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    Amidino substituted tetrahydrobenzo thiophene or furan derivatives and their use as urokinase inhibitors
    1.
    发明授权
    Amidino substituted tetrahydrobenzo thiophene or furan derivatives and their use as urokinase inhibitors 失效
    脒基取代的四氢苯并噻吩或呋喃衍生物及其用作尿激酶抑制剂

    公开(公告)号：US06274619B1

    公开(公告)日：2001-08-14

    申请号：US09584136

    申请日：2000-05-31

    Applicant: Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

    Inventor： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

    IPC: C07D30785

    CPC classification number: C07D513/04 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  Y02P20/55

    Abstract: A compound of the formula: in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, —S— or —SO2—, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.

    Abstract translation: 下式化合物：其中R 1为氢，任选取代的低级烷基氨基甲酰基（低级）亚烷基，低级亚烷基，低级烷基，任选取代的芳（低级）烷基，环（低级）烷基（低级）烷基，被保护的羧基 ，羧基（低级）烷基，羟基（低级）烷基，任选取代的低级烷基氨基甲酰基（低级）烷基，低级烷硫基（低级）烷基，羧基（低级）烷酰基，受保护羧基（低级）烷酰基，芳酰基，低级烷酰基或任选取代 芳基氨基甲酰基（低级）烷基，R2是氢，羧基，保护的羧基，甲酰基或N-（低级）烷基-N-（低级）烷氧基氨基甲酰基，R3是氢或脒基保护基，A是低级亚烷基或羰基，X是Y 低级亚烷基，-S-或-SO 2 - ，Z是-S-或-O-，并且行：是 单键或双键，或其药学上可接受的盐，其可用作药物。

    Benzothiophene derivatives, their preparation and use as urokinase inhibitors
    2.
    发明授权
    Benzothiophene derivatives, their preparation and use as urokinase inhibitors 失效
    苯并噻吩衍生物，其制备和用作尿激酶抑制剂

    公开(公告)号：US6093710A

    公开(公告)日：2000-07-25

    申请号：US147812

    申请日：1999-03-12

    Applicant: Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

    Inventor： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

    IPC: C07D333/24 ,  A61K31/343 ,  A61K31/381 ,  A61K31/542 ,  A61P9/00 ,  A61P15/18 ,  A61P19/02 ,  A61P19/10 ,  A61P27/02 ,  A61P35/00 ,  C07D307/82 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  C07D513/04 ,  C07D493/04 ,  C07D495/04

    CPC classification number: C07D513/04 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  Y02P20/55

    Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy)lower)alkyl, carboxy)lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl,R.sup.2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl,R.sup.3 is hydrogen or amidino-protective group,A is lower alkylene or carbonyl,X is ##STR2## Y is --S-- or --SO.sub.2 --, Z is --S-- or --O--,or pharmaceutically acceptable salts thereofwhich is useful as a medicament.

    Abstract translation: PCT No.PCT / JP97 / 03215 Sec。 371 1999年3月12日 102（e）1999年3月12日PCT PCT 1997年9月12日PCT公布。 出版物WO98 / 11089 日本公开的化合物，其中R 1为氢，低级烷基，任选取代的芳（低级）烷基，环（低级）烷基（低级）烷基，被保护的羧基）低级烷基，羧基）低级）烷基， 羟基（低级）烷基，任选取代的低级烷基氨基甲酰基（低级）烷基，低级烷硫基（低级）烷基，羧基（低级）烷酰基，受保护的羧基（低级）烷酰基，芳酰基，低级烷酰基或任选取代的芳基氨基甲酰基 （低级）烷基-N-（低级）烷氧基氨基甲酰基，R3是氢或脒基保护基，A是低级亚烷基或羰基，X是Y是-S-或-SO2 - ，Z是-S-或-O-，或其药学上可接受的盐，其可用作药物。

    PKC-EPSILON ACTIVATOR
    3.
    发明申请
    PKC-EPSILON ACTIVATOR 有权

    公开(公告)号：US20130331454A1

    公开(公告)日：2013-12-12

    申请号：US13885751

    申请日：2011-11-15

    Applicant: Tomoyuki Nishizaki ,  Akito Tanaka

    Inventor： Tomoyuki Nishizaki ,  Akito Tanaka

    IPC: C07C53/132

    CPC classification number: C07C53/132 ,  A61K31/235 ,  C07B2200/07

    Abstract: The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-ε activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient.A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-ε activator containing same as an active ingredient, and is the like.

