摘要:
Compounds of formula I: as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
摘要:
The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.
摘要:
A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.
摘要:
The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要:
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
摘要:
Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
摘要:
Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
摘要:
There are disclosed avermectin derivatives which incorporate a spacer between the disaccharide and the aglycone. The synthetic spacer-containing analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.
摘要:
There are disclosed synthetic marcfortine derivatives of the natural products marcfortine A, marcfortine B, and marcfortine C. The synthetic derivatives are described in the following formula: ##STR1## wherein: n is 0 or 1R.sub.1 is hydrogen, loweralkyl, benzyl, lower alkanoyl, benzenesulfonyl in which the benzene ring is substituted with from 0 to 3 substituents selected from lower alkyl groups, lower alkoxy groups and halogen atoms, lower alkylamino-carbonyl, lower alkoxy-carbonyl;R.sub.24 is hydrogen, halogen or lower alkoxy (provided that R.sub.24 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position),R.sub.25 is hydrogen or halogen (provided that R.sub.25 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position);R.sub.29 is hydrogen, lower alkyl, alkoxyalkyl, haloalkyl, lower alkenyl, lower alkynyl, benzyl, lower alkanoyl, substituted benzenesulfonyl, lower alkylamino-carbonyl, not hydrogen or methyl if R.sub.1 is hydrogen; and the broken line represents a single or double bond between carbons 24 and 25.The compounds are active antiparasitic agents useful in particular against insect and nematode pests, and compositions for that use are disclosed.