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1. 发明授权

US4892947A 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：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。

2. 发明授权

US5098900A 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：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. 发明授权

US4783462A 3(2H)pyridazinone, and anti-allergic agent containing it 失效
标题翻译： 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。

4. 发明授权

US5318968A 5-heteroarylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-杂芳基氨基-6-氧基取代的3（2H） - 哒嗪酮
公开(公告)号：US5318968A
公开(公告)日：1994-06-07
申请号：US994413
申请日：1992-12-21
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.
摘要翻译：式（Ⅰ）化合物或其药学上可接受的盐，其制备方法和药物组合物的特征在于含有这些化合物作为有效成分。这些化合物具有强的抗血栓形成活性，强心剂活性，血管扩张剂活性和抗SRS-A活性，可用作各种血栓形成，充血性心力衰竭，高血压，哮喘，立即型过敏性疾病等的预防或治疗剂。

5. 发明授权

US5314883A 5-heteroarylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-杂芳基氨基-6-氧基取代的3（2H） - 哒嗪酮
公开(公告)号：US5314883A
公开(公告)日：1994-05-24
申请号：US994404
申请日：1992-12-21
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula: ##STR1## or its pharmaceutically acceptable salt and pharmaceutical compositions containing these compounds as effective ingredients. These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic afflictions, congestive heart failure, hypertension, asthma, immediate-type allergy diseases and the like.
摘要翻译：下式的化合物：其含有这些化合物作为有效成分的药学上可接受的盐和药物组合物。这些化合物具有强的抗血栓活性，强心剂活性，血管扩张剂活性和抗SRS-A活性，可用作各种血栓形成疾病，充血性心力衰竭，高血压，哮喘，立即型过敏性疾病等的预防或治疗剂。

6. 发明授权

US5202323A 5-arylmethylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-氨基甲酰胺-6-氧代替3（2H） - 吡啶并[
公开(公告)号：US5202323A
公开(公告)日：1993-04-13
申请号：US768182
申请日：1991-10-16
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.

7. 发明授权

US4978665A 3(2H)pyridazinone, and antagonistic agent against SRS-A containing it 失效
标题翻译： 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.

8. 发明授权

US5929074A Pyridazinone derivatives with pharmaceutical activity 失效
标题翻译：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。

9. 发明授权

US5728702A Pyridazinone derivatives with pharmaceutical activity 失效
标题翻译：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。

10. 发明授权

US06555574B1 4-oxybenzopyran derivative 失效
标题翻译： 4-羟基苯并吡喃衍生物
公开(公告)号：US06555574B1
公开(公告)日：2003-04-29
申请号：US10049996
申请日：2002-03-29
申请人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K3135
CPC分类号： C07D405/12 , C07D311/22
摘要： This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or a C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; n represents an integer of 0-4; X represents —C(═O)NR7—, —NR8—, —NHC(═O)NH— or —S(O)2NH—; R5 represents a hydrogen atom or (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), or (l); R6 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to an antiarrhythmic agent having the prolongation effect of the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及式（I）的4-氧代苯并吡喃衍生物，其中R1和R2各自独立地表示氢原子，C1-6烷基或苯基; R3表示羟基或C1-6烷基羰基氧基; R 4表示氢原子，C 3-6环烷基，C 1-6烷基，C 1-6烷基羰基，C 1-6烷基氨基羰基，二-C 1-6烷基氨基羰基，芳基或杂芳基 ; n表示0-4的整数; X表示-C（= O）NR 7 - ， - NR 8 - ， - NHC（= O）NH-或-S（O）2 NH-; R5代表氢原子或（a），（b），（c），（d），（e），（f），（g），（h），（i），（j），（k）或（l）; R6表示氢原子，卤素原子，硝基或氰基; 或其药学上可接受的盐。本发明还涉及具有作为活性成分的所述化合物或其药学上可接受的盐的具有功能性不应期的延长作用的抗心律失常药。

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