公开(公告)号：US07803801B2

公开(公告)日：2010-09-28

申请号：US11363563

申请日：2006-02-28

申请人： Yoshitoshi Kodama ,  Satoru Noji ,  Katsuaki Imamura ,  Ryo Mizojiri ,  Kenta Aoki ,  Hideo Takagi ,  Yuichi Naka ,  Goro Ito ,  Kiyotaka Shinoda ,  Akihito Fujiwara ,  Kazunori Kurihara ,  Masaru Tanaka

发明人： Yoshitoshi Kodama ,  Satoru Noji ,  Katsuaki Imamura ,  Ryo Mizojiri ,  Kenta Aoki ,  Hideo Takagi ,  Yuichi Naka ,  Goro Ito ,  Kiyotaka Shinoda ,  Akihito Fujiwara ,  Kazunori Kurihara ,  Masaru Tanaka

IPC分类号： C07D401/00 ,  A61K31/47

CPC分类号： C07D417/14

摘要： The present invention relates to an aminopyridine compound represented by the following general formula (I) or a salt thereof and an Syk inhibitor containing the compound or a salt thereof as an active ingredient. Here, X1, X2, X3, Z, Y1, Y2 represent a carbon atom or a nitrogen atom, R, R1, R5, R6 represent a hydrogen atom, an alkyl group, etc., and R7 represents a hydrogen atom, a halogen atom, a nitro group, a cyano group, —CpH2(p-1)(Ra1)(Ra2)—O—Ra3, —C(═O)—Rd1, a 5- or 6-membered saturated heterocyclic group, an aromatic heterocyclic group, —N(Rh1)(Rh2), etc. The aminopyridine compound of the present invention has not only high Syk inhibitory activity but also properties to selectively inhibit Syk.

摘要翻译： 本发明涉及由以下通式（I）表示的氨基吡啶化合物或其盐和含有该化合物或其盐作为有效成分的Syk抑制剂。 这里，X1，X2，X3，Z，Y1，Y2表示碳原子或氮原子，R，R1，R5，R6表示氢原子，烷基等，R7表示氢原子，卤素 原子，硝基，氰基，-CpH2（p-1）（Ra1）（Ra2）-O-Ra3，-C（= O）-Rd1，5或6元饱和杂环基，芳香族 杂环基，-N（Rh1）（Rh2）等。本发明的氨基吡啶化合物不仅具有高的Syk抑制活性，而且具有选择性抑制Syk的性质。

公开(公告)号：US20060205731A1

公开(公告)日：2006-09-14

申请号：US11363563

申请日：2006-02-28

申请人： Yoshitoshi Kodama ,  Satoru Noji ,  Katsuaki Imamura ,  Ryo Mizojiri ,  Kenta Aoki ,  Hideo Takagi ,  Yuichi Naka ,  Goro Ito ,  Kiyotaka Shinoda ,  Akihito Fujiwara ,  Kazunori Kurihara ,  Masaru Tanaka

发明人： Yoshitoshi Kodama ,  Satoru Noji ,  Katsuaki Imamura ,  Ryo Mizojiri ,  Kenta Aoki ,  Hideo Takagi ,  Yuichi Naka ,  Goro Ito ,  Kiyotaka Shinoda ,  Akihito Fujiwara ,  Kazunori Kurihara ,  Masaru Tanaka

IPC分类号： A61K31/506 ,  A61K31/497 ,  A61K31/501 ,  A61K31/444 ,  C07D417/14

CPC分类号： C07D417/14

摘要： The present invention relates to an aminopyridine compound represented by the following general formula (I) or a salt thereof and an Syk inhibitor containing the compound or a salt thereof as an active ingredient. Here, X1, X2, X3, Z, Y1, Y2 represent a carbon atom or a nitrogen atom, R, R1, R5, R6 represent a hydrogen atom, an alkyl group, etc., and R7 represents a hydrogen atom, a halogen atom, a nitro group, a cyano group, —CpH2(p-1)(Ra1)(Ra2)—O—Ra3, —C(═O)—Rd1, a 5- or 6-membered saturated heterocyclic group, an aromatic heterocyclic group, —N(Rh1)(Rh2), etc. The aminopyridine compound of the present invention has not only high Syk inhibitory activity but also properties to selectively inhibit Syk.

