Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
  • Patent number: 11008312
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, p, q A, B, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: May 18, 2021
    Assignee: Genentech, Inc.
    Inventors: Sarah M. Bronner, James J. Crawford, Andrew Cridland, Patrick Cyr, Benjamin Fauber, Emanuela Gancia, Alberto Gobbi, Christopher Hurley, Jonathan Killen, Wendy Lee, Olivier Rene, Monique Bodil Van Niel, Stuart Ward, Paul Winship, Jason Zbieg
  • Patent number: 10150740
    Abstract: The invention provides novel compounds having the general formula: wherein R1 to R6 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: December 11, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zhanling Cheng, Xingchun Han, Yongguang Wang, Song Yang
  • Patent number: 9464085
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: October 11, 2016
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Clarissa Jakob
  • Patent number: 9290512
    Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: March 22, 2016
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Publication number: 20150126449
    Abstract: The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Jorma Haßfeld, Tom KINZEL, Johannes Köbberling, Yolanda CANCHO GRANDE, Kristin BEYER, Susanne Röhrig, Maria Köllnberger, Michael SPERZEL, Nils BURKHARDT, Karl-Heinz SCHLEMMER, Christian STEGMANN, Joachim SCHUHMACHER, Matthias WERNER, Manuel ELLERMANN
  • Patent number: 9024039
    Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: May 5, 2015
    Assignee: Women & Infants' Hospital of Rhode Island
    Inventors: Laurent Brard, Satyan Kalkunte, Rakesh Kumar Singh
  • Patent number: 9005777
    Abstract: A heterocyclic compound represented by Formula 1 below, and an organic light-emitting diode including the heterocyclic compound, and a flat display device including the organic light-emitting diode. wherein Ar1 to Ar4, X1, X2, Y1, Y2, L1, and m are defined as in the specification.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Samsung Display Co., Ltd.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Jong-Hyuk Lee
  • Patent number: 8999530
    Abstract: The present invention provides a new compound and an organic electronic device using the same. The compound according to the present invention may serve as hole injection, hole transporting, electron injection and transporting, and light emitting materials and the like in an organic electronic device comprising an organic light emitting device, and the organic electronic device according to the present invention shows excellent properties in terms of efficiency, driving voltage and service life.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: April 7, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Changhwan Shin, Kongkyeom Kim, Dong Hoon Lee, Jungi Jang, Minseung Chun
  • Patent number: 8999987
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: April 7, 2015
    Assignee: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu
  • Patent number: 8999524
    Abstract: An organic light-emitting device includes a first electrode, a mixed organic layer, an emission layer, an electron transport layer, and a second electrode. The mixed organic layer contains a fluorene derivative and a pyrazine derivative, and the electron transport layer contains a lithium quinolate and a pyridine derivative.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: April 7, 2015
    Assignee: Samsung Display Co., Ltd.
    Inventors: Dong-Heon Kim, Tae-Shick Kim, Kwan-Hee Lee, Min-Seung Chun, Jung-Ha Son, Jae-Hyun Kwak, Mi-Kyung Kim, Choon-Woo Lim
  • Publication number: 20150094302
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Wendy B. Young
  • Publication number: 20150087043
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 26, 2015
    Applicants: Coferon, Inc, Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
  • Patent number: 8986852
    Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: March 24, 2015
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
  • Patent number: 8986858
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in luminous efficiency, sufficiently secures driving stability, and has a simple configuration. This organic EL device comprises organic layers between an anode and a cathode piled one upon another on a substrate and at least one organic layer selected from a light-emitting layer, a hole-transporting layer, an electron-transporting layer, and a hole-blocking layer contains a carbazole compound represented by the following formula (1). In the case where the light-emitting layer of the organic electroluminescent device contains a phosphorescent dopant and a host material, it is the carbazole compound that is contained as the host material.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: March 24, 2015
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Masashi Tada, Junya Ogawa, Takahiro Kai, Megumi Matsumoto, Yasuhisa Tsutsumi
  • Publication number: 20150079028
    Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
    Type: Application
    Filed: August 5, 2013
    Publication date: March 19, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD
    Inventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo
  • Publication number: 20150065528
    Abstract: The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 5, 2015
    Applicant: ALGENIS SPA
    Inventors: Max Rutman, Jean-Jacques Pilorget, Jimmy Stehberg, Wolfgang Vanscheidt, Constanza Sigala
  • Patent number: 8962157
    Abstract: Compounds of formula I may be used in optoelectronic devices wherein R1, R2 and R4 are, independently at each occurrence, H, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; R3 is H or a is, independently at each occurrence, 1 or 2; b is, independently at each occurrence, an integer ranging from 0-3; c is, independently at each occurrence, an integer ranging from 0-4; Ar is independently at each occurrence, H, or heteroaryl; and at least two of Ar are heteroaryl.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: February 24, 2015
    Assignee: General Electric Company
    Inventors: Qing Ye, Jie Liu, Kelly Scott Chichak, Yangang Liang
  • Patent number: 8945728
    Abstract: The invention provides an organic compound incorporating a specific structure into a pyridine skeleton or a 1,3,5-triazine skeleton and adapting the molecular weight to a specific range, a composition comprising the organic compound and a solvent, organic electroluminescent element comprising a layer that is formed by using the composition, and the uses thereof.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Koichi Ishibashi, Hideki Gorohmaru, Wataru Shimizu, Tomomi Okamoto
  • Patent number: 8937067
    Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: January 20, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
  • Publication number: 20150018309
    Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 23, 2013
    Publication date: January 15, 2015
    Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
  • Publication number: 20150011461
    Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Applicant: GENENTECH, INC.
