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1. 发明授权

US07659266B2 Amidine derivatives and their applications as a medicament 失效
标题翻译：脒衍生物及其作为药物的应用
公开(公告)号：US07659266B2
公开(公告)日：2010-02-09
申请号：US12090991
申请日：2006-10-18
申请人： Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier De Lassauniere , Bernadette Pignol
发明人： Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier De Lassauniere , Bernadette Pignol
IPC分类号： C07D279/20 , C07D417/12 , A61K31/5415
CPC分类号： C07D417/12 , C07D279/16 , C07D279/20
摘要： The invention concerns amidine derivatives of general formula (I) exhibiting an inhibitory activity of calpains and/or a trapping activity of reactive forms of oxygen.
摘要翻译：本发明涉及显示钙激素抑制活性和/或氧反应形式捕获活性的通式（I）的脒衍生物。

2. 发明申请

US20090149430A1 COMPOSITION CONTAINING AMIDINE DERIVATIVES OR CARBOXAMIDE DERIVATIVES AND STEROIDS, AS A MEDICAMENT 失效
标题翻译：含有氨基衍生物或羧甲酰胺衍生物和甾体的组合物作为药物
公开(公告)号：US20090149430A1
公开(公告)日：2009-06-11
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： A61K31/5415 , A61K31/573 , A61P29/00 , A61P37/00 , A61P35/00 , A61P31/12 , A61K8/49
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。

3. 发明申请

US20090018120A1 AMIDINE DERIVATIVES AND THEIR APPLICATIONS AS A MEDICAMENT 失效
标题翻译：氨基衍生物及其作为药物的应用
公开(公告)号：US20090018120A1
公开(公告)日：2009-01-15
申请号：US12090991
申请日：2006-10-18
申请人： Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier De Lassauniere , Bernadette Pignol
发明人： Serge Auvin , Dennis Bigg , Pierre-Etienne Chabrier De Lassauniere , Bernadette Pignol
IPC分类号： A61K31/5415 , C07D279/18 , A61P29/00 , A61P37/00 , A61P9/00 , A61P25/00 , A61P19/10 , A61P35/00 , A61P31/12
CPC分类号： C07D417/12 , C07D279/16 , C07D279/20
摘要： The invention concerns amidine derivatives of general formula (I) exhibiting an inhibitory activity of calpains and/or a trapping activity of reactive forms of oxygen.
摘要翻译：本发明涉及显示钙激素抑制活性和/或氧反应形式捕获活性的通式（I）的脒衍生物。

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. 发明申请

US20050222045A1 Novel derivatives of 2-hydroxytetrahydrofuran and their use as medicaments 失效
标题翻译： 2-羟基四氢呋喃的新型衍生物及其作为药物的用途
公开(公告)号：US20050222045A1
公开(公告)日：2005-10-06
申请号：US11115480
申请日：2005-04-27
申请人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
发明人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/078 , C07K5/097 , C07K5/117 , A61K38/05 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K38/04
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： The invention relates to derivatives of 2-hydroxytetrahydrofuran corresponding to general formula (I) in which A represents the radical, in which R1, R2, R4, R5 and R6 represent (in particular), independently, H, a halogen atom, OH, alkyl or alkoxy, R3 represents H, alkyl or —COR10, R10 representing H, alkyl or alkoxy, and W represents a bond, —CH2—CH2—, —CH═CH—, —O—, —S— or —NR11— in which R11 represents H or alkyl; X represents —CO—, —Y—CO—, —O—Y—CO— or —NR12—Y—CO—, Y represents an alkylene or haloalkylene alkyl, R12 represents H, alkyl or —COR13, R13 represents H, alkyl, haloalkyl or alkoxy, AA represents, each time that it occurs, a natural or non-natural amino acid; n represents 2 or 3; and finally R represents H, alkyl or —CO—R19, R19 representing alkyl. These compounds have a calpain inhibiting activity and/or an activity which traps the reactive oxygen species and can be used for preparing a medicament intended to treat the inflammatory and immunological diseases, cardio-vascular and cerebro-vascular diseases, disorders of the central or peripheral nervous system, cachexia, osteoporosis, muscular dystrophy, proliferative diseases, cataract, rejection reactions following organ transplants and autoimmune and viral diseases.
摘要翻译：本发明涉及对应于通式（I）的2-羟基四氢呋喃的衍生物，其中A表示基团，其中R 1，R 2，R 4， R 5和R 6独立地表示H，卤素原子，OH，烷基或烷氧基，R 3，代表H，烷基或-COR 10，R 10表示H，烷基或烷氧基，W表示键，-CH 2 -CH 2 - ， - CH-，-O-，-S-或-NR 11 - ，其中R 11表示 H或烷基; X表示-CO-，-Y-CO-，-OY-CO-或-NR 12 -Y-CO-，Y表示亚烷基或卤代亚烷基烷基，R 12 >表示H，烷基或-COR 13，R 13表示H，烷基，卤代烷基或烷氧基，AA表示每次发生时，天然或非天然氨基酸; n表示2或3; 最后R代表烷基，烷基或-CO-R 19，R 19代表烷基。这些化合物具有钙蛋白酶抑制活性和/或捕获活性氧的活性，并且可用于制备旨在治疗炎症和免疫疾病，心血管和脑血管疾病，中枢或外周疾病的药物神经系统，恶病质，骨质疏松症，肌营养不良，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。

