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Last Updated: April 19, 2024

Claims for Patent: 8,207,143


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Summary for Patent: 8,207,143
Title:Methods of treating cancer and other conditions or disease states using LFMAU and LDT
Abstract: The present invention relates to the use of the compound according to formula (I), below for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states: Where X is H or F; R.sup.1 and R.sup.2 are independently H, an acyl group, a C.sub.1-C.sub.20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (A) or (B) group; Where Nu is a radical of a biologically active compound such as an anticancer, antiviral or antihyperproliferative compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R.sup.8 is independently H, or a C.sub.1-C.sub.20 alkyl or ether group, preferably a C.sub.1-C.sub.12 alkyl group; k is 0-12, preferably, 0-2; and pharmaceutically acceptable salts thereof. ##STR00001##
Inventor(s): Cheng; Yung-chi (Woodbridge, CT)
Assignee: Yale University (New Haven, CT)
Application Number:13/004,401
Patent Claims:1. A method of treating psoriasis, genital warts or a hyperproliferative disease in a patient in need thereof comprising administering to said patient an effective amount of a compound according to the structure: ##STR00008## where X is H or F; R.sup.1 and R.sup.2 are independently H, an acyl group, a C.sub.1-C.sub.20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a ##STR00009## where Nu is a radical of a biologically active anticancer, antihyperproliferative or antiviral compound such that an amino group or hydroxyl group from said biologically active compound forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R.sup.8 is independently H, or a C.sub.1-C.sub.20 alkyl or ether group; and k is 0-12, or pharmaceutically acceptable salts thereof.

2. A method according to claim 1 wherein R.sup.1 is H, a C.sub.2-C.sub.18 acyl group or a phosphate group and R.sup.2 is H.

3. The method according to claim 1 wherein R.sup.1 is H and R.sup.2 is H.

4. The method according to claim 1 wherein said hyperproliferative disease is hyperkeratosis, ichthyosis, keratoderma or lichen planus.

5. A method of treating HCV or a chronic inflammatory disease comprising administering to a patient in need of treatment an effective amount of a compound according to the structure: ##STR00010## where X is H or F; R.sup.1 and R.sup.2 are independently H, an acyl group, a C.sub.1-C.sub.20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a ##STR00011## where Nu is a radical of a biologically active compound such that an amino group or hydroxyl group from said biologically active compound forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R.sup.8 is independently H, or a C.sub.1-C.sub.20 alkyl or ether group; and k is 0-12, or a pharmaceutically acceptable salts thereof, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient.

6. The method according to claim 5 wherein said chronic inflammatory disease is rheumatoid arthritis or osteoarthritis.

7. A compound according to the structure: ##STR00012## where X is H or F; R.sup.1 and R.sup.2 are independently a ##STR00013## where Nu is a radical of a biologically active compound such that an amino group or hydroxyl group from said biologically active compound forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R.sup.2 is independently H, or a C.sub.1-C.sub.20 alkyl or ether group; k is 0-12; and pharmaceutically acceptable salts thereof.

8. The compound according to claim 7 wherein said biologically active compound is an anticancer, agent selected from the group consisting of Aldesleukin; Alemtuzumab; alitretinoin; allopurinol; altretamine; amifostine; anastrozole; arsenic trioxide; Asparaginase; BCG Live; bexarotene capsules; bexarotene gel; bleomycin; busulfan intravenous; busulfan oral; calusterone; capecitabine; carboplatin; carmustine; carmustine with Polifeprosan 20 Implant; celecoxib; chlorambucil; cisplatin; cladribine; cyclophosphamide; cytarabine; cytarabine liposomal; dacarbazine; dactinomycin; actinomycin D; Darbepoetin alfa; daunorubicin liposomal; daunorubicin, daunomycin; Denileukin diftitox, dexrazoxane; docetaxel; doxorubicin; doxorubicin liposomal; Dromostanolone propionate; Elliott's B Solution; epirubicin; Epoetin alfa estramustine; etoposide phosphate; etoposide (VP-16); exemestane; Filgrastim; floxuridine (intraarterial); fludarabine; fluorouracil (5-FU); fulvestrant; gemtuzumab ozogamicin; gleevec; goserelin acetate; hydroxyurea; Ibritumomab Tiuxetan; idarubicin; ifosfamide; imatinib mesylate; Interferon alfa-2a; Interferon alfa-2b; irinotecan; letrozole; leucovorin; levamisole; lomustine (CCNU); meclorethamine (nitrogen mustard); megestrol acetate; melphalan (L-PAM); mercaptopurine (6-MP); mesna; methotrexate; methoxsalen; mitomycin C; mitotane; mitoxantrone; nandrolone phenpropionate; Nofetumomab; LOddC; Oprelvekin; oxaliplatin; paclitaxel; pamidronate; pegademase; Pegaspargase; Pegfilgrastim; pentostatin; pipobroman; plicamycin; mithramycin; porfimer sodium; procarbazine; quinacrine; Rasburicase; Rituximab; Sargramostim; streptozocin; surafenib; talbuvidine (LDT); talc; tamoxifen; tarceva; temozolomide; teniposide (VM-26); testolactone; thioguanine (6-TG); thiotepa; topotecan; toremifene; Tositumomab; Trastuzumab; tretinoin (ATRA); Uracil Mustard; valrubicin; valtorcitabine (monoval LDC); vinblastine; vinorelbine; zoledronate; and mixtures thereof.

9. The compound according to claim 7 wherein said biologically active compound is an anti-viral compound.

10. The compound according to claim 7 wherein said biologically active compound is an anticancer, antihyperproliferative or antiviral compound.

11. The compound according to claim 7 wherein said biologically active compound is an anticancer compound.

12. The compound according to claim 7 wherein said biologically active compound is an antihyperproliferative compound.

13. The compound according to claim 7 wherein X is H.

14. The compound according to claim 7 wherein X is F.

15. The compound according to claim 8 wherein X is H.

16. The compound according to claim 8 wherein X is F.

17. The compound according to claim 10 wherein X is H.

18. The compound according to claim 10 wherein X is F.

19. A pharmaceutical composition comprising an effective amount of a compound according to claim 7 in combination with a pharmaceutically acceptable carrier, additive or excipient.

20. A pharmaceutical composition comprising an effective amount of a compound according to claim 8 in combination with a pharmaceutically acceptable carrier, additive or excipient.

Details for Patent 8,207,143

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Recordati Rare Diseases, Inc. ELSPAR asparaginase For Injection 101063 01/10/1978 ⤷  Try a Trial 2025-06-07
Merck Teknika Llc TICE BCG bcg live For Injection 102821 06/21/1989 ⤷  Try a Trial 2025-06-07
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 06/04/1986 ⤷  Try a Trial 2025-06-07
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 ⤷  Try a Trial 2025-06-07
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b Injection 103132 ⤷  Try a Trial 2025-06-07
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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