US5773464A
Expired / Lapsed
US
⏱️ 0.0 years remaining
C-10 epoxy taxanes
Assignee: Bristol Myers Squibb Co
•
Filing: 1997-08-29
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Granted: 1998-06-30
•
Expires: 2017-08-29
Abstract
Abstract The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
Inventors
- 👤 Michael A. Walker
- 👤 John F. Kadow
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 18:43
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/02; C07D493/10; C07D305/00; C07D305/14
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
146 words
A compound of formula I, or a pharmaceutically acceptable salt thereof ##STR20## wherein: R is phenyl, p-fluorophenyl, C 3-6 cycloalkyl, C 1-6 alkyl or C 1-6 alkenyl; R A is hydrogen; R B is independently --NHC(O)Ph or --NHC(O)O-(C 1-6 alkyl); R C is hydrogen; R D is hydroxy; R 2 is phenyl; R 4 is methyl; L is O; R 6 and R 6' are each hydrogen; R 7' is hydrogen; R 7 is hydrogen, hydroxy, --OCH 2 OCH 3 , --OCH 2 SCH 3 or when taken together with R 19 forms a cyclopropane ring; R 9 and R 9' together form an oxo (keto) group; R 10 and R 10' together form an epoxide group which can be optionally substituted with C 1-6 alkyl; R 14 is hydrogen; and R 19 is methyl or when taken together with R 7 forms a cyclopropane ring.
Claim 2
Dependent Claim
146 words
A compound of formula I, or a pharmaceutically acceptable salt thereof ##STR20## wherein: R is phenyl, p-fluorophenyl, C 3-6 cycloalkyl, C 1-6 alkyl or C 1-6 alkenyl; R A is hydrogen; R B is independently --NHC(O)Ph or --NHC(O)O-(C 1-6 alkyl); R C is hydrogen; R D is hydroxy; R 2 is phenyl; R 4 is methyl; L is O; R 6 and R 6' are each hydrogen; R 7' is hydrogen; R 7 is hydrogen, hydroxy, --OCH 2 OCH 3 , --OCH 2 SCH 3 or when taken together with R 19 forms a cyclopropane ring; R 9 and R 9' together form an oxo (keto) group; R 10 and R 10' together form an epoxide group which can be optionally substituted with C 1-6 alkyl; R 14 is hydrogen; and R 19 is methyl or when taken together with R 7 forms a cyclopropane ring.
Claim 3
Dependent Claim
112 words
The compound of claim 1, or a pharmaceutically acceptable salt thereof wherein: R is phenyl or p-fluorophenyl; R A is hydrogen; R B is independently --NHC(O)Ph or --NHC(O)OtBu; R C is hydrogen; R D is hydroxy; R 2 is phenyl; R 4 is methyl; L is O; R 6 and R 6' are each hydrogen; R 7' is hydrogen; R 7 is hydroxy, --OCH 2 OCH 3 or --OCH 2 SCH 3 ; R 9 and R 9' together form an oxo (keto) group; R 10 and R 10' together form an epoxide group which can be optionally substituted with C 1-6 alkyl; R 14 is hydrogen; and R 19 is methyl.
Claim 4
Dependent Claim
16 words
The compound of claim 2 having the formula Ia or a pharmaceutically acceptable salt thereof, ##STR21##
Claim 5
Dependent Claim
16 words
The compound of claim 2 having the formula Ib or a pharmaceutically acceptable salt thereof, ##STR22##
Claim 6
Dependent Claim
16 words
The compound of claim 2 having the formula Ic, or a pharmaceutically acceptable salt thereof, ##STR23##
Claim 7
Dependent Claim
16 words
The compound of claim 2 having the formula Id, or a pharmaceutically acceptable salt thereof, ##STR24##
Claim 8
Dependent Claim
16 words
The compound of claim 2 having the formula Ie, or a pharmaceutically acceptable salt thereof, ##STR25##
Claim 9
Dependent Claim
16 words
The compound of claim 2 having the formula If, or a pharmaceutically acceptable salt thereof, ##STR26##
Claim 10
Dependent Claim
16 words
The compound of claim 2 having the formula Ig, or a pharmaceutically acceptable salt thereof, ##STR27##
Claim 11
Dependent Claim
16 words
A compound of claim 2 having the formula Ih, or a pharmaceutically acceptable salt thereof, ##STR28##
Claim 12
Dependent Claim
16 words
The compound of claim 1 having the formula Ij, or a pharmaceutically acceptable salt thereof, ##STR29##
Claim 13
Dependent Claim
16 words
The compound of claim 1 having the formula Ik, or a pharmaceutically acceptable salt thereof, ##STR30##
Claim 14
Dependent Claim
16 words
The compound of claim 1 having the formula Im, or a pharmaceutically acceptable salt thereof, ##STR31##
Claim 15
Dependent Claim
16 words
The compound of claim 1 having the formula In, or a pharmaceutically acceptable salt thereof, ##STR32##
Claim 16
Dependent Claim
16 words
The compound of claim 1 having the formula Io or a pharmaceutically acceptable salt thereof, ##STR33##
Claim 17
Dependent Claim
16 words
The compound of claim 1 having the formula Ip or a pharmaceutically acceptable salt thereof, ##STR34##
Claim 18
Dependent Claim
16 words
The compound of claim 1 having the formula Iq, or a pharmaceutically acceptable salt thereof, ##STR35##
Claim 19
Dependent Claim
16 words
The compound of claim 1 having the formula Ir, or a pharmaceutically acceptable salt thereof, ##STR36##
Claim 20
Dependent Claim
16 words
The compound of claim 2 having the formula Is, or a pharmaceutically acceptable salt thereof, ##STR37##
Claim 21
Dependent Claim
16 words
The compound of claim 2 having the formula It, or a pharmaceutically acceptable salt thereof, ##STR38##
Claim 22
Dependent Claim
23 words
A pharmaceutical formulation which comprises an antitumor effective amount of a compound of formula I as claimed in any one of claims 1-20.
Claim 23
Independent Claim
34 words
A method for inhibiting tumor growth in a mammalian host which comprises administering to said mammal a tumor-growth inhibiting amount of a compound of formula I as claimed in any one of claims 1-20.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 2001-06-29 | 2001-12-29 | 2002-06-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2005-06-29 | 2005-12-29 | 2006-06-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2009-06-29 | 2009-12-29 | 2010-06-30 | $7700.00 | Window Closed / Lapsed |