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, lower alkyl, lower alkoxy, or trifluoromethyl; R<1> is hydrogen or halogen; or R and R<1> may be together with the ring carbon atoms to which they are attached -CH=CH-CH=CH-; R<2> and R<2'> are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R<2> and R<2'> may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R<3>, R<3'> are independently from each other hydrogen, lower alkyl or cycloalkyl; R<4>, R<4'> are independently from each other -(CH2)mOR<6> or lower alkyl; or R<4> and R<4'> form together with the N-atom to which they are attached a cyclic tertiary amine of the group (II) R<5> is hydrogen, hydroxy, lower alkyl, -lower alkoxy, -(CH2)mOH, -COOR<3>, -CON(R<3>)2,-N(R<3>)CO-lower alkyl or -C(O)R<3>; R<6> is hydrogen, lower alkyl or phenyl; X is -C(O)N(R<6>)-, -N(R<6>)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 be uses as prodrugs for the treatment or prevention of illnesses, related to the NK1 receptor.
申请公布号 WO0206236(A1) 申请公布日期 2002.01.24
申请号 WO2001EP07850 申请日期 2001.07.09
申请人 F. HOFFMANN-LA ROCHE AG 发明人 HOFFMANN, TORSTEN;POLI, SONIA, MARIA;SCHNIDER, PATRICK;SLEIGHT, ANDREW
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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