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Novel anti-PD-L1 compound and applications thereof, and composition containing novel anti-PD-L1 compound

A compound and hydrate technology, applied in the field of biomedicine, can solve problems such as low bioavailability and poor therapeutic activity of solid tumors

Pending Publication Date: 2019-05-07
GUANGZHOU WELLHEALTH BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Technical Problems to be Solved by the Invention The existing PD-1 / PD-L1 monoclonal antibody drug needs intravenous injection, and has disadvantages such as poor therapeutic activity and low bioavailability for solid tumors. Therefore, the present invention provides a novel Anti-PD-L1 compound, its application and composition containing it, the compound is a small molecule PD-L1 inhibitor, which has the advantages of high activity, high bioavailability, stable drug, and oral administration, and the compound can be Cause and enhance the body's own immune response

Method used

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  • Novel anti-PD-L1 compound and applications thereof, and composition containing novel anti-PD-L1 compound
  • Novel anti-PD-L1 compound and applications thereof, and composition containing novel anti-PD-L1 compound
  • Novel anti-PD-L1 compound and applications thereof, and composition containing novel anti-PD-L1 compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0136] Example 1 Preparation of Compound I-1

[0137]

[0138] Compound I-1a (43 mg, 0.1 mmol), S-piperidine-2-carboxylic acid (13.6 mg, 0.105 mmol), and sodium triacetoxyborohydride (21.2 mg, 0.25 mmol) were added to 10 mL of dichloromethane solution The crude product was purified by preparative LC / MS with stirring at 80-85°C for 1 hour, and its purity was estimated to be 98% by LCMS analysis.

Embodiment 2

[0139] Example 2 Preparation of Compound I-14

[0140]

[0141] Compound I-14a (39 mg, 0.1 mmol), piperidine-2-carboxylic acid (13.6 mg, 0.105 mmol), and sodium triacetoxyborohydride (21.2 mg, 0.25 mmol) were added to 10 mL of dichloromethane solution, After stirring at 80-85°C for 45 minutes, the crude product was purified by preparative LC / MS and evaluated to be 97% pure by LCMS analysis.

Embodiment 3

[0142] Example 3 Preparation of compound I-20

[0143]

[0144] Compound I-20a (35 mg, 0.1 mmol), piperidine-2-carboxylic acid (13.6 mg, 0.105 mmol), and sodium triacetoxyborohydride (21.2 mg, 0.25 mmol) were added to 10 mL of dichloromethane solution, After stirring at 80-85°C for 50 minutes, the crude product was purified by preparative LC / MS and evaluated to be 98% pure by LCMS analysis.

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PUM

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Abstract

The present invention discloses a novel anti-PD-L1 compound and applications thereof, and a composition containing the novel anti-PD-L1 compound, and provides a substituted biaryl compound representedby a formula I, a pharmaceutically acceptable salt, a hydrate, a solvate, a metabolite, a stereoisomer, a tautomer or a prodrug thereof. The formula I is defined in the specification.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a novel anti-PD-L1 compound, its application and a composition containing the same. Background technique [0002] PD-1 / PD-L1 signaling pathway is one of the hottest topics in the field of cancer treatment and research. New immunotherapy drugs approved for marketing in the past two years, such as Merck's Keytruda and Bristol-Myers Squibb's Opdivo, both target this signaling pathway, using monoclonal antibodies to bind to PD-1 receptors to block signal transmission, thereby activating the body's own immune system The system attacks the tumor. The two new drugs are already approved to treat cancers such as melanoma, and have shown great potential in clinical trials for a number of other cancers. At present, the US FDA has approved 3 macromolecular PD-L1 inhibitors to market, namely Atezolizumab (Tecentriq, the treatment of bladder cancer and non-small cell lung cancer, is the first PD-L1 ...

Claims

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Application Information

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IPC IPC(8): C07D211/60C07D213/69C07D295/13C07C217/58C07D205/08C07D405/12C07D319/18C07D401/12C07D417/12C07D405/14C07D487/04C07D471/04A61K31/4458A61K31/4402A61K31/44A61K31/5375A61K31/137A61K31/397A61K31/443A61K31/4433A61K31/36A61K31/4439A61K31/4427A61K31/497A61K31/501A61K31/5025A61K31/519A61K31/437A61K31/4375A61P35/00
Inventor 许勇黄璐林当胡海
Owner GUANGZHOU WELLHEALTH BIO PHARMA CO LTD
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