IP Library Granted Patent US 7,291,622
Granted Patent B2
US 7,291,622 · App. 11/192,961 · Granted Nov 6, 2007

Medical uses of carbamate-substituted pyrazolo-pyridine derivatives

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Quick Facts
Patent No.
US 7,291,622
App. No.
11/192,961
Granted
Nov 6, 2007
Kind
B2
Abstract

This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R 1 is H or a di-C 1-6 -alkylaminocarbonyl radical, and R 2 is a radical of the formula —O—C(X)—NR 3 R 4 wherein X is O or S. The compound may also be administered 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).

Claims (19)

1. A method for the treatment of sexual dysfunction, comprising administering to a patient an effective amount of a compound of the formula (I)

in which

R 1 is hydrogen or a di-C 1-6 -alkylaminocarbonyl radical,

R 2 is a radical of the formula —O—CX—NR 3 R 4 ,

where

X is O or S;

R 3 and R 4 may be identical or different from one another and each is a radical chosen from H, optionally substituted C 1-6 -alkyl, optionally substituted C 1-6 -alkoxy-C 1-6 -alkyl, optionally substituted hydroxy-C 1-6 -alkyl, optionally substituted C 2-6 -alkenyl, optionally substituted C 1-6 -alkylcarbonyloxy-C 1-6 -alkyl, optionally substituted C 1-6 -alkoxycarbonyl-C 1-6 -alkyl, optionally substituted hydroxycarbonyl-C 1-6 -alkyl, phenyl which is optionally substituted by a C 1-6 -alkyl radical, a saturated five- to seven-membered heterocycle which is optionally linked via a C 1-6 -alkyl radical to the nitrogen atom, and optionally substituted C 3-8 -cycloalkyl, where R 3 and R 4 cannot simultaneously be H;

or

R 3 and R 4 together with the nitrogen atom to which they are bonded form a five- to seven-membered saturated heterocycle which may optionally contain a further heteroatom chosen from N, O, and S and/or may optionally be substituted or fused to a phenyl ring;

or a salt, stereoisomer, tautomer, or hydrate thereof.

2. The method according to claim 1 , wherein the compound of the formula (I) 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).

3. A process for producing medicaments, which comprises converting at least one compound of the formula (I)

in which

R 1 is hydrogen or a di-C 1-64 -alkylaminocarbonyl radical,

R 2 is a radical of formula —O—CX—NR 3 R 4 , where

X is O or S;

R 3 and R 4 may be identical or different from one another and each is a radical chosen from H, optionally substituted C 1-6 -alkyl, optionally substituted C 1-6 -alkoxy-C 1-6 -alkyl, optionally substituted hydroxy-C 1-6 -alkyl, optionally substituted C 2-6 -alkenyl, optionally substituted C 1-6 -alkylcarbonyloxy-C 1-6 -alkyl, optionally substituted C 1-6 -alkoxycarbonyl-C 1-6 -alkyl, optionally substituted hydroxycarbonyl-C 1-6 -alkyl, phenyl which is optionally substituted by a C 1-6 -alkyl radical, a saturated five- to seven-membered heterocycle which is optionally linked via a C 1-6 -alkyl radical to the nitrogen atom, and optionally substituted C 3-8 -cycloalkyl, where R 3 and R 4 cannot simultaneously be H; or

R 3 and R 4 together with the nitrogen atom to which they are bonded form a five- to seven-membered saturated heterocycle which may optionally contain a further heteroatom chosen from N, O, and S and/or may optionally be substituted or fused to a phenyl ring;

or a salt, stereoisomer, tautomer, or hydrate thereof, where appropriate with conventional excipients and additives, into a suitable administration form.

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