Thienopyrimidine compounds, their production and use

Details Thienopyrimidine compounds, their production and use Thienopyrimidine compounds, their production and use

C - Chemistry, Metallurgy

07

D

C07D 495/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2368108

A compound of formula (I) wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula (A) wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH- antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.

L'invention concerne un composé représenté par la formule (I) dans laquelle R<1> et R<2> représentent chacun hydrogène, hydroxy, alcoxy C1-4, alcoxy-carbonyle C1-4 ou alkyle C1-4 qui peuvent être substitués; R<3> représente hydrogène, halogène, hydroxy ou alcoxy C1-4 qui peuvent être substitués; ou deux R<3> adjacents peuvent former alkylènedioxy C1-4; R<4> représente hydrogène ou alkyle C1-4; R<6> représente alkyle C1-4 qui peut être substitué ou un groupe représenté par la formule (A) dans laquelle R<5> représente hydrogène ou R<4> et R<5> peuvent former un hétérocycle; et n vaut 0-5, ou un sel correspondant présente une remarquable activité antagoniste de GnRH, et est utile pour prévenir ou traiter des maladies dépendantes des hormones sexuelles.

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