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Tricyclic heterocycles and jak inhibitors

A compound, cycloalkyl technology, used in anti-inflammatory agents, organic chemistry, drug combinations, etc., can solve the problem of limited expression

Inactive Publication Date: 2016-08-17
NISSAN CHEM IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 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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  • Tricyclic heterocycles and jak inhibitors
  • Tricyclic heterocycles and jak inhibitors
  • Tricyclic heterocycles and jak inhibitors

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[3446] Granule formulations were prepared comprising the following ingredients.

[3447]

[3448]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

[3450] A powder formulation for encapsulation was prepared comprising the following ingredients.

[3451]

[3452] 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

[3454] A granule formulation for encapsulation was prepared comprising the following ingredients.

[3455]

[3456] 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 activity are provided. A tricyclic heterocyclic compound represented by the following formula (Ia): wherein, ring Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a, L2a, L3a and na are as defined in the specification.

Description

technical field [0001] The present invention relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activity. Background technique [0002] 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. [0003] 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-mediated signaling pathways, such as IL (interleukin)-2, IL -4, IL-7, IL-9, IL-15 and IL-21 signaling (Non-Patent Documents 1 and 2). [0004] Decreased JAK3 protein levels and a common gamma chain gene defect were observed in immunodeficiency patients known as X-linked severe combined immunodeficiency (XSCID), suggesting that blocking the JAK3 signaling pathway results in immunosuppr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/14A61K31/519A61P37/00
CPCC07D471/14C07D487/14C07D498/14C07D513/14A61P11/00A61P11/06A61P17/00A61P17/04A61P17/06A61P17/10A61P17/14A61P19/02A61P21/04A61P25/00A61P25/28A61P29/00A61P35/00A61P35/02A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61P5/14A61P9/00A61P9/10A61P3/10A61K31/4375A61K31/519A61K31/5365A61K31/542
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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