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    3(2H)pyridazinone, and antagonistic agent against SRS-A containing it
    1.
    发明授权
    3(2H)pyridazinone, and antagonistic agent against SRS-A containing it 失效
    3（2H）哒嗪酮，和含有它的SRS-A拮抗剂

    公开(公告)号：US4978665A

    公开(公告)日：1990-12-18

    申请号：US144173

    申请日：1988-01-15

    申请人： Keizo Tanikawa ,  Ryozo Sakoda ,  Ken-ichi Shikada ,  Sakuya Tanaka

    发明人： Keizo Tanikawa ,  Ryozo Sakoda ,  Ken-ichi Shikada ,  Sakuya Tanaka

    IPC分类号： A61K31/50 ,  A61P37/08 ,  C07D237/22

    CPC分类号： C07D237/22

    摘要： A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen, 2-propenyl or straight chained or branched C.sub.1 -C.sub.4 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; X is chlorine or bromine; Y is hydrogen, nitro, -NHR.sub.3 wherein R.sub.3 is hydrogen or straight chained or branched C.sub.1 -C.sub.4 alkyl, -AR.sub.4 wherein A is oxygen or sulfur and R.sub.4 is hydrogen, straight chained or branched C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl having one double bond, C.sub.3 -C.sub.6 alkynyl having one triple bond, phenyl or ##STR2## wherein R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl, or halogen; Z.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, -OR.sub.6 wherein R.sub.6 is hydrogen, straight chained or branched C.sub.1 -C.sub.8 alkyl or ##STR3## wherein n is an integer of from 1 to 4, -N(R.sub.7).sub.2 wherein R.sub.7 is C.sub.1 -C.sub.4 alkyl, or halogen; Z.sub.2 is C.sub.1 -C.sub.4 alkyl, -OR.sub.6 wherein R.sub.6 is as defined above, -N(R.sub.7).sub.2 wherein R.sub.7 is as defined above, or halogen, provided that when R.sub.1 is straight chained or branched C.sub.2 -C.sub.4 alkyl, Y is not hydrogen and when R.sub.1 is hydrogen, methyl or 2-propenyl, Y and R.sub.2 are not simultaneously hydrogen, or a pharmaceutically acceptable salt thereof.

    3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it
    3.
    发明授权
    3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it 失效
    3（2H）哒嗪酮，其制备方法和含有它的抗过敏剂

    公开(公告)号：US4892947A

    公开(公告)日：1990-01-09

    申请号：US854521

    申请日：1986-04-22

    申请人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    发明人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    IPC分类号： A61K31/50 ,  C07D237/22

    CPC分类号： A61K31/50 ,  C07D237/22

    摘要： A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen, methyl, C.sub.3 -C.sub.6 alkenyl, C.sub.5 or C.sub.6 cycloalkyl, benzyl, phenyl, --(CH.sub.2).sub.m CO.sub.2 R.sub.3 (wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.5 alkyl, and m is an integer of from 1 to 4), --(CH.sub.2).sub.n A (wherein A is --OH or --N(R.sub.4).sub.2 wherein R.sub.4 is C.sub.1 -C.sub.3 alkyl, and n is an integer of from 2 to 6) or --CH.sub.2 CF.sub.3 ; R.sub.2 is chlorine or bromine; each of Y.sub.1 and Y.sub.2 which may be the same or different, is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --OR.sub.5 (wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.8 alkyl or ##STR2## wherein q is an integer of from 1 to 4), --CO.sub.2 R.sub.6 (wherein R.sub.6 is hydrogen or C.sub.1 -C.sub.5 alkyl), --N(R.sub.7).sub.2 (wherein R.sub.7 is C.sub.1 -C.sub.4 alkyl) or --SR.sub.8 (wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl); and Y.sub.3 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --OR.sub.5 (wherein R.sub.5 is as defined above), --CO.sub.2 R.sub.6 (wherein R.sub.6 is as defined above), --N(R.sub.7).sub.2 (wherein R.sub.7 is as defined above) or --SR.sub.8 (wherein R.sub.8 is as defined above), or a pharmaceutically acceptable salt thereof.

