Banyu Pharmaceutical Co. Ltd

Msd K.k.

Makoto Jitsuoka

Akio Kanatani

Nagaaki Sato

Yuji Haga

Shigeru Tokita

Norikazu Ohtake

Daisuke Tsukahara

Takehiro Fukami

Norikazu Otake

Yasuyuki Ishii

Akane Ishihara

Osamu Okamoto

Akira Naya

Keita Nagai

Takuya Suga

Ryo Yoshimoto

Tsuyoshi Nagase

Minoru Moriya

Hidekazu Takahashi

Shunji Sakuraba

Hiroyuki Kishino

Minoru Kameda

[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

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

Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.

Heteroaryloxy nitrogenous saturated heterocyclic 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

Compound of the formula: (I) [wherein each of X, Xand Xindependently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc. 

The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

Azole derivatives

The present invention provides an imidazopyridine compound represented by formula (I), wherein Rand Reach independently represent a Calkyl group et al; Rand Reach independently represent a hydrogen atom, a methyl et al; Aris a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Arrepresents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents &#x2014;(CH)et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

Imidazopyridine compound

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

The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

Growing community of inventors

Moriya, Japan

Makoto Jitsuoka