Quinoxalines (including Hydrogenated) Patents (Class 514/234.8)
  • Patent number: 10752590
    Abstract: Described herein are quinoline compounds useful for, among other things, inhibition of the proteasome and for treatment of cancer and inflammation.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: August 25, 2020
    Assignee: Board of Trustees of Michigan State University
    Inventors: Aaron Odom, Jetze J. Tepe, Theresa A. Lansdell
  • Patent number: 10548891
    Abstract: The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R10, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: February 4, 2020
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Yuichi Fukuda, Toshimi Kanai, Yoshisuke Nakasato, Keisuke Kimpara
  • Patent number: 10144726
    Abstract: The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O?); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and di
    Type: Grant
    Filed: February 15, 2016
    Date of Patent: December 4, 2018
    Assignee: SENTINEL ONCOLOGY LIMITED
    Inventors: Robert George Boyle, David Winter Walker
  • Patent number: 9890125
    Abstract: A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R2CH2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: February 13, 2018
    Assignee: UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS
    Inventors: Steven P. Nolan, Sebastien Meiries
  • Patent number: 9295671
    Abstract: Chemical entities that are benzenesulfonamide derivatives of quinoxaline, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 29, 2016
    Assignee: NEUPHARMA, INC.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Patent number: 9150569
    Abstract: The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R10, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: October 6, 2015
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Yuichi Fukuda, Toshimi Kanai
  • Patent number: 9067923
    Abstract: A nitrogen-containing heterocyclic compound represented by formula (I-A): (wherein R1A represents lower alkyl which may be substituted with lower alkoxy, R3A represents lower alkyl substituted with fluorine atom(s), and R4A represents an optionally substituted aromatic heterocyclic group) or the like, or a pharmaceutically acceptable salt thereof; and the like, are provided.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: June 30, 2015
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Toshimi Kanai, Kenji Uchida, Masakazu Honma, Yuichi Fukuda
  • Publication number: 20150148311
    Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • Publication number: 20150141422
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20150105368
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 2, 2014
    Publication date: April 16, 2015
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William MURRAY, Valerio BERDINI, Gilbert Ebai BESONG, Christopher Charles Frederick HAMLETT, Christopher Norbert JOHNSON, Steven John WOODHEAD, Michael READER, David Charles REES, Laurence Anne MEVELLEC, Patrick René ANGIBAUD, Eddy Jean Edgard FREYNE, Tom Cornelis Hortense GOVAERTS, Johan Erwin Edmond WEERTS, Timothy Pietro Suren PERERA, Ronaldus Arnodus Hendrika Joseph GILISSEN, Berthold WROBLOWSKI, Jean Fernand Armand LACRAMPE, Alexandra PAPANIKOS, Oliver Alexis Georges QUEROLLE, Elisabeth Thérèse Jeanne PASQUIER, Isabelle Noëlle Constance PILATTE, Pascal Ghislain André BONNET, Werner Constant Johan EMBRECHTS, Rhalid AKKARI, Lieven MEERPOEL
  • Patent number: 9006240
    Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: April 14, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Toshimitsu Uenaka, Yuji Yamamoto, Junji Matsui
  • Patent number: 8975256
    Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: March 10, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Masato Nagatsuka, Sachiko Kobayashi
  • Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Patent number: 8969344
    Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: March 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Junji Matsui, Yuji Yamamoto, Toshimitsu Uenaka
  • Publication number: 20150057276
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: September 20, 2012
    Publication date: February 26, 2015
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20150057277
    Abstract: Chemical entities that are quinoxaline kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: January 25, 2013
    Publication date: February 26, 2015
    Inventors: Yong-liang Zhu, Xiangping Qian
  • Publication number: 20150031679
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 29, 2015
    Inventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
  • Publication number: 20150031669
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: January 29, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Publication number: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Publication number: 20140357632
    Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: August 13, 2012
    Publication date: December 4, 2014
    Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
  • Publication number: 20140343128
    Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the JAK2-STAT5 pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 20, 2014
    Applicant: Novartis AG
    Inventors: Mohamed Bentires-Alj, Adrian Britschgi
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140275059
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Patent number: 8748422
    Abstract: The present invention relates to a pharmaceutical composition containing one or more quinazoline compounds as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: June 10, 2014
    Assignee: Korea Institute of Science and Technology
    Inventors: Ghil Soo Nam, Hye Whon Rhim, Ae Nim Pae, Hyun Ah Choo, Kyung Il Choi, Seung Yeol Nah
  • Publication number: 20140141099
    Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Inventors: Julian Golec, John Pollard, James Westcott, Hayley Binch, Michael Mortimore, Daniel Robinson
  • Publication number: 20140128392
    Abstract: Disclosed herein are new heterocyclic compounds of Formula IIa: and compositions thereof, and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 19, 2010
    Publication date: May 8, 2014
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero
  • Publication number: 20140107073
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 17, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Publication number: 20140100215
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Application
    Filed: December 7, 2013
    Publication date: April 10, 2014
