Astellas Pharma Gmbh

Cytokinetics, Inc.

Kayoko Mihara

Bradley Paul Morgan

Hiroaki Tanaka

Pu-Ping Lu

Fady Malik

Luke W Ashcraft

Takashi Kamikubo

Scott E Collibee

Masanori Miura

Jeffrey Warrington

Tomoyuki Saito

Susumu Yamaki

Ippei Sato

Yuji Matsushima

Yasuhiro Shiina

Marc Andrew Garard

Hiroshi Kiyohara

Munemichi Ohe

Seiji Yoshimura

Noriyuki Kawano

Takanori Koike

Hideyuki Watanabe

Nobuyuki Shiraishi

Ryosuke Munakata

Hiroaki Hoshii

Daisuke Sasuga

Hiroki Fukudome

Tomoaki Kawano

Scott Emile Collibee

Jeffrey Michael Warrington

Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

Tetrahydroisoquinoline derivatives

[Problem] A compound, which can be used for preventing or treating diseases, in which 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with &#x2014;O&#x2014; (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11&#x3b2;-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Triazole derivative or salt thereof

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Tokyo, Japan

Kayoko Mihara