IP Library › Granted Patent US 12,215,101
Granted Patent B2
US 12,215,101 · App. 18/538,309 · Granted Feb 4, 2025

Pro drugs of PDE10 compounds

Inventors: Sachin Mittal (Bridgewater, NJ); Jason W. Skudlarek (Audubon, PA); Izzat T. Raheem (Doylestown, PA)
Assignee: Merck Sharp & Dohme LLC
C07D417/14
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Quick Facts
Patent No.
US 12,215,101
App. No.
18/538,309
Granted
Feb 4, 2025
Kind
B2
Abstract

The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Claims (7)

1. A compound of structural Formula I:

or pharmaceutically acceptable salt thereof, wherein:

R 1 is —C(O)OC 1-6 alkyl, said alkyl optionally substituted with 1 to 3 groups of R a , wherein the C 1-6 alkyl of —C(O)OC 1-6 alkyl is not t-butyl;

and

R a is independently selected from the group consisting of C 1-6 alkyl, OC 1-6 alkyl, oxo, and halogen.

2. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

3. A method for treating schizophrenia, Parkinson's disease, Huntington's disease, obsessive-compulsive disorders, addiction or psychosis in a mammalian patient in need thereof which comprises administering to the patient a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 21, 2023
From: MITTAL, SACHIN; SKUDLAREK, JASON W.; RAHEEM, IZZAT T.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 065930/0351 →
MERGER Recorded Dec 21, 2023
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 065930/0445 →
Continuity (3)
Continuation 17695125 · Mar 15, 2022
Provisional Application 63162333 · Mar 17, 2021
Related Publication 20240158388A1 · May 16, 2024
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