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Title:
エストロン誘導体およびその製造方法
Document Type and Number:
Japanese Patent JP4481660
Kind Code:
B2
Abstract:
Estrone derivatives (I) are new. Estrone derivatives of formula (I) and their stereoisomers, hydrates, salts or ester are new. [Image] X 1, X 2H or (CH 2) mCH(COOH)(CH 2) nR 1; R 11-7C haloalkyl; R aOH; and R b2-5C alkynyl; or CR aR b= CO; m : 2-14; n : 2-7; and provided that X 1and X 2are not both H. ACTIVITY : Cytostatic; Osteopathic. In tests using ICR mice, administration of 10-(3-hydroxy-17-oxo-estra-1,3,5 (10)-trien-11beta -yl)-2-(4,4,5,5,6,6,7,7,7-nonafluoroheptyl)decanoic acid (Ia) at 10 mg/kg orally for 3 days inhibited 99% of estrogen activity. MECHANISM OF ACTION : Aromatase-Inhibitor; Anti-Estrogen.

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Inventors:
Yoshiaki Nabuchi
Hiroshi Araya
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Kazumi Morikawa
Yoshitake Kannabe
Yoshihito Otake
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Kenji Taniguchi
Toshiaki Hengsei
Takasu Nao
Application Number:
JP2003584076A
Publication Date:
June 16, 2010
Filing Date:
April 02, 2003
Export Citation:
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Assignee:
Chugai Pharmaceutical Co., Ltd.
International Classes:
C07J1/00; A61K31/566; A61P19/10; A61P35/00; A61P43/00; C07J9/00
Foreign References:
WO2001042186A1
Attorney, Agent or Firm:
Kazuo Shamoto
Tadashi Masui
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Takumi Terachi