IP Library Granted Patent US 8,148,386
Granted Patent B2
US 8,148,386 · App. 12/244,432 · Granted Apr 3, 2012

Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound

Assignee: Dong-A Pharmtech Co., Ltd.
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Quick Facts
Patent No.
US 8,148,386
App. No.
12/244,432
Granted
Apr 3, 2012
Kind
B2
Abstract

The present invention relates to an agent for preventing and treating benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) associated with BPH and a relaxant for relaxing urethral smooth muscle or prostatic smooth muscle comprising a pyrazolopyrimidinone compound as an effective ingredient. The agent in accordance with the present invention can provide nitric oxides by inhibiting the activity of PDE-5 that decomposes c-GMP, and the provided nitric oxides relax the urethral smooth muscle or the prostatic smooth muscle to lower the intraurethral pressure (IUP), thus treating BPH and LUTS associated with BPH. Furthermore, the time required for reaching a maximum blood concentration is shorter and the half-life is longer than the other PDE-5 inhibitors, thus reducing the frequency of administration. Moreover, the agent of the invention causing few side effects can be efficiently used as a safe drug.

Claims (11)

1. A method for treating benign prostatic hyperplasia (BPH) or a BPH associated symptom comprising administering an effective amount of a compound of Formula 1

to a subject in need thereof.

2. The method of claim 1 , wherein the BPH associated symptom is lower urinary tract symptom (LUTS).

3. The method of claim 1 , wherein the compound of Formula 1 relaxes prostatic smooth muscle or urethral smooth muscle.

4. The method of claim 1 , wherein the compound of Formula 1 lowers intraurethral pressure (IUP).

5. The method of claim 1 , wherein the compound of Formula 1 inhibits an activity of PDE-5.

6. The method of claim 1 , wherein the compound of Formula 1 does not inhibit the activity of PDE-11 but inhibits an activity of PDE-5.

7. The method of claim 1 , wherein the compound of Formula 1 does not cause testicle toxicity or myalgia, since it does not have an inhibitory action for the activity of PDE-11.

8. The method of claim 1 , wherein the compound of Formula 1 is effective for 12 to 24 hours with a low frequency of administration.

9. The method of claim 1 , wherein a maximum blood concentration of the compound of Formula 1 is reached within 50 to 70 minutes.

10. The method of claim 1 , wherein a half-life of the compound of Formula 1 is 9 to 15 hours.

Assignments (3)
CHANGE OF NAME Recorded Jul 2, 2013
From: DONG-A PHARMTECH CO., LTD.
To: MEZZION PHARMA CO., LTD.
Reel/Frame 030729/0072 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 11, 2009
From: DONG-A PHARM. CO., LTD.
To: DONG-A PHARMTECH CO., LTD.
Reel/Frame 023076/0768 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2008
From: YU, JAE YOUNG; CHOI, SEUL MIN; KANG, KYUNG KOO; AHN, BYOUNG OK; YOO, MOOHI
To: DONG-A PHARMACEUTICAL CO., LTD
Reel/Frame 021625/0032 →
Continuity (2)
Continuation PCTKR2006001242 · Apr 4, 2006
Related Publication 20090099357A1 · Apr 16, 2009