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11. 发明申请

WO1992018475A2 NEW CENTRALLY ACTING SUBSTITUTED PHENYLAZACYCLOALKANES 审中-公开
标题翻译：新的中央行动取代的苯甲酰氯
公开(公告)号：WO1992018475A2
公开(公告)日：1992-10-29
申请号：PCT/US1992002227
申请日：1992-03-26
申请人： THE UPJOHN COMPANY , SVENSSON, Kjell, Anders, Ivan , WIKSTRÖM, Håkan, Vilhem , CARLSSON, Per, Arvid, Emil , BOIJE, Anna, Maria, Persdotter , WATERS, Ross, Nicholas , SONESSON, Clas, Ake , STJERULOF, Nils, Peter , ANDERSSON, Bengt, Ronny , HANSSON, Lars, Olor
发明人： THE UPJOHN COMPANY
IPC分类号： C07D0
CPC分类号： C07D207/08 , C07D207/09 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/28 , C07D211/34 , C07D211/76 , C07D223/04 , C07D409/06 , C07D409/10 , C07D455/02 , C07D487/04
摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof wherein n is 0-3; R and R are independently H (provided only one is H at the same time), -OH (provided R is other than hydrogen), CN, CH2CN, 2- or 4-CF3, CH2CF3, CH2CHF2, CH=CF2, (CH2)2CF3, ethenyl, 2-propenyl, OSO2CH3, OSO2CF3, SSO2CF3, COR , COOR , CON(R )2, SOxCH3 (where, x is 0-2), SOxCF3, O(CH2)xCF3, SO2N(R )2, CH=NOR , COCOOR , COCOON(R )2, C1-8 alkyls, C3-8 cycloalkyls, CH2OR , CH2(R )2, NR SO2CF3, NO2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R is hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R (where m is 1-8), CH2SCH3 or a C4-C8 alkyl bonded to said nitrogen and one of its adjacent carbon atoms inclusive to form a cyclic structure; R is independently hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R where m is 1-8; R is phenyl, phenyl (substituted with a CN, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl), 2-thiophenyl, 3-thiophenyl, -NR CONR R , or -CONR R ; R and R are independently hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkylmethyl, C2-C8 alkenyl or C2-C8 alkynyl; and with the proviso that when R is 2-CN or 4-CN, R is H, R is n-Pr and n is 1 or 3 then such compound is a pure enantiomer. The formula (I) compounds possess selective pharmacological properties and are useful in treating central nervous system disorders related to dopamine receptor activity including depression symptoms, geriatric disorders in the improvement of mental and motor functions, schizophrenia, narcolepsy, MBD, obesitas, and disturbances of sexual functions and impotence.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中n为0-3; R 1和R 2独立地是H（同时只有一个是H），-OH（提供的R 4不是氢），CN，CH 2 CN，2-或4- CF 3，CH 2 CF 3 ，CH 2 CF 2，（CH 2）2 CF 3，乙烯基，2-丙烯基，OSO 2 CH 3，OSO 2 CF 3，SSO 2 CF 3，COR 4，COOR 4，CON（R 4）2，SO x CH 3（其中，x为0 -2），SO x CF 3，O（CH 2）x CF 3，SO 2 N（R 4）2，CH = NOR 4，COCOOR 4，COCOON（R 4）2，C 1-8烷基，环烷基，CH 2 OR 4，CH 2（R 4）2，NR 4 SO 2 CF 3，NO 2，卤素，2,3或4位的苯基，噻吩基，呋喃基，吡咯，恶唑，噻唑，N-吡咯啉，三唑，四唑或吡啶; R 3是氢，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基，3,3,3-三氟丙基，（CH 2）m R 5（其中m为1-8），CH 2 SCH 3或与所述氮键合的C 4 -C 8烷基及其相邻碳原子之一，以形成环状结构; R 4独立地是氢，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基，3,3,3-三氟丙基，，4-三氟丁基， - （CH 2）m R 5，其中m为1-8; R 5是苯基（被CN，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基），2-噻吩基， 3-噻吩基，-NR 6 CONR 6 R 7或-CONR 6 R 7; R 6和R 7独立地是氢，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基甲基，C 2 -C 8烯基或C 2 -C 8炔基; 并且条件是当R 1为2-CN或4-CN时，R 2为H，R 3为n-Pr，n为1或3，则该化合物为纯对映异构体。式（I）化合物具有选择性药理学性质，并且可用于治疗与多巴胺受体活性相关的中枢神经系统疾病，包括抑郁症状，改善精神和运动功能的老年疾病，精神分裂症，发作性睡病，脑血管疾病，肥胖症和干扰性功能和阳。。

