Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Masashi Funatsu

Makoto Takeuchi

Souichirou Kawazoe

Yasuhiro Yonetoku

Akira Toyoshima

Hirokazu Kubota

Jun Ishikawa

Keizo Sugasawa

Yoshinori Okamoto

Hiroyuki Koshio

Fukushi Hirayama

Yuzo Matsumoto

Tsukasa Ishihara

Tomihisa Kawasaki

Keizou Sugasawa

Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning:D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, &#x2014;O-Alk, &#x2014;COOH, &#x2014;COO-Alk and -Hal,n: 0 or 1,B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk,X: &#x2014;NR&#x2014;CRR&#x2014;, &#x2014;CRR&#x2014;NR&#x2014;, &#x2014;NR&#x2014;SO&#x2014;, &#x2014;SO&#x2014;NR&#x2014; or &#x2014;CR&#x2550;CR&#x2014;, andA: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).

Pyrazole derivative

Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning:

The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I)which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.

Pharmaceutical compound comprising a pyrazole derivative and methods of using the same for the treatment of calcium release-activated calcium channel associated diseases

Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: &mdash;CO&mdash;, &mdash;CONH&mdash;, &mdash;CSNH&mdash;, &mdash;SO,&mdash;, &mdash;SO,NH&mdash;, or the like; Y: a bond or alkylene; R,: hydrogen, alkyl, &mdash;Y&mdash;(hetero) aryl, or the like; R,: hydrogen, alkoxy, &mdash;COOH, or the like; R,: amidino or a group capable of being converted into amidino; and R,, R,: each independently hydrogen or lower alkyl.

Hexahydro-1,4-diazepine derivatives or salts thereof

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Ibaraki, Japan

Masashi Funatsu