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Last Updated: November 30, 2021

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Claims for Patent: 10,202,357

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Summary for Patent: 10,202,357
Title:Class of quinolone heterocyclic aromatic molecules for cancer treatment
Abstract: The invention is directed to new class of quinolone heterocyclic aromatic molecules (Renotinibs) and their use in the treatment of cancer, in particular, cancer that harbor abnormal human epidermal growth factor receptors (EGFRs).
Inventor(s): Wang; Jujun (Plano, TX), Tsao; Allen (Wind Lake, WI), Liu; Xiaomei (Flushing, NY)
Assignee: RenoTarget Therapeutics, Inc. (Wind Lake, WI)
Application Number:15/803,478
Patent Claims:1. A compound having the structure of Formula I: ##STR00013## wherein: R1 is selected from the group consisting of: ##STR00014## where n is 0, 1, 2, 3, or 4; R2 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, --NO.sub.2 and a halogen, R3 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, and a halogen, R4 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, --NO.sub.2, and a halogen, R5 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, and a halogen, R6 is selected from the group consisting of: --H, and a halogen, R7 is selected from the group consisting of: --H, and a halogen, R8 is selected from the group consisting of: --H, and an ethynyl, and R9 is selected from the group consisting of: --H, and a halogen, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1, having the structure of Formula II: ##STR00015## wherein R is a halogen, or the pharmaceutically acceptable salt thereof.

3. The compound or the pharmaceutically acceptable salt thereof of claim 2, wherein R is selected from the group consisting of: fluoride, chloride, and bromide.

4. The compound of claim 3, wherein R is a fluoride.

5. The compound of claim 1, having the structure of Formula III: ##STR00016## wherein R is a halogen, or the pharmaceutically acceptable salt thereof.

6. The compound or pharmaceutical acceptable salt thereof of claim 5, wherein R is selected from the group consisting of: fluoride, chloride, bromide, and iodide.

7. A pharmaceutical composition comprising: a compound having the structure of Formula I: ##STR00017## wherein: R1 is selected from the group consisting of: ##STR00018## where n is 0, 1, 2, 3, or 4; R2 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, and a halogen, R3 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, and a halogen, R4 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, --NO.sub.2, and a halogen, R5 is selected from the group consisting of: --H, --CH.sub.3, --OCH.sub.3, and a halogen, R6 is selected from the group consisting of: --H, and a halogen, R7 is selected from the group consisting of: --H, and a halogen, R8 is selected from the group consisting of: --H, and an ethynyl, and R9 is selected from the group consisting of: --H, and a halogen, or a salt thereof; and a pharmaceutically acceptable carrier.

8. The pharmaceutical composition of claim 7, further comprising at least one additional anti-cancer agent selected from the group consisting of: a conventional chemotherapeutic agent, a protein kinase inhibitor, a topoisomerase inhibitor, a mitotic kinesin inhibitor, a histone deacetylase inhibitor, a mTOR inhibitor, a growth factor inhibitor, a growth factor receptor inhibitor, a transcriptional factor inhibitor, an anticancer monoclonal antibody, and glucocorticoid hormones for the simultaneous, separate, or sequential treatment of cancer.

9. The composition of claim 8, wherein the conventional chemotherapeutic agent is selected from the group consisting of: an alkylating agent, an anti-metabolitic agent, an antibiotic, an anti-tubule agent, and an anti-hormonal agent.

10. The composition of claim 8, wherein the conventional chemotherapeutic agent is selected from the group consisting of: mechlorethamine, cyclophosphamide, Busulfan, chlorambucil, leukeran, paraplatin, cisplatin, carboplatin, platinol, Methotrexate (MTX), 6-mercaptopurine (6-MP), cytarabine (Ara-C), floxuridine (FUDR), fluorouracil, hydroxyurea (Hydrea), etoposide (VP16), actinomycin D, bleomycin, mithramycin, daunorubicin, paclitaxel, and its derivatives, vinca and its derivatives, bicalutamide, Flutamide, Tamoxifen, and Megestrol.

11. The composition of claim 8, wherein the protein kinase inhibitor is selected from the group consisting of: inhibitors of cyclin-dependent kinases, tyrosine kinases, phosphoinositide 3-kinase PI3K/AKT, protein kinase C, casein kinases, MAP kinases, and Src kinases.

12. The composition of claim 8, wherein the protein kinase inhibitor is selected from the group consisting of: midostaurin, 7-hydroxystaurosporine, bryostatin 1, perifosine, ilmofosine, Ro 31-8220, Ro 32-0432, GO 6976, ISIS-3521, macrocyclic bis (indolyl) maleimides, AZD9291, and erlotinib.

13. The composition of claim 8, wherein the anticancer monoclonal antibody is selected from the group consisting of: Cetuximab, Herceptin, and Bevacizumab.

14. The composition of claim 8, wherein the glucocorticoid hormone is selected from the group consisting of: dexamethasone, prednisone, prednisolone, metyylprednisolone, and hydrocoritisone.

Details for Patent 10,202,357

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 1998-09-25 ⤷  Free Forever Trial 2036-11-09
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 2017-02-10 ⤷  Free Forever Trial 2036-11-09
Eli Lilly And Company ERBITUX cetuximab Injection 125084 2004-02-12 ⤷  Free Forever Trial 2036-11-09
Eli Lilly And Company ERBITUX cetuximab Injection 125084 2007-03-28 ⤷  Free Forever Trial 2036-11-09
Genentech, Inc. AVASTIN bevacizumab Injection 125085 2004-02-26 ⤷  Free Forever Trial 2036-11-09
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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