12. 发明申请

WO1996029316A1 NEW SULFONE ESTER ANALOGUES OF iso-CLOZAPINE AND RELATED STRUCTURES: ATYPICAL NEUROLEPTICS 审中-公开
标题翻译：异硫氰酸酯的新型硫酸酯类似物及相关结构：原位神经元
公开(公告)号：WO1996029316A1
公开(公告)日：1996-09-26
申请号：PCT/SE1996000344
申请日：1996-03-19
申请人： WIKSTRÖM, Håkan , DE BOER, Peter , LIAO, Yi
IPC分类号： C07D243/38
CPC分类号： C07D281/14 , C07D243/38 , C07D267/18
摘要： A compound of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein R1 is H, (C1-C8) alkyl or haloalkyl or hydroxyalkyl, alkenyl, alkynyl, cyclopropylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; R2 is H, (C1-C8) alkyl, alkenyl, alkynyl, cyclopropylalkyl or (C1-C8) haloalkyl, hydroxyalkyl, hydroxyalkyloxyalkyl or 1-(alkyl-2-imidazolidinone); X is NH, NR1, O, S, SO, SO2. The compounds of this invention possess affinity to one or several receptor systems, e.g. DA (D1-D4), alpha 1, muscarinic (M1-M4) and 5-HT (5-HT2A, 5-HT2C and 5-HT7). The central nervous system disorders to be treated with the compounds of the present invention include psychoses-schizophrenia, autism, Tourette's syndrome, restless legs, Huntington's chorea, motion sickness, nausea, vomiting and severe anxiety.
摘要翻译：式（I）化合物或其药学上可接受的酸加成盐，其中R 1是H，（C 1 -C 8）烷基或卤代烷基或羟烷基，烯基，炔基，环丙基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基; R2是H，（C1-C8）烷基，烯基，炔基，环丙基烷基或（C1-C8）卤代烷基，羟烷基，羟基烷氧基烷基或1-（烷基-2-咪唑啉酮）。 X是NH，NR1，O，S，SO，SO2。本发明的化合物对一种或几种受体系统具有亲和力，例如， DA（D1-D4），α1，毒蕈碱（M1-M4）和5-HT（5-HT2A，5-HT2C和5-HT7）。用本发明化合物治疗的中枢神经系统疾病包括精神病精神分裂症，自闭症，图雷特综合征，不宁腿，亨廷顿氏舞蹈病，晕车症，恶心，呕吐和严重焦虑症。

13. 发明申请

WO1996021662A1 THE USE OF HETEROCYCLIC COMPOUNDS AS ANTIOXIDANTS, RADICAL SCAVENGERS, Fe2+ COMPLEXING AGENTS, TISSUE- AND/OR NEUROPROTECTANTS 审中-公开
标题翻译：作为抗氧化剂，放射治疗剂，Fe 2+复合物，组织和/或神经病变的杂环化合物的使用
公开(公告)号：WO1996021662A1
公开(公告)日：1996-07-18
申请号：PCT/SE1996000007
申请日：1996-01-09
申请人： RISE, Frode , WIKSTRÖM, Håkan , UGLAND, Sigurd , DIJKSTRA, Durk , GUNDERSEN, Lise-Lotte , DE BOER, Peter , BAST, Aalt , HAENEN, Guido , ANTONSEN, Öyvind, Gunnar , LIAO, Yi , NASIR, Achmad, Izuddin
IPC分类号： C07D471/14
CPC分类号： C07D209/80 , A61K31/4188 , C07D471/04 , C07D487/04 , C07F7/1804
摘要： The invention relates to the new use of compounds of formula (I), wherein X is a member selected from the group consisting of O, S, Se, Te, SO, SO2, SeO, SeO2, TeO, TeO2; for the manufacture of a pharmaceutical composition having the effect of an antioxidant, radical scavenger, Fe complexing agent, tissue- and/or neuroprotectant. The invention also relates to new compounds falling within Formula (I) and pharmaceutical compositions containing them as well as a method for the prevention or treatment of diseases causes by oxidative stress.
摘要翻译：本发明涉及式（I）化合物的新用途，其中X是选自O，S，Se，Te，SO，SO 2，SeO，SeO 2，TeO，TeO 2的成员; 用于制造具有抗氧化剂，自由基清除剂，Fe 2+络合剂，组织和/或神经保护剂的作用的药物组合物。本发明还涉及落入式（I）中的新化合物和含有它们的药物组合物以及用于预防或治疗由氧化应激引起的疾病的方法。

