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1. 发明授权

US5292771A Substituted .beta.-diketones and their use 失效
标题翻译：取代的β-二酮及其用途
公开(公告)号：US5292771A
公开(公告)日：1994-03-08
申请号：US958487
申请日：1992-10-08
申请人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
发明人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
IPC分类号： A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C205/45 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , A61K31/38 , A61K31/44 , A61K31/47
CPC分类号： C07C205/45 , A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C2101/02
摘要： Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.
摘要翻译：式（Ⅰ）化合物其中n为0或1，R 1和R 2独立地为甲基，乙基或环丙基，R为任选取代的苯基或杂芳基或其盐或酯可用于治疗炎症性肠病。

2. 发明授权

US5288750A Substituted .beta.-diketones 失效
标题翻译：取代的β-二酮
公开(公告)号：US5288750A
公开(公告)日：1994-02-22
申请号：US646714
申请日：1991-01-31
申请人： Pentti Pohto , Paivi A. Aho , Reijo J. Backstrom , Erkki J. Honkanen , Inge-Britt Y. Linden , Erkki A. O. Nissinen
发明人： Pentti Pohto , Paivi A. Aho , Reijo J. Backstrom , Erkki J. Honkanen , Inge-Britt Y. Linden , Erkki A. O. Nissinen
IPC分类号： C07C49/14 , A61K31/00 , A61K31/06 , A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P1/04 , C07C20060101 , C07C45/68 , C07C49/00 , C07C49/15 , C07C49/203 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/794 , C07C65/38 , C07C69/60 , C07C253/30 , C07C255/56 , C07D307/46 , C07D333/22 , C07D333/32 , A61K3/12
CPC分类号： A61K31/12 , A61K31/00 , A61K31/06
摘要： ##STR1## wherein R
1 and R
2 are each independently hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, hydroxy, aryl or heteroaryl or amino, the alkyl, aryl, heteroaryl or amino group being optionally substituted; R
3 is hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms or optionally substituted aryl or heteroaryl and salts, ethers and esters thereof are useful as cytoprotective agents, especially as antitulcerogenic or gastroprotective agents.
摘要翻译： PCT No.PCT / FI89 / 00165 Sec。 371日期1991年1月31日 102（e）日期1991年1月31日PCT提交1989年9月1日PCT公布。出版物WO90 / 02724 （*化学结构*）（Ia）（*化学结构*）（Ib）其中R 1和R 2各自独立地为氢，1至6个碳原子的烷基，1至6个碳原子的烷氧基，羟基，芳基或杂芳基或氨基，烷基，芳基，杂芳基或氨基任选被取代; R 3是氢，任选取代的1至6个碳原子的烷基或任选取代的芳基或杂芳基，其盐，醚和酯可用作细胞保护剂，特别是作为抗精神病药或胃保护剂。

3. 发明授权

US5185370A Substituted .beta.-diketones and their use 失效
标题翻译：取代的β-二酮及其用途
公开(公告)号：US5185370A
公开(公告)日：1993-02-09
申请号：US648641
申请日：1991-01-31
申请人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
发明人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
IPC分类号： A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C205/45 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24
CPC分类号： C07C205/45 , A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C2101/02
摘要： Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.
摘要翻译：式（Ⅰ）化合物其中n为0或1，R 1和R 2独立地为甲基，乙基或环丙基，R为任选取代的苯基或杂芳基或其盐或酯可用于治疗炎症性肠病。

