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Apaf-1 inhibitor compounds

A compound, CH2 technology, applied in anti-inflammatory agents, drug combinations, organic chemistry, etc., can solve the problem of not containing active molecules of apoptosis

Active Publication Date: 2015-02-25
SPIRAL THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are solutions on the market that provide a buffered and sterile environment for transport organs, but they do not contain any active molecules that prevent apoptosis

Method used

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  • Apaf-1 inhibitor compounds
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  • Apaf-1 inhibitor compounds

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Experimental program
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Embodiment Construction

[0086] abbreviation:

[0087]

[0088]

[0089] The following examples help to better explain the present invention, but are not considered to limit the present invention.

[0090] The nomenclature used in this document is based on the CFW_CHEMICAL_NAME function in Chemdraw for Excel version 12.

[0091] General data:

[0092] Compounds were synthesized using polystyrene AM RAM resin obtained from Lapp Polymers, Germany. In the reaction, a polystyrene syringe with a polystyrene disc was used and an HS501 digital IKA laboratory technology stirrer was used. In the microwave-performed reactions, a microwave extraction apparatus (CEM Discover) model with a 10 ml glass reactor was used.

[0093] Product Analysis:

[0094] • Method A: Reverse Phase-High Performance Liquid Chromatography using Hewlett Packard Series 1100 (UV Detector 1315A) equipment and X-Terra C18 (15 x 0.46 cm, 5 μm) reverse phase column. The wavelength of UV detection is 210 nm. Use 1ml / min of CH 3...

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PUM

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Abstract

Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and / or treatment of a pathological and / or physiological condition associated with an increase of apoptosis.

Description

technical field [0001] The present invention relates to compounds for preventing and / or treating diseases caused by apoptosis or preventing degenerative processes caused by apoptosis. technical background [0002] Apoptosis or programmed cell death is a complex physiological phenomenon concerned with maintaining cellular homeostasis. Due to its critical role in health maintenance, apoptosis is regulated by a variety of cellular control mechanisms. Many pathologies are based on dysfunction of apoptosis. Thus, excess apoptosis may affect tissue function (eg, cardiomyocyte death in the context of myocardial infarction), whereas excessive inhibition of apoptosis leads to uncontrolled cell survival (eg, tumorigenic processes). Cellular components that regulate apoptosis in healthy cells are in stable homeostasis. There are at least two well-characterized activation pathways of the caspase cascade for apoptosis. One of these extrinsic pathways is activated by extracellular sig...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D241/06A61K31/495
CPCC07D401/12C07D405/14C07D403/12C07D409/12C07D405/12C07D403/14C07D409/14C07D241/08A61P3/10A61P9/00A61P9/10A61P17/02A61P19/02A61P25/14A61P25/16A61P25/28A61P27/02A61P27/06A61P29/00A61P31/00A61P31/12A61P31/18A61P37/04A61P43/00A61K31/495
Inventor 安赫尔·梅塞盖尔·佩波亚历杭德拉·莫雷·费尔南德斯丹尼尔·冈萨雷斯·皮纳乔伊莎贝尔·马西普·马西普恩里克·法勒斯·帕亚纳蒂夫达德·加西亚·维勒埃斯特尔·蒙洛里奥·马斯朱瓦洛·卡泰纳·鲁伊斯
Owner SPIRAL THERAPEUTICS INC