The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
  • Patent number: 10358451
    Abstract: Provided are compounds of Formula (I) shown below using for treatment of diseases or disorders mediated by IDO and/or TDO, pharmaceutical compositions and methods of preparation thereof.
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: July 23, 2019
    Assignee: Hangzhou Innogate Pharma Co., Ltd.
    Inventors: Hancheng Zhang, Shifeng Liu
  • Patent number: 9434743
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: September 6, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
  • Patent number: 9321902
    Abstract: The present invention relates to a composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation, which is a polymer, an oligohydroxy compound, a wax, a fat or a mineral oil, with the proviso that the polymer is not a polypeptide, agar-agar or a component of agar-agar and the oligohydroxy compound is not glucose or a component of agar-agar; and b) a compound of formula (I) n is 1, 2, 3 or 4; when n is 1, R5 is H, C1-C30-alkyl, C3-C10-cycloalkyl, C6-C10-aryl, which is unsubstituted or substituted by C1-C8-alkyl, C1-C8-alkoxy, halogen or one phenyl, C7-C13-aralkyl, C2-C22-alkenyl, C3-C12-alkinyl, OH, C1-C30-alkyloxy, C3-C10-cycloalkyloxy, C6-C12-aryloxy, C7-C13-aralkyloxy, hydroxy-C1-C8-alkyl, carboxy-C1-C12-alkyl, C1-C12-alkoxycarbonyl-C1-C12-alkyl, C2-C30-alkyl, which is interrupted by one or more oxygen atoms, C2-C16-alkyl, which is interrupted by one sulfur atom, or NR?1R?2; when n is 2, R5 is C1-C12-alkane-diyl, C6-C14-arylene, C4-C8-cycloalkane-bis-(C1-
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: April 26, 2016
    Assignee: BASF SE
    Inventors: Werner Hoelzl, Bruno Rotzinger
  • Patent number: 9200007
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110?, and therefore have utility in therapy.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 1, 2015
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Thomas James Hill, Franck Alexandre Silva
  • Patent number: 9062061
    Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: June 23, 2015
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150132352
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • 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: 20150119388
    Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 30, 2015
    Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIA
    Inventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
  • Patent number: 9018201
    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 associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: April 28, 2015
    Assignee: Biomarin Pharmaceuticial Inc.
    Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard Edwin Post
  • Publication number: 20150105381
    Abstract: The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
    Type: Application
    Filed: May 21, 2013
    Publication date: April 16, 2015
    Inventors: Stanislas Mayer, Stephan Schann
  • Publication number: 20150079081
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Application
    Filed: October 27, 2014
    Publication date: March 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQuing Wei
  • Publication number: 20150080374
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: William Scott, Ningshu LIU, Manfred MÖWES, Andrea HÄGEBARTH, Ursula MÖNNING, Ulf BÖMER
  • Publication number: 20150045359
    Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.
    Type: Application
    Filed: January 8, 2013
    Publication date: February 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
  • Publication number: 20150018348
    Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Francis Xavier Tavares
  • Publication number: 20150011531
    Abstract: Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted —(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inhibitor of HIV replication.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 8, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Claudio Sturino, Pierre Beaulieu, Patrick Deroy, Martin Duplessis, Clint James, Jean-Eric Lacoste, Joannie Minville, Louis Morency, Sébastien Morin, Bruno Simoneau, Martin Tremblay
  • 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
  • Publication number: 20150011543
    Abstract: Pyrimido[4,5-b]indole derivatives are provided. These compounds are useful to expand hematopoietic stem cell populations, particularly, human hematopoietic stem cell populations. The compounds are also useful in the medical treatment of diseases that involve hematopoietic stem cells.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 8, 2015
    Applicant: UNIVERSITE DE MONTREAL
    Inventors: Guy Sauvageau, Yves Gareau
  • Patent number: 8927543
    Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: January 6, 2015
    Assignee: Galapagos NV
    Inventors: Frédéric Gilbert Labéguére, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Saniére, Stephen Robert Fletcher
  • 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: 20140378432
    Abstract: Heteroaryl pyridone and aza-pyridone compounds 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 heteroaryl pyridone and aza-pyridone compounds 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: September 8, 2014
    Publication date: December 25, 2014
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140371216
    Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
    Type: Application
    Filed: April 18, 2014
    Publication date: December 18, 2014
    Applicant: Incyte Corporation
    Inventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
  • Publication number: 20140364395
    Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
  • 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
  • Patent number: 8895549
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: November 25, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: William Johnston Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
  • Patent number: 8883781
    Abstract: The present invention relates to compounds of formula IA-i useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: June 12, 2007
    Date of Patent: November 11, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Lev T. D. Fanning, Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson, Yulian Zhang
  • Patent number: 8883799
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 11, 2014
    Assignee: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
  • Publication number: 20140329800
    Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 6, 2014
    Inventors: Daxin Gao, Heping Yang, Yajun Yu
  • Publication number: 20140315883
    Abstract: The invention provides a compound of Formula (I as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: April 18, 2014
    Publication date: October 23, 2014
    Applicant: ABBVIE INC.
