Claims for Patent: 10,077,280

Summary for Patent: 10,077,280

Title:	Mixed ligand gold(I) complexes as anti-cancer agents
Abstract:	Gold(I) complex with mixed ligands as an anticancer agent. The gold(I) ion is coordinated to a dithiocarbamate ligand and a phosphorus-containing ligand (e.g. phosphines). Also described are a pharmaceutical composition incorporating the gold(I) complex, a methods of synthesizing the gold(I) complex, and a method for treating cancer.
Inventor(s):	Al-Jaroudi; Said S. (Dhahran, SA), Alhoshani; Ali (Riyadh, SA), Altaf; Muhammad (Dhahran, SA), Isab; Anvarhusein Abdulkadir (Dhahran, SA)
Assignee:	King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA)
Application Number:	15/351,585
Patent Claims:	1. A gold(I) complex represented by formula (I): ##STR00006## a salt thereof, a solvate thereof, or a combination thereof; wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, an unsubstituted alkyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkylalkyl, an optionally substituted arylalkyl, an optionally substituted heteroaryl, an optionally substituted aryl, an optionally substituted heterocyclyl, an optionally substituted arylolefin, an optionally substituted C.sub.4-C.sub.10 alkenyl, and an optionally substituted vinyl; R.sub.3, R.sub.4, and R.sub.5 are independently selected from the group consisting of H, an optionally substituted C.sub.1-C.sub.3 alkyl, an optionally substituted C.sub.3-C.sub.5 cycloalkyl, an optionally substituted cycloalkylalkyl, an optionally substituted arylalkyl, an optionally substituted heteroaryl, an optionally substituted aryl, an optionally substituted heterocyclyl, an optionally substituted arylolefin, an optionally substituted vinyl, an optionally substituted alkylamino, an optionally substituted arylamino, an optionally substituted alkylarylamino, an optionally substituted alkoxy, and an optionally substituted aryloxy; and with the proviso that R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are not each an ethyl. 2. The gold(I) complex of claim 1, wherein R.sub.1 and R.sub.2 are the same unsubstituted alkyl group, and R.sub.3, R.sub.4, and R.sub.5 are the same optionally substituted C.sub.1-C.sub.3 alkyl group. 3. The gold(I) complex of claim 2, wherein R.sub.1 and R.sub.2 are methyls, and R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of methyl, ethyl, and isopropyl. 4. The gold(I) complex of claim 2, wherein R.sub.1 and R.sub.2 are ethyls, and R.sub.3, R.sub.4, and R.sub.5 are methyls. 5. The gold(I) complex of claim 1, wherein R.sub.1 and R.sub.2 are independently an unsubstituted alkyl selected from the group consisting of isopropyl, sec-butyl, isobutyl, and tert-butyl. 6. A composition comprising: the gold(I) complex of claim 1; and a pharmaceutically acceptable carrier or excipient. 7. The composition of claim 6, which comprises 0.01-50 .mu.M of the gold(I) complex relative to the total composition. 8. The composition of claim 6, further comprising at least one chemotherapeutic agent selected from the group consisting of aflibercept, asparaginase, bleomycin, busulfan, carmustine, chlorambucil, cladribine, cyclophosphamide, cytarabine, dacarbazine, daunorubicin, doxorubicin, etoposide, fludarabine, gemcitabine, hydroxyurea, idarubicin, ifosfamide, irinotecan, lomustine, mechlorethamine, melphalan, mercaptopurine, methotrexate, mitomycin, mitoxantrone, pentostatin, procarbazine, topotecan, vinblastine, vincristine, retinoic acid, oxaliplatin, carboplatin, 5-fluorouracil, teniposide, amasacrine, docetaxel, paclitaxel, vinorelbine, bortezomib, clofarabine, capecitabine, actinomycin D, epirubicin, vindesine, methotrexate, 6-thioguanine, tipifarnib, imatinib, erlotinib, sorafenib, sunitinib, dasatinib, nilotinib, lapatinib, gefitinib, temsirolimus, everolimus, rapamycin, bosutinib, pzopanib, axitinib, neratinib, vatalanib, pazopanib, midostaurin, enzastaurin, trastuzumab, cetuximab, panitumumab, rituximab, bevacizumab, mapatumumab, conatumumab, and lexatumumab. 9. The gold(I) complex of claim 1, wherein R.sub.3, R.sub.4, and R.sub.5 are independently selected from the group consisting of H, an optionally substituted C.sub.1-C.sub.2 alkyl, an optionally substituted C.sub.3-C.sub.5 cycloalkyl, an optionally substituted cycloalkylalkyl, an optionally substituted arylalkyl, an optionally substituted heteroaryl, an optionally substituted aryl, an optionally substituted heterocyclyl, an optionally substituted arylolefin, an optionally substituted vinyl, an optionally substituted alkylamino, an optionally substituted arylamino, an optionally substituted alkylarylamino, an optionally substituted alkoxy, and an optionally substituted aryloxy. 10. The gold(I) complex of claim 1, wherein R.sub.3, R.sub.4, and R.sub.5 are an optionally substituted C.sub.1-C.sub.2 alkyl group. 11. The gold(I) complex of claim 1, wherein R.sub.1 and R.sub.2 are the same alkyl group selected from the group consisting of a methyl group and an ethyl group, and R.sub.3, R.sub.4, and R.sub.5 are the same alkyl group selected from the group consisting of a methyl group and an ethyl group. 12. The gold(I) complex of claim 1, wherein R.sub.1 and R.sub.2 are methyls and R.sub.3, R.sub.4, and R.sub.5 are ethyls. 13. The gold(I) complex of claim 1, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each a methyl group.

Details for Patent 10,077,280

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	01/10/1978		2036-04-22
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2036-04-22
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2036-04-22