The present invention relates to a compound represented by Formula (I):
(wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar
2
represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X
1
represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R
1
and R
2
represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted)
or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.
Synthesis and .BETA.-adrenergic blocking activity of 2-(N-substituted amino)-1,2,3,4-tetrahydronaphthalen-1-ol derivatives.
作者:KATSUMI ITOH、AKIO MIYAKE、NORIO TADA、MINORU HIRATA、YOSHIKAZU OKA
DOI:10.1248/cpb.32.130
日期:——
In a search for a new structural type of β-adrenergic antagonist. a series of trans-2-(N-substituted amino)-1, 2, 3, 4-tetrahydronaphthalen-1-ol derivatives (3-36) was synthesized in several steps from 3, 4-dihydro-1 (2H)-naphthalenone (37) having a variety of substituents at the 5-, 6-, 7-and 8-positions. Compounds 3-36 were tested in vitro for β-adrenergic activity. Among them, 2-benzhydrylamino-6-chloro-1, 2, 3, 4-tetrahydronaphthalen-1-ol (28c) was found to show a fairly potent β-adrenergic blocking activity.
The present invention relates to a compound represented by Formula (I):
(wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar
2
represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X
1
represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R
1
and R
2
represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.
The present invention relates to a process for preparing a compound of formula (6a):
wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents shown below; Ar
2
represents a pyridinyl group, a pyrimidinyl group or a phenyl group which may be substituted with 1 to 3 substituents; and R
11
represents a group selected from certain substituents.