IP Library Granted Patent US 8,426,403
Granted Patent B2
US 8,426,403 · App. 12/601,322 · Granted Apr 23, 2013

Gamma secretase modulators

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Quick Facts
Patent No.
US 8,426,403
App. No.
12/601,322
Granted
Apr 23, 2013
Kind
B2
Abstract

In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Claims (15)

1. A compound of the general formula:

or a pharmaceutically acceptable salt thereof,

wherein

R 1 and R 2 are joined together to form a piperidinyl ring or a morpholinyl ring, wherein the piperidinyl ring or morpholinyl ring is optionally substituted by alkyl;

R 6 and R 7 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, or phenyl, wherein each alkyl, alkenyl, alkynyl or phenyl is optionally substituted with 1-3 substituents selected from —OH or halo;

R8 is selected from the group consisting of hydrogen, alkyl, alkenyl or alkynyl; and

V is a bond.

2. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 6 or R 7 is phenyl optionally substituted by 1-3 fluoro.

3. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 8 is hydrogen.

4. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 join together to form a piperidinyl ring optionally substituted with a methyl.

5. The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein R 6 or R 7 are alkyl optionally substituted with —OH, or phenyl optionally substituted with 1-3 fluoro.

6. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of

7. The compound according to claim 6 or a pharmaceutically acceptable salt thereof, wherein the compound is

8. A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

9. A pharmaceutical composition comprising a compound according to claim 6 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →