Invention Application
- Patent Title: 5-aminoalkyl and 5-aminocarbonyl substituted indoles
- Patent Title (中): 5-氨基烷基和5-氨基羰基取代的吲哚
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Application No.: US10097126Application Date: 2002-03-08
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Publication No.: US20020169169A1Publication Date: 2002-11-14
- Inventor: Kim Andersen , Jens Kristian Perregaard , Thomas Balle
- Applicant: H. Lundbeck A/S
- Applicant Address: DK Valby-Copenhagen
- Assignee: H. Lundbeck A/S
- Current Assignee: H. Lundbeck A/S
- Current Assignee Address: DK Valby-Copenhagen
- Priority: DKPA199901273 19990909
- Main IPC: A61K031/496
- IPC: A61K031/496 ; A61K031/454 ; C07D417/14 ; C07D413/14 ; C07D43/14

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.
Public/Granted literature
- US06833376B2 5-aminoalkyl and 5-aminocarbonyl substituted indoles Public/Granted day:2004-12-21
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