Banyu Pharmaceutical Co. Ltd

Other

Msd K.k.

Merck + Co., Inc.

Akio Kanatani

Takehiro Fukami

Yasuyuki Ishii

Yuji Haga

Akane Ishihara

Toshihiro Sakamoto

Takahiro Fukuroda

Toshiyuki Takahashi

Masaki Ihara

Nagaaki Sato

Shigeru Tokita

Minoru Moriya

Takahiro Itoh

Norikazu Otake

Tsuyoshi Nagase

Makoto Jitsuoka

Keita Nagai

Ryo Yoshimoto

Lihu Yang

Ying-Duo Gao

Yoshio Ogino

Douglas J MacNeil

Norikazu Ohtake

Nancy R Morin

Sayaka Mizutani

Akira Naya

Kenji Matsuda

Hisashi Iwaasa

Makoto Ando

Yoshikazu Nagae

Takao Suzuki

Shunji Sakuraba

Osamu Okamoto

Takuya Suga

Hidekazu Takahashi

Shiho Ishikawa

Hiroyuki Kishino

Makoto Ishikawa

Toshiaki Mase

Yoshimi Tsuchiya

Kazuhiko Takahashi

Hiraku Itadani

Takashi Mizutani

Hidehito Kotani

Satoshi Mashiko

Minoru Kameda

Hiromitsu Araki

Masato Chiba

Takayoshi Okabe

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

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

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

Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein Xand Xindependently represent a nitrogen atom or CH; Y represents a specific group; Xrepresents O&#x2014;(CH); Rand Rindependently resent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt. 

Piperidine derivative

The present invention relates to compounds of Formula (I) wherein A, B and C are independently methine, said methine being optionally substituted; D is nitrogen; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted and least two of T, U, V and W are said methine groups; X is &#x2014;N(SOR)&#x2014;, N(COR)&#x2014; or &#x2014;CO&#x2014;; Y is C(R)(R)&#x2014;, &#x2014;O&#x2014; or &#x2014;N(R) and a pharmaceutically acceptable salt, ester or N-oxide derivative thereof.

Benzimidazole derivatives

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

The invention provides pyridone derivatives represented by a general formula (I) 

Pyridone derivative

The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: 

Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient

The present invention relates to compounds of the general formula (I):   The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.

Sulfonamide derivatives

The present invention relates to a compound of the formula (I): (wherein A,,and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is &#x2014;N(SOR)&#x2014;, &#x2014;N(COR)&#x2014; or &#x2014;CO&#x2014;; Y is &#x2014;C(R)(R)&#x2014;, &#x2014;O&#x2014; or &#x2014;N(R)&#x2014;, provided that the compound (I) when E is nitrogen, n is 0, X is &#x2014;CO&#x2014;, and Y is &#x2014;O&#x2014; is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY.

The invention provides a compound or its pharmaceutically-acceptable salt of formula wherein Ais a hydrogen, etc.; j and k are 0 or 1;is a double bond, etc.;is a double bond, etc.;one of Wand Wis E&#x2014;O&#x2014;W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1): which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.

Nitrogenous fused heteroaromatic ring 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

Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein Xand Xindependently represent a nitrogen atom or CH; Y represents a specific group; Xrepresents O&#x2014;(CH); Rand Rindependently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt. 

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Tsukuba, Japan

Akio Kanatani