Provided are inhibitors of sphingosine kinase Type I that are useful in a number of applications, indications and diseases, as well as for monitoring pharmacokinetics and patient management. These compounds are applicable to treating tumors of the central nervous system, such as glioblastoma multiforme (GBM).

The present disclosure provides boron-containing diacylhydrazines having Formula I: ##STR00001##
and the pharmaceutically acceptable salts and solvates thereof, wherein A, R.sup.4, and R.sup.5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.

The present disclosure provides boron-containing diacylhydrazines having Formula I: ##STR00001##
and the pharmaceutically acceptable salts and solvates thereof, wherein A, R.sup.4, and R.sup.5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.

The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.

The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.

A novel method for synthesizing NCA compounds. Also, a new use of a peptide coupling agent. The method makes it possible to obtain NCA compounds from ?-amino-acids, under mild and non-racemic reaction conditions, and in the absence of constraining reagents of use, such as phosgene, which may lead to the formation of undesirable by-products.

A novel method for synthesizing NCA compounds. Also, a new use of a peptide coupling agent. The method makes it possible to obtain NCA compounds from ?-amino-acids, under mild and non-racemic reaction conditions, and in the absence of constraining reagents of use, such as phosgene, which may lead to the formation of undesirable by-products.

Provided are inhibitors of sphingosine kinase Type I and their use in the treatment of asthma, among other indications and diseases.

Provided are inhibitors of sphingosine kinase Type I and their use in the treatment of asthma, among other indications and diseases.

The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.