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    Pyrazolo�1,5-A!pyrimidine derivatives and anti-inflammatory agent containing the same
    1.
    发明授权
    Pyrazolo�1,5-A!pyrimidine derivatives and anti-inflammatory agent containing the same 失效
    吡唑并[1,5-A]嘧啶衍生物和含有它们的抗炎剂

    公开(公告)号：US5688949A

    公开(公告)日：1997-11-18

    申请号：US133086

    申请日：1993-10-07

    申请人： Makoto Inoue ,  Kinji Hashimoto ,  Toshiko Kuwahara ,  Yukio Sugimoto ,  Takuji Uesako ,  Toshiaki Funato

    发明人： Makoto Inoue ,  Kinji Hashimoto ,  Toshiko Kuwahara ,  Yukio Sugimoto ,  Takuji Uesako ,  Toshiaki Funato

    IPC分类号： A61K31/505 ,  A61P29/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Pyrazolo�1,5-a!pyrimidine derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, carboxyl, lower alkoxy-carbonyl, phenyl, lower alkyl optionally having a substituent selected from OH, carboxyl and lower alkoxy-carbonyl, or cycloalkyl, or R.sub.1 and R.sub.2 may combine each other to form lower alkylene; R.sub.5 is group of --SR.sub.6 or group of --NR.sub.7 R.sub.8 in which R.sub.6 is pyridyl or phenyl optionally having 1 to 3 substituents selected from OH and lower alkyl; and R.sub.7 and R.sub.8 are H, phenyl optionally having 1 to 3 substituents selected from OH, lower alkyl, lower alkoxycarbonyl and carboxyl, or R.sub.7 and R.sub.8 may combine each other to form with a nitrogen atom with which they bond 1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, or 1-piperazinyl group substituted by a phenyl group optionally being substituted by halogen or trihalomethyl, hydroxy-lower alkyl or diphenyl-lower alkyl, or a salt thereof, and anti-inflammatory agent containing as active ingredient compound of the above formula, wherein R.sub.1, R.sub.3 and R.sub.4 are H, R.sub.2 is lower alkyl or cycloalkyl, R.sub.5 is group of --NR.sub.7 R.sub.8 (R.sub.7 is H, R.sub.8 is phenyl substituted by OH and two lower alkyl).

    摘要翻译： PCT No.PCT / JP91 / 01043 Sec。 371日期：1993年10月7日 102（e）日期1993年10月7日PCT 1991年8月6日PCT PCT。 出版物WO92 / 18504 日期：1992年10月29日具有下式的吡唑并[1,5-a]嘧啶衍生物：其中R1，R2，R3和R4是H，羧基，低级烷氧基 - 羰基，苯基，任选具有选自 OH，羧基和低级烷氧基 - 羰基或环烷基，或者R 1和R 2可以相互结合形成低级亚烷基; R5是-SR6或-NR7R8基团的基团，其中R6是吡啶基或任选具有1至3个选自OH和低级烷基的取代基的苯基; 并且R 7和R 8是H，任选具有1至3个选自OH，低级烷基，低级烷氧基羰基和羧基的取代基的苯基，或者R 7和R 8可以彼此结合形成氮原子，与它们键合1-吡咯烷基， 被卤素或三卤代甲基，羟基 - 低级烷基或二苯基 - 低级烷基或其盐任选取代的苯基取代的1-氧代-1-吡咯烷基或1-哌嗪基，以及含有作为活性成分的化合物的抗炎剂 其中R1，R3和R4是H，R2是低级烷基或环烷基，R5是-NR7R8基团（R7是H，R8是被OH取代的苯基和两个低级烷基）。

    Pyrazolo[1,5-a]pyrimidine derivatives
    2.
    发明授权
    Pyrazolo[1,5-a]pyrimidine derivatives 失效
    吡唑并[1,5-a]嘧啶衍生物

    公开(公告)号：US5985882A

    公开(公告)日：1999-11-16

    申请号：US930974

    申请日：1997-10-10

    申请人： Makoto Inoue ,  Takashi Okamura ,  Yasuo Shoji ,  Kinji Hashimoto ,  Masayuki Ohara ,  Tsuneo Yasuda

