| US 7,468,385 B2 | ||
| Triazoles as oxytocin antagonists | ||
| Anna Quattropani, Geneva (Switzerland); Matthias Schwarz, Geneva (Switzerland); Russell J. Thomas, Siena (Italy); and Thomas Coulter, Wantage (United Kingdom) | ||
| Assigned to Laboratoires Serono SA, Coinsins (Switzerland) | ||
| Appl. No. 10/498,356 PCT Filed Dec. 19, 2002, PCT No. PCT/EP02/14594 § 371(c)(1), (2), (4) Date Mar. 29, 2005, PCT Pub. No. WO03/053437, PCT Pub. Date Jul. 03, 2003. |
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| Claims priority of application No. 01000778 (EP), filed on Dec. 20, 2001. | ||
| Prior Publication US 2005/0187275 A1, Aug. 25, 2005 | ||
| Int. Cl. A61K 31/41 (2006.01); C07D 249/08 (2006.01) | ||
| U.S. Cl. 514—383 [548/262.2] | 11 Claims |
1. The triazole derivative of Formula I:
 its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms,
as well as salts thereof, wherein:
R1 and R2 are independently selected from the group consisting of H, C1-C6-alkyl, aryl C1-C6-alkyl, heteroarylC1-C6-alkyl, C3-C6-cycloalkyl C1-C6-alkyl and C3-C6-heterocycloalkyl C1-C6-alkyl;
R1 and R2, together with the nitrogen atom they are linked to, form a substituted or unsubstituted 5-8-membered saturated, partially
unsaturated or aromatic ring containing optionally one or more additional heteroatoms selected from O, N, S;
A is C(O);
R3 is selected from the group consisting of H, C1-C6-alkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, aryl, heteroaryl, C3-C6-cycloalkyl C1-C6-alkyl, C3-C6-heterocycloalkyl C1-C6-alkyl, C2-C6-alkenyl;
B is S;
R4 and R5 are selected from the group consisting of H, C1-C6-alkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, acyl, aryl acyl, heteroaryl acyl, C3-C6-cycloalkyl C1-C6-alkyl, C3-C6-heterocycloalkyl C1-C6-alkyl, C2-C6-alkenyl;
n is an integer from 2 to 10.
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