# US 12,595,232 B2 · DRG-MDM2-1 for use as a novel Mouse Double Minute 2 (MDM2) inhibitor

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- Number: US 12,595,232 B2
- Document ID: US12595232B2
- Status: Granted
- Kind: B2
- Application number: 17/904,403
- Filed: 2021-02-16
- Published: 2023-03-09
- Granted: 2026-04-07
- Earliest claimed: 2020-02-17
- Assignees: Bahcesehir Universitesi; Istanbul Teknik Universitesi
- Applicants: Bahcesehir Universitesi; Istanbul Teknik Universitesi
- Inventors: Timucin Avsar; Serdar Durdagi; Muge Didem Orhan; Maide Nur Paksoy; Gulsah Aydin; Mine Yurtsever
- Web page: https://patentgrep.com/patent/US12595232B2

## CPC

- C07D 209/18: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- A61K 31/404: Indoles, e.g. pindolol
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/02: specific for leukemia
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to compound shown with formula (I) or a pharmaceutically acceptable derivative thereof for use as a novel inhibitor of MDM2 activity.

## Claims

### Claim 1

A pharmaceutical composition comprising an effective amount of a compound of Formula I, or a pharmaceutically acceptable derivative thereof,
and one or more additional pharmaceutically active agents selected from the group consisting of anti-proliferative agents, immunomodulatory agents, antiviral agents, antimicrobial agents, anti-infective agents, anesthetic agents, antiemetics, and combinations thereof,
wherein the pharmaceutically acceptable derivative of Formula I is a hydrate, a solvate, a stereoisomer, a salt, or a tautomer thereof.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the anti-proliferative agents are selected from the group consisting of alkylating agents, anthracyclines, taxanes or cytoskeletal disruptors, epothilones, histone deacetylase inhibitors, inhibitors of topoisomerase I, inhibitors of topoisomerase II, kinase inhibitors, tyrosine kinase inhibitors, nucleotide analogs and nucleotide precursor analogs, peptide antibiotics, platinum-based agents, retinoids, vinca alkaloids, methotrexate, pemetrexed, pralatrexate, raltitrexed, etoposide, teniposide, abiraterone, bicalutamide, cyproterone, degarelix, exemestane, fulvestrant, goserelin, histrelin, leuprolide, mifepristone, triptorelin, lenalidomide, pomalidomide, thalidomide, everolimus, temsirolimus, anagrelide, ceritinib, dabrafenib, idelalisib, ibrutinib, palbociclib, vemurafenib, bleomycin, dactinomycin, eribulin, estramustine, ixabepilone, mitomycin, procarbazine, alectinib, fluoxymesterone, iobenguane, imiquimod, interferon, ixazomib, lanreotide, lentinan, octreotide, omacetaxine, tegafur, gimeracil, oteracil, uracil, combretastatin, and derivatives thereof.