US 7,745,470 B2 · Isophthalates as beta-secretase inhibitors

Abstract

There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Claims2

Dependent claims

The compound having formula (Id);

or a stereoisomer thereof,
wherein
R1 is hydrogen or C1-6alkyl;
R2 is C1-6alkyl or phenyl(C1-4alkyl) in which said phenyl is optionally substituted with halogen;
or R1 and R2 are joined together with the nitrogen to form a 5- or 6-membered ring optionally substituted by R4;
R3 is hydrogen, C1-6alkyl, oxazole, thiazole, or NR12—(CO)—R13 in which R12 and R13 are independently C1-6alkyl or are joined together with the nitrogen to form a 5- or 6-membered ring;
R4 is C1-4alkyl optionally substituted with C1-4alkoxy;
and
R5 is C1-6alkyl or phenyl(C1-4alkyl) in which each group is optionally substituted with one or two halogen;
or a nontoxic pharmaceutically acceptable salt thereof.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application

11/370,728Filed 8 Mar 2006 · us provisional application

Priority

10 Mar 2005

Published

US 2006/0229309 A112 Oct 2006

Granted

29 Jun 2010

Term ends

Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07D 265/30
1,4-Oxazines; Hydrogenated 1,4-oxazines: not condensed with other rings
A61P 25/28
Drugs for disorders of the nervous system: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents,…
C07D 207/09
With hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms: radicals substituted by nitrogen atoms, not forming part of…
C07D 207/12
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…

Isophthalates as beta-secretase inhibitors

Life of this patent

Isophthalates as beta-secretase inhibitors

Life of this patent

Abstract

Claims2