6. 发明授权

US5480999A Dual inhibitors of NO synthase and cyclooxygenase, therapeutical compositions containing them 失效
标题翻译： NO合酶和环加氧酶的双重抑制剂，含有它们的治疗组合物
公开(公告)号：US5480999A
公开(公告)日：1996-01-02
申请号：US995792
申请日：1992-12-23
申请人： Pierre-Etienne Chabrier De Lassauniere , Pierre Braquet , Colette Broquet , Serge Auvin
发明人： Pierre-Etienne Chabrier De Lassauniere , Pierre Braquet , Colette Broquet , Serge Auvin
IPC分类号： A61K31/195 , A61K31/196 , A61K31/197 , A61K31/198 , A61K31/22 , A61K31/415 , A61K31/60 , A61P3/06 , A61P9/00 , A61P9/10 , A61P43/00 , C07C57/30 , C07C65/10 , C07C69/157 , C07C69/86 , C07C229/58 , C07C249/02 , C07C251/08 , C07C257/14 , C07C257/22 , C07C279/12 , C07C279/14 , C07C279/34 , C07C279/36 , C07C317/44 , C07D209/28 , C12N9/99 , A61K31/155 , A61K31/405 , C07C229/26 , C07C251/04 , C07D207/33
CPC分类号： C07C65/10 , C07C229/58 , C07C279/14 , C07C279/36 , C07C317/44 , C07C57/30 , C07C69/157 , C07D209/28
摘要： The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein:A represents a cyclooxygenase inhibitor having an accessible acidic function andB represents the L-form of arginine analogues of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent various substituents, process for the preparation of such compounds and pharmaceutical composition thereof.
摘要翻译：本发明涉及通式为AB的化合物，其可以是盐或酰胺，其中：A表示具有可接近的酸性官能团的环氧合酶抑制剂，B代表下式的L-型精氨酸类似物，其中R1 ，R2和R3代表各种取代基，制备这些化合物的方法及其药物组合物。

7. 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。

8. 发明授权

US07384933B2 Derivatives of 2-hydroxytetrahydrofuran and their use as medicaments 失效
标题翻译： 2-羟基四氢呋喃的衍生物及其用作药物
公开(公告)号：US07384933B2
公开(公告)日：2008-06-10
申请号：US11115480
申请日：2005-04-27
申请人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
发明人： Serge Auvin , Pierre-Etienne Chabrier De Lassauniere
IPC分类号： C07D417/02 , A61K31/5415
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。

9. 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。

10. 发明申请

US20080146627A1 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：US20080146627A1
公开(公告)日：2008-06-19
申请号：US12001439
申请日：2007-12-11
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： A61K31/426 , C07D277/02
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 Q 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特别独立地为氢，烷基或环烷基，Q为-NR 46，或者-OR 48，R 46和R 47非常独立地是氢，烷基，环烷基或 - （CH 2）2 - ， - OR 51，R 51特别是烷基或卤代烷基，R SUP 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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