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1. 发明授权

US06951875B2 Conjugated aromatic compounds with a pyridine substituent 失效
标题翻译：具有吡啶取代基的共轭芳族化合物
公开(公告)号：US06951875B2
公开(公告)日：2005-10-04
申请号：US10277002
申请日：2002-10-21
申请人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
IPC分类号： A61K31/44 , A61K31/381 , A61K31/4409 , A61K31/4418 , A61K31/4436 , A61P21/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D213/38 , C07D213/73 , C07D213/74 , C07D409/04
CPC分类号： C07D213/73 , C07D213/38 , C07D213/53 , C07D213/74 , C07D213/79 , C07D213/84 , C07D409/04
摘要： The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.
摘要翻译：本发明涉及式的化合物本发明的化合物是NMDA（N-甲基-D-天冬氨酸）受体亚型阻断剂，用于治疗与该受体有关的疾病。

2. 发明授权

US06831087B2 Pyridine substituted isoquinoline derivatives 失效
标题翻译：吡啶取代的异喹啉衍生物
公开(公告)号：US06831087B2
公开(公告)日：2004-12-14
申请号：US10282365
申请日：2002-10-29
申请人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
IPC分类号： C07D40102
CPC分类号： C07D401/04
摘要： The invention relates to compounds of formulae: Compounds of the invention have a good affinity to the NMDA receptor and are useful for the treatment of diseases related to this receptor.
摘要翻译：本发明涉及式的化合物：本发明化合物对NMDA受体具有良好的亲和力，可用于治疗与该受体有关的疾病。

3. 发明授权

US06359138B1 4-hydroxy-piperidine derivatives 失效
标题翻译： 4-羟基 - 哌啶衍生物
公开(公告)号：US06359138B1
公开(公告)日：2002-03-19
申请号：US08976540
申请日：1997-11-24
申请人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , René Wyler
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/48 , C07D405/06
摘要： The present invention relates to 4-hydroxy-piperidine derivatives of the general formula wherein X denotes —O—, —NH—, —CH2—, —CH═, —CHOH—, —CO—, —S—, —SO— or —SO2—; R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido; R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy; a and b may be a double bond, provided that when “a” is a double bond, “b” cannot be a double bond; n is 0-2; m is 1-3; p is 0 or 1 and to pharmaceutically acceptable addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.
摘要翻译：本发明涉及通式为Ⅳ的4-羟基 - 哌啶衍生物，其中X表示-O - ， - NH - ， - CH 2 - ， - CH =， - CHOH-， - CO - ， - S - ， - SO-或-SO 2 - ; R 1 -R 4彼此独立地为氢，羟基，低级 - 烷基 - 磺酰基氨基，1-或2-咪唑基或乙酰氨基; R5-R8彼此独立地为氢，羟基，低级 - 烷基，卤素低级烷氧基，三氟甲基或三氟甲氧基; a和b可以是双键，条件是当“a”是双键时，“b”不能是双键; n是0-2; m是1-3; p是0或1，以及其药学上可接受的加成盐。本发明的化合物是NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂，其可用于介导中枢神经系统发育的过程，包括学习和记忆形成和功能。

4. 发明授权

US06265426B1 Triazole derivatives 失效
标题翻译：三唑衍生物
公开(公告)号：US06265426B1
公开(公告)日：2001-07-24
申请号：US09619518
申请日：2000-07-19
申请人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
IPC分类号： C07D24914
CPC分类号： C07D233/64 , C07D249/08 , C07D401/06 , C07D403/10 , C07D405/10
摘要： The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
摘要翻译：本发明涉及式I的三唑和咪唑衍生物及其药学上可接受的酸加成盐。这些化合物是NMDA受体亚型阻断剂，可用于治疗与NMDA受体有关的疾病。

