The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

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The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

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The invention discloses a compound with the following formula (I), wherein, K is selected from: cycloalkyl ##STR00001##
and halo alkyl ##STR00002##
or NR6. The invention also discloses a tyrosine kinase inhibitor containing the above compound and the use of the compound in preparing drugs for treating cancers. The tyrosine kinase inhibitor of the invention can inhibit the bioactivity of multiple signal conduction kinases such as C-MET, VEGF, KDR, etc., can effectively inhibit cell proliferation and has favorable therapeutic effects on various diseases such as cancer. In particular, the present invention has significant therapeutic effects especially on lung cancer, gastric cancer, ovarian cancer, malignant glioma, etc., and has a very broad application prospect. ##STR00003##

The invention discloses a compound with the following formula (I), wherein, K is selected from: cycloalkyl ##STR00001##
and halo alkyl ##STR00002##
or NR6. The invention also discloses a tyrosine kinase inhibitor containing the above compound and the use of the compound in preparing drugs for treating cancers. The tyrosine kinase inhibitor of the invention can inhibit the bioactivity of multiple signal conduction kinases such as C-MET, VEGF, KDR, etc., can effectively inhibit cell proliferation and has favorable therapeutic effects on various diseases such as cancer. In particular, the present invention has significant therapeutic effects especially on lung cancer, gastric cancer, ovarian cancer, malignant glioma, etc., and has a very broad application prospect. ##STR00003##

Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

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Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

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An amine compound serving as a semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, and an application thereof in medicines that can be used for treating inflammation and/or inflammation related diseases, diabetes and/or a disease related diabetes, psychiatric disorder, ischemic disease, vascular disease, fibrosis, or tissue transplant rejection.

The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), 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 thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), 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 thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

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:

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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.