Banyu Pharmaceutical Co. Ltd

Msd K.k.

Teruyuki Nishimura

Hiroyuki Takahashi

Jun-ichi Eiki

Tomoharu Iino

Fumiko Sakai

Yasuhiro Sasaki

Yoshio Ogino

Keiji Takahashi

Makoto Bamba

Noriaki Hashimoto

Hitomi Watanabe

Keisuke Arakawa

Hiroshi Nakashima

Katsumasa Nonoshita

Makoto Ishikawa

Morihiro Mitsuya

Toshio Nagase

Yoshiyuki Sato

Tadashi Shimamura

Masanori Asai

Yasufumi Nagata

Daisuke Tsukahara

Yufu Sagara

Yoshikazu Nagae

Yuichi Sugimoto

Chisato Nakama

Jun-Ichi Eiki

The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein Xrepresents a nitrogen atom, sulfur atom, oxygen atom or the like; Rrepresents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; Rand Rare the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.

2-pyridinecarboxamide derivatives

The present invention relates to a compound represented by formula (I): (wherein R, R, Rand Reach independently represent a hydrogen or halogen atom; Rand Reach independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof. 

Isoindolin-1-one derivative

Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity.  Rand Reach independently represent a lower alkyl group; Xrepresent a group of a formula (II-1): wherein:Rand Reach independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, Rand Rmay form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH), Rand Rmay form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.

2-pyridinecarboxamide derivative having GK-activating effect

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein Xto Xindependently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; Xrepresents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; Rrepresents an aryl or the like; Rrepresents a formyl group or the like; and Rrepresents a &#x2014;Calkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.

Heterocycle-substituted benzimidazole derivative

A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein Rand Rrepresent a hydrogen, etc.; Rrepresents a hydrogen atom, a halogen atom, etc.; Reach independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); Rand Reach represent a hydrogen atom, a lower alkyl group, etc.; X, X, Xand Xeach independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group &#x3b2;; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of Xto Xare carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.

Aryloxy-substituted benzimidazole derivatives

Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, Rrepresents an aryl or the like; Rrepresents an aryl or the like; Rrepresents a formyl or the like, Rrepresents a Calkyl or the like; Rrepresents a hydrogen atom or the like; Zrepresents &#x2014;O&#x2014; or the like; Zrepresents &#x2014;O&#x2014; or the like; Y-Yrespectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.

2-Heterocycle-substituted indole derivatives for treating diabetes and associated conditions

Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein Xrepresents oxygen, etc., Xrepresents oxygen, etc., Rrepresents a group on Ring A such as alkylsulfonyl, etc., Rrepresents C3-7 cyclic alkyl optionally substituted with a halogen, etc., Rrepresents a substituent on Ring B such as lower alkyl, etc., formula (II):[Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III):[Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by Rabove, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C&#x2550;N bond with the nitrogen atom of the ring],as well as their pharmaceutically acceptable salts.

Heteroarylcarbamoylbenzene derivatives

A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; (in the formula, X represents a carbon atom or a nitrogen atom); Rrepresents an aryl, etc.; Rrepresents a hydroxy, etc.; Rrepresents a &#x2014;Calkyl, etc.; Rrepresents a &#x2014;Calkyl, etc.; Xrepresents &#x2014;O&#x2014;, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

2-heteroaryl-substituted benzimidazole derivative

The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; Ris an optionally substituted five to six-membered heteroaryl group, etc.; Ris hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

Substituted quinazoline or pyridopyrimidine derivative

2-pyridine carboxamide derivatives

Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.

Heteroarylcarbamoylbenzene derivative

This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R; The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.

Growing community of inventors

Ushiku, Japan

Teruyuki Nishimura