Patent
Quinazoline derivatives as angiogenesis inhibitors
Stokes Elaine Sophie Elizabeth,Darren Mckerrecher,Laurent Francois Andre Hennequin,Patrick Ple +3 more
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TLDR
In this paper, the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S, was discussed.Abstract:
The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C?1-3?alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NR?3R4? (wherein R?3 and R4?, which may be the same or different, each represents hydrogen or C?1-3?alkyl), or R?5X1?- (wherein X?1 and R5? are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C?1-4?alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group R?56X10? (wherein X?10 and R56? are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.read more
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Patent
Targeted binding agents against b7-h1
Christophe Queva,Michelle Morrow,Scott A. Hammond,Marat Alimzhanov,Babcook John,Ian Foltz,Jaspal Singh Kang,Laura Sekirov,Boyle Melanie,Chodorge Matthieu,Stewart Ross,Kathleen Ann Mulgrew +11 more
TL;DR: Human monoclonal antibodies directed against B7-H1 and uses of these antibodies in diagnostics and for the treatment of diseases associated with the activity and/or expression of B7H1 are disclosed in this article.
Patent
Quinazoline derivatives as VEGF inhibitors
TL;DR: In this paper, the quinazoline derivatives of formula (I) were defined, where m is an integer from 1 to 3; R 1 represents halogeno or C?1-3?alkyl; X?1? represents -O-; R 2 is selected from one of the following three groups: 1) piperidin-4-yl, C?2-5?alkynylR?3? (wherein R 3 is as defined hereinbefore); and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of
Journal ArticleDOI
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
Vito Guagnano,Pascal Furet,Carsten Spanka,Vincent Bordas,Mickaël Le Douget,Christelle Stamm,Josef Brueggen,Michael Rugaard Jensen,Christian Schnell,Herbert A. Schmid,Markus Wartmann,Joerg Berghausen,Peter Drueckes,Alfred Zimmerlin,Dirksen E. Bussiere,Jeremy Murray,Diana Graus Porta +16 more
TL;DR: In vivo evaluation of compound 1h showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3 and support the potential therapeutic use of 1h as a new anticancer agent.
Patent
c-Met modulators and methods of use
Lynne Canne Bannen,Diva Sze-Ming Chan,Jeff Chen,Lisa Esther Dalrymple,Timothy Patrick Forsyth,Tai Phat Huynh,Vasu Jammalamadaka,Richard George Khoury,James W. Leahy,Morrisson B. Mac,Grace Mann,Larry W. Mann,John M. Nuss,Jason Jevious Parks,Craig Stacy Takeuchi,Yong Wang,Wie Xu +16 more
TL;DR: In this article, the authors provide compounds for modifying protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion.
Patent
Nitrogen-containing aromatic derivatives
Yasuhiro Funahashi,Akihiko Tsuruoka,Masayuki Matsukura,Toru Haneda,Yoshio Fukuda,Junichi Kamata,Keiko Takahashi,Tomohiro Matsushima,Kazuki Miyazaki,Kenichi Nomoto,Tatsuo Watanabe,Hiroshi Obaishi,Atsumi Yamaguchi,Sachi Suzuki,Katsuji Nakamura,Fusayo Mimura,Yuji Yamamoto,Junji Matsui,Kenji Matsui,Takako Yoshiba,Yasuyuki Suzuki,Itaru Arimoto +21 more
TL;DR: In this paper, the authors defined a general formula for groups represented by the following general formula: Ag is an optionally substituted 5-to 14-membered heterocyclic group, etc.
References
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Book
Molecular Cloning: A Laboratory Manual
TL;DR: Molecular Cloning has served as the foundation of technical expertise in labs worldwide for 30 years as mentioned in this paper and has been so popular, or so influential, that no other manual has been more widely used and influential.
Book
Baculovirus expression vectors: a laboratory manual.
TL;DR: This laboratory manual simplifies selection of the most appropriate baculovirus vector design for a given problem by describing each step of the implementation process - from vector construction to large-scale protein production.
PatentDOI
Tyrosine kinase inhibitors
TL;DR: In this article, the imidazo[1,2-a]pyrimidine derivatives are used for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET.
Patent
Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
TL;DR: In this article, a method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono-and/or bicyclic aryl/or heteroaryl compound and their preparation of said compounds and their use in pharmaceutical compositions used in this method.
Patent
Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
Malcolm Clive Carter,George Stuart Cockerill,Stephen Barry Guntrip,Karen Elizabeth Lackey,Kathryn Jane Smith +4 more
TL;DR: Substituted heteroaromatic compounds are protein tyrosine kinase inhibitors as discussed by the authors, in which one ring is a pyridine or pyrimidine of formula (I).