US2005250844A1PendingUtilityA1
Methods of treating cancer using C-4 carbonate taxanes
Est. expiryFeb 3, 2020(expired)· nominal 20-yr term from priority
Inventors:John F. KadowHarold MastalerzQiufen XueSteven HanselMary ZoecklerWilliam RoseJames G. Tarrant
A61K 31/337C07D 305/14
48
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Claims
Abstract
A process for the preparation of novel C-4 carbonate taxanes useful as antitumor agents.
Claims
exact text as granted — not AI-modified1 - 30 . (canceled)
31 . A method for treating cancer comprising administering to a patient in need thereof a therapeutically effective dose of one or more compounds of formula I
wherein:
R is phenyl, isopropyl, or tert butyl;
R 1 is —C(O)R Z in which R Z is (CH 3 ) 3 CO—, (CH 3 ) 3 CCH 2 —, CH 3 (CH 2 ) 3 O—, cyclobutyl-, cyclohexyloxy, or (2-furyl); and
R 2 is CH 3 C(O)O—,
or a pharmaceutically acceptable salt thereof.
32 . The method of claim 31 wherein one or more compounds of formula I are selected from the group consisting of compounds as shown in the table
R
R 1
R 2
Compound
(CH 3 ) 3 C—
(CH 3 ) 3 COC(O)—
CH 3 C(O)O—
Ia
(CH 3 ) 2 CH—
(CH 3 ) 3 COC(O)—
CH 3 C(O)O—
Ib
Phenyl-
(CH 3 ) 3 CCH 2 C(O)—
CH 3 C(O)O—
Ic
Phenyl-
CyclobutylC(O)—
CH 3 C(O)O—
Id
(CH 3 ) 3 C—
CyclohexylOC(O)—
CH 3 C(O)O—
Ie
(CH 3 ) 3 C—
(CH 3 ) 3 CCH 2 C(O)—
CH 3 C(O)O—
If
Phenyl-
(CH 3 ) 3 COC(O)—
CH 3 C(O)O—
Ig
Phenyl-
CH 3 (CH 2 ) 3 OC(O)—
CH 3 C(O)O—
Ih
(CH 3 ) 3 C—
CyclobutylC(O)—
CH 3 C(O)O—
Ij
(CH 3 ) 3 C—
(2-furyl)C(O)—
CH 3 C(O)O—
Ik
33 . The method of claim 32 wherein the compound of formula I is Compound Ia.
34 . The method of claim 31 wherein the cancer being treated is selected from the group consisting of cancers of the lungs, prostate, gastric, breast, liver and sarcomas.
35 . The method of claim 34 wherein the lung cancer being treated is non-small cell lung cancer.
36 . The method of claim 31 wherein the compound is administered orally.
37 . The method of claim 33 wherein the compound is administered orally.Cited by (0)
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