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1. 发明授权

US06809088B2 Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译： 2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06809088B2
公开(公告)日：2004-10-26
申请号：US10191950
申请日：2002-07-09
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
IPC分类号： A61K3133
CPC分类号： C07D333/34 , C07D333/38 , C07D409/12 , C07D417/12
摘要： The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac or cerebral infarctions. These compounds include: N-{4-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2-carboximidamide; N-{3-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2-carboximidamide; N-(4-{[{[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}(methyl)amino]methyl}phenyl)thiophene-2-carboximidamide; N-[3-({[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-(3-{[(3,5-di-tert-butyl-4-hydroxybenzyl)amino]methyl}phenyl)thiophene-2-carboximidamide; N-[3-({[2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-[3-({[3-(4-hydroxy-3,5-diisopropylphenyl)propyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-(3-{[(4-hydroxy-3,5-diisopropylbenzyl)amino]methyl}phenyl) thiophene-2-carboximidamide; N-[3-({[2-(4-hydroxy-3,5-diisopropylphenyl)ethyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-2-(3,5-di-tert-butyl-4-hydroxybenzoyl)-N-1-(4-{[imino(thien-2-yl)methyl]amino}phenyl)-L-leucinamide; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及作为NO合酶抑制剂的2-（亚氨基甲基）氨基 - 苯基的新衍生物，并可捕获活性氧。这些化合物可以显着地用于治疗中风，神经变性疾病和缺血性或血液性心脏病或脑梗塞。这些化合物包括：N- {4 - [（{[4-（3,5-二叔丁基 -4-羟基苯基）-1,3-噻唑-2-基]甲基}氨基）甲基]苯基}噻吩-2-甲脒; N- {3 - [（{[4-（3,5-二 - 丁基-4-羟基苯基）-1,3-噻唑-2-基]甲基}氨基）甲基]苯基}噻吩-2-甲脒; N-（4 - {[{[4-（3,5-二叔丁基（3-（3,5-二叔丁基-4-羟基苯基）-1,3-噻唑-2-基]甲基}（甲基）氨基]甲基}苯基）噻吩-2-甲脒; N-〔3 - 二 - 叔丁基-4-羟基苯基）丙基]氨基}甲基）苯基]噻吩-2-甲脒; N-（3 - {[（3,5-二叔丁基-4-羟基苄基）氨基]甲基} 苯基）噻吩-2-甲脒; N- [3 - （{[2-（3,5-二叔丁基-4-羟基苯基）乙基]氨基}甲基）苯基]噻吩-2-甲脒; N- [ 3 - （{[3-（4-羟基-3,5-二异丙基苯基）丙基]氨基}甲基）苯基]噻吩-2-甲脒; N-（3 - {[（4-羟基-3,5-二异丙基苄基）氨基]甲基}苯基）硫代 2- [3 - （{[2-（4-羟基-3,5-二异丙基苯基）乙基]氨基}甲基）苯基]噻吩-2-亚甲代酰胺; N-2- 二 - 叔丁基-4-羟基苯甲酰基）-N-1-（4 - {[亚氨基（噻吩-2-基）甲基]氨基}苯基）-L-亮氨酰胺;及其药学上可接受的盐。

2. 发明授权

US06599903B2 Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译： 2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06599903B2
公开(公告)日：2003-07-29
申请号：US09945782
申请日：2001-09-04
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
IPC分类号： A61K315523
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12
摘要： Intermediate compounds having the formula wherein the substituents are defined as set forth in the disclosure.
摘要翻译：具有取代基的取代基的中间体化合物如本公开所述定义。

