Claims for Patent: 10,071,953

Summary for Patent: 10,071,953

Title:	Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof
Abstract:	The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.
Inventor(s):	Penning; Trevor M. (Springfield, PA), Adeniji; Adegoke O. (Drexel Hill, PA), Byrns; Michael C. (Philadelphia, PA), Winkler; Jeffrey (Wynnewood, PA), Twenter; Barry (Philadelphia, PA)
Assignee:	The Trustees of the University of Pennsylvania (Philadelphia, PA)
Application Number:	14/993,742
Patent Claims:	1. A compound of Formula (II) or a salt thereof: ##STR00052## wherein: R.sup.3 is nitro; and, each occurrence of R.sup.4 and R.sup.5 is independently selected from the group consisting of H, C.sub.1-C.sub.6 alkyl, haloalkyl, halogen, --CN, C.sub.1-C.sub.6 alkoxy, --C(.dbd.O)H, --C(.dbd.O)OH, --C(.dbd.O)--(C.sub.1-C.sub.6 alkyl), and SO.sub.3H. 2. The compound of claim 1, wherein each occurrence of R.sup.4 is independently selected from the group consisting of H, methyl, tert-butyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and acetyl. 3. The compound of claim 1, wherein each occurrence of R.sup.5 is independently selected from the group consisting of H, methyl, tert-butyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and acetyl. 4. A pharmaceutical composition comprising at least one compound of claim 1 and a pharmaceutically acceptable carrier. 5. The pharmaceutical composition of claim 4, further comprising at least one therapeutic agent selected from the group consisting of indomethacin, desatinib, selegiline, seliciclib, TOK-001, SAHA, docetaxel, bevacizumab, taxotere, thalidomide, prednisone, Sipuleucel-T, cabazitaxel, MDV3100, ARN-509, abiraterone, temozolomide, tamoxifen, anastrozole, letrozole, vorozole, exemestane, fadrozole, formestane, raloxifene, any mixtures thereof, and any salts thereof. 6. The compound 3-((4-nitronaphthalen-1-yl)amino)benzoic acid, or a salt thereof: ##STR00053## 7. A pharmaceutical composition comprising the compound of claim 6 and a pharmaceutically acceptable carrier. 8. The pharmaceutical composition of claim 7, further comprising at least one therapeutic agent selected from the group consisting of indomethacin, desatinib, selegiline, seliciclib, TOK-001, SAHA, docetaxel, bevacizumab, taxotere, thalidomide, prednisone, Sipuleucel-T, cabazitaxel, MDV3100, ARN-509, abiraterone, temozolomide, tamoxifen, anastrozole, letrozole, vorozole, exemestane, fadrozole, formestane, raloxifene, any mixtures thereof, and any salts thereof.

Details for Patent 10,071,953

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	February 26, 2004		2036-01-12
Dendreon Pharmaceuticals Llc	PROVENGE	sipuleucel-t	Injection	125197	April 29, 2010		2036-01-12