Msd K.k.

Banyu Pharmaceutical Co. Ltd

Tsuyoshi Nagase

Nagaaki Sato

Akio Kanatani

Toshiyuki Takahashi

Shigeru Tokita

Takahide Sasaki

Shiho Ishikawa

Keita Nagai

Makoto Ando

Hidekazu Takahashi

Takashi Mizutani

Toshihiro Wada

Makoto Jitsuoka

Daisuke Tsukahara

[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

[Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; Rrepresents Calkyl, Ccycloalkyl, or the like; Rrepresents aryl or heteroaryl; Rrepresents a hydrogen atom, Calkyl, or the like; and M, M, M, and Mindependently represent a hydrogen atom, Calkyl, or the like, or M, together with M, M, or M, forms &#x2014;CH&#x2014; or the like.

3-substituted sulfonyl piperidine derivative

[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

[PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms &#x2014;CH2-CH2- or the like, or M4 together with M2 or M3 forms &#x2014;CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one &#x2014;CH2- or &#x2014;CH2-CH2- group is formed thereamong.

4-sulfonylpiperidine 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

[Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2,Y represents CRor N, Rrepresents a Calkyl, Ccycloalkyl, etc., Rrepresents phenyl or a heteroaryl, etc., Rand Reach independently represent a hydrogen atom, a Calkyl, etc., M, M, M, and Meach independently represent a hydrogen atom, a Calkyl, etc.]

Sulfonyl-substituted 6-membered ring 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

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

A compound of the formula (I): (wherein Arand Arare independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl;

N-substituted-2-oxodihydropyridine derivatives

A compound of the formula (I): wherein Ris hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; Rand Rare each independently hydrogen, halogen or halo-lower alkyl; and Rand Rare each independently hydrogen or halogen, is useful as a pharmaceutical composition for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, etc., nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

Pyridone derivatives

A compound of the formula (I):(wherein Arand Arare independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; Rand Rare independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R, Rand Rare independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.

Growing community of inventors

Tokushima, Japan

Tsuyoshi Nagase