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Phosphodiesterase 4 inhibitor capable of avoiding vomiting reaction

A technology of phosphodiesterase and inhibitors, applied in the direction of medical preparations containing active ingredients, digestive system, organic active ingredients, etc., can solve the problems of PDE4 inhibitors that cannot avoid vomiting, and achieve improved cognitive ability, high Inhibit activity, prevent vomiting effect

Active Publication Date: 2012-07-25
兰晟生物医药(苏州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The first generation of PDE4 inhibitors such as rolipram has a good antidepressant effect, the reason why it cannot be marketed is the side effects such as nausea and vomiting caused by the inhibition of PDE4
Compared with the first-generation PDE4 inhibitors, the second-generation PDE4 inhibitors have better therapeutic effects, but so far no PDE4 inhibitors that can prevent vomiting have been marketed

Method used

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  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting reaction
  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting reaction
  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting reaction

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Embodiment Construction

[0031] Embodiments of the present invention will be further described in detail below in conjunction with the accompanying drawings.

[0032] A kind of phosphodiesterase 4 inhibitor that can avoid vomiting reaction, wherein, by formula (I) as

[0033]

[0034] Representative compounds or prodrugs or solvates,

[0035] R 1 are independently methoxy, bromo and substituted aryl;

[0036] X is an optionally substituted six-membered heterocyclic ring;

[0037] Y is - (CH 2 ) n -, -NH(CH 2 ) n -, -NH(CH 2 ) n -O-, wherein, the value of n can be any one digit in 0, 1, 2, 3;

[0038] Z is an optionally substituted aryl ring or an optionally substituted heteroaryl ring.

[0039] The above-mentioned formula (II) is

[0040]

[0041] Representative compounds or prodrugs or pharmaceutically acceptable salts or solvates;

[0042] Wherein: Z is any substituted aromatic ring.

[0043] The above-mentioned formula (III) is

[0044]

[0045] Representative compounds or pr...

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Abstract

The invention relates to a phosphodiesterase 4 inhibitor capable of avoiding a vomiting reaction. The phosphodiesterase 4 inhibitor is a compound or a pro-drug or a solvate represented by formula (I), wherein R1 is independent methoxyl, bromine and substituted aryl; X is a randomly substituted six-membered heterocycle; Y is -(CH2)n-, -NH(CH2)n- and -NH(CH2)n-O-, wherein n can be any one of 0, 1, 2 or 3; and Z is a randomly substituted aromatic ring or a randomly substituted heteroaromatic ring. The phosphodiesterase 4 inhibitor capable of avoiding the vomiting reaction is a novel biphenyl PDE4D inhibitor which is applicable to treating depression and Alzheimer's disease and improving cognitive competence, and is capable of avoiding a side effect such as the vomiting.

Description

technical field [0001] The present invention relates to the technical field of compounds capable of inhibiting phosphodiesterase, especially a biphenyl PDE4D inhibitor, specifically a phosphodiesterase 4 inhibitor capable of avoiding vomiting. Drugs can be used to treat depression, Alzheimer's disease and improve cognition. Background technique [0002] Phosphodiesterase 4 (PDE4) is mainly distributed in inflammatory cells (mast cells, macrophages, lymphocytes and epithelial cells) and nerve cells. PDE4 is closely related to the functions of the central nervous system and the immune system, and its inhibitors are considered to be new anti-inflammatory drugs and central nervous system drug candidates acting on intracellular targets. Since PDE4 specifically catalyzes the hydrolysis of cAMP, it plays a key role in regulating the concentration of intracellular cAMP. Inhibiting PDE4 causes cAMP to accumulate in cells and produce various biological effects, including anti-inflamm...

Claims

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Application Information

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IPC IPC(8): C07D295/096C07D237/14C07D237/22A61K31/495A61K31/50A61K31/501A61P25/24A61P25/28
CPCC07D237/14C07D237/02A61K31/495C07D403/04C07D295/096C07D237/22C07D295/04A61K31/496A61K31/501A61K31/50C07D295/092A61P1/08A61P25/24A61P25/28A61P43/00
Inventor 徐江平周中振
Owner 兰晟生物医药(苏州)有限公司
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