Title:
抗腫瘍性として活性な2-アルコキシエストラジオール・スルファメート
Document Type and Number:
Japanese Patent JP2005501849
Kind Code:
A
Abstract:
The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In said formula, R<1> and R<2> independently of one another represent H, methyl, C1-C4 acyl or benzyl, R<3> represents C1-C4 alkyl, or a group of formula CnFmHo, where n = 1, 2, 3, 4, 5 or 6, m > 1 and m + o = 2n + 1, R<4> and R<5> independently represent H, or together represent a methylene group or an additional bond, R<6> represents H and R<7> represents OH, OC1-C4 alkyl, OC1-C11 acyl or OSO2NR<1>R<2>, whereby in the B and C ring of the steroid skeleton the broken lines can additionally represent up to two double bonds. The inventive compounds are characterised by a 2-alkoxy substitution in conjunction with a 17-hydroxy substitution. They exhibit the specific activity of inhibiting tubulin polymerisation and can be used, for example, for treating prostatic carcinoma.
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Inventors:
Sherlitz-Hoffman, Ina
Hoffman, Jens
Hirish, alexander
Unger, Eberhard
Neumann, Tobias
Schwarz, Siegfried
Peters, Olaf
Michel, Thomas
Hoffman, Jens
Hirish, alexander
Unger, Eberhard
Neumann, Tobias
Schwarz, Siegfried
Peters, Olaf
Michel, Thomas
Application Number:
JP2003520751A
Publication Date:
January 20, 2005
Filing Date:
August 01, 2002
Export Citation:
Assignee:
Schering Actien Gezel Shaft
International Classes:
A61K31/565; A61P13/08; A61P15/00; A61P35/00; A61P43/00; C07J1/00; C07J31/00; (IPC1-7): A61K31/565; A61P13/08; A61P15/00; A61P35/00; A61P43/00; C07J1/00
Domestic Patent References:
| JPH07501515A | 1995-02-16 | |||
| JPH10507741A | 1998-07-28 |
