C07D455/08

METHOD FOR EXTRACTING AND REFINING ALKALOIDS FROM IPECAC
20170368126 · 2017-12-28 ·

Provided is a method for extracting and refining alkaloids from ipecac, comprising: (1) grinding ipecac, adding acidic methanol/ethanol solution for extraction, obtaining an extraction solution A, concentrating under a reduced pressure, and obtaining a concentrated solution B; (2) using reversed-phase polymer filler J for adsorption, and performing desorption by washing with water, collecting a washing solution C, eluting with an alcoholic solution E and collecting a desorption solution D; (3) injecting the washing solution C and the desorption solution D into a preparative high performance liquid chromatograph for separation and purification respectively, to collect a solution G, and a solution H and a solution I respectively; and (4) concentrating the solutions G, H and I, which are then subjected to reversed-phase polymer filler K for adsorption respectively; eluting them respectively after adsorption with an alcoholic solution F; concentrating obtained eluates to dryness; and then performing vacuum drying.

Emetine derivatives, prodrugs containing same, and methods of treating conditions using same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Emetine derivatives, prodrugs containing same, and methods of treating conditions using same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Method for extracting and refining alkaloids from ipecac

Provided is a method for extracting and refining alkaloids from ipecac, comprising: (1) grinding ipecac, adding acidic methanol/ethanol solution for extraction, obtaining an extraction solution A, concentrating under a reduced pressure, and obtaining a concentrated solution B; (2) using reversed-phase polymer filler J for adsorption, and performing desorption by washing with water, collecting a washing solution C, eluting with an alcoholic solution E and collecting a desorption solution D; (3) injecting the washing solution C and the desorption solution D into a preparative high performance liquid chromatograph for separation and purification respectively, to collect a solution G, and a solution H and a solution I respectively; and (4) concentrating the solutions G, H and I, which are then subjected to reversed-phase polymer filler K for adsorption respectively; eluting them respectively after adsorption with an alcoholic solution F; concentrating obtained eluates to dryness; and then performing vacuum drying.

Method for extracting and refining alkaloids from ipecac

Provided is a method for extracting and refining alkaloids from ipecac, comprising: (1) grinding ipecac, adding acidic methanol/ethanol solution for extraction, obtaining an extraction solution A, concentrating under a reduced pressure, and obtaining a concentrated solution B; (2) using reversed-phase polymer filler J for adsorption, and performing desorption by washing with water, collecting a washing solution C, eluting with an alcoholic solution E and collecting a desorption solution D; (3) injecting the washing solution C and the desorption solution D into a preparative high performance liquid chromatograph for separation and purification respectively, to collect a solution G, and a solution H and a solution I respectively; and (4) concentrating the solutions G, H and I, which are then subjected to reversed-phase polymer filler K for adsorption respectively; eluting them respectively after adsorption with an alcoholic solution F; concentrating obtained eluates to dryness; and then performing vacuum drying.

Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same

Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

FUSED RING COMPOUND

The present invention relates to a fused ring compound; specifically, provided in the present invention is the use of a compound of formula I, or an optical isomer thereof, or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, or a deuterated compound thereof, in the preparation of a composition or a formulation for the prevention and/or treatment of tumours. The compound of the present invention has a significant and excellent precise therapeutic effect on tumours with low expression or no expression and low activity or no activity of mitochondrial permeability transition pores, low expression or no expression and low activity or no activity of peptidyl prolyl isomerase F, low expression or no expression of NNMT genes, high expression of DNA methylase, high expression of UHRFI, high methylation levels of NNMT gene nucleotide sites, and/or high methylation levels of DNA CpG sites in the NNMT gene region.

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