Takeda Pharmaceutical Company Limited

Scohia Pharma, Inc.

Tsuyoshi Maekawa

Hideyuki Igawa

Yu Momose

Hiroyuki Odaka

Hiroyuki Kimura

Nobuyuki Takakura

Shizuo Kasai

Toshitake Kobayashi

Jumpei Aida

Naoyoshi Noguchi

Koji Watanabe

Satoshi Sasaki

Hiroki Sakamoto

Takanobu Kuroita

Minoru Sasaki

Shigemitsu Matsumoto

Hideki Furukawa

Yasufumi Miyamoto

Yasuhiro Hirata

Seiji Miwatashi

Nozomu Sakai

Yuko Hitomi

Yayoi Nakayama

Kouhei Asano

Koji Fuji

Norihito Tokunaga

Kazuaki Takami

Tomohiro Okawa

Keiko Kakegawa

Minoru Yoshida

Akito Shibuya

Jun Kunitomo

Masatoshi Hazama

Ayumu Niida

Hiroshi Imoto

Asato Kina

Tatsuya Ito

Mrinalkanti Kundu

Minoru Ikoma

Tomoko Asakawa

Uttam Khamrai

Toru Kawamura

Ryoma Hara

Hideto Fukushi

A compound represented by the following formula (I): wherein each symbol in the formula is as described herein or a salt thereof has an NRF2 activating activity, and is expected to be useful as a preventive or therapeutic agent for diseases associated with oxidative stress, in particular, hepatic disease (for example, non-alcoholic steatohepatitis (NASH)), cardiovascular disease (for example, heart failure or pulmonary arterial hypertension), lung disease (for example, chronic obstructive pulmonary disease (COPD)), kidney disease (for example, chronic kidney disease (CKD) or acute kidney injury (AKI)), central nervous system disease (for example, Parkinson's disease), mitochondrial disease (for example, Friedreich motor ataxia, mitochondrial myopathy), inflammatory disease (for example, multiple sclerosis (MS), inflammatory bowel disease (IBD)), sickle cell disease, cancer, or the like.

Macrocyclic compound and use thereof

Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.

Aromatic compound

Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy. 

Substituted cyclyl-acetic acid derivatives for the treatment of metabolic disorders

The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.

Benzimidazole derivatives as MCH receptor antagonists

Provided is a novel compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor &#x3b3; agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.

Fused ring compound and use thereof

Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor &#x3b3; agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.

A compound represented by the formula (I): wherein R1 is an oxo group, &#x2550;N&#x2014;R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, &#x2014;CO&#x2014;R8 or &#x2014;O&#x2014;R8', or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=&#x2014;CR3; X1=&#x2014;CR2 or &#x2014;NR2; and X2=&#x2014;CR5 or &#x2014;NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

Substituted pyrimidines and [1,2, 4] triazoles and the use thereof for treating prophylaxis, cardiovascular diseases, metabolic diseases and/or central nervous system diseases

A compound represented by the formula (I):    

Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases

The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NR&#x2014;, &#x2014;CONR&#x2014; or &#x2014;NRCO&#x2014; (Ris a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; Ris an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be &#x2014;O&#x2014;, or a salt thereof.

Agent for preventing or treating neuropathy

The present invention provides a compound represented by the formula: wherein Ris an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is &#x2014;(CH)-Z- or -Z-(CH)&#x2014; (n is an integer of 0 to 8, Zis a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; Ris a hydrogen atom, a cyano group, &#x2014;PO(OR)(OR) (Rand Rare the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and Rand Rare optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic action and a hypolipidemic action, and which is useful as an agent for the prophylaxis or treatment of obesity, diabetes mellitus, hyperlipidemia, impaired glucose tolerance, hypertension and the like.

Five-membered heterocyclic compounds

The present invention relates to a compound represented by the formula wherein Ris an optionally substituted 5-membered heterocyclic group; X is a bond etc.; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond etc.; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is &#x2014;(CH)&#x2014;Z&#x2014; (n is an integer of 0 to 8 and Zis a bond etc.) and the like; ring B is a 5-membered heterocycle optionally further having 1 to 3 substituents; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; Ris &#x2014;OH etc., or a salt thereof. A pharmaceutical composition containing this compound is useful as a prophylactic or therapeutic agent of diseases such as diabetes mellitus and the like.

Five-membered heterocyclic alkanoic acid derivative

An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula wherein Ris an optionally substituted 5-membered aromatic heterocyclic group; X is a bond and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond and the like; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is &#x2014;(CH)-Z-(n is an integer of 1 to 8 and Zis an oxygen atom and the like) and the like; ring B is a pyridine ring optionally further having 1 to 3 substituents, and the like; U is a bond and the like; W is a divalent hydrocarbon group having 1 to 20 carbon atoms; and Ris &#x2014;OH and the like, provided that, when ring B is a benzene ring optionally further having 1 to 3 substituents, U should be a bond, or a salt thereof.

Alkanoic acid derivatives process for their production and use thereof

The present invention provides a retinoid-related receptor (except retinoic acid receptors) function regulating agent comprising a compound represented by the formula: wherein one of Rand Ris an optionally substituted monocyclic aromatic hydrocarbon group or an optionally substituted monocyclic aromatic heterocyclic group containing one heteroatom, and the other is a hydrogen atom and the like; B is a 5- or 6-membered heterocycle (except 1,3-azole); A is an optionally substituted aromatic hydrocarbon group or an optionally substituted aromatic heterocyclic group; and Ris a hydrogen atom and the like, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of diabetes mellitus, hyperlipidemia, impaired glucose tolerance or the like.

Function regulator for retinoid relative receptor

Growing community of inventors

Osaka, Japan

Tsuyoshi Maekawa