701298-37-5Relevant articles and documents
INHIBITORS OF SPHINGOSINE KINASE
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Page/Page column 90, (2012/10/08)
The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12,
Potent CCR4 antagonists: Synthesis, evaluation, and docking study of 2,4-diaminoquinazolines
Yokoyama, Kazuhiro,Ishikawa, Noriko,Igarashi, Susumu,Kawano, Noriyuki,Masuda, Naoyuki,Hattori, Kazuyuki,Miyazaki, Takahiro,Ogino, Shin-ichi,Orita, Masaya,Matsumoto, Yuzo,Takeuchi, Makoto,Ohta, Mitsuaki
, p. 7968 - 7974 (2008/12/23)
A series of CC chemokine receptor-4 (CCR4) antagonists were examined in a previous report in an attempt to improve metabolic stability in human liver microsomes. In this study, the cycloheptylamine moiety of N-cycloheptyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine 1 was replaced with the p-chloroaniline moiety, and the resulting compound, N-(4-chlorophenyl)-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine (8c), retained its potency ([35S]GTPγS-binding inhibition and CCL22-induced chemotaxis in humans/mice). Based on the structure-activity relationships (SAR), a homology model was constructed for CCR4 to explain the binding mode of 8c. Overall, there was good agreement between the docking pose of the CCR4 homology model and the human [35S]GTPγS assay results. Administration of 8c in a murine model of acute dermatitis showed anti-inflammatory activity (oxazolone-induced contact hypersensitivity test).
UREA DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page/Page column 95, (2010/11/23)
The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis. The derivative is represented by Formula (I): [Chemical formula I] wherein Cy is an aromatic hydrocarbon group which may be substituted or an aromatic heterocyclic group which may be substituted; R1 is a hydrogen atom or a hydrocarbon group which may be substituted; V is -C(O)-, -S(O)-, or -S(O)2-; W is -N(R2)-, -O-, or a bond (wherein R2 is a hydrogen atom or a hydrocarbon group which may be substituted); X is alkylene which may be substituted; Y is -C(O)-, -S(O)-, or -S(O)2-; Z is a bond, a chain hydrocarbon group which may be substituted, or -N=; ring A is a non-aromatic nitrogen-containing heterocyclic ring which may be substituted; ring B is a nitrogen-containing heterocyclic ring which may be substituted; and [Chemical formula 2]------ ̄?,?------? are each independently a single bond or a double bond; provided that R1 may be bonded to R2 to form a non-aromatic nitrogen-containing heterocyclic ring and that R2 may be bonded to a substituent of X to form a non-aromatic nitrogen-containing heterocyclic ring which may be substituted.