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1. 发明申请

US20110172434A1 DERIVATIVES OF HETEROCYCLES WITH 5 MEMBERS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS 有权
标题翻译：具有5个成员的杂环化合物的衍生物，其制备及其作为药物的用途
公开(公告)号：US20110172434A1
公开(公告)日：2011-07-14
申请号：US13053092
申请日：2011-03-21
申请人： Pierre-Etienne CHABRIER DE LASSAUNIERE , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
发明人： Pierre-Etienne CHABRIER DE LASSAUNIERE , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
IPC分类号： C07D277/28
CPC分类号： C07D277/28 , A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , C07D233/64 , C07D261/04 , C07D263/32 , C07D277/24 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06
摘要： The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and Ω is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl.These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
摘要翻译：本发明涉及噻唑，恶唑，咪唑，异恶唑和其中Het为噻唑，恶唑，咪唑，异恶唑或异恶唑啉的通式（I）的异恶唑啉衍生物，n为0至6的整数，A特别选自各种任选取代的芳基，B特别是氢，烷基或苯基，R 1和R 2特别独立地是氢，烷基或环烷基，和OHgr; 是-NR46R47或-OR48，R46和R47独特地是氢，烷基，环烷基或 - （CH2）k-COOR51，R51尤其是烷基或卤代烷基，R48特别是氢或烷基。这些化合物具有有利的药理学性质，其允许其用于治疗学，特别是用于治疗神经变性疾病或疼痛。

2. 发明授权

US07576241B2 Derivatives of amidines, their preparation, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译：脒的衍生物，其制备，作为药物的用途以及含有它们的药物组合物
公开(公告)号：US07576241B2
公开(公告)日：2009-08-18
申请号：US11250783
申请日：2005-10-14
申请人： Serge Auvin , Pierre-Etienne Chabrier de Lassauniere , Jeremiah Harnett , Dominique Pons , Gerard Ulibarri
发明人： Serge Auvin , Pierre-Etienne Chabrier de Lassauniere , Jeremiah Harnett , Dominique Pons , Gerard Ulibarri
IPC分类号： C07C211/00
CPC分类号： C07D409/12 , C07C217/84 , C07D333/20 , C07D333/36 , C07D333/38 , C07D409/14 , C07D417/12 , C07D473/08
摘要： A compound of the formula wherein the substituents are defined as in the specification useful as intermediates.
摘要翻译：下式的化合物，其中取代基如本说明书中所定义可用作中间体。

3. 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。

4. 发明申请

US20060166893A1 Novel 2-hydroxytetrahydrofurane derivatives and use thereof as medicaments 失效
标题翻译：新型2-羟基四氢呋喃衍生物及其作为药物的用途
公开(公告)号：US20060166893A1
公开(公告)日：2006-07-27
申请号：US10532731
申请日：2004-12-08
申请人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
发明人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
IPC分类号： A61K38/04 , A61K31/5415 , C07D417/02
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06165 , C07K5/0821
摘要： A hydroxytetrahydrofuran of formula wherein A is with the substituents as defined in the specification, having a calpain inhibiting activity and/or an activity which traps the reactive oxygen species useful for treating inflammatory and immunological diseases, cardio-vascular and cerebro-vascular diseases, disorders of the central or peripheral nervous system, osteoporosis, muscular dystrophy, proliferative diseases, cataract, rejection reactions following organ transplants and autoimmune and viral diseases.
摘要翻译：具有下式的羟基四氢呋喃其中A具有本说明书中所定义的取代基，具有钙蛋白酶抑制活性和/或捕获可用于治疗炎性和免疫疾病，心血管和脑血管疾病，病症的活性氧的活性中枢或周围神经系统，骨质疏松症，肌营养不良症，增殖性疾病，白内障，器官移植后的排斥反应以及自身免疫性和病毒性疾病。

5. 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。

6. 发明申请

US20050038087A1 Derivatives of heterocycles with 5 members, their preparation and their use as medicaments 失效
标题翻译：具有5个成员的杂环衍生物，其制备及其作为药物的用途
公开(公告)号：US20050038087A1
公开(公告)日：2005-02-17
申请号：US10915001
申请日：2004-08-10
申请人： Pierre-Etienne Chabrier De Lassauniere , Jermiah Harnett , Dennis Bigg , Ann-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau , Zheng Xin Dong
发明人： Pierre-Etienne Chabrier De Lassauniere , Jermiah Harnett , Dennis Bigg , Ann-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau , Zheng Xin Dong
IPC分类号： A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , A61P25/08 , A61P25/28 , A61P29/00 , C07D233/50 , C07D233/54 , C07D261/04 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , A61K31/425 , A61K31/4164
CPC分类号： C07D233/64 , A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , C07D233/50 , C07D261/04 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl or R1 and R2, taken together with the carbon atom which carries them, form a carbocycle with 3 to 7 members and Ω is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
摘要翻译：本发明涉及噻唑，恶唑，咪唑，异恶唑和其中Het为噻唑，恶唑，咪唑，异恶唑或异恶唑啉的通式（I）的异恶唑啉衍生物，n为0至6的整数，A特别选自各种任选取代的芳基，B特别是氢，烷基或苯基，R 1和R 2独特地独立地表示氢，烷基或环烷基或R 1和R 2与携带它们的碳原子一起，形成具有3至7个成员的碳环，并且ω是-NR 46 R 47或-OR 48，R 46和R 47独立地是氢，烷基，环烷基或 - （CH 2）k -COOR 51，R 51特别是烷基或卤代烷基，R 48特别是氢或烷基。这些化合物具有有利的药理学性质，其允许其用于治疗学，特别是用于治疗神经变性疾病或疼痛。

7. 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。

8. 发明授权

US06762176B1 2-aminopyridine derivatives, their use as medicines and pharmaceutical compositions containing them 失效
标题翻译： 2-氨基吡啶衍生物，它们作为药物和含有它们的药物组合物的用途
公开(公告)号：US06762176B1
公开(公告)日：2004-07-13
申请号：US09743043
申请日：2001-03-08
申请人： Pierre-Etienne Chabrier de Lassauniere , Serge Auvin , Jerry Harnett , Dominique Pons , Gérard Ulibarri , Dennis Bigg
发明人： Pierre-Etienne Chabrier de Lassauniere , Serge Auvin , Jerry Harnett , Dominique Pons , Gérard Ulibarri , Dennis Bigg
IPC分类号： A61K3133
CPC分类号： C07K14/70575 , A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/03 , A01K2267/0325 , A01K2267/0368 , A01K2267/0381 , A61K2039/505 , C07D213/73 , C07D401/04 , C07D405/12 , C07K16/2875 , C07K16/2878 , C12N15/8509
摘要： The invention concerns novel 2-aminopyridine derivatives having an activity inhibiting NO-synthase enzymes producing nitrogen monoxide NO and/or trapping reactive forms of oxygen, the methods for preparing them, pharmaceutical compositions containing them and their therapeutic uses, particularly their use as NO-synthase inhibitors and for trapping reactive forms of oxygen whether selectively or not.
摘要翻译：本发明涉及具有抑制产生一氧化氮NO和/或捕获反应性形式的氧的NO合成酶的活性的新型2-氨基吡啶衍生物，其制备方法，含有它们的药物组合物及其治疗用途，特别是其作为NO- 合成酶抑制剂和用于捕获反应性形式的氧，无论是否有选择性。

9. 发明授权

US08642591B2 Composition containing amidine derivatives or carboxamide derivatives and steroids, as a medicament 失效
标题翻译：含有脒衍生物或羧酰胺衍生物和类固醇作为药物的组合物
公开(公告)号：US08642591B2
公开(公告)日：2014-02-04
申请号：US12282131
申请日：2007-03-06
申请人： Bernadette Pignol , Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier de Lassauniere
发明人： Bernadette Pignol , Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier de Lassauniere
IPC分类号： A61K31/54 , A61K31/56 , A01N45/00
CPC分类号： A61K31/341 , A61K31/5415 , A61K31/573 , A61K31/58 , A61K31/585 , A61K2300/00
摘要： The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.
摘要翻译：本发明涉及包含至少一种通式（I）或（A）的脒衍生物或羧酰胺衍生物与至少一种选自类固醇，皮质激素或皮质类固醇的化合物组合的组合物，其中所述组合物适用于制备药物。

10. 发明授权

US08288560B2 Derivatives of heterocycles with 5 members, their preparation and their use as medicaments 有权
标题翻译：具有5个成员的杂环衍生物，其制备及其作为药物的用途
公开(公告)号：US08288560B2
公开(公告)日：2012-10-16
申请号：US13053092
申请日：2011-03-21
申请人： Pierre-Etienne Chabrier De Lassauniere , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
发明人： Pierre-Etienne Chabrier De Lassauniere , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
IPC分类号： C07D277/28
CPC分类号： C07D277/28 , A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , C07D233/64 , C07D261/04 , C07D263/32 , C07D277/24 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06
摘要： The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and Ω is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
摘要翻译：本发明涉及噻唑，恶唑，咪唑，异恶唑和其中Het为噻唑，恶唑，咪唑，异恶唑或异恶唑啉的通式（I）的异恶唑啉衍生物，n为0至6的整数，A特别选自各种任选取代的芳基，B特别是氢，烷基或苯基，R 1和R 2特别独立地是氢，烷基或环烷基，和OHgr; 是-NR46R47或-OR48，R46和R47独特地是氢，烷基，环烷基或 - （CH2）k-COOR51，R51尤其是烷基或卤代烷基，R48特别是氢或烷基。这些化合物具有有利的药理学性质，其允许其用于治疗学，特别是用于治疗神经变性疾病或疼痛。

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