Astellas Pharma Gmbh

Cytokinetics, Inc.

Takeda Pharmaceutical Company Limited

Susumu Yamaki

Bradley Paul Morgan

Pu-Ping Lu

Scott E Collibee

Daisuke Suzuki

Hiroaki Tanaka

Fady Malik

Luke W Ashcraft

Takashi Kamikubo

Norio Seki

Masanori Miura

Jeffrey Warrington

Tomoyuki Saito

Ippei Sato

Yuji Matsushima

Kousei Yoshihara

Tomoyoshi Imaizumi

Yasuhiro Shiina

Kayoko Mihara

Marc Andrew Garard

Hiroshi Kiyohara

Munemichi Ohe

Hiroyoshi Yamada

Jiro Fujiyasu

Hisashi Mihara

Takanori Koike

Itsuro Shimada

Kazuyuki Tsuchiya

Wenyue Wang

Tomoaki Abe

Kazushi Watanabe

Takahiro Nigawara

Takuya Makino

Shigeki Kunikawa

Ikumi Kuriwaki

Kazuyuki Kuramoto

Toshio Kurosaki

Keisuke Arakawa

Michinori Akaiwa

Takanobu Araki

Eriko Honjo

Ryuichi Sekioka

Satoshi Sasamura

Yuka Koizumi

Yoshiki Satake

Naoto Katoh

Chris Evans

Makoto Yamasaki

Tomohki Satou

Masashi Shimazaki

Makoto Inoue

Koichi Yonezawa

Yuji Koga

Kazuhiro Yokoyama

Kazuhiko Ohne

Masahiro Neya

Takeshi Hondo

Toru Asano

Yasuharu Urano

Keisuke Matsuura

Osamu Kaneko

Takashi Ogiyama

Shuichirou Kakimoto

Yuka Koike

Jun-ichi Shishikura

Hidetsugu Okada

Scott Emile Collibee

Jeffrey Michael Warrington

Provided herein are compounds of formula (I): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X, X, R, R, R, R, R, and Rare as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.

Bicyclic 1,4-diazepanones and therapeutic uses thereof

Provided herein are compounds of formula (1): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X, X, R, R, R, R, R, and Rare as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.

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] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.

Quinazoline compound

[Problem] To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. [Means for Solution] The present inventors have studied compounds having a trypsin inhibitory activity, and have confirmed that a guanidinobenzoic acid ester compound has a trypsin inhibitory activity, thereby completing the present invention. The guanidinobenzoic acid ester compound of the present invention can be used as an agent for preventing and/or treating kidney diseases (for example, chronic kidney disease, acute glomerulonephritis, acute kidney injury, and the like) as an agent which will substitute low-protein diet therapy, and/or as an agent for preventing and/or treating trypsin-related diseases (for example, chronic pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like).

Guanidinobenzoic acid ester compound

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

Guanidine compound

[Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

Guanidinobenzoic acid compound

Compounds of formula (I) defined herein exhibit VAP-1 inhibitory activity, and as a result, are useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention.

Glycine compound

Provided is a compound useful as an N-type Cachannel blocker. As a result of intensive studies of compounds having an action of blocking N-type Cachannels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Cachannels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.

1-substituted tetrahydroisoquinoline compound

Growing community of inventors

Tokyo, Japan

Susumu Yamaki