Claims for Patent: 9,402,850

Summary for Patent: 9,402,850

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 (Galveston, TX)
Assignee:	Emory University (Atlanta, GA) Board of Regents, The University of Texas System (Austin, TX)
Application Number:	14/709,580
Patent Claims:	1. A method of treating lung cancer comprising administering an effective amount of a compound of Formula IB, to a subject in need thereof, ##STR00035## 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. The method of claim 1, wherein the compound is administered in combination with a second chemotherapeutic agent. 5. The method of claim 4, 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, 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 9,402,850

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2034-08-17
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2034-08-17
Eli Lilly And Company	ERBITUX	cetuximab	Injection	125084	02/12/2004		2034-08-17
Eli Lilly And Company	ERBITUX	cetuximab	Injection	125084	03/28/2007		2034-08-17