160809-39-2Relevant academic research and scientific papers
FUSED PYRIMIDINE COMPOUND, INTERMEDIATE, PREPARATION METHOD THEREFOR, AND COMPOSITION AND APPLICATION THEREOF
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Paragraph 0273; 0274, (2016/08/17)
Disclosed are a fused pyrimidine compound, an intermediate, a preparation method therefor, and a composition and an application thereof. The present invention provides a fused pyrimidine compound shown in formula I, pharmaceutically acceptable salt, hydrate, solvate, and an optical isomer or prodrug of the compound. The present invention further provides applications of the fused pyrimidine compound shown in formula I, the pharmaceutically acceptable salt, the hydrate, solvate, and the optical isomer or the prodrug of the compound in the preparing drugs for curing and/or preventing a kinase-related disease. The fused pyrimidine compound I of the present invention is an efficient PI3 kinase depressor, and can be used to prepare drugs for preventing and/or curing cell-proliferation diseases such as cancer, infection, inflammation, and an autoimmune disease.
AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS
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Page/Page column 37, (2010/06/16)
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment
AZAARENE DERIVATIVES
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Page/Page column 63-64, (2008/06/13)
A compound represented by the general formula: wherein X1 represents a nitrogen atom or a group represented by the formula -CR10=; X2 represents a nitrogen atom or a group represented by the formula -CR11=; Y represents an oxygen atom or the like; R1 represents a C1-6 alkoxy group, an optionally substituted C6-10 aryloxy group, a group represented by the formula -NR12aR12b or the like; R2 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like; R3, R4, R5, R6, R7, R8, R10 and R11 each independently represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, or the like; R9 represents a group represented by the formula -NR16aR16b or the like; and R12a, R12b, R16a and R16b each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, a salt thereof, or a hydrate of the foregoing.
4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK2) receptor
Jacobs, Robert T.,Shenvi, Ashok B.,Mauger, Russell C.,Ulatowski, Terrance G.,Aharony, David,Buckner, Carl K.
, p. 1935 - 1940 (2007/10/03)
A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK2) receptor antagonist SR-48968 (1) is described. Simple aliphatic derivatives were found to be poorly active, but appropriate placement of an alcohol functional group afforded compounds that were of similar activity to 1. Several representatives in this series, such as the 4- (1-hydroxy-1-ethylpropyl)piperidine (14), were found to exhibit oral activity in a model of labored abdominal breathing in guinea pigs. These results expand the latitude of substituents available in this region of this series of NK2 receptor antagonists.
