16535-67-4Relevant academic research and scientific papers
TARGETING OF ENDOPLASMIC RETICULUM DYSFUNCTION AND PROTEIN FOLDING STRESS TO TREAT NEUROLOGICAL CONDITIONS
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Page/Page column 00139; 00140-00141; 00154-00156, (2019/10/15)
Methods and therapeutic compositions are disclosed for treating neurological disorders, such as Amyotrophic Lateral Sclerosis (ALS), Alzheimer's disease, Parkinson's disease and/or Huntington's disease, using Salubrinal analogs, or pharmaceutically acceptable salts, hydrates, or solvates thereof.
Novel Urea Compounds, Preparation Methods and Uses Thereof
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Paragraph 0179-0180, (2016/11/14)
The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic.
Thiazole Compounds and Uses Thereof
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Paragraph 0034; 0062; 0063; 0064, (2015/05/05)
The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.
UREA COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS
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Paragraph 0038, (2013/03/28)
The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof. The present invention also relates to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. Further, the present invention relates to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for anti-apoptosis, preventing or treating a disease or disorder associated with apoptosis; especially useful for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
UREA COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS
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Paragraph 0052; 0053; 0054, (2013/05/22)
A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
SAR, cardiac myocytes protection activity and 3D-QSAR studies of salubrinal and its potent derivatives
Liu,He,Li,Li,Liu,Zhong,Li
, p. 6072 - 6079 (2013/02/22)
Salubrinal is a selective inhibitor of endoplasmic reticulum (ER) stress and affords remarkable protection to cardiomyocytes. By studying the structure-activity relationship (SAR) of salubrinal, it was found that modification of the quinoline ring terminus and thiourea unit could confer the compound PP1-24 with markedly enhanced cardioprotective activity (EC 50 2 = 0.741, r2 = 0.991).
Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative
Long, Kai,Boyce, Michael,Lin, He,Yuan, Junying,Ma, Dawei
, p. 3849 - 3852 (2007/10/03)
The synthesis and structure-activity relationships (SAR) of salubrinal, a small molecule that protects cells from apoptosis induced by endoplasmic reticulum (ER) stress, are described. It is revealed that the trichloromethyl group greatly contributes to the activity. Based on the SAR results, salubrinal was converted into a biotinylated derivative which retains activity and can be used as a biological tool for target identification.
