发明名称 N-OXIDES AS NK1 RECEPTOR ANTAGONIST PRODRUGS OF 4-PHENYL-PYRIDINE DERIVATIVES
摘要 The invention relates to compounds of formula (I) wherein R is hydrogen, low er alkyl, lower alkoxy, 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 substituted by one or two substituents selected from lowe r alkyl or lower alkoxy; R3, R3' are independently from each other hydrogen, lower alkyl or cycloalkyl; R4, R4' are independently from each other - (CH2)mOR6 or lower alkyl; or R4 and R4' form together with the N-atom to whi ch they are attached a cyclic tertiary amine of the group (II) 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(R 6)- , -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 be en found that these compounds may be uses as prodrugs for the treatment or prevention of illnesses, related to the NK1 receptor.
申请公布号 CA2415890(A1) 申请公布日期 2002.01.24
申请号 CA20012415890 申请日期 2001.07.09
申请人 F. HOFFMANN-LA ROCHE AG 发明人 SLEIGHT, ANDREW;SCHNIDER, PATRICK;HOFFMANN, TORSTEN;POLI, SONIA MARIA
分类号 C07D213/76;A61K31/44;A61K31/4427;A61K31/4439;A61K31/4545;A61K31/455;A61K31/496;A61K31/5377;A61K31/541;A61P1/00;A61P1/08;A61P9/10;A61P11/00;A61P11/06;A61P13/00;A61P17/02;A61P19/02;A61P25/00;A61P25/06;A61P25/22;A61P25/24;A61P25/28;A61P25/36;A61P27/02;A61P29/00;A61P29/02;A61P37/02;A61P37/08;A61P43/00;C07D213/75;C07D213/82;C07D401/04;C07D401/12;C07D413/04;C07D417/04;(IPC1-7):C07D213/76 主分类号 C07D213/76
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