IP Library Granted Patent US 7,045,631
Granted Patent B2
US 7,045,631 · App. 10/484,133 · Granted May 16, 2006

Substituted 2-thio-3, 5-dicyano-4-phenyl-6-aminopyridines and their use as adenosine receptor-selective ligands

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Quick Facts
Patent No.
US 7,045,631
App. No.
10/484,133
Granted
May 16, 2006
Kind
B2
Abstract

Compounds of the formula (I) a process for preparing them, and their use as medicaments are described.

Claims (25)

1. A compound of the formula (I)

in which

R 1 denotes (C 1 –C 4 )-alkyl, (C 1 –C 4 )-alkoxy, mono- or di-(C 1 –C 4 )-alkylamino, and

R 2 denotes pyridyl or thiazolyl, which radicals can be substituted by halogen, amino or (C 1 –C 4 )-alkyl,

or a salt, hydrate, or hydrate of the salt thereof.

2. The compound of the formula (I) according to claim 1 , in which

R 1 denotes methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl or tert-butyl, and

R 2 denotes 2-pyridyl, thiazol-4-yl or thiazol-5-yl, which radicals can be substituted by chlorine, amino or methyl,

or a salt, hydrate, or hydrate of the salt, thereof.

3. The compound according to claim 1 or claim 2 having the following structure

or a salt, hydrate, or hydrate of the salt, thereof.

4. A process for preparing a compound of the formula (I)

in which

R 1 denotes (C 1 –C 4 )-alkyl, (C 1 –C 4 )-alkoxy, mono- or di-(C 1 –C 4 )-alkylamino, and

R 2 denotes pyridyl or thiazolyl, which radicals can be substituted by halogen, amino or (C 1 –C 4 )-alkyl,

wherein

a compound of the formula (II)

in which

R 1 has the meaning given above,

is reacted with a compound of the formula (III)

R 2 —CH 2 —X  (III)

in which

R 2 has the meaning given above and X represents a leaving group.

5. A pharmaceutical composition comprising one or more compounds of the formula (I), according to claim 1 , and at least one pharmaceutically acceptable carrier.

6. A method for treatment of hypertension comprising administering an effective amount of a compound of claim 1 .

Assignments (1)
MERGER Recorded Jan 12, 2010
From: BAYER HEALTHCARE AG
To: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Reel/Frame 023769/0122 →