Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Hiroshi Imoto

Yu Momose

Hiroyuki Odaka

Hiroyuki Kimura

Junichi Sakamoto

Masaki Seto

Makoto Kamata

Takahiro Sugimoto

Toshihiro Imaeda

Taiji Asami

Yuya Oguro

Yasuyoshi Arikawa

Tsuyoshi Maekawa

Naoki Nishizawa

Taku Kamei

Ikuo Fujimori

Jinichi Yonemori

Mark Allan Wolf

Masahiro Kamaura

Ayumu Niida

Mack Flinspach

Kentaro Rikimaru

Tomohiro Ohashi

Mari Adachi

Yoko Kanematsu

Abhijit Suresh Bhat

Derek Cecil Cole

Nick Scorah

Yoshiaki Horiguchi

Goushi Nishida

Takashi Miki

The present disclosure provides GIP receptor agonist peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and/or prevention of diabetes, obesity, emesis, or a symptom or condition associated with diabetes, obesity, or emesis. Specifically, a GIP receptor agonist peptide containing a sequence represented by the formula (I) or a salt thereof, and a medicament comprising the same are provided. Formula I: P-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-A40-A41-P(SEQ ID NO: 4), or a salt thereof, wherein each symbol is as defined herein, with the proviso that the GIP receptor agonist peptide does not have an amino acid sequence as provided in SEQ ID NOs: 328-893.

GIP receptor agonist peptide compounds and uses thereof

The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Heterocyclic compound

A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein

Fused heterocyclic ring compound

A compound represented by the formula wherein R, R, Rand Rare the same or different and each is a hydrogen atom or a substituent; one of Rand Ris a hydrogen atom and the other is a group represented by the formula: &#x2014;C(&#x2550;X)&#x2014;Rwherein X is N&#x2014;O&#x2014;Ror N&#x2014;NH&#x2014;Rwherein Rand Rare the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and Ris a hydrogen atom or a substituent, and the like and a salt thereof have a superior I&#x3ba;B kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.

6-azaindole compound

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

To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance. A compound represented by the formula: wherein Ris an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, &#x2014;CO&#x2014;, &#x2014;CH(OH)&#x2014; or a group represented by &#x2014;NR&#x2014; wherein Ris a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, &#x2014;SO&#x2014;, &#x2014;SO&#x2014; or a group represented by &#x2014;NR&#x2014; wherein Ris a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; Ris a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; Ris a hydroxy group, OR(Ris an optionally substituted hydrocarbon group.) or NRR(Rand Rare the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or Rand Rcombine together to form a ring); Rand Rare the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein Rmay form a ring with R; provided that when Ris a ethoxymethyl, a Calkyl, phenyl or p-methoxyphenyl and q=m=0, Ris NRR; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methyl pyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof.

Oxyiminoalkanoic acid derivatives

Crystals of (E)-4-&lsqb;4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino&rsqb;-4-phenylbutyric acid (provided that crystals having a melting point of 126&deg; C. to 127&deg; C. are excluded), which have an excellent anti-diabetic action.

Crystals of an oxyiminoalkanoic acid derivative and their use as antidiabetics

This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.

Oxyiminoalkanoic acid derivatives with hypoglycemic and hypolipidemic activity

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Kusatsu, Japan

Hiroshi Imoto