Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma

• US 7,129,257 B1
• Filed: 12/15/2004
• Issued: 10/31/2006
• Est. Priority Date: 12/15/2003
• Status: Expired due to Fees

• Current Assignee: Alcon Incorporated
• Original Assignee: Alcon Incorporated
• Inventors: May, Jesse A., Dantanarayana, Anura P.
• Primary Examiner(s): Wang, Shengjun
• Assistant Examiner(s): Chong, Yong S.
• Application Number:
  US11/012,410
• Time in Patent Office: 685 Days
• Field of Search: 514/403, 514/360, 514/375, 514/913, 548/359.5
• US Class Current: 514/360
• CPC Class Codes: A61K 31/424 condensed with heterocyclic ring systems, e.g. clavulanic acid
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: C07D 491/04 Ortho-condensed systems

Abstract

Pyrazolo[3,4-e]benzoxazoles and analogues thereof for lowering intraocular pressure and treating glaucoma are disclosed.

Claims

1. A method of lowering and/or controlling intraocular pressure in an eye of a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of a compound of formula I:

2. The method of claim 1, wherein the compound is administered topically.

3. The method of claim 1, wherein the compound is administered as a solution, suspension or emulsion in an ophthalmically acceptable vehicle.

4. The method of claim 1, wherein the concentration of the compound is from about 0.01 to about 2 percent by weight.

5. The method of claim 2, wherein for the compound of Formula I:

A=N;

X=N;

Y=C; and

--- in the oxazole ring is a double bond; and

pharmaceutically acceptable salts, solvates and prodrugs thereof.

6. The method of claim 5, wherein for the compound of Formula I:

R¹, R²=H.

7. The method of claim 6, wherein for the compound of Formula I:

R³=methyl.

8. The method of claim 5, wherein the compound is administered as a solution, suspension or emulsion in an ophthalmically acceptable vehicle.

9. The method of claim 8, wherein the compound is administered as a solutin having a pH from about 6.5 to about 7.5.