- QUINOLYL-CONTAINING COMPOUND AND PHARMACEUTICAL COMPOSITION, AND USE THEREOF
-
Provided is a quinolyl-containing compound as shown in general formula (I) or (II) or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an isotopic label, or an isomer thereof, and further provided are a pharmaceutical composition comprising the compound and use of the compound and the pharmaceutical composition. The provided compound has a dual molecule function, can serve as multi -target inhibitors of novel tyrosine kinase/histone deacetylase, can simultaneously achieve the effect of two inhibitors, has excellent biological activity and pharmacokinetic properties, and has the application potential particularly in the field of treatment of tumors.
- -
-
-
- Preparation methods of tyrosine kinase inhibitor XJF007 and its intermediate
-
The invention discloses preparation methods of tyrosine kinase inhibitor XJF007 with a general structural formula (I) and its intermediate. The preparation method of the tyrosine kinase inhibitor XJF007 employs a collecting synthesis strategy of construct
- -
-
-
- CARBAMATE AND UREA COMPOUNDS AS MULTIKINASE INHIBITORS
-
The present disclosure describes carbamate and urea compounds as novel multikinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such multikinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders associated with kinases are also described.
- -
-
Paragraph 076; 085
(2019/07/13)
-
- A tyrosine kinase inhibitor and intermediate preparation method
-
The invention provides preparation methods of a tyrosine kinase inhibitor and intermediates thereof, specifically preparation methods of N-[3-fluoro-4-[[6-methoxy-7-[oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (Foretinib), and analogs and intermediates thereof. 1,1-cyclopropane dicarboxylic acid diester is used as the raw material to prepare a compound of the formula VI; and the compound of the formula VI is hydrolyzed and then reacts with a compound of the formula VIII, so as to prepare the Foretinib and the analogs thereof. The condition of each reaction step is mild, the preparation method is easy to operate, the price of the raw materials is low, and thus the production cost is reduced, the yield is relatively high, and the preparation methods are suitable for industrialized production.
- -
-
-
- A alkyne generation quinoline derivatives and its preparation and use
-
The invention discloses alkynylquinoline derivatives, and a preparation method and application thereof. The acetylenoquinoline derivatives are alkynylquinoline compounds as shown in a general formula I which is described in the specification and pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof. The invention also provides the preparation method for the derivatives and relates to inhibition activity of the compounds as shown in the formula I to a variety of protein tyrosine kinases (e.g. C-Met and VEGFR). Thus, the compounds can be used as anticancer drugs for treatment of human cancers.
- -
-
-
- HYDROXAMIC ACID COMPOUND CONTAINING QUINOLYL AND PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THIS COMPOUND AND USE THEREOF
-
Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc.
- -
-
-
- Quinolyl-containing Hydroxamic Acid Compound and Preparation Method Thereof, and Pharmaceutical Composition Containing This Compound and Use Thereof
-
Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc.
- -
-
-
- C-MET MODULATORS AND METHODS OF USE
-
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
- -
-
-