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1. 发明授权

US6080743A 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives 失效
公开(公告)号：US6080743A
公开(公告)日：2000-06-27
申请号：US29525
申请日：1998-02-27
申请人： Pierre Acklin , Hans Allgeier , Yves Auberson , Michel Biollaz , Robert Moretti , Silvio Ofner , Siem Jacob Veenstra
发明人： Pierre Acklin , Hans Allgeier , Yves Auberson , Michel Biollaz , Robert Moretti , Silvio Ofner , Siem Jacob Veenstra
IPC分类号： A61K31/00 , A61K31/495 , A61K31/498 , A61K31/502 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61K31/662 , A61P25/28 , A61P43/00 , C07D241/44 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/12 , C07D491/113 , C07F9/6509
CPC分类号： C07D401/06 , C07D241/44 , C07D401/12 , C07D417/12 , C07F9/650994
摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), ##STR1## wherein one of the radicals R.sub.1, and R.sub.2 is a group R.sub.5 and the other is a group of formula --CH(R.sub.6)--alk--R.sub.7 (Ia), --alk--CH(R.sub.6 -R.sub.7 (Ib), --alk--N(R.sub.8)--X--R.sub.7 (Ic), --alk--N.sup.+ (R.sub.8)(R.sup.9)--X--R.sub.7 A.sup.- (Id), --alk--O--X--R.sub.7 (Ie) or --alk--S--X--R.sub.7 (If), R.sub.3, R.sub.4 and R.sub.5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R.sub.6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R.sub.7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R.sub.8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R.sub.7 and R.sub.8, together with X and the nitrogen atom bonding R.sub.8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R.sub.9 is an aliphatic or araliphatic radical, or R.sub.7, R.sub.8 and R.sub.9 together with X and the nitrogen atom bonding R.sub.8, R.sub.9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A.sup.- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R.sub.7 and R.sub.8 and the nitrogen atom bonding R.sub.8 and X or together with the nitrogen atom bonding R.sub.8, R.sub.9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

2. 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。

3. 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。

4. 发明授权

US5965562A Aroyl-piperidine derivatives 失效
标题翻译：芳酰基 - 哌啶衍生物
公开(公告)号：US5965562A
公开(公告)日：1999-10-12
申请号：US961546
申请日：1997-10-30
申请人： Silvio Ofner , Siem Jacob Veenstra , Walter Schilling
发明人： Silvio Ofner , Siem Jacob Veenstra , Walter Schilling
IPC分类号： C07D211/58 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/45 , A61K31/47 , A61K31/505 , A61P1/04 , A61P9/12 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl-amino)-piperidines of the formula ##STR1## wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及下式的新型N-（3,5-双 - 三氟甲基 - 苯甲酰基）-2-苄基-4-（氮杂萘甲酰基 - 氨基） - 哌啶，其中X和Y各自独立地为N和/或CH 并且环A是未取代的或被选自低级烷基，低级烷氧基，卤素，硝基和三氟甲基的取代基单取代或多取代; 及其盐，其用途，其制备方法和包含本发明化合物或其药学上可接受的盐的药物组合物。

5. 发明申请

US20100022500A1 Macrocyclic Lactams and Pharmaceutical Use Thereof 审中-公开
标题翻译：大环内酰胺及其制药用途
公开(公告)号：US20100022500A1
公开(公告)日：2010-01-28
申请号：US12566928
申请日：2009-09-25
申请人： Yves AUBERSON , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer MacHauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
发明人： Yves AUBERSON , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer MacHauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
IPC分类号： A61K31/395 , C07D245/02 , C07D291/02 , A61P25/00
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及下式的新型大环化合物其中R1，R2，R3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数为14 ，15,16或17，以游离碱形式或以酸加成盐形式，用于制备，用作药物和包含它们的药物组合物。

6. 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.

7. 发明授权

US07612055B2 Macrocyclic lactams and pharmaceutical use thereof 失效
标题翻译：大环内酰胺及其药物用途
公开(公告)号：US07612055B2
公开(公告)日：2009-11-03
申请号：US10577260
申请日：2004-11-04
申请人： Yves Auberson , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer Machauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
发明人： Yves Auberson , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer Machauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
IPC分类号： A01N43/00 , A61K31/33 , C07D245/00
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及下式的新型大环化合物其中R1，R2，R3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数为14 ，15,16或17，以游离碱形式或以酸加成盐形式，用于制备，用作药物和包含它们的药物组合物。

8. 发明授权

US07612054B2 Dibenzo[b,f]oxepine-10-carboxamides and pharmaceutical uses thereof 失效
标题翻译：二苯并[b，f]氧杂七环-10-甲酰胺及其药物用途
公开(公告)号：US07612054B2
公开(公告)日：2009-11-03
申请号：US10565456
申请日：2004-07-23
申请人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
发明人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
IPC分类号： A01N43/00 , A61K31/33 , C07D313/00
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to novel dibenzo[b,f]oxepine-10-carboxamides compound to a process for the preparation of such compounds of formula I, their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula I.
摘要翻译：本发明涉及新的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β-谷氨酸相关的神经和血管疾病，淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。

9. 发明授权

US09284284B2 Oxazine derivatives and their use in the treatment of disease 有权
公开(公告)号：US09284284B2
公开(公告)日：2016-03-15
申请号：US14350938
申请日：2012-10-11
申请人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： C07D265/30 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K31/5375 , A61K31/5377
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

10. 发明申请

US20100056490A1 Cyclic sulfones with aminobenzyl substitution useful as BACE inhibitors 失效
标题翻译：具有氨基苄基取代基的环砜用作BACE抑制剂
公开(公告)号：US20100056490A1
公开(公告)日：2010-03-04
申请号：US12500093
申请日：2009-07-09
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/397 , C07D401/12 , C07D205/02 , C07D335/02 , A61K31/4535 , A61K31/382 , A61P25/00 , A61P9/10
CPC分类号： C07D335/02 , C07D409/10 , C07D409/12 , C07D413/12 , C07F7/0812
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。

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