Patent classifications
C07D215/22
HETEROARYL COMPOUNDS FOR THE TREATMENT OF PAIN
- Mark Thomas MILLER ,
- Dennis James HURLEY ,
- Timothy Donald Neubert ,
- Elamprakash Nesan Savariar ,
- Urvi Patel ,
- Sara Sabina Hadida Ruah ,
- Jason McCartney ,
- Jinglan Zhou ,
- Robert Martin Demoret ,
- Roman Askatovich Valiulin ,
- Alexander Frederik Kintzer ,
- Peter Webb ,
- David Robert Slochower ,
- Kathleen Aertgeerts ,
- Elizabeth Mary Beck ,
- Ronald Marcellus Alphonsus Knegtel ,
- Ewa Iwona Chudyk ,
- Joanne Louise Pinder
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
HETEROARYL COMPOUNDS FOR THE TREATMENT OF PAIN
- Mark Thomas MILLER ,
- Dennis James HURLEY ,
- Timothy Donald Neubert ,
- Elamprakash Nesan Savariar ,
- Urvi Patel ,
- Sara Sabina Hadida Ruah ,
- Jason McCartney ,
- Jinglan Zhou ,
- Robert Martin Demoret ,
- Roman Askatovich Valiulin ,
- Alexander Frederik Kintzer ,
- Peter Webb ,
- David Robert Slochower ,
- Kathleen Aertgeerts ,
- Elizabeth Mary Beck ,
- Ronald Marcellus Alphonsus Knegtel ,
- Ewa Iwona Chudyk ,
- Joanne Louise Pinder
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
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
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-ffuorophenyl)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
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-ffuorophenyl)cyclopropane-1,1-dicarboxamide.
Methods of using c-Met modulators
Methods of treating cancer by administering a compound of Formula I, ##STR00001##
or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R.sup.1 is halo; R.sup.2 is halo; and Q is CH or N.
Crystalline Form of Compound, Method for Preparing the Same, Pharmaceutical Composition and Use
The present disclosure relates to the field of pharmaceutical technology, providing three crystalline forms, i.e., a crystalline form AB, a crystalline form M and a crystalline form F, of the compound 6-[[4-[2-fluoro-4-[[1-[(4-fluorophenyl)aminoformyl]cyclopropanecarbonyl]-amino]phenoxy]-6-methoxy-7-quinolyl]oxy]hexanoic acid for treatment of diseases related to protein kinases AXL and/or VEGFR2. The present disclosure also provides methods for preparing these three crystalline forms and pharmaceutical compositions comprising these three crystalline forms. The crystalline form AB, the crystalline form M and the crystalline form F of the present disclosure all have good chemical stability, and the preparation processes of the three crystalline forms of the present disclosure are simple for implementation with high product yield and purity, allowing stable and mass production that facilitates promotion and application.
Crystalline Form of Compound, Method for Preparing the Same, Pharmaceutical Composition and Use
The present disclosure relates to the field of pharmaceutical technology, providing three crystalline forms, i.e., a crystalline form AB, a crystalline form M and a crystalline form F, of the compound 6-[[4-[2-fluoro-4-[[1-[(4-fluorophenyl)aminoformyl]cyclopropanecarbonyl]-amino]phenoxy]-6-methoxy-7-quinolyl]oxy]hexanoic acid for treatment of diseases related to protein kinases AXL and/or VEGFR2. The present disclosure also provides methods for preparing these three crystalline forms and pharmaceutical compositions comprising these three crystalline forms. The crystalline form AB, the crystalline form M and the crystalline form F of the present disclosure all have good chemical stability, and the preparation processes of the three crystalline forms of the present disclosure are simple for implementation with high product yield and purity, allowing stable and mass production that facilitates promotion and application.
PROCESS FOR THE PREPARATION OF ARIPIPRAZOLE LAUROXIL
It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric anhydride in the presence of DMAP and a solvent.
##STR00001##
PROCESS FOR THE PREPARATION OF ARIPIPRAZOLE LAUROXIL
It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric anhydride in the presence of DMAP and a solvent.
##STR00001##
Crystalline solid forms of salts of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1, 1-dicarboxamide, processes for making, and methods of use
The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).