Banyu Pharmaceutical Co. Ltd

Msd K.k.

Nissan Chemical Industries Limited

Taisho Pharmaceutical Co., Ltd.

Nagaaki Sato

Hiroaki Tanaka

Tsuyoshi Nagase

Akio Kanatani

Shigeru Tokita

Makoto Jitsuoka

Keita Nagai

Shiho Ishikawa

Daisuke Tsukahara

Takashi Mizutani

Makoto Ando

Takehiro Fukami

Toshiyuki Takahashi

Yasuyuki Ishii

Akane Ishihara

Hajime Asanuma

Osamu Okamoto

Hirofumi Ota

Shoichi Kuroda

Hidekazu Takahashi

Tomomichi Chonan

Takumi Okada

Yudai Imai

Shigetada Sasako

Takanori Kawaguchi

Keiko Fusegi

Masahiro Bohno

Seishi Ishiyama

Shin Itoh

Toshihiro Wada

Norikazu Ohtake

Takahiro Oi

Keishi Hayashi

Takahide Sasaki

Yoshihisa Shirasaki

Noriko Saito

Souichi Monma

Tsuyoshi Busujima

Rui Jibiki

Kengo Watatani

Kanako Iwakiri

Marie Mizutani

This 2-pyridone compound represented by formula [1] or a tautomer of said compound, or a pharmaceutically acceptable salt of said compound or said tautomer, or a solvate of said compound or the like has a superior GK-activating effect and is useful as a pharmaceutical. 

2-pyridone compound

There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein wherein

Nitrogen-containing condensed heterocyclic compound

A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1],the ring represented by A represents a benzene ring or a pyridine ring,X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, andW represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)},a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.

2-pyridone compounds

[Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a Calkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a Calkyl, etc.; A, A, Aand Aeach independently represent CH or N].

Long-chain fatty acyl elongase inhibitor comprising arylsulfonyl derivative as active ingredient

[PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein Rrepresents optionally halogenated Calkyl, etc.; Rrepresents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents Calkylene, etc. and R represents Calkyl, etc.); Rrepresents hydrogen, Calkyl, etc.; X represents &#x2014;O&#x2014;, &#x2014;NH&#x2014;, etc.; and Y, Y, Y, and Yeach independently represents &#x2014;CH&#x2014;, &#x2014;N&#x2014;, etc.].

Benzoxazinone derivative

The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, Xis a nitrogen atom, sulfur atom or oxygen atom, Ris a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, Rand Rare amino groups or alkylamino groups, and Xis represented by formula (II): (where Rand Rare lower alkyl groups, and n is an integer from 2 to 4).]

Fused ring 4-oxopyrimidine derivative

Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof.  This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; Xrepresents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; Xrepresents a group represented by the following formula (II): (wherein Rand Rrespectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X-Xrespectively represent &#x2014;CH&#x2014;, a nitrogen atom or the like. 

Benzoxathiin derivative

A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents &#x2014;O&#x2014; or the like, B represents &#x2014;C(O)&#x2014; or the like, D represent &#x2014;(CH)m-, &#x2014;O&#x2014; or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R, Rand Rindependently represent a lower alkyl group or the like]. 

Aza-substituted spiro derivatives

Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.

Piperidine derivative

A compound represented by the general formula (I-a): [wherein R1and R2each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4and R5each means lower alkyl, lower cycloalkyl, etc. or R4and R5are bonded to each other to form lower cycloalkylidene; and R6means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.

Indoledione derivative

A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent &#x2014;C(O)&#x2014;, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein Rrepresents a lower alkyl, etc; and Rand Reach independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.

Carbamoyl-substituted spiro derivative

This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein Rrepresents a lower alkyl group et al; Rand Rare same and different and represents hydrogen atm et al; Rrepresents the substituent of the formula (II) et al; Xrepresents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.

Quinazoline derivative

The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.

Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone

Compounds represented by the general formula (I): wherein Arand Arare each aryl or heteroaryl; Ris lower cycloalkyl, &#x2014;Ar, or a group of the general formula (a), (b) or (c): and Rand Rare each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when Rand Rare simultaneously hydrogen, Ar, Arand Rdo not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.

Imidazoline compounds

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Tsukuba, Japan

Nagaaki Sato