The present invention provides a novel and improved process for the preparation of Crisaborole of Formula (I) and its pharmaceutically acceptable salts. The present invention also provides novel intermediates and process for the preparation of intermediates used in the preparation of Crisaborole. The present invention also provides an improved process for the preparation of Crisaborole and pharmaceutically acceptable salts thereof, that is commercially and industrially scalable.

The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Novel polymorphic forms of tavaborole, Form A and Form B, and methods of making same are disclosed. Methods are disclosed for the manufacture of the novel polymorphic Forms A and B. Methods include dissolving tavaborole in a pharmaceutically acceptable solvent to obtain a mixture, heating the mixture until a clear solution is obtained, cooling the clear solution, stirring the clear solution to obtain a crystalline product, filtering the crystalline product, and drying the crystalline product to obtain the pharmaceutically acceptable crystalline form of tavaborole. Pharmaceutical composition are disclosed including a pharmaceutically acceptable crystalline form of tavaborole Form A and/or Form B.

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The present invention relates to four crystal forms of crisaborole in free form and the preparation method thereof. The present invention also relates to the pharmaceutical composition containing the crystal forms and the use thereof.

##STR00001##

Disclosed herein are kinase inhibitor compounds having the structure (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R.sup.1, R.sup.2, X, L, Q, and Y are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

##STR00001##

The present invention relates to cyclopropyl-(hetero)aryl substituted ethylsulphonyl-pyridine derivatives of formula (I)

##STR00001##

wherein the variables are as defined in the description and in the claims, which can be used as antiparasitic agents for the treatment, prevention and/or control of parasitic infections and/or infestations in animals.

An intermediate is provided herein, and it has the structure shown in the formula (1) as follows:

##STR00001##

formula (1). In the formula (1), R.sub.1 is —Cl, —Br, —I, —OSO.sub.2CF.sub.3, —B(OH).sub.2, or

##STR00002##

R.sub.2 is —F, —.sup.18F, —Cl, —Br, —I, —SnMe.sub.3, —SnBu.sub.3, —B(OH).sub.2, or

##STR00003##

and A is a chiral auxiliary.

Borylated Amino Acid (“BAA”) compositions and methods of making BAAs are disclosed herein. Consequently, the BAAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders and other disease by utilizing a Neutron Capture Therapy modality.