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1.发明授权
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。
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2.发明授权
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。
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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。
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4.发明授权
公开(公告)号：US5112861A
公开(公告)日：1992-05-12
申请号：US587791
申请日：1990-09-25
申请人： Reijo 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 Pystynen
发明人： Reijo 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 Pystynen
IPC分类号： A61K31/09 , C07C43/23 , C07C45/56 , C07C45/67 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07D207/32 , C07D207/333 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04 , A01N37/12 , A01N35/00 , A01N37/44
CPC分类号： C07D207/333 , 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 , 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： The invention concerns a method for the treatment of Parkinson's Disease. The method comprises administering a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, alkylcarbamoyl of 2 to 5 carbon atoms or alkylcarbonyl of 2 to 5 carbon atoms, X represents 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 cyano; alkylcarbonyl of 2 to 5 carbon atoms; or carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms, or hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable salts or esters thereof; and a sufficient amount of levodopa to treat Parkinson's Disease. A peripheral decarboxylase inhibitor such as carbidopa or benzerazide is also preferably administered.
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