34 results about "Camptothecin Analog" patented technology

The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell proliferative diseases, such as cancer.

This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and / or drugs.

The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR / MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

A compound and a method of synthesizing a compound having general formula (1): wherein R<1> and R<2> are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxy group, an aryloxy group, an acyloxy group, -OC(O)OR, wherein R is an alkyl group, a carbamoyloxy group, a halogen, a hydroxy group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an acyl group, an amino group, -SR, wherein R is hydrogen, an acyl group, an alkyl group, or an aryl group, or R<1> and R<2> together form a group of the formula -O(CH2)nO- wherein n represents the integer 1 or 2; R<3> is H, F, a halogen atom, a nitro group, an amino group, a hydroxy group, or a cyano group; or R<2> and R<3> together form a group of the formula -O(CH2)n O- wherein n represents the integer 1 or 2; R<4> is H, a trialkylsilyl group, F, a C1-3 alkyl group, a C2-3 alkenyl group, a C2-3 alkynyl group, or a C1-3 alkoxy group; R<5> is a C1-10 alkyl group, an allyl group, a benzyl group or a propargyl group; and R<6>, R<7> and R<8> are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a -(CH2)NR<9> group, wherein N is an integer within the range of 1 through 10 and R<9> is a hydroxy group, alkoxy group, an amino group, alkylamino group, a dialkylamino group, a halogen atom, a cyano group or a nitro group; and R<11> is an alkylene group or an alkenylene group, and pharmaceutically acceptable salts thereof.

(20 S )esters of camptothecin analogs are provided. The compounds are (20 S ) esters of an oxyalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.