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1. 发明授权

US06812235B2 Beta-alanine derivatives and their use as receptor anatgonists 失效
标题翻译： β-丙氨酸衍生物及其作为受体拮抗剂的用途
公开(公告)号：US06812235B2
公开(公告)日：2004-11-02
申请号：US10182909
申请日：2002-08-02
申请人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Masatoshi Minagawa , Toshiaki Aoki , Kayoko Harada , Jiro Seki
发明人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Masatoshi Minagawa , Toshiaki Aoki , Kayoko Harada , Jiro Seki
IPC分类号： A61K31445
CPC分类号： C07K5/0202 , A61K38/00 , C07D211/60 , Y02P20/55
摘要： A beta-alanine derivative of the formula (I) wherein R1 is hydrogen atom or an amino protective group; A is a lower alkylene group or a lower alkenylene group; R2 is hydrogen atom or an amino group which may be substituted with an acyl group; R3 is hydrogen atom or an aryl or aralkyl group which may be substituted with one or more of hydroxy and/or lower alkoxy, a moiety represented by the formula (II), which is a bivalent N-containing 6- to 8-membered heterocyclic group, or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的β-丙氨酸衍生物，其中R 1是氢原子或氨基保护基; A是低级亚烷基或低级亚烯基; R 2是氢原子或可被酰基取代的氨基; R 3是氢原子或可以被一个或多个羟基和/或低级烷氧基取代的芳基或芳烷基，即由式（II）表示的部分，其是二价含N的6-8 杂环基或其药学上可接受的盐。

2. 发明授权

US06538007B1 N-[(R)-1-[3-(4-piperidyl)propionyl]-3-piperidylcarbonyl]-2(S)-acetylamino-&bgr;-alanine trihydrate, compositions thereof, and methods for its use 失效
标题翻译： N - [（R）-1- [3-（4-哌啶基）丙酰] -3-哌啶基羰基] -2（S） - 乙酰氨基-β-丙氨酸三水合物，其组合物及其使用方法
公开(公告)号：US06538007B1
公开(公告)日：2003-03-25
申请号：US09806483
申请日：2001-04-12
申请人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Hisashi Takasugi , Yosuke Fujii , Keiichi Koga , Eiki Oikawa , Ryoki Orii , Shunsuke Goto
发明人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Hisashi Takasugi , Yosuke Fujii , Keiichi Koga , Eiki Oikawa , Ryoki Orii , Shunsuke Goto
IPC分类号： A61K31445
CPC分类号： C07D211/60 , Y02P20/55
摘要： The trihydrates of &bgr;-alanine of the formula Are disclosed. Also method of antogonizing glycoprotein IIb/IIIa activity using these compounds is also disclosed.
摘要翻译：公开了β-丙氨酸的三水合物。还公开了使用这些化合物使糖蛋白IIb / IIIa活性钝化的方法。

3. 发明授权

US08211919B2 Amide derivatives as rock inhibitors 失效
标题翻译：酰胺衍生物作为岩石抑制剂
公开(公告)号：US08211919B2
公开(公告)日：2012-07-03
申请号：US12065043
申请日：2006-08-29
申请人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
发明人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
IPC分类号： A61K31/44 , A61K31/47 , A61K31/505 , A61K31/54 , C07D239/02 , C07D413/00 , C07D499/48
CPC分类号： C07D213/40 , C07D213/61 , C07D213/75 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要翻译：本发明涉及新颖的酰胺衍生物及其盐。更具体地说，本发明涉及作为ROCK抑制剂的新型酰胺衍生物及其盐，涉及包含该酰胺衍生物及其盐的治疗和/或预防ROCK相关疾病的方法。

