"PHENYL-AND PYRIDINYL DERIVATIVES"
Application IN/PCT/2001/1141/CHE published 2005-03-04, filed 2001-08-13
The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together -CH-CH-CH-CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the group (a): R5 is, independently from each other, hydrogen. C3-6-cycloakyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyll, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5) C(O)-, C(O)O- or -N(R5)(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R5)-; Z is -N-, -CH- or -C(C1)-; n is 0 -4; and, is I or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.
Applicant
F HOFFMANN-LA ROCHE AG
of 124 Grenzacherstrasse,, CH-4070 Basle,, a Swiss Company, Switzerland.
Inventor
International Info
Classification: C07D 213/00
Publication Number: PCT/EP00/01224
Priority Information
99103502.3 EP 1999-02-24