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    Heat shock factor activity inhibitor
    1.
    发明授权
    Heat shock factor activity inhibitor 失效
    热休克因子活性抑制剂

    公开(公告)号：US06613780B2

    公开(公告)日：2003-09-02

    申请号：US09939901

    申请日：2001-08-27

    申请人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    发明人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    IPC分类号： A61K31445

    CPC分类号： C07D405/06

    摘要： A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    摘要翻译： 通过控制由热休克因子诱导的蛋白质的表达来提供疾病治疗。新化合物苯并-1,3-二氧杂环戊烷提供HSF活性的抑制剂或诱导由HSF调节的蛋白质的产生的抑制剂，其中 抑制热休克因子的活性，转录调节因子，从而进一步抑制基因区域中具有热休克元件序列的结构基因的转录，用于转录调节成RNA，从而抑制基因转化为蛋白质， 并导致抑制由该基因编码的RNA或蛋白质的产生。 它还提供通过热疗治疗或预防癌症的药物和用于治疗或预防压力疾病如抑郁症的药物。

    Methods of treating cancer using a heat shock factor activity inhibitor
    2.
    发明授权
    Methods of treating cancer using a heat shock factor activity inhibitor 失效
    使用热休克因子活性抑制剂治疗癌症的方法

    公开(公告)号：US06903116B2

    公开(公告)日：2005-06-07

    申请号：US10339063

    申请日：2003-01-09

    申请人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    发明人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    IPC分类号： C07D405/06 ,  A61K31/445 ,  A61K31/40

    CPC分类号： C07D405/06

    摘要： A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor.The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequenc in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    摘要翻译： 通过控制由热休克因子诱导的蛋白质的表达来提供疾病治疗。 新型化合物苯并-1,3-二氧杂环戊烷提供HSF活性的抑制剂或诱导由HSF调节的蛋白质产生的抑制剂，其抑制热休克因子（转录调节因子）的活性，从而进而抑制转录 在基因区域中具有用于转录调节RNA的热休克元件的结构基因的结构基因，从而抑制基因翻译成蛋白质，并导致抑制由该基因编码的RNA或蛋白质的产生。 它还提供通过热疗治疗或预防癌症的药物和用于治疗或预防压力疾病如抑郁症的药物。

    Heat shock factor activity inhibitors
    3.
    发明授权
    Heat shock factor activity inhibitors 失效
    热休克因子活性抑制剂

    公开(公告)号：US06281229B1

    公开(公告)日：2001-08-28

    申请号：US09446286

    申请日：2000-03-27

    申请人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    发明人： Shin-ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    IPC分类号： A61K31445

    CPC分类号： C07D405/06

    摘要： A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    摘要翻译： 通过控制由热休克因子诱导的蛋白质的表达来提供疾病治疗。新化合物苯并-1,3-二氧杂环戊烷提供HSF活性的抑制剂或诱导由HSF调节的蛋白质的产生的抑制剂，其中 抑制热休克因子的活性，转录调节因子，从而进一步抑制基因区域中具有热休克元件序列的结构基因的转录，用于转录调节成RNA，从而抑制基因转化为蛋白质， 并导致抑制由该基因编码的RNA或蛋白质的产生。 它还提供通过热疗治疗或预防癌症的药物和用于治疗或预防压力疾病如抑郁症的药物。

    Phenoxybenzene derivative
    5.
    发明授权
    Phenoxybenzene derivative 失效
    苯氧基苯衍生物

    公开(公告)号：US5270339A

    公开(公告)日：1993-12-14

    申请号：US938164

    申请日：1992-12-03

    申请人： Kozo Yamamoto ,  Yoshihide Fuse ,  Hideyuki Kishida ,  Naoko Yasuhara ,  Toshiaki Miwa ,  Ikuo Katsumi ,  Takayoshi Hidaka

    发明人： Kozo Yamamoto ,  Yoshihide Fuse ,  Hideyuki Kishida ,  Naoko Yasuhara ,  Toshiaki Miwa ,  Ikuo Katsumi ,  Takayoshi Hidaka

    IPC分类号： C07D207/08 ,  C07D207/20 ,  C07D207/24 ,  C07D207/26 ,  C07D207/36 ,  C07D405/12 ,  C07D207/06

    CPC分类号： C07D207/26 ,  C07D207/08 ,  C07D207/20 ,  C07D207/24 ,  C07D207/36 ,  C07D405/12

    摘要： There are described a phenoxybenzene derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom; an alkyl group having 1 to 3 carbon atoms; --OR.sup.6 or a halogen atom,R.sup.2 is hydrogen atom, nitro group or amino group,R.sup.3 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 5 carbon atoms, allyl group, vinyl group or --(CH.sub.2)n.sup.1 R.sup.7R.sup.4 is hydrogen atom, an alkyl group having 1 to 3 carbon atoms or --(CH.sub.2)n.sup.3 R.sup.25R.sup.5 hydrogen atom; an alkyl group having 1 to 3 carbon atoms; or phenyl group,X is ##STR2## wherein Y is oxygen atom or sulfur atom; or --CHR.sup.27 -- and line means a single bond or a double bond provided that n is 2 in case that the line means a single bond and n is 1 in case that the line means a double bond, ora pharmacologically acceptable salt thereof,a cognition enhancer comprising the same as an effective ingredient andan antidepressant comprising the same as an effective ingredient.

