You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Claims for Patent: 8,552,056


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,552,056
Title:Biologically active taxane analogs and methods of treatment by oral administration
Abstract: The present invention relates to a novel chemical compound of formula S-(1): ##STR00001## for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
Inventor(s): McChesney; James D. (Etta, MS), Tapolsky; Gilles (Boulder, CO), Emerson; David E. (Longmont, CO), Marshall; John (Washington, DC), Ahmed; Tauseef (Hawthorne, NY), Cohn; Allen (Denver, CO), Kurman; Michael (Upper Saddle River, NJ), Modiano; Manuel (Tucson, AZ)
Assignee: Tapestry Pharmaceuticals, Inc. (Boulder, CO)
Application Number:13/620,852
Patent Claims:1. A composition comprising a compound having a structure of formula S-(1): ##STR00031## a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the stereochemistry of the 7,9-vinyl acetal in the compound has S-configuration in a diastereomeric excess of at least 90%; and one or more pharmaceutically acceptable ingredient selected from the group consisting of inert or physiologically active excipients, diluents, and adjuvants.

2. The composition of claim 1, wherein the one or more pharmaceutically acceptable ingredient is selected from the group consisting of inert or physiologically active excipients, diluents or adjuvants is/are selected from the group consisting of phomopsin, dolastatin, bevacizumab (Avastin.TM.), steganacin, paclitaxel, taxotere, vinblastine, vincristine, vindesine, vinorelbine, navelbine, colchicine, maytansine, ansamitocin, Iressa, Tarceva, Herceptin, lapatinib, vandetanib, Sorafenib, BAY-57-9006, bevacizumab, cetuximab, gemtuzumab, panitumumab, rituximab, tositumomab, trastuzumab, apolizumab, oregovomab, mitumomab, alembuzumab, ibritumomab, vitaxin, SU-6668, semaxanib, sunitinib malate, SU-14813, vandetanib, Recentin, CP-547632, CEP-7055, AG-013736, pazopanib, combretastatin, squalamine, combrestatin A4 phosphate, TNP-470, neovastat, dasatinib, imatinib, nilotinib, sorafenib, sunitinib, triethylenethiophosphoramine, alitretinoin, altretamine, arsenic trioxide, asparaginase, bexarotene, denileukin diftitox, hydroxycarbamide, masoprocol, mitotane, pegaspargase, tretinoin, raltitrexed, IL-10, IL-12, bortezomib, leuprolide, interferon .beta., pegylated interferons, atrasentan, melphalan, cyclophosphamide, chlormethine, chlorambucil, trofosfamide, ifosfamide, nitromin, busulfan, thiotepa, chlorambucil, CC-1065, temozolomide, pipobroman, dacarbazine, mechlorethamine, procarbazine, uramustine, RSU-1069, CB-1954, hexamethylmelamine, cisplatin, carboplatin, oxaliplatin, BBR3464, satraplatin, tetraplatin, iproplatin, amsacrine, netropsin, pibenzimol, mitomycin, duocarmycin, dactinomycin, distamycin, mithramycin, chromomycin, olivomycin, anthramycin, bleomycin, liblomycin, rifamycin, actinomycin, adramycin, trichostatin A, propamidine, stilbamidine, rhizoxin, nitroacridine, geldamycin, 17-AAG, 17-DMAG, plicamycin, deoxycoformycin, levamisole, daunorubicin, doxorubicin, epirubicin, idarubicin, mitroxantrone, valrubicin, carmustine, fotemustine, lomustine, streptozocin, gemcitabine, 5-fluorouracil (5-FU), fludarabine, cytarabine, capecitabine, mercaptopurine, cladribine, clofarabine, thioguanine, pentostatin, floxuridine, pentostatin, aminopterin, methotrexate, pemetrexed, camptothecin, irinotecan, topotecan, epipodophyllotoxin, etoposide, teniposide, aminogluthetimide, anastrozole, exemestane formestane, letrozole, fadrozole, aminoglutethimide, leuprorelin, buserelin, goserelin, triptorelin, abarelix, estramustine, megestrol, flutamide, casodex, anandron, cyproterone acetate, finasteride, bicalutamide, tamoxifen or its citrate salt, droloxifene, trioxifene, raloxifene or zindoxifene, a derivative of 17-.beta.-estradiol such as ICI 164, ICI 384, ICI 182, ICI 780, testolactone, fulvestrant, toremifene, testosterone, fluoxymesterone, dexamethasone, triamcinolone, dromostanolone propionate, megestrol acetate, methyltestosterone, chlorotrianisene, hydroxyprogesterone, medroxyprogesterone acetate, reloxafine, etanercept, thalidomide, revimid (CC-5013), aziridoquinones, misonidazole, NLA-1, RB-6145, misonidazole, nimorazole, RSU-1069, SR-4233, porfimer, photofrin, verteporfin, merocyanin 540, tin etiopurpurin, PUVA, aminolevulinic acid, methyl aminolevulinate, minodronate, zoledronic acid, ibandronate sodium hydrate or clodronate disodium, misonidazole, misonidazole, amifostene, oblimersen, TIMP-1 or TIMP-2, marimastat, TLK-286 and mixtures thereof.

