Abstract: The present invention relates to long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled texture, and uses thereof. Said compounds show ultralong acting anaesthetic effect, and belong to N-diethylaminoacetyl-2,6-dimethylaniline compounds, having a structure according to formula (I). Said compounds may self-assemble into micelle or gel in an aqueous solvent, and exert an in vivo elongated local anesthetic actions. Local anesthesia and/or analgesic activity can last more than 72 hours. The biomaterials can self-assemble into micelles or gels in water and have local anesthetic effect, as well as can further be used as the coating of medicinal bioactive molecules for treatment of pain, itching and the like and/or the drug carriers, together with as pharmaceutical adjuvants for delivery system. Thus, said materials have a favorable perspective.
Type:
Grant
Filed:
July 22, 2015
Date of Patent:
July 3, 2018
Assignee:
WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
Inventors:
Lei Tang, Jin Liu, Wensheng Zhang, Jun Yang, Bowen Ke, Qinqin Yin
Abstract: The present invention relates to an N-substituted imidazole carboxylic ester chiral compound containing an ether side chain and to its preparation and application. The structure of this compound is represented by Formula (I). This compound can induce a rapid and reversible general anesthesia effect. Animal experiments show that this compound has rapid and short-acting pharmacological characteristics, so that it can be used as a rapid and short-acting general anesthesia medicine. Compared with etomidate, this compound can reduce the inhibition on the synthesis of adrenal cortical hormone, with an advantage of rapid and full recovery of the post-operative patient. The only chiral carbon in the compound structure belongs to the R form.
Type:
Grant
Filed:
October 30, 2014
Date of Patent:
May 15, 2018
Assignee:
WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
Inventors:
Wensheng Zhang, Jun Yang, Jin Liu, Lei Tang, Bowen Ke
Abstract: Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y?C1-4 straight carbon chain. The compound can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia.
Abstract: Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y?C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
Type:
Grant
Filed:
October 13, 2010
Date of Patent:
January 26, 2016
Assignees:
West China Hospital, Sichuan University, Yichang Humanwell Pharmaceutical Co., Ltd.
Abstract: Use of low dose streptozocin in the preparation of an animal model for screening drugs for treatment of antoimmune type 1 diabetes is disclosed, in which streptozocin is administrated intravenously at a dose of 15-30 mg/kg per time for 5 days and administrated again on the 7th day and 14th day after last time of offering drug. A method for preparing rhesus monkey model of autoimmune type 1 diabetes and autoimmune type 1 diabetes animal model obtained are also disclosed.
Type:
Grant
Filed:
March 26, 2010
Date of Patent:
November 17, 2015
Assignee:
West China Hospital, Sichuan University
Inventors:
Yanrong Lu, Jingqiu Cheng, Shaoping Deng, Younan Chen, Bole Tian, Gang Mai, Yan Ren, Li Wang, Hongxia Li, Lingling Wei, Xi Jin, Chaofeng Qiao, Wensheng Zhang, Sirong He, Li Zeng
Abstract: Use of low dose streptozocin in the preparation of an animal model for screening drugs for treatment of antoimmune type 1 diabetes is disclosed, in which streptozocin is administrated intravenously at a dose of 15-30 mg/kg per time for 5 days and administrated again on the 7th day and 14th day after last time of offering drug. A method for preparing rhesus monkey model of autoimmune type 1 diabetes and autoimmune type 1 diabetes animal model obtained are also disclosed.
Type:
Application
Filed:
March 26, 2010
Publication date:
June 13, 2013
Applicant:
West China Hospital, Sichuan University
Inventors:
Yanrong Lu, Jingqiu Cheng, Shaoping Deng, Younan Chen, Bole Tian, Gang Mai, Yan Ren, Li Wang, Hongxia Li, Lingling Wei, Xi Jin, Chaofeng Qiao, Wensheng Zhang, Sirong He, Li Zeng
Abstract: Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y=C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
Type:
Application
Filed:
October 13, 2010
Publication date:
April 4, 2013
Applicants:
Yichang Humanwell Pharmaceutical Co., Ltd., West China Hospital, Sichuan University
Abstract: Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y?C14 straight carbon chain. The compound can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia.