Quinoxalines (including Hydrogenated) Patents (Class 514/234.8)
-
Publication number: 20120245148Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: May 30, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Alain Jean Braun, Olivier Crespin, Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Christophe Philippo, Olivier Venier
-
Publication number: 20120232056Abstract: 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: ApplicationFiled: March 2, 2012Publication date: September 13, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero, Robert C. Kelly
-
Publication number: 20120232068Abstract: A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur associated disorders, and other disorders mediated by ion channel function.Type: ApplicationFiled: September 1, 2010Publication date: September 13, 2012Applicant: Briston-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
-
Publication number: 20120225863Abstract: 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: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
-
Publication number: 20120225859Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Matthew BURGER, Zhi-Jie NI, Sabina PECCHI, Gordana ATALLAH, Sarah BARTULIS, Kelly FRAZIER, Aaron SMITH, Joelle VERHAGEN, Yanchen ZHANG, Allan WAGMAN, Simon NG, Keith PFISTER, Daniel POON, Alicia LOUIE, Teresa PICK, Paul BARSANTI, Edwin IWANOWICZ, Wendy FANTL, Thomas HENDRICKSON, Mark KNAPP, Hanne MERRITT, Charles VOLIVA, Marion WIESMANN, Xiaohua XIN
-
Publication number: 20120220589Abstract: 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: ApplicationFiled: January 5, 2012Publication date: August 30, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
-
Publication number: 20120196849Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: April 10, 2012Publication date: August 2, 2012Applicant: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
-
Publication number: 20120165318Abstract: 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: ApplicationFiled: February 29, 2012Publication date: June 28, 2012Applicant: BIOENERGENIXInventors: John M. McCall, John McKearn, Donna L. Romero, Michael Clare
-
Publication number: 20120122837Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Inventors: CLIFFORD CHENG, GERALD W. SHIPPS, JR., XIAOHUA HUANG, YING HUANG, NING SHAO, ASHWIN RAO, ANANDAN PALANI, PETER ORTH, JOHANNES H. VOIGT, ROBERT J. HERR, LANA MICHELE ROSSITER, QI ZENG, XIANFENG SUN
-
Patent number: 8163725Abstract: Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.Type: GrantFiled: September 22, 2011Date of Patent: April 24, 2012Assignee: Galderma R&D SNCInventors: Jean-Christophe Buge, Karine Nadau-Fourcade, Cyril Meunier
-
Publication number: 20120094976Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n 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: ApplicationFiled: April 19, 2011Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Christiane Kofink, Darryl McConnell
-
Publication number: 20120094998Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
-
Publication number: 20120071478Abstract: The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O?); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.Type: ApplicationFiled: May 26, 2010Publication date: March 22, 2012Applicant: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker
-
Patent number: 8124604Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: GrantFiled: January 10, 2011Date of Patent: February 28, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
-
Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
-
Patent number: 8119633Abstract: Substituted sulfonamide compounds corresponding to formula I pharmaceutical compositions comprising them, a process for preparing them, and the use of such compounds to treat or inhibit pain and other disorders or disease states.Type: GrantFiled: April 30, 2008Date of Patent: February 21, 2012Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Werner Englberger, Timo Struenker, Ruth Jostock, Sabine Hees, Edward Bijsterveld, Fritz Theil, Heinz Graubaum
-
Publication number: 20110319410Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: August 31, 2011Publication date: December 29, 2011Applicant: MERCK SERONO SAInventors: PASCALE GAILLARD, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church
-
Publication number: 20110312960Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: August 31, 2011Publication date: December 22, 2011Applicant: MERCK SERONO SAInventors: Pascale Gaillard, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church
-
Publication number: 20110294803Abstract: Methods for treating CNS disorders such as schizophrenia, psychosis and cognitive disorders using specific inhibitors of phosphatidylinositol-3-kinase p110 delta (PIK3CD) expression and/or activity are described. Methods of determining risk of CNS disorders and methods of determining treatment response are also described. An integrative systems biology approach to identify a signaling mechanism and genetic network associated with schizophrenia and with schizophrenia-associated risk variation in ErbB4. A risk pathway associated with ErbB4 genetic variation involving increased expression of a PI3K-linked ErbB4 receptor CYT-1 and a specific PI3K enzyme, PIK3CD has been identified.Type: ApplicationFiled: December 4, 2009Publication date: December 1, 2011Inventors: Amanda J. Law, Daniel R. Weinberger
