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2. 发明公开

EP0440324A3 Substituted beta-diketones and their use 失效
标题翻译：取代的BETA-DIKETONES及其使用
公开(公告)号：EP0440324A3
公开(公告)日：1993-06-16
申请号：EP91300005.5
申请日：1991-01-02
申请人： ORION-YHTYMÄ OY
发明人： Backstrom, Reijo Johannes , Honkanen, Erkki Juhani , Pystynen, Jarmo Johan , Luiro, Anne Maria , Aho, Paivi Annikki , Linden, Inge-Britt Yvonne , Nissinen, Erkki Aarne Olavi , Pohto, Pentti
IPC分类号： A61K31/255 , A61K31/165 , A61K31/12 , A61K31/345 , A61K31/38 , A61K31/44 , A61K31/47 , A61K31/19 , A61K31/275 , C07C309/73 , C07C309/66 , C07C49/567 , C07C65/38
CPC分类号： A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C205/45 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , C07C2601/02
摘要： Compounds of formula

wherein n is 0 or 1, R₁ and R₂ 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：式的化合物，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。

3. 发明公开

EP0440324A2 Substituted beta-diketones and their use 失效
标题翻译：取代基β-Diketone和deren Verwendung。
公开(公告)号：EP0440324A2
公开(公告)日：1991-08-07
申请号：EP91300005.5
申请日：1991-01-02
申请人： ORION-YHTYMÄ OY
发明人： Backstrom, Reijo Johannes , Honkanen, Erkki Juhani , Pystynen, Jarmo Johan , Luiro, Anne Maria , Aho, Paivi Annikki , Linden, Inge-Britt Yvonne , Nissinen, Erkki Aarne Olavi , Pohto, Pentti
IPC分类号： A61K31/255 , A61K31/165 , A61K31/12 , A61K31/345 , A61K31/38 , A61K31/44 , A61K31/47 , A61K31/19 , A61K31/275 , C07C309/73 , C07C309/66 , C07C49/567 , C07C65/38
CPC分类号： A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C205/45 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , C07C2601/02
摘要： Compounds of formula

wherein n is 0 or 1, R₁ and R₂ 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：式的化合物，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. 发明公开

EP0359439A1 Substituted pyridazinones 失效
标题翻译：取代哒嗪酮。
公开(公告)号：EP0359439A1
公开(公告)日：1990-03-21
申请号：EP89308767.6
申请日：1989-08-30
申请人： ORION-YHTYMÄ OY
发明人： Bäckström, Reijo Johannes , Heinola, Kalevi Evert , Nore, Pentti Tapio , Pystynen, Jarmo Johan , Sellin, Lawrence , Honkanen, Erkki Juhani , Haikala, Heimo Olavi
IPC分类号： C07D237/04 , C07D237/14 , C07D401/12 , C07D403/04 , A61K31/50
CPC分类号： C07D401/12 , C07D237/04 , C07D237/14 , C07D403/04
摘要： Substituted benzylideneiminophenylpyridazinones or dihydropyridazinones of formula I
in which R₁ and R₈ independently mean hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, trifluoromethyl, hydroxy alkyl, halogen alkyl, alkoxy alkyl, pyridyl, furyl, thienyl or cycloalkyl or one of optionally substituted groups; aryl, aralkyl, aralkenyl or nitrogen containing heterocyclic ring joining through an alkyl or alkenyl group and R₃, R₄ and R₅ independently mean hydrogen, lower alkyl, hydroxy alkyl, halogen, hydroxy, alkoxy, acyloxy, aroyloxy, formyl, acyl, cyano, amino, carboxy or trifluoromethyl, R₆ and R₇ independently mean hydrogen, amino, lower alkyl, hydroxy, nitro or cyano or R₂ and R₇ together form a -CH₂-NH- or -CH=N- group and A means phenyl, naphtyl or a nitrogen containing heterocyclic ring. The compounds may be used in the treatment of congestive heart failure.
摘要翻译：取代的亚苄基亚氨基苯基哒嗪酮或式I的二氢哒嗪酮其中R 1和R 8独立地表示氢或低级烷基，R 2是氢，低级烷基，三氟甲基，羟基烷基，卤素烷基，烷氧基烷基，吡啶基，呋喃基，噻吩基或环烷基或任选取代的基团; 通过烷基或烯基连接的芳基，芳烷基，芳烯基或含氮杂环，R3，R4和R5独立地表示氢，低级烷基，羟基烷基，卤素，羟基，烷氧基，酰氧基，芳氧基，甲酰基，酰基，氰基，氨基，羧基或三氟甲基，R6和R7独立地表示氢，氨基，低级烷基，羟基，硝基或氰基或R2和R7一起形成-CH 2 -NH-或-CH = N-基团，A表示苯基，萘基或氮含杂环。该化合物可用于治疗充血性心力衰竭。

5. 发明公开

EP0426468A3 Stabile polymorphic form of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide and the process for its preparation 失效
标题翻译：（E）-N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺的稳定多晶型及其制备方法
公开(公告)号：EP0426468A3
公开(公告)日：1992-05-06
申请号：EP90311963.4
申请日：1990-11-01
申请人： ORION-YHTYMÄ OY
发明人： Pippuri, Aino Kyllikki , Honkanen, Erkki Juhani , Haarala, Jorma Veikko
IPC分类号： C07C255/41
CPC分类号： C07C255/41
摘要： Stable and crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitro-phenyl)acrylamide may be prepared by crystallizing crude synthesis product from lower aliphatic carboxylic acid such as formic or acetic acid with a catalytic amount of hydrochloric or hydrobromic acid added. The product is a potent inhibitor of catechol-O-methyl-transferase enzyme (COMT).

