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Last Updated: September 24, 2020

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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 Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX search
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 001 1997-11-26   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX search
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 002 1997-11-26   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX search
Genentech HERCEPTIN trastuzumab VIAL; INTRAVENOUS 103792 001 1998-09-25   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX Orphan search
Imclone ERBITUX cetuximab VIAL; INTRAVENOUS 125084 001 2004-06-18   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX Orphan search
Genentech AVASTIN bevacizumab VIAL; INTRAVENOUS 125085 001 2004-02-26   Start Trial King Fahd University of Petroleum and Minerals (Dhahran, SA) King Saud University (Riyadh, SA) 2036-04-22 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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