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Substituted indole derivatives as modulators of G secretase
专利权人:
INC.;JANSSEN PHARMACEUTICALS
发明人:
申请号:
ARP120102548
公开号:
AR087182A1
申请日:
2012.07.13
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
This compound is the modulator of the G Secretariat. The preparation process of these compounds; pharmaceutical compounds containing these compounds as active ingredients, and the process of using these compounds as drugs.a. A tautometer or stereoisomer of the compound, wherein R3 is selected from the tar groups of hydrogen, C1-4, cyanogen and het1; A1 is cr4a or N; R4A is hydrogen, halogenated or C1-4 tar, which can be replaced by one or more alternatives selected from the tar groups of C1-4; A2 is cr4b or N; R4b is hydrogen, halogen, C1-4 hydrocarbon, cyanogen or het2; A3 is cr4c or N; r4c is hydrogen, halogen or C1-4 hydrocarbon; the condition is that A1, A2 and A3 are n; het1 and het2 represent 5 to 6 heteromorphic members selected from pyridine, pyrazole and oxazolo, respectively,1,2,4-methyl trinitrate and pyridine methanol; 5 or 6 members of isoprene can be replaced by one or more C1-4 tar substitutes; and it is n or CRA; RA is hydrogen, halogen or C1-4 tar, and it can be replaced by hydroxyl; X is n or CH; R1 and R2 combine to form a bivalent radical R1-R2 with (CH2) m-z-ch2 or ch2-z (CH2) m - (CH2) formula;M stands for 2, 3 or 4; Z stands for direct link, nr5u; wherein R5 is hydrogen, C1-4 tar, AR1, [C = O) - AR1 or C1-4 tar, which can be replaced by one or more fluorine substitutes; Where (CH2) m-z-ch2 - or ch2-z (CH2) m - is replaced by one or more CH2 groups, it is composed of one or two substitutes independent of ar2 groups, including ar2, (C = O) - ar2, o-ar2, nr6-ar2, c1-4carboni, fluor, hydroxi and C1-4 tar, replacing one or more fluorine substitutes; each AR1 and ar2 represents, Independently, phenyl, pyridyldine, or pyridine, where we say, phenyl,Pyridinediene or pyridinediene can be replaced by one or more alternatives that are independent of halogen, cyanogen, nr7r8, morphine, cyclopentadiene c3-7, C1-4 optional tar, and the alternatives are replaced by one or more alternatives that are independent of C1-4 hydrocarbon group, Fluorine and cyclopen
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