| abstract |
The α-hydroxyamide derivative of general formula (I) is a bradykinin B1 antagonist or adverse agent that is useful for the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R 2a is (1) a group selected from R a , (2) (CH 2 ) n NR b C (O) R a , (3) (CH 2 ) n NR b SO 2 R d , (4) (CH 2 ) n NR b CO 2 R a , (5) 1 to 3 groups independently selected from halogen, nitro, cyano, OR a , SR a , C 1-4 alkyl and C 1-3 haloalkyl Optionally substituted (CH 2 ) k -heterocycle, which has (a) a ring heteroatom selected from N, O and S, and up to 3 additional rings A 5-membered aromatic heterocycle optionally having nitrogen atoms (the ring may optionally be benzo-fused) or (b) 6 containing 1 to 3 ring nitrogen atoms Selected from membered aromatic heterocycles and their N-oxides, said rings optionally being benzo-fused And (6) (CH 2 ) k CO 2 R a and (7) (CH 2 ) C (O) NR b R c . R 2b is OH or a group selected from R 2a , or R 2a and R 2b together with the carbon atom to which they are attached, halogen, OR a , C 1-4 alkyl and C 1 Forms a 3- to 7-membered carbocycle optionally substituted with 1 to 4 groups independently selected from -4 haloalkyl. |