34 results about "Macrocycle Compounds" patented technology

To provide a method for producing a bipyridine derivative, which enables obtaining a high-purity target compound (including an intermediate) without performing purification by column chromatography, provides a high yield, and is industrially advantageous.SOLUTION: A method for producing a bipyridine derivative represented by formula (3) comprises a step of obtaining a metal complex as an intermediate. In the formula, each of R13 to R20 is a hydrogen atom or a substituent; a plurality of R13 to R20 may be the same or different; at least one of six R14 to R16 is a substituent; at least one of two R17 is a hydrogen atom; any two substituents of R13 to R20 may be linked to each other to form a ring; R17 to R20 may contain a pyrrolyl group which may contain a halogen atom or a substituent; and at least one of R14 to R16 may have a halogen atom or a substituent.SELECTED DRAWING: None

The present disclosure relates to a macrocyclic compound represented by formula I, a pharmaceutical composition containing the compound or a pharmaceutically acceptable salt, prodrug, solvate, polymorph, isomer and stable isotopic derivative thereof, a preparation method therefor, and a use thereof as a TRK, ROS1, c-Met, CSF1 and / or ALK inhibitor.

The disclosure provides solid forms of Compound A, as described herein. The disclosure also provides pharmaceutical compositions comprising the disclosed solid forms and methods of using the disclosed solid forms and pharmaceutical compositions (e.g., to treat cancer).

The present disclosure relates to solid forms of Compound 1, or a pharmaceutically acceptable form thereof, a pharmaceutically acceptable salt of Compound 1, or pharmaceutically acceptable solvate thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a farnesylated protein, using the same.

The application discloses a compound shown in formula I. The compound shown in formula I is a 3,5-dimethoxyaniline FGFR2 macrocycle inhibitor. The compound of the application can effectively inhibit the growth of various tumor cells and has FGFR2 inhibiting effect, and thus can be used for preparing an antitumor drug. The application further relates to the compound shown in formula I, a pharmaceutical composition containing the compound shown in formula I and the use of the compound in treating FGFR2-mediated related diseases and preparing a drug for treating FGFR2-mediated related diseases.

The present invention relates to aryl thiol macrocycles of Formula (I) wherein R1, R2, RA1, X1, X2, X3, X4, L, X5, and Ring A are as described in the description, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of Formula (I), and their use as agonists of the orexin-2 receptor.

This application relates to the technical field of medicines and relates to a macrocyclic compound containing an amide substitution, in particular to a compound shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as to a method of preparation, a pharmaceutical composition containing the compound and its use in the treatment of diseases.

The present application relates to a broad-spectrum RAS inhibitor having a macrocyclic structure as represented by formula (I). Specifically, the present invention relates to a compound as represented by formula (I), a preparation method therefor, and a pharmaceutical composition thereof, and further relates to the use of the compound and pharmaceutical composition thereof in the preparation of a drug for treating KRAS protein-related diseases, for example, for treating cancer.

The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt, isotope variant, tautomer or stereoisomer thereof, as a generic RAS mutant inhibitor. The invention also provides pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts, isotope variants, tautomers or stereoisomers thereof, and uses thereof in the treatment of cancer.

The present invention relates to compounds of formula (I) that have the potential to be used as metal complexes in radiotherapy. TIFF2024538619000043.tif85132 (wherein A is CO2R 1 , and PO3R 1 and B is selected from the group consisting of COR 2 , and PO3R 2 R 1 , R 2 and R 3 are each independently H and C1 to C 12 alkyl, and each R a is independently selected from the group consisting of H, F, Cl, Br, I, CH3, CH2CH3, CH(CH3)2, OH, OCH3, OCH2CH3, CF3, OCF3, NO2, NH2, and CN; b are independently selected from the group consisting of H, F, Cl, Br, I, CH3, CH2CH3, CH(CH3)2, OH, OCH3, OCH2CH3, CF3, OCF3, NO2, NH2, and CN, and L is a linker having 1 to 20 atoms in the normal chain), or a pharma- ceutically acceptable salt thereof.

The application discloses a carbazole-maleimide alternating conjugated macrocyclic material for efficient capture of radioactive triiodide and a preparation method thereof. The conjugated macrocyclic compound has a rigid pi conjugated skeleton, can be efficiently synthesized through one-step tandem condensation reaction, and can obtain two different crystal conformations (MC-Czalpha and MC-Czbeta) through crystal condition regulation. The two conformations show significant differences when adsorbing triiodide (I3 ‑ ), wherein the MC-Czalpha conformation has superfast adsorption kinetics, the rate constant can reach 5.44*10 ‑2 g·mg ‑1 ·min ‑1 , and high removal efficiency is maintained in a wide pH range, and the reuse performance is stable. The conjugated macrocyclic compound has a clear structure, excellent adsorption performance, and has a good application prospect in the fields of nuclear waste treatment, environmental remediation and iodine detection.

This invention relates to a novel spiro macrocyclic compound of general formula (I) that is an orexin 2 receptor agonist. [Formula 1] JPEG2026518313000385.jpg27170

The present disclosure features macrocyclic compounds capable of inhibiting Ras proteins, as well as pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer.

The present invention relates to novel spiro-macrocyclic compounds of general formula (I) which are Orexin 2 receptor agonists.

The present disclosure provides macrocyclic compounds and pharmaceutical compositions and protein complexes thereof capable of inhibiting Ras proteins, and their use in treating cancer.

The present invention provides the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof, stereoisomer, in combination with a MEK inhibitor in the preparation of a medicament for treating a disease.

The present application relates to the technical field of medicines, and relates to a macrocyclic compound containing amide substitution, in particular to a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof in the treatment of disease.

The present invention relates to macrocyclic compounds of any one of Formula (I), or a pharmaceutically acceptable form thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a famesylated protein, using the same.

Macrocyclic compounds containing substituted 2-(1H-indol-7-yl)-3,4-dihydropyrazino[1,2-a]indol-1(2H)-ones inhibit binding of Mcl-1 to Bcl-2 family members, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

The application relates to the technical field of chemical medicines, in particular to a kind of dianilopyrimidine macrocycle containing crown ether fragment and its preparation method and application.A series of dianilopyrimidine macrocycle containing crown ether fragment is synthesized in the application, and the problem of poor clinical effect of drug in current brain glioma treatment is overcome.The series of compounds have good inhibitory activity on brain glioma, and are suitable for treating brain glioma and related drug research and development.Moreover, the drug is widely distributed in vivo and is rapidly cleared, so that the possibility of drug accumulation poisoning is avoided;oral bioavailability is moderate (F=18.7%);these findings highlight the advantages and challenges of the pharmacokinetic characteristics of compound 13, and lay a foundation for further optimizing and improving the in-vivo stability and bioavailability strategy.

The present invention relates to novel spiro-macrocyclic compounds of general formula (1) which are Orexin 2 receptor agonists.