[EN] (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING [FR] DÉRIVÉS DE (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE ET COMPOSÉS ASSOCIÉS UTILISÉS EN TANT QU'INHIBITEURS DE LA BÊTA-SÉCRÉTASE POUR LE TRAITEMENT
[EN] (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING [FR] DÉRIVÉS DE (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE ET COMPOSÉS ASSOCIÉS UTILISÉS EN TANT QU'INHIBITEURS DE LA BÊTA-SÉCRÉTASE POUR LE TRAITEMENT
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.
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.
A compound represented by Formula (I) is provided:
wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar
2
represents 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 which may be substituted, or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.
(3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
申请人:CoMentis, Inc.
公开号:US08299267B2
公开(公告)日:2012-10-30
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.