    Inventors: Eric Breinlinger, Heather Davis, Michael Hoemann, Bin Li, Biqin Li, Gagandeep Somal, Stacy Van Epps, Lu Wang, Lu Wang
  • Publication number: 20140275064
    Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: September 18, 2014
    Applicant: DIAXONHIT
    Inventors: Bertrand Leblond, Anne-Sophie Casagrande, Laurent Desire, Alicia Foucourt, Thierry Besson
  • Publication number: 20140275023
    Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Nivedita Namdev, Jianqiang Wang
  • Publication number: 20140256679
    Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Applicants: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian Alvin JOHNS, Jason Gordon WEATHERHEAD, Toshikazu HAKOGI, Yasunori AOYAMA
  • Publication number: 20140256706
    Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
  • Publication number: 20140243327
    Abstract: The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: Global Alliance for TB Drug Development
    Inventors: Kai Liu, Christopher B. Cooper, Haihong Huang, Chun Li, Binna Liu, Yang Liu, Zhenkun Ma, Jingbin Wang, Dali Yin, Dongfeng Zhang, Gang Zhang, Hao Zhang
  • Publication number: 20140243320
    Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.
    Type: Application
    Filed: July 12, 2012
    Publication date: August 28, 2014
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
  • Publication number: 20140200344
    Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Publication number: 20140194417
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: January 8, 2014
    Publication date: July 10, 2014
    Applicant: Nimbus Iris, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
  • Publication number: 20140155386
    Abstract: Bridged bicyclic aryl or 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: December 2, 2013
    Publication date: June 5, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak
  • Publication number: 20140147386
    Abstract: The present invention relates to novel 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE 10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabelled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron-emission tomography (PET).
    Type: Application
    Filed: June 26, 2012
    Publication date: May 29, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: José Ignacio Andrés-Gil, Peter Jacobus Johannes Antonius Buijnsters, Andrés Avelino Trabanco-Suárez, Meri De Angelis, Greta Constantia Peter Vanhoof, Jérôme Emile Georges Guillemont, Frederik Jan Rita Rombouts, Maarten Vliegen, Guy Maurits R. Bormans, SofleJeanne Leopoldine Celens
  • Patent number: 8735386
    Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: May 27, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Matthias Treu
  • Patent number: 8729082
    Abstract: The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.
    Type: Grant
    Filed: April 24, 2010
    Date of Patent: May 20, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Marcus Koppitz, Benjamin Bader, Ulf Bömer, Bertolt Kreft, Philip Lienau, Tobias Marquardt, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Patent number: 8716292
    Abstract: The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Global Alliance for TB Drug Development
    Inventors: Kai Liu, Christopher B. Cooper, Haihong Huang, Chun Li, Binna Liu, Yang Liu, Zhenkun Ma, Jingbin Wang, Dali Yin, Dongfeng Zhang, Gang Zhang, Hao Zhang
  • Publication number: 20140121204
    Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: GALAPAGOS NV
    Inventors: Frédéric Gilbert Labéguère, Gregory John Robert NEWSOME, Luke Jonathan ALVEY, Laurent Raymond Maurice Sanière, Stephen Robert FLETCHER
  • Publication number: 20140113896
    Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 8, 2011
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: William Johnston Scott, Orlin Pertov, Manfred Möwes, Ningshu Liu, Ulf Bömer
  • Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Publication number: 20140072529
    Abstract: The present invention relates:—to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II): or a tautomer, solvate or hydrate thereof;—to methods of preparing said dihydrochloride salt;—to said dihydrochloride salt for the treatment and/or prophylaxis of a disease;—to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer;—to a pharmaceutical composition comprising said dihydrochloride salt; and to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agent
    Type: Application
    Filed: March 29, 2012
    Publication date: March 13, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jan-Georg Peters, Hans-Christian Militzer, Hartwig Müller
  • Publication number: 20140057896
    Abstract: Pyridone and aza-pyridone 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: Application
    Filed: October 22, 2013
    Publication date: February 27, 2014
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • Publication number: 20140051697
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Helen Anderson
  • Publication number: 20140045833
    Abstract: The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.
    Type: Application
    Filed: April 3, 2012
    Publication date: February 13, 2014
    Applicant: PHARMASCIENCE INC.
    Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith