Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.

We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension.

A Short Introduction to Intellectual Property Rights.

Intellectual property (IP) is a term that describes a number of distinct types of intangible assets. IP protection allows a rightsholder to exclude others from interfering with or using the property right in specified ways. The main forms of IP are patents, copyrights, trademarks, and trade secrets. Each type of IP protection is different, varying in the subject matter that can be covered, timeframe of protection, and total expense. Although some inventions may be covered by multiple types of IP protection, it is important to consider a number of business and legal factors before selecting the best protection strategy. Some technologies require strong IP protection to commercialize, but unnecessary costs can derail bringing a product to market. IP departments of organizations weigh these various considerations and perform essential IP protection functions. This primer introduces researchers to the main forms of IP and its legal aspects.

Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.

We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for other known KSP inhibitors.