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21. 发明授权

US5929067A 1-aryl-2-acylamino-ethane compounds and their use as neurokinin especially neurokinin 1 antagonists 失效
标题翻译： 1-芳基-2-酰基氨基 - 乙烷化合物及其作为神经激肽，特别是神经激肽1拮抗剂的用途
公开(公告)号：US5929067A
公开(公告)日：1999-07-27
申请号：US913352
申请日：1997-08-21
申请人： Marc Gerspacher , Andreas Von Sprecher , Silvio Roggo , Robert Mah , Silvio Ofner , Siem Jacob Veenstra , Claudia Betschart , Yves Auberson , Walter Schilling
发明人： Marc Gerspacher , Andreas Von Sprecher , Silvio Roggo , Robert Mah , Silvio Ofner , Siem Jacob Veenstra , Claudia Betschart , Yves Auberson , Walter Schilling
IPC分类号： C07D249/08 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/454 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C231/02 , C07C231/12 , C07C237/22 , C07C255/29 , C07C311/51 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/20 , C07D211/16 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D211/62 , C07D213/40 , C07D213/70 , C07D213/81 , C07D215/46 , C07D223/12 , C07D223/16 , C07D231/38 , C07D233/60 , C07D235/16 , C07D235/28 , C07D239/28 , C07D239/42 , C07D241/14 , C07D241/20 , C07D295/13 , C07D295/135 , C07D295/14 , C07D295/18 , C07D295/185 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/10 , C07D521/00 , C07D223/10
CPC分类号： C07D213/40 , C07C237/22 , C07C255/29 , C07C311/51 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D213/70 , C07D215/46 , C07D223/12 , C07D231/12 , C07D231/38 , C07D233/56 , C07D235/16 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： 1-Aryl-2-acylaminoethane compounds of formula I ##STR1## wherein R.sub.1 -R.sub.4, X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1 antagonists.
摘要翻译： PCT No.PCT / EP96 / 00555 Sec。 371日期1997年8月21日 102（e）日期1997年8月21日PCT 1996年2月9日PCT公布。 WO96 / 26183 PCT出版物日期1961年8月29日 - 式I的芳基-2-酰基氨基乙烷化合物，其中R 1 -R 4，X和Am如说明书中所定义，具有有价值的药物性质，并且作为NK-1拮抗剂特别有效。

22. 发明授权

US4424366A Tricyclic imidyl derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US4424366A
公开(公告)日：1984-01-03
申请号：US349420
申请日：1982-02-16
申请人： Hans Zweifel , Walter Schilling , Angelo Storni , Daniel Bellus
发明人： Hans Zweifel , Walter Schilling , Angelo Storni , Daniel Bellus
IPC分类号： C07D209/50 , C07C61/39 , C07D209/58 , C07D209/66 , C07D209/70 , C07D209/76 , C07D405/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C08F8/30 , C08F20/00 , C08F20/34 , C08F20/36 , C08G73/00 , C08G73/10 , C08G85/00 , G03F7/038
CPC分类号： C07D491/04 , C07C61/39 , C07D209/66 , C07D209/70 , C08G85/00 , G03F7/0388
摘要： Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## �n=1 or 2, Y=a bridge member and X=a functional group! are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.
摘要翻译：描述了新的三环亚氨基衍生物，例如式[IMAGE] [n = 1或2，Y =桥连构件和X =官能团]的那些。新型三环亚氨基衍生物适用于通过结合到现有聚合物链中或通过根据定义通过聚合或缩聚与合适的官能团X从三环亚氨基衍生物构建聚合物链来制备可光致交联聚合物。通过这种方法获得的可光致交联聚合物可用于例如印刷胶印技术的印刷版，特别是作为光致抗蚀剂。

