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US5395850A Expired / Lapsed US ⏱️ 0.0 years remaining

6,7-epoxy paclitaxels

Assignee: Bristol Myers Squibb Co
•
Filing: 1994-03-10
•
Granted: 1995-03-07
•
Expires: 2014-03-10
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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 05:57
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

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1998-03-06 1998-09-05 1999-03-07 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2002-03-06 2002-09-05 2003-03-07 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2006-03-06 2006-09-05 2007-03-07 $7700.00 Window Closed / Lapsed

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