3. 发明授权

US06340700B1 2-(iminomethyl) amino-phenyl derivatives, preparation, application as medicines and pharmaceutical compositions containing same 有权
标题翻译： 2-（亚氨基甲基）氨基 - 苯基衍生物，制备，作为药物的应用和含有它们的药物组合物
公开(公告)号：US06340700B1
公开(公告)日：2002-01-22
申请号：US09381749
申请日：1999-09-22
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet
IPC分类号： A61K3138
CPC分类号： C07C235/30 , C07C235/56 , C07C275/36 , C07C281/14 , C07D209/42 , C07D243/08 , C07D295/185 , C07D295/192 , C07D311/66 , C07D333/38 , C07D409/12 , C07D409/14
摘要： A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
摘要翻译：取代基中的取代基的化合物如说明书中所定义，并且其药学上可接受的盐具有NOS和ROS活性。

4. 发明授权

US06300499B1 &agr;1-adrenergic receptor antagonists 失效
标题翻译： α1-肾上腺素能受体拮抗剂
公开(公告)号：US06300499B1
公开(公告)日：2001-10-09
申请号：US09155535
申请日：1998-09-28
申请人： Dennis Bigg , Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Michel Auguet
发明人： Dennis Bigg , Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Michel Auguet
IPC分类号： C07D24104
CPC分类号： C07D295/13
摘要： Phenylpiperazine derivatives having high affinity for the &agr;1-adrenoreceptor and pharmaceutical compositions containing them. Also disclosed is a method of using the such derivatives to treat benign prostatic hyperplasia.
摘要翻译：对α1-肾上腺素受体具有高亲和力的苯基哌嗪衍生物和含有它们的药物组合物。还公开了使用这些衍生物治疗良性前列腺增生的方法。

5. 发明授权

US06630461B2 Derivatives of 2-(iminomethyl) amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译： 2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06630461B2
公开(公告)日：2003-10-07
申请号：US09882264
申请日：2001-06-15
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
IPC分类号： A61K31395
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12
摘要： A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein A selected from the group consisting of hydrogen and wherein the substituents are defined as set forth in the specification.
摘要翻译：一种用于治疗温血动物中的神经退行性疾病的方法，其包括向有需要的温血动物施用一定数量的选自氢并且其中所述取代基的选择性化合物的化合物定义如说明书。

6. 发明授权

US06335445B1 Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 有权
标题翻译： 2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06335445B1
公开(公告)日：2002-01-01
申请号：US09456205
申请日：1999-12-07
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
IPC分类号： C07D24104
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12
摘要： A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.
摘要翻译：选自由下列组成的组的化合物选自由以下组成的组中，并且其它取代基在本说明书中定义，其具有产生氮一氧化物的NO合成酶和/或捕获的活性的抑制活性活性氧。

7. 发明授权

US06586454B2 Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 有权
标题翻译： 2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06586454B2
公开(公告)日：2003-07-01
申请号：US09953682
申请日：2001-09-17
申请人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
发明人： Pierre Etienne Chabrier de Lassauniere , Serge Auvin , Dennis Bigg , Michel Auguet , Jeremiah Harnett
IPC分类号： A61K31425
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12
摘要： A compound of the formula XXV(H) wherein the substituents are defined as set forth in the specification which are useful intermediates for the production of derivatives of 2-(iminomethyl)-amino-phenyl having inhibitory activity on NO-synthase enzymes.
摘要翻译：式XXV（H）的化合物，其中取代基如本说明书所述定义，其是制备具有对NO-合酶的抑制活性的2-（亚氨基甲基） - 氨基 - 苯基的衍生物的有用中间体。

8. 发明申请

US20080207709A1 Thiazole Derivatives for Treating Dyskinesias Caused by a Chemical Treatment 有权
标题翻译：噻唑衍生物治疗由化学治疗引起的运动障碍
公开(公告)号：US20080207709A1
公开(公告)日：2008-08-28
申请号：US11995092
申请日：2006-07-07
申请人： Pierre-Etienne Chabrier De Lassauniere , Michel Auguet , Brigitte Spinnewyn
发明人： Pierre-Etienne Chabrier De Lassauniere , Michel Auguet , Brigitte Spinnewyn
IPC分类号： A61K31/425 , A61P43/00
CPC分类号： A61K31/426 , A61K31/198 , A61K31/427 , C07D277/28
摘要： The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of dyskinesias caused by a chemical treatment. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of dyskinesias caused by a chemical treatment.
摘要翻译：本发明涉及具有通式（I）的噻唑衍生物在制备用于治疗或预防由化学治疗引起的运动障碍的药物中的用途。本发明还涉及具有通式（I）的噻唑衍生物和选自神经安定药或作用于多巴胺能系统的产品的至少一种化合物的组合，用于治疗或预防由化学治疗引起的运动障碍。

