Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Fumio Itoh

Hiroshi Banno

Hiroyuki Tawada

Masaki Kawamura

Tetsuya Aono

Shuji Kitamura

Zen-ichi Terashita

Tomohiro Kawamoto

Masuo Yamaoka

Shuji Hinuma

Hiromi Kobayashi

Naoyuki Kanzaki

Hiroshi Akimoto

Keiji Kubo

Hiroyuki Kimura

Tomohiro Kaku

Eiji Kimura

Jun Kunitomo

Morihisa Saitoh

Shogo Marui

Yuji Ishichi

Masafumi Nakao

Taisuke Tawaraishi

Yuji Kawamata

Koichiro Ootsu

Katsuhito Murase

Hiroshi Hosono

Hiroki Iwashita

Hideki Igata

Mitsuru Sasaki

Mariko Hirohashi

For the purpose of providing a GSK-3&#x3b2; inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3&#x3b2;-related pathology or disease, the present invention provides a GSK-3&#x3b2; inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

GSK-3&#x3b2; inhibitor

It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B' represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases. 

Receptor agonists

A JNK inhibitor containing a compound having an isoquinolinone skeleton or a salt thereof, such as a compound represented by the formula wherein ring A and ring B are each an optionally substituted benzene ring, X is &#x2014;O&#x2014;, &#x2014;N&#x2550;, &#x2014;NR&#x2014; or &#x2014;CHR&#x2014;, Ris an acyl group, an optionally esterified or thioesterified carboxyl group, an optionally substituted carbamoyl group or an optionally substituted amino group and the like, a broken line shows a single bond or a double bond, and Ris a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like, and the like.

JNK inhibitor

Novel carbamate derivatives which are useful as drugs because of inhibiting activated blood coagulation factor X and thus exerting an anticoagulant effect. Compounds represented by the formula: wherein Rrepresents a group represented by the formula: (wherein Yrepresents CH&#x2550;CH, etc.), which may be substituted, etc.; the ring A represents an oxo-substituted nitrogen-containing heterocyclic ring which may be further substituted; Rrepresents a hydrogen atom, optionally substituted Calkyl, etc.; Rrepresents optionally substituted Calkyl, etc.; and Z represents an optionally substituted nitrogen containing heterocyclic group, etc., or salts thereof.

Carbamate derivatives, process for producing the same and use thereof

Acylhydrazine derivatives, their production and use

Sulfonamide derivatives, their production and use

Fused ring compounds, process for producing the same and use thereof

Sulfonamide derivatives, processes for producing the same and utilization thereof

Heterocyclic compounds, their production and use

A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.

Pyrrolopyrimidinyalglutaminate derivatives and their use

Growing community of inventors

Toyonaka, Japan

Fumio Itoh