JP2001518114A - 新規な2−(イミノメチル)アミノフェニル誘導体、その製造、医薬としての用途及びこれを含有する医薬組成物 - Google Patents
新規な2−(イミノメチル)アミノフェニル誘導体、その製造、医薬としての用途及びこれを含有する医薬組成物Info
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- JP2001518114A JP2001518114A JP54510998A JP54510998A JP2001518114A JP 2001518114 A JP2001518114 A JP 2001518114A JP 54510998 A JP54510998 A JP 54510998A JP 54510998 A JP54510998 A JP 54510998A JP 2001518114 A JP2001518114 A JP 2001518114A
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- phenyl
- bis
- dimethylethyl
- methyl
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 一般式(I) 〔式中、 Aは下記の基: (上記の基中、R1とR2は、独立して、水素原子、ハロゲン、OH基、1〜6個の 炭素原子を有する直鎖又は分岐鎖アルキル又はアルコキシ基を表し、R3は水素 原子、1〜6個の炭素原子を有する、直鎖又は分岐鎖アルキル基又は-COR4基を 表し、R4は1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル基を表す)、 又は下記の基: (上記の基中、R3は前記の意義を有する)、又は下記の基: (上記の基中、R5は水素原子、OH基又は1〜6個の炭素原子を有する直鎖又は 分岐鎖アルキル又はアルコキシ基を表す)を表し; Bは1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル基、O、S、Nから 選ばれた1〜4個のヘテロ原子を含有する5又は6員の炭素環式又は複素環式ア リール基、特に、チオフェン、フラン、ピロール又はチアゾール基を表し、上記 アリール基は場合により1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル、 アルケニル又はアルコキシ基から選ばれた1個又はそれ以上の基によって置換さ れていてもよく; Xは-Z1-、-Z1-CO-、-CH=CH-CO-、-Z1-NR3-CO-、-Z1-NR3-CS-、-Z1-NR3-SO2- 又は単結合を表し; Yは-Z2-Q-、ピペラジン、ホモピペラジン、2-メチルピペラジン、2,5-ジメチ ルピペラジン、4-アミノピペリジン、-NR3-Z2-Q-、-NR3-CO-Z2-Q-、-NR3-NH-CO- Z2-、-NH-NH-Z2-、-NR3-O-Z2-、-NR3-SO2-NR3-Z2、-O-Z2-Q-、-O-CO-Z2-Q-又は- S-Z2-Q-基(但し、上記の基中のQは単結合、O-Z3、R3-N-Z3又はS-Z3を表す)から 選ばれる基を表し; Z1、Z2及びZ3は、独立して、単結合又は1〜6個の炭素原子を有する直鎖 又は分岐鎖アルキレン基を表し;好ましくはZ1、Z2及びZ3は、好ましくは-(C H2)m-(mは0〜6の整数である)を表し; R6は水素原子又はOH基を表す〕で表される化合物又は一般式(I)の化合物の塩 (但し、次の式: で表される化合物を除く)。 2. 下記の化合物: - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{4-[(2-チエニル(イミノ )メチル)アミノ]フェニル}ベンズアミド; - 3,5-ビス-(1,1,-ジメチルエチル)-4-ヒドロキシ-N-{4-[[(2-チエニル(イミ ノ)メチル)アミノ]フェニル]メチル}ベンズアミド; - 4-アセトキシ-3,5-ジメトキシ-N-{4-[[(2-チエニル(イミノ)メチル)アミノ ]フェニル]メチル}ベンズアミド; - 3,5-ジメトキシ-4-ヒドロキシ-N-{4-[[(2-チエニル(イミノ)メチル)アミノ ]フェニル]メチル}ベンズアミド; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{4-[2-[(2-チエニル(イ ミノ)メチル)アミノ]フェニル]エチル}ベンズアミド; - 4-アセトキシ-3,5-ジメトキシ-N-{4-[2-[(2-チエニル(イミノ)メチル)アミ ノ]フェニル]エチル}ベンズアミド; - 3,5-ジメトキシ-4-ヒドロキシ-N-{4-[2-[(2-チエニル(イミノ)メチル)アミ ノ]フェニル]エチル}ベンズアミド; - 3,4,5-トリヒドロキシ-N-{4-[2-[(2-チエニル(イミノ)メチル)アミノ]フェ ニル]エチル}ベンズアミド; - N-{4-[4-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシベンゾイル]-1-ピ ペラジニル]フェニル}-2-チオフェンカルボキシイミドアミド; - N-{4-[4-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシベンジル]-1-ピペ ラジニル]フェニル]-2-チオフェンカルボキシイミドアミド; - N-{4-[4-[3,5-ジメトキシ-4-ヒドロキシベンゾイル]-1-ピペラジニル]フェ ニル}-2-チオフェンカルボキシイミドアミド; - 3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-N-{4-[(2-チエニル(イ ミノ)メチル)アミノ]フェニル}-2H-1-ベンゾピラン-2-カルボキシアミド; - N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベン ゾピラン-2-イル)カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカルボ キシイミドアミド; - N-{4-[4-[(5-メトキシ-1H-インドール-3-イル)メチルカルボニル]-1-ピペ ラジニル]フェニル}-2-チオフェンカルボキシイミドアミド; - N-[4-[4-[{3-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-1- オキソ-2-プロペニル}-1-ピペラジニル]フェニル]]-2-チオフェンカルボキシイ ミドアミド; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{3-[[(2-チエニル(イミ ノ)メチル)アミノ]フェニル]メチル}ベンズアミド; - N-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{{4-[(2- チエニル(イミノ)メチル)アミノ]フェニル}メチル}尿素; - N-[5-[{3-(3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル)-1-オ キソ-2-プロペニル}アミノ]-2-ヒドロキシフェニル]-2-チオフェンカルボキシイ ミドアミド; - N-[3-[{3-{3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル)-1-オ キソ-2-プロペニル}アミノ]-4-ヒドロキシフェニル]-2-チオフェンカルボキシイ ミドアミド; - N-{4-[4-[3,4,5-トリヒドロキシベンゾイル]-1-ピペラジニル]フェニル}-2 -チオフェンカルボキシイミドアミド; - N-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{{4-[(2- チエニル(イミノ)メチル)アミノ]フェニル}カルボニルアミノ}尿素; - N-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{{4-[(2- チエニル(イミノ)メチル)アミノ]フェニル}メチル}チオ尿素; - N-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{2-{4-[(2 -チエニル(イミノ)メチル)アミノ]フェニル}エチル}尿素; - N-(4-{4-[(3,4-ジヒドロ-6-メトキシ-2,5,7,8-テトラメチル-2H-1-ベンゾ ピラン-2-イル)カルボニル]-1-ピペラジニル}フェニル)-2-チオフェンカルボキ シイミドアミド; - N-(4-{4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベン ゾピラン-2-イル)カルボニル]-1H-1,4-ジアゼピン-1-イル}フェニル]-2-チオフ ェンカルボキシイミドアミド; - (R)-N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)-カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; - (S)-N-{4-[4I[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)-カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{2-[3-[(2-チエニル(イ ミノ)メチル)アミノ]フェニル]エチル}ベンズアミド; - N-{4-(4-[2-(3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル)-1- オキソ-エチル]-1-ピペラジニル)フェニル}-2-チオフェンカルボキシイミドアミ ド; - 2-{4-[(2-チエニル(イミノ)メチル)アミノ]フェニル}エチル 3,5-ビス-(1, 1-ジメチルエチル)-4-ヒドロキシベンゾエート; - 2-{3-[(2-チエニル(イミノ)メチル)アミノ]フェニル}エチル 3,5-ビス-(1, 1-ジメチルエチル)-4-ヒドロキシベンゾエート; - 2-{2-[(2-チエニル(イミノ)メチル)アミノ]フェニル}エチル 3,5-ビス-(1, 1-ジメチルエチル)-4-ヒドロキシベンゾエート; のうちの一つ又は上記の化合物の一つの塩、特に塩酸塩、二塩酸塩、フマル酸塩 又はヘミフマル酸塩である、請求項1に記載の化合物。 