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![(Pyrido/thieno)-[f]-oxazepine-5-one derivatives](/abs-image/US/2009/07/28/US07566778B2/abs.jpg.150x150.jpg)
公开(公告)号：US07566778B2
公开(公告)日：2009-07-28
申请号：US12024597
申请日：2008-02-01
IPC分类号： C07D498/14
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R 4和R 5独立地为H或（C 1-4 - ）烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，羟基，卤素和 氧代 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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![(PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES](/abs-image/US/2009/06/25/US20090163473A1/abs.jpg.150x150.jpg)
公开(公告)号：US20090163473A1
公开(公告)日：2009-06-25
申请号：US12389968
申请日：2009-02-20
IPC分类号： A61K31/553 , A61P25/24 , A61P25/28
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素 和氧代; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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![(Pyrido/thieno)-[f]-oxazepine-5-one derivatives](/abs-image/US/2011/10/11/US08034804B2/abs.jpg.150x150.jpg)
公开(公告)号：US08034804B2
公开(公告)日：2011-10-11
申请号：US12389968
申请日：2009-02-20
IPC分类号： A61K31/553 , A61P25/28
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R4和R5独立地是H或（C1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素 和氧代; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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![(PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES](/abs-image/US/2008/10/23/US20080262221A1/abs.jpg.150x150.jpg)
公开(公告)号：US20080262221A1
公开(公告)日：2008-10-23
申请号：US12024597
申请日：2008-02-01
IPC分类号： C07D498/04
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂5-酮衍生物，其中R 1，R 2，R 2和 > 3个独立地为H或（C 1-4烷基）烷基; Ar表示任选被一个或多个选自（C 1-4烷基）烷基，（C 1-4烷基）烷氧基，（C 1-4 - （C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基，氰基，NR 4 O R 5，S 4，S 4，C 6，和C 4 R 5 R 5， R 4和R 5独立地是H或（C 1-4 - ） - 烷基; 或R 4和R 5和它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外的选自O ，S或NR 6; R 6是（C 1-4 - ）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4烷基）烷基的取代基取代， 烷氧基，羟基，卤素和氧代; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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公开(公告)号：US20080139529A1
公开(公告)日：2008-06-12
申请号：US11924451
申请日：2007-10-25
IPC分类号： A61K31/553 , A61P25/00
CPC分类号： C07D515/04
摘要： The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or S02; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
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公开(公告)号：US07307073B2
公开(公告)日：2007-12-11
申请号：US10480623
申请日：2002-06-05
IPC分类号： C07D498/04
CPC分类号： C07D515/04
摘要： The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system
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7.发明授权公开(公告)号：US07504390B2
公开(公告)日：2009-03-17
申请号：US11924451
申请日：2007-10-25
CPC分类号： C07D515/04
摘要： The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的苯并氧氮杂衍生物，其中X代表CO或SO2; R1，R2，R3和R4独立地选自H，（C1-4）烷基，（C1-4）烷氧基，（C1-4）烷氧基（C1-4）烷基，卤素，硝基，氰基，NR8R9，NR8COR10， 并且CONR 8 R 9，R 5，R 6和R 7独立地为H或（C 1-4）烷基; R8和R9独立地为H或（C1-4）烷基; 或R8和R9与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR11的杂原子; R 10为（C 1-4）烷基; R11为（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，羟基，卤素和 氧代 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些苯并恶氮平衍生物在治疗神经系统疾病和精神病学障碍中的应用，所述神经疾病和精神疾病对中枢神经系统中AMPA受体介导的突触应答的增强有反应。
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![(Pyrido/thieno)—[f]—oxazepine-5-one derivatives](/abs-image/US/2008/03/18/US07345036B2/abs.jpg.150x150.jpg)
公开(公告)号：US07345036B2
公开(公告)日：2008-03-18
申请号：US10480569
申请日：2002-06-10
IPC分类号： A61P25/28
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式（I）的（吡啶并噻吩并） - [f] - 氧氮杂-5-酮衍生物或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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公开(公告)号：US20130023566A1
公开(公告)日：2013-01-24
申请号：US13382608
申请日：2010-07-06
IPC分类号： A61K31/4439 , A61P25/00 , A61K31/423 , C07D413/10 , C07D261/20
CPC分类号： C07D261/20
摘要： The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
摘要翻译： 本发明涉及具有通式（I）的2-（1,2-苯并异恶唑-3-基）苄胺衍生物，其中R1代表基团CONR2R3，其位于5- 1,2-苯并异恶唑环; R2和R3独立地为H或（C1-4）烷基; R4是环丙基，2-吡啶基或苯基，任选被一个或多个卤素取代; 或其药学上可接受的盐用于包含其的药物组合物，以及这些衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。
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10.发明授权Compounds with medicinal effects due to interaction with the glucocorticoid receptor 有权与糖皮质激素受体相互作用具有药效的化合物公开(公告)号：US07960365B2
公开(公告)日：2011-06-14
申请号：US11641524
申请日：2006-12-19
申请人： Niall Morton Hamilton , Simon James Anthony Grove , Michael John Kiczun , John Richard Morphy , Brad Sherborne , Peter Thomas Albert Littlewood , Angus Richard Brown , Celia Kingsbury , Michael Ohhlmeyer , Koc-Kan Ho , Steven G. Kultgen
发明人： Niall Morton Hamilton , Simon James Anthony Grove , Michael John Kiczun , John Richard Morphy , Brad Sherborne , Peter Thomas Albert Littlewood , Angus Richard Brown , Celia Kingsbury , Michael Ohhlmeyer , Koc-Kan Ho , Steven G. Kultgen
IPC分类号： C07D401/00 , A01N57/00
CPC分类号： C07C311/17 , C07C311/29 , C07D213/61 , C07D261/10 , C07D307/64 , C07D333/34 , C07D401/12
摘要： The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.
摘要翻译： 本发明提供具有式I结构的化合物，其中：X是碳原子或氮原子; Ar是苯基或杂芳环; R1是氢，卤素，CN或（1C-4C）烷基; R2是氢，卤素或任选氟化的（1C-3C）烷氧基; 任选卤代（1C-4C）烷氧基，任选卤代芳基（1C-4C）烷氧基，任选卤代（1C-4C）烯基或羟甲基; R4是氢，卤素，任选卤代（1C-4C）烷氧基或任选的卤代芳基（1C-4C）烷氧基; R6是氢，苄基，任选被一个或多个卤素或（1C-4C）烷基取代，或R6任选被卤代（1C-4C）烷基取代; 每个R 7独立地是氢，卤素，任选卤代（1C-4C）烷基或任选卤代（1C-4C）烷氧基及其药学上合适的酸加成盐，用作糖皮质激素受体调节剂，特别是用于治疗中枢神经系统疾病。
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