Mitsubishi Tanabe Pharma Corporation

Yasunori Moritani

Yasunori Tsuboi

Mariko Oi

Koichi Tanimoto

Atsushi Sato

Ritsuo Imashiro

Masami Takahashi

Rikako Kono

Hidetoshi Asai

Tsutomu Miyake

Taketoshi Ishii

Chieko Okagaki

Naomitsu Hirano

Akira Oku

Shigeru Furukubu

Kimihiro Shirai

Rikako Towa City Coop 401 Kono

Tsutomu 8-59-601 Motoyamaminami-Machi Miyake

Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein Rand Rare the same or different and each is an optionally substituted aryl group, etc., 

Pyrazolo[1,5-a] pyrimidine compounds as CB1 receptor antagonist

The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein Rand Rare the same or different and an optionally substituted aryl group etc.  

Pyrazolo[1,5-A]pyrimidine compounds

The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which Rand Rare the same or different and each an optionally substituted aryl group etc, Ris hydrogen atom, an alkyl group etc, E is a group of the formula: &#x2014;C(&#x2550;O)&#x2014; or &#x2014;SO&#x2014;, R is a group of the following formula [i], [ii]or [iii] etc: Ring A is (a) a Ccycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, Ris an alkyl group optionally substituted by an alkylthio group, Ris hydrogen atom, an alkyl group etc, one of Rand Ris an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof. 

Pyrazolo[1,5-A] pyrimidine compounds as CB1 receptor antagonist

The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of Rand Ris (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of Rand Ris hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of Rand Rcombine to form oxo group, Ris hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: &#x2014;N(R)&#x2014;, Ris optionally substituted hydrocarbon group or optionally substituted cyclic group, Ris alkyl or alkyloxycarbonylalkyl, provided that Ris not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the Rand Ris hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof. 

Pyrrolidine compound and a process for preparing the same

The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein 

Pyrazole compounds having cannabinoid receptor (CB1) antagonizing activity

The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, Rrepresents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein Rand Rare the same or different, and each represents hydrogen atom, a substituted carbonyl group, a substituted sulfonyl group, an optionally substituted alkyl group, etc., Rrepresents hydrogen atom, etc., Z represents oxygen atom or a group represented by &#x2014;N(R)&#x2014;, Rrepresents hydrogen atom or an alkyl group, etc., Rrepresents hydrogen atom or an alkyl group, etc., or a pharmaceutically acceptable salt thereof. 

Piperidine compounds

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Osaka, Japan

Yasunori Moritani