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1. 发明申请

WO2002102808A2 (PYRIDO/THIENO)-[f]-OXAZEPIN-5-ONE DERIVATIVES 审中-公开
标题翻译：（吡啶/噻吩） - [f] -OXAZEPIN-5-ONE衍生物
公开(公告)号：WO2002102808A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006364
申请日：2002-06-10
申请人： AKZO NOBEL N.V. , GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
发明人： GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
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 R 1 , R 2 and R 3 are independently H or (C 1-4 )alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy(C 1-4 )alkyl, CF 3 , halogen, nitro, cyano, NR 4 R 5 , NR 4 COR 6 , and CONR 4 R 5 ; R 4 and R 5 are independently H or (C 1-4 )-alkyl; or R 4 and R 5 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 NR 6 ; R 6 is (C 1-4 )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 (C 1-4 )alkyl, (C 1-4 )-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，NR 4 R 5，NR 4 COR 6和CONR 4 R 5; 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，任选地含有另外选自O，S或NR 6的杂原子; 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，（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。

2. 发明申请

WO2009037220A1 TRICYCLIC HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：三元杂环衍生物
公开(公告)号：WO2009037220A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062229
申请日：2008-09-15
申请人： N.V. ORGANON , GROVE, Simon James Anthony , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , WISHART, Grant
发明人： GROVE, Simon James Anthony , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , WISHART, Grant
IPC分类号： C07D491/052 , A61K31/40 , A61P25/00
CPC分类号： C07D491/052
摘要： The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义。本发明还涉及包含这些化合物的药物组合物及其在治疗中的用途，特别是用于治疗5-羟色胺介导的障碍，例如肥胖，精神分裂症和认知功能障碍。

3. 发明申请

WO2002100861A1 1-(3-PHENYLOXYPROPYL)PIPERIDINE DERIVATIVES 审中-公开
标题翻译： 1-（3-苯基丙基）哌啶衍生物
公开(公告)号：WO2002100861A1
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006313
申请日：2002-06-07
申请人： AKZO NOBEL N.V. , COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
发明人： COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
IPC分类号： C07D471/10
CPC分类号： C07D401/04 , C07D471/10
摘要： The present invention relates to 1(3-phenyloxypropyl)-piperidine derivative having general Formula (I), wherein R1 is (C 1-6 )alkyl or (C 4-8 )cycloalkyl or phenyl, optionally substituted with (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R2 is H or (C 1-6 )alkyl; or R1 and R2 form together with the carbon atom to which they are bound (C 4-8 )cycloalkyl, optionally substitutes with (C 1-6 )alkyloxy or halogen; R3 is H, OH, (C 1-6 )alkyloxy or (C 1-6 )alkylcarbonyloxy; R4 represents 1-5 substituents independently selected from H, (C 1-6 )alkyl, (C 1-6 )alkyloxy and halogen; Y represents (a), (b) and Z is H; or Y and Z together with the carbon atom to which they are bound represent the spiro atom in the spiro atom in the spiro system formed with (c) *represents the spiro carbon atom; R6 is H, (C 1-6 )alkyl or (CO)n-(CH 2 )m-R12; n is 0 or 1; m is 1-4; R8 and R10 are independently H or(C 1-6 )alkyl; R7, R9 and R11 are independently H, (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R12 is hydroxy, (C 1-4 )alkyloxy, (C 1-4 )alkylthio, (C 1-4 )alkyloxycarbonyl, (C 1-4 )alkylcarbonyloxy, 2-tetrahydrofuranyl, 4-morpholinyl or di(C 1-4 )alkylamino; or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 1-(3-phenyloxypropyl)-piperidine derivatives in therapy.
摘要翻译：本发明涉及具有通式（I）的1（3-苯氧基丙基） - 哌啶衍生物，其中R 1为（C 1-6）烷基或（C 4-8）环烷基或任选被（C 1-6）烷基取代的苯基，（C 1-6）烷氧基或卤素; R2是H或（C1-6）烷基; 或R 1和R 2与它们所连接的碳原子一起形成（C 4-8）环烷基，任选地与（C 1-6）烷氧基或卤素取代; R3是H，OH，（C1-6）烷氧基或（C1-6）烷基羰基氧基; R 4表示独立地选自H，（C 1-6）烷基，（C 1-6）烷氧基和卤素的1-5个取代基; Y表示（a），（b），Z表示H; 或者Y和Z与它们所连接的碳原子一起表示在（c）中形成的螺系中的螺原子中的螺原子*代表螺
碳原子; R6是H，（C1-6）烷基或（CO）n-（CH2）m-R12; n为0或1; m为1-4; R 8和R 10独立地为H或（C 1-6）烷基; R 7，R 9和R 11独立地为H，（C 1-6）烷基，（C 1-6）烷氧基或卤素; R 12是羟基，（C 1-4）烷氧基，（C 1-4）烷硫基，（C 1-4）烷氧基羰基，（C 1-4）烷基羰基氧基，2-四氢呋喃基，4-吗啉基或二（C 1-4）烷基氨基; 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1-（3-苯氧基丙基） - 哌啶衍生物在治疗中的用途。

4. 发明申请

WO1997040027A1 SUBSTITUTED BENZYLAMINES AND THEIR USE