US2023192750A1PendingUtilityA1
Salts of diphosphate phosphoramidate of nucleosides as anticancer compounds
Est. expiryDec 5, 2037(~11.4 yrs left)· nominal 20-yr term from priority
C07H 19/10A61P 35/02C07H 19/207A61P 35/00A61K 31/7052C07H 19/20A61K 31/7068A61K 31/7076
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Claims
Abstract
The present invention relates to compounds comprising a salt of a diphosphate phosphoramidate of a nucleoside drug, e.g., clofarabine. The compounds are useful in the treatment of cancer, e.g., leukemia.
Claims
exact text as granted — not AI-modifiedWe claim:
1 . A compound of formula (I), or a pharmaceutically acceptable salt thereof:
wherein
R 1 is selected from: C 1 -C 24 -alkyl, C 0 -C 4 -alkylene-C 3 -C 8 -cycloalkyl and C 0 -C 4 -alkylene-aryl;
R 2 and R 3 are independently selected from H, C 1 -C 6 -alkyl and C 1 -C 3 -alkylene-R 7 ;
R 4 is H;
R 5 is aryl;
R 6 is
R 7 is selected from aryl, imidazole, indole, SR a , OR a , CO 2 R a , CO 2 NR a R a , NR a R b and NH(=NH)NH 2 ;
Z 1 is 0;
X is at each occurrence a pharmaceutically acceptable cation;
wherein each aryl is either phenyl or naphthyl;
wherein where any of R 1 , R 2 , R 3 , R 5 or R 7 is an alkyl, cycloalkyl, or aryl, that alkyl, cycloalkyl, or aryl group is optionally substituted with from 1 to 4 substituents selected from: halo, nitro, cyano, NR a R a , NR a S(O) 2 R a , NR a C(O)R a , NR a CONR a R a , NR a CO 2 R a , OR a , SR a , SOR a , SO3R a , SO 2 R a , SO 2 NR a R a , CO 2 R a , C(O)R a , CONR a R a , CR a R a NR a R a , C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl and C 1 -C 4 -haloalkyl;
wherein R a is independently at each occurrence selected from: H and C 1 -C 4 -alkyl; and R b is independently at each occurrence selected from: H, and C 1 -C 4 -alkyl and C(O)—C 1 -C 4 -alkyl.
2 . The compound of claim 1 , wherein R 1 is selected from C 5 -C 7 -cycloalkyl, C 1 -C 8 -alkyl, and benzyl.
3 . The compound of claim 1 , wherein R 1 is selected such that it comprises five or more carbon atoms.
4 . The compound of claim 2 , wherein R 1 is benzyl.
5 . The compound of claim 4 , wherein R 1 is unsubstituted benzyl.
6 . The compound of claim 2 , wherein R 1 is C 1 -C 8 -alkyl.
7 . The compound of claim 1 , wherein R 3 is H
8 . The compound of claim 1 , wherein R 2 is selected from C 1 -C 6 -alkyl and C 1 -C 3 -alkylene-R 7 .
9 . The compound of claim 8 , wherein R 2 is C 1 -C 4 -alkyl.
10 . The compound of claim 1 , wherein R 2 is H.
11 . The compound of claim 1 , wherein R 5 is phenyl.
12 . The compound of claim 11 , wherein R 5 is unsubstituted phenyl.
13 . The compound of claim 1 , wherein R 5 is naphthyl.
14 . The compound of claim 13 , wherein R 5 is 1-naphthyl.
15 . The compound of claim 13 , wherein R 5 is unsubstituted naphthyl.
16 . The compound of claim 15 , wherein R 5 is unsubstituted 1-naphthyl.
17 . A method for treating cancer, comprising administering to a patient in need thereof a compound of claim 1 , wherein the cancer is a leukemia or a lymphoma.
18 . The method of claim 17 , wherein the cancer is a leukemia selected from the group consisting of acute myeloid leukemia (AML), acute lymphoid leukemia (ALL), chronic myeloid leukemia (CIVIL), chronic lymphoid leukemia (CLL) and biphenotypic acute leukemia (BAL).
19 . The method of claim 17 , wherein the cancer is a lymphoma selected from the group consisting of Hodgkin's lymphoma and non-hodgkin's lymphoma.
20 . A pharmaceutical composition comprising the compound of claim 1 , and at least one pharmaceutically acceptable excipient.Join the waitlist — get patent alerts
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