207297-92-5Relevant articles and documents
A kind of diaryl hydanto?n derivatives, its preparation method, pharmaceutical composition and application
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Paragraph 0439, (2016/10/20)
Provided are a compound as represented by formula I, or pharmaceutically acceptable salt, solvate, precursor drug, stereoisomer, tautomer, polymorph or metabolite thereof, pharmaceutical composition containing same, and uses thereof in the preparation of drugs for treating androgen receptor related diseases.
Design, structure-activity relationships and in vivo characterization of 4-Amino-3-benzimidazol-2-ylhydroquinolin-2-ones: Novel class of receptor tyrosine kinase inhibitors
Renhowe, Paul A.,Pecchi, Sabina,Shafer, Cynthia M.,Machajewski, Timothy D.,Jazan, Elisa M.,Taylor, Clarke,Antonios-McCrea, William,McBride, Christopher M.,Frazier, Kelly,Wiesmann, Marion,Lapointe, Gena R.,Feucht, Paul H.,Warne, Robert L.,Heise, Carla C.,Menezes, Daniel,Aardalen, Kimberly,Ye, Helen,He, Molly,Le, Vincent,Vora, Jayesh,Jansen, Johanna M.,Wernette-Hammond, Mary Ellen,Harris, Alex L.
experimental part, p. 278 - 292 (2009/10/17)
The inhibition of key receptor tyrosine kinases (RTKs) that are implicated in tumor vasculature formation and maintenance, as well as tumor progression and metastasis, has been a major focus in oncology research over the last several years. Many potent small molecule inhibitors of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) kinases have been evaluated. More recently, compounds that act through the complex inhibition of multiple kinase targets have been reported and may exhibit improved clinical efficacy. We report herein a series of potent, orally efficacious 4-amino- 3-benzimidazol-2-ylhydroquinolin-2-one analogues as inhibitors of VEGF, PDGF, and fibroblast growth factor (FGF) receptor tyrosine kinases. Compounds in this class, such as 5 (TKI258), are reversible ATP- competitive inhibitors of VEGFR-2, FGFR-1, and PDGFRβ with IC50 values 0.1 μM. On the basis of its favorable in vitro and in vivo properties, compound 5 was selected for clinical evaluation and is currently in phase I clinical trials.
CHEMICAL PROCESS
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Page/Page column 52, (2008/06/13)
The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]- 5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermed
On the Synthesis of 2-Amino-4,6-difluorobenzonitrile: Highly Selective Formation of 5-Fluoro-3-nitro-1,2-benzoquinone 2-Diazide in the Attempted Sandmeyer Cyanation of 2,4-Difluoro-6-nitrobenzenediazonium Cation
Camps, Pelayo,Morral, Jordi,Munoz-Torrero, Diego
, p. 144 - 145 (2007/10/03)
Attempted cyanation of a diazonium salt derived from 2,4-difluoro-6-nitroaniline gives 5-fluoro-3-nitro-1,2-benzoquinone 2-diazide? in good yield by selective nucleophilic substitution of the 2-fluoride group by hydroxide, instead of the desired 2-amino-4
Cyclic hydrocarbon derivative and liquid crystal composition containing the same
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, (2008/06/13)
A cyclic hydrocarbon derivative represented by formula (I): STR1 wherein each of Y1 and Y2 is independently F, Cl, CN, OCN, SCN, OCF3, OCF2 H, OCF2 CF3, CF3, R, --OR, --COOR or --OCOR, wherein R is alkyl, alkenyl or alkoxyalkyl, provided that at least one of Y1 and Y2 is R, --OR, --COOR or --OCOR; each of Z, Z1, Z2, Z3 and Z4 is independently a single bond, --CH2 CH2 --, --CH=CH--, --C C--, --COO--, --OCO--, --CH2 O--, OCH2 --, --(CH2)4 --, --(CH2)3 --O-- or --O--(CH2)3 --; ring A is group of formula (II): STR2 wherein each of X1, X2, X3, X4, X5, X6, X7, X8, X9, and X10 is independently H or D, provided that at least one of them is D; each of rings K, L, J, M and N is independently trans-1,4-cyclohexylene, 1,4-cyclohexenylene, substituted trans-1,4-cyclohexylene, 1,4-phenylene, substituted 1,4-phenylene, 1,3-dioxane-2,6-diyl, pyrimidine-2,5-diyl, pyridine-2,5-diyl, pyarazine-2,5-diyl or a group of formula (III): STR3 wherein each of X11, X12, X13, X14, X15, X16, X17, X18, X19, and X20 is independently H or D, provided that at least one of them is D; in which the ring of formula (III) may be the same as or different from ring A; and k, l, m, and n each independently is 0 or 1, provided that the sum of k, l, m, and n is 0, 1 or 2. The compound is useful as an electro-optic liquid crystal display material.