Abstract:
The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms.
Abstract:
The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same. In certain embodiments, the present invention provides pharmaceutical formulations comprising provided compounds. In certain embodiments, the present invention provides a method of decreasing enzymatic activity of a Tec kinase family member. In some embodiments, such methods include contacting a Tec kinase family member with an effective amount of a Tec kinase family member inhibitor. In certain embodiments, the present invention provides a method of treating a disorder responsive to Tec kinase family inhibition in a subject in need thereof.
Abstract:
The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
Abstract:
Biaryl-substituted tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.
Abstract:
Provided herein are light protective pharmaceutical packages for enantiomerically pme (+)-l,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylarnino)-l-pyrrolidinyl]-4-oxo-l-(2- thiazolyl)-l,8-naphthyridine-3-carboxylic acid. In certain embodiments, the pharmaceutical packages comprise a glass vial containing SNS-595 drug product within a secondary container.
Abstract:
Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.
Abstract:
The present invention is directed to Aurora constructs that are useful for structural and functional studies of Aurora. Specifically, engineered Aurora enzymes are provided, along with polynucleotides encoding said enzymes, vectors comprising said polynucleotides, and host cells comprising the vectors. In addition, a process of using the engineered Aurora enzymes to identify Aurora modulators is provided.
Abstract:
The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the beta-secretase enzyme is involved.
Abstract:
The present invention is directed to engineered polypeptides having BACE activity. In certain embodiments, the polypeptides also comprise an engineered cleavage site. Also provided are polypeptides comprising a prodomain, an engineered cleavage site, and a protease domain; the polypeptides are properly folded and are cleaved at the engineered cleavage site in vitro, producing homogeneous preparations of purified protease having BACE activity. The invention further pertains to nucleic acids, expression vectors, and host cells comprising the expression vectors for making the engineered polypeptides.
Abstract:
The present invention relates to SNS-595 and methods of treating cancer using the same. Figure 1 depicts the plasma concentrations of SNS-595 over time among the various patient cohorts.