摘要翻译： 本发明涉及由以下通式（I）表示的氨基吡啶化合物或其盐和含有该化合物或其盐作为有效成分的Syk抑制剂。 这里，X 1，X 2，X 3，Z，Y 1，Y 2， / SUP>表示碳原子或氮原子，R 1，R 1，R 5，R 6表示氢原子，烷基 基团等，R 7表示氢原子，卤素原子，硝基，氰基，-C 2 H 2 H（H） （R a1）（R a2） - 或 - a3 - ， - （ - O - ） - 5或6元饱和杂环基，芳香族杂环基，-N（R h1H1）（R h2H2）等。 本发明的氨基吡啶化合物不仅具有高Syk抑制活性，而且具有选择性抑制Syk的性质。

公开(公告)号：US5036086A

公开(公告)日：1991-07-30

申请号：US501727

申请日：1990-03-30

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

IPC分类号： A61K31/425 ,  A61K31/428 ,  A61P37/08 ,  C07D277/82

CPC分类号： C07D277/82

摘要： Novel benzothiazole derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group or a lower acyl group; X and Y are the same or different and are each hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, nitro group, amino group, cyano group, trifluoromethyl group, a group of the formula: --COOR.sup.2 (wherein R.sup.2 is hydrogen atom, a lower alkyl group, an alkali metal, an alkaline earth metal, or a cation of amine), or a group of the formula: --CONR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen atom or a lower alkyl group) or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the compound as set forth above as an active ingredient.

公开(公告)号：US5624961A

公开(公告)日：1997-04-29

申请号：US535077

申请日：1995-12-11

申请人： Masakazu Ban ,  Kiyotaka Shinoda ,  Mitsuru Takahashi ,  Shuhei Deguchi ,  Hiroaki Taguchi ,  Takeo Katsushima

发明人： Masakazu Ban ,  Kiyotaka Shinoda ,  Mitsuru Takahashi ,  Shuhei Deguchi ,  Hiroaki Taguchi ,  Takeo Katsushima

IPC分类号： A61K31/135 ,  A61K31/165 ,  A61K31/22 ,  A61P9/00 ,  C07C213/02 ,  C07C213/04 ,  C07C217/18 ,  C07C217/58 ,  C07C217/84 ,  C07C219/28 ,  C07C231/12 ,  C07C233/18 ,  C07C233/25 ,  C07C303/32 ,  C07C309/30

CPC分类号： C07C217/84 ,  C07C217/18 ,  C07C217/58 ,  C07C219/28 ,  C07C233/18 ,  C07C233/25

摘要： Novel benzylaminoethoxybenzene derivatives of the formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, a lower hydroxyalkyl, a lower alkoxyalkyl, an allyl or a benzyl; R.sup.2 is a hydrogen atom, a lower alkyl, a lower acyl, an allyl or a benzyl; R.sup.3 is a hydrogen atom, a lower alkyl, a lower alkoxyalkyl, a lower dialkylaminoalkyl or a lower acyl; and R.sup.4 is a hydrogen atom, a halogen atom, a lower alkoxy, an amino, a lower acylamino, a hydroxy, a lower acyloxy, a lower acyl, a carboxy or a lower alkoxycarbonyl, salts thereof and solvates thereof. An .alpha..sub.1 -adrenoceptor blocker obtained from this compound has a strong .alpha..sub.1 -adrenoceptor blocking effect and causes less side effects such as orthostatic hypotension.

摘要翻译： PCT No.PCT / JP95 / 00187 Sec。 371 1995年12月11日第 102（e）日期1995年12月11日PCT提交1995年2月10日PCT公布。 出版物WO95 / 21811 日期：1995年8月17日式（I）的新型苄基氨基乙氧基苯衍生物其中R 1为氢原子，低级烷基，低级羟烷基，低级烷氧基烷基，烯丙基或苄基; R2是氢原子，低级烷基，低级酰基，烯丙基或苄基; R3是氢原子，低级烷基，低级烷氧基烷基，低级二烷基氨基烷基或低级酰基; R4为氢原子，卤素原子，低级烷氧基，氨基，低级酰基氨基，羟基，低级酰氧基，低级酰基，羧基或低级烷氧基羰基，其盐及其溶剂合物。 从该化合物获得的α1-肾上腺素受体阻滞剂具有强α1-肾上腺素能受体阻断效应并且引起较少的副作用，例如直立性低血压。

公开(公告)号：US5041462A

公开(公告)日：1991-08-20

申请号：US476515

申请日：1990-02-07

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

IPC分类号： A61K31/165 ,  A61K31/275 ,  A61P37/08 ,  C07C237/30 ,  C07C237/42 ,  C07C237/44 ,  C07C255/60 ,  C07D295/155

CPC分类号： C07D295/155 ,  C07C237/42 ,  C07C237/44 ,  C07C255/60

摘要： Novel substituted acetamide compounds of the formula ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a lower acyl group, or an aryl group; R.sup.2 is cyano group or aminocarbonyl group; R.sup.3 is a halogen atom, nitro group, a lower alkoxy group, a group of the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 is hydrogen atom, a lower alkyl group or a group of the formula: --COCH.sub.2 OR.sup.1 ; R.sup.5 is hydrogen atom or a lower alkyl group), or a cyclic amino group of the formula: ##STR2## (wherein R.sup.6 and R.sup.7 are each an alkylene group having 1 to 3 carbon atoms, and X is oxygen atom or methylene), or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.