5. 发明授权

US06451819B2 Heterocyclic compounds useful as NMDA receptor selective subtype blockers 失效
标题翻译：可用作NMDA受体选择亚型阻断剂的杂环化合物
公开(公告)号：US06451819B2
公开(公告)日：2002-09-17
申请号：US09833450
申请日：2001-04-12
申请人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , Rene Wyler
IPC分类号： A61K31435
CPC分类号： C07D263/58 , C07D205/04 , C07D207/12 , C07D209/34 , C07D211/54 , C07D231/56
摘要： The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q, X, A, Y B are as defined in the specification.
摘要翻译：本发明涉及通过选择性阻断NMDA受体来治疗神经变性，其中化合物是由羟基，低级烷基，卤素，氨基，硝基，苄氧基或低级烷氧基 - 低级烷氧基取代的吡啶基或苯基，或其中Z 1为五含有一个或两个选自N或O的杂原子; R 1是氢，羟基或氧代基; Ar 2是吡啶基或苯基，任选地被羟基，低级烷基，卤素，氨基，硝基，苄氧基或低级烷氧基 - 低级烷氧基，或者是其中Z 2是五或六元环的基团，其任选地含有一个或两个选自N或O的杂原子; 且Q，X，A，Y B如说明书中所定义。

6. 发明授权

US06432985B1 Neuroprotective substituted piperidine compounds with activity as NMDA NR2B subtype selective antagonists 有权
公开(公告)号：US06432985B1
公开(公告)日：2002-08-13
申请号：US09811888
申请日：2001-03-19
申请人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , Rene Wyler
IPC分类号： A61K31445
摘要： The invention relates to a compound of the formula its R,R-, S,S-enantiomers and racemic mixtures thereof and to their pharmaceutically acceptable acid addition salts. The compound of formula I and its R,R- and S,S-enantiomers may be used as medicaments for the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

7. 发明授权

US06407235B1 Prodrug acid esters of [2-(4-benzyl-3-hydroxy-piperidin-1-yl)-ethansulfonyl]phenol 有权
标题翻译： [2-（4-苄基-3-羟基 - 哌啶-1-基） - 乙二磺酰基]苯酚的前药酸酯
公开(公告)号：US06407235B1
公开(公告)日：2002-06-18
申请号：US09931431
申请日：2001-08-16
申请人： Alexander Alanine , Bernd Buettelmann , Holger Fischer , Marie-Paule Heitz Neidhart , Joerg Huwyler , Georg Jaeschke , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Holger Fischer , Marie-Paule Heitz Neidhart , Joerg Huwyler , Georg Jaeschke , Emmanuel Pinard , René Wyler
IPC分类号： C07D21142
CPC分类号： C07D211/42 , C07F9/59
摘要： The invention is a compound of the formula wherein R is a) —C(O)(CH2)nC(O)OH, b) wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl, c) —P(O)(OH)2, or is d) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); and R2/R3 are hydrogen or lower alkyl; n is 1, 2, 3 or 4; or a pharmaceutically acceptable acid addition salt thereof
摘要翻译：本发明是式（I）-C（O）（CH 2）n C（O）OH，b）其中R 1是-N（R 2）（R 3）的化合物，或者是五或六元芳族或非芳香族的化合物 c）-P（O）（OH）2或isd）-C（O）（CH 2）n NHC（O）（O）（O） CH2）nN（R2）（R3）; 和R2 / R3是氢或低级烷基; n是1,2,3或4;或其药学上可接受的酸加成盐

8. 发明授权

US06339093B1 Isoquinoline derivatives 失效
标题翻译：异喹啉衍生物
公开(公告)号：US06339093B1
公开(公告)日：2002-01-15
申请号：US09669648
申请日：2000-09-26
申请人： Alexander Alanine , Serge Burner , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Serge Burner , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
IPC分类号： A61K3147
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to compounds of the formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is hydrogen, lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-yl-methanol or —NHCH2CHROH; R3 is hydrogen or halogen; R is hydrogen, lower alkyl or —CH2OH; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof which are are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.
摘要翻译：本发明涉及式Ⅳ的化合物是氢，低级烷基，低级烷氧基，羟基，氨基，硝基，氰基，低级烷基 - 氨基，二 - 低级烷基 - 氨基或卤素; R2是氢，低级烷基，氨基， -3-醇，吡咯烷-2-基 - 甲醇或-NHCH 2 CHROH; R 3为氢或卤素; R为氢，低级烷基或-CH 2 OH; n为1或2;以及其药学上可接受的酸加成盐，其为NMDA （N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂。

