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Title:
【発明の名称】タモキシフェンおよびタモキシフェン類縁体の向子宮効果を削減する方法
Document Type and Number:
Japanese Patent JPH10506111
Kind Code:
A
Abstract:
The present invention provides a method of minimizing the uterotrophic effect of non-steroidal antiestrogen compounds of formula II wherein either R<4> is H or a lower alkyl radical and R<5> is a lower alkyl radical, or R<4> and R<5> are joined together with the adjacent nitrogen atom to form a heterocyclic radical; R<6> is H or a lower alkyl radical; R<7> is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical; R<8> is H or OH; and n is 2; or a pharmaceutically acceptable salt thereof, wherein said formula II compound is administered to a woman for the treatment or prevention of breast carcinoma, comprising concurrently or sequentially administering to said woman a compound of formula I wherein R<1> is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); R<2> is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); n is 2 or 3; and R<3> is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. The present invention further provides pharmaceutical compositions comprising a compound of formula I and a compound of formula II together with a pharmaceutically acceptable carrier, excipient, or diluent.

Inventors:
Bryant, Henry Earlman
Fontana, Stephen Anthony
Application Number:
JP51113195A
Publication Date:
June 16, 1998
Filing Date:
September 18, 1995
Export Citation:
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Assignee:
ELI LILLY AND COMPANY
International Classes:
A61K31/135; A61K31/138; A61K31/40; A61K31/445; A61K31/452; A61K31/535; A61K31/5375; C07D295/08; A61K31/55; A61K45/06; A61P13/02; A61P15/00; A61P35/00; C07D207/06; (IPC1-7): C07D295/08; A61K31/135; A61K31/40; A61K31/445; A61K31/535; A61K31/55; C07D207/06
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)