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    Isoxazole derivatives as peroxisome proliferator-activated receptors agonists
    1.
    发明申请
    Isoxazole derivatives as peroxisome proliferator-activated receptors agonists 审中-公开
    异恶唑衍生物作为过氧化物酶体增殖物激活受体激动剂

    公开(公告)号：US20070054902A1

    公开(公告)日：2007-03-08

    申请号：US10581322

    申请日：2004-11-29

    申请人： Yoshikazu Fukui ,  Takasi Sasatani ,  Ken-ichi Sasatani ,  Natsuki Ishizuka ,  Toshisada Yano ,  Yasuhiko Kanda ,  Nobuo Chomei

    发明人： Yoshikazu Fukui ,  Takasi Sasatani ,  Ken-ichi Sasatani ,  Natsuki Ishizuka ,  Toshisada Yano ,  Yasuhiko Kanda ,  Nobuo Chomei

    IPC分类号： A61K31/5383 ,  A61K31/4245 ,  A61K31/42 ,  C07D413/14

    CPC分类号： C07D417/12 ,  C07D261/08 ,  C07D261/18 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12

    摘要： A compound of formula (I): (wherein R1-R10 are each independently hydrogen, halogen, optionally substituted lower alkyl or the like, X1 is —O—, —S—, —NR11— (wherein R11 is hydrogen, lower alkyl or the like), —CR12R13CO—, —(CR12R13)mO—, —O(CR12R13)m- (wherein R12 and R13 are each independently hydrogen or lower alkyl and m is a integer between 1 and 3) or the like, X2 is a bond, —O—, —S—, —NR14— (wherein R14 is hydrogen, lower alkyl or the like, R14 and R6 can be taken together with the neighboring atom to form a ring) or —CR15R16— (wherein R15 and R16 are each independently hydrogen or lower alkyl, R15 and R6 or R10 can be taken together with the neighboring carbon atom to form a ring, R16 and R9 can be joined together to form a bond), X3 is COOR17, C(═NR17)NR18OR19 or the like), a pharmaceutically acceptable salt or a solvate thereof.

    摘要翻译： 式（I）的化合物：其中R 1〜R 10各自独立地为氢，卤素，任选取代的低级烷基等，X 1， / SUP>是-O - ， - S - ， - NR 11 - （其中R 11是氢，低级烷基等），-CR 12 - （CR 12）13 - ， - （CR 12）， - （CR 12） （其中R 12和R 12各自独立地为氢或低级烷基，m为1和...之间的整数） 3）等，X 2是一个键，-O - ， - S-，-NR 14 - （其中R 14是 氢，低级烷基等，R 14和R 6可以与相邻原子一起形成环）或-CR 15 R 16 - （其中R 15和R 16各自独立地是氢或低级烷基，R 15和 R 6或R 10可以与相邻的碳原子一起形成环，R 16和R 9， S 可以连接在一起形成键），X 3是COOR 17，C（-NR 17）NR 18 其药学上可接受的盐或其溶剂化物。

    Isoxazole derivative and isothiazole derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1
    3.
    发明授权
    Isoxazole derivative and isothiazole derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1 有权
    具有抑制活性的异恶唑衍生物和异噻唑衍生物

    公开(公告)号：US08017638B2

    公开(公告)日：2011-09-13

    申请号：US12293246

    申请日：2007-03-28

    申请人： Tomoyuki Ogawa ,  Nobuo Chomei ,  Koji Masuda ,  Satoru Tanaka

    发明人： Tomoyuki Ogawa ,  Nobuo Chomei ,  Koji Masuda ,  Satoru Tanaka

    IPC分类号： A61K31/42 ,  C07D261/06

    CPC分类号： C07D261/18 ,  C07D275/02 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10

    摘要： Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is a group of the formula: —C(═O)NR4R5, (wherein R4 and R5 are each independently, hydrogen, optionally substituted alkyl or the like) or a group of the formula: —NR6C(═O)R7, (wherein R6 and R7 are each independently, hydrogen, optionally substituted alkyl or the like), X and Y are each independently —O— or the like, Z is a bond or the like, R2 is optionally substituted alkyl, optionally substituted alkenyl or the like, R3 is optionally substituted alkyl, optionally substituted alkenyl or the like.

