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1.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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3.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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