US2013143950A1PendingUtilityA1
Compounds and Methods for the Treatment of Cancer
Individually held — no corporate assignee on recordPriority: Jan 13, 2006Filed: Jul 3, 2012Published: Jun 6, 2013
Est. expiryJan 13, 2026(expired)· nominal 20-yr term from priority
Inventors:Ralph A. Zingaro
A61K 48/00A61K 31/203A61P 35/02C07F 9/72A61K 31/555A61K 45/06A61K 31/285C07F 9/82A61P 35/00
48
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Claims
Abstract
The present invention provides organic arsenicals which may be used to treat numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.
Claims
exact text as granted — not AI-modified1 - 10 . (canceled)
11 . A method for treating cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof
wherein
X is S or Se;
W is O, S, or (R)(R), where each occurrence of R is independently H or a C 1-2 alkyl; n is an integer from 2 to 8;
R 1 and R 2 are independently C 1-10 alkyl;
R 3′ is —H, C 1-10 alkyl, or C 0-6 alkyl-COOR 6 ;
R 3 is H, amino, cyano, halogen, aryl, aralkyl, heteroaryl, heteroaralkyl, carboxyl, C 1-10 alkyl, C 1-10 alkyl, or C 1-10 alkenyl; C 1-10 alkynyl;
R 4 is —OH, —H, —CH 3 , amino, —OC(O)C 1-10 aralkyl, —OC(O)C 1-10 alkyl, or —OC(O)aryl;
R 5 is —OH, cyano, C 1-10 alkoxy, amino, O-aralkyl, —OC(O)C 1-10 aralkyl, —OC(O)C 1-10 alkyl, or —OC(O)aryl, or a glycine substituent; and
R 6 is H or C 1-10 alkyl.
12 . The method of claim 11 , wherein said cancer comprises a solid tumor.
13 . The method of claim 12 , wherein said cancer is brain, lung; liver, spleen, kidney, lymph node, small intestine, pancreas, blood cells, bone, colon/colorectal, stomach, breast, endometrium, prostate, testicle, ovary, central nervous system, skin, head and neck, esophagus, or bone marrow cancer.
14 . The method of claim 11 , wherein said cancer is a hematological cancer.
15 . The method of claim 12 , wherein said cancer is leukemia, lymphoma, multiple myeloma, myelodysplasia, myeloproliferative disease, or refractory leukemia.
16 . The method of claim 13 , wherein said cancer is acute promyelocytic leukemia.
17 . The method of claim 11 , wherein said cancer is a central nervous system cancer.
18 . The method of claim 11 , wherein the cancer is kidney cancer.
19 . The method of claim 18 , wherein the cancer is renal cell cancer.
20 . The method of claim 11 , wherein the cancer is colon/colorectal cancer.
21 . The method of claim 11 , wherein said therapeutically effective amount is 0.1-1000 mg/kg.
22 . The method of claim 21 , wherein said therapeutically effective amount is 1-500 mg/kg.
23 . The method of claim 22 , wherein said therapeutically effective amount is 10-100 mg/kg.
24 . The method of claim 11 , wherein said compound is administered daily.
25 . The method of claim 11 , wherein said compound is administered by injection.
26 . The method of claim 11 , wherein an additional agent or therapy is administered to said patient.
27 . The method of claim 26 , wherein said additional agent is all-transretinoic acid, 9-cis retinoic acid, Am-80 or ascorbic acid.
28 . The method of claim 26 , wherein said additional agent or therapy is selected from a chemotherapeutic agent or therapy, an immunotherapeutic agent or therapy, gene therapy, and surgery.
29 - 42 . (canceled)
43 . The method of claim 11 , wherein W is O.
44 . The method of claim 11 , wherein R 3 and R 3′ are both H.
45 . The method of claim 11 , wherein R 4 is H.
46 . The method of claim 11 , wherein R 5 is selected from OH and C 1-6 alkoxy.
47 . The method of claim 11 , wherein R 5 is OH.
48 . The method of claim 11 , wherein X is S.
49 . The method of claim 11 , wherein R 1 and R 2 are the same and are together selected from methyl, ethyl, propyl, and isopropyl.
50 . The method of claim 11 , wherein R 3 and R 3′ are both H.
51 . The method of claim 11 , wherein R 4 is H.Join the waitlist — get patent alerts
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