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1. 发明公开

EP0201765A2 3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 3（2H）哒嗪酮，它们的制备方法和含有抗过敏剂。
公开(公告)号：EP0201765A2
公开(公告)日：1986-11-20
申请号：EP86105537.4
申请日：1986-04-22
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
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:
wherein R 1 is hydrogen, methyl, C 3 -C 6 alkenyl, C 5 or C 6 cycloalkyl, benzyl, phenyl, -(CH 2 ) m CO 2 R 3 (wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4), -(CH 2 ) n A (wherein A is -OH or-N(R 4 ) 2 wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6) or -CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen, C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, -OR 5 (wherein R 5 is hydrogen, C 1 -C 8 alkyl or
wherein q is an integer of from 1 to 4),-CO 2 R 6 (wherein R 6 is hydrogen or C 1 -C 5 alkyl),-N(R 7 ) 2 (wherein R 7 is C 1 -C 4 alkyl) or-SR 8 (wherein R 8 is C 1 -C 4 alkyl); and Y 3 is C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, -OR 5 (wherein R 5 is as defined above), -CO 2 R 6 (wherein R 6 is as defined above), -N(R 7 ) 2 (wherein R 7 is as defined above) or-SR 8 (wherein R 8 is as defined above), or a pharmaceutically acceptable salt thereof.
摘要翻译：式A 3（2H）哒嗪酮： worin R1是氢，甲基，C3-C6链烯基，C5或C6环烷基，苄基，苯基， - （CH2）mCO2R3（worin R3是氢或C1-C5烷基，且m是从1到4的整数）， - （CH 2）NA（worin A是-OH或-N（R 4）2 worin R4是C1-C3烷基，且n为2至6）或的整数 - CF 3; R 2是氯或溴; 氢中，Y1和Y2的其中可以是相同或不同的，是氢，C，C5烷基，C2-C8链烯基，卤素，-OR 5（R 5是worin，C1-C8烷基或 worin q是整数（从1到4的），-CO2R6 worin R6是氢或C1-C5烷基）， - N（R 7）2（worin R7是C1-C4烷基）或-SR 8（worin R8是C1-C4烷基）; 和Y 3是C1-C5烷基，C2-C8链烯基，卤素，-OR 5（worin R5是如上定义的），是-CO2R6如上所定义）， - N（R 7）2（R 7 worin如上所定义）或 - SR8（worin R8是如上定义的），或其药学上可接受的盐。

2. 发明公开

EP0186817A1 3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 有权
标题翻译： 3（2H）哒嗪酮，其制备方法和含有该抗过敏剂的过程。
公开(公告)号：EP0186817A1
公开(公告)日：1986-07-09
申请号：EP85115655.4
申请日：1985-12-09
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： C07D237/22 , A61K31/50
CPC分类号： C07D405/12 , C07D237/22 , Y10S514/826
摘要： A 3(2H)pyridazinone of the formula:
wherein R, is C 2 -C 5 alkyl; R 2 is hydrogen, C 1 -C 3 alkyl, chlorine or bromine; R 3 is hydrogen or C 1 -C 4 alkyl; and each of Y 1 , Y 2 and Y 3 which may be the same or different, is hydrogen, C 1 -C 8 alkyl. C 2 -C 8 alkenyl, halogen, -(CH 2 ),A [wherein A is substituted amino of the formula -N(R 4 )(R 5 ) (wherein each of R 4 and R 5 which may be the same or different, is C 1 -C 4 alkyl, or R 4 and R 5 together form C 4- C 5 alkylene), morpholino, 4-R 6 -piperazin-1-yl (wherein R 6 is C 1 -C 3 alkyl) or-OR 7 (wherein R 7 is hydrogen or C,-C 3 alkyl), and I is an integer of 0 to 3], -OR 8 [wherein R 8 is hydrogen, C 1 -C 8 alkyl, C 3 -C 5 alkenyl, benzyl or -(CH 2 ) q R 9 [wherein R 9 is CO 2 R 3 (wherein R 3 is as defined above), -CONHR 3 (wherein R 3 is as defined above) or -CH 2 OR 7 (wherein R 7 is as defined above), and q is an integer of 1 to 5]], -CO 2 R 3 (wherein R 3 is as defined above), -CON(R 10 )(R 11 ) [wherein each of R, o and R,, which may be the same or different, is hydrogen, C 1 -C 4 alkyl or C 3 -C 5 alkenyl, or R 10 and R 11 together form C 1 -C 6 alkylene, -(CH 2 ) 2 O(CH 2 ) 2 or -(CH 2 ) 2 N(R 6 )(CH 2 ) 2 - (wherein R 6 is as defined above)], -CONH(CH 2 ) m A (wherein A is as defined above, and m is an integer of 2 to 4), -CH = CHCOR, 2 (wherein R 12 is hydroxy, C 1 -C 4 alkoxy or -N(R 13 )(CH 2 ) n CO 2 R 3 (wherein R 13 is hy- d rogen, C 1 -C 6 alkyl or cycloalkyl, R 3 is as defined above, and n is an integer of 1 to 4)), -SR 14 (wherein R 14 is C 1 -C 4 alkyl),
(wherein R 3 is as defined above), or two of Y 1 Y 2 and Y 3 together form
(wherein p is an integer of 1 or 2), and a pharmaceutically acceptable salt thereof.

