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Generated: August 26, 2019

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Claims for Patent: 9,399,627

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Summary for Patent: 9,399,627
Title:Substituted macrocyclic compounds having proteasome inhibitory activity
Abstract: The disclosure provides for novel compounds which have proteasome inhibitory activity, pharmaceutical compositions made thereof, and methods of use thereof to treat various disorders, including cancer and nonmalignant tumors.
Inventor(s): Pirrung; Michael C. (Riverside, CA)
Assignee: The Regents of the University of California (Oakland, CA)
Application Number:14/408,140
Patent Claims:1. A compound having a structure of Formula II(a): ##STR00028## or a pharmaceutically acceptable salt thereof, wherein: X is NH, A.sup.1-A.sup.4 are each independently selected from hydrogen, deuterium, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkenyl, (C.sub.1-C.sub.6)alkynyl, (C.sub.1-C.sub.5)hetero-alkyl, (C.sub.1-C.sub.5)hetero-alkenyl, and (C.sub.1-C.sub.5)hetero-alkynyl; A.sup.6-A.sup.8 are each independently selected from hydrogen, deuterium, hydroxyl, halo, cyano, amino, nitro, alkoxy, alkoxycarbonyl, (C.sub.1-C.sub.4)alkyl, (C.sub.1-C.sub.4)alkenyl, (C.sub.1-C.sub.4)alkynyl, (C.sub.1-C.sub.3)hetero-alkyl, (C.sub.1-C.sub.3)hetero-alkenyl, and (C.sub.1-C.sub.3)hetero-alkynyl; A.sup.12 is selected from hydrogen, deuterium, hydroxyl, halo, cyano, amino, carboxamido, carboxyl, nitro, alkoxy, alkoxycarbonyl, (C.sub.1-C.sub.8)alkyl, (C.sub.1-C.sub.8)alkenyl, (C.sub.1-C.sub.8)alkynyl, (C.sub.1-C.sub.7)hetero-alkyl, (C.sub.1-C.sub.7)hetero-alkenyl, (C.sub.1-C.sub.7)hetero-alkynyl, cycloalkyl, aryl, and heterocycle; A.sup.13 is selected from hydrogen, deuterium, hydroxyl, halo, cyano, amino, carboxamido, carboxyl, nitro, alkoxy, alkoxycarbonyl, (C.sub.1-C.sub.4)alkyl, (C.sub.1-C.sub.4)alkenyl, (C.sub.1-C.sub.4)alkynyl, (C.sub.1-C.sub.3)hetero-alkyl, (C.sub.1-C.sub.3)hetero-alkenyl, (C.sub.1-C.sub.3)hetero-alkynyl, cycloalkyl, aryl, and heterocycle; and A.sup.14 is selected from hydrogen, deuterium, (C.sub.12-C.sub.16)alkyl, (C.sub.12-C.sub.16)alkenyl, (C.sub.12-C.sub.16)alkynyl, (C.sub.12-C.sub.15)hetero-alkyl, (C.sub.12-C.sub.15)hetero-alkenyl, (C.sub.12-C.sub.15)hetero-alkynyl, cycloalkyl, aryl, and heterocycle, wherein the heteroatoms making up the hetero-alkyl, hetero-alkenyl, hetero-alkynyl, and heterocycle are selected from N, O and/or S.

2. The compound of claim 1, wherein the compound is selected from: ##STR00029## ##STR00030## ##STR00031## or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1, comprising a structure of Formula II(b): ##STR00032## or a pharmaceutically acceptable salt thereof, wherein: X is NH; A.sup.14 is selected from hydrogen, deuterium, (C.sub.12-C.sub.16)alkyl, (C.sub.12-C.sub.16)alkenyl, (C.sub.12-C.sub.16)alkynyl, (C.sub.12-C.sub.15)hetero-alkyl, (C.sub.12-C.sub.15)hetero-alkenyl, (C.sub.12-C.sub.15)hetero-alkynyl, cycloalkyl, aryl, and heterocycle, wherein the heteroatoms making up the hetero-alkyl, hetero-alkenyl, hetero-alkynyl, and heterocycle are selected from N, O and/or S.

4. The compound of claim 3, wherein the compound is selected from: ##STR00033## or a pharmaceutically acceptable salt thereof.

5. A compound having the structure of: ##STR00034## or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutically acceptable carriers.

7. The pharmaceutical composition of claim 6, wherein the composition is formulated to be administered intravenously or subcutaneously.

8. The pharmaceutical composition of claim 7, wherein the intravenous or subcutaneously dose comprises between 1 mg/mL to 5 mg/mL of the compound.

9. A method of treating a subject having or suspected of having a cancer comprising administering a therapeutically effective amount of the compound of claim 1 to the subject in need thereof, wherein the subject has a cancer selected from the group consisting of ovarian cancer, breast cancer, colorectal cancer, colon cancer, rectal cancer, prostate cancer, kidney or renal cancer, CNS neoplasms, neuroblastomas, glioblastomas, melanomas, non-small cell lung cancer and leukemia.