    摘要翻译： 具有下式的3（2H）哒嗪酮：其中R 1是氢，甲基，C 3 -C 6烯基，C 5或C 6环烷基，苄基，苯基， - （CH 2）m CO 2 R 3（其中R 3是氢或C1- C5烷基，m为1〜4的整数）， - （CH2）nA（其中A为-OH或-N（R4）2，其中R4为C1-C3烷基，n为2〜 6）或-CH 2 CF 3; R2是氯或溴; 可以相同或不同的Y 1和Y 2各自为氢，C 1 -C 5烷基，C 2 -C 8烯基，卤素，-OR 5（其中R 5为氢，C 1 -C 8烷基或其中q为 1至4），-CO 2 R 6（其中R 6是氢或C 1 -C 5烷基），-N（R 7）2（其中R 7是C 1 -C 4烷基）或-SR 8（其中R 8是C 1 -C 4烷基）; 并且Y 3是C 1 -C 5烷基，C 2 -C 8烯基，卤素，-OR 5（其中R 5如上定义），-CO 2 R 6（其中R 6如上定义），-N（R 7）2（其中R 7如上所述 ）或-SR 8（其中R8如上定义）或其药学上可接受的盐。

    3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it
    6.
    发明授权
    3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 失效
    3（2H）吡咯烷酮，其制备方法和含有其的抗过敏剂

    公开(公告)号：US5098900A

    公开(公告)日：1992-03-24

    申请号：US180599

    申请日：1988-04-11

    申请人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    发明人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    IPC分类号： A61K31/50 ,  A61K31/535 ,  A61P11/00 ,  A61P11/08 ,  A61P27/16 ,  A61P37/08 ,  C07D237/00 ,  C07D237/14 ,  C07D237/22 ,  C07D317/00 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D237/22 ,  Y10S514/826

    摘要： A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.sub.3 is as defined above) or --CH.sub.2 OR.sub.7 (wherein R.sub.7 is as defined above), and q is an integer of 1 to 5]], --CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CON(R.sub.10) (R.sub.11) [wherein each of R.sub.10 and R.sub.11 which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.5 alkenyl, or R.sub.10 and R.sub.11 together form C.sub.4 -C.sub.6 alkylene, --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 N(R.sub.6)(CH.sub.2).sub.2 -- (wherein R.sub.6 is as defined above)], --CONH(CH.sub.2).sub.m A (wherein A is as defined above, and m is an integer of 2 to 4), --CH.dbd.CHCOR.sub.12 (wherein R.sub.12 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --N(R.sub.13) (CH.sub.2).sub.n CO.sub.2 R.sub.3 (wherein R.sub.13 is hydrogen, C.sub.1 -C.sub.6 alkyl or cycloalkyl, R.sub.3 is as defined above, and n is an integer of 1 to 4)), --SR.sub.14 (wherein R.sub.14 is C.sub.1 -C.sub.4 alkyl), --CN or ##STR2## wherein R.sub.3 is as defined above), or two of Y.sub.1, Y.sub.2 and Y.sub.3 together form ##STR3## (wherein p is an integer of 1 or 2), and a pharmaceutically acceptable salt thereof.

