Nevel 36 derivatives (6), bonding the phenolic hydroxyl group of 7-ethyl-10-hydroxycamptothecin (4) with diamines through a monocarbamate linkage, were synthesized and their antitumor activity was evaluated in vivo. The derivatives were soluble in water as their HC1 salts wiht the E lactone ring intact and exhibited significant antitumor activity. One of the derivatives, 6-27 showed excellent activity against L1210 leukemia and other murine tumors.The structure of its hydrochloride trihydrate (CPT-11) was determined by spectroscopic and crystallographic methods.
10A-AZALIDE COMPOUND CROSSLINKED AT 10A- AND 12-POSITIONS
申请人:Sugimoto Tomohiro
公开号:US20110237784A1
公开(公告)日:2011-09-29
A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even
Hemophilus influenzae
, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).
Substituted azetidinones as anti-inflammatory and antidegenerative agents
申请人:MERCK & CO. INC.
公开号:EP0525973A2
公开(公告)日:1993-02-03
New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.