163671-48-5Relevant articles and documents
Synthesis method of 4-substituent cyclohexanone liquid crystal intermediate
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Paragraph 0062-0064, (2021/05/19)
The invention discloses a synthesis method of a 4-substituent cyclohexanone liquid crystal intermediate, which comprises the following step: carrying out oxidation catalytic reaction on 4-substituent cyclohexanol under the action of trichloroisocyanide urea to obtain the 4-substituent cyclohexanone liquid crystal intermediate. The method is high in reaction selectivity, high in yield, environment-friendly, simple in post-treatment and suitable for industrial production.
Tetrahydrobenzo [4,5] thieno [2,3-d] pyrimidine compound and application thereof
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Paragraph 0037; 0038; 0041-0043, (2019/07/04)
The invention belongs to the technical field of medicines and relates to a tetrahydrobenzo [4,5] thieno [2,3-d] pyrimidine compound as well as a preparation method and application of the compound as an epidermal growth factor receptor tyrosine kinase inhibitor. The tetrahydrobenzo [4,5] thieno [2,3-d] pyrimidine compound, a prodrug, medicine active metabolite and a pharmaceutically acceptable saltthereof have the structural formulae as shown in the specification, in the formulae, R is independently selected from hydrogen, C1-C4 alkyl, C1-C4 alkoxy and halogen; R' is independently selected from hydrogen, C1-C4 alkyl, C1-C4 alkoxy and halogen. A synthesis method of the compound provided by the invention is simple and convenient and applicable to industrial production, and bioactivity testing shows that the compound has the activity of inhibiting epidermal growth factors, a human lung cancer cell strain A549 and a human ovarian carcinoma cell strain SKOV3, and is an epidermal growth factor receptor tyrosine kinase inhibitor with an anti-tumor function.
Piperazine structure containing four tetrahydrobenz [4, 5] thieno [2, 3 - d] pyrimidine compound and use thereof
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Paragraph 0020; 0024-0026, (2017/08/08)
The invention belongs to the technical field of medicine, and relates to piperazine-structure-containing tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine compounds and application thereof as an epidermal growth factor receptor tyrosine kinase inhibitor, and a preparation method of the compounds. The piperazine-structure-containing tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine compounds and pharmaceutically acceptable salts thereof, and a pharmaceutically compatibility-acceptable carrier or diluter can be used as an epidermal growth factor receptor tyrosine kinase inhibitor. The structural general formula is disclosed in the specification, wherein R1, R2 and R3 are disclosed in the specification. The compounds are simple in synthesis method and suitable for industrial production. The bioactivity test shows that the compounds have the activity of inhibiting epidermal growth factor, human lung cancer cell strain A549, human oophoroma cell strain SKOV3 and human osteosarcoma cell U2OS-EGFP-4A12G, and are an epidermal growth factor receptor tyrosine kinase inhibitor with antitumor function.
Benzylamine structure containing four tetrahydrobenz [4, 5] thieno [2, 3 - d] pyrimidine compound and use thereof
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Paragraph 0020; 0023; 0024, (2017/08/25)
The invention belongs to the technical field of medicines and relates to a tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidine compound containing a benzylamine structure and application of the tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidine compound as an epidermal growth factor receptor tyrosine kinase inhibitor and a preparation method of the tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidine compound. The tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidine compound containing the benzylamine structure, pharmaceutically acceptable salt, and a pharmaceutically compatibility acceptable carrier or a diluent are used as the epidermal growth factor receptor tyrosine kinase inhibitor. The structural general formula of the compound is shown in the description, wherein R1 is H or C1-C4 alkyl groups, and R2 is independently selected from H, halogen or C1-C4 alkoxy groups. The compound provided by the invention is simple and convenient in synthesis method, and suitable for industrial production, and a biological activity test result shows that the compound has the effect of restraining activity of epidermal growth factors, activity of human lung cancer cell line A549, activity of human ovarian cancer cell line SKOV3 and activity of human osteosarcoma cell U2OS-EGFP-4A12G, and is the epidermal growth factor receptor tyrosine kinase inhibitor with an anti-tumor effect.
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides
Chu, Xin-Jie,Bartkovitz, David,Danho, Waleed,Swistok, Joseph,Cheung, Adrian Wai-Hing,Kurylko, Grazyna,Rowan, Karen,Yeon, Mitch,Franco, Lucia,Qi, Lida,Chen, Li,Yagaloff, Keith
, p. 4910 - 4914 (2007/10/03)
Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His 6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides.
Selective cyclic peptides with melanocortin-4 receptor (MC4-R) agonist activity
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, (2008/06/13)
Peptides cyclized via disulfide or lactam bridges having melanocortin-4 receptor (MC4-R) agonist activity useful for treatment of obesity.
Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity
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, (2008/06/13)
Peptides of formulae I, II and III selectively activate melanocortin-4 (MC-4) receptor activity.