    发明人： Makoto Inoue ,  Takashi Okamura ,  Yasuo Shoji ,  Kinji Hashimoto ,  Masayuki Ohara ,  Tsuneo Yasuda

    IPC分类号： C07D487/04 ,  A61K31/505 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The invention provides pyrazolo[1,5-a]pyrimidine derivatives which are useful as potent analgesics and represented by the formula ##STR1## wherein R.sup.1 is lower alkenyl, hydroxy(lower)alkyl, (lower)alkylthio(lower)alkyl, (lower)alkanoyloxy(lower)alkyl, (lower)alkoxy(lower)alkyl, furyl or thienyl, R.sup.2 is pyridyl, 1-oxide-pyridyl, lower alkyl-substituted pyrazinyl, lower alkyl-substituted pyrimidinyl, or phenyl which may have 1 to 3 substituents selected from the group consisting of lower alkyl, lower alkoxy and halogen, R.sup.3 is hydrogen or halogen, and A is a single bond or lower alkylene.

    摘要翻译： PCT No.PCT / JP96 / 00955 Sec。 371日期：1997年10月10日 102（e）1997年10月10日PCT PCT 1996年4月5日PCT公布。 公开号WO96 / 32394 日期：1996年10月17日本发明提供了吡唑并[1,5-a]嘧啶衍生物，其可用作强力止痛剂并由下式表示：其中R1为低级烯基，羟基（低级）烷基，（低级）烷硫基（低级）烷基， （低级）烷酰氧基（低级）烷基，（低级）烷氧基（低级）烷基，呋喃基或噻吩基，R2是吡啶基，1-氧化物 - 吡啶基，低级烷基取代的吡嗪基，低级烷基取代的嘧啶基或苯基， 至3个选自低级烷基，低级烷氧基和卤素的取代基，R3为氢或卤素，A为单键或低级亚烷基。

    Pyrimidine derivatives, method of manufacturing the same, and androgen inhibitor
    3.
    发明授权
    Pyrimidine derivatives, method of manufacturing the same, and androgen inhibitor 失效

    公开(公告)号：US5420128A

    公开(公告)日：1995-05-30

    申请号：US854619

    申请日：1992-06-09

    申请人： Hiroshi Kiyokawa ,  Satoshi Yamada ,  Keisuke Miyajima ,  Kinji Hashimoto ,  Masatoshi Inai ,  Makoto Inoue ,  Kunihiko Tatsumi ,  Takeshi Yamauchi ,  Kazunobu Kurisu ,  Yoshifumi Chone

    发明人： Hiroshi Kiyokawa ,  Satoshi Yamada ,  Keisuke Miyajima ,  Kinji Hashimoto ,  Masatoshi Inai ,  Makoto Inoue ,  Kunihiko Tatsumi ,  Takeshi Yamauchi ,  Kazunobu Kurisu ,  Yoshifumi Chone

    IPC分类号： C07D487/04 ,  A61K31/53 ,  A61K31/505 ,  C07D231/38

    CPC分类号： C07D487/04

    摘要： The invention discloses a pyrimidien derivative expressed in Formula [I]: ##STR1## where R.sup.1 denotes a hydrogen atom or hydroxyl group, R.sup.2 denotes a hydrogen atom, lower alkoxycarbonyl group, lower alkoxy group, halogen atom, lower alkyl group, cycloalkyl group with 3 to 8 carbon atoms, lower alkoxycarbonyl lower alkyl group, carboxyl group, carboxy lower alkyl group, group: --CONHR.sup.6 (R.sup.6 represents a hydrogen atom, a phenyl group, which may possess halogen atom, or lower alkyl group), cyano group, phenyl group which may possess a group selected from the group consisting of hydroxyl group, halogen atom, lower alkyl group, lower alkoxy group and phenylthio group as a substituent, phenyl lower alkyl group which may possess a group selected from the group consisting of hydroxyl group and lower alkoxy group as a substituent on a phenyl ring, lower alkanoyloxy lower alkyl group, benzoyl group, lower alkanoyl group which may possess a halogen atom, or hydroxy lower alkyl group which may possess a group selected from the group consisting of phenyl group and halogen atom as a substituent, R.sup.3 denotes a hydrogen atom, hydroxyl group, lower alkyl group, cycloalkyl group with 3 to 8 carbon atoms, halogen lower alkyl group, or phenyl group, R.sup.4 denotes a hydrogen atom, lower alkyl group, or lower alkoxy group, and R.sup.5 denotes a hydrogen atom, lower alkyl group, lower alkoxy lower alkyl group, or halogen lower alkyl group; provided that R.sup.2 and R.sup.3 may be bonded to each other to form a lower alkylene group with 3 to 5 carbon atoms, or its pharmaceutically available salt. This derivative is excellent in therapeutic effects of benign prostatic hypertrophy, prostatic carcinoma, female hairiness, male baldness or pimple as an androgen inhibitor.

