Banyu Pharmaceutical Co. Ltd

Takahiro Itoh

Akio Kanatani

Takehiro Fukami

Toshihiro Sakamoto

Toshiyuki Takahashi

Yuji Haga

Yasuyuki Ishii

Akane Ishihara

Toshiaki Mase

Atsushi Akao

Masato Chiba

Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]: [III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]: [II] or a salt thereof in the presence of a palladium compound such as Pd(dba), a base such as i-PrNEt and a phosphorus compound represented by the following formula [AA].

Method for producing thioether compound

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

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

Spiro compounds of the general formula (I):

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Okazaki, Japan

Takahiro Itoh