Banyu Pharmaceutical Co. Ltd

Akane Ishihara

Akio Kanatani

Takehiro Fukami

Yasuyuki Ishii

Toshihiro Sakamoto

Toshiyuki Takahashi

Yuji Haga

Takahiro Itoh

Nagaaki Sato

Osamu Okamoto

Makoto Jitsuoka

Minoru Moriya

Keita Nagai

Hisashi Iwaasa

Kazuhiko Takahashi

Hiraku Itadani

Hidehito Kotani

Takao Suzuki

Satoshi Mashiko

Hiromitsu Araki

Masato Chiba

This invention relates to a benzimidazole derivative of the general formula [I] [wherein B, B, and Brepresent hydrogen atom or lower alkyl; Rand Rare same or different and represent lower alkyl, etc.; Rand Rrepresent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.

Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient

In the examination of obesity or leanness, the examination is based on the expression level of the MCP-1 gene or the MCP-1 protein in a tissue or cell analyte, or on the polymorphism in the gene. In the evaluation of compounds, including screening for therapeutic agents for obesity or leanness, the properties of the MCP-1 gene or the MCP-1 protein are utilized to carry out the evaluation.

Method for examining obesity or leanness

This invention provides 2-aminoquinoline derivatives represented by a general formula [I] 

2-aminoquinoline derivatives

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

Compounds represented by the general formula (I) wherein Arrepresents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.

Spiro compounds

Imidazonline compounds

The present invention is directed to novel spiro compounds useful as neuropeptide Y receptor antagonists.

Spiro compounds of the general formula (I):

Growing community of inventors

Tsukuba, Japan

Akane Ishihara