公开(公告)号：US08044206B2

公开(公告)日：2011-10-25

申请号：US10548197

申请日：2004-03-05

申请人： Kazumi Kikuchi ,  Makoto Oku ,  Jiro Fujiyasu ,  Norio Asai ,  Toshihiro Watanabe ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

发明人： Kazumi Kikuchi ,  Makoto Oku ,  Jiro Fujiyasu ,  Norio Asai ,  Toshihiro Watanabe ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

IPC分类号： C07D211/08 ,  A61K31/47

CPC分类号： C07D211/12

摘要： The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

摘要翻译： 本发明提供了具有2,6-二取代苯乙烯基的新型含氮杂环衍生物及其药学上可接受的盐，以及包含含氮杂环衍生物及其药学上可接受的盐的药物组合物，特别是作为 钠通道抑制剂，具有优异的镇痛作用，特别是对神经性疼痛具有最小的副作用。

公开(公告)号：US20070099956A1

公开(公告)日：2007-05-03

申请号：US10548197

申请日：2004-03-05

申请人： Kazumi Kikuchi ,  Makoto Oku ,  Jiro Fujiyasu ,  Norio Asai ,  Toshihiro Watana ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

发明人： Kazumi Kikuchi ,  Makoto Oku ,  Jiro Fujiyasu ,  Norio Asai ,  Toshihiro Watana ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

IPC分类号： A61K31/47 ,  A61K31/44 ,  C07D215/12 ,  C07D213/81

CPC分类号： C07D211/12

摘要： The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

摘要翻译： 本发明提供了具有2,6-二取代苯乙烯基的新型含氮杂环衍生物及其药学上可接受的盐，以及包含含氮杂环衍生物及其药学上可接受的盐的药物组合物，特别是作为 钠通道抑制剂，具有优异的镇痛作用，特别是对神经性疼痛具有最小的副作用。

公开(公告)号：US20080070898A1

公开(公告)日：2008-03-20

申请号：US11661446

申请日：2005-08-31

申请人： Kazumi Kikuchi ,  Jiro Fujiyasu ,  Toshihiro Watanabe ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

发明人： Kazumi Kikuchi ,  Jiro Fujiyasu ,  Toshihiro Watanabe ,  Yukinori Nagakura ,  Hiroshi Tomiyama ,  Motoharu Sonegawa ,  Kazuo Tokuzaki ,  Yoshinori Iwai

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/553 ,  A61P25/04 ,  C07D273/01 ,  C07D401/06 ,  C07D413/06

CPC分类号： C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D487/08 ,  C07D491/10

摘要： The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (—R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [—C(═O)—R4], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect

摘要翻译： 其中哌啶环的4位通过亚乙烯基键合到单取代的（-R 1）或未取代的苯环上的本发明的哌啶衍生物和1-取代的 哌啶环具有酰基[-C（-O）-R 4]，或其药学上可接受的盐具有优异的钠通道抑制作用和优异的镇痛作用，并显示出高镇痛作用 特别是神经源性疼痛。 本发明化合物可用作低副作用的钠通道抑制剂

公开(公告)号：US6124460A

公开(公告)日：2000-09-26

申请号：US441515

申请日：1999-11-17

申请人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takeyuki Imamaki ,  Naoto Ueyama ,  Motoharu Sonegawa ,  Satoru Takeuchi

发明人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takeyuki Imamaki ,  Naoto Ueyama ,  Motoharu Sonegawa ,  Satoru Takeuchi

IPC分类号： A61K31/00 ,  A61K31/435 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61P3/00 ,  A61P3/06 ,  A61P43/00 ,  C07D453/06

CPC分类号： C07D453/06

摘要： New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.

摘要翻译： 异喹啉衍生物的新治疗剂由下式表示，或其盐酸盐。 （羧基）苯基，2-（羧基） - 噻吩-5-基，喹啉-5-基，4-（乙氧基羰基）苯基， （喹啉-5-基）苯基或4-（3-氧代-2-氮杂双环[2.2.2]辛烷-2-基） - 苯基; R2是氢或烯丙基; X1和X2都是氢和X1 X2可以形成氧基，m表示0〜2的整数。）这些化合物对角鲨烯合酶的抑制活性优异，可用作高胆固醇血症的治疗剂。

公开(公告)号：US5240944A

公开(公告)日：1993-08-31

申请号：US665662

申请日：1991-03-07

申请人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Tadashi Shirai ,  Shuuichi Wakabayashi ,  Tomoyuki Kawai ,  Naoto Ueyama ,  Motoharu Sonegawa

发明人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Tadashi Shirai ,  Shuuichi Wakabayashi ,  Tomoyuki Kawai ,  Naoto Ueyama ,  Motoharu Sonegawa

IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D471/14 ,  C07D487/04

摘要： Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:A--S--Rwherein A is ##STR1## R.sub.1 represent a lower alkyl or substituted phenyl or unsubstituted phenyl group; R.sub.2 is a lower alkyl; R.sub.3 is H or a lower alkyl; R is lower alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, dialkylaminoalkyl, cyanoalkyl, alkoxycarbonylalkyl, carboxylalkenyl, alkoxycarbonyl, alkoxyalkylcarbonyl, dialkylaminocarbonyl, dialkylaminothiocarbonyl, phenoxyalkylcarbonyl, piperidinoalkyl, pyridine carbonyl, substituted or unsubstituted benzoyl, or substituted or unsubstituted benzyl group. The compounds of the present invention are useful as anti-ulcerative agents.

摘要翻译： 公开了由下式表示的环状胍的衍生物：A-S-R其中A为低级烷基或取代的苯基或未取代的苯基; R2是低级烷基; R3是H或低级烷基; R是低级烷基，烯基，炔基，烷酰基，烯酰基，二烷基氨基烷基，氰基烷基，烷氧基羰基烷基，羧基烯基，烷氧基羰基，烷氧基烷基羰基，二烷基氨基羰基，二烷基氨基硫代羰基，苯氧基烷基羰基，哌啶子基烷基，吡啶羰基，取代或未取代的苯甲酰基或取代或未取代的苄基。 本发明的化合物可用作抗溃疡剂。

公开(公告)号：US5409947A

公开(公告)日：1995-04-25

申请号：US64446

申请日：1993-05-21

申请人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takashi Yanagisawa ,  Naoto Ueyama ,  Tomoyuki Kawai ,  Motoharu Sonegawa ,  Hiromi Baba ,  Makoto Haketa

发明人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takashi Yanagisawa ,  Naoto Ueyama ,  Tomoyuki Kawai ,  Motoharu Sonegawa ,  Hiromi Baba ,  Makoto Haketa

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61P9/00 ,  A61P9/12 ,  A61P27/02 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  A61K31/41 ,  C07D257/04

CPC分类号： C07D235/02 ,  C07D403/10

摘要： New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line "- - - -" is two double bonds or saturated single bonds).These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.

摘要翻译： 公开了由下式表示的环庚咪唑衍生物的新治疗剂或其碱加成盐。 起床 R2表示低级烷基; R 3表示羧酸或四唑基。 A和A 1为4或8位的取代基，当A为氢或A且A 1为氧代基时，A 1为氢或羟基。 虚线“ - - - ”是两个双键或饱和单键）。 这些化合物可用作抗高血压或抗充血性心力衰竭剂。

公开(公告)号：US5008282A

公开(公告)日：1991-04-16

申请号：US450264

申请日：1989-12-13

申请人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Tadashi Shirai ,  Shuuichi Wakabayashi ,  Tomoyuki Kawai ,  Naoto Ueyama ,  Motoharu Sonegawa

发明人： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Tadashi Shirai ,  Shuuichi Wakabayashi ,  Tomoyuki Kawai ,  Naoto Ueyama ,  Motoharu Sonegawa

IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D471/14 ,  C07D487/04

摘要： Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:A--S--Rwherein A is ##STR1## R.sub.1 represent a lower alkyl or substituted phenyl or unsubstituted phenyl group; R.sub.2 is a lower alkyl; R.sub.3 is H or a lower alkyl; R is lower alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, dialkylaminoalkyl, cyanoalkyl, alkoxycarbonylalkyl, carboxylalkenyl, alkoxycarbonyl, alkoxyalkylcarbonyl, dialkylaminocarbonyl, dialkylaminothiocarbonyl, phenoxyalkylcarbonyl, piperidinoalkyl, pyridine carbonyl, substituted or unsubstituted benzoyl, or substituted or unsubstituted benzyl group.The compounds of the present invention are useful as anti-ulcerative agents.

摘要翻译： 公开了由下式表示的环状胍的衍生物：A-S-R，其中A为低级烷基或取代的苯基或未取代的苯基; R2是低级烷基; R3是H或低级烷基; R是低级烷基，烯基，炔基，烷酰基，烯酰基，二烷基氨基烷基，氰基烷基，烷氧基羰基烷基，羧基烯基，烷氧基羰基，烷氧基烷基羰基，二烷基氨基羰基，二烷基氨基硫代羰基，苯氧基烷基羰基，哌啶子基烷基，吡啶羰基，取代或未取代的苯甲酰基或取代或未取代的苄基。 本发明的化合物可用作抗溃疡剂。