摘要:
The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.
摘要:
The present invention relates to a pyrrolo[2,1- f ][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1- f ][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1- f ][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
摘要:
Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.
摘要:
Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R 1 and R 2 are each independently hydrogen, straight or branched chained C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R 1 and R 2 together with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; R 3 is a hydrogen atom or a chlorine atom; R 4 is a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N.
摘要翻译:本发明提供了通式Ⅰ所示的2-芳基苯并呋喃-7-甲酰胺化合物或其药理学或生理学上可接受的盐,其制备方法和其制备抗肿瘤药物的用途,其中R 1和R 2 各自独立地为氢,直链或支链C 1 -C 4烷基,C 3 -C 4环烷基或含有氧或氮的饱和5-或6-元杂环基; 或R 1和R 2与N一起形成含有至少一个杂原子的未取代或取代的饱和的5-或6-元杂环基,其中杂原子是O,N和S,取代基是N上的甲基; R 3为氢原子或氯原子; R 4为氢原子或氟原子; X是CH,CF或N; Y为CH,CF或N.
摘要:
A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound of the present invention can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia.
摘要:
A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerising factor activity inhibitors and actin-aggregation inhibitors.
摘要:
Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.
摘要:
New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
摘要:
Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.