US2011301183A1PendingUtilityA1
Chemical synthesis of a highly potent epothilone
Individually held — no corporate assignee on recordPriority: Nov 22, 2005Filed: Aug 19, 2011Published: Dec 8, 2011
Est. expiryNov 22, 2025(expired)· nominal 20-yr term from priority
C07D 493/04C07D 519/00A61P 35/00C07D 417/06C07D 405/06
40
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Claims
Abstract
A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
Claims
exact text as granted — not AI-modified1 . A compound that corresponds in structure to Formula A-1, A-2, A-3 or A-4
wherein R A is an aromatic ring having the structure
wherein the depicted five-membered ring is aromatic and contains at least two ring atoms that are other than carbon,
each of X 1 , X 2 and X 3 is independently S, NR 1 , N, CH, or CR 2 ,
R 1 is C 1 -C 8 -hydrocarbyl or methylene-C 1 -C 8 -hydrocarbylether, and
R 2 is selected from the group consisting of C 1 -C 8 -hydrocarbyl, O—C 1 -C 8 -hydrocarbyl, halo, S—C 1 -C 8 -hydrocarbyl, methylenethio-C 1 -C 8 -hydrocarbyl and methylenethio-C 1 -C 8 -acyl, and
X 2 and X 3 together form a six-membered aromatic ring fused to the depicted five-membered aromatic ring.
2 - 5 . (canceled)
6 . The compound according to claim 1 wherein X 1 is S.
7 - 17 . (canceled)
18 . The compound according to claim 1 wherein R A is
19 . The compound according to claim 1 that corresponds in structure to Formula A-1.
20 . A compound that corresponds in structure to Formula B-1, B-2, B-3 or B-4
wherein R B is an aromatic ring having the structure
wherein
R 1 is selected from the group consisting of C 1 -C 8 -hydrocarbyl and methylene-C 1 -C 8 -hydrocarbylether, and
R 2 is selected from the group consisting of C 1 -C 8 -hydrocarbyl, O—C 1 -C 8 -hydrocarbyl, halo, S—C 1 -C 8 -hydrocarbyl, methylenethio-C 1 -C 8 -hydrocarbyl and methylenethio-C 1 -C 8 -acyl.
21 . The compound according to claim 20 wherein R 1 is C 1 -C 8 -hydrocarbyl.
22 . The compound according to claim 20 wherein R 2 is S—C 1 -C 8 -hydrocarbyl.
23 . The compound according to claim 20 wherein R 1 is O—C 1 -C 8 -hydrocarbyl.
24 . The compound according to claim 20 wherein R 1 is halo.
25 . A compound that corresponds in structure to Formula C-1, C-2, C-3 or C-4
wherein R C is an aromatic ring having a structure selected from the group consisting of
26 . A compound that corresponds in structure to the formula
27 - 28 . (canceled)
29 . A composition containing a pharmaceutically effective amount of a compound of claim 1 dissolved or dispersed in a pharmaceutically acceptable diluent.
30 . The composition according to claim 29 wherein R A is
31 . A pharmaceutical composition comprising a compound according to claim 19 present in an effective amount dissolved or dispersed in a pharmaceutically acceptable diluent.
32 . The composition according to claim 31 wherein R B isJoin the waitlist — get patent alerts
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