14. 发明申请

WO1996009282A1 IODINATED X-RAY CONTRAST MEDIA 审中-公开
标题翻译： IODINATED X-RAY对比媒体
公开(公告)号：WO1996009282A1
公开(公告)日：1996-03-28
申请号：PCT/GB1995002265
申请日：1995-09-22
申请人： NYCOMED IMAGING A/S , REED, Michael, Antony , ALMÉN, Torsten , ANDERSSON, Sven , WISTRAND, Lars-Göran , GOLMAN, Klaes , ANTONSEN, Oyvind , FOSSHEIM, Rune , WIGGEN, Unni, Nordby , WIKSTRÖM, Håkan , KLINGSTEDT, Tomas , LEUNBACH, Ib , BERG, Arne , DUGSTAD, Harald
发明人： NYCOMED IMAGING A/S , REED, Michael, Antony
IPC分类号： C07C237/46
CPC分类号： C07C33/46 , A61K49/0433 , C07C33/483 , C07C235/16 , C07C237/46
摘要： The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula (I), wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one, and preferably two or three, R groups in each C6R5 moiety being M or M1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M1 independently represents a C1-4alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M1 moiety; with the proviso that where n is zero either at least one M1 group other than a hydroxymethyl or 1,2-dihydroxyethyl group is present or then if one hydroxymethyl or 1,2-dihydroxyethyl M1 group is present at least one nitrogen-attached or hydroxylated-C3-4 alkyl moiety-containing M group is also present and isomers thereof.
摘要翻译：本发明提供了可用作式（I）的X射线造影剂的低粘度碘化芳基化合物，其中n为0或1，并且其中n为1，每个C 6 R 5部分可以相同或不同; 每个基团R是氢原子，碘原子或亲水部分M或M1，每个C 6 R 5部分中两个或三个不相邻的R基团是碘，并且每个C 6 R 5部分中至少一个，优选两个或三个R基团是M或M1部分; X表示键或提供连接两个C 6 R 5部分的1至7个原子链的基团，或其中n为0，X表示基团R; 每个M独立地是非离子亲水部分; 并且每个M1独立地表示被至少一个羟基取代的C 1-4烷基，并且任选地通过羰基，砜或亚砜基与苯环连接，至少一个R基团是M1部分; 条件是在n为0的情况下，至少一个除羟甲基或1,2-二羟乙基之外的M1基团存在或如果一个羟甲基或1,2 - 二羟乙基M1基团存在至少一个含氮连接或羟基化的含C3-4烷基部分的M基团以及其异构体。

15. 发明申请

WO1995000478A1 ARYLTRIFLATES AND RELATED COMPOUNDS 审中-公开
标题翻译：亚苄基和相关化合物
公开(公告)号：WO1995000478A1
公开(公告)日：1995-01-05
申请号：PCT/DK1994000244
申请日：1994-06-20
申请人： H. LUNDBECK A/S , WIKSTRÖM, Håkan , BARF, Tjeerd, Andries
发明人： H. LUNDBECK A/S
IPC分类号： C07D207/09
CPC分类号： C07D265/30 , C07C309/66 , C07C2603/40 , C07D207/09 , C07D209/14 , C07D209/16 , C07D209/88 , C07D211/14 , C07D211/58 , C07D219/10 , C07D221/10 , C07D223/22 , C07D277/82 , C07D401/12 , C07D405/04 , C07D405/12 , C07D487/04 , C07J31/006
摘要： Described are aryltriflates and related derivatives of raclopride, riluzole, cisapride, omeprazole, lanzoprazole, pantoprazole, paroxetine, fenfluramine, sotalol, estradiol, RU 486, tacrine, moclobemide, ifenprodil, brofaromine, melatonin, N-Acetyl-2[(7-trifluoromethylsulfonyloxy-1-naphtyl)ethyl]amine, prenalterol, sumatriptane, 6-substituted 3-amino-1,2,3,4-tetrahydrocarbazole, mianserin, trans-(4aS, 10bS)-7-hydroxy-4-n-Propyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinoline and carbamazepine. The compounds are useful as drugs with, in particular for the treatment of disorders of the central nervous system.
摘要翻译：描述了格列吡嗪，利鲁唑，西沙必利，奥美拉唑，兰唑唑，泮托拉唑，奥美拉唑，芬氟拉明，索他洛尔，雌二醇，RU 486，他克林，吗氯贝胺，ifenprodil，溴吡啶，褪黑激素，N-乙酰基-2 [（7-三氟甲基磺酰氧基 -1-萘基）乙基]胺，前列氮醇，舒沙普坦，6-取代的3-氨基-1,2,3,4-四氢咔唑，米安思林，反 - （4aS，10bS）-7-羟基-4-正丙基 - 1,2,3,4,4a，5,6,10b-八氢苯并[f]喹啉和卡马西平。该化合物可用作特别用于治疗中枢神经系统疾病的药物。

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