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Use of fibroblast growth factor receptor inhibitor

A technology of isomers and compounds, applied in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc., can solve problems such as unmet clinical needs

Pending Publication Date: 2021-08-31
TRANSTHERA SCIENCES (NANJING) INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, although some FGFR inhibitors have been proved to have a certain effect on FGFR-mutated cholangiocarcinoma in preclinical experiments and clinical trials, there is still a lot of room for improvement in the efficacy of cholangiocarcinoma, and there is a huge unmet clinical need

Method used

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  • Use of fibroblast growth factor receptor inhibitor
  • Use of fibroblast growth factor receptor inhibitor
  • Use of fibroblast growth factor receptor inhibitor

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0419] For the preparation of the compound of general formula (I) described in the present invention, please refer to the specific embodiments of WO2018040885.

[0420] Beneficial effects of the present invention

[0421] The compound represented by the general formula (I) of the present invention or its pharmaceutically acceptable salts and isomers can effectively treat cholangiocarcinoma. Studies have shown that it has a very good therapeutic effect on FGFR mutant cholangiocarcinoma.

[0422] The results of the kinase spectrum experiment show that the compound of the present invention has a good inhibitory effect on FGFR1-4. Can effectively and selectively inhibit FGFR1-3 relative to FGFR4.

[0423] The PK / PD study of the nude mouse cancer cell line xenograft (cell-derived xenograft, CDX) model shows that the tumor inhibitory rate of the compound of the present invention is linearly positively correlated with its systemic exposure.

[0424] According to the in vivo PK exp...

experiment example 1

[0429] Experimental example 1 compound of the present invention is paired In vivo drug efficacy test of human cholangiocarcinoma CC6204 subcutaneous xenograft tumor model

[0430] List of acronyms:

[0431] Qd once a day

[0432] Qw once a week

[0433] CMC-Na Carboxymethylcellulose sodium test substance: the compound in the present invention, its structure is shown in Table 1, and its preparation can be found in the specific implementation section of WO2018040885.

[0434] Gemcitabine hydrochloride was purchased from Shanghai Titan Technology Co., Ltd.

[0435] Source of tumor mass: CC6204 was established from a female patient with cholangiocarcinoma Xenograft model. The pathological diagnosis was intrahepatic cholangiocarcinoma with FGFR2-BICC1 fusion mutation.

[0436] Animals: Balb / c nude mice, female at 5-6 weeks (the age of the mice at the time of inoculation), were purchased from Jiangsu Jicui Yaokang Biotechnology Co., Ltd.

[0437] experiment method:

[0438...

experiment example 2

[0454] Experimental Example 2 Compounds of the present invention pair In vivo pharmacodynamic study of human cholangiocarcinoma CC6702 subcutaneous xenograft tumor model

[0455] Acronym list

[0456] Qd once a day

[0457] Qw once a week

[0458] CMC-Na Sodium Carboxymethyl Cellulose

[0459] Test substance: the compound of the present invention, the structure of which is shown in Table 1, and the preparation can be found in the specific embodiment section of WO2018040885.

[0460] Animals, source of tumor mass, patient information and other materials:

[0461] CC6702 was established from an Asian female patient with cholangiocarcinoma Xenograft model. The pathological diagnosis was intrahepatic cholangiocarcinoma with FGFR2-TTC28 fusion mutation.

[0462] Balb / c nude mice, female at 6-7 weeks (the age of mice at the time of inoculation), were sourced from Jiangsu Jicui Yaokang Biotechnology Co., Ltd.

[0463] experiment method:

[0464] 1. Construction and grouping ...

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Abstract

The invention belongs to the technical field of medicines, relates to use of a fibroblast growth factor receptor inhibitor and particularly relates to a compound represented by a general formula (I) for treating cholangiocarcinoma and pharmaceutically acceptable salts and isomers thereof, a pharmaceutical composition containing the compound or pharmaceutically acceptable salts and isomers thereof, a method for treating the cholangiocarcinoma by using the compound or pharmaceutically acceptable salts and isomers thereof, use of the compound or pharmaceutically acceptable salts and isomers thereof in cholangiocarcinoma treatment and use of the compound or pharmaceutically acceptable salts and isomers thereof in preparation of drugs for treating the cholangiocarcinoma of mammals. Each variable of the general formula is as defined in the description. Shown by researches, the compound represented by the general formula (I) or pharmaceutically acceptable salts and isomers thereof has a remarkable therapeutic action on the cholangiocarcinoma and has very great clinical application potentials.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a fibroblast growth factor receptor inhibitor for treating cholangiocarcinoma, a pharmaceutically acceptable salt and an isomer thereof, and a pharmaceutical composition containing it, which is used to treat cholangiocarcinoma A disease method, its use for treating cholangiocarcinoma, and its use in the preparation of a medicament for treating mammalian cholangiocarcinoma. Background technique [0002] Cholangiocarcinoma (CCA) is a malignant tumor with strong heterogeneity. Its location spreads from the capillary bile duct to the common bile duct, and can originate from any part of the biliary system. According to the anatomical site, cholangiocarcinoma can be divided into intrahepatic cholangiocarcinoma (iCCA), perihilarcholangiocarcinoma (pCCA) and distal cholangiocarcinoma (dCCA), which have special similarities, But there are also inter-tumor and intra-tumor dif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P35/00
CPCA61K31/517A61P35/00A61K31/5377A61K31/553A61K45/06A61P35/02C07D401/12C07D403/12C07D403/14C07D413/12
Inventor 盛泽娟强晓妍吴永谦
Owner TRANSTHERA SCIENCES (NANJING) INC
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