    摘要翻译： 具有下式的3（2H）哒嗪酮：其中R 1是C 2 -C 5烷基; R2是氢，C1-C3烷基，氯或溴; R3是氢或C1-C4烷基; 并且可以相同或不同的Y 1，Y 2和Y 3各自为氢，C 1 -C 8烷基，C 2 -C 8烯基，卤素， - （CH 2）l A [其中A为式-N（R 4） （R 5）（其中可以相同或不同的R 4和R 5各自为C 1 -C 4烷基，或R 4和R 5一起形成C 4 -C 6亚烷基），吗啉代，4-R 6 - 哌嗪-1-基（其中R 6 是C 1 -C 3烷基）或-OR 7（其中R 7是氢或C 1 -C 3烷基），l是0-3的整数]，-OR 8 [其中R8是氢，C1-C8烷基，C3-C5链烯基， 苄基或 - （CH 2）q -R 9 [其中R 9是CO 2 R 3（其中R 3如上定义），-CONHR 3（其中R 3如上定义）或-CH 2 OR 7（其中R 7如上所定义），q是整数 1〜5]]，-CO 2 R 3（其中R 3如上定义），-CON（R 10）（R 11）[其中R 10和R 11可以相同或不同，为氢，C 1 -C 4烷基或C 3 （CH 2）2 O（CH 2）2 - 或 - （CH 2）2 N（R 6）（CH 2）2 - （其中R 6如上所定义）]， - （C 1 -C 6）烷基，或者R 10和R 11一起形成C 1 -C 6亚烷基， CONH（CH2）mA（其中 在A中如上所定义，m为2〜4的整数），-CH = CHCOR 12（其中，R 12为羟基，C 1〜C 4烷氧基或-N（R 13）（CH 2）n CO 2 R 3（式中，R 13为氢， C6烷基或环烷基，R3如上所定义，n是1至4的整数）），-SR 14（其中R 14是C 1 -C 4烷基），-CN或其中R 3如上定义），或 Y1，Y2和Y3中的两个一起形成（其中p为1或2的整数）及其药学上可接受的盐。

    3(2H)pyridazinone, and anti-allergic agent containing it
    7.
    发明授权
    3(2H)pyridazinone, and anti-allergic agent containing it 失效
    3（2H）哒嗪酮和含有它的抗过敏剂

    公开(公告)号：US4783462A

    公开(公告)日：1988-11-08

    申请号：US833607

    申请日：1986-02-27

    申请人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    发明人： Motoo Mutsukado ,  Keizo Tanikawa ,  Ken-ichi Shikada ,  Ryozo Sakoda

    IPC分类号： A61K31/50 ,  A61P11/00 ,  A61P11/08 ,  A61P27/16 ,  A61P37/08 ,  C07D237/00 ,  C07D237/16 ,  C07D237/22 ,  C07D403/12 ,  C07D405/12 ,  C07D237/06

    CPC分类号： C07D403/12 ,  C07D237/16 ,  C07D237/22 ,  C07D405/12

    摘要： A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, chlorine or bromine; A is --NR.sub.3 -- or --O--; X is --(CH.sub.2).sub.n --, --CH(OR.sub.4)--, --CO-- or a single bond; when X is --(CH.sub.2).sub.n -- or a single bond, B is --O--, --S--, --NH--, --OSO.sub.2 --, or --OCO-- or a single bond, when X is --CH(OR.sub.4)--, B is --O--, --S--, --NH-- or --OSO.sub.2 --, and when X is --CO--, B is --O-- or --S--; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, ##STR2## or two of Y.sub.1, Y.sub.2 and Y.sub.3 together form ##STR3## and a pharmaceutically acceptable salt thereof.

    摘要翻译： 具有下式的3（2H）哒嗪酮：其中R 1是氢或C 1 -C 5烷基; R2是氢，C1-C8烷基，氯或溴; A是-NR 3 - 或-O-; X是 - （CH 2）n - ， - CH（OR 4） - ， - CO-或单键; 当X是 - （CH 2）n - 或单键时，当X是-CH（OR 4） - 时，B是-O - ， - S - ， - NH - ， - OCOO-或-OCO-或单键 ，B是-O - ， - S - ， - NH-或-OSO 2 - ，当X是-CO-时，B是-O-或-S-; 可以相同或不同的Y 1，Y 2和Y 3各自为氢，C 1〜C 8烷基，C 2〜C 8烯基，卤素，R 3 CON（R 8）（R 9），COR 10， ，Y2和Y3一起形成及其药学上可接受的盐。