6. 发明公开

EP0357403A3 Substituted beta-diketones 失效
标题翻译：取代的β-二酮
公开(公告)号：EP0357403A3
公开(公告)日：1992-02-05
申请号：EP89308779.1
申请日：1989-08-30
申请人： ORION-YHTYMÄ OY
发明人： Pohto, Pentti , Aho, Paivi Annikki , Backstrom, Reijo Johannes , Honkanen, Erkki Juhani , Linden, Inge-Britt Yvonne , Nissinen, Erkki Aarne Olavi
IPC分类号： C07C49/248 , C07C49/235 , C07C49/255 , C07C49/213 , C07C49/217 , C07C49/203 , C07D333/22 , C07D307/46 , C07C255/56 , A61K31/12
CPC分类号： A61K31/12 , A61K31/00 , A61K31/06
摘要： Compounds of formula

wherein R₁ and R₂ 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; R₃ 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：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，所述烷基，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及其盐，醚和酯可用作细胞保护剂，特别是作为抗促黄体素或胃保护剂。

7. 发明公开

EP0357403A2 Substituted beta-diketones 失效
标题翻译：取代基β-二酮。
公开(公告)号：EP0357403A2
公开(公告)日：1990-03-07
申请号：EP89308779.1
申请日：1989-08-30
申请人： ORION-YHTYMÄ OY
发明人： Pohto, Pentti , Aho, Paivi Annikki , Backstrom, Reijo Johannes , Honkanen, Erkki Juhani , Linden, Inge-Britt Yvonne , Nissinen, Erkki Aarne Olavi
IPC分类号： C07C49/248 , C07C49/235 , C07C49/255 , C07C49/213 , C07C49/217 , C07C49/203 , C07D333/22 , C07D307/46 , C07C255/56 , A61K31/12
CPC分类号： A61K31/12 , A61K31/00 , A61K31/06
摘要： Compounds of formula

wherein R₁ and R₂ 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; R₃ 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：式的化合物，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，杂芳基或氨基任选地取代; 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或胃保护剂。

8. 发明授权

EP0046635B1 Process for the preparation of cimetidine 失效
标题翻译：制备CIMETIDINE的方法
公开(公告)号：EP0046635B1
公开(公告)日：1985-07-03
申请号：EP81303378.4
申请日：1981-07-23
申请人： ORION-YHTYMÄ OY
发明人： Kairisalo, Pekka Juhani , Honkanen, Erkki Juhani
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07C323/44

9. 发明授权

EP0383449B1 Pyridazinone derivatives and processes for preparing the same 失效
标题翻译：哒嗪酮衍生物和它们的制备方法。
公开(公告)号：EP0383449B1
公开(公告)日：1995-09-06
申请号：EP90300875.3
申请日：1990-01-29
申请人： ORION-YHTYMÄ OY
发明人： Haikala, Heimo Olavi , Nore, Pentti Tapio , Honkanen, Erkki Juhani , Pystynen, Jarmo Johan , Lönnberg, Kari Kalevi , Luiro, Anne Maria , Pippuri, Aino Kyllikki
IPC分类号： C07D237/04 , C07D253/06 , C07D273/04 , C07D285/16 , C07D285/18 , A61K31/50 , A61K31/53 , A61K31/535
CPC分类号： C07D285/16 , C07D237/04 , C07D237/14 , C07D237/32 , C07D253/07 , C07D273/04 , C07D401/12

10. 发明公开

EP0383449A3 Pyridazinone derivatives and processes for preparing the same 失效
标题翻译：杂环化合物
公开(公告)号：EP0383449A3
公开(公告)日：1991-07-03
申请号：EP90300875.3
申请日：1990-01-29
申请人： ORION-YHTYMÄ OY
发明人： Haikala, Heimo Olavi , Nore, Pentti Tapio , Honkanen, Erkki Juhani , Pystynen, Jarmo Johan , Lönnberg, Kari Kalevi , Luiro, Anne Maria , Pippuri, Aino Kyllikki
IPC分类号： C07D237/04 , C07D253/06 , C07D273/04 , C07D285/16 , C07D285/18 , A61K31/50 , A61K31/53 , A61K31/535
CPC分类号： C07D285/16 , C07D237/04 , C07D237/14 , C07D237/32 , C07D253/07 , C07D273/04 , C07D401/12
摘要： New heterocyclic compounds of formula I
In which Het means one of following groups;
wherein R₁₁, R₁₃ and R₁₄ mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, -CH=CH-, or -CH₂-CH₂- group; R₁ and R₂ independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups;
wherein R₆ means hydrogen or lower alkyl group, R₈ means lower alkyl, R₇ means cyano or COOR₁₀, wherein R₁₀ means hydrogen or lower alkyl or R₁ and R₂ together form a susbtituted or unsubstituted 5 or 6 membered ring which may contain 1 or 2 heteroatom N; R₃, R₄, and R₅ mean independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.

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