4. 发明授权

US5446194A Pharmacologically active catechol derivatives 失效
标题翻译：药理活性儿茶酚衍生物
公开(公告)号：US5446194A
公开(公告)日：1995-08-29
申请号：US121617
申请日：1993-09-16
申请人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka I. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
发明人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka I. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
IPC分类号： C07C43/23 , C07C45/56 , C07C45/67 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07C205/19 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/53 , C07D207/32 , C07D207/333 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04 , C07C255/50
CPC分类号： C07C43/23 , C07C205/19 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/00 , C07C317/00 , C07C323/00 , C07C45/565 , C07C45/673 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07D207/333 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04
摘要： A compound according to formula 1 ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, carbamoyl which is substituted by an alkyl of 1 to 4 carbon atoms, alkylcarbonyl of 2 to 5 carbon atoms or phenyl carbonyl, X represents halogen nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms or which is substituted with hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable esters and salts thereof, and a pharmaceutically acceptable carrier therefor, as well as pharmaceutical compositions containing said compounds as COMT inhibitors.
摘要翻译：根据式1的化合物其中R 1和R 2独立地表示氢，被1至4个碳原子的烷基取代的氨基甲酰基，2至5个碳原子的烷基羰基或苯基羰基，X表示卤素硝基或氰基， R 3表示其中R 4表示氰基或2至5个碳原子的烷基羰基，R 5表示未被取代或被1至8个碳原子的烷基或被1至8个碳原子的羟基烷基取代的氨基甲酰基或药学上可接受的酯及其盐及其药学上可接受的载体，以及含有所述化合物作为COMT抑制剂的药物组合物。

5. 发明授权

US4963590A Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same 失效
标题翻译：药理活性化合物，其制备方法和含有它们的组合物
公开(公告)号：US4963590A
公开(公告)日：1990-10-16
申请号：US126911
申请日：1987-11-27
申请人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka T. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
发明人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka T. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
IPC分类号： C07C27/00 , A61K31/00 , A61K31/04 , A61K31/045 , A61K31/047 , A61K31/05 , A61K31/06 , A61K31/075 , A61K31/085 , A61K31/11 , A61K31/12 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/33 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/47 , A61K31/495 , A61P9/12 , A61P25/00 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07C20060101 , C07C39/08 , C07C39/24 , C07C39/26 , C07C39/373 , C07C43/20 , C07C43/23 , C07C45/00 , C07C45/56 , C07C45/67 , C07C45/74 , C07C47/52 , C07C47/565 , C07C47/575 , C07C49/20 , C07C49/245 , C07C49/747 , C07C49/76 , C07C49/83 , C07C49/835 , C07C49/84 , C07C59/40 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/68 , C07C59/90 , C07C65/00 , C07C65/03 , C07C65/21 , C07C67/00 , C07C69/017 , C07C69/035 , C07C69/73 , C07C69/76 , C07C205/20 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C213/00 , C07C231/00 , C07C233/00 , C07C233/12 , C07C235/44 , C07C235/54 , C07C235/66 , C07C239/00 , C07C253/00 , C07C255/37 , C07C255/53 , C07C301/00 , C07C309/65 , C07C311/15 , C07C317/22 , C07D207/32 , C07D207/325 , C07D207/333 , C07D211/14 , C07D211/22 , C07D211/30 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/08 , C07D295/13 , C07D295/18 , C07D295/185 , C07D317/52 , C07D317/62 , C07D319/24 , C07D405/04 , C07D405/06
CPC分类号： C07D207/333 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/00 , C07C317/00 , C07C323/00 , C07C43/23 , C07C45/565 , C07C45/673 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04
摘要： Pharmacologically active catechol derivatives of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently comprise hydrogen, alkyl, acyl, optionally substituted aroyl, lower alkylsulfonyl or alkylcabamoyl or taken together form a lower alkylidene or cycloalkylidene, X comprises an electronegative substituent such as halogen, nitro, cyano, lower alkylsulfonyl, sulfonamido, aldehyde, caboxyl or trifluoromethyl and R.sub.3 comprises hydrogen, halogen, hydroxy alkyl, amino, nitro, cyano, trifluoromethyl, lower alkylsulfonyl, sulfonamide, aldehyde, alkyl carbonyl, aralkylidene carbonyl or carboxyl or a group selected from ##STR2## wherein R.sub.4 comprises hydrogen, alkyl, cyano, carboxyl or acyl and R.sub.5 comprises hydrogen, cyano, carboxyl, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, optionally substituted aroyl or heteroaroyl, hydroxyalkyl or carboxyalkyl or R.sub.4 and R.sub.5 together form a five to seven membered substituted cycloalkanone ring;--(CO).sub.n (CH.sub.2).sub.m --CORwherein n is 0-1 and m is 0-7 and R comprises hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; ##STR3## wherein R.sub.8 and R.sub.9 independently comprise hydrogen or one of the following optionally substituted groups; alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, or together form an optionally substituted piperidyl group;--NH--CO--R.sub.10wherein R.sub.10 comprises a substituted alkyl group.
摘要翻译：式I的药理活性儿茶酚衍生物其中R 1和R 2独立地包括氢，烷基，酰基，任选取代的芳酰基，低级烷基磺酰基或烷基氨基甲酰基，或一起形成低级亚烷基或环烷叉基，X包括电负性取代基如卤素，硝基，氰基，低级烷基磺酰基，亚磺酰氨基，醛，呋喃甲酰基或三氟甲基，R3包括氢，卤素，羟基烷基，氨基，硝基，氰基，三氟甲基，低级烷基磺酰基，磺酰胺，醛，烷基羰基，亚烷基羰基或羧基或选自其中R 4包括氢，烷基，氰基，羧基或酰基，R 5包括氢，氰基，羧基，烷氧基羰基，羧基烯基，硝基，酰基，任选取代的芳酰基或杂芳酰基，羟基烷基或羧基烷基或R4和R5一起形成五至七元取代的环烷酮环; - （CO）n（CH 2）m -COR其中n为0-1，m为0-7，R为羟基，烷基，羧基烷基，任选取代的烯烃，烷氧基或任选取代的氨基; 其中R8和R9独立地包含氢或以下任选取代的基团之一; 烷基，烯基，炔基，环烷基，芳烷基，或一起形成任选取代的哌啶基; -NH-CO-R 10，其中R 10包含取代的烷基。

