zhong, Ling Yang, Hongjiang Xu
  • HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
    Publication number: 20130245022
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: Janssen Pharmaceutica NV
    Inventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
  • Therapeutic agents useful for treating pain
    Patent number: 8536177
    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: September 17, 2013
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Laykea Tafesse, Sam Victory
  • GPR119 agonist
    Patent number: 8536176
    Abstract: A cyclic amine derivative represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes. wherein Ar0 is phenyl or phenyl having a substituent such as C1-8 alkylsulfonyl or the like, pyridyl, or pyridyl having a substituent such as C1-8 alkylsulfonyl; A0 is (CH2)p, O, or the like; B0 is (CH2)q, or the like, provided that B0 is neither O nor NR25 when A0 is O or NR24; one of U0 and V0 is N, and the other is N or CR26; each of X0 and Y0 is C1-3 alkylene or C1-3 alkylene having a substituent; R23 is a C1-8 alkyl group or the like; each of R21 and R22 is hydrogen, a halogen atom, or the like.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: September 17, 2013
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Tsuyoshi Endo, Rie Takahashi, Hiroto Tanaka, Toshihiro Kunigami, Takaichi Hamano, Mai Okamura, Kaoru Hara
  • PYRIDAZINE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
    Publication number: 20130237545
    Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20130237515
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.
    Type: Application
    Filed: February 28, 2013
    Publication date: September 12, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
  • Substituted pyrimidinyl-amines as protein kinase inhibitors
    Patent number: 8530480
    Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: September 10, 2013
    Assignee: The Scripps Research Institute
    Inventors: Theodore Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
  • Substituted 6-(1-piperazinyl)-pyridazines as 5-HTreceptor antagonists
    Patent number: 8530474
    Abstract: The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) wherein R1, R2, R3 and X have the meaning defined in the claims, having 5-HT6-antagonistic properties. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicine.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 10, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool, Susana Conde-Ceide, Francisca Delgado-Jiménez
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20130231344
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: September 5, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Compounds and Method for Treatment of Cancer
    Publication number: 20130231345
    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 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: Application
    Filed: March 13, 2013
    Publication date: September 5, 2013
    Applicant: CRITICAL OUTCOME TECHNOLOGIES, INC.
    Inventors: Wayne R. Danter, Cheuk Kun Lau
  • Substituted dihydropyrazolones and use thereof as HIF-prolyl-4-hydroxylase inhibitors
    Patent number: 8524699
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: September 3, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
  • PYRAZOLOQUINOLINE COMPOUND
    Publication number: 20130225553
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: August 29, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventor: ASTELLAS PHARMA INC.
  • NOVEL HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME (AS AMENDED)
    Publication number: 20130225596
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
  • IMIDOTHIAZOLE KINASE INHIBITORS
    Publication number: 20130225591
    Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 29, 2013
    Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
  • 2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
    Patent number: 8518943
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: August 27, 2013
    Assignee: UCB Pharma, S.A.
    Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
  • (Heterocycle/tetrahydropyridine)-(piperazinyl)-1-alcanone and (heterocycle/dihydropyrrolidine)-(piperazinyl)-1-alcanone derivatives, and use thereof as p75 inhibitors
    Patent number: 8518947
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: August 27, 2013
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • 2-amido pyrazines for inflammation and immune related uses
    Patent number: 8518950
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: August 27, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • Compounds as casein kinase inhibitors
    Patent number: 8518944
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: August 27, 2013
    Assignee: Pfizer Inc.
    Inventors: Chakrapani Subramanyam, Travis T. Wager
  • Homocysteine synthase inhibitor
    Patent number: 8513235
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: August 20, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • Pyridazinone compounds
    Patent number: 8513251
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: August 20, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo
  • INDOLE COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC RECEPTOR
    Publication number: 20130210773
    Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic 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: June 21, 2011
    Publication date: August 15, 2013
    Inventor: Craig W. Lindsley
  • 1H-IMIDAZO[4,5-C]QUINOLINES
    Publication number: 20130210832
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
    Type: Application
    Filed: May 17, 2011
    Publication date: August 15, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Darryl McConnell, Harald Engelhardt, Christiane Kofink
  • PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF
    Publication number: 20130210831
    Abstract: The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.
    Type: Application
    Filed: August 18, 2011
    Publication date: August 15, 2013
    Inventors: Wei-Guo Su, Wei Deng, Jinshui Li, Jianguo Ji
  • Tetrasubstituted pyridazine hedgehog pathway antagonists
    Patent number: 8507490
    Abstract: The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or trifluoromethyl; R4 is pyrrolidinyl, morpholinyl or pyridyl, amino or dimethylamino; R5 is trifluoromethyl or methylsulfonyl; R6 is hydrogen or methyl; and R7, R8, R9, R10 and R11 are independently hydrogen fluoro, cyano, chloro, methyl, trifluoromethyl, trifluoromethoxy or methylsulfonyl, provided that at least two of R7, R8, R9, R10 and R11 are hydrogen useful in the treatment of cancer.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: August 13, 2013
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Julia Marie Clay, Jeffrey Daniel Cohen, Philip Arthur Hipskind, Karen Lynn Lobb, Daniel Jon Sall, Michelle Lee Thompson, Takako Wilson (nee Takakuwa)
  • Compounds and compositions as hedgehog pathway inhibitors
    Patent number: 8507491
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: August 13, 2013
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME
    Publication number: 20130203987
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • PYRROLIDINE COMPOUNDS
    Publication number: 20130203728
    Abstract: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds 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: March 13, 2013
    Publication date: August 8, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20130203747
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
    Publication number: 20130203763
    Abstract: The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against c-Met and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: August 8, 2013
    Applicant: Xcovery Holding Company, LLC
    Inventor: Congxin Liang
  • 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators
    Patent number: 8501946
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: August 6, 2013
    Assignee: Glaxo Group Limited
    Inventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Daryl Simon Walter
  • Thiazole and oxazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 8501933
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Medicaments
    Patent number: 8501739
    Abstract: Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: August 6, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Rolf Hohlweg, Knud Erik Andersen, Jan Lindy Sorensen, Jane Marie Lundbeck
  • Derivatives of 6[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one having antitumor activity
    Patent number: 8501731
    Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: August 6, 2013
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
  • HETEROCYCLIC COMPOUNDS AS INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20130196967
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: January 29, 2013
    Publication date: August 1, 2013
    Inventors: Alessandra BARTOLOZZI, Zhidong CHEN, Jonathon Alan DINES, Ho Yin LO, Pui Leng LOKE, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES
    Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS
    Publication number: 20130197008
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 1, 2013
    Applicant: Pfizer Inc.
    Inventors: Robert O. HUGHES, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS
    Publication number: 20130190298
    Abstract: The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases.
    Type: Application
    Filed: October 7, 2011
    Publication date: July 25, 2013
    Applicant: Xcovery Holding Company, LLC.
    Inventor: Congxin Liang