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Propionamide derivative and application for schizophrenia

A schizophrenia and mental technology, applied in the field of medicine, can solve the problems of weakening the therapeutic effect of amisulpiride and the recognition disorder of new objects in animals

Active Publication Date: 2021-03-12
NHWA PHARMA CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chronic administration of PCP can cause new object recognition barriers in animals, and amisulpride can improve this symptom, and its effect is similar to that of inhibiting 5-HT 7 Receptor-related, 5-HT 7 Receptor agonists can attenuate the therapeutic effect of amisulpride

Method used

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  • Propionamide derivative and application for schizophrenia
  • Propionamide derivative and application for schizophrenia
  • Propionamide derivative and application for schizophrenia

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: preparation method

[0022] The preparation method of 112-9

[0023]

[0024] Synthesis of Intermediate 1:

[0025] Weigh 5g of 7-methoxy-3,4-dihydroisoquinolin-1(2H)-one, add 25mL of 48% HBr solution, heat to reflux, react for 8 hours, and TLC monitors that the reaction is complete. Add 200mL of water to dilute, extract with dichloromethane (3x100mL), wash the organic phase with 100ml of saturated brine, anhydrous Na 2 SO 4 After drying, the solvent was evaporated under reduced pressure and separated by column chromatography (ethyl acetate / petroleum ether=1:1) to obtain 3.3 g of solid with a yield of 72.1%.

[0026] Synthesis of Intermediate 2:

[0027] Take 3.3g intermediate 1, 8.2g 1,3-dibromopropane, 8.4g K 2 CO 3 and 50ml of acetonitrile in a 100ml reaction flask, heated up to 50°C and reacted overnight, after the reaction was completed, lowered to room temperature, filtered with suction, concentrated the dry solvent under reduced pressure, s...

Embodiment 2

[0032] Embodiment 2: pharmacological embodiment

[0033] 112-9 Pharmacologically Related Research

[0034] 1. In vitro Ki determination

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Abstract

The invention belongs to the field of medicines, and particularly relates to a propionamide derivative and application thereof in schizophrenia. The propionamide derivative is CY150112-9, and tests show that the in-vitro affinity of the propionamide derivative is similar to that of CY150112. The CY150112-9 has high affinity with 5-HT2A and D2 receptors, the affinity with 5-HT2A is higher than thatof D2 receptors, it is speculated that the CY150112-9 has a certain effect on negative symptoms while positive symptoms are improved, and the CY150112-9 has a low extrapyramidal side reaction. CY150112-9 also has certain affinity to D3 and 5-HT7, and it is speculated that CY150112-9 may have the effect of improving cognition clinically. And the maximum tolerance of CY150112-9 is higher than 112.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a propionamide derivative and its use for schizophrenia. Background technique [0002] Schizophrenia is the most serious and harmful disease among all mental diseases, with a global incidence of about 1-2%. The lifetime prevalence rate of patients with schizophrenia is 0.7-0.8%, and there is no obvious correlation with gender, race, or social boundaries, and the mortality rate is 2-3 times higher than that of the general population. The latest research shows that the social burden of mental illness ranks first among diseases in China, surpassing diseases such as cardiovascular and cerebrovascular diseases, respiratory system and malignant tumors. [0003] After decades of research, it was found that D 2 , 5-HT 1A , 5-HT 2A and H 1 Five receptors are very important for schizophrenia. with D 2 Receptor action can be effective in treating positive symptoms of schizophrenia...

Claims

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Application Information

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IPC IPC(8): C07D413/14A61P25/18A61K31/4725
CPCC07D413/14A61P25/18
Inventor 于民权窦飞邱印利侯媛媛樊振华孙庆弟徐祥清
Owner NHWA PHARMA CORPORATION
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