Title:
6-置換エストラジオール誘導体およびその使用方法
Document Type and Number:
Japanese Patent JP2013512260
Kind Code:
A
Abstract:
Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ═CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n; R12 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH2]COOCH2, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)nCH3, —C2-C8 alkenyl-N—(CH2)nCH3, —C2-C8 alkynyl-O—(CH2)nCH3, —C2-C8 alkynyl-S—(CH2)nCH3, —C2-C8 alkynyl-N—(CH2)nCH3, —(CH2)m—OH, —(CH2)m—O—NH2, —(CH2)m—S—NH2, —NH(CH2)mCH3, —NH(CH2)mOCH3, —NH(CH2)mCHOH—COOH, —N(CH3)2, —(CH2)m(NH)CH2OH, —NHCOOH, —(CH2)mNHCOOH, —NO2, —SCN, —SO2alkyl, —B(OH)2, —(CH2)m N(CH3)—SO2—NH3, —(CH2)m—NH—SO2—NH2, —NHC(═S)CH3, and —NHNH2; and Y is selected from hydrogen, ═O, —OCO(R6) and —OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.
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Inventors:
Jager, James, Gee.
Application Number:
JP2012541227A
Publication Date:
April 11, 2013
Filing Date:
November 30, 2010
Export Citation:
Assignee:
Endies Incorporated
International Classes:
C07J1/00; A61K31/5685; A61P35/00; A61P43/00
Domestic Patent References:
| JPS4945866B1 | 1974-12-06 | |||
| JP2011522825A | 2011-08-04 | |||
| JPS4945866B1 | 1974-12-06 | |||
| JP2011522825A | 2011-08-04 |
Foreign References:
| WO2008067450A2 | 2008-06-05 | |||
| WO2007041564A2 | 2007-04-12 | |||
| WO2008067450A2 | 2008-06-05 | |||
| WO2007041564A2 | 2007-04-12 |
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JPN6014042367; Ｊｏｕｒｎａｌ ｏｆ Ｓｔｅｒｏｉｄ Ｂｉｏｃｈｅｍｉｓｔｒｙ ＆ Ｍｏｌｅｃｕｌａｒ Ｂｉｏｌｏｇｙ ９６, 2005, ５１-５８
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JPN6014042368; Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｉｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ １５, 2007, ７１４-７２６
JPN6014042369; Ｊｏｕｒｎａｌ ｏｆ Ｓｔｅｒｏｉｄ Ｂｉｏｃｈｅｍｉｓｔｒｙ １７, 1982, ５１１-５１５
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JPN6014042369; Ｊｏｕｒｎａｌ ｏｆ Ｓｔｅｒｏｉｄ Ｂｉｏｃｈｅｍｉｓｔｒｙ １７, 1982, ５１１-５１５
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JPN6014042369; Ｊｏｕｒｎａｌ ｏｆ Ｓｔｅｒｏｉｄ Ｂｉｏｃｈｅｍｉｓｔｒｙ １７, 1982, ５１１-５１５
Attorney, Agent or Firm:
Hatta International Patent Corporation