4. 发明申请

US20090105231A1 AMIDE DERIVATIVES AS ROCK INHIBITORS 失效
标题翻译：酰胺衍生物作为岩石抑制剂
公开(公告)号：US20090105231A1
公开(公告)日：2009-04-23
申请号：US12065043
申请日：2006-08-29
申请人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
发明人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
IPC分类号： A61K31/541 , C07D213/56 , A61K31/4409 , A61K31/4725 , C07D409/12 , A61P25/28 , A61K31/506 , C07D401/12 , C07D417/12
CPC分类号： C07D213/40 , C07D213/61 , C07D213/75 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要翻译：本发明涉及新颖的酰胺衍生物及其盐。更具体地说，本发明涉及作为ROCK抑制剂的新型酰胺衍生物及其盐，涉及包含该酰胺衍生物及其盐的治疗和/或预防ROCK相关疾病的方法。

5. 发明授权

US06826033B2 Aminoalcohol derivatives 失效
标题翻译：氨基醇衍生物
公开(公告)号：US06826033B2
公开(公告)日：2004-11-30
申请号：US10380627
申请日：2003-03-21
申请人： Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
发明人： Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
IPC分类号： H01G902
CPC分类号： C07D207/416 , C07C233/43 , C07C233/62 , C07C233/80 , C07C235/56 , C07C275/40 , C07C275/42 , C07C275/54 , C07C311/08 , C07C2601/10 , C07C2601/14 , C07C2602/10 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/40 , C07D209/42 , C07D209/88 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D215/48 , C07D215/50 , C07D217/22 , C07D217/26 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D237/28 , C07D241/20 , C07D241/42 , C07D241/44 , C07D249/08 , C07D261/14 , C07D261/18 , C07D261/20 , C07D263/34 , C07D277/28 , C07D277/56 , C07D295/215 , C07D307/54 , C07D307/66 , C07D307/68 , C07D307/82 , C07D333/36 , C07D333/38 , C07D333/66 , C07D333/70 , C07D487/04 , Y02P20/55
摘要： The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.
摘要翻译：本发明涉及其中X 1为键或-O-CH 2 - ，（II）或（III）R 1为氢或氨基保护基的化合物式（I），a为苯基，吲哚基或咔唑基，各自为可以被一个或两个取代基取代，B是氢; 卤素; 低级烷基低级烷氧基羰基; 环（低级）烷基; 或杂环基，萘基，1,2,3,4-四氢萘基，苄基或苯基，其各自可以被一个或两个取代基取代，或其盐。本发明的化合物（I）及其药学上可接受的盐可用于预防和/或治疗感染或尿失禁。

6. 发明授权

US6124456A Pyrazolopyridine compound and pharmaceutical use thereof 失效
标题翻译：吡唑并吡啶化合物及其药物用途
公开(公告)号：US6124456A
公开(公告)日：2000-09-26
申请号：US147543
申请日：1999-01-19
申请人： Atsushi Akahane , Satoru Kuroda , Hiromichi Itani , Yasuyo Shimizu
发明人： Atsushi Akahane , Satoru Kuroda , Hiromichi Itani , Yasuyo Shimizu
IPC分类号： A61K31/501 , A61P1/04 , A61P3/10 , A61P9/00 , A61P11/06 , A61P13/12 , A61P25/00 , A61P37/06 , A61P43/00 , C07D471/04 , A61K31/497
CPC分类号： C07D471/04
摘要： A pyrazolopyridine compound of formula (I) wherein R.sup.1 is aryl, and R.sup.2 is lower alkyl substituted with unsaturated 3 to 8-membered heteromonocyclic group containing 1 or 2 sulfur atom(s) and 1 to 3 nitrogen atom(s) which may have one or more substituent(s); a group of formula (1) wherein R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl or acyl, R.sup.4 is hydrogen or hydroxy, A is lower alkylene, m is an integer of 0 or 1, and n is an integer of 1 or 2; a group of formula (2) wherein R.sup.5 and R.sup.6 are each lower alkyl; or quinuclidinyl, or a salt the The pyrazolopyridine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, etc.), anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure, and the like.
摘要翻译： PCT No.PCT / JP97 / 02493 Sec。 371日期1999年1月19日 102（e）1999年1月19日PCT PCT 1997年7月17日PCT公布。第WO98 / 03507号公报日本1998年1月29日，式（I）的吡唑并吡啶化合物，其中R1为芳基，R2为被1或2个硫原子和1〜3个氮原子（s）的不饱和3〜8元杂单环取代的低级烷基），其可以具有一个或多个取代基; 式（1）的基团，其中R 3是氢，低级烷基，芳基（低级）烷基或酰基，R 4是氢或羟基，A是低级亚烷基，m是0或1的整数，n是整数1 或2; 式（2）的基团，其中R 5和R 6各自为低级烷基; 或奎宁环基或其盐本发明的吡唑并吡啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默病，脑血管性痴呆，帕金森病等）），焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

