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N-OXIDES AS NK1 RECEPTOR ANTAGONIST PRODRUGS OF 4-PHENYL-PYRIDINE DERIVATIVES
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
TORSTEN HOFFMANN,SONIA MARIA POLI,PATRICK SCHNIDER,ANDREW SLEIGHT
申请号:
MYPI 20013310
公开号:
MY154976A
申请日:
2001.07.12
申请国别(地区):
MY
年份:
2015
代理人:
摘要:
THE INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN R IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY, HALOGEN OR TRIFLUOROMETHYL; R1 IS HYDROGEN OR HALOGEN; OR R AND R1 MAY BE TOGETHER WITH THE RING CARBON ATOMS TO WHICH THEY ARE ATTACHED -CH=CH-CH=CH-; R2 AND R2' ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN, HALOGEN, TRIFLUOROMETHYL, LOWER ALKOXY OR CYANO; OR R2 AND R2' MAY BE TOGETHER -CH=CH-CH=CH-, OPTIONALLY SUBSTITUED BY ONE OR TWO SUBSTITUENTS SELECTED FROM LOWER ALKYL OR LOWER ALKOXY; R3, R3' ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN, LOWER ALKYL OR CYCLOALKYL; R4, R4' ARE INDENPENDENTLY FROM EACH OTHER -(CH2)mOR6 OR LOWER ALKYL; OR R4 AND R4' FORM TOGETHER WITH THE N-ATOM TO WHICH THEY ARE ATTACHED A CYCLIC TERTIARY AMINE OF THE GROUP R5 IS HYDROGEN, HYDROXY, LOWER ALKYL, -LOWER ALKOXY, -(CH2)mOH, -COOR3, -CON(R3)2, -N(R3)CO-LOWER ALKYL OR -C(O)R3; R6 IS HYDROGEN, LOWER ALKYL OR PHENYL; X IS -C(O)N(R6)-, -N(R6)C(O)-, -(CH2)mO- OR -O(CH2)m-; N IS 0, 1, 2, 3 OR 4; AND m IS 1, 2 OR 3; AND TO PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. IT HAS BEEN FOUND THAT THESE COMPOUNDS MAY USED AS PRODRUGS FOR THE TREATMENT OR PREVENTION OF ILLNESSES, RELATED TO THE NK1 RECEPTOR.
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中国工程科技知识中心
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