Academic drug discovery is a vital component to current drug discovery and development environments. In this study, we investigated 798 drug discovery projects that took place between 1991 and 2015 at 36 academic institutions in the United States. The observed success rates of academic drug discovery and development were 75% at phase I, 50% at phase II, 59% at phase III, and 88% at the new drug application/biologics license application (NDA/BLA) phase. These results were similar to the corresponding success rates of the pharmaceutical industry. Collaboration between academic institutions and the pharmaceutical industry seemed more important at later stages than earlier ones; all projects that succeeded at phase III or the NDA/BLA stage involved academic‐industrial collaboration. Many academic research projects involved neoplasms and infectious diseases, and were focused on small molecules and biologics. The success rates and possible effects of academic‐industrial collaboration seemed to vary depending on disease domains and drug modalities.

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The renin−angiotensin−aldosterone system (RAAS) plays a key role in the regulation of blood pressure. Renin, the first and rate-limiting enzyme of the RAAS, is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. Therefore, various direct renin inhibitors (DRIs) have been researched over recent decades; however, most exhibited poor pharmacokinetics and oral bioavailability due to the peptidomimetic or nonpeptidomimetic structures with a molecular weight (MW) of >600, and only aliskiren is approved. This study introduces a novel class of DRIs comprised of a 2-carbamoyl morpholine scaffold. These compounds have a nonpeptidomimetic structure and a MW of <500. The representative compound 26 was highly potent despite not occupying S1′−S2′ sites or the opened flap region used by other DRIs and exerted a significant antihypertensive efficacy via oral administration on double transgenic mice carrying both the human angiotensinogen and the human renin genes.

The usefulness of (1-nosyl-5-nitroindol-3-yl)methyl esters as a novel protective group for carboxylic acid is fully demonstrated. The novel protective group is stable under a broad range of conditions and can easily be deprotected under the mild conditions used for removal of the nosyl (Ns) group. It is orthogonal to the existing protective groups for carboxylic acids such as t-butyl and allyl esters.

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