    摘要翻译： PCT No.PCT / JP92 / 00410 Sec。 371日期1992年12月3日 102（e）日期1992年12月3日PCT提交1992年4月2日PCT公布。 WO92 / 17447 PCT出版物 描述了具有式（I）的苯氧基苯衍生物：其中R 1是氢原子;（I）其中R 1是氢原子; 具有1至3个碳原子的烷基; -OR 6或卤原子，R 2为氢原子，硝基或氨基，R 3为氢原子，碳原子数1〜8的烷基，碳原子数3〜5的环烷基，烯丙基，乙烯基或 - （CH2）n1R7 R4为氢原子，碳原子数1〜3的烷基或 - （CH2）n3R25 R5氢原子; 具有1至3个碳原子的烷基; 或苯基，X是其中Y是氧原子或硫原子; 或-CHR27-，并且线表示单键或双键，条件是在线表示单键的情况下n为2，并且在该线表示双键的情况下n为1，或其药理学上可接受的盐， 包含与有效成分相同的认知增强剂和包含其作为有效成分的抗抑郁药。

    Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids
    6.
    发明授权
    Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids 有权
    制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰氨基酸的药理学可接受盐的方法

    公开(公告)号：US06335453B1

    公开(公告)日：2002-01-01

    申请号：US09269107

    申请日：1999-03-19

    申请人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    发明人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    IPC分类号： C07K5062

    CPC分类号： C07K5/0222 ,  C07K5/06026

    摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

    摘要翻译： 提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，和 形成其药理学上可接受的盐，其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

    Process for preparing pharmacologically acceptable salt of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid
    8.
    发明授权
    Process for preparing pharmacologically acceptable salt of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效
    制备正（（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法

    公开(公告)号：US06518436B2

    公开(公告)日：2003-02-11

    申请号：US09989186

    申请日：2001-11-21

    申请人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    发明人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    IPC分类号： C07D20704

    CPC分类号： C07K5/0222 ,  C07K5/06026

    摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S) -ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxy-anhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

    摘要翻译： 提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸， 并形成其药学上可接受的盐，其中通过在含水液体中进行一系列操作直至形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

    Process for producing 2-aralkylpropionic acid derivative
    10.
    发明申请
    Process for producing 2-aralkylpropionic acid derivative 审中-公开
    2-芳烷基丙酸衍生物的制备方法

    公开(公告)号：US20050143593A1

    公开(公告)日：2005-06-30

    申请号：US10501731

    申请日：2003-01-17

    申请人： Yoshihide Fuse ,  Koichi Kinoshita ,  Hiroaki Kawasaki

    发明人： Yoshihide Fuse ,  Koichi Kinoshita ,  Hiroaki Kawasaki

    IPC分类号： C07C51/235 ,  C07C303/30 ,  C07C309/66 ,  C07C327/32 ,  C07C327/22 ,  C07C51/16

    CPC分类号： C07C303/30 ,  C07B2200/07 ,  C07C51/235 ,  C07C327/32 ,  C07C309/66

    摘要： A process for easily and industrially advantageously producing a high-purity 2-aralkyl-3-acetylthiopropionic acid and a high-purity 2-aralkylpropionic acid having a leaving group in the 3-position from easily available compounds. A 2-aralkyl-1-propanol having a sulfonyloxy group or halogen atom in the 3-position is oxidized with a permanganate under acidic conditions to produce a high-purity 2-aralkylporpionic acid having sulfonyloxy or the halogen in the 3-position. This acid is reacted with a thioacetate in the presence of water to produce a high-purity 2-aralkyl-3-acetylthiopropionic acid.

    摘要翻译： 一种在容易获得的化合物中容易和工业上有利地制备高纯度2-芳烷基-3-乙酰硫基丙酸和在3-位具有离去基团的高纯度2-芳烷基丙酸的方法。 在酸性条件下，用高锰酸盐在3-位上具有磺酰氧基或卤素原子的2-芳烷基-1-丙醇在3-位上产生具有磺酰氧基或卤素的高纯度2-芳烷基糠酸。 该酸在水存在下与硫代乙酸酯反应以产生高纯度2-芳烷基-3-乙酰硫基丙酸。