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Amino acid derivative, preparation method and application thereof

An alkyl and phenyl technology, applied in the field of new amino acid derivatives, which can solve the problems that clinical data have not been fully published, and there is no clinical phase III candidate compound.

Pending Publication Date: 2022-01-18
西安禾渼生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] To sum up, from the perspective of drug development trends, in terms of small molecule compounds, at least several groups of compounds are undergoing druggability research, but clinical data based on drug efficacy have not yet been fully published, and no candidate compounds are in Phase III clinical trials.

Method used

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  • Amino acid derivative, preparation method and application thereof
  • Amino acid derivative, preparation method and application thereof
  • Amino acid derivative, preparation method and application thereof

Examples

Experimental program
Comparison scheme
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Embodiment approach

[0071] selected from

[0072] where tilde Indicates the point of attachment of the group to the rest of the molecule.

[0073] R 19 Can be H or CH 3 ;

[0074] R 20 Can be -CO 2 R 21 ;

[0075] R 21 for C 1 to C 6 straight-chain alkanes.

[0076] According to some embodiments of the invention, the compounds of the invention have the structure of formula II:

[0077]

[0078] Among them, R 1 , R 2 , R 3 , R 6 , R 7 , R 8 , m and n are as defined above.

[0079] B is any one of the following structures,

[0080] R 22 each independently selected from -COOH, -COOCH 3 、-COOCH 2 CH 3 、-COOC(CH 3 ) 3 、-COOCH 2 OCOOCH 2 CH 3 、-COOCH 2 OCOOCH (CH 3 ) 2 、-COOCH(CH 3 )OCOOCH 2 CH 3 、-COOCH(CH 3 )OCOOCH(CH 3 ) 2 , -CONHSO 2 CH 3 , -CH 2 COOH, -OCH 3 , -OCHF 2 , -Cl, -F, -NHCOOCH 3 and-SO 2 NHCOCH 3 ,

[0081] where tilde Indicates the point of attachment of the group to the rest of the molecule.

[0082] On the basis of ...

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Abstract

The invention discloses an amino acid derivative capable of being used for inhibiting blood coagulation factor XIa and application of the amino acid derivative. The invention provides a compound as shown in a formula I or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a polymorphic substance, a solvate, N-oxide, metabolite or a prodrug thereof. According to the invention, a plurality of in-vitro biological test results show that an obvious inhibitory activity effect can be generated on a blood coagulation factor (Factor XIa) at an extremely low concentration, some of the preferred compounds can significantly prolong the human whole blood coagulation time under the condition of low concentration, whether the coagulation time is 1.5 times or 2.0 times, and the compound achieves a practical standardand has an optimistic patent medicine prospect; and the compound can be used as an inhibitor of a blood coagulation factor XIa, and a pharmaceutical composition containing the compound, a preparation method of the compound and application of the compound in preparation of drugs for preventing or treating thrombus and vascular embolism related diseases are provided.

Description

technical field [0001] The present invention relates to a new class of amino acid derivatives, which can be used as inhibitors of blood coagulation factor XIa, pharmaceutical compositions containing them, their preparation methods and their use in the preparation of drugs for preventing or treating diseases related to thrombosis and vascular embolism . Background technique [0002] Thrombus is a pathological product, which is a solid mass formed by coagulation of blood or coagulation of certain formed components in the heart and blood vessels. After the thrombus forms, some or all of it falls off, and with the blood flow, it blocks the blood vessel and becomes an embolism. Thrombosis or thromboembolism can cause a series of cardiovascular and cerebrovascular diseases and has become a major cause of morbidity and mortality worldwide. More than 26 million people die from various thrombotic diseases every year in the world, and the incidence rate in our country is also increa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D257/04C07D401/12C07D403/12C07D235/24A61K31/41A61K31/496A61K31/454A61K31/5377A61K31/4184A61K31/541A61P7/02
CPCC07D257/04C07D401/12C07D403/12C07D235/24A61P7/02C07B2200/07Y02P20/55
Inventor 王雪菊戴静芳吴少平张俊清
Owner 西安禾渼生物医药有限公司
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