Thienopyrimidine compounds and use thereof

Details Thienopyrimidine compounds and use thereof Thienopyrimidine compounds and use thereof

C - Chemistry, Metallurgy

07

D

C07D 495/04 (2006.01) A61K 31/519 (2006.01) A61P 1/04 (2006.01) A61P 5/04 (2006.01) A61P 5/24 (2006.01) A61P 13/08 (2006.01) A61P 15/00 (2006.01) A61P 15/08 (2006.01) A61P 15/18 (2006.01) A61P 17/10 (2006.01) A61P 17/14 (2006.01) A61P 25/28 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2514407

The present invention provides a compound represented by the formula: (see above formula) wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1') a halogen, (2') a hydroxy group, (3) a C1-4 alkyl and (4') a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1') a halogen, (2') a C1-4 alkoxy-C1-4 alkyl, (3') a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4) a C1-4 alkoxy and (5') a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

L'invention concerne un composé représenté par la formule générale suivante, ou un sel de celui-ci, dans laquelle R?1¿ représente un alkyle C¿1-4?; R?2¿ représente (1) un groupe hétérocyclique de 5 à 7 chaînons contenant de l'azote avec un substituant sélectionné parmi (1') halogéno, (2') hydroxy, (3') un alkyle C¿1-4? et (4') un alkoxy C¿1-4?, (2) un phényle contenant éventuellement un substituant sélectionné parmi (1') halogéno, (2') un alkyle C¿1-4? alkoxy C¿1-4?, (3') un mono alkyle C¿1-4? alkyle-carbamoyle C¿1-4?, (4') un alkoxy C¿1-4? et (5') un mono alkoxy C¿1-4? alkyle-carbamoyle C¿1-4?, etc.; R?3¿représente un alkyle C¿1-4?; R?4¿ représente un alkoxy C¿1-4?, etc.; et n est un entier de 1 à 4. Ce composé est un composé de thiénopyrimidine antagoniste de la gonadolibérine.¿?

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