US 10,647,721 B2 · Bicyclic heteroaryl derivatives

Abstract

The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and R1 may be different if n is 2 or 3; R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )m is —(CH2)m—; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein R3 is hydrogen, methyl or chloro; R4 is hydrogen or methyl; R5 is F, Cl, CHF2 or CF3; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Claims16

Dependent claims

A compound of formula I

wherein:
R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen;
and R1 may be different if n is 2 or 3;
R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen;
X is CH or N;
m is 1, 2 or 3;
-( )m is —(CH2)m—;
n is 1, 2 or 3;
and
Ar is a five membered heteroaryl group, selected from
wherein
R3 is hydrogen, methyl or chloro;
R4 is hydrogen or methyl;
and
R5 is F, Cl, CHF2 or CF3;
or a pharmaceutically active acid addition salt thereof.

13 more elements

Dependencies are inferred from the claim text.

Bicyclic heteroaryl derivatives

Life of this patent

Bicyclic heteroaryl derivatives

Life of this patent

Abstract

Claims16