    Pyridazinone derivatives with pharmaceutical activity
    8.
    发明授权
    Pyridazinone derivatives with pharmaceutical activity 失效
    具有药物活性的哒嗪酮衍生物

    公开(公告)号：US5929074A

    公开(公告)日：1999-07-27

    申请号：US986420

    申请日：1997-12-08

    申请人： Keizo Tanikawa ,  Akira Saito ,  Mitsuaki Hirotsuka ,  Ken-ichi Shikada

    发明人： Keizo Tanikawa ,  Akira Saito ,  Mitsuaki Hirotsuka ,  Ken-ichi Shikada

    IPC分类号： C07D237/22 ,  A61K31/4985 ,  A61K31/50 ,  A61K31/501 ,  A61P7/02 ,  A61P11/08 ,  A61P37/08 ,  C07D237/20 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D237/20

    摘要： A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.

    摘要翻译： 式（I）的3（2H） - 哒嗪酮衍生物及其制备方法和含有它的药物组合物。 其中R 1，R 2和R 3彼此独立地为氢原子或C 1-4烷基，X为氯原子或溴原子，Y 1为氢原子，卤原子，硝基 氨基或C 1-4烷氧基，Y 2是氢原子，卤素原子，羟基，C 1-4烷基或C 1-4烷氧基，A是C 1-5亚烷基链，其可以是 被羟基取代，B是可被C 1-4烷基取代的羰基或亚甲基链，R 4和R 5各自独立地为C 1-4烷基，或 R4是氢原子，R5是-Z-Ar（其中Z是C1-5亚烷基链，Ar是可以含有氮原子的芳族六元环），或者R4和R5一起形成C2-6 环状亚烷基或R 4和R 5与相邻的氮原子一起形成下式的4-取代的哌嗪环：其中R 6是C 1-4烷基。

    Pyridazinone derivatives with pharmaceutical activity
    9.
    发明授权
    Pyridazinone derivatives with pharmaceutical activity 失效
    具有药物活性的哒嗪酮衍生物

    公开(公告)号：US5728702A

    公开(公告)日：1998-03-17

    申请号：US564277

    申请日：1996-03-22

    申请人： Keizo Tanikawa ,  Akira Saito ,  Mitsuaki Hirotsuka ,  Ken-ichi Shikada

    发明人： Keizo Tanikawa ,  Akira Saito ,  Mitsuaki Hirotsuka ,  Ken-ichi Shikada

    IPC分类号： C07D237/22 ,  A61K31/4985 ,  A61K31/50 ,  A61K31/501 ,  A61P7/02 ,  A61P11/08 ,  A61P37/08 ,  C07D237/20 ,  C07D401/12 ,  C07D403/12 ,  C07D703/12

    CPC分类号： C07D401/12 ,  C07D237/20

    摘要： A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.

    摘要翻译： PCT No.PCT / JP94 / 01015 Sec。 371日期：1996年3月22日 102（e）1996年3月22日PCT 1994年6月24日PCT公布。 出版物WO95 / 01343 日期1995年1月12日A式（I）的3（2H） - 哒嗪酮衍生物及其制备方法和含有它的药物组合物。 其中R 1，R 2和R 3彼此独立地为氢原子或C 1-4烷基，X为氯原子或溴原子，Y 1为氢原子， 卤素原子，硝基，氨基或C1-4烷氧基，Y2是氢原子，卤素原子，羟基，C1-4烷基或C1-4烷氧基，A是C1 可以被羟基取代的亚烷基链，B是可以被C 1-4烷基取代的羰基或亚甲基链，并且彼此独立的R 4和R 5各自是C1 -4-烷基，或R4为氢原子，R5为-Z-Ar（其中Z为C1-5亚烷基链，Ar为可含有氮原子的芳香族6-元环）或R4和R5 一起形成C 2-6环状亚烷基，或者R 4和R 5与相邻的氮原子一起形成下式的下式的4-取代的哌嗪环：其中R 6是C 1-4烷基。