IP Library Granted Patent US 7,115,599
Granted Patent B2
US 7,115,599 · App. 10/432,572 · Granted Oct 3, 2006

Sulfonamide-substituted pyrazolopyridine compounds

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Quick Facts
Patent No.
US 7,115,599
App. No.
10/432,572
Granted
Oct 3, 2006
Kind
B2
Abstract

This invention relates to compounds of the formula in which R 1 , R 2 , and R 3 are as defined in the claims, to a process for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods of using such compounds for treatment of hypertension and sexual dysfunction.

Claims (31)

1. A compound of the formula (I)

in which

R 1 is H, Cl or NH 2 ; and

R 2 and R 3 together with the heteroatoms to which they are bonded form a five- to seven-membered heterocycle which may be saturated or partially unsaturated, may optionally contain one or more other heteroatoms from the group of N, O, S, and may optionally be substituted;

or a salt, stereoisomer or hydrates thereof.

2. A compound as claimed in claim 1 ,

in which

R 1 is H, Cl or NH 2 ; and

R 2 and R 3 together with the heteroatoms to which they are bonded form a five- to seven-membered heterocycle which may be saturated or partially unsaturated, and may optionally contain one or more other heteroatoms chosen from the group of N, O, S;

or a salt, stereoisomer or hydrates thereof.

3. A compound as claimed in claim 1 ,

in which

R 1 is H, Cl or NH 2 ; and

R 2 and R 3 together with the heteroatoms to which they are bonded form a saturated five- to seven-membered heterocycle;

or a salt, stereoisomer or hydrates thereof.

4. A process for preparing compounds of the formula I,

wherein R 1 , R 2 , and R 3 are as defined above in claim 1 ,

comprising reaction of a compound of the formula (II)

where R 1 is as definded above in claim 1 ;

with a compound of the formula X-L-SO 2 X

where

X is a leaving group which can be replaced by an amino group,

L is an alkanediyl group or an alkenediyl group having in each case 3 to 5 carbon atoms, where one or more carbon atoms may be replaced by one or more heteroatoms chosen from N, O, and S, and where the group may optionally be substituted;

in the presence of an organic base at room temperature and subsequent reaction with a base in an organic solvent with heating.

5. The process of claim 4 wherein in the formula X-L-SO 2 X, the group X is Cl.

6. A pharmaceutical composition comprising at least one compound of the formula (I) as defined in claim 1 .

7. A pharmaceutical composition comprising at least one compound of the formula (I) as defined in claim 1 in combination with at least one organic nitrate or NO donor.

8. A pharmaceutical composition comprising at least one compound of the formula (I) as defined in claim 1 in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).

9. A method for the treatment of hypertension comprising administering an effective amount of a compound of formula (I) as defined in claim 1 .

10. A method for the treatment of sexual dysfunction comprising administering an effective amount of a compound of formula (I) as defined in claim 1 .

11. The method as defined in claim 9 or 10 , where the compound of the general formula (I) as claimed in claim 1 is employed in combination with at least one organic nitrate or NO donor or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).

Assignments (2)
MERGER Recorded Jan 12, 2010
From: BAYER HEALTHCARE AG
To: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Reel/Frame 023769/0122 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 20, 2003
From: STASCH, JOHANNES-PETER; FEURER, ACHIM; WEIGAND, STEFAN; STAHL, ELKE; FLUBACHER, DIETMAR; ALONSO-ALIJA, CRISTINA; WUNDER, FRANK; LANG, DIETER; DEMBOWSKY, KLAUS; STRAUB, ALEXANDER; PERZBORN, ELISABETH
To: BAYER PHARMACEUTICALS CORPORATION
Reel/Frame 014056/0906 →