This disclosure provides functional templates that direct Pd to functionalize multiple CH bonds in polycyclic aza-arenes such as quinolines and related heterocycles at locations that are difficult to isolate and reach for substitution. Herein disclosed are two conceptually distinct directing templates (T) that enable site-selective C6 and C7-H activation of polycyclic aza-arenes. These catalytic pyridine-based templates recruit the aza-arene substrate through N-coordination, enabling the directing arm to deliver the catalyst and precisely activate remote and adjacent C6 or C7-H bond (FIG. 1d). In parallel, we discovered that the use of a simple and readily prepared template chaperone (TC) can turn over the directing template, allowing it to be used catalytically for the first time. Notably, chiral recognition is vital in the granular discrimination between competing C3 and C7-H bonds when the differentiation via distance and geometry is insufficient. Thus, precise recognition of a directing template's distance, geometry and chirality now enables the iterative CH editing of quinoline and related pharmacophores at any desired site and order. The methods disclosed herein can also be used for diverse and late-stage modification of heterocycle-based drug molecules and pharmacophores.

A compound is provided which has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The compound relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by Formula (I) or a pharmacologically acceptable salt thereof. The compound or a pharmacologically acceptable salt thereof have antagonist activity against a thyroid-stimulating hormone receptor and is useful as a therapeutic agent for thyroid-related diseases, for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer.

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A compound is provided which has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The compound relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by Formula (I) or a pharmacologically acceptable salt thereof. The compound or a pharmacologically acceptable salt thereof have antagonist activity against a thyroid-stimulating hormone receptor and is useful as a therapeutic agent for thyroid-related diseases, for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer.

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