Msd K.k.

Banyu Pharmaceutical Co. Ltd

Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Tomoharu Iino

Teruyuki Nishimura

Jun-ichi Eiki

Lihu Yang

Jun Shibata

Takeru Yamakawa

Hideki Jona

Kenji Niiyama

Masanori Asai

Akio Ohno

Toshio Nagase

Norikazu Otake

Mitsuru Ohkubo

Tadashi Shimamura

Keiji Takahashi

Makoto Ishikawa

Takuya Suga

Noriaki Hashimoto

Yoshiyuki Sato

Jun Kusunoki

Hiroshi Nakashima

Hideaki Imamura

Koji Yamada

Norikazu Ohtake

Yasufumi Nagata

Masayuki Nakamura

Hideki Kurihara

Hitomi Watanabe

Seiichi Inamura

Jun-Ichi Eiki

Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; Rrepresents a group of a formula: (wherein Rand Reach independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.;Rrepresents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).

Heteroaryl quinazoline derivatives

The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof. 

Oxotetrahydrofuran-2-yl-benzimidazole derivative

Heteroaryloxy quinazoline derivative

The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases. 

Spirochromanon derivatives

The invention relates to a compound of a general formula (I): wherein Arrepresents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; Rand Reach represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q-N(R)-Q-R; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; Rand Reach represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of &#x2014;N(R)R; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

Substituted spirochromanone derivatives

The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders. 

Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors

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

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

The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.

Spirochromanone derivatives

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.

Aminobenzamide derivative

Isoindole derivatives

Growing community of inventors

Tsukuba, Japan

Tomoharu Iino