23. 发明授权

US4418199A Tricyclic imidyl derivatives 失效
公开(公告)号：US4418199A
公开(公告)日：1983-11-29
申请号：US349120
申请日：1982-02-16
申请人： Hans Zweifel , Walter Schilling , Angelo Storni , Daniel Bellus
发明人： Hans Zweifel , Walter Schilling , Angelo Storni , Daniel Bellus
IPC分类号： C07D209/50 , C07C61/39 , C07D209/58 , C07D209/66 , C07D209/70 , C07D209/76 , C07D405/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C08F8/30 , C08F20/00 , C08F20/34 , C08F20/36 , C08G73/00 , C08G73/10 , C08G85/00 , G03F7/038
CPC分类号： C07D491/04 , C07C61/39 , C07D209/66 , C07D209/70 , C08G85/00 , G03F7/0388
摘要： Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.

24. 发明授权

US4259338A Benzofuranyl-tetrahydropyridines and -piperidines, their acid addition salts and antidepressant preparations thereof 失效
标题翻译：苯并呋喃基 - 四氢吡啶和哌啶，它们的酸加成盐和抗抑郁药制剂
公开(公告)号：US4259338A
公开(公告)日：1981-03-31
申请号：US140405
申请日：1980-04-14
申请人： Romeo Paioni , Walter Schilling , Raymond Bernasconi
发明人： Romeo Paioni , Walter Schilling , Raymond Bernasconi
IPC分类号： C07D405/04 , A61K31/443 , A61K31/445 , A61P25/24 , A61P25/26 , C07D307/79 , C07D307/86 , C07D307/91 , A61K31/44 , C07D405/02
CPC分类号： C07D307/79 , C07D307/86 , C07D307/91
摘要： The present invention provides new benzofuranyl-tetrahydropyridines and -piperidines of the general formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are hydrogen or lower alkyl or together are lower alkylene, R.sub.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl and Y.sub.1 and Y.sub.2 are each hydrogen or together are an additional bond, and the ring A is not further substituted or is further substituted by lower alkyl, lower alkoxy, halogen with an atomic number not more than 35, cyano or hydroxyl and the pharmaceutically acceptable acid addition salts thereof, and antidepressant preparations containing these compounds. The compounds according to the invention have valuable pharmacological properties. In particular, they inhibit the absorption of serotonin by mesencephalic synaptosomes, the serotonin depletion induced in the brain of rats by H 75/12, the absorption of noradrenalin by mesencephalic synaptosomes in rats and the noradrenalin depletion induced in the brain of rats by H 77/77. In the same dosage they also effect inhibition of monoamino-oxidase in the brain of rats and in the liver of rats. Furthermore, they intensify the "head twitch" induced by 5-hydroxy-tryptophan, and are distinguished by good tolerance. The compounds of the general formula I and their pharmaceutically acceptable acid addition salts can therefore be used as psychopharmaceuticals and in particular as antidepressants.
摘要翻译：本发明提供了通式Ⅰ（I）的新的苯并呋喃基 - 四氢吡啶和哌啶，其中R 1和R 2彼此独立地是氢或低级烷基或一起是低级亚烷基，R 3是氢，低级烷基，低级烯基，低级炔基，环低级烷基或环低级烷基 - 低级烷基，Y 1和Y 2各自为氢或一起为附加键，并且环A不被进一步取代或进一步被低级烷基，低级烷氧基，原子数不超过35的卤素，氰基或羟基及其药学上可接受的酸加成盐，以及含有这些化合物的抗抑郁制剂。根据本发明的化合物具有有价值的药理学性质。特别是，它们通过中脑突触体抑制5-羟色胺的吸收，H75 / 12的大鼠脑内诱导的血清素消耗，大鼠中脑突触体的去甲肾上腺素的吸收以及大鼠脑内诱发的去甲肾上腺素的耗竭 / 77。在相同的剂量下，它们也影响大鼠脑和大鼠肝脏中单氨氧氧化酶的抑制。此外，它们加剧了由5-羟基色氨酸引起的“头部抽搐”，并且具有良好的耐受性。因此，通式I的化合物及其药学上可接受的酸加成盐可以用作心理药物，特别是抗抑郁药。

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