Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
160 words
A compound of formula I in which R¹ is -COR z in which R z is RO- or R; R² is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, or a radical of the formula -W-R x in which W is a bond, C₂₋₆ alkenediyl, or -(CH₂) t -, in which t is one to six; and R x is naphthyl, phenyl, or heteroaryl, and furthermore R x can be optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups; R a is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; R b and R c are both hydroxy or together form a bond with the carbon atoms to which they are attached; and R and R o are independently C₁₋₆ alkyl, C₂₋₆ alkenyl, C₃₋₆ cycloalkyl, C₂₋₆ alkynyl, or phenyl, optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups.
Claim 2
Dependent Claim
41 words
A compound of claim 1 in which R¹ is benzoyl or t-butoxycarbonyl; R² is phenyl, furyl, or thienyl; R a is acetyloxy; and R b and R c together form a bond with the carbon atoms to which they are attached.
Claim 3
Dependent Claim
8 words
The compound of claim 2 that is 6,7-dehydropaclitaxel.
Claim 4
Dependent Claim
8 words
The compound of claim 2 that is 6,7-dehydro-3'-(2-furyl)-3'-N-debenzoyl-N-t-butoxycarbonylpaclitaxel.
Claim 5
Dependent Claim
8 words
The compound of claim 2 that is 6,7-dehydro-3'-(2-furyl)paclitaxel.
Claim 6
Dependent Claim
8 words
The compound of claim 2 that is 6,7-dehydro-3'-(2-thienyl)-3'-N-debenzoyl-N-t-butoxycarbonylpaclitaxel.
Claim 7
Dependent Claim
30 words
A compound of claim 1 in which R¹ is benzoyl or t-butoxycarbonyl; R² is phenyl, furyl, or thienyl; R a is acetyloxy; and R b and R c are hydroxy.
Claim 8
Dependent Claim
8 words
The compound of claim 7 that is 6α-hydroxy-7α-hydroxypaclitaxel.
Claim 9
Dependent Claim
39 words
A pharmaceutical formulation which comprises as an active ingredient a compound as claimed in any one of claims 1 to 8, or a pharmaceutically acceptable salt thereof, associated with one or more pharmaceutically acceptable carriers, excipients or diluents therefor.
Claim 10
Dependent Claim
26 words
The use of at least one compound as claimed in any one of claims 1 to 8 for preparing a pharmaceutical composition for treating mammalian tumors.
Claim 11
Dependent Claim
5 words
The compound of the formula
Claim 12
Dependent Claim
115 words
A process for making the compounds of claims 1 to 8 comprising: (a) reacting compound of formula IIa, in which Cbz is benzyloxycarboyl, with diethylaminosulfur trifluoride to afford compound of formula IIIa or b) reacting a compound of formula VIa with a compound of formula VII, in which R³ is a hydroxy protecting group, to afford a compound of formula VIII or c) reacting a compound of formula II, in which R j is -OCOR, H, -OR, -OR³, -OSO₂R, -OCONR o R, -OCONHR, -OCO₂(CH₂) t R, or -OCO₂R, with diethylaminosulfur trifluoride to afford a compound of formula III or d) reacting a compound of formula XIII with OsO₄ to afford a compound of formula XII
Claim 13
Dependent Claim
22 words
A process for making the compound of claim 11 comprising: reacting compound Ia with an ester reducing agent and isolating compound VIa.
Claim 14
Dependent Claim
14 words
The process of claim 13 in which the ester reducing agent is tetrabutylammonium borohydride.