    Inventors: James John Crawford, Wendy Lee, Wendy B. Young
  • Patent number: 8927121
    Abstract: Disclosed herein are compounds represented by Formula 1, wherein R1, Ar1, X, Ar2, Ar3, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: January 6, 2015
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyun Sik Chae, Brett T. Harding
  • Publication number: 20150005300
    Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:
    Type: Application
    Filed: March 13, 2014
    Publication date: January 1, 2015
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: BRIDGET M. COLE, RICHARD A. NUGENT, ANDREW KOLODZIEJ, KAREN HANDLEY, YEVGEN BARSUKOV
  • Publication number: 20140378462
    Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 25, 2014
    Applicant: ZAFGEN, INC.
    Inventors: Thomas D. Pallin, Hazel J. Dyke, Susan M. Cramp, Robert Zahler
  • Patent number: 8916703
    Abstract: The present invention relates to new dithiinopyridazinone derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinone derivatives.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: December 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Rinolfi
  • Publication number: 20140371225
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • Patent number: 8911886
    Abstract: A material for electroluminescent devices which comprises a compound in which a heterocyclic group having nitrogen is bonded to carbazolyl group and an organic electroluminescent device having at least one organic thin film layer which is sandwiched between the cathode and the anode and contains the above material in at least one layer, are provided. The material can provide organic electroluminescent devices emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: December 16, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Chishio Hosokawa, Hidetsugu Ikeda, Seiji Tomita, Takashi Arakane
  • Publication number: 20140364409
    Abstract: In one aspect, the invention relates to substituted pyrazolo[3?,4?:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 11, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, James M. Salovich
  • Publication number: 20140350244
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
  • Publication number: 20140343045
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • 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
  • Publication number: 20140323490
    Abstract: Polycyclic 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: Application
    Filed: April 24, 2014
    Publication date: October 30, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
  • Publication number: 20140275070
    Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).
    Type: Application
    Filed: March 10, 2014
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
  • Patent number: 8809364
    Abstract: Polycyclic aryl and polycyclic 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 catalytic activity are also disclosed.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Publication number: 20140228369
    Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 14, 2014
    Applicant: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Shichun Peng
  • Patent number: 8785003
    Abstract: An organic EL device material includes at least a unit including 3,5-biscarbazolylphenyl group, a unit including 4-carbazolylphenyl group, and a compound including a unit including a nitrogen-containing aromatic heterocyclic ring bonding the unit including 3,5-biscarbazolylphenyl group and the unit including 4-carbazolylphenyl group.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: July 22, 2014
    Assignee: Idemtisu Kosan Co., Ltd.
    Inventors: Tetsuya Inoue, Kumiko Hibino, Kei Yoshida, Kazuki Nishimura, Toshihiro Iwakuma
  • Patent number: 8771845
    Abstract: Disclosed herein are compounds represented by Formula 1, wherein R1, Ar1, X, Ar2, Ar3, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: July 8, 2014
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyun Sik Chae, Brett T. Harding
  • Patent number: 8765945
    Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: July 1, 2014
    Assignee: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Quan Jiang, Lei Lu
  • Publication number: 20140171417
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
  • Patent number: 8748014
    Abstract: The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2); and an organic electroluminescent device having a pair of electrodes and at least one organic layer interposed therebetween, in which the compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2), is used as a constituent material of the aforementioned at least one organic layer.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: June 10, 2014
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Norimasa Yokoyama, Shuichi Hayashi, Kouki Kase, Hiroshi Ohkuma, Eiji Takahashi, Daizou Kanda
  • Publication number: 20140142088
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
    Type: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
  • Patent number: 8729072
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 20, 2014
    Assignee: F. Hoffman-La Roche AG
    Inventors: James John Crawford, Wendy B. Young
  • Publication number: 20140128400
    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: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Patent number: 8685969
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: April 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
  • Patent number: 8679647
    Abstract: The invention relates to organic electroluminescent devices which comprise triazine derivatives as the electron transport material.
    Type: Grant
    Filed: November 26, 2009
    Date of Patent: March 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Christof Pflumm, Simone Leu, Joachim Kaiser, Amir Hossain Parham, Frank Voges, Jonas Valentin Kroeber, Arne Buesing
  • Publication number: 20140051695
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Clarissa JAKOB
  • Patent number: 8637669
    Abstract: The present invention relates to an improved method of preparing adefovir dipivoxil of Formula 1. The method of the present invention is characterized by using dimethylsulfoxide as a reaction solvent, and comprises a process of preparing adefovir dipivoxil of Formula 1 by allowing adefovir of Formula 2 to react with chloromethylpivalate at a reaction temperature of 30 to 50° C. under the presence of dimethylsulfoxide and triethylamine solvents.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: January 28, 2014
    Assignee: CJ Cheiljedang Corporation
    Inventors: Kwang Do Choi, Yong Tack Lee, Myeong Sik Yoon, Hye Suk Hong, Il Hwan Cho, Si Beum Lee, Seong Cheol Bang, Da Won Oh, Min Kyoung Lee
  • Publication number: 20140023614
    Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.
    Type: Application
    Filed: March 21, 2012
    Publication date: January 23, 2014
    Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
  • Patent number: 8623523
    Abstract: A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R1 to R12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: January 7, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Masakazu Egawa, Sachiko Kawakami, Nobuharu Ohsawa, Hideko Inoue, Satoshi Seo, Ryoji Nomura