6. 发明授权

US5283352A Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same 失效
标题翻译：药理活性化合物，其制备方法和含有它们的组合物
公开(公告)号：US5283352A
公开(公告)日：1994-02-01
申请号：US987245
申请日：1992-12-07
申请人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka I. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
发明人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka I. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
IPC分类号： C07C43/23 , C07C45/56 , C07C45/67 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07C205/19 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/53 , C07D207/32 , C07D207/333 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04 , C07C255/33 , C07C49/213 , C07C255/34
CPC分类号： C07C43/23 , C07C205/19 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/00 , C07C317/00 , C07C323/00 , C07C45/565 , C07C45/673 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07D207/333 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04
摘要： Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.
摘要翻译：其中R1，R2，R3和X如本文所述的式I的儿茶酚化合物是有效的儿茶酚-O-甲基转移酶抑制剂。

7. 发明授权

US5001152A Use of catechol-O-methyl transferase (COMT) inhibitors and their physiologically acceptable salts for ulcer treatment 失效
标题翻译：儿茶酚-O-甲基转移酶（COMT）抑制剂及其生理学上可接受的盐用于溃疡治疗
公开(公告)号：US5001152A
公开(公告)日：1991-03-19
申请号：US288979
申请日：1988-12-23
申请人： Paivi A. Aho , Pentti Pohto , Inge-Britt Y. Linden , Reijo J. Backstrom , Erkki J. Honkanen , Erkki A. O. Nissenen
发明人： Paivi A. Aho , Pentti Pohto , Inge-Britt Y. Linden , Reijo J. Backstrom , Erkki J. Honkanen , Erkki A. O. Nissenen
IPC分类号： A61K31/05 , A61K31/00 , A61K31/047 , A61K31/06 , A61K31/085 , A61K31/10 , A61K31/11 , A61K31/12 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/33 , A61K31/445 , A61P1/04 , C07C205/13 , C07C255/49 , C07D295/18 , C07D317/62
CPC分类号： A61K31/06 , A61K31/00 , A61K31/12 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： The invention is concerned with the new use of known catechol derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms; X is nitro, halogen or cyano and R.sub.3 is chlorine, nitro, cyano or a radical of the formula ##STR2## wherein R.sub.4 is hydrogen, cyano, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms and R.sub.5 is cyano, alkanoyl having 2 to 5 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, carboxyl or phenylcarbonyl unsubstituted or substituted with one to three methoxy groups or pharmaceutically acceptable salt thereof. The new use is the treatment and prophylaxis of ulcers and lesions in the gastrointestinal tract.

