Title:
アスパラギン酸プロテアーゼ阻害活性を有する大環状化合物およびその医薬的使用
Document Type and Number:
Japanese Patent JP2009513510
Kind Code:
A
Abstract:
The present invention relates to macro-cyclic compounds of formula (I), wherein R1, is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, hydroxy(C1-6)alkyl, (C1-4)alkylthio(C1-4)alkyl, (C1-6)alkenyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, piperidinyl or pyrrolidinyl, R2 and R4, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl or heteroaryl(C1-4)alkyl, or R2 and R4, together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R3 is hydrogen or (C1-4)alkyl, X1 is CH2, X2 is CH2, O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C1-4)alkyl, Y is (C1-8)alkylen or (C1-8)alkylenoxy(C1-6)alkylen, (C1-8)alkenylen or (C1-8)alkenylenoxy(C1-6)alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X1, and X2 are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S02, AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation.
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Inventors:
Claudia Bettuart
Marina Tinternaught-Bromlai
Marina Tinternaught-Bromlai
Application Number:
JP2006518098A
Publication Date:
April 02, 2009
Filing Date:
July 02, 2004
Export Citation:
Assignee:
NOVARTIS AG
International Classes:
C07D273/02; A61K31/33; A61K31/395; A61P9/14; A61P25/00; A61P25/28; A61P43/00; C07D281/00; C07D285/00; C07D291/08
Attorney, Agent or Firm:
Aoyama Aoi
Mitsutaka Iwasaki
Mitsutaka Iwasaki