Title:
新規なステロイドおよびステロイド模倣物;それらの製造のための方法;ならびにそれらの使用
Document Type and Number:
Japanese Patent JP2006518715
Kind Code:
A
Abstract:
The invention relates to the production and use of novel 14beta-alkyl-18-norsteroids, 8alpha,14beta-dialkyl-18-norsteroids, spiro[cyclopentano-perhydronaphthalin]-3,1'-pentanes or hexanes in addition to 14beta-fluoro-15beta,17beta-dihydroxy-steroids, by reacting 17-hydroxy-14,15-epoxi-steroids with water-free acids or Lewis acids and followed by derivatisation. The resulting compounds can be used as intermediate products for or as medicaments in human and veterinary medicine, whereby the emphasis is on improving inflammatory processes, hormone replacement therapy and the use thereof as enzyme inhibitors in the treatment of tumours.
Inventors:
Kash, Helmut
Rietoke, Beatrice
Rietoke, Beatrice
Application Number:
JP2006501482A
Publication Date:
August 17, 2006
Filing Date:
January 28, 2004
Export Citation:
Assignee:
Sterix limited
International Classes:
C07J1/00; A61K31/122; A61K31/566; A61P5/00; A61P25/28; A61P31/00; A61P35/00; A61P39/06; A61P43/00; C07J75/00
Other References:
JPN6010024166, ＢＵＬＬ，Ｊ．Ｒ． ｅｔ ａｌ, "Ｓｔｅｒｅｏｓｅｌｅｃｔｉｖｅ ｓｙｎｔｈｅｓｉｓ ｏｆ １４β−ｅｔｈｙｌ−１９−ｎｏｒｓｔｅｒｏｉｄｓ", Ｓｏｕｔｈ Ａｆｒｉｃａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ, 1990, Ｖｏｌ．４３， Ｎｏ．１, ｐ．４２−４５
JPN6010024169, ＢＵＬＬ，Ｊ．Ｒ． ｅｔ ａｌ, "Ｃｏｎｆｏｒｍａｔｉｏｎ ｏｆ ａ ｄｅｒｉｖａｔｉｚｅｄ １４α−ｍｅｔｈｙｌ−９β−ｅｓｔｒａｄｉｏｌ ｆｒｏｍ ５００ ＭＨｚ ｈｙｄｒｏｇｅｎ ＮＭＲ ｓｐｅｃｔｒｏｓｃｏｐｙ", Ｓｏｕｔｈ Ａｆｒｉｃａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ, 1990, Ｖｏｌ．４３， Ｎｏ．１, ｐ．４６−４７
JPN6010024170, ＢＩＳＣＨＯＦＢＥＲＧＥＲ，Ｋ． ｅｔ ａｌ, "１４−Ｍｅｔｈｙｌ ｓｔｅｒｏｉｄｓ． Ｐａｒｔ ６． Ｓｙｎｔｈｅｓｉｓ， ｃｏｎｆｏｒｍａｔｉｏｎａｌ ａｎａｌｙｓｉｓ， ａｎｄ ｘ−ｒａｙ ｃｒｙｓｔａｌｌｏｇｒａｐｈｙ ｏｆ １４α−", Ｓｏｕｔｈ Ａｆｒｉｃａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ, 1987, Ｖｏｌ．４０， Ｎｏ．２, ｐ．１２３−１３０
JPN6010024173, ＢＩＳＣＨＯＦＢＥＲＧＥＲ，Ｋ． ｅｔ ａｌ, "１４−Ｍｅｔｈｙｌ ｓｔｅｒｏｉｄｓ． Ｐａｒｔ ３． Ｓｙｎｔｈｅｓｉｓ ｏｆ （±）−１４α−ｍｅｔｈｙｌ−９β−ｅｓｔｒａｄｉｏｌ ａｎｄ ｒｅｌａｔｅｄ １４α−ｍｅｔｈｙｌ−１９", Ｔｅｔｒａｈｅｄｒｏｎ, 1985, Ｖｏｌ．４１， Ｎｏ．２, ｐ．３６５−３７４
JPN6010024176, ＪＣＳ Ｃｈｅｍ． Ｃｏｍｍ．, 1980, Ｎｏ．９, ｐ．３９８−３９９
JPN6010024169, ＢＵＬＬ，Ｊ．Ｒ． ｅｔ ａｌ, "Ｃｏｎｆｏｒｍａｔｉｏｎ ｏｆ ａ ｄｅｒｉｖａｔｉｚｅｄ １４α−ｍｅｔｈｙｌ−９β−ｅｓｔｒａｄｉｏｌ ｆｒｏｍ ５００ ＭＨｚ ｈｙｄｒｏｇｅｎ ＮＭＲ ｓｐｅｃｔｒｏｓｃｏｐｙ", Ｓｏｕｔｈ Ａｆｒｉｃａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ, 1990, Ｖｏｌ．４３， Ｎｏ．１, ｐ．４６−４７
JPN6010024170, ＢＩＳＣＨＯＦＢＥＲＧＥＲ，Ｋ． ｅｔ ａｌ, "１４−Ｍｅｔｈｙｌ ｓｔｅｒｏｉｄｓ． Ｐａｒｔ ６． Ｓｙｎｔｈｅｓｉｓ， ｃｏｎｆｏｒｍａｔｉｏｎａｌ ａｎａｌｙｓｉｓ， ａｎｄ ｘ−ｒａｙ ｃｒｙｓｔａｌｌｏｇｒａｐｈｙ ｏｆ １４α−", Ｓｏｕｔｈ Ａｆｒｉｃａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ, 1987, Ｖｏｌ．４０， Ｎｏ．２, ｐ．１２３−１３０
JPN6010024173, ＢＩＳＣＨＯＦＢＥＲＧＥＲ，Ｋ． ｅｔ ａｌ, "１４−Ｍｅｔｈｙｌ ｓｔｅｒｏｉｄｓ． Ｐａｒｔ ３． Ｓｙｎｔｈｅｓｉｓ ｏｆ （±）−１４α−ｍｅｔｈｙｌ−９β−ｅｓｔｒａｄｉｏｌ ａｎｄ ｒｅｌａｔｅｄ １４α−ｍｅｔｈｙｌ−１９", Ｔｅｔｒａｈｅｄｒｏｎ, 1985, Ｖｏｌ．４１， Ｎｏ．２, ｐ．３６５−３７４
JPN6010024176, ＪＣＳ Ｃｈｅｍ． Ｃｏｍｍ．, 1980, Ｎｏ．９, ｐ．３９８−３９９
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita
Takaaki Yasumura
Natsuki Morishita