    摘要翻译： 公开了一种可用作11型β-羟基类固醇脱氢酶抑制剂的化合物。下式表示的化合物：其药学上可接受的盐或溶剂合物，其中R 1是下式的基团：-C（= O）NR 4 R 5，（ 其中R 4和R 5各自独立地为氢，任选取代的烷基等）或下式的基团：-NR 6 C（= O）R 7，（其中R 6和R 7各自独立地为氢，任选取代的烷基等） X和Y各自独立地为-O-等，Z为键或类似物，R 2为任选取代的烷基，任选取代的烯基等，R 3为任选取代的烷基，任选取代的烯基等。

    Cyanoiminoquinoxaline derivatives
    4.
    发明授权
    Cyanoiminoquinoxaline derivatives 失效
    氰基亚氨基喹喔啉衍生物

    公开(公告)号：US06525054B1

    公开(公告)日：2003-02-25

    申请号：US09701383

    申请日：2000-12-01

    申请人： Susumu Takada ,  Nobuo Chomei ,  Tsuyoshi Kihara

    发明人： Susumu Takada ,  Nobuo Chomei ,  Tsuyoshi Kihara

    IPC分类号： C07D24144

    CPC分类号： C07D241/52 ,  C07D241/44 ,  C07D401/04 ,  C07D403/12

    摘要： A cyanoiminoquinoxaline derivative of the formula (II) is useful as a preventive or therapeutic agent for diseases due to hyperexcitation of glutamate receptors. (wherein, X and Y each is independently O or NCN, provided that at least one of X and Y is NCN; R1, R2, R3, and R4 each is independently hydrogen, halogen, nitro, optionally substituted heterocyclic group etc.; R5 is hydrogen etc.; R1 and R2, R2 and R3, R3 and R4, and R4 and R5, each taken together with the adjacent atoms may form a carbocycle which may be substituted or may contain a heteroatom(s).)

    摘要翻译： 式（II）的氰基亚氨基喹喔啉衍生物可用作由于谷氨酸受体过激引起的疾病的预防或治疗剂（其中，X和Y各自独立地为O或NCN，条件是X和Y中的至少一个为NCN ; R 1，R 2，R 3和R 4各自独立地为氢，卤素，硝基，任选取代的杂环基等; R 5为氢等; R 1和R 2，R 2和R 3，R 3和R 4以及R 4和R 5 与相邻的原子一起可以形成可以被取代或可以含有杂原子的碳环。）

    Process for the preparation of 3-isoxazolecarboxylic acid
    5.
    发明授权
    Process for the preparation of 3-isoxazolecarboxylic acid 失效
    3-异恶唑羧酸的制备方法

    公开(公告)号：US5696271A

    公开(公告)日：1997-12-09

    申请号：US687330

    申请日：1996-08-07

    申请人： Susumu Takada ,  Nobuo Chomei ,  Masaaki Uenaka

    发明人： Susumu Takada ,  Nobuo Chomei ,  Masaaki Uenaka

    IPC分类号： C07D261/04 ,  C07D261/18 ,  C07D263/34

    CPC分类号： C07D263/34 ,  C07D261/04 ,  C07D261/18 ,  Y02P20/55

    摘要： A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali: ##STR1## wherein R.sup.1 is a lower alkyl, R.sup.2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.

    摘要翻译： PCT No.PCT / JP95 / 00211 Sec。 371日期：1996年7月8日 102（e）日期1996年7月8日PCT提交1995年2月15日PCT公布。 公开号WO95 / 22533 日期1995年8月24日提供了制备用于制备有用化合物的中间体的3-异恶唑羧酸的方法，其特征在于式（I）化合物与羟胺反应，得到式 II），由如此得到的化合物用碱处理：其中R1是低级烷基，R2是羧基保护基，X是卤素原子，Y是一个 氢原子或X和Y一起可以形成单键。

    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11(beta)-HYDROXYSTEROID DEHYDROGENASE TYPE I
    6.
    发明申请
    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11(beta)-HYDROXYSTEROID DEHYDROGENASE TYPE I 有权
    含有11（β） - 羟基脱氢酶脱氢酶I型的异噻唑衍生物和异噻唑衍生物具有抑制活性

    公开(公告)号：US20090131491A1

    公开(公告)日：2009-05-21

    申请号：US12293246

    申请日：2007-03-28

    申请人： Tomoyuki Ogawa ,  Nobuo Chomei ,  Koji Masuda ,  Satoru Tanaka

    发明人： Tomoyuki Ogawa ,  Nobuo Chomei ,  Koji Masuda ,  Satoru Tanaka

    IPC分类号： A61K31/42 ,  C07D261/02 ,  A61P3/10

    CPC分类号： C07D261/18 ,  C07D275/02 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10

    摘要： Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is a group of the formula: —C(═O)NR4R5, (wherein R4 and R5 are each independently, hydrogen, optionally substituted alkyl or the like) or a group of the formula: —NR6C(═O)R7, (wherein R6 and R7 are each independently, hydrogen, optionally substituted alkyl or the like), X and Y are each independently —O— or the like, Z is a bond or the like, R2 is optionally substituted alkyl, optionally substituted alkenyl or the like, R3 is optionally substituted alkyl, optionally substituted alkenyl or the like.

