Heterocyclic compound

A technology of compounds and heterocycles, applied in the direction of active ingredients of heterocycles, organic chemistry, drug combination, etc., can solve problems such as shortage of platelet preparations

Pending Publication Date: 2021-04-13
OTSUKA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, as long as platelet preparations are provided exclusively through blood donations, it can be expected that a decrease in the number of blood donors will lead to a shortage of platelet preparations in the near future

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0081] (1) In formula [I], ring A is benzene or pyridine, and the hydrogen on the ring of benzene or pyridine is optionally substituted by fluorine, methyl or -CN;

[0082] (2) In formula [I], ring B is represented by the following formula:

[0083] [chemical formula 3]

[0084]

[0085] where R 7 is halogen, C optionally substituted by halogen 1-6 Alkyl, -CN, -OR 5 、-SR 5 、-COOR 5 、-C 1-6 Alkylene-CONR 5 R 6 、-C 1-6 Alkylene-OCOR 5 ,-CONR 5 R 6 , -NR 5 COOR 6 、-SO 2 R 5 or -NR 5 R 6 (R 5 and R 6 the same or different and each independently represents hydrogen or C optionally substituted by halogen 1-6 alkyl),

[0086] m is 0, 1 or 2, when m is 2, each R 7 are independently the same or different substituents,

[0087] For example, (R 7 )m represents fluorine, two fluorine, chlorine, methyl, ethyl, trifluoromethyl, hydroxyl, methoxy, -CN, -CON(CH 3 ) 2 、-CH 2 CON(CH 3 ) 2 , methylsulfonyl, or fluorine and -CN are each substituted;

[0088] (3) In ...

Embodiment

[0226] The present invention is explained in detail below by referring to Test Examples, Reference Examples and Examples, which are not construed as limiting, and the present invention can be changed within the scope of the present invention.

[0227] In this specification, the following abbreviations may be used.

[0228]

[0229]

[0230]

[0231] In the following examples, "room temperature" generally refers to about 10°C to about 35°C. The ratios indicated for mixed solvents are volume mixing ratios unless otherwise stated. % are by weight unless otherwise stated.

[0232] 1 HNMR (proton nuclear magnetic resonance spectrum) was measured by Fourier-transform NMR (Bruker AVANCE III 400 (400 MHz) or Bruker AVANCE III HD (500 MHz)).

[0233] Mass spectra (MS) were determined by LC / MS (ACQUITY UPLC H-Class). As the ionization method, the ESI method is used. The data represent actually measured values ​​(actually measured values). Typically, molecular ion peaks ar...

reference example 1

[0238] Synthesis of 2-amino-6-chloro-9-(1-hydroxy-2-methylpropan-2-yl)-7H-purin-8-one

[0239] A solution of 2,5-diamino-4,6-dichloropyrimidine (10.0 g) and 2-amino-2-methyl-1-propanol (11.7 ml) in NMP (10 ml) was stirred overnight at 140°C. The reaction mixture was purified by column chromatography (Hexane / AcOEt / MeOH). To a solution of the product in THF (150ml) was added CDI (19.9g) at 0°C, and the mixture was stirred for 1 hr. To the mixture were added 50% aqueous MeOH (300 ml) and 5N aqueous NaOH (44.7 ml), and the mixture was stirred for 1 hr. The reaction mixture was concentrated, 5N aqueous HCl solution was added to the residue, and the solid precipitate was collected by filtration to obtain the title compound (10.9 g).

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Abstract

Provided is a novel heterocyclic compound having an aryl hydrocarbon receptor antagonist activity and useful for the promotion of platelet production, the compound being represented by the general formula [I]: wherein ring A, ring B, R1, R2, R3, R4, n, and X are as defined above, or a salt thereof.

Description

technical field [0001] The present invention relates to a heterocyclic compound. More specifically, the present invention relates to a compound having aryl hydrocarbon receptor (AhR) antagonist activity and promoting platelet production in vitro by platelet progenitor cells such as megakaryocytes. Background technique [0002] Platelet preparations may be given to patients who experience heavy bleeding during surgery or injury, or who are prone to bleeding due to decreased platelets after treatment with anticancer drugs, to treat bleeding symptoms and prevent unexpected bleeding. [0003] Currently, platelet preparations rely on blood donations and have a shelf life of about 4 days, which is very short. Furthermore, as long as platelet preparations are provided only by blood donation, it can be expected that a decrease in the number of blood donors will lead to a shortage of platelet preparations in the near future. [0004] In order to meet these needs, methods of produci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/14C07D513/14A61P7/04A61K31/519
CPCC07D498/14C07D513/14A61P7/04C07D473/32A61K31/519A61K31/52A61K31/554C07D519/00
Inventor 大达一弘藤森悠介牧田直也古关教孝林秀树坂元裕树峰野胡桃多贺亮介
Owner OTSUKA PHARM CO LTD
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