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Last Updated: April 25, 2024

Claims for Patent: 8,026,278


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Summary for Patent: 8,026,278
Title:Inhibitors of pyruvate kinase as therapeutic agents for cancer
Abstract: The present invention relates to compounds for the inhibition of pyruvate kinase and ATP production which are capable of inhibiting cancer cells proliferation.
Inventor(s): Smith; Brian R. (Lasalle, CA), Chan; Tak-Hang (Montreal, CA), Leyland-Jones; Brian (Montreal, CA)
Assignee:
Application Number:11/915,664
Patent Claims:1. A method of inhibiting a breast cancer cell growth in a subject comprising administering to the subject an effective amount of an inhibitor selected from the group consisting of: a compound of formula II: wherein, ##STR00015## X and Y represent H, halide, or alkyl group; A is ##STR00016## R and R' represent H, alkyl, or aryl or heteroaryl ester; R'' represents H, or alkyl, or aryl or heteroaryl ester; any isomers or salts thereof; with the proviso that the compound of formula II is not ##STR00017## wherein R.sub.a.dbd.H, (Z)--F, (Z)--Cl, (E)-Cl and (Z)--CH.sub.3; ##STR00018##

2. The method of claim 1, which further comprising administering a second chemotherapeutic agent.

3. The method of claim 2, wherein the second chemotherapeutic agent is selected from the group consisting of: altretamine, asparaginase, BCG, bleomycin sulfate, busulfan, carboplatin, carmusine, chlorambucil, cisplatin, claladribine, 2-chlorodeoxyadenosine, cyclophosphamide, cytarabine, dacarbazine imidazole carboxamide, dactinomycin, daunorubicin-dunomycin, dexamethosone, doxurubicin, docetaxol, trastuzumab, etoposide, floxuridine, fluorouracil, fluoxymesterone, flutamide, fludarabine, goserelin, hydroxyurea, idarubicin HCl, ifosfamide, interferon alfa, interferon alfa 2a, interferon alfa 2b, interferon alfa n3, irinotecan, leucovorin calcium, leuprolide, levamisole, lomustine, inegestrol, melphalan, L-sarcosylin, melphalan hydrochloride, MESNA, mechlorethamine, methotrexate, mitomycin, mitoxantrone, mercaptopurine, paclitaxel, plicamycin, prednisone, procarbazine, streptozocin, tamoxifen, 6-thioguanine, thiotepa, vinblastine, vincristine and vinorelbine tartrate.

4. The method of claim 1, wherein the effective amount of the inhibitor is delivered by direct intravenous or intraarterial injection to a tumor, or using a delivery system, or administered orally in the form of a tablet, capsule or liquid.

5. The methods of claim 1, wherein the inhibitor is delivered using a delivery system.

6. The methods of claim 2, wherein the second chemotherapeutic agent is delivered using a delivery system.

7. The method of claim 5, wherein the delivery system is selected from the group consisting of micelles, liposomes, transdermal and inhalation.

8. The method of claim 1, wherein the compound of formula II is chosen from: ##STR00019## wherein, X and Y represent H, halide, or alkyl group; A is ##STR00020## R and R' represent CH.sub.3; R'' represents CH.sub.3 or C.sub.2H.sub.5; any isomers or salts thereof.

Details for Patent 8,026,278

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 2039-03-29
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2039-03-29
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2039-03-29
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2039-03-29
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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