    摘要翻译： 公开了用作11β-羟类固醇脱氢酶1型抑制剂的化合物。下式表示的化合物：其药学上可接受的盐或溶剂合物，其中R 1是下式的基团：-C（-O）NR 4 R 5，（其中 R 4和R 5各自独立地为氢，任选取代的烷基等）或下式-NR 6 C（-O）R 7的基团（其中R 6和R 7各自独立地为氢，任选取代的烷基等）， X和Y各自独立地为-O-等，Z为键或类似物，R 2为任选取代的烷基，任选取代的烯基等，R 3为任选取代的烷基，任选取代的烯基等。

    Oxopyridinylquinoxaline derivative
    7.
    发明授权
    Oxopyridinylquinoxaline derivative 失效
    氧吡嗪基喹喔啉衍生物

    公开(公告)号：US5677305A

    公开(公告)日：1997-10-14

    申请号：US418196

    申请日：1995-04-07

    申请人： Susumu Takada ,  Nobuo Chomei ,  Makoto Adachi ,  Masami Eigyo ,  Kazuo Kawasaki

    发明人： Susumu Takada ,  Nobuo Chomei ,  Makoto Adachi ,  Masami Eigyo ,  Kazuo Kawasaki

    IPC分类号： C07D401/04 ,  C07D241/36 ,  A01N43/60 ,  C07D241/38

    CPC分类号： C07D401/04

    摘要： An oxopyridinylquinoxaline derivative represented by the following Formula I or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1 is hydrogen, halogen, nitro, or trihalomethyl; R.sup.2 is hydrogen, halogen, nitro, cyano, trihalomethyl, carbamoyl, carbamoyl substituted with lower alkyl, sulfamoyl, or sulfamoyl substituted with lower alkyl; R.sup.3 is hydrogen, nitro, or halogen; R.sup.4 is hydrogen, lower alkyl, substituted lower alkyl, lower cycloalkyl, or substituted lower cycloalkyl; R.sup.5 's are substituents independently selected from the group consisting of halogen, nitro, cyano, lower alkyl, carbamoyl, and carbamoyl substituted with lower alkyl; and n is an integer of 0 to 4. The derivative works as an antagonistic agent against both the NMDA receptors and the AMPA receptors, so that it is effective as a therapeutic agent for neurological disorders caused by excitatory amino acids binding to the receptors.

    摘要翻译： 由下式I表示的氧代吡啶基喹喔啉衍生物或其药学上可接受的盐：其中R 1是氢，卤素，硝基或三卤代甲基; R2是氢，卤素，硝基，氰基，三卤甲基，氨基甲酰基，被低级烷基取代的氨基甲酰基，氨磺酰基或被低级烷基取代的氨磺酰基; R3是氢，硝基或卤素; R4是氢，低级烷基，取代的低级烷基，低级环烷基或取代的低级环烷基; R 5是独立地选自卤素，硝基，氰基，低级烷基，氨基甲酰基和被低级烷基取代的氨基甲酰基的取代基。 并且n为0至4的整数。该衍生物作为对NMDA受体和AMPA受体的拮抗剂起作用，因此其作为由与受体结合的兴奋性氨基酸引起的神经障碍的治疗剂是有效的。

    Process for the preparation of 3-isoxazolecarboxylic acid
    8.
    发明授权
    Process for the preparation of 3-isoxazolecarboxylic acid 失效
    3-异恶唑羧酸的制备方法

    公开(公告)号：US5760244A

    公开(公告)日：1998-06-02

    申请号：US901133

    申请日：1997-07-28

    申请人： Susumu Takada ,  Nobuo Chomei ,  Masaaki Uenaka

    发明人： Susumu Takada ,  Nobuo Chomei ,  Masaaki Uenaka

    IPC分类号： C07D261/04 ,  C07D261/18 ,  C07D263/34 ,  C07D261/08

    CPC分类号： C07D263/34 ,  C07D261/04 ,  C07D261/18 ,  Y02P20/55

    摘要： A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali: ##STR1## wherein R.sup.1 is a lower alkyl, R.sup.2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.

    摘要翻译： 提供了制备作为制备有用化合物的中间体的3-异恶唑羧酸的方法，所述方法的特征在于式（I）化合物与羟胺反应得到式（II）化合物， 如下得到的化合物用碱处理：其中R 1是低级烷基，R 2是羧基保护基，X是卤素原子，Y是氢原子，或X 和Y一起可以形成单键。