IP Library Granted Patent US 7,030,121
Granted Patent B2
US 7,030,121 · App. 10/479,622 · Granted Apr 18, 2006

Pyrazolopyrazine compound and pharmaceutical use thereof

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 7,030,121
App. No.
10/479,622
Granted
Apr 18, 2006
Kind
B2
Abstract

A pyrazolopyrazine compound of the following formula (I). wherein R 1 is hydrogen or a suitable substituent; and R 2 is hydrogen or halogen, or a salt thereof. The pyrazolopyrazine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

Claims (24)

1. A pyrazolopyrazine compound of the following formula (I):

wherein

R 1 is hydrogen, lower alkyl, ar(lower)alkyl or cyclo(lower)alkyl which may be interrupted by an oxygen atom;

R 2 is hydrogen or halogen,

or a salt thereof.

2. A process for the preparation of the pyrazolopyrazine compound of claim 1 or a salt thereof, which comprises,

(1) hydrolyzing a compound of the formula (II):

wherein

R 2 is hydrogen or halogen;

R 3 is lower alkyl;

or a salt thereof,

to give a compound of the formula (Ia):

wherein R 2 is as defined above or a salt thereof,

(2) reacting a compound of the formula (Ia) or a salt thereof, with a compound of the formula (III):

R 1a —X  (III)

wherein R 1a is hydrogen, lower alkyl, ar(lower)alkyl or cyclo(lower)alkyl which may be interrupted by an oxygen atom;

X is a leaving group,

or a salt thereof

to give a compound of the formula (Ib):

wherein R 1a and R 2 are as defined above or a salt thereof.

3. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier.

4. A method for treating a disease selected from the group consisting of depression, dementia, Parkinson's disease and anxiety, which comprises administering the compound of claim 1 or a pharmaceutically acceptable salt thereof to a human being or an animal in need thereof.

5. A process for preparing a pharmaceutical composition which comprises admixing the compound of claim 1 or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier.

6. An in vitro method for evaluation of adenosine antagonism which comprises contacting the compound of claim 1 or a pharmaceutically acceptable salt thereof with a human A 1 or A 2a receptor.

Assignments (2)
MERGER Recorded Dec 12, 2005
From: FUJISAWA PHARMACEUTICAL CO., LTD.
To: ASTELLAS PHARMA INC.
Reel/Frame 017073/0257 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 12, 2004
From: AKAHANE, ATSUSHI; TANAKA, AKIRA
To: FUJISAWA PHARMACEUTICAL CO.,LTD.
Reel/Frame 015315/0396 →