3. 发明授权

EP0275997B1 3(2H)pyridazinone, process for its preparation and antagonistic agent against SRS-A containing it 失效
标题翻译： 3（2H）PYRIDAZINONE，其制备和防止含有SRS-A的ANAGONISTIC AGENT的方法
公开(公告)号：EP0275997B1
公开(公告)日：1992-12-23
申请号：EP88100798.3
申请日：1988-01-20
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Tanikawa, Keizo , Sakoda, Ryozo , Shikada, Ken-ichi Nissan Chemical Ind. Ltd., , Sakuya, Tanaka Nissan Chemical Ind. Ltd.,
IPC分类号： C07D237/22 , A61K31/50
CPC分类号： C07D237/22

4. 发明授权

EP0186817B1 3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 有权
标题翻译： 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：EP0186817B1
公开(公告)日：1989-08-02
申请号：EP85115655.4
申请日：1985-12-09
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： C07D237/22 , A61K31/50
CPC分类号： C07D405/12 , C07D237/22 , Y10S514/826

5. 发明授权

EP0193853B1 3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 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：EP0193853B1
公开(公告)日：1990-09-12
申请号：EP86102467.7
申请日：1986-02-26
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： C07D237/22 , C07D237/16 , C07D403/12 , C07D405/12 , A61K31/50
CPC分类号： C07D403/12 , C07D237/16 , C07D237/22 , C07D405/12

6. 发明公开

EP0193853A2 3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 3（2H） - 哒嗪酮，其制备方法及含有该antiallergetische代理进程。
公开(公告)号：EP0193853A2
公开(公告)日：1986-09-10
申请号：EP86102467.7
申请日：1986-02-26
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： C07D237/22 , C07D237/16 , C07D403/12 , C07D405/12 , A61K31/50
CPC分类号： C07D403/12 , C07D237/16 , C07D237/22 , C07D405/12
摘要： A3(2H)pyridazinone of the formula:

wherein R 1 is hydrogen or C 1 -C 5 alkyl; R 2 is hydrogen, C 1 -C 8 -alkyl, chlorine or bromine; A is -NR 3 - or -0-; X is -(CH 2 ) n- , -CH(OR 4 )-, -CO- or a single bond; when X is -(CH 2 ) n - or a single bond, B is -O-, -S-, -NH-, -OS0 2 -, or -OCO- or a single bond, when X is -CH(OR 4 )-, B is -0-, -S-, -NH- or -OS0 2 -, and when X is -CO-, B is -O- or -S-; and each of Y 1 , Y 2 and Y 3 which may be the same or different, is hydrogen, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, halogen, -OR S , -C0 2 R 6 , -CH=CHCO 2 R 7 , -CN,

-CON(R 8 )(R 9 ), -COR 10 , or two of Y 1 , Y 2 and Y 3 togetherform

and a pharmaceutically acceptable salt thereof.

7. 发明授权

EP0201765B1 3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 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：EP0201765B1
公开(公告)日：1991-09-18
申请号：EP86105537.4
申请日：1986-04-22
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： A61K31/50 , C07D237/22
CPC分类号： A61K31/50 , C07D237/22

8. 发明公开

EP0275997A1 3(2H)pyridazinone, process for its preparation and antagonistic agent against SRS-A containing it 失效
标题翻译： 3（2H）哒嗪酮，其制备方法和含有针对SRS-A这个代理进程。
公开(公告)号：EP0275997A1
公开(公告)日：1988-07-27
申请号：EP88100798.3
申请日：1988-01-20
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Tanikawa, Keizo , Sakoda, Ryozo , Shikada, Ken-ichi Nissan Chemical Ind. Ltd., , Sakuya, Tanaka Nissan Chemical Ind. Ltd.,
IPC分类号： C07D237/22 , A61K31/50
CPC分类号： C07D237/22
摘要： A 3(2H)pyridazinone of the formula:
wherein R₁ is hydrogen, 2-propenyl or straight chained or branched C₁-C₄ alkyl; R₂ is hydrogen or C₁-C₃ alkyl; X is chlorine or bromine; Y is hydrogen, nitro, -NHR₃ wherein R₃ is hydrogen or straight chained or branched C₁-C₄ alkyl, -AR₄ wherein A is oxygen or sulfur and R₄ is hydrogen, straight chained or branched C₁-C₆ alkyl, C₃-C₆ alkenyl having one double bond, C₃-C₆ alkynyl having one triple bond, phenyl or
wherein R₅ is hydrogen or C₁-C₄ alkyl, or halogen; Z₁ is hydrogen, C₁-C₄ alkyl, -OR₆ wherein R₆ is hydrogen, straight chained or branched C₁-C₈ alkyl or
wherein n is an integer of from 1 to 4, -N(R₇)₂ wherein R₇ is C₁-C₄ alkyl, or halogen; Z₂ is C₁-C₄ alkyl, -OR₆ wherein R₆ is as defined above, -N(R₇)₂ wherein R₇ is as defined above, or halogen, provided that when R₁ is straight chained or branched C₂-C₄ alkyl, Y is not hydrogen and when R₁ is hydrogen, methyl or 2-propenyl, Y and R₂ are not simultaneously hydrogen, or a pharmaceutically acceptable salt thereof.
摘要翻译：式A 3（2H）哒嗪酮： worin R1为氢，2-丙烯基或直链或支链的C1-C4烷基; R2是氢或C1-C3烷基; X是氯或溴; Y为氢，硝，-NHR 3 worin R 3是氢或直链或支链C1-C4烷基，-AR4 worin A是氧或硫，R 4是氢，直链或支链C1-C6烷基，具有一个C3-C6链烯基双键，C 3 -C 6具有一个三键，苯基或炔worin R5是氢或C1-C4烷基，或卤素; Z1为氢，C1-C4烷基，-OR 6 worin R6是氢，直链或支链的C1-C8烷基或其中n是从1至4的整数，-N（R 7）2 worin R7是C1- C4烷基，或卤素; Z2是C1-C4烷基，-OR 6 worin R6如上述所定义，-N（R 7）2 worin R7如以上所定义，或卤素，条件做当R 1为直链或支链C2-C4烷基，Y不是氢并且当R 1为氢，甲基或2-丙烯基，Y和R 2不都为氢。同时，或其药学上可接受的盐。

