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Last Updated: April 23, 2024

Claims for Patent: 10,144,749


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Summary for Patent: 10,144,749
Title:Gold complexes of alkylated phosphines
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:15/993,163
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 alkyl groups independently selected from the group consisting of methyl, ethyl, and isopropyl; R.sub.3, R.sub.4, and R.sub.5 are independently selected from the group consisting of an optionally substituted C.sub.1-C.sub.3 alkyl, an optionally substituted arylalkyl, an optionally substituted aryl, an optionally substituted vinyl, 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 ethyls, and R.sub.3, R.sub.4, and R.sub.5 are methyls.

4. A composition comprising: the gold(I) complex of claim 1; and a pharmaceutically acceptable carrier or excipient.

5. The composition of claim 4, which comprises 0.01-50 .mu.M of the gold(I) complex relative to the total composition.

6. The composition of claim 4, 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.

7. The gold(I) complex of claim 1, wherein R.sub.3, R.sub.4, and R.sub.5 are an C.sub.1-C.sub.2 alkyl group.

8. 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.

9. 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.

Details for Patent 10,144,749

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Recordati Rare Diseases, Inc. ELSPAR asparaginase For Injection 101063 01/10/1978 ⤷  Try a Trial 2036-04-22
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2036-04-22
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2036-04-22
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2036-04-22
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2036-04-22
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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