    Abstract translation: 本发明旨在获得DCP-LA的光学异构体，其表现出更优异的活性并且适用于临床应用，并提供具有优异PKC-ε活化作用的药剂，用于神经递质释放障碍的预防和/或治疗剂 ，以及含有异构体作为活性成分的神经精神疾病的预防和/或治疗剂。 由下式表示的化合物或其药学上可接受的盐以及含有作为活性成分的选择性PKC-ε活化剂等。

    NOVEL TARGET PROTEIN OF ANTICANCER AGENT AND NOVEL ANTICANCER AGENT (SPNAL) CORRESPONDING THERETO
    4.
    发明申请
    NOVEL TARGET PROTEIN OF ANTICANCER AGENT AND NOVEL ANTICANCER AGENT (SPNAL) CORRESPONDING THERETO 审中-公开
    新药抗体药剂和新型抗感染药物（SPNAL）相关药物的新目标蛋白

    公开(公告)号：US20110189789A1

    公开(公告)日：2011-08-04

    申请号：US12632905

    申请日：2009-12-08

    Applicant: Akito Tanaka ,  Akira Yamazaki ,  Takeshi Tsutsumi ,  Tomohiro Terada ,  Masayuki Haramura

    Inventor： Akito Tanaka ,  Akira Yamazaki ,  Takeshi Tsutsumi ,  Tomohiro Terada ,  Masayuki Haramura

    IPC: G01N33/53

    CPC classification number: C07D231/12 ,  A61K45/06 ,  C07C317/44 ,  C07C323/62

    Abstract: The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.

    Abstract translation: 本发明提供含有与KSRP或其功能片段特异性结合的化合物作为活性成分的药物组合物和该化合物的筛选方法。 KSRP是抗癌剂的新型靶蛋白; 能够调节这种蛋白质的表达和活性的化合物和含有该蛋白质的药物组合物对于增殖性疾病，特别是作为抗癌剂是非常有用的。 通过提供新的靶蛋白，可以阐明通常不可解释的抗癌作用背后的机制。

    Solid support having ligand immobilized thereon by using photocleavable linker
    7.
    发明授权
    Solid support having ligand immobilized thereon by using photocleavable linker 有权
    通过使用可光致发光的接头，其上固定有配体的固体支持物

    公开(公告)号：US07456022B2

    公开(公告)日：2008-11-25

    申请号：US11572972

    申请日：2005-07-28

    Applicant: Masayuki Haramura ,  Akito Tanaka

    Inventor： Masayuki Haramura ,  Akito Tanaka

    IPC: B01J20/26 ,  G01N33/547

    CPC classification number: B01J20/289 ,  B01J20/261 ,  B01J20/286 ,  B01J20/321 ,  B01J20/3219 ,  B01J20/3251 ,  B01J20/3253 ,  B01J20/3255 ,  B01J2220/54 ,  G01N33/54353 ,  Y10T436/207497

    Abstract: The present invention provides a method of analyzing the interaction between a ligand and a target molecule, which uses a solid support wherein the ligand is immobilized via a linker cleavable by photoirradiation, particularly a method of searching and purifying a target molecule. By intervening a linker specifically cleavable by photoirradiation between the ligand molecule and the solid support, release and elution of the target molecule from the solid support without using a ligand or salt at a high concentration can be enabled, and suppression of release and elution of a nonspecific protein can be enabled.

    Abstract translation: 本发明提供了一种分析配体和靶分子之间的相互作用的方法，其使用固体支持物，其中通过光照射可切割的接头固定配体，特别是搜索和纯化靶分子的方法。 通过插入通过配体分子和固体支持体之间的光照射可以特异性地切割的接头，可以使得目标分子从固体支持物中释放和洗脱而不使用高浓度的配体或盐，并且抑制释放和洗脱 可以启用非特异性蛋白质。

    PKC-ε activator
    10.
    发明授权
    PKC-ε activator 有权
    PKC-＆egr 活化剂

    公开(公告)号：US09012500B2

    公开(公告)日：2015-04-21

    申请号：US13885751

    申请日：2011-11-15

    Applicant: Tomoyuki Nishizaki ,  Akito Tanaka

    Inventor： Tomoyuki Nishizaki ,  Akito Tanaka

    IPC: A61K31/235 ,  C07C53/132

    CPC classification number: C07C53/132 ,  A61K31/235 ,  C07B2200/07

    Abstract: The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-ε activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient.A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-ε activator containing same as an active ingredient, and is the like.

    Abstract translation: 本发明旨在获得DCP-LA的光学异构体，其具有更优异的活性并且适用于临床应用，并提供具有优异PKC- 活化作用，神经递质释放障碍的预防和/或治疗剂，以及含有异构体作为活性成分的神经精神疾病的预防和/或治疗剂。 由下式表示的化合物或其药学上可接受的盐和选择性PKC- 含有与活性成分相同的活化剂，等等。

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