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • Patent number: 8673908
    Abstract: Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: March 18, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kimpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
  • Publication number: 20140045842
    Abstract: A method for treating a non-ocular inflammatory disease comprising administering to a patient in need thereof a therapeutically effective amount of a compound represented by the following formula (1) or a salt thereof: R1 represents: R2 represents a lower alkyl group, a lower cycloalkyl group or an aralkyl group; R3 represents a lower alkyl group; R4, R5, R6 or R7 each represents a halogen atom, a lower alkyl group, a hydroxyl group, a lower alkoxy group, a cyano group or a nitro group; m, n, p or q each represents 0, 1 or 2; in the case where m, n, p or q is 2, each of R4, R5, R6 or R7 is the same or different.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Masatomo KATO, Miwa Takai, Takahiro Matsuyama, Tatsuji Kurose, Yumi Hagiwara, Kenji Oki, Mamoru Matsuda, Toshiyuki Mori
  • Patent number: 8648069
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: February 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn George, Lu Wang, Biqin Li, N. St. John Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Patent number: 8642584
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: February 4, 2014
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • Publication number: 20140010892
    Abstract: The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: January 9, 2014
    Applicant: Astex Therapeutics Limited
    Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Eva Figueroa NAVARRO, Adrian Liam GILL, Steven HOWARD, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
  • Publication number: 20130324519
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 5, 2013
    Applicant: Novartis AG
    Inventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
  • Patent number: 8592415
    Abstract: The present invention relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I: or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present invention further provides novel compounds and compositions as well as their methods of preparation and use of the same as JAK3 inhibitors in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 26, 2013
    Assignees: Reaction Biology Corp., Synerga Limited
    Inventors: Haiching Ma, Sorin Vasile Filip, Matthew Alexander Henry, James Alexander Dolan, Bartosz Dietrich
  • Publication number: 20130303537
    Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.
    Type: Application
    Filed: July 9, 2013
    Publication date: November 14, 2013
    Inventors: Mamoru MATSUDA, Toshiyuki MORI, Kenji KAWASHIMA, Minoru YAMAMOTO, Masatomo KATO, Miwa TAKAI, Masato NAGATSUKA, Sachiko KOBAYASHI
  • Patent number: 8551991
    Abstract: An object of the present invention is to synthesize a novel 1,2,3,4-tetrahydroquinoxaline derivative represented by formula (1) and to find a pharmacological action of the derivative. In the formula, the R1 represents a halogen, an alkyl, cycloalkyl, aryl or heterocyclic group, or the like; p represents 0 to 5; R2 represents a halogen, an alkyl, hydroxyl or alkoxy group, or the like; q represents 0 to 2; R3 represents hydrogen, an alkyl, alkenyl, alkylcarbonyl or arylcarbonyl group, or the like; R4 and R5 independently represent hydrogen, a halogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; R6 represents hydrogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; and X represents O or S.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: October 8, 2013
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Masato Nagatsuka, Sachiko Kobayashi
  • Patent number: 8551950
    Abstract: A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT2 receptor) antagonists is disclosed. The AT2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: October 8, 2013
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventor: Maree Therese Smith
  • Patent number: 8529927
    Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants can be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, including reduction of an elevated intraocular pressure.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: September 10, 2013
    Assignee: Allergan, Inc.
    Inventors: James N. Chang, Lon T. Spada, Wendy M. Blanda, Werhner C. Orilla, James A. Burke, Patrick M. Hughes
  • Publication number: 20130217670
    Abstract: Compounds of the formula I in which R, R1 and R2 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 22, 2011
    Publication date: August 22, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
  • Patent number: 8481001
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 9, 2013
    Assignee: Exelixis, Inc.
    Inventors: Peter Lamb, David Matthews
  • Publication number: 20130123257
    Abstract: The present invention relates to quinoxalinone derivatives of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: Merck Patent GmbH
    Inventor: Merck Patent GmbH
  • Publication number: 20130102576
    Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.
    Type: Application
    Filed: October 19, 2012
    Publication date: April 25, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130072457
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 28, 2011
    Publication date: March 21, 2013
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, Michael Reader, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Oliver Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
  • Publication number: 20130053384
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
    Type: Application
    Filed: August 24, 2012
    Publication date: February 28, 2013
    Applicant: NeuPharma, Inc.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Publication number: 20120309741
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Inventors: Pascal FURET, Diana GRAUS PORTA, Vito GUAGNANO
  • Publication number: 20120302545
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Application
    Filed: August 7, 2012
    Publication date: November 29, 2012
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • Publication number: 20120264748
    Abstract: The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 18, 2012
    Applicant: NOVARTIS AG
    Inventors: Sangamesh Badiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Simona Cotesta, Jürgen Hans-Hermann Hinrichs, Silvio Ofner, Chetan Pandit, Jürgen Wagner
  • Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach