Patent ID: 6642226
Filing Date: 2003-11-04
Classification: A61P,C07D

Abstract:
A compound of formula whereinR1 a) is unsubstituted phenyl or phenyl substituted by at least one substituent selected from the group R1â€²consisting of halogen, trifluoromethyl, unsubstituted piperazinyl or piperazinyl substituted by at least one substitutent selected from the group consisting of lower alkyl, -morpholinyl, NH-phenyl, pyrrolidinyl, NH(CH2)nâ€”O-lower alkyl, NRaRb, NH(CH2)n-cycloalkyl, and NH(CH2)n-NRcRd, or is b) unsubstituted morpholinyl or morpholinyl substituted by one or two lower alkyl groups, or is c) unsubstituted piperazinyl or piperazinyl substituted in the 4-position by the group R1â€³ which is selected from the group consisting of lower alkyl, cycloalkyl, phenyl, benzoxazolyl, pyridinyl, pyrimidinyl pyrazinyl, (CH2)n-cycloalkyl, (CH2)n-phenyl, (CH2)n-hydroxy, (CH2)nâ€”CF3, (CH2)nâ€”C(O)-morpholinyl, (CH2)nâ€”C(O)â€”N(Re)-unsubstituted phenyl, or â€”(CH2)nâ€”C(O)â€”N(Re)-phenyl substituted by lower alkyl or halogen, (CH2)nâ€”C(O)â€”NRfRg, C(O)-unsubstituted phenyl or phenyl substituted by a substitutent selected from the group consisitng of trifluoromethyl, C(O)â€”(CH2)n-phenyl, C(O)â€”NRhRi, C(O)â€”NRjâ€”(CHRk)n-phenyl, C(O)-lower alkyl, C(O)â€”CF3, C(O)-cycloalkyl, C(O)-morpholinyl, C(O)O-lower alkyl, C(O)â€”Oâ€”(CH2)n-NRlRm and S(O)2-lower alkyl, or isd) unsubstituted pyrrolidinyl or pyrrolidinyl substituted by at least one group R1â€²â€³, which is selected from the group consisting of halogen, hydroxy, &boxH;O, NRnRo, N(cycloalkyl)2, N[(CH2)ncycloalkyl]2, NRpâ€”C(O)-cycloalkyl and Oâ€”(CH2)n-cycloalkyl, or is e) unsubstituted piperidinyl or piperidinyl substituted by at least one group R1â€³â€³ in the 3 or 4-positionselected from the group consisting of hydroxy, &boxH;O, halogen, morpholinyl, NRqRr, NRs-cycloalkyl, NRtâ€”C(O)-cycloalkyl, NRuâ€”C(O)-phenyl, NRvâ€”C(O)â€”(CH2)n-phenyl and Oâ€”(CH2)n-cycloalkyl, or isf) thiomorpholinyl, 1-oxo-thiomorpholinyl or 1,1-dioxothiomorpholinyl; R2 is, independently, selected from the group consisting of hydrogen, halogen, lower alkyl, â€”NHâ€”(CH2)nâ€”O-lower alkyl pyrrolidinyl and morpholinyl; R3/R4 are, independently from each other, trifluoromethyl or halogen; R, Ra-v are independently hydrogen or lower alkyl; n is 1, 2, 3 or 4; and m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof.