Auristatin analogues and their conjugates with cell-binding molecules

A technique of combining auristatin and molecules, which is applied in the field of derivatives of methyl auristatin F, which can solve the problems of reduced activity and unfavorable transport across cell membranes
CN107921144APending Publication Date: 2018-04-17HANGZHOU DAC BIOTECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HANGZHOU DAC BIOTECH
Publication Date
2018-04-17

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Abstract

This invention relates to analogues of auristatins, in particular monomethyl auristatin F (MMAF), as cytotoxic agents, conjugates of such cytotoxic agents with a cell-binding agent, the preparation and the therapeutic uses of these cytotoxic agents and conjugates thereof to arrest or retard abnormal cell growth and / or proliferation.
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Description

technical field

[0001] The present invention describes a class of auristatin cytotoxic small molecules, in particular derivatives of methylauristatin F (MMAF), their conjugation to cell-binding molecules and their use to block cell growth and proliferation Methods. technical background

[0002] Chemotherapy is one of the main means of traditional cancer treatment. Treatment of tumors with chemotherapy drugs is based on the drug's ability to distinguish cancer cells from normal cells and preferentially kill cancer cells. Lack of selectivity and systemic toxicity to humans are the main drawbacks of chemotherapeutic agents.

[0003] In order to improve the anti-cancer efficacy of drugs, the activity of drugs can be improved to achieve therapeutic effects without adverse reactions at lower doses, or the selectivity of drugs to tumors can be improved, and higher doses can be used to ensure more effective treatment. good therapeutic effect.

[0004] Predecessors have done a lo...

Claims

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