STEROID DERIVATIVE

Japanese Patent JPH0656670

A

PURPOSE: To obtain a new derivative useful for treatment of hyperlipemia, having ability to regulate directly or indirectly, synthesis of LDL receptor at chromosome level. CONSTITUTION: The compound of formula I R<1> is 1-4C alkyl or 1-4C haloalkyl; R<2> is H, methyl, etc.; R<3> is H, 1-6C alkyl, etc.; R<4> is H, =C-X<4> (X<4> is H, OH, etc.), etc.; R<5> is -A-Z-R<10> -X<3> [A is O, CH2 , etc.; Z is a bond, O, etc.; R<10> is divalent group derived from (substituted) 1-12C alkane, etc.; X<3> is H, (substituted) phenyl, etc.]; R<3> is H when the steroid skeleton is saturated, and R<13> is absent when the skeleton is unsaturated at the 4,5-positions; X<1> is hydroxy, amino, etc.; X<2> is O, H and H, etc.}, and pharmaceutically acceptable its salt. For example, [4α(E), 5α]-4-(2-butenyl) cholestan-3α-ol. The compound is, e.g. prepared by the reductive alkylation of 4-cholesten-3-one with alkylhalide in an inert solvent in the presence of a strong base and a proton souse.

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ROBAATO AREN AACHIYAA
RISA SERUSAMU BIIBAAZU
ROBAATO ARAN GATSUDOSUKII
HOOSHIEN RIN
DON BII MAKUKURUURE
JIEFUAASON REI MAKUKOOWAN
JIYOZEFU MASHIYUU POORATSUKU
ASHIYURAFU ARI RANPERUSAUDO
ROBAATO JIYON SHIYUMITSUTO
TERI AN SHIYUREIYAA
MERUBIN JIYOZEFU YUU

JP6796893A

March 01, 1994

March 26, 1993

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LILLY CO ELI

A61K31/56; A61K31/57; A61K31/575; A61K31/58; A61K38/44; A61P9/10; C07J1/00; C07J3/00; C07J7/00; C07J9/00; C07J13/00; C07J17/00; C07J21/00; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): A61K31/56; A61K31/575; C07J9/00

Aoyama Ryo (1 person outside)

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