9. 发明公开

EP0201765A3 3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 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：EP0201765A3
公开(公告)日：1987-08-26
申请号：EP86105537
申请日：1986-04-22
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
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:
wherein R 1 is hydrogen, methyl, C 3 -C 6 alkenyl, C 5 or C 6 cycloalkyl, benzyl, phenyl, -(CH 2 ) m CO 2 R 3 (wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4), -(CH 2 ) n A (wherein A is -OH or-N(R 4 ) 2 wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6) or -CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen, C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, -OR 5 (wherein R 5 is hydrogen, C 1 -C 8 alkyl or
wherein q is an integer of from 1 to 4),-CO 2 R 6 (wherein R 6 is hydrogen or C 1 -C 5 alkyl),-N(R 7 ) 2 (wherein R 7 is C 1 -C 4 alkyl) or-SR 8 (wherein R 8 is C 1 -C 4 alkyl); and Y 3 is C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, -OR 5 (wherein R 5 is as defined above), -CO 2 R 6 (wherein R 6 is as defined above), -N(R 7 ) 2 (wherein R 7 is as defined above) or-SR 8 (wherein R 8 is as defined above), or a pharmaceutically acceptable salt thereof.

10. 发明公开

EP0193853A3 3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it 失效
标题翻译： 3（2H）哒嗪酮，其制备方法和含有它的抗过敏剂
公开(公告)号：EP0193853A3
公开(公告)日：1987-07-22
申请号：EP86102467
申请日：1986-02-26
申请人： NISSAN CHEMICAL INDUSTRIES LTD.
发明人： Mutsukado, Motoo , Tanikawa, Keizo , Shikada, Ken-ichi , Sakoda, Ryozo
IPC分类号： C07D237/22 , C07D237/16 , C07D403/12 , C07D405/12 , A61K31/50
CPC分类号： C07D403/12 , C07D237/16 , C07D237/22 , C07D405/12
摘要： A3(2H)pyridazinone of the formula:

wherein R 1 is hydrogen or C 1 -C 5 alkyl; R 2 is hydrogen, C 1 -C 8 -alkyl, chlorine or bromine; A is -NR 3 - or -0-; X is -(CH 2 ) n- , -CH(OR 4 )-, -CO- or a single bond; when X is -(CH 2 ) n - or a single bond, B is -O-, -S-, -NH-, -OS0 2 -, or -OCO- or a single bond, when X is -CH(OR 4 )-, B is -0-, -S-, -NH- or -OS0 2 -, and when X is -CO-, B is -O- or -S-; and each of Y 1 , Y 2 and Y 3 which may be the same or different, is hydrogen, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, halogen, -OR S , -C0 2 R 6 , -CH=CHCO 2 R 7 , -CN,

-CON(R 8 )(R 9 ), -COR 10 , or two of Y 1 , Y 2 and Y 3 togetherform

and a pharmaceutically acceptable salt thereof.
摘要翻译：下式的A3（2H）哒嗪酮：其中R1是氢或C1-C5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 - ， - SO 2 O-或-OCO-或单键，B是-O - ， - S - ， - NH-或-OSO 2 - ，并且当X是-CO-时，B是-O-或-S-; 并且Y 1，Y 2和Y 3中的每一个可以相同或不同，为氢，C 1 -C 8烷基，C 2 -C 8烯基，卤素，-OR 6，-CO 2 R 6，-CH = CHCO 2 R 7，-CN，-CON（R 8）（R9）， - COR10或两个Y1，Y2和Y3一起形成其药学上可接受的盐。

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