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Last Updated: April 26, 2024

Claims for Patent: 10,512,630


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Summary for Patent: 10,512,630
Title:Compositions and methods for treating cancer
Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.
Inventor(s): Pietras; Richard J. (Sherman Oaks, CA), Jung; Michael E. (Los Angeles, CA), Marquez-Garban; Diana C. (Los Angeles, CA), Deng; Gang (Los Angeles, CA)
Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA (Oakland, CA)
Application Number:15/764,724
Patent Claims:1. A method of treating lung cancer or breast cancer in a patient in need of said treatment, said method comprising administering to the patient a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the formula: ##STR00082## wherein L.sup.1 is a substituted or unsubstituted alkylene; L.sup.2 is a substituted or unsubstituted heteroalkylene, or --O--; R.sup.1 is hydrogen, or substituted or unsubstituted alkyl; and R.sup.2 is hydrogen, or substituted or unsubstituted aryl.

2. The method of claim 1, wherein L.sup.1 is a substituted or unsubstituted C.sub.1-C.sub.4 alkylene; L.sup.2 is a substituted or unsubstituted heteroalkylene, or --O--; R.sup.1 is hydrogen, or substituted or unsubstituted C.sub.1-C.sub.6 alkyl; and R.sup.2 is hydrogen, or substituted or unsubstituted aryl.

3. The method of claim 1, or a pharmaceutically acceptable salt thereof, having the formula: ##STR00083##

4. The method of claim 1, wherein L.sup.1 is unsubstituted methylene.

5. The method of claim 1, wherein L.sup.1 is substituted or unsubstituted propylene.

6. The method of claim 1, wherein L.sup.1 is --C(R.sup.8).sub.2--; R.sup.8 is independently oxo, halogen, --CX.sup.8.sub.3, --CHX.sup.8.sub.2, --CH.sub.2X.sup.8, --OCX.sup.8.sub.3, --OCH.sub.2X.sup.8, --OCHX.sup.8.sub.2, --CN, --OH, --NH.sub.2, --COOH, --CONH.sub.2, --SH, --NHNH.sub.2, --ONH.sub.2, --NHC(O)NHNH.sub.2, --NHC(O)NH.sub.2, --NHC(O)H, --NHC(O)OH, --NHOH, R.sup.9-substituted or unsubstituted alkyl, R.sup.9-substituted or unsubstituted heteroalkyl, R.sup.9-substituted or unsubstituted cycloalkyl, R.sup.9-substituted or unsubstituted heterocycloalkyl, R.sup.9-substituted or unsubstituted aryl, or R.sup.9-substituted or unsubstituted heteroaryl; R.sup.9 is independently oxo, halogen, --CX.sup.9.sub.3, --CHX.sup.9.sub.2, --CH.sub.2X.sup.9, --OCX.sup.9.sub.3, --OCH.sub.2X.sup.9, --OCHX.sup.9.sub.2, --CN, --OH, --NH.sub.2, --COOH, --CONH.sub.2, --SH, --NHNH.sub.2, --ONH.sub.2, --NHC(O)NHNH.sub.2, --NHC(O)NH.sub.2, --NHC(O)H, --NHC(O)OH, --NHOH, R.sup.10-substituted or unsubstituted alkyl, R.sup.10-substituted or unsubstituted heteroalkyl, R.sup.10-substituted or unsubstituted cycloalkyl, R.sup.10-substituted or unsubstituted heterocycloalkyl, R.sup.10-substituted or unsubstituted aryl, or R.sup.10-substituted or unsubstituted heteroaryl; R.sup.10 is independently oxo, halogen, --CX.sup.10.sub.3, --CHX.sup.10.sub.2, --CH.sub.2X.sup.10, --OCX.sup.10.sub.3, --OCH.sub.2X.sup.10, --OCHX.sup.10.sub.2, --CN, --OH, --NH.sub.2, --COOH, --CONH.sub.2, --SH, --NHNH.sub.2, --ONH.sub.2, --NHC(O)NHNH.sub.2, --NHC(O)NH.sub.2, --NHC(O)H, --NHC(O)OH, --NHOH, unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, unsubstituted heterocycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl; and X.sup.8, X.sup.9, and X.sup.10 are independently --F, --Cl, --Br, or --I.

7. The method of claim 1, wherein L.sup.1 is --C(R.sup.8).sub.2--; R.sup.8 is independently oxo, halogen, --CX.sup.8.sub.3, --CHX.sup.8.sub.2, --CH.sub.2X.sup.8, --OCX.sup.8.sub.3, --OCH.sub.2X.sup.8, --OCHX.sup.8.sub.2, --CN, --OH, --NH.sub.2, --COOH, --CONH.sub.2, --SH, --NHNH.sub.2, --ONH.sub.2, --NHC(O)NHNH.sub.2, --NHC(O)NH.sub.2, --NHC(O)H, --NHC(O)OH, --NHOH, unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, unsubstituted heterocycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl; and X.sup.8 is independently --F, --Cl, --Br, or --I.

8. The method of claim 1, wherein the compound is: ##STR00084##

9. The method of claim 1, wherein the compound is: ##STR00085##

10. The method of claim 1, wherein the compound is: ##STR00086##

11. The method of claim 1 wherein the cancer is lung cancer.

12. The method of claim 1 wherein the cancer is non-small cell lung cancer.

13. The method of claim 1 wherein the cancer is breast cancer.

14. The method of claim 1 wherein the cancer is triple negative breast cancer.

15. The method of claim 1 wherein the cancer is resistant to an anti-cancer agent.

16. The method of claim 1, further comprising administering a second agent, wherein the second agent is an anti-cancer agent.

17. The method of claim 16, wherein the second agent is glembatumumab vedotin, capecitabine, nab-paclitaxel, sacituzumab govitecan, vantictumab, atezolizumab, gemcitabine, metformin, iniparib, irinotecan, trastuzumab, trastuzumab emtansine, anastrozole, exemestane, fulvestrant, goserelin, letrozole, leuprolide, megestrol acetate, tamoxifen, toremifene, palbociclib, everolimus, cyclophosphamide, docetaxel, doxorubicin, epirubicin, methotrexate, paclitaxel, 5-fluorouracil, capecitabine, carboplatin, cisplatin, eribulin, ixabepilone, liposomal doxorubicin, vinorelbine, pertuzumab, lapatinib, erlotinib, gefitinib, cetuximab, panitumumab, afatinib, cisplatin, carboplatin, or nedaplatin.

18. A method of decreasing the level of activity of NF-.kappa.B or mTOR in a cell comprising contacting the cell with an effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the formula: ##STR00087## wherein L.sup.1 is a substituted or unsubstituted alkylene; L.sup.2 is a substituted or unsubstituted heteroalkylene, or --O--; R.sup.1 is hydrogen, or substituted or unsubstituted alkyl; and R.sup.2 is hydrogen, or substituted or unsubstituted aryl.

19. A method of increasing the level of activity of TSC1 or TSC2 in a cell comprising contacting the cell with an effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the formula: ##STR00088## wherein L.sup.1 is a substituted or unsubstituted alkylene; L.sup.2 is a substituted or unsubstituted heteroalkylene, or --O--; R.sup.1 is hydrogen, or substituted or unsubstituted alkyl; and R.sup.2 is hydrogen, or substituted or unsubstituted aryl.

Details for Patent 10,512,630

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 2035-09-30
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2035-09-30
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2035-09-30
Eli Lilly And Company ERBITUX cetuximab Injection 125084 03/28/2007 ⤷  Try a Trial 2035-09-30
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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