Foreign References:
| WO2000066095A2 | 2000-11-09 | |||
| US5830886A | 1998-11-03 |
Other References:
JPN5003023892, ＭＡＣＣＡＲＴＨＹ−ＭＯＲＲＯＧＨ Ｌ, ＣＡＮＣＥＲ ＲＥＳＥＡＲＣＨ, 20001001, Ｖ６０ Ｎ１９, Ｐ５４４１−５４５０, US, ＡＭＥＲＩＣＡＮ ＡＳＳＯＣＩＡＴＩＯＮ ＦＯＲ ＣＡＮＣＥＲ ＲＥＳＥＡＲＣＨ
JPN5003019432, ＰＵＲＯＨＩＴ Ａ, ＩＮＴＥＲＮＡＴＩＯＮＡＬ ＪＯＵＲＮＡＬ ＯＦ ＣＡＮＣＥＲ, 20000215, Ｖ８５Ｎ４, Ｐ５８４−５８９, US
JPN5003019433, ＰＵＲＯＨＩＴ Ａ, ＪＯＵＲＮＡＬ ＯＦ ＳＴＥＲＯＩＤ ＢＩＯＣＨＥＭＩＳＴＲＹ ＡＮＤ ＭＯＬＥＣＵＬＡＲ ＢＩＯＬＯＧＹ, 1998, Ｖ６４Ｎ５, Ｐ２６９−２７５, GB, ＥＬＳＥＶＩＥＲ ＳＣＩＥＮＣＥ ＬＴＤ．
JPN6009011912, ＰＲＯＨＩＴＡ， Ａ．ｅｔ ａｌ．, "Ｎｏｎ−ｓｔｅｒｏｉｄａｌ ａｎｄ ｓｔｅｒｏｉｄａｌ ｓｕｌｆａｍａｔｅｓ： ｎｅｗ ｄｒｕｇｓ ｆｏｒ ｃａｎｃｅｒ ｔｈｅｒａｐｙ", ｏｌｅｃｕｌａｒ ａｎｄ Ｃｅｌｌｕｌａｒ Ｅｎｄｏｃｒｉｎｏｌｏｇｙ, 20010122, Ｖｏｌｕｍｅ １７１， Ｉｓｓｕｅｓ １−２, Ｐａｇｅｓ １２９−１３５
JPN6009060100, ＬＡＷＲＥＮＣＥ， Ｌ．Ｗ． ｅｔ ａｌ．, "Ｏｅｓｔｒｏｎｅ ３−Ｏ−（Ｎ−ａｃｅｔｙｌ）ｓｕｌｐｈａｍａｔｅ， ａ ｐｏｔｅｎｔｉａｌ ｍｏｌｅｃｕｌａｒ ｐｒｏｂｅ ｏｆ ｔｈｅ ａｃｔｉｖｅ ｓｉｔｅ ｏｆ ｏｅｓｔｒｏｎｅ ｓｕｌｐｈａ", Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｌｅｔｔｅｒｓ, 1997, Ｖｏｌｕｍｅ ７， Ｉｓｓｕｅ ２４, Ｐａｇｅｓ ３０７５−３０８０
JPN5003019432, ＰＵＲＯＨＩＴ Ａ, ＩＮＴＥＲＮＡＴＩＯＮＡＬ ＪＯＵＲＮＡＬ ＯＦ ＣＡＮＣＥＲ, 20000215, Ｖ８５Ｎ４, Ｐ５８４−５８９, US
JPN5003019433, ＰＵＲＯＨＩＴ Ａ, ＪＯＵＲＮＡＬ ＯＦ ＳＴＥＲＯＩＤ ＢＩＯＣＨＥＭＩＳＴＲＹ ＡＮＤ ＭＯＬＥＣＵＬＡＲ ＢＩＯＬＯＧＹ, 1998, Ｖ６４Ｎ５, Ｐ２６９−２７５, GB, ＥＬＳＥＶＩＥＲ ＳＣＩＥＮＣＥ ＬＴＤ．
JPN6009011912, ＰＲＯＨＩＴＡ， Ａ．ｅｔ ａｌ．, "Ｎｏｎ−ｓｔｅｒｏｉｄａｌ ａｎｄ ｓｔｅｒｏｉｄａｌ ｓｕｌｆａｍａｔｅｓ： ｎｅｗ ｄｒｕｇｓ ｆｏｒ ｃａｎｃｅｒ ｔｈｅｒａｐｙ", ｏｌｅｃｕｌａｒ ａｎｄ Ｃｅｌｌｕｌａｒ Ｅｎｄｏｃｒｉｎｏｌｏｇｙ, 20010122, Ｖｏｌｕｍｅ １７１， Ｉｓｓｕｅｓ １−２, Ｐａｇｅｓ １２９−１３５
JPN6009060100, ＬＡＷＲＥＮＣＥ， Ｌ．Ｗ． ｅｔ ａｌ．, "Ｏｅｓｔｒｏｎｅ ３−Ｏ−（Ｎ−ａｃｅｔｙｌ）ｓｕｌｐｈａｍａｔｅ， ａ ｐｏｔｅｎｔｉａｌ ｍｏｌｅｃｕｌａｒ ｐｒｏｂｅ ｏｆ ｔｈｅ ａｃｔｉｖｅ ｓｉｔｅ ｏｆ ｏｅｓｔｒｏｎｅ ｓｕｌｐｈａ", Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｌｅｔｔｅｒｓ, 1997, Ｖｏｌｕｍｅ ７， Ｉｓｓｕｅ ２４, Ｐａｇｅｓ ３０７５−３０８０
Attorney, Agent or Firm:
Atsushi Aoki
Takashi Ishida
Tetsuji Koga
Kazuhiro Nakamura
Masaya Nishiyama
Takashi Ishida
Tetsuji Koga
Kazuhiro Nakamura
Masaya Nishiyama