Invention Application
US20020169169A1 5-aminoalkyl and 5-aminocarbonyl substituted indoles 失效
5-氨基烷基和5-氨基羰基取代的吲哚

5-aminoalkyl and 5-aminocarbonyl substituted indoles
Abstract:
1 The present invention relates to 5-aminoalkyl and 5-aminocarbonyl substituted indole derivatives having formula (1), wherein R1 is-(CH2)n-1-CONR10R11, -(CH2)n-CONR10R11 or (a), wherein R10 and R11 independently are selected from substituents defined herein; n is 1 to 3 and q is 2 to 5; G is N, C, or CH; Ar is phenyl optionally substituted with one or more substituents, or Ar is heterocyclic; R2, R3, R4, R5 and R6 are independently selected from substituents defined herein; m is an integer from 2-6; W is O or S; U is N or CH; Z is null(CH2)p-, p being 2 or 3, or Z is nullCHnullCHnullor 1 ,2-phenylene, or Z isnullCOCH2- or nullCSCH2-; V is O, S, CH2, or NR9; X is N, C, or CH; Y is N, C, or CH; provided at least one of X and Y is N; or a pharmaceutically acceptable acid addition salt thereof. The novel 5-substituted indoles have high affinity for null1-adrenoceptors and are considered useful for the treatment of diseases or disorders responsive to null1-adrenoceptor antagonists. Further, as the compounds are selective null1-adrenoceptor ligands they may be particularly useflul as PET or SPECT ligands.
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