The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

Formula (I)

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The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

Formula (I)

##STR00001##

Provided is a modifier of a four-membered ring derivative, a preparation method and application thereof. In particular, provided is a compound represented by the general formula (IX-A), a preparation method thereof, a pharmaceutical composition containing the compound, and a use thereof as a G protein-coupled receptor modulator in the treatment or prevention of central nervous system diseases and/or mental diseases. The definition of each substituents in the general formula (IX-A) is same as the definition in the specification.

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The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.

The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.

The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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.

The present invention relates to a process for producing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, including: coupling 4-(4-amino-2-fluorophenoxy)-7-methoxy-N-methylquinoline-6-carboxamide to 2-phenylacetyl isothiocyanate.

The present invention relates to a process for producing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, including: coupling 4-(4-amino-2-fluorophenoxy)-7-methoxy-N-methylquinoline-6-carboxamide to 2-phenylacetyl isothiocyanate.