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Tricycle heterocyclic compounds and JAK inhibitors

A compound and solvate technology, applied in the field of novel tricyclic pyrimidine compounds and tricyclic pyridine compounds, can solve problems such as limited expression

Inactive Publication Date: 2015-10-28
NISSAN CHEM IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although this family of kinases is ubiquitously expressed in tissues other than JAK3, JAK3 expression is restricted to immune cells

Method used

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  • Tricycle heterocyclic compounds and JAK inhibitors
  • Tricycle heterocyclic compounds and JAK inhibitors
  • Tricycle heterocyclic compounds and JAK inhibitors

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[3447] Granule formulations were prepared comprising the following ingredients.

[3448] Element

[3449]

[3450] The compound represented by formula (I) and lactose were sieved through a 60-mesh sieve. Cornstarch was sieved through a 120 mesh sieve. They are mixed in a V-blender. The powder mixture is kneaded with an aqueous solution of low viscosity hydroxypropylcellulose (HPC-L), granulated (extrusion granulation, die size 0.5-1 mm) and dried. The resulting dried granules were sieved through a shaker sieve (12 / 60 mesh) to obtain a granule formulation.

preparation Embodiment 2

[3452] A powder formulation for encapsulation was prepared comprising the following ingredients.

[3453] Element

[3454]

[3455] The compound represented by formula (I) and lactose were sieved through a 60-mesh sieve. Cornstarch was sieved through a 120 mesh sieve. They are blended with magnesium stearate in a V-blender. 10% of the powder is placed in No. 5 hard gelatin capsules, 100 mg per capsule.

preparation Embodiment 3

[3457] A granule formulation for encapsulation was prepared comprising the following ingredients.

[3458] Element

[3459]

[3460] The compound represented by formula (I) and lactose were sieved through a 60-mesh sieve. Cornstarch was sieved through a 120 mesh sieve. They are mixed in a V-blender. The powder mixture was kneaded with an aqueous solution of low viscosity hydroxypropyl cellulose (HPC-L), granulated and dried. The resulting dry granules were sieved through a shaker sieve (12 / 60 mesh). The granules are placed in No. 4 hard gelatin capsules, 150 mg per capsule.

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PUM

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Abstract

Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.

Description

[0001] This application is an international application number PCT / JP2012 / 070876, and the international application date is August 10, 2012. After the PCT international application entered the Chinese phase, the national application number is 201280039516.6 and the title is "Tricyclic Heterocyclic Compounds and JAK Inhibitors" divisional application of the Chinese patent application. technical field [0002] The present invention relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activity. Background technique [0003] The JAK (Janus kinase) family is a tyrosine kinase family consisting of four members JAK1, JAK2, JAK3 and Tyk2 (tyrosine kinase 2), and plays an important role in cytokine signaling. [0004] Although this family of kinases is ubiquitously expressed in tissues other than JAK3, JAK3 expression is restricted to immune cells. This is consistent with the fact that JAK3 plays an important role in various receptor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/14A61K31/519A61P29/00A61P19/02A61P37/00A61P37/08
CPCC07D513/14C07D471/14C07D487/14C07D498/14A61P11/00A61P11/06A61P17/00A61P17/04A61P17/06A61P17/10A61P17/14A61P19/02A61P21/04A61P25/00A61P25/28A61P29/00A61P35/00A61P35/02A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61P5/14A61P9/00A61P9/10A61P3/10A61K31/4375A61K31/519A61K31/5365A61K31/542
Inventor 林圭史渡边恒夫外山公二加门淳司南昌孝宇仁巳由纪奈须麻莉子
Owner NISSAN CHEM IND LTD
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