10. The method of claim 9, wherein the cancer is kidney cancer.

11. The method of claim 9, further comprising the administration of one or more additional therapeutic agents.

12. The method of claim 11, wherein the one or more additional therapeutic agents are one or more chemotherapeutic agents.

13. The method of claim 12, wherein the one or more chemotherapeutic agents is selected from cisplatin, carboplatin, vinblastine, platinum, arginine deiminase, asparaginase, thiotepa, cyclosphosphamide, busulfan, improsulfan, piposulfan, calusterone, dromostanolone propionate, epitiostanol, mepitiostane, testolactone, aminoglutethimide, mitotane, trilostane, flutamide, nilutamide, bicalutamide, leuprolide, goserelin, aclacinomysins, actinomycin, authramycin, azaserine, bleomycins, cactinomycin, calicheamicin, carabicin, caminomycin, carzinophilin, chromomycins, dactinomycin, daunorubicin, detorubicin, 6-diazo-5-oxo-L-norleucine, doxorubicin, epirubicin, esorubicin, idarubicin, marcellomycin, mitomycins, mycophenolic acid, nogalamycin, olivomycins, peplomycin, potfiromycin, puromycin, quelamycin, rodorubicin, streptonigrin, streptozocin, tubercidin, ubenimex, zinostatin, zorubicin, tamoxifen, raloxifene, 4-hydroxytamoxifen, trioxifene, keoxifene, LY 117018, onapristone, toremifene, methotrexate, 5-fluorouracil, denopterin, methotrexate, pteropterin, trimetrexate, benzodopa, carboquone, meturedopa, uredopa, ethylenimines, altretamine, triethylenemelamine, trietylenephosphoramide, triethylenethiophosphaoramide, trimethylolomelamine, frolinic acid, chlorambucil, chlornaphazine, cholophosphamide, estramustine, ifosfamide, mechlorethamine, mechlorethamine oxide hydrochloride, melphalan, novembichin, phenesterine, prednimustine, trofosfamide, uracil mustard, carmustine, chlorozotocin, fotemustine, lomustine, nimustine, ranimustine, fludarabine, 6-mercaptopurine, thiamiprine, thioguanine, ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, enocitabine, floxuridine, paclitaxel, docetaxel, RFS 2000, thymidylate synthase inhibitors, aceglatone, aldophosphamide glycoside, aminolevulinic acid, amsacrine, bestrabucil, bisantrene, edatraxate, defofamine, demecolcine, diaziquone, difluoromethylornithine (DMFO), elformithine, elliptinium acetate, etoglucid, gallium nitrate, hydroxyurea, lentinan, lonidamine, mitoguazone, mitoxantrone, mopidamol, nitracrine, pentostatin, phenamet, pirarubicin, podophyllinic acid, 2-ethylhydrazide, procarbazine, razoxane, sizofuran, spirogermanium, tenuazonic acid, triaziquone, 2,2',2''-trichlorotriethylamine, urethane, vindesine, dacarbazine, mannomustine, mitobronitol, mitolactol, pipobroman, gacyto sine, arabinoside ("Ara-C"), chlorambucil, gemcitabine, 6-thioguanine, mercaptopurine, methotrexate, etoposide, ifosfamide, mitomycin C, mitoxantrone, vincristine, vinorelbine, navelbine, novantrone, teniposide, daunomycin, aminopterin, xeloda, ibandronate, CPT-11, retinoic acid, esperamicins, and capecitabine.

14. The method of claim 12, wherein the one or more chemotherapeutic agents is selected from vinblastine, floxuridine, 5-fluorouracil, capecitabine, gemcitabine, bortezomib, cyclophosphamide, melphalan, doxorubicin, idarubicin, cisplatin, etoposide, and bendamustine.

15. The compound of claim 1, wherein the compound has a structure of Formula II(a): ##STR00035## or a pharmaceutically acceptable salt thereof, wherein: X is NH; A.sup.1-A.sup.4, A.sup.6-A.sup.8, A.sup.12 are hydrogen; A.sup.13 is a 1-hydroxyethyl group; and A.sup.14 is a (C.sub.12-C.sub.16)alkenyl group.

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PCT Information
PCT FiledJune 14, 2013PCT Application Number:PCT/US2013/045854
PCT Publication Date:December 19, 2013PCT Publication Number:WO2013/188750

Details for Patent 9,399,627

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10 ➤ Sign Up The Regents of the University of California (Oakland, CA) 2032-06-15 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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International Patent Family for US Patent 9,399,627

Country Patent Number Publication Date
World Intellectual Property Organization (WIPO) 2013188750 Dec 19, 2013
World Intellectual Property Organization (WIPO) 2013188750 Feb 13, 2014
United States of America 2015141392 May 21, 2015
European Patent Office 2861565 Apr 22, 2015
European Patent Office 2861565 Dec 21, 2016
European Patent Office 2861565 Nov 11, 2015
>Country >Patent Number >Publication Date

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