CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

    公开(公告)号:NZ596000A

    公开(公告)日:2013-10-25

    申请号:NZ59600010

    申请日:2010-05-06

    Abstract: 596000 Disclosed herein are carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

    Carboxamide compounds and their use as calpain inhibitors

    公开(公告)号:AU2010244443A1

    公开(公告)日:2011-11-17

    申请号:AU2010244443

    申请日:2010-05-06

    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R, R, R, R, R, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R, r, R, R, R, R, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH-CH, CH-CH-CH, N(R)-CH2, N(R)-CH-CH or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals R, wherein Rand R have the meanings mentioned in the claims.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

    公开(公告)号:CA2750993A1

    公开(公告)日:2010-08-26

    申请号:CA2750993

    申请日:2010-02-19

    Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula (I) in which W-R2 is selected from formulae (1), (2) and (3) and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentionend in the claims.

Patent Agency Ranking