-
Patent number: 8053427Abstract: Improved topical gel compositions, such as those containing brimonidine, for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.Type: GrantFiled: June 13, 2011Date of Patent: November 8, 2011Assignee: Galderma R&D SNCInventors: Jean-Christophe Buge, Karine Nadau-Fourcade, Cyril Meunier
-
Publication number: 20110237584Abstract: 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: ApplicationFiled: November 9, 2009Publication date: September 29, 2011Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kinpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
-
Publication number: 20110195965Abstract: The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula (I) as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.Type: ApplicationFiled: April 12, 2011Publication date: August 11, 2011Inventors: Dirk FINSINGER, Armin De Meijere
-
Publication number: 20110190293Abstract: Quinazolinone compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Inventors: Weibo Wang, Liana M. Lagniton, Ryan N. Constantine, Manoj C. Desai
-
Publication number: 20110160206Abstract: The present invention provides a tri-substituted pyrimidine compound having an excellent PDE10 inhibitory activity. The present invention relates to a tri-substituted pyrimidine compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compound for PDE10 inhibitor, and a pharmaceutical composition comprising said compounds as an active ingredient: wherein: either one of X1 and X2 is N, and the other of X1 and X2 is CH; A is *-CH?CH—, *-C(Alk)=CH—, *-CH2—CH2— or *-O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted quinoxalinyl or an optionally substituted quinolyl; Y0 is mono- or di-substituted amino group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 3, 2009Publication date: June 30, 2011Inventors: Eiji Kawanishi, Takehiko Matsumura
-
Publication number: 20110152243Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 21, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Neil Wishart, Theresa Dunstan, Jeremy J. Edmunds, Anna M. Ericsson, Catherine R. Ferenz, Adrian D. Hobson, David C. Ihle, Kent D. Stewart, Lei Wang, Lu Wang
-
Publication number: 20110123434Abstract: 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: ApplicationFiled: April 8, 2008Publication date: May 26, 2011Applicant: Exelixis, IncInventors: Peter Lamb, David Matthews
-
Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
-
Publication number: 20110071149Abstract: 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: ApplicationFiled: February 11, 2010Publication date: March 24, 2011Applicants: REACTION BIOLOGY CORP., SYNERGA LIMITEDInventors: Haiching MA, Sorin Vasile FILIP
-
Publication number: 20110053909Abstract: Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a ?-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.Type: ApplicationFiled: July 30, 2010Publication date: March 3, 2011Inventors: Lilian Alcaraz, Andrew Bailey, Nicholas Kindon
-
Publication number: 20110053933Abstract: The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group ?; Y represents a group such as —CO—, —O— or —NRa—, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.Type: ApplicationFiled: March 24, 2009Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kayoko Motoki, Kiichi Kawagoe, Shigeyuki Nishinaka, Sachie Masuda, Atsunobu Sakamoto, Satoru Kaneko, Tsuyoshi Arita, Aki Yokomizo
-
Publication number: 20110021495Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium 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: ApplicationFiled: January 15, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus Gonzalez, III, Dean Wilson, Andreas Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin Petzoldt, Lev T.D. Fanning, Timothy Neubert, Roger Tung, Esther Martinborough, Nicole Hilgraf
-
Publication number: 20110015194Abstract: 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: ApplicationFiled: January 15, 2009Publication date: January 20, 2011Applicant: Merck Patent GesellschaftInventors: Gérard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
-
Publication number: 20110009391Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: July 26, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
-
Publication number: 20100297118Abstract: Provided are methods for treating non-small cell lung cancer by administering a therapeutically effective amount of a hedgehog inhibitor.Type: ApplicationFiled: April 16, 2010Publication date: November 25, 2010Inventors: John MacDougall, Kip A. West
-
Publication number: 20100298321Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
-
Publication number: 20100292159Abstract: This invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory conditions.Type: ApplicationFiled: March 20, 2007Publication date: November 18, 2010Applicant: UNIVERSITY OF QUEENSLANDInventor: Maree Therese Smith
-
Publication number: 20100291025Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 13, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