9. 发明授权

US6153624A Pyrrolidine and piperidine derivatives and treatment of neurodegenerative disorders 失效
标题翻译：吡咯烷和哌啶衍生物和治疗神经退行性疾病
公开(公告)号：US6153624A
公开(公告)日：2000-11-28
申请号：US362932
申请日：1999-07-28
申请人： Alexander Alanine , Bernd Buttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
IPC分类号： C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04
CPC分类号： A61K31/5383 , A61K31/40 , A61K31/4025 , A61K31/424 , A61K31/437 , A61K31/445
摘要： The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH3; or taken together are --O--CH.sub.2 --O--;R.sup.5 is hydrogen or lower alkyl;X and Y are, independently from each other --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)-; andin, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.
摘要翻译：本发明涉及以下通式的吡咯烷和哌啶衍生物的用途：其中R 1和R 2彼此独立地为氢，低级烷氧基，羟基，卤素，-CONH 2或-C（O）O-低级烷基; 或一起使用-O-CH 2 O; R 3和R 4彼此独立地为氢，低级烷氧基，苄氧基，卤素，羟基，-CONH 2或-SCH 3; 或一起为-O-CH 2 -O-; R5是氢或低级烷基; X和Y彼此独立地为-CH（OH） - ， - （CH 2）n - ， - C（O） - 或-CH（低级烷氧基） - ; 而n，p为1或2; 以及其药学上可接受的加成盐，用于治疗由NMDA受体亚型的过度活化引起的疾病。

10. 发明授权

US5889026A 4-hydroxy-piperodine derivatives 失效
标题翻译： 4-羟基 - 胡萝卜素衍生物
公开(公告)号：US5889026A
公开(公告)日：1999-03-30
申请号：US891781
申请日：1997-07-14
申请人： Alexander Alanine , Bernd Buttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
发明人： Alexander Alanine , Bernd Buttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
IPC分类号： C07D211/14 , A61K31/445 , A61K31/452 , A61K31/4523 , A61P25/00 , A61P25/16 , A61P25/28 , A61P43/00 , C07D20060101 , C07D211/18 , C07D211/20 , C07D211/48 , C07D401/06 , C07D401/08 , C07D401/12 , C07D521/00 , C07D211/00 , A01N43/40
CPC分类号： C07D231/12 , C07D211/48 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12
摘要： The present invention relates to compounds of the formula ##STR1## wherein x is --O--, --NH--, --CH.sub.2 --, --CH.dbd., --CO.sub.2 --, --CONH--, --CON(lower alkyl)--, --S-- and --SO.sub.2 --;R.sup.1 -R.sup.4 are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido;R.sup.5, R.sup.6 are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo;R.sup.7 -R.sup.10 are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy;n is 0 or 1;and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.
摘要翻译：本发明涉及下式化合物其中x为-O - ， - NH - ， - CH 2 - ， - CH =， - CO 2 - ， - CONH-，-CON（低级烷基） - ， - - 和-SO 2 - ; R 1 -R 4彼此独立地为氢，卤素，羟基，氨基，硝基，低级烷基 - 磺酰基氨基，1-或2-咪唑基，1-（1,2,4-三唑基）或乙酰氨基; R5，R6彼此独立地为氢，低级烷基，羟基，低级烷氧基或氧代; R 7 -R 10彼此独立地为氢，低级烷基，卤素，三氟甲基或低级烷氧基; n为0或1; 及其药学上可接受的酸加成盐。本发明化合物是NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂。

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