Astellas Pharma Gmbh

Cytokinetics, Inc.

Yuji Matsushima

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

Yasuhiro Shiina

Kayoko Mihara

Marc Andrew Garard

Hiroshi Kiyohara

Munemichi Ohe

Hisao Hamaguchi

Fusako Nishigaki

Satoshi Aoki

Hiroshi Nagata

Atsushi Akahane

Tadashi Terasaka

Yoshinori Okamoto

Hirokazu Kubota

Takeshi Hondo

Shinya Nagashima

Toru Kontani

Minoru Kameda

Takeshi Terasawa

Shugo Honda

Yukihito Sugano

Hiroyuki Usuda

Tadatsura Koshika

Satoshi Yonishi

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] To provide a compound useful as a novel agent which is excellent in preventing and/or treating cannabinoid receptor type 2-related diseases, based on agonist action on a cannabinoid receptor type 2 [Means for Solution] The present inventors conducted thorough investigation regarding compounds having agonist action on a cannabinoid receptor type 2. They confirmed that the fused ring pyridine compound of the present invention has excellent agonist action on the cannabinoid receptor type 2, thereby completing the present invention. The fused ring pyridine compound of the present invention has agonist action on the cannabinoid receptor type 2, and can be used as an agent for preventing and/or treating cannabinoid receptor type 2-related diseases, for example, inflammatory diseases and pain.

Fused ring pyridine compound

A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.

Pyrimidine compound

[PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic Mreceptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [MEANS For SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic Mreceptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic Mreceptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic Mreceptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

Aza-bridged-ring compound

A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

Pyrazine derivatives and pharmaceutical use thereof

Growing community of inventors

Tokyo, Japan

Yuji Matsushima