公开(公告)号：US07291641B2

公开(公告)日：2007-11-06

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 ,  C07D233/61

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： Thiaxozle, oxazole, imidazole, isoxazole and isoxazoline compounds of the formula wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is selected from the various optionally substituted aromatic radicals defined in the specification, B is hydrogen, alkyl or phenyl, R1 and R2 are 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 —NH46R47 or —OR48, R46 and R47 are independently hydrogen, alkyl, cycloalkyl or —(CH2)kCOOR51, R51 is alkyl or haloalkyl and R48 is hydrogen or alkyl having advantageous pharmacological properties which allow their use in therapeutics, for treating neurodegenerative disorders or pain.

摘要翻译： 噻唑，恶唑，咪唑，异恶唑和异恶唑啉化合物，其中Het是噻唑，恶唑，咪唑，异恶唑或异恶唑啉，n是0至6的整数，A选自说明书中定义的各种任选取代的芳族基， B是氢，烷基或苯基，R 1和R 2独立地是氢，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-NH 46和/或 48，R 46和R 47独立地是氢，烷基，环烷基或 - （CH 2 CH 2） C 51，R 51是烷基或卤代烷基，R 48是具有有利药理学性质的氢或烷基，其允许它们用于治疗学 用于治疗神经变性疾病或疼痛。

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。