9. 发明授权

US06872738B1 Product comprising at least a no synthase inhibiting substance associated with at least a phospholipase a2 inhibiting substance 失效
标题翻译：至少含有与至少磷脂酶a2抑制物质相关联的无合酶抑制物质的产品
公开(公告)号：US06872738B1
公开(公告)日：2005-03-29
申请号：US10111139
申请日：2000-11-03
申请人： Michel Auguet , Pierre-Etienne Chabrier de Lassauniere
发明人： Michel Auguet , Pierre-Etienne Chabrier de Lassauniere
IPC分类号： A61K45/00 , A61K31/155 , A61K31/343 , A61K31/36 , A61K31/416 , A61K31/427 , A61K31/473 , A61K45/06 , A61P1/00 , A61P1/08 , A61P1/10 , A61P1/12 , A61P3/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/28 , A61P27/00 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P41/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/343 , A61K31/416 , A61K31/427 , A61K31/473 , A61K2300/00
摘要： The invention concerns a product comprising at least a NO synthase inhibiting substance associated with at least a phospholipase A2 inhibiting substance, separately or combined, for simultaneous therapeutic use, separately or spread over time for treating pathologies in which nitrogen monoxide and/or phospholipases A2 are involved. The invention also concerns a pharmaceutical composition comprising, an active principle, at least a NO synthase inhibiting substance and at least a phospholipase A2 inhibiting substance, and optionally a pharmaceutically acceptable.
摘要翻译：本发明涉及包含至少一种与至少一种磷脂酶A2抑制物质相关联的NO合成酶抑制物质的产品，其单独或组合用于同时治疗用途，分开或随着时间推移用于治疗其中一氧化氮和/或磷脂酶A2为涉及。本发明还涉及一种药物组合物，其包含活性成分，至少一种NO合成酶抑制物质和至少一种磷脂酶A2抑制物质，以及任选的药学上可接受的物质。

10. 发明授权

US09080220B2 Simultaneous, separate or sequential therapeutic use of at least one botulinum neurotoxin and of at least one opiate derivative 有权
标题翻译：至少一种肉毒杆菌神经毒素和至少一种阿片衍生物的同时，单独或连续的治疗用途
公开(公告)号：US09080220B2
公开(公告)日：2015-07-14
申请号：US12305191
申请日：2007-06-11
申请人： Michel Auguet , Christine Favre , Pierre-Etienne Chabrier De Lassauniere
发明人： Michel Auguet , Christine Favre , Pierre-Etienne Chabrier De Lassauniere
IPC分类号： A61K38/48 , A61K39/08 , A61K9/00 , A61K31/485 , A61K45/06
CPC分类号： C12Y304/24069 , A61K31/485 , A61K38/4893 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a composition comprising: at least one botulinum neurotoxin, and at least one opiate derivative or its salt. The invention also relates to a product comprising at least one botulinum neurotoxin and at least one opiate derivative or its salt, as a combination product for simultaneous, separate or sequential therapeutic use in the treatment or prevention of pain and of neuromuscular disorders.
摘要翻译：本发明涉及一种组合物，其包含：至少一种肉毒杆菌神经毒素和至少一种阿片剂衍生物或其盐。本发明还涉及包含至少一种肉毒杆菌神经毒素和至少一种阿片剂衍生物或其盐作为用于治疗或预防疼痛和神经肌肉疾病的同时，分开或顺序治疗用途的组合产品的产品。

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