# US 12,215,101 B2 · Pro drugs of PDE10 compounds

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- Number: US 12,215,101 B2
- Document ID: US12215101B2
- Status: Granted
- Kind: B2
- Application number: 18/538,309
- Filed: 2023-12-13
- Published: 2024-05-16
- Granted: 2025-02-04
- Earliest claimed: 2021-03-17
- Assignees: Merck Sharp & Dohme Corp.
- Applicants: Merck Sharp & Dohme LLC
- Inventors: Sachin Mittal; Jason W. Skudlarek; Izzat T. Raheem
- Web page: https://patentgrep.com/patent/US12215101B2

## CPC

- C07D 417/14: containing three or more hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## 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

### Claim 1

A compound of structural Formula I:
or pharmaceutically acceptable salt thereof, wherein:
R1 is —C(O)OC1-6 alkyl, said alkyl optionally substituted with 1 to 3 groups of Ra, wherein the C1-6 alkyl of —C(O)OC1-6 alkyl is not t-butyl;
and
Ra is independently selected from the group consisting of C1-6 alkyl, OC1-6 alkyl, oxo, and halogen.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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.