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Combination treatment of acute myeloid leukemia

A technology of composition and activity, applied in the direction of drug combination, organic active ingredients, active ingredients of heterocyclic compounds, etc., can solve the problems of limited toxicity and high activity

Pending Publication Date: 2020-09-04
BOEHRINGER INGELHEIM INT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem underlying the present invention is the development of combination therapy and improved dosing regimens for combination therapy of voracetib and BET inhibitors in AML with maximal activity and limited toxicity

Method used

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  • Combination treatment of acute myeloid leukemia
  • Combination treatment of acute myeloid leukemia
  • Combination treatment of acute myeloid leukemia

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preparation example Construction

[0095] According to the preparative high-pressure chromatography (HPLC) of the embodiment compound of the present invention, the chromatographic column (name: Sunfire C18 OBD, 10 μm, 30x100mm, part number 186003971; X-Bridge C18 OBD, 10 μm, 30x100mm, part number 186003930) manufactured by Waters was used conduct. use different H 2 Compounds were eluted with an O / ACN gradient with 0.2% HCOOH added to water (acidic conditions). When performing chromatographic analysis under alkaline conditions, the water should be adjusted to alkaline according to the following formula: 5mL ammonium bicarbonate solution (158g in 1L H 2 O) and 2 mL of 32% ammonia (aqueous) in H 2 O to make up to 1L.

[0096] Analytical HPLC (reaction monitoring) of the intermediate compound was performed with columns manufactured by Waters and Phenomenex. In each case, the analytical equipment is also equipped with a mass detector.

[0097] HPLC mass spectrometry / UV spectrometry

[0098] Use the HPLC-MS dev...

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Abstract

The present invention relates to the use of volasertib, or a pharmaceutically acceptable salt thereof or a hydrate thereof, in combination with a BET inhibitor, or a pharmaceutically acceptable salt thereof or a hydrate thereof for treating patients suffering from acute myeloid leukemia (AML).

Description

[0001] This paper relates to the combination of volasertib or its pharmaceutically acceptable salt or its hydrate and BET inhibitor or its pharmaceutically acceptable salt or its hydrate for the treatment of suffering from acute myelogenous leukemia (AML) patient use. Background technique [0002] Acute myeloid leukemia (AML), also known as acute myelogenous leukemia, is a cancer of the myeloid lineage of blood cells characterized by the rapid growth of abnormal white blood cells that accumulate in the bone marrow and interfere with normal Production of blood cells. As an acute leukemia, AML progresses rapidly and is typically fatal within weeks or months if left untreated. AML is the most prevalent form of leukemia in adults, especially the elderly, and is slightly more common in men than women. There are an estimated 30,000 cases in the US and 47,000 in Europe. [0003] The incidence of AML increases with age, with a median age at diagnosis of 67 years. The CAGR of AML i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/437A61K31/4412A61K31/4985A61K31/519A61K31/55A61K31/5517A61P35/02
CPCA61K31/437A61K31/4412A61K31/4985A61K31/519A61K31/55A61K31/5517A61P35/02A61K2300/00A61K31/4188A61K31/501A61K31/5377A61K31/551
Inventor U·汤奇-格伦特A·鲍姆D·I·鲁道夫
Owner BOEHRINGER INGELHEIM INT GMBH
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