摘要:
A process of making taxane derivatives by reacting Baccatin III derivatives with an oxazolidine which contains a thioester substituent at the 4-position.
摘要:
A compound which is a benzocyclodecane of the formula I: wherein: at positions 8-9 and 11-12 independently represents a single or double bond, —R1 is ═O, or —OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH═CHR8, R8 is aryl or heterocyclyl; —R2 and —R3 are H, ═O or —OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then —R4 represents ═O, ═CH2, ═CHCOOR10, R10 is C1-C10 alkyl or aryl; ═CH(OCH3), —OR9; —CH2OR11, R11 is H or a sugar residue, —COR12, R12 is H, —OH or —OR10; or when at position 11-12 there is a double bond, then —R4 is —CH2OR11 or —COR12; —R5 and —R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 ═O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
摘要:
Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
摘要:
Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
摘要:
There are provided sarcodictyin derivatives or pharmaceutically acceptable salts thereof, which are characterized by a simplified chemical structure and have anti-tumor activity. A process for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
摘要:
The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.8 CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2;and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.
摘要:
Use, in the preparation of a medicament for use in the treatment of multiple sclerosis, of a compound which is a ureido derivative of formula (I) ##STR1## wherein each of m and n, which are the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a naphthyl group substituted by 1 to 3 sulfonic acid groups, or a pharmaceutically acceptable salt thereof.
摘要:
A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4##