-
Publication number: 20100216726Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.Type: ApplicationFiled: February 24, 2010Publication date: August 26, 2010Applicants: PURDUE PHARMA L.P., SHIONOGI & CO., LTD.Inventors: Kouki FUCHINO, R. Richard Goehring, Akira Matsumura, Bin Shao, Yoshiyuki Taoda, Naoki Tsuno, John William Frank Whitehead, Jiangchao Yao
-
Publication number: 20100197674Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.Type: ApplicationFiled: July 31, 2008Publication date: August 5, 2010Applicants: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Ryuji Tamai, Minoru Ito, Masami Kobayashi, Takashi Mitsunari, Yuki Nakano
-
Publication number: 20100168062Abstract: The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R8 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.Type: ApplicationFiled: June 6, 2008Publication date: July 1, 2010Inventors: Marc Gerspacher, Pascal Furet, Eric Vangrevelinghe, Carole Pissot Sondermann, Christoph Gaul, Philipp Holzer
-
Publication number: 20100152183Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: December 4, 2009Publication date: June 17, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
-
Publication number: 20100152169Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: February 25, 2010Publication date: June 17, 2010Applicant: ASTRAZENECA ABInventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
-
Publication number: 20100137307Abstract: The compounds represented in general formula (1) or a salt thereof are useful for glucocorticoid receptor modulators. In the formula, R1 represents a lower alkyl group, a lower cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, a lower alkyl group and the like; R3 represents a hydrogen atom, a lower alkyl group and the like; R4 and R5 represent a hydrogen atom, a lower alkyl group and the like; R6 represents a hydrogen atom, a lower alkyl group and the like; R7 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group and the like; W represents an oxygen atom, a sulfur atom, NR8 and the like; R8 represents a hydrogen atom, a lower alkyl group and the like; X represents an oxygen atom or a sulfur atom; Y represents a lower alkylene group and the like; Z represents an oxygen atom, a sulfur atom, NR9, OCO or OSO2; R9 represents a hydrogen atom, a lower alkyl group and the like respectively.Type: ApplicationFiled: May 29, 2008Publication date: June 3, 2010Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Mamoru Matsuda, Toshiyuki Mori, Masato Nagatsuka, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
-
Publication number: 20100137308Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: February 21, 2008Publication date: June 3, 2010Applicant: MERCK SERONO SAInventors: Pascale Gaillard, Vincent Pomel, Isabelle Jeanclaude-Etter, Jerome Dorbais, Jasna Klicic, Cyril Montagne
-
Publication number: 20100105667Abstract: 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: ApplicationFiled: May 21, 2009Publication date: April 29, 2010Inventors: Pascal FURET, Diana Graus Porta, Vito Guagnano
-
Publication number: 20100092490Abstract: 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: ApplicationFiled: August 2, 2006Publication date: April 15, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Toshimitsu Uenaka, Yuji Yamamoto, Junji Matsui
-
Publication number: 20100081657Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. 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: ApplicationFiled: August 13, 2009Publication date: April 1, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Guy W. Bemis, John P. Duffy
-
Publication number: 20100075947Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.Type: ApplicationFiled: August 16, 2007Publication date: March 25, 2010Applicant: EXELIXIS, INC.Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
-
Publication number: 20100056505Abstract: The invention is related to compounds of formula (I) as antagonists of the TGF? family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGF? family signaling activity is desirable.Type: ApplicationFiled: November 21, 2006Publication date: March 4, 2010Inventors: Wen-Cherng Lee, Mary Beth Carter, Claudio Chuaqui, Kevin Guckian, Edward Lin, Michael J. Choi, Zhan Deng, Paula Ann Boriack-Sjodin, Lihong Sun
-
Publication number: 20090306072Abstract: A method of treating inflammatory diseases of the airways or intestines which comprises administering substances selected from the group consisting of: (a) quinazolines of general formula wherein A, B, C, D, X, Ra, Rb, Rc and n are as defined herein, (b) the compounds (1) 4-[(3-chloro-4-fluorophenyl)amino]-6-[(4-dimethylamino-cyclohexyl)amino]-pyrimido[5,4-d]pyrimidine, (2) 4-[(R)-(1-phenylethyl)amino]-6-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimidine, and (3) 4-{[3-chloro-4-(3-fluoro-4-benzyloxy)-phenyl]amino}-6-(5-{[(2-methanesulphonyl-ethyl)amino]methyl}-furan-2-yl)quinazoline or (d) the antibodies Cetuximab C225, Trastuzumab, ABX-EGF and Mab ICR-62, and (f) EGFR-antisense.Type: ApplicationFiled: August 19, 2009Publication date: December 10, 2009Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Birgit JUNG, Hubert Pueschner