8. 发明授权

US5489614A Catechol derivatives, their physiologically acceptable salts, esters and use 失效
标题翻译：儿茶酚衍生物，其生理学上可接受的盐，酯和用途
公开(公告)号：US5489614A
公开(公告)日：1996-02-06
申请号：US461752
申请日：1995-06-05
申请人： Tapio J. Korkolainen , Erkki A. O. Nissinen , Reijo J. Backstrom , Aino K. Pippuri
发明人： Tapio J. Korkolainen , Erkki A. O. Nissinen , Reijo J. Backstrom , Aino K. Pippuri
IPC分类号： A61K31/12
CPC分类号： A61K31/12
摘要： Known and new catechol derivates may be used as medicinal antioxidants in the prevention or treatment of tissue damage induced by lipid peroxidation. The conditions and diseases to be treated are for example heart disease, rheumatoid arthritis, cancer, inflammatory disease, a rejection reaction in organ transplants, ischemia, cancer and aging.
摘要翻译：已知和新的儿茶酚衍生物可用作药物抗氧化剂，以预防或治疗由脂质过氧化引起的组织损伤。待治疗的病症和疾病是例如心脏病，类风湿性关节炎，癌症，炎性疾病，器官移植物中的排斥反应，缺血，癌症和老化。

9. 发明授权

US5512572A Anti-ischemic medicament 失效
标题翻译：抗缺血药物
公开(公告)号：US5512572A
公开(公告)日：1996-04-30
申请号：US331607
申请日：1994-11-22
申请人： Heimo O. Haikala , Juoko M. Levijoki , Reijo J. Backstrom , Pentti T. Nore , Erkki J. Honkanen
发明人： Heimo O. Haikala , Juoko M. Levijoki , Reijo J. Backstrom , Pentti T. Nore , Erkki J. Honkanen
IPC分类号： C07D237/04 , A61K31/50 , A61P9/08 , A61P9/10 , C07D237/08
CPC分类号： A61K31/50
摘要： A method for preventing or treating myocardial ischemia in a mammalian organism is disclosed. The compound 4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl!hydrazono!propanedinitrile or its enantiomer or a pharmaceutically acceptable salt there is administered to a mammalian organism in need of such prevention or treatment. The compound may be administered in its racemic form or in a form which is substantially free of the (+)-enantiomer or substantially free of the (-)-enantiomer.
摘要翻译： PCT No.PCT / FI93 / 00191 Sec。 371日期：1994年11月22日 102（e）日期1994年11月22日PCT提交1993年5月5日PCT公布。第WO93 / 21921号公报日本11月11日，日本公开了一种预防或治疗哺乳动物生物体内的心肌缺血的方法。将化合物[[4-（1,4,5,6-四氢-4-甲基-6-氧代-3-哒嗪基）苯基]亚肼基]丙二腈或其对映体或药学上可接受的盐向哺乳动物生物体施用需要这样的预防或治疗。化合物可以其外消旋形式或基本上不含（+） - 对映异构体或基本上不含（ - ） - 对映体的形式施用。