3. The composition of claim 1, wherein the one or more adjuvants is selected from the group consisting of an anti-mitotic agent and an anti-microtubule agent.

4. The composition of claim 1, formulated as a solid formulation.

5. The composition of claim 4, wherein the solid formulation is formulated as immediate and/or modified release.

6. The composition of claim 5, wherein the modified release formulation is selected from the group consisting of delayed-, sustained-, pulsed-, controlled-, targeted and programmed release.

7. The composition of claim 4, wherein the solid formulation is in a form selected from the group consisting of tablets, capsules containing particulates, liquids or powders, lozenges (including liquid-filled), chews, multi- and nano-particulates, gels, solid solution, liposome, films, and ovules.

8. The composition of claim 7, wherein the solid formulation is in the form of tablets.

9. The composition of claim 8, wherein the solid formulation contains a disintegrant selected from the group consisting of sodium starch glycolate, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium, crospovidone, polyvinylpyrrolidone, methyl cellulose, microcrystalline cellulose, lower alkyl-substituted hydroxypropyl cellulose, starch, pregelatinised starch and sodium alginate.

10. The composition of claim 8, wherein the tablets comprise a binder, the binder selected from the group consisting of microcrystalline cellulose, gelatin, sugars, polyethylene glycol, natural and synthetic gums, polyvinylpyrrolidone, pregelatinised starch, hydroxypropyl cellulose and hydroxypropyl methylcellulose.

11. A method of treating cancer, the method comprising administering to a subject a composition comprising a compound having a structure represented by the following formula S-(1): ##STR00032## a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the stereochemistry of the 7,9-vinyl acetal in said compound has S-configuration in a diastereomeric excess of at least 90%.

12. The method of claim 11, wherein a therapeutically effective amount of the compound of formula S-(1) is administered by week or by 21 days for a total dose selected from the group consisting of from about 7 mg/m.sup.2 to about 555 mg/m.sup.2, from about 7 mg/m.sup.2 to about 240 mg/m.sup.2, from about 7 mg/m.sup.2 to about 185 mg/m.sup.2 during a 21 day period.

13. The method of claim 11, wherein the composition is administered by oral, pulmonary, intraperitoneal (ip), intravenous (iv), intramuscular (im), subcutaneous (sc), transdermal, buccal, nasal, sublingual, ocular, rectal or vaginal administration.

14. The method of claim 13, wherein the parenteral administration is selected from intravenous injection and intravenous infusion.

15. The method of claim 13, wherein the parenteral administration is for about 60 minutes or less.

16. The method of claim 14, wherein the said intravenous infusion is once every 7 days for 3 weeks, followed by a 7 day rest period, in a 28 day cycle, for at least one cycle.

17. The method of claim 14, wherein the intravenous infusion is once every 21 days, in a 21 day cycle, for at least one cycle.

18. The method of claim 11, wherein the composition comprises the compound of formula S-(1) at a dose of 240 mg/m.sup.2 or less, or 185 mg/m.sup.2 or less.

19. The method of claim 11, wherein the composition comprises the compound of formula S-(1) at a dose of 185 mg/m.sup.2 or less, or 160 mg/m.sup.2 or less.

20. The method of claim 11, wherein the composition comprises the compound of formula S-(1) in a unit dose selected from the group consisting of about 200 mg to 400 mg.

21. The method of claim 20, wherein the composition comprises the compound of formula S-(1) in a unit dose selected from the group consisting of about 250 mg, 300 mg and 350 mg.

Details for Patent 8,552,056

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 2039-02-26
Servier Pharmaceuticals Llc ONCASPAR pegaspargase Injection 103411 02/01/1994 ⤷  Try a Trial 2039-02-26
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2039-02-26
Idec Pharmaceuticals Corp. RITUXAN rituximab Injection 103737 02/19/2002 ⤷  Try a Trial 2039-02-26
Eisai, Incorporated ONTAK denileukin diftitox Injection 103767 02/05/1999 ⤷  Try a Trial 2039-02-26
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.