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Novel pharmaceutical composition for treating nociceptive pain

A kind of sensory pain, composition technology, applied in the field of new pharmaceutical composition

Inactive Publication Date: 2011-08-10
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no information about the effect of morpholine derivatives including indenolazine or its optically active form (+)-2-[(inden-7-yloxy)methyl]morpholine on rheumatoid arthritis or osteoarthritis. Nociceptive Pain Effective Reports

Method used

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  • Novel pharmaceutical composition for treating nociceptive pain
  • Novel pharmaceutical composition for treating nociceptive pain
  • Novel pharmaceutical composition for treating nociceptive pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Synthesis of (+)-2-[(inden-7-yloxy)methyl]morpholine (hereinafter referred to as compound A) hydrobromide

[0084]Under ice cooling and stirring, 2.92 g of 47% hydrobromic acid was dissolved in a mixed solvent of 500 ml of water-500 ml of methanol. Under the same conditions, 1000 ml of diethyl ether was added, followed by 10 g of Compound A(-)-(2R,3R)-di-O-benzoyl tartrate, followed by vigorous stirring for 30 minutes. After standing still, the water layer was separated and washed 4 times with 500ml diethyl ether. The resulting aqueous layer was concentrated under reduced pressure at room temperature or lower, dissolved in methanol, and filtered. After the filtrate was concentrated under reduced pressure at a temperature below room temperature, it was azeotroped with toluene at a temperature below room temperature. After the obtained oily substance was crystallized from isopropanol-diethyl ether, the crystals were filtered off. The obtained crystals were recrystalliz...

Embodiment 2

[0089] The preparation of embodiment 2 compound A besylate (α type crystal)

[0090] Under ice cooling, add 1000mg of compound A(-)-(2R,3R)-di-O-benzoyl tartrate into 20ml ethyl acetate-20ml saturated aqueous sodium bicarbonate solution, and stir rapidly under the same conditions After that, the organic layer was separated. After the obtained organic layer was washed 2 times with 20 ml of ice-cooled saturated aqueous sodium bicarbonate solution, then with 10 ml of ice-cooled saturated brine, and after drying with anhydrous magnesium sulfate, it was added to the , 269mg of benzenesulfonic acid in 10ml of ethanol formed in the solution. After concentrating the resulting solution under reduced pressure at a temperature below room temperature, crystallization was carried out with ethanol-diethyl ether, and the crystals were filtered and washed with diethyl ether. The obtained crystals were recrystallized from 3 ml of acetone-0.1 ml of water-3 ml of diethyl ether to obtain 422 mg...

Embodiment 3

[0096] Analgesic Effects of Monoiodoacetate (MIA)-Induced Osteoarthritis Model

[0097] This disease model was prepared according to the description in Toxicol Pathol 31(6), 619-624(2003). Male SD rats (6-7 weeks old, Chiya-ruzuriba, Japan) were anesthetized with halothane (Takeda Pharmaceuticals), and sodium iodoacetate (MIA; Sigma, St. Single injection (20mg / ml) into the joint cavity. MIA was dissolved in saline and 50 μl was injected with a 26G 0.5 inch needle. After 3 weeks of administration of MIA (after the occurrence of osteoarthritis), the solvent (Vehicle) and the dilution obtained after diluting Compound A with a solvent to a predetermined concentration were orally administered to rats in each group (8 rats were used in each group). ). The solvent is distilled water. One hour after the administration, the weight difference between the left and right hind limbs was measured with an Incapacitance Tester (Linton Instrumentation, Norfork, UK). The inhibition rate of...

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Abstract

The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present invention is useful in providing an excellent pharmaceutical composition for treating nociceptive pain. In addition, the present invention is particularly useful in providing a pharmaceutical composition for treating pain accompanying a disease selected from the group consisting of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, spondylosis deformans, gouty arthritis, juvenile arthritis, scapulohumeral periarthritis, and cervical syndrome, lumbago, lumbago accompanying spondylosis deformans, menalgia, pain and tumentia after inflammation, operation or injury, pain after odontectomy, and cancer pain. In addition, the present invention is particularly useful for alleviating pain in a damaged cartilage region, and is particularly useful for osteoarthritis in which NSAIDs are not effective.

Description

Technical field [0001] The present invention relates to novel pharmaceutical compositions of morpholine derivatives or pharmaceutically acceptable salts thereof for the treatment of nociceptive pain. Background technique [0002] Pain is a spontaneous complex sensation reflecting substantial or potential tissue damage and an emotional response to the sensation, which is diverse. In addition, pain can be roughly divided into somatic pain and psychogenic pain, and the former can be further divided into nociceptive pain and neuropathic pain. Nociceptive pain is pain caused by external stimuli or pain resulting from visceral disease. Nociceptive pain can be divided into acute and chronic diseases, most of which are acute diseases that disappear once the underlying disease is cured and function as biological signals caused by the disorder. Neuropathic pain is chronic pain caused by dysfunction of the nervous system in peripheral nerves or central nervous system, including pain ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5375A61P25/04C07D265/30
CPCC07D265/30A61K31/5375A61P19/00A61P19/02A61P19/06A61P25/04A61P29/00A61K31/015
Inventor 竹下畅昭西垣扶佐子青木俊明田村诚司菊池和美黑田昭雄
Owner ASTELLAS PHARMA INC
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