10. 发明授权

US4963677A Heterocyclic lactam compounds 失效
标题翻译：杂环内酰胺化合物
公开(公告)号：US4963677A
公开(公告)日：1990-10-16
申请号：US268450
申请日：1988-11-08
申请人： Lawrence Sellin , Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Tord K. W. Langenskiold , Irma O. Ojala , Aino K. Pippuri , Jarmo J. Pystynen
发明人： Lawrence Sellin , Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Tord K. W. Langenskiold , Irma O. Ojala , Aino K. Pippuri , Jarmo J. Pystynen
IPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07D513/16
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： A compound of the formula ##STR1## and pharmaceutically acceptable salts thereof, in which A is --N.dbd.N--NH--, --X--C(R.sub.2).dbd.N--, --N.dbd.C(R.sub.2)--X--, --X--C(R.sub.2)--CH(R.sub.2).dbd.N-- or --N.dbd.C(R.sub.2)--CH(R.sub.2)--X--, wherein X is sulphur, oxygen or nitrogen and R.sub.2 is provided that where two R.sub.2 -groups are present in the A group one of the R.sub.2 groups is hydrogen, amino, substituted amino, C.sub.1-6 alkyl, substituted acylamino or one of the following groups: ##STR2## wherein R.sub.a is hydrogen, amino, substituted amino, C.sub.1-6 alkoxy, heterocyclic five membered ring or --NHCOR', wherein R' is C.sub.1-6 alkyl, aryl or heterocyclic five membered ring, R.sub.b is hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or hydroxy, R.sub.c is hydrogen, C.sub.1-6 alkyl or oxygen and R.sub.d is C.sub.1-6 alkyl or oxygen, R.sub.e is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sub.f is C.sub.1-6 alkyl, provided that where two R.sub.2 -groups are present in the A group, one of the R.sub.2 groups is hydrogen; B is --(CH.sub.2).sub.m --C(R.sub.3 R.sub.4)--(CH.sub.2).sub.n --, --C(R.sub.3).dbd.CH--, --CH.dbd.C(R.sub.3)--, --O--[C(R.sub.3 R.sub.4)].sub.n --, --[C(R.sub.3 R.sub.4)].sub.n --O--, --S--[C(R.sub.3 R.sub.4)].sub.n -- or --[C(R.sub.3 R.sub.4)].sub.n --S-- wherein R.sub.3 and R.sub.4, which can be independently the same or different, are hydrogen, C1-.sub.6 alkyl, aryl (preferably phenyl) or pyridyl and m and n are independently zero or 1; D is either oxygen or sulphur; the two R-groups are indepenently hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, amino, acylamino or substituted acylamino, nitro, halogen, cyano, aldehyde, carboxy, carbamoyl; R.sub.1 is a hydrogen or C.sub.1-6 alkyl or R and R.sub.1 form together a fused 6-membered heterocyclic ring. The compound is effective in the treatment of congestive heart failure.
摘要翻译：其中A为-N = N-NH-，-XC（R2）= N-，-N = C（R2）-X的式I化合物及其药学上可接受的盐 - ，-XC（R2）-CH（R2）= N-或-N = C（R2）-CH（R2）-X-，其中X为硫，氧或氮，R2为两个R2-基团存在于A基团中的一个R2基团是氢，氨基，取代的氨基，C 1-6烷基，取代的酰基氨基或以下基团之一：其中R a是氢，氨基，取代的氨基，C 1-6烷氧基，杂环五元环或-NHCOR'，其中R'是C 1-6烷基，芳基或杂环五元环，R b是氢， C 1-6烷氧基，C 1-6烷硫基或羟基，R c是氢，C 1-6烷基或氧，R d是C 1-6烷基或氧，Re是氢，羟基或C 1-6烷氧基，R f是C 1-6烷基，条件是其中两个R 2 - A组存在，R2基团之一为氢; B是 - （CH 2）m C（R 3 R 4） - （CH 2）n - ， - C（R 3）= CH-，-CH = C（R 3） - ，-O- [C（R 3 R 4）] n - （R3R4）] nO-，-S- [C（R3R4）] n - 或 - [C（R3R4）] nS-，其中R3和R4可以独立地相同或不同，是氢，C1-6烷基，芳基（优选苯基）或吡啶基，m和n分别为0或1; D是氧或硫; 两个R基团是独立的氢，C 1-6烷氧基，C 1-6烷基，氨基，酰氨基或取代的酰基氨基，硝基，卤素，氰基，醛，羧基，氨基甲酰基; R 1是氢或C 1-6烷基，或R 1和R 1一起形成稠合的6元杂环。该化合物可有效治疗充血性心力衰竭。

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