C07D215/22

CRYSTALLINE FORM OF FLUVATINIB OR FLUVATINIB METHANESULFONATE AND PREPARATION METHOD THEREFOR

Disclosed in the present invention is a crystalline form of fluvatinib or fluvatinib methanesulfonate, and a preparation method therefor. The crystalline form I of the fluvatinib has characteristic diffraction peaks as shown in FIG. 1. The crystalline form of the fluvatinib methanesulfonate may take multiple forms, including seven crystalline forms, forms I-VII, wherein crystalline form III has characteristic diffraction peaks as shown in FIG. 9. Said crystalline forms are suited to manufacturing processes for fluvatinib methanesulfonate formulations.

ISOQUINOLINONE COMPOUND FOR INHIBITING SSAO/VAP-1, AND USE THEREOF

An isoquinolinone compound acts as an inhibitor of semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1), and the use thereof, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be used to prepare a drug for preventing, treating or ameliorating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases in patients, and especially can be used to prepare a drug for preventing, treating or ameliorating non-alcoholic fatty liver diseases in patients.

SELECTIVE NON-CYCLIC NUCLEOTIDE ACTIVATORS FOR THE CAMP SENSOR EPAC1

The invention relates generally to novel EPAC1 activators, such as Formula I and II and the preparation thereof as well as the use of EPAC1 activators disclosed herein as to selectively activate EPAC1 in cells.

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SELECTIVE NON-CYCLIC NUCLEOTIDE ACTIVATORS FOR THE CAMP SENSOR EPAC1

The invention relates generally to novel EPAC1 activators, such as Formula I and II and the preparation thereof as well as the use of EPAC1 activators disclosed herein as to selectively activate EPAC1 in cells.

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SUBSTITUTED AMINOQUINOLONES AS DGKALPHA INHIBITORS FOR IMMUNE ACTIVATION

The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.

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SUBSTITUTED AMINOQUINOLONES AS DGKALPHA INHIBITORS FOR IMMUNE ACTIVATION

The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.

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Notch Inhibitors and Uses Thereof

Disclosed herein, inter alia, are compounds for inhibiting Notch and uses thereof.

Notch Inhibitors and Uses Thereof

Disclosed herein, inter alia, are compounds for inhibiting Notch and uses thereof.

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.

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.