Teijin Limited

Yoshiyuki Sawai

Yoshiyuki Matsumoto

Susumu Takeuchi

Minoru Imai

Akinobu Nakanishi

Kunio Minamizono

Tomonori Yokoyama

Naoki Tsuchiya

Hiroshi Saitoh

Tsuyoshi Mizuno

Tomohide Ida

The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides 4,4-(disubstituted)piperidine derivatives represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C-Calkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis. 

4,4-disubstituted piperidine derivatives having CCR3 antagonism

The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C-Calkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis. 

Piperidine derivatives having CCR3 antagonism

The present invention is 3,4-disubstituted-benzo[b]thiophene derivatives represented by general formula (I) and processes for preparing compounds represented by general formula (V) from compounds represented by general formula (IV), preparing a mixture of compounds represented by the following formula (II) and the following formula (III) and preparing the benzo[b]thiophene derivatives represented by the above formula (I):wherein, Rand Rrepresent each a halogen atom, a trihalomethyl group, a Calkyl group or a Calkoxy group; X represents a hydroxy group or a halogen atom; Rand Rrepresent each a hydrogen or a halogen atom, a trihalomethyl group, a Calkyl group or a Calkoxy group; and Rrepresents a Calkyl group or a trifluoromethyl group.

Benzo[b]thiophene derivatives and process for preparing the same

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Tokyo, Japan

Yoshiyuki Sawai