Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma

• US 7,338,972 B1
• Filed: 12/15/2004
• Issued: 03/04/2008
• 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): Saeed; Kamal A.
• Application Number:
  US11/012,552
• Time in Patent Office: 1,175 Days
• Field of Search: 514/406, 548/361.1
• US Class Current: 514/406
• CPC Class Codes: A61K 31/416 condensed with carbocyclic ring systems, e.g. indazole
• CPC Class Codes: C07D 231/56 Benzopyrazoles; Hydrogenated benzopyrazoles

Abstract

Substituted 1-alkylamino-1H-indazoles 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:

G=H or C<sub>1−

4</sub> alkyl;

R¹, R²=H;

R³=H; and

R⁴=C<sub>1−

4</sub> alkyl; and

pharmaceutically acceptable salts, solvates and prodrugs thereof.

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

R=NR⁶R⁷ or OC<sub>1−

6</sub>alkyl optionally substituted with halogen or hydroxyl, wherein R⁶ and R⁷ are independently hydrogen or C<sub>1−

4</sub>alkyl; and

pharmaceutically acceptable salts, solvates and prodrugs thereof.

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

8. The method of claim 7, wherein the compound is administered as a solution having a pH from about 6.5 to about 7.5.