C07D215/22

CRYSTALLINE OF COMPOUND AS C-MET KINASE INHIBITOR AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present application falls within the field of medicinal chemistry, relates to the crystalline of a compound as a c-Met kinase inhibitor, and specifically relates to the crystalline of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystalline for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystalline of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.

CRYSTALLINE OF COMPOUND AS C-MET KINASE INHIBITOR AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present application falls within the field of medicinal chemistry, relates to the crystalline of a compound as a c-Met kinase inhibitor, and specifically relates to the crystalline of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystalline for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystalline of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.

QUINOLINE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF

A quinoline derivative, and preparation methods and uses thereof; specifically, a quinoline derivative of Formula (I) or a stereoisomer, an N-oxide and a salt thereof, their preparation methods, and their uses as pesticides, forms of a pesticide composition thereof, and methods of controlling pests by using these compounds or compositions in agriculture or gardens; wherein R1, R2, R3, R4, R5, RA, RB, RC, RC1, RC2, R6, R7, R8, R9, R10, R11, Rx and n have the definitions as described herein.

##STR00001##

Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer
20210024467 · 2021-01-28 ·

Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.

Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer
20210024467 · 2021-01-28 ·

Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.

Multi-tyrosine kinase inhibitors derivatives and methods of use
10899712 · 2021-01-26 · ·

The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.

Multi-tyrosine kinase inhibitors derivatives and methods of use
10899712 · 2021-01-26 · ·

The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.

Derivatives and composition of quinoline and naphthyridine

Derivatives of quinoline and naphthyridine, methods of making such compounds, and methods of using such compounds for the treatment or prophylaxis of HIV infection and certain cancers.

SMALL MOLECULES FOR TREATING CANCER, INHIBITING CHEMOKINE ACTIVITY AND/OR INDUCING CELL DEATH
20240002347 · 2024-01-04 · ·

Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or in treating cancer, are provided herein. The compounds are collectively represented by Formulae Ia or Ib:

##STR00001##

wherein A, B, D, E, G and R.sub.1-R.sub.5 are as defined in the specification, with one or more of D, E and G, preferably E, is hydroxy.

SMALL MOLECULES FOR TREATING CANCER, INHIBITING CHEMOKINE ACTIVITY AND/OR INDUCING CELL DEATH
20240002347 · 2024-01-04 · ·

Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or in treating cancer, are provided herein. The compounds are collectively represented by Formulae Ia or Ib:

##STR00001##

wherein A, B, D, E, G and R.sub.1-R.sub.5 are as defined in the specification, with one or more of D, E and G, preferably E, is hydroxy.