Azabicyclo and diazepine derivatives

Patent metadata

Field	Value
Publication number	US-11884666-B2
Application number	US-202217699606-A
Country	US
Kind code	B2
Filing date	Mar 21, 2022
Priority date	Nov 3, 2017
Publication date	Jan 30, 2024
Grant date	Jan 30, 2024

Abstract

The present invention provides in one aspect azabicyclo and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator.

First claim

What is claimed is:

1. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is presented by formula (II):

wherein
Me=CH 3 ;
W=N or CH;
X=—O—Y—Z, —S—Y—Z, or —NR 5 —Y—Z;
R 5 =H or C 1 -C 20 straight or branched alkyl groups, C 1 -C 10 straight or branched haloalkyl groups;
Y is a bivalent radical having the following meaning:
a) straight or branched C 1 -C 20 alkyl, being optionally substituted with one or more of the substituents selected from the group consisting of: halogen atoms and hydroxyl;
b) —C(O)(C 1 -C 10 alkyl)- or —C(O)(CH 2 ) n C(O)O—(C 1 -C 10 alkyl)- or —(C 1 -C 10 alkyl)—;

wherein n is an integer from 0 to 20;
R 6 and R 7 are independently H or C 1 -C 10 , straight or branched alkyl groups, C 1 -C 10 straight or branched haloalkyl groups;
and
Z is H, —OH, C 1-6 alkoxy, —COOH.

2. A pharmaceutical composition comprising: (1) a compound of claim 1 and/or a pharmaceutically acceptable salt thereof; and (2) one or more pharmaceutically acceptable carriers.

3. The composition according to claim 2 , wherein said composition is an ophthalmically compatible composition.

4. The composition according to claim 3 , wherein said composition comprises a therapeutically effective amount of said compound, and/or said pharmaceutically acceptable salt.

5. The composition according to claim 3 , wherein said composition comprises from about 0.01 to about 10.0 weight percent of said compound and/or said pharmaceutically acceptable salt.

6. The composition according to claim 3 , wherein said composition comprises: from about 0.01 percent weight/volume to about 5 weight/volume percent of said compound and/or said pharmaceutically acceptable salt; or from about 0.1 to 5.0 weight percent of said compound and/or said pharmaceutically acceptable salt.

7. The composition according to claim 2 , wherein said composition is a topical composition.

8. The composition according to claim 3 , wherein said composition is a topical composition.

9. The composition according to claim 4 , wherein said composition is a topical composition.

10. The composition according to claim 5 , wherein said composition is a topical composition.

11. The composition according to claim 6 , wherein said composition is a topical composition.

12. A method of treating a mammalian subject having or at risk of having an ocular disorder, said method comprising administering to the subject an effective amount of: (a) a compound according to claim 1 and/or (b) a pharmaceutically acceptable salt thereof.

13. A combination comprising: (1) a therapeutically effective amount of a compound according to claim 1 and/or a pharmaceutically acceptable salt thereof; and (2) one or more therapeutically active agents.

Assignees

• Alcon Inc

Inventors

• Ellis David
• Ketelson Howard Allen

Classifications

• C07D471/08 Primary

  Bridged systems · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61P27/10 Primary

  for accommodation disorders, e.g. myopia · CPC title

• C07D243/38

  [b, e]- or [b, f]-condensed with six-membered rings · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title