7. 发明授权

US5286721A 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds 失效
标题翻译： 1-氮杂双环[3.2.0]庚-2-烯-2-羧酸化合物
公开(公告)号：US5286721A
公开(公告)日：1994-02-15
申请号：US853746
申请日：1992-06-12
申请人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
发明人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
IPC分类号： C07D477/14 , C07D477/00
CPC分类号： C07D477/14
摘要： 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds of the formula: ##STR1## in which R.sup.1 is carboxy, COO.sup.-- or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.8 is hydrogen or lower alkyl,Z is a group of the formula: ##STR2## wherein R.sup.3 is hydrogen; lower alkyl or lower alkenyl, each of which is optionally substituted by the group consisting of lower alkoxy, carbamoyl, hydroxy, halogen, mono(or di)(lower)alkylcarbamoyl, mono(or di)(lower)alkenylcarbamoyl, mono(or bis)[hydroxy(lower)alkyl]carbamoyl, optionally substituted cyclic-aminocarbonyl, acylamino, ureido, optionally substituted heterocyclic-carbonylamino, carbamoyloxy, mono(or di)(lower)alkylcarbamoyloxy, lower alkylthio, halo(lower)alkylthio, optionally substituted heterocyclicthio, optionally substituted heterocyclic group, optionally substituted aryl, and acyl;R.sup.9 is hydrogen or lower alkyl, andR.sup.10 is lower alkyl,or pharmaceutically acceptable salts thereof, which is useful as an antimicrobial agent.
摘要翻译： PCT No.PCT / JP91 / 01394 Sec。 371日期：1992年6月12日 102（e）日期1992年6月12日PCT 1991年10月14日PCT PCT。出版物WO92 / 06978 日期：4月30日，1992.1-氮杂双环（3.2.0）庚-2-烯-2-羧酸化合物，其结构式如下：（*化学结构*）其中R 1为羧基，COO-或被保护的羧基，R 2为羟基（低级）烷基或被保护的羟基（低级）烷基，R 8是氢或低级烷基，Z是下列基团：（*化学结构*）其中R 3是氢; 羟基，卤素，单（或二）（低级）烷基氨基甲酰基，单（或二）（低级）烯基氨基甲酰基，单（或双（低级））链烯基氨基甲酰基，）（羟基（低级）烷基）氨基甲酰基，任选取代的环氨基羰基，酰氨基，脲基，任选取代的杂环羰基氨基，氨基甲酰氧基，单（或二）（低级）烷基氨基甲酰氧基，低级烷硫基，卤（低级）烷硫基，，任选取代的杂环基，任选取代的芳基和酰基; R9为氢或低级烷基，R10为低级烷基，或其药学上可接受的盐，可用作抗微生物剂。

8. 发明授权

US5102877A 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds 失效
标题翻译： 1-氨基胆碱（3.2.0）HEPT-2-环己-2-羧酸化合物
公开(公告)号：US5102877A
公开(公告)日：1992-04-07
申请号：US508167
申请日：1990-04-12
申请人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
发明人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/14 , C07D519/00 , C07F7/18
CPC分类号： C07D477/14 , C07F7/186 , Y02P20/55
摘要： 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxyic acids having antimicrobial activity have been prepared.

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