    Pyrazolo�1,5-a!pyrimidine derivative
    6.
    发明授权
    Pyrazolo�1,5-a!pyrimidine derivative 失效
    吡唑并[1,5-a]嘧啶衍生物

    公开(公告)号：US5707997A

    公开(公告)日：1998-01-13

    申请号：US602824

    申请日：1996-02-21

    申请人： Yasuo Shoji ,  Makoto Inoue ,  Takashi Okamura ,  Kinji Hashimoto ,  Masayuki Ohara ,  Tsuneo Yasuda

    发明人： Yasuo Shoji ,  Makoto Inoue ,  Takashi Okamura ,  Kinji Hashimoto ,  Masayuki Ohara ,  Tsuneo Yasuda

    IPC分类号： C07D487/04 ,  A61K31/505 ,  C07D403/02

    CPC分类号： C07D487/04

    摘要： The invention provides a pyrazolo�1,5-a!pyrimidine derivative of the following formula (1): ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, Q, A and n are defined in the description; and R.sup.2 is naphthyl, cycloalkyl, furyl, thienyl, optionally halogen-substituted pyridyl, optionally halogen-substituted phenoxy, or phenyl which may have 1 to 3 substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro, halogen-substituted lower alkyl, halogen-substituted lower alkoxy, lower alkoxycarbonyl, hydroxyl, phenyl(lower)alkoxy, amino, cyano, lower alkanoyloxy, phenyl and di(lower)alkoxyphos-phoryl(lower)alkyl. This derivative is useful as a potent analgesic.

    摘要翻译： PCT No.PCT / JP95 / 01104 Sec。 371日期1996年2月21日 102（e）日期1996年2月21日PCT提交1995年6月5日PCT公布。 出版物WO95 / 35298 日期：1995年12月28日本发明提供下述通式（1）的吡唑并[1,5-a]嘧啶衍生物：d n在说明书中定义; R 2为萘基，环烷基，呋喃基，噻吩基，任选卤素取代的吡啶基，任选卤素取代的苯氧基，或可具有1至3个选自低级烷基，低级烷氧基，卤素，硝基， 取代的低级烷基，卤素取代的低级烷氧基，低级烷氧基羰基，羟基，苯基（低级）烷氧基，氨基，氰基，低级烷酰氧基，苯基和二（低级）烷氧基磷酰基（低级）烷基。 该衍生物作为有效的止痛剂是有用的。

    System for notifying mail-receiving error information
    7.
    发明授权
    System for notifying mail-receiving error information 有权
    用于通知邮件接收错误信息的系统

    公开(公告)号：US08825771B2

    公开(公告)日：2014-09-02

    申请号：US12716012

    申请日：2010-03-02

    申请人： Makoto Inoue

    发明人： Makoto Inoue

    IPC分类号： G06F15/16 ,  H04L12/58 ,  G06Q10/10

    CPC分类号： G06Q10/107 ,  H04L51/22 ,  H04L51/24

    摘要： In a case where mail can not be stored in a mail box in a mail receiving server due to capacity excess, a detail content of the mail can be notified to an addressee of the mail. A mail receiving server comprises a mail receiving unit, a first mail box, a determining unit, a temporal storage space, an extracting unit, an information notice mail managing unit, and a second mail box.

    摘要翻译： 在由于容量过剩而不能将邮件存储在邮件接收服务器的邮箱中的情况下，可以将邮件的详细内容通知邮件的收件人。 邮件接收服务器包括邮件接收单元，第一邮箱，确定单元，临时存储空间，提取单元，信息通知邮件管理单元和第二邮箱。