# US 11,993,611 B2 · Indolocarbazole analogs of staurosporine and methods of synthesis thereof

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- Number: US 11,993,611 B2
- Document ID: US11993611B2
- Status: Granted
- Kind: B2
- Application number: 17/363,370
- Filed: 2021-06-30
- Published: 2022-01-06
- Granted: 2024-05-28
- Earliest claimed: 2020-07-02
- Assignees: Baylor University
- Applicants: Baylor University
- Inventors: John L. Wood; Ke Kong; Kevin Gayler
- Web page: https://patentgrep.com/patent/US11993611B2

## CPC

- C07D 498/22: in which the condensed system contains four or more hetero rings
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 35/00: Antineoplastic agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Equipotent indolocarbazole-derived analogs of staurosporine identified herein are prepared through C—H borylation chemistry. Functionality resides at C2 and C10 of the indolocarbazole aromatic region. Introducing functionality in this previously inaccessible region does not abrogate kinase activity and is shown to change the selectivity profile.

## Claims

### Claim 1

A compound having a structure of:
wherein R1, R2, and R3 are each independently H or a substituent comprising boron, and wherein at least one of R2 and R3 is a substituent comprising boron.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the substituent comprising boron is pinacolato borane.