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Diazepinone derivatives as capsid assembly modulators

A compound, heteroaryl technology, applied in the field of novel diazepine compounds, can solve problems such as difficult selection of resistance selection

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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it may be difficult to select for resistance to HBV core / capsid protein-binding compounds without major effects on viral replication fitness

Method used

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  • Diazepinone derivatives as capsid assembly modulators
  • Diazepinone derivatives as capsid assembly modulators
  • Diazepinone derivatives as capsid assembly modulators

Examples

Experimental program
Comparison scheme
Effect test

no. 1 example

[0169] By the first example of the substituent, if the substituent S 1 实例 Be s 1 S 2 One of them, and substituent S 2 实例 Be s 3 S 4 One of them, these assignments refer to embodiments of the disclosure given in accordance with the following: s 1 实例 Be s 1 And s 2 实例 Be s 3 S 1 实例 Be s 1 And s 2 实例 Be s 4 S 1 实例 Be s 2 And s 2 实例 Be s 3 S 1 实例 Be s 2 And s 2 实例 Be s 4 And the equivalents of each of this type of selection. For the sake of simplicity, this paper uses shorter terms accordingly "S 1 实例 Be s 1 S 2 One of them, and s 2 实例 Be s 3 S 4 One ", but not by way of limitation. In general terms, according to the above example on substituent terminology Zi are intended to illustrate various substituent groups herein according to the assignment. Forth herein for the above specification extends to substituents such as R when applicable 1 R 2 R 3 R 4 , PG and X, and any other generic substituent used herein is a member of group symbols.

[0170] Further, when more than on...

example

[0195] An exemplary compound which can be used in the present disclosure is now described with reference to the illustrative synthesis schemes used in the general preparations thereof and subsequent specific examples. The skilled person will recognize that in order to obtain a variety of compounds herein, the starting material can be appropriately selected such that the final desired substituent will be carried in or without suitable protection by a reaction scheme to produce a desired product. Alternatively, it may be necessary or desirable to use a suitable group instead of the final desired substituent, the suitable group can be carried by the reaction scheme and is replaced by the desired substituent. Unless otherwise stated, the variables are as defined above with reference formula (I) above. The reaction can be carried out between the melting point of the solvent and the reflux temperature, preferably between the reflux temperature of 0 ° C and the solvent. Conventional heat...

example 1

[0345] Example 1: N- (3-cyano-4-fluorophenyl) -10-methyl-11-oxo-8- (1H-1, 2, 4-triazole-3-yl) -3, 4 , 8,9,10,11-hexapyridine - pyridine and [4 ', 3': 3, 4] pyrazole [1,5-A] [1,4] Diazazhi-2 (7h) - formamide.

[0346]

[0347] Step A.10-methyl-8- (1H-1, 2, 4-triazole-3-yl) -3, 4, 7, 8, 9, 10-hexahydro-1H-pyridine [4 ', 3 ': 3,4] Pyrazole [1,5-A] [1,4] Diazazepo - 11 (2H) - ketone.

[0348] The 10-methyl-11-oxo -8- (1H-1,2,4- triazol-3-yl) -1,3,4,7,8,9- hexahydro-pyrido [2,3- ] pyrazolo [2,4-b] [1,4] diazepine-2-carboxylate (intermediate 2,40.00mg, 103.24μmol) solution was added TFA (3.00 mL) in DCM, (770.00mg, 6.75mmol, 500.00μL). The reaction mixture was stirred for 30min at 15 ℃. The mixture was concentrated under reduced pressure to afford the title compound as a yellow oil (40.00 mg, crude, TFA salt), which was used directly without purification in the next step.

[0349] Step B.N- (3-cyano-4-fluorophenyl) -10-methyl-11-oxo-8- (1H-1, 2, 4-triazole-3-yl) -3, 4, 8,9,10,11-...

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PUM

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Abstract

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the HBV CAM. Such compounds are represented by Formula (I) as follows, wherein R1, R2, R3, X, and R4, are defined herein.

Description

Technical field [0001] The present disclosure relates to novel diazepin ketone compounds, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds, and their use in treating an animal (particularly a human) associated with the use of HBV infection diseases. Background technique [0002] Chronic hepatitis B virus (HBV) infection is a major global health problem, affecting more than 5% of the world's population (over 350 million people worldwide, the United States has 125 million people). [0003] Despite prophylactic HBV vaccines are available, but the burden of chronic HBV infection remains a major global unmet medical problems, because the treatment of choice for most areas of developing countries is not ideal, but sustained rate of new infections . Current treatments do not cure, and only two agents (nucleoside analogs and interferon-α / viral polymerase inhibitor); resistance, low efficacy and tolerability problem limiting their ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14A61K31/551A61P31/12
CPCC07D471/14A61K31/551A61P31/20A61K2300/00
Inventor S·D·库杜克
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