Patent ID: 7304051
Filing Date: 2007-12-04
Classification: A61P,C04B,C07D

Abstract:
1. A compound having CCK2 antagonist activity of formula (I): wherein R 1 and R 2 are each independently selected from the group consisting of a) H, C b) naphthyl-(CR R c) Ar d) Ar e) Ar f) Ar g) C where R R R or, alternatively, R 1 and R 2 may be taken together with the nitrogen to which they are attached and are selected from the group consisting of i) 10-oxa-4-aza-tricyclo[5.2.1.0 R ii) a 4-7 membered heterocyclic ring said heterocyclic ring having 0 or 1 additional heteroatom members separated from the nitrogen of attachment by at least one carbon member and selected from O, S, —N═, >NH or >NR iii) a benzo fused 4-7 membered heterocyclic ring said heterocyclic ring having 0 or 1 additional heteroatom members separated from the nitrogen of attachment by at least one carbon member and selected from O, S, —N═, >NH or >NR iv) a 4-7 membered heterocyclic ring said heterocyclic ring having 0 or 1 additional heteroatom members separated from the nitrogen of attachment by at least one carbon member and selected from O, S, —N═, >NH or >NR v) 8-oxo-1,5,6,8-tetrahydro-2H,4H-1,5-methano-pyrido[1,2-a][1,5]diazocin-3-yl, optionally having 0, 1 or 2 substituents R R a is independently selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, phenyl, furanyl, thienyl, benzyl, pyrrol-1-yl, —OH, —OC 1-6 alkyl, —OC 3-6 cycloalkyl, -Ophenyl, -Obenzyl, —SH, —SC 1-6 alkyl, —SC 3-6 cycloalkyl, -Sphenyl, -Sbenzyl, —CN, —NO 2 , —N(R y )R z (wherein R y and R z are independently selected from H, C 1-4 alkyl or C 1-6 cycloalkylC 1-4 alkyl), —(C═O)C 1-4 alkyl, —SCF 3 , halo, —CF 3 , —OCF 3 , and —COOC 1-4 alkyl, or, alternatively, two adjacent R a , may be taken together with the carbons of attachment to form a fused ring and selected from the group consisting of phenyl, pyridyl and pyrimidinyl; or alternatively, R 2 and one of R a can be taken together to be —CH 2 — or >C═O and to form a fused ring to the phenyl; R b is, independently, selected from the group consisting of C 1-4 alkyl and halogen; and enantiomers, diastereomers, hydrates and pharmaceutically acceptable salts, esters and amides thereof.