Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to
address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and …

Leukotriene biosynthesis inhibitors have potential as new therapeutic agents for asthma
and inflammatory diseases. A series of novel substituted 2-cyanoquinolines have been …

Benzylisoquinoline alkaloids (BIAs) represent a large class of plant secondary metabolites,
including pharmaceuticals such as morphine, codeine and their derivatives. Large-scale …

The P2-P3 amide of dipeptide cathepsin K inhibitors can be replaced by the metabolically
stable trifluoroethylamine group. The non-basic nature of the nitrogen allows the important …

Compounds containing a 1-cyanopyrrolidinyl ring were identified as potent and reversible
inhibitors of cathepsins K and L. The original lead compound 1 inhibits cathepsins K and L …

Morphinan alkaloids are the most powerful narcotic analgesics currently used to treat
moderate to severe and chronic pain. The feasibility of morphinan synthesis in recombinant …

The lysosomal cysteine protease cathepsin K is a target for osteoporosis therapy. The aryl-piperazine-containing
cathepsin K inhibitor CRA-013783/L-006235 (1) displays greater than …

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for
treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel …

The therapeutic action of nonsteroidal anti-inflammatory drugs (NSAIDs) is exerted through
the inhibition of prostaglandin G/H synthase (PGHS), which is expressed as two isoenzymes, …

The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI)
led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior …