Title:
複素芳香族スルホンアミドプロドラッグ
Document Type and Number:
Japanese Patent JP2009517425
Kind Code:
A
Abstract:
Sulfonamide prodrugs (I) are new. Sulfonamide prodrugs of fromula (I) are new Drug-OCO-X-SO 2NH 2 (I) X : optionally substituted heteroaromatic group or alkyl-heteroaromatic group; Drug : pharmaceutical able to form a carboxylate ester through an hydroxy group, such as steroids, antimalarials, nucleosides, isoflavonoids, optionally substituted . An independent claim is included for methods for preparing (I). ACTIVITY : Contraceptive; Antiinfertility; Cytostatic; Gynecological; Antiinflammatory; Antiallergic; Protozoacide. MECHANISM OF ACTION : Inhibition of carboanhydrase (CA). The compound 3-hydroxyestra-1,3,5(10)-trien-17beta -yl 6'-sulfamoylnicotinate has ID50 against human CAI and CAII of 2900 and 31 nM, respectively.
Inventors:
Burba, Ralph
Nubemaier, Reinhard
Nubemaier, Reinhard
Application Number:
JP2008542679A
Publication Date:
April 30, 2009
Filing Date:
November 27, 2006
Export Citation:
Assignee:
Bayer Schering Pharma Aktiengesellschaft
International Classes:
C07J43/00; A61K31/565; A61K31/567; A61K31/569; A61K31/575; A61K31/58; A61P5/00; A61P15/00; A61P15/18; A61P29/00; A61P35/00; A61P37/08; A61P43/00; C07J33/00; C07B61/00
Domestic Patent References:
| JP2003534386A | 2003-11-18 |
Other References:
JPN6012034924; Ｐｒｏｃｅｅｄｉｎｇｓ ｏｆ ｔｈｅ Ｒｏｙａｌ Ｓｏｃｉｅｔｙ ｏｆ Ｌｏｎｄｏｎ， Ｓｅｒｉｅｓ Ｂ：Ｂｉｏｌｏｇｉｃａｌ Ｓｃｉｅｎｃｅｓ Ｖｏｌ．１９３， Ｎｏ．１１１１, 1976, ｐ．１０７-１２５
Attorney, Agent or Firm:
Atsushi Aoki
Takashi Ishida
Fukumoto product
Tetsuji Koga
Kazuhiro Nakamura
Yoichi Watanabe
Masaru Nakajima
Takashi Ishida
Fukumoto product
Tetsuji Koga
Kazuhiro Nakamura
Yoichi Watanabe
Masaru Nakajima