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21. 发明申请

US20120264748A1 DIAZA-SPIRO[5.5]UNDECANES 失效
标题翻译： DIAZA-SPIRO [5.5] UNDECANES
公开(公告)号：US20120264748A1
公开(公告)日：2012-10-18
申请号：US13517111
申请日：2010-12-20
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Simona Cotesta , Jürgen Hans-Hermann Hinrichs , Silvio Ofner , Chetan Pandit , Jürgen Wagner
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Simona Cotesta , Jürgen Hans-Hermann Hinrichs , Silvio Ofner , Chetan Pandit , Jürgen Wagner
IPC分类号： C07D471/10 , A61K31/438 , A61K31/506 , A61K31/5377 , A61P3/00 , A61K31/5025 , A61P25/00 , A61P25/30 , A61P25/28 , A61K31/502 , A61K31/538
CPC分类号： C07D471/10
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

22. 发明申请

US20080146647A1 ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有MGLUR 5拮抗活性的乙酰衍生物
公开(公告)号：US20080146647A1
公开(公告)日：2008-06-19
申请号：US12040081
申请日：2008-02-29
申请人： Fabrizio Gasparini , Yves Auberson , Silvio Ofner
发明人： Fabrizio Gasparini , Yves Auberson , Silvio Ofner
IPC分类号： A61K31/404 , C07D209/04 , A61P43/00
CPC分类号： C07C271/16 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12
摘要： The invention provides compounds of formula I wherein n, A, R, R′, R″, Ro, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
摘要翻译：本发明提供式I化合物，其中n，A，R，R'，R“，R”，X和Y如说明书中所定义，及其制备。式I的化合物可用作药物。

23. 发明授权

US06117873A Substituted aminoalkane phosphonic acids 有权
标题翻译：取代的氨基烷烃膦酸
公开(公告)号：US06117873A
公开(公告)日：2000-09-12
申请号：US297010
申请日：1999-04-23
申请人： Pierre Acklin , Hans Allgeier , Yves Auberson , Silvio Ofner , Siem Jacob Veenstra
发明人： Pierre Acklin , Hans Allgeier , Yves Auberson , Silvio Ofner , Siem Jacob Veenstra
IPC分类号： A61K31/675 , A61P9/00 , A61P25/00 , A61P25/08 , A61P43/00 , C07F9/6509 , A61K31/495 , C07F9/02
CPC分类号： C07F9/650994
摘要： Compounds of the formula I ##STR1## in which R.sub.1 is hydroxyl or an aliphatic, araliphatic or aromatic radical,X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical,R.sub.2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene andR.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro,and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.
摘要翻译： PCT No.PCT / EP97 / 05843 Sec。 371日期1999年4月23日第 102（e）1999年4月23日PCT PCT 1997年10月22日PCT公布。第WO98 / 17672号PCT公告日期：1998年4月30日，其中R 1为羟基或脂族，芳脂族或芳族基团的式I化合物，X为二价脂族，脂环族，脂环族 - 脂族，芳脂族，杂芳基脂族或芳族基团，R2为氢或脂族或芳族芳脂肪族基团，烷基是亚烷基，R3，R4和R5彼此独立地是氢，低级烷基，卤素，三氟甲基，氰基或硝基，并且它们的盐可用于治疗响应兴奋性氨基酸阻断的病理状况酸受体和用于制备药物制剂。

24. 发明授权

US5935951A 1-acyl-4-aliphatylaminopiperidine compounds 失效
公开(公告)号：US5935951A
公开(公告)日：1999-08-10
申请号：US809277
申请日：1997-03-05
申请人： Silvio Ofner , Siem Jacob Veenstra
发明人： Silvio Ofner , Siem Jacob Veenstra
IPC分类号： A61K31/445 , A61K31/4468 , A61K31/451 , A61P43/00 , C07D211/58 , A61K31/54 , A61K31/43 , C07D211/08 , C07D417/60
CPC分类号： C07D211/58
摘要： The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.5 is (i) hydrogen, alkyl or alkyl which is substituted by halogen, lower alkoxy amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, (ii) hydroxyl, cycloalkoxy, lower alkoxy or lower alkoxy which is substituted by lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylamino-alkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, or (iii) amino or amino substituted by lower alkyl, cycloalkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene; X.sub.1 is methyelene, ethylene, a direct bond; a free or ketalized carbonyl group or a free or etherified hydroxymethylene group and n is 0 or 1, and their salts, processes for the preparation of the compounds according to the invention, pharmaceutical compositions containing these and their use as pharmaceutical active ingredients.

25. 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。

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