Patent US5395850A successfully refreshed from Google Patents.
US5395850A
Expired / Lapsed
US
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6,7-epoxy paclitaxels
Assignee: Bristol Myers Squibb Co
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Filing: 1994-03-10
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Granted: 1995-03-07
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Expires: 2014-03-10
Abstract
Abstract The present invention provides paclitaxel derivatives of formula I ##STR1## in which R 1 is --COR z , in which R z is RR o N--, RHN--, RO-- or R; R 2 is C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, or a radical of the formula --W--R x in which W is a bond, C 2-6 alkenediyl, or --(CH 2 ) 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 C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups; R and R o are independently C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, C 2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups. Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.
Inventors
- 👤 Gregory Roth
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 15:56
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/02; C07D493/08; A; A61; A61P; A61P35/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
145 words
A compound of formula I ##STR26## in which R 1 is --COR z , in which R z is RR o N--, RHN--, RO-- or R; R 2 is C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, or a radical of the formula --W--R x in which W is a bond, C 2-6 alkenediyl, or --(CH 2 ) 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 C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups; R and R o are independently C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, C 2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups.
Claim 2
Dependent Claim
145 words
A compound of formula I ##STR26## in which R 1 is --COR z , in which R z is RR o N--, RHN--, RO-- or R; R 2 is C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, or a radical of the formula --W--R x in which W is a bond, C 2-6 alkenediyl, or --(CH 2 ) 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 C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups; R and R o are independently C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, C 2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C 1-6 alkyl, C 1-6 alkoxy, halogen or --CF 3 groups.
Claim 3
Dependent Claim
29 words
A compound of claim 1 in which is RO-- or R; R 2 is C 2-6 alkenyl, phenyl, furyl or thienyl; and R is C 1-6 alkyl or phenyl.
Claim 4
Dependent Claim
8 words
The compound of claim 2 that is 6,7-α-epoxypaclitaxel.
Claim 5
Dependent Claim
8 words
The compound of claim 2 that is 3'-N-debenzoyl-N-t-butoxycarbonyl-3'-desphenyl-3'-(2-furyl)-6,7-α-epoxypaclitaxel.
Claim 6
Dependent Claim
8 words
The compound of claim 2 that is 3'-desphenyl-3'-(2-furyl)-6,7-α-epoxypaclitaxel.
Claim 7
Dependent Claim
8 words
The compound of claim 2 that is 3'-N-debenzoyl-N-t-butoxycarbonyl-3'-desphenyl-3'-isobutenyl-6,7-α-epoxypaclitaxel.
Claim 8
Dependent Claim
39 words
A pharmaceutical formulation which comprises as an active ingredient a compound as claimed in any one of claims 1 to 6, or a pharmaceutically acceptable salt thereof, associated with one or more pharmaceutically acceptable carriers, excipients or diluents therefor.
Claim 9
Independent Claim
29 words
A method for treating mammalian tumors which comprises administering to a mammal a tumor sensitive amount of a compound as claimed in any one of claims 1 to 6.
Claim 10
Dependent Claim
7 words
6,7-α-Epoxy Baccatin III of the formula ##STR27##
Claim 11
Dependent Claim
7 words
6,7-α-Epoxy Baccatin III of the formula ##STR27##
References Cited (Backward Citations)
US5227400A
Cited
US5254580A
Cited
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