1032568-63-0

Usage

Uses

Used in Oncology:
BAY 80-6946 (Copanlisib) is used as an anticancer agent for the treatment of various malignancies. It targets the PI3K enzyme, which is frequently overactive in cancer cells, leading to uncontrolled cell growth and proliferation. By inhibiting this enzyme, Copanlisib aims to slow down or stop tumor growth, making it a promising therapeutic option for patients with certain types of cancer.
Used in Drug Development:
In the pharmaceutical industry, BAY 80-6946 (Copanlisib) serves as a key compound in the development of novel cancer treatments. Its potent and selective inhibition of the PI3K enzyme makes it a valuable asset in the search for more effective and targeted therapies for cancer patients. Researchers and drug developers utilize Copanlisib to study its potential synergistic effects with other cancer-fighting agents and to explore its role in combination therapies.
Used in Clinical Trials:
BAY 80-6946 (Copanlisib) is also used in clinical trials to evaluate its safety, efficacy, and optimal dosing regimens for various types of cancer. These trials are essential in determining the potential benefits and risks associated with the use of Copanlisib as a cancer treatment, ultimately guiding its approval and integration into standard cancer care practices.

Upstream product

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Relevant academic research and scientific papers

A preparation method of the storehouse pan nixi

The invention discloses a preparation method of copanlisib (BAY80-6946). The target compound copanlisib is prepared by a known raw material 2-amino-3-methoxyl-4-(3-morpholine-4-propoxy) cyanophenyl by virtue of reactions such as heterocyclization, amidation, substitution-cyclization and the like. The preparation method is novel in route design, easy for obtaining the raw material, simple in process, economical, environment-friendly and suitable for industrialized production.

SYNTHESIS OF COPANLISIB AND ITS DIHYDROCHLORIDE SALT

The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.

SYNTHESIS OF COPANLISIB AND ITS DIHYDROCHLORIDE SALT

The present invention relates to a novel method of preparing copanlisib, and copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib.

Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946)

The phosphoinositide 3-kinase (PI3K) pathway is aberrantly activated in many disease states, including tumor cells, either by growth factor receptor tyrosine kinases or by the genetic mutation and amplification of key pathway components. A variety of PI3K isoforms play differential roles in cancers. As such, the development of PI3K inhibitors from novel compound classes should lead to differential pharmacological and pharmacokinetic profiles and allow exploration in various indications, combinations, and dosing regimens. A screening effort aimed at the identification of PI3Kγ inhibitors for the treatment of inflammatory diseases led to the discovery of the novel 2,3-dihydroimidazo[1,2-c]quinazoline class of PI3K inhibitors. A subsequent lead optimization program targeting cancer therapy focused on inhibition of PI3Kα and PI3Kβ. Herein, initial structure–activity relationship findings for this class and the optimization that led to the identification of copanlisib (BAY 80-6946) as a clinical candidate for the treatment of solid and hematological tumors are described.

Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines

The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma

The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS

This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.