Exelixis, Inc.

Disclosed herein are compounds according to Formula I. (I). Compounds according to Formula I inhibit PKMYT1 and are useful for the treatment of cancer and other disease. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

The present disclosure provides 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine compounds of formula (I), which are therapeutically useful as USP1 inhibitors. These compounds are useful in the treatment and/or prevention of diseases and/or disorders responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer. The present disclosure also provides processes for preparation of the compounds and pharmaceutical formulations comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

The subject matter described herein is directed to somatostatin receptor activating compounds, methods of making the compounds, pharmaceutical compositions, and their use in the treatment of diseases associated with somatostatin receptors.

Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.

The present invention relates to processes for the synthetic preparation of c-Met inhibitors of Formula I, or pharmaceutically acceptable salts thereof. The present invention further relates to processes for the synthetic preparation of the c-Met inhibitor, Compound 1, or a pharmaceutically acceptable salt thereof. The present invention also relates to processes for the synthetic preparation of Compound 1·hemifumarate. The invention further relates to large scale processes for the synthetic preparation of the c-Met inhibitor, Compound 1 and Compound 1·hemifumarate.

The present invention relates to crystalline free base of the tyrosine kinase inhibitor, Compound 1. The invention also relates to crystalline salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.

Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.

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 present disclosure provides 5T4 binding agents (e.g., antibodies, including multispecific antibodies such as bispecific antibodies, and antibody-drug conjugates) and uses thereof.

The present disclosure provides 5T4 antibody-drug conjugates and uses thereof.