Patent US5773464A successfully refreshed from Google Patents.
US5773464A
Expired / Lapsed
US
⏱️ 0.0 years remaining
C-10 epoxy taxanes
Assignee: Bristol Myers Squibb Co
•
Filing: 1997-08-29
•
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 18:55
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.
References Cited (Backward Citations)
US4814470A
Cited
US4960790A
Cited
WO1993002067A1
Cited
WO1993006093A1
Cited
US5272171A
Cited
US5352806A
Cited
US5248796A
Cited
EP0590267A2
Cited
WO1994008984A1
Cited
EP0600517A1
Cited
FR2698871A1
Cited
WO1994013655A1
Cited
WO1994014787A1
Cited
WO1994015929A1
Cited
WO1994015599A1
Cited
US5254580A
Cited
WO1994020485A1
Cited
EP0617034A1
Cited
US5395850A
Cited
WO1995033736A1
Cited
EP0764643A1
Cited
WO1996003394A1
Cited
GB2296239A
Cited
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 |