Anthony Robert Basile

US Patent:

20220218676, Jul 14, 2022

Filed:

Mar 15, 2022

Appl. No.:

17/695262

Inventors:

- Rahway NJ, US
Anthony S. Basile - Flourtown PA, US
Tjerk Johannes Helena Bueters - Lansdale PA, US
Michael F. Egan - Villanova PA, US
Nancy Dohee Kim - Lexington MA, US
Fiona Hamilton Marshall - Villanova PA, US
Yuki Mukai - Cream Ridge NJ, US
Arie Struyk - Doylestown PA, US
Jason Martin Uslaner - Worcester PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/439
C07D 491/04
C07D 491/18
A61K 31/166
C07D 221/24

Abstract:

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I):and ring B, n, R, R, R, R, and Rare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

US Patent:

20210023049, Jan 28, 2021

Filed:

Feb 28, 2020

Appl. No.:

16/805334

Inventors:

- ROCKVILLE MD, US
Anthony BASILE - Flourtown PA, US
Zhengming CHEN - Belle Meade NJ, US
Joseph W. EPSTEIN - Monroe NY, US

International Classification:

A61K 31/403
C07D 209/52

Abstract:

The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

US Patent:

20210015800, Jan 21, 2021

Filed:

Sep 25, 2020

Appl. No.:

17/032626

Inventors:

- Rahway NJ, US
Anthony S. Basile - Flourtown PA, US
Tjerk Johannes Helena Bueters - Lansdale PA, US
Michael F. Eagan - Villanova PA, US
Nancy Dohee Kim - Lexington MA, US
Fiona Hamilton Marshall - Villanova PA, US
Yuki Mukai - Cream Ridge NJ, US
Arie Struyk - Doylestown PA, US
Jason Martin Uslaner - Worcester PA, US

International Classification:

A61K 31/439
C07D 491/04
C07D 491/18
A61K 31/166
C07D 221/24

Abstract:

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I):or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from:and ring B, n, R, R, R, R, and Rare as defined herein. The compounds of the invention are useful as mGuR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGuR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

US Patent:

20190070148, Mar 7, 2019

Filed:

Jul 5, 2018

Appl. No.:

16/028257

Inventors:

- Rockville MD, US
Anthony BASILE - Flourtown PA, US
Zhengming CHEN - Belle Meade NJ, US
Joseph W. EPSTEIN - Monroe NY, US

International Classification:

A61K 31/403
C07D 209/52

Abstract:

The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.