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Last Updated: March 29, 2024

Claims for Patent: 9,040,567


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Summary for Patent: 9,040,567
Title:BAX agonist, compositions, and methods related thereto
Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
Inventor(s): Deng; Xingming (Lilburn, GA), Zhou; Jia (League City, TX), Ding; Chunyong (Shanghai, CN)
Assignee: Emory University (Atlanta, GA) Board of Regents of the University of Texas System (Austin, TX)
Application Number:14/239,177
Patent Claims:1. A compound of Formula IB, ##STR00036## or salt thereof wherein, Z is O, S, CH.sub.2, or NH; W is hydroxy, amino, alkylamino, dialkylamino, aryl, or heterocyclyl wherein W is optionally substituted with one or more R.sup.11; R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are each individually and independently hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl).sub.2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, aryl, or heterocyclyl, wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are optionally substituted with one or more, the same or different R.sup.10; R.sup.2 is nitro or amino wherein R.sup.2 is optionally substituted with one or more, the same or different R.sup.10; R.sup.10 is alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl).sub.2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, aryl, or heterocyclyl, wherein R.sup.10 is optionally substituted with one or more, the same or different R.sup.11; R.sup.11 is alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl).sub.2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, aryl, or heterocyclyl, wherein R.sup.11 is optionally substituted with one or more, the same or different R.sup.12; and R.sup.12 is halogen, nitro, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, formyl, carboxy, carbamoyl, mercapto, sulfamoyl, methyl, ethyl, methoxy, ethoxy, acetyl, acetoxy, methylamino, ethylamino, dimethylamino, diethylamino, N-methyl-N-ethylamino, acetylamino, N-methylcarbamoyl, N-ethylcarbamoyl, N,N-dimethylcarbamoyl, N,N-diethylcarbamoyl, N-methyl-N-ethylcarbamoyl, methylthio, ethylthio, methylsulfinyl, ethylsulfinyl, mesyl, ethylsulfonyl, methoxycarbonyl, ethoxycarbonyl, N-methylsulfamoyl, N-ethylsulfamoyl, N,N-dimethylsulfamoyl, N,N-diethylsulfamoyl, N-methyl-N-ethylsulfamoyl, carbocyclyl, aryl, or heterocyclyl.

2. The compound claim 1, wherein R.sup.2 is nitro.

3. The compound of claim 1, selected from the group: 4-{2-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethyl}-morpholine; 1-{2-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethyl}-piperazine; 2-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethanol; 2-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethylamine; 4-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-piperidine; 1-(4-Fluoro-benzenesulfonyl)-4-{2-[2-(2-nitro-fluoren-9-ylidenemethyl)-ph- enoxy]-ethyl}-piperazine; 1-(4-{2-[2-(2-Nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethyl}-piperazin-1-- yl)-ethanone; 1-Cyclopropanesulfonyl-4-{2-[2-(2-nitro-fluoren-9-ylidenemethyl)-phenoxy]- -ethyl}-piperazine; and 1-Methanesulfonyl-4-{2-[2-(2-nitro-fluoren-9-ylidenemethyl)-phenoxy]-ethy- l}-piperazine or salts thereof.

4. A pharmaceutical composition comprising a compound of claim 1, and a pharmaceutically acceptable excipient.

5. The pharmaceutical composition of claim 4, further comprising a second therapeutic agent.

6. A method of treating breast cancer comprising administering a pharmaceutical composition of claim 4 to a subject diagnosed with, exhibiting symptoms of, or at risk of cancer.

7. The method of claim 6, wherein the pharmaceutical compositions is administered in combination with a second chemotherapeutic agent.

8. The method of claim 7, wherein the second chemotherapeutic agent is gefitinib, erlotinib, docetaxel, cis-platin, 5-fluorouracil, gemcitabine, tegafur, raltitrexed, methotrexate, cytosine arabinoside, hydroxyurea, adriamycin, bleomycin, doxorubicin, daunomycin, epirubicin, idarubicin, mitomycin-C, dactinomycin and mithramycin, vincristine, vinblastine, vindesine, vinorelbine taxol, taxotere, etoposide, teniposide, amsacrine, topotecan, camptothecin bortezomib, anegrilide, tamoxifen, toremifene, raloxifene, droloxifene, iodoxyfene fulvestrant, bicalutamide, flutamide, nilutamide, cyproterone, goserelin, leuprorelin, buserelin, megestrol anastrozole, letrozole, vorazole, exemestane, finasteride, marimastat, trastuzumab, cetuximab, dasatinib, imatinib, bevacizumab, combretastatin, thalidomide, and/or lenalidomide or combinations thereof.

Details for Patent 9,040,567

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2039-02-26
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2039-02-26
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2039-02-26
Eli Lilly And Company ERBITUX cetuximab Injection 125084 03/28/2007 ⤷  Try a Trial 2039-02-26
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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