Compound having cyclic structure

A compound and heterocyclic technology, applied in the field of compounds with a ring structure, can solve the problem that the anti-inflammatory activity is not known, and achieve the effect of excellent liver toxicity

Pending Publication Date: 2020-05-01
DAIICHI SANKYO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Patent Document 1 reports the following 5-membered aromatic heterocyclic compounds, but the anti-inflammatory activity of these compounds is not known

Method used

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  • Compound having cyclic structure
  • Compound having cyclic structure
  • Compound having cyclic structure

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0756] (Formulation Example 1) Powdered Drug

[0757] The compound of the present invention or its salt (5 g), lactose (895 g) and cornstarch (100 g) were mixed in a blender to obtain a powdered drug.

preparation Embodiment 2

[0758] (Formulation Example 2) Granules

[0759] A compound of the present invention or a salt thereof (5 g), lactose (865 g) and low-substituted hydroxypropylcellulose (100 g) were mixed, and then a 10% aqueous solution of hydroxypropylcellulose (300 g) was added thereto. The mixture was kneaded, granulated by an extrusion granulator, and dried to obtain granules.

preparation Embodiment 3

[0760] (Formulation Example 3) tablet

[0761] The compound of the present invention or its salt (5 g), lactose (90 g), cornstarch (34 g), crystalline cellulose (20 g) and magnesium stearate (1 g) were mixed in a blender and compressed into tablets by a tablet machine And get the tablet.

[0762] The pharmacological activity of the compound of the present invention or a pharmacologically acceptable salt thereof was examined by the following test.

[0763] (Test Example) Measurement of IL-10 Growth Rate

[0764] The test substance was suspended in 0.5% (w / v) methylcellulose and orally administered to mice at a dose of 100 mg / kg. One hour later, lipopolysaccharide (LPS, Sigma-Aldrich, L2630 (trade name)) (0.4 mg / kg) was intraperitoneally administered to induce inflammation. One hour after LPS administration, blood was collected from the vena cava under isoflurane anesthesia, placed in a test tube containing a serum separator, allowed to stand at room temperature for 20-30 min...

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PUM

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Abstract

The present invention addresses the problem of providing a compound having an anti-inflammatory effect, a pharmacologically acceptable salt thereof, etc. The means for solution according to the present invention is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (The symbols in the formula are defined as follows. A: benzene, etc.; E: -CH2-, etc.; G: afive-membered aromatic heterocycle, etc.; X: cyclohexane, etc.; J: a five-membered aromatic heterocycle, etc.; Y: a phenyl group, etc.; R1, R2, and R3: a halogen atom, etc.; R4: a C1-6 alkyl group, etc.; R5: a hydrogen atom, etc.; R6a, R6b, R6c, and R6d: a hydrogen atom, etc.; R7: a hydrogen atom, etc.; R8: a hydrogen atom, etc.; n1, n2, n3: 1, etc.)

Description

technical field [0001] The present invention relates to a compound with a specific chemical structure or a pharmacologically acceptable salt thereof with peripheral and / or central anti-inflammatory activity, and a preparation method thereof. The present invention also relates to the mechanism of action, the pharmaceutical composition, the preparation method of the pharmaceutical composition, the prevention and / or treatment methods related to the compound or its pharmacologically acceptable salt, etc. Background technique [0002] Patent Document 1 reports the following 5-membered aromatic heterocyclic compounds, but the anti-inflammatory activity of these compounds is not known. [0003] [Formula 1] [0004] [0005] With the progress of research, the relationship between psychiatric or neurodegenerative diseases and inflammation has been reported in recent years (Non-Patent Documents 1 and 2). [0006] It has been reported that stress increases the production of inflam...

Claims

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Application Information

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IPC IPC(8): C07D249/08A61K31/4196A61K31/4439A61K31/454A61K31/5377A61P1/00A61P1/02A61P1/04A61P1/16A61P1/18A61P3/00A61P3/10A61P9/04A61P9/10A61P11/00A61P11/06A61P11/08A61P17/00A61P17/02A61P17/06A61P17/10A61P17/14A61P19/02A61P21/02A61P25/00A61P25/02A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/26A61P25/28A61P25/30A61P27/02A61P27/14A61P27/16A61P29/00A61P31/18A61P37/02A61P37/06A61P37/08A61P43/00C07D401/14C07D403/14C07D405/14C07D413/14C07D491/052
CPCA61P1/00A61P1/02A61P1/04A61P1/16A61P1/18A61P3/00A61P3/10A61P9/04A61P9/10A61P11/00A61P11/06A61P11/08A61P17/00A61P17/02A61P17/06A61P17/10A61P17/14A61P19/02A61P21/02A61P25/00A61P25/02A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/26A61P25/28A61P25/30A61P27/02A61P27/14A61P27/16A61P29/00A61P31/18A61P37/02A61P37/06A61P37/08A61P43/00C07D249/08C07D401/14C07D403/14C07D405/14C07D413/14C07D491/052C07D491/107C07D498/10A61K31/4196A61K31/5377C07D471/04A61K31/4439C07B2200/13A61K31/454Y02P20/55
Inventor 谷口亨岩本理斋藤启志中岛胜义小川泰之栗川伸也长田圣子伊藤香织来生江利子
Owner DAIICHI SANKYO CO LTD
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