3(2H)Pyridazinone, process for its preparation and anti-allergic agent
containing it
    4.
    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

    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, and antagonistic agent against SRS-A containing it
    5.
    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

    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
    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

    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

    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

    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

    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。

    Pyridazinone derivatives
    10.
    发明授权
    Pyridazinone derivatives 失效
    哒嗪酮衍生物

    公开(公告)号:US5750523A

    公开(公告)日:1998-05-12

    申请号:US676227

    申请日:1996-07-23

    CPC分类号: C07D401/12 C07D237/22

    摘要: Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.

    摘要翻译: PCT No.PCT / JP95 / 00069 Sec。 371日期:1996年7月23日 102(e)日期1996年7月23日PCT提交1995年1月24日PCT公布。 WO95 / 19969 PCT公开 日期:1997年7月27日由式(I)表示的哒嗪酮衍生物和含有它们的抗血小板剂:其中R是氢原子或C1-C4烷基,X是氢原子,氯原子 或溴原子,Ar是吡啶基或被OR 1取代的苯基(其中R1是氢原子或C1-C4烷基)和A {其中A是氢原子,卤原子,C1-C4 烷基或OR 2(其中R 2是氢原子或C 1 -C 4烷基)}是其中一个碳原子被一个OR 1基团取代的C 1 -C 8亚烷基(其中R 1与上述定义相同) ,Z 1和Z 2独立地为氢原子,卤素原子,C 1 -C 4烷基或OR 1基(其中R 1与上述定义相同)]。 这些化合物具有很强的抗血小板作用,非常安全,可用作各种血栓性疾病的预防和治疗药物的活性成分。