3. Xが1〜6個の炭素原子を有する直鎖又は分岐鎖アルキレン基を表し、 Yがピペラジン、ホモピペラジン、2-メチルピペラジン、2,5-ジメチルピペラジ ン、4-アミノピペリジン、-NR3-Z2-Q-、-NR3-NH-CO-Z2-、-NH-NH-Z2-又は-NR3-O -Z2-基を表すか;あるいは、 Xが-Z1-CO-又は-CH=CH-CO-を表し、Yがピペラジン、ホモピペラジン、2-メ チルピペラジン、2,5-ジメチルピペラジン、4-アミノピペリジン、-NR3-Z2-Q-、 -NR3-NH-CO-Z2-、-NH-NH-Z2-、-NR3-O-Z2-、-O-Z2-Q基又は-NR3CO-Q'-基(Q'=R3 -N-Z3)を表すか;あるいは、 Xが-Z1-NR3-CO-を表し、Yが-Z2-Q-、-NH-Z2-Q-、-NH-CO-Z2-Q"(Q"=O-Z3- 、R3N-Z3-又はS-Z3-)を表すか又はYが-NR3-SO2-NR3-Z2-又は-O-Z2-Q-を表すか ;あるいは、 Xが-Z1-NH-CO-を表し、Yがピペラジン、ホモピペラジン、2-メチルピペラジ ン、2,5-ジメチルピペラジン、4-アミノピペリジン、-NR3-Z2-Q-、-NR3-NH-CO-Z2 -、-NH-NH-Z2-又は-NR3-O-Z2-基を表すか;あるいは、 Xが-Z1-NR3-SO2-を表し、Yが-Z2-Q"-(Q"=O-Z3-、R3-N-Z3-又はS-Z3-) を表すか又はYが-NR3-Z2-Q-を表すか;あるいは、 Xが-Z1-を表し、Yが-O-CO-Z2-Q-を表すか;あるいは、 Xが-Z1-NR3-CS-を表し、Yが-NH-Z2-Q-又はピペラジン、ホモピペラジン、2- メチルピペラジン、2,5-ジメチルピペラジン、4-アミノピペリジン、-NR3-Z2-Q- 、-NH-NH-Z2-又は-NR3-O-Z2-基を表すか;あるいは、 Xが結合を表し、Yが-O-Z2-NH-又は-S-Z2-NH-を表す、請求項1に記載の化合 物。 4. Aが、 を表し、Xが-CO-又は-NH-CO-を表し、Yが-NH-Z2-Q-又はピペラジン基を表し、 Qが結合、O-Z3、R3-N-Z3又はS-Z3を表し、Z2及びZ3が、独立して、結合又は 1〜6個の炭素原子を有する直鎖又は分岐鎖アルキレン基を表し、R3が水素原 子又は1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル基を表す、請求項1 〜3のいずれかに記載の化合物。 5. 下記の化合物: - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{4-[2-[(2-チエニル(イ ミノ)メチル)アミノ]フェニル]エチル}ベンズアミド; - 3,4,5-トリヒドロキシ-N-{4-[2-[(2-チエニル(イミノ)メチル)アミノ]フェ ニル]エチル}ベンズアミド; - N-{4-[4-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシベンゾイル]-1-ピ ペラジニル]フェニル}-2-チオフェンカルボキシイミドアミド; - N-{4-[4-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシベンジル]-1-ピペ ラジニル]フェニル}-2-チオフェンカルボキシイミドアミド; - 3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-N-{4-[(2-チエニル(イ ミノ)メチル)アミノ]フェニル}-2H-1-ベンゾピラン2-カルボキシイミド; - N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベン ゾピラン-2-イル)カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカルボ キシイミドアミド; - N-{4-[4-[(5-メトキシ-1H-インドール-3-イル)メチルカルボニル]-1-ピペ ラジニル]フェニル}-2-チオフェンカルボキシイミドアミド; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-{3-[[(2-チエニル(イミ ノ)メチル)アミノ]フェニル]メチル}ベンズアミド; - N-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{{4-[(2- チエニル(イミノ)メチル)アミノ]フェニル}メチル}尿素; - N-[5-[{3-(3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル)-1-オ キソ-2-プロペニル}アミノ]-2-ヒドロキシフェニル]-2-チオフェンカルボキシイ ミドアミド; - N-[3-[{3-(3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシフェニル)-1-オ キソ-2-プロペニル}アミノ]-4-ヒドロキシフェニル]-2-チオフェンカルボキシイ ミドアミド; - N-{4-[4-[3,4,5-トリヒドロキシベンゾイル]-1-ピペラジニル]フェニル}-2 -チオフェンカルボキシイミドアミド; - N-[3,5-ビス-{1,1-ジメチルエチル)-4-ヒドロキシフェニル]-N'-{{4-[(2- チエニル(イミノ)メチル)アミノ]フェニル}カルボニルアミノ}尿素; - (R)-N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)-カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; - (S)-N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; の一つ又はその塩、特に塩酸塩、二塩酸塩、フマル酸塩又はヘミフマル酸塩であ る、請求項1又は2に記載の化合物。 6. 下記の化合物: - 4-アセトキシ-3,5-ジメトキシ-N-{4-[2-[2-チエニル(イミノメチル)アミ ノ]フェニル]エチル}ベンズアミド; - 3,5-ジメトキシ-4-ヒドロキシ-N-{4-[2-[2-チエニル(イミノメチル)アミノ ]フェニル]エチル}ベンズアミド; の一つ又はその塩、特に塩酸塩、二塩酸塩、フマル酸塩又はヘミフマル酸塩であ る、請求項1又は2に記載の化合物。 7. N-{4-[4-[3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシベンジル]-1- ピペラジニル]フェニル}-2-チオフェンカルボキシイミドアミド又はその塩、特 に塩酸塩、二塩酸塩、フマル酸塩又はヘミフマル酸塩である、請求項1又は2に 記載の化合物。 8. 下記の化合物: - N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベン ゾピラン-2-イル)カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカルボ キシイミドアミド; - (R)-N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)-カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; - (S)-N-{4-[4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1- ベンゾピラン-2-イル)-カルボニル]-1-ピペラジニル]フェニル}-2-チオフェンカ ルボキシイミドアミド; の一つ又はその塩、特に塩酸塩、二塩酸塩、フマル酸塩又はヘミフマル酸塩であ る、請求項1又は2に記載の化合物。 9. 新規工業製品としての、下記の化合物: - 1-{3,4-ジヒドロ-6-メトキシ-2,5,7,8-テトラメチル-2H-1-ベンゾピラン-2 -イル}カルボニル}-4-(4-ニトロフェニル)ピペラジン; - 1-{3,4-ジヒドロ-6-メトキシ-2,5,7,8-テトラメチル-2H-1-ベンゾピラン-2 -イル}カルボニル}-4-(4-アミノフェニル)ピペラジン; - ヘキサヒドロ-4-(4-ニトロフェニル)-1H-1,4-ジアゼピン; - 1-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベンゾピラ ン-2-イル)カルボニル]ヘキサヒドロ-4-(4-ニトロフェニル)-1H-1,4-ジアゼピ ン; - 1-(4-アミノフェニル)-4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメ チル-2H-1-ベンゾビラン-2-イル)カルボニル]ヘキサヒドロ-1H-1,4-ジアゼピン ; - N-[4-{4-[(3,4-ジヒドロ-6-ヒドロキシ-2,5,7,8-テトラメチル-2H-1-ベン ゾピラン-2-イル)カルボニル]-1H-1,4-ジアゼピン-1-イル}フェニル]-2-チオフ ェンカルボキシイミドアミド塩酸塩 - (R)-3,4-ジヒドロ-2,5,7,8-テトラメチル-2-{4-[(4-ニトロフェニル)-1-ピ ペラジニル]カルボニル}-2H-1-ベンゾピラン-6-オール; - (R)-3,4-ジヒドロ-2,5,7,8-テトラメチル-2-{4-[(4-アミノフェニル)-1-ピ ペラジニル]カルボニル}-2H-1-ベンゾピラン-6-オール; - (S)-3,4-ジヒドロ-2,5,7,8-テトラメチル-2-{4-[(4-ニトロフェニル)-1-ピ ペラジニル]カルボニル}-2H-1-ベンゾピラン-6-オール; - (S)-3,4-ジヒドロ-2,5,7,8-テトラメチル-2-{4-[(4-アミノフェニル)-1-ピ ペラジニル]カルボニル}-2H-1-ベンゾピラン-6-オール; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-[2-(3-ニトロフェニル) エチル]ベンズアミド; - 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキシ-N-[2-(3-アミノフェニル) エチル]ベンズアミド; - 2-(4-ニトロフェニル)エチル3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキ シベンゾエート; - 2-(4-アミノフェニル)エチル 3,5-ビス-(1,1-ジメチルエチル)-4-ヒドロキ シベンゾエート; の一つ又はその塩。 10. 新規工業製品としての、次の一般式(II)A: 〔式中、 Wはアミノ又はニトロ基を表し; Aは下記の基: (上記の基中、R1及びR2は、独立して、水素原子、ハロゲン、OH基又は1〜6 個の炭素原子を有する、直鎖又は分岐鎖アルキル又はアルコキシ基を表し、R3 は水素原子、1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル基又は-COR4 基を表し、R4は1〜6個の炭素原子を有する直鎖又は分岐鎖アルキル基を表す) 、又は下記の基: (上記の基中、R3は前記と同一の意義を有する)、又は下記の基: (上記の基中、R5は水素原子、OH基又は1〜6個の炭素原子を有する直鎖又は 分岐鎖アルキル又はアルコキシ基を表す)を表し; Xは-Z1-、-Z1-CO-、-CH=CH-CO-、-Z1-NR3-CO-、-Z1-NR3-CS-、-Z1-NR3-SO2- 又は単結合を表し; Yは-Z2-Q-、ピペラジン、ホモピペラジン、2-メチルピペラジン、2,5-ジメチ ルピペラジン、4-アミノピペリジン、-NR3-Z2-Q-、-NR3-CO-Z2-Q-、-NR3-NH-CO- Z2-、-NH-NH-Z2-、-NR3-O-Z2-、-NR3-SO2-NR3-Z2、-O-Z2-Q-、-O-CO-Z2-Q-又は- S-Z2-Q-基(但し、上記の基中のQは単結合、O-Z3-、R3-N-Z3又はS-Z3を表す) から選ばれる基を表し; Z1、Z2及びZ3は、独立して、単結合又は1〜6個の炭素原子を有する直鎖 又は分岐鎖アルキレン基を表し;好ましくはZ1、Z2及びZ3は-(CH2)m-(mは0〜6 の整数である)を表し; R6は水素原子又はOH基を表す〕で表される化合物〔但し、3,5-ビス-(1,1-ジ メチルエチル)-4-ヒドロキシ-N-(4-ニトロフェニル)ベンズアミドを除く〕、又 は一般式(II)Aの化合物の塩、但し、下記の式の化合物は除外される: 11. 一般式(III): の化合物を、メタノール、エタノール、イソプロピルアルコール又はt-ブタノー ルのごとき低級アルコール、好ましくはイソプロピルアルコール中で、一般式(I V): の化合物と反応させること、上記一般式(IV)の化合物は、場合により、無機酸G 、好ましくはHCl、HBr又はHIで塩化されており、そして、一般式(III)及び(IV) の化合物において、 Aは下記の基: (上記の基中、R1及びR2は、独立して、水素原子、ハロゲン、OH基又は1〜6 個の炭素原子を有する直鎖又は分岐鎖アルキル又は1〜6個の炭素原子を有する 直鎖又は分岐鎖アルコキシ基を表し、R3は水素原子、1〜6個の炭素原子を有 する直鎖又は分岐鎖アルキル基又は-COR4基を表し、R4は1〜6個の炭素原子を 有する直鎖又は分岐鎖アルキル基を表す)、又は下記の基: (上記の基中、R3は前記と同一の意義を有する)、又は下記の基: (上記の基中、R5は水素原子、OH基又は1〜6個の炭素原子を有する直鎖又は 分岐鎖アルキル又はアルコキシ基を表す)を表し; Bは1〜6個の炭素原子を有する、直鎖又は分岐鎖アルキル基、O、S、Nか ら選ばれた1〜4個のヘテロ原子を含有する5又は6頁の炭素環式又は複素環式 アリール基、特に、チオフェン、フラン、ピロール又はチアゾール基を表し、上 記アリール基の炭素原子は、場合により1〜6個の炭素原子を有する直鎖又は分 岐鎖アルキル、アルケニル又はアルコキシ基から選ばれた1個又はそれ以上の基 によって置換されていてもよく; Lは脱離性基、特にチオアルキル、スルホン酸、トリフルオロメタンスルホン 酸、ハライド、アリールアルコール又はトシル基を表し; Xは-Z1-、-Z1-CO-、-CH=CH-CO-、-Z1-NR3-CO-、-Z1-NR3-CS-、-Z1-NR3-SO2- 又は結合を表し; Yは-Z2-Q-、ピペラジン、ホモピペラジン、2-メチルピペラジン、2,5-ジメチ ルピペラジン、4-アミノピペリジン、-NR3-Z2-Q-、-NR3-CO-Z2-Q-、-NR3-NH-CO- Z2-、-NH-NH-Z2-、-NR3-O-Z2-、-NR3-SO2-NR3-Z2、-O-Z2-Q-、-O-CO-Z2-Q-又は- S-Z2-Q-基(上記の基中のQは結合、O-Z3-、R3-N-Z3又はS-Z3を表す)を表し; Z1、Z2及びZ3は、独立して、結合又は1〜6個の炭素原子を有する、直鎖 又は分岐鎖アルキレン基を表し; R6は水素原子又はOH基を表す;ことを特徴とする、請求項1〜8のいずれか に記載の化合物の製造方法。 12. 医薬しての、請求項1〜8のいずれかに記載の一般式(I)の化合物又は その薬剤学的に許容される塩。 13. 請求項12に記載の化合物の少なくとも1種を活性成分として含有する医 薬組成物。 14. 神経NOシンターゼを抑制するための医薬の製造における、請求項1〜8 のいずれかに記載の一般式(I)の化合物又はその薬剤学的に許容される塩の使用 。 15. 誘導性NOシンターゼを抑制するための医薬の製造における、請求項1〜 8のいずれかに記載の一般式(I)の化合物又はその薬剤学的に許容される塩の使 用。 16. 脂質過剰酸化を抑制するための医薬の製造における、請求項1〜8のい ずれかに記載の一般式(I)の化合物又はその薬剤学的に許容される塩の使用。 17. NOシンターゼ抑制活性と脂質過剰酸化抑制活性の両者を有する医薬の製 造における、請求項1〜8のいずれかに記載の一般式(I)の化合物又はその薬剤 学的に許容される塩の使用。
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US6335445B1 (en) * | 1997-03-24 | 2002-01-01 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them |
US6809088B2 (en) * | 1997-03-24 | 2004-10-26 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them |
AR019190A1 (es) * | 1998-07-08 | 2001-12-26 | Sod Conseils Rech Applic | Derivados de 2-aminopiridinas, productos intermedios para su preparacion, medicamentos y composiciones farmaceuticas que los contienen y su uso para preparar medicamentos |
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RU2380362C2 (ru) * | 1999-10-11 | 2010-01-27 | Сосьете Де Консей Де Решерш З | Производные пятичленных гетероциклов, способ их получения и их применение в качестве лекарственных средств |
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EP1264820A4 (en) * | 2000-03-14 | 2004-09-15 | Fujisawa Pharmaceutical Co | amide compounds |
AU4424401A (en) * | 2000-03-16 | 2001-09-24 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Novel lipoic acid heterocyclic or benzene derivatives, preparation and use thereof as medicines |
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DE10162114A1 (de) * | 2001-12-12 | 2003-06-26 | Schering Ag | Neue Amidin-Derivate und deren Verwendung in Arzneimitteln |
DE10240735A1 (de) * | 2002-08-29 | 2004-03-18 | Eberhard-Karls-Universität Tübingen Universitätsklinikum | Verwendung von Modulatoren der NO-Signalkaskade und pharmazeutische Zusammensetzung |
EP1577289A1 (en) * | 2004-03-18 | 2005-09-21 | Revotar Biopharmaceuticals AG | Non-glycosylated/-glycosidic/-peptidic small molecule selectin inhibitors for the treament of inflammatory disorders |
EP1893583B1 (en) | 2005-05-31 | 2012-04-04 | Pfizer Inc. | Substituted aryloxy-n-bicyclomethyl acetamide compounds as vr1 antagonists |
EP1764095A1 (en) * | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel nitrocatechol derivatives having selectin ligand activity |
EP1764093A1 (en) * | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel aromatic compounds and their use in medical applications |
EP1764096A1 (en) * | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel phloroglucinol derivatives having selectin ligand activity |
EP1764094A1 (en) * | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel multi-cyclic compounds and their use |
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AU6286294A (en) * | 1993-03-23 | 1994-10-11 | Astra Aktiebolag | Guanidine derivatives useful in therapy |
IL110643A (en) * | 1993-08-12 | 1998-07-15 | Astra Ab | History of amidine, their preparation and the pharmaceutical preparations containing them |
ATE182889T1 (de) * | 1994-05-07 | 1999-08-15 | Astra Ab | Bicyclische amidinderivate als no-synthetase inhibitoren |
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Cited By (1)
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JP2015522067A (ja) * | 2012-07-12 | 2015-08-03 | コンドリオン アイピー ビー.ブイ.Khondrion Ip B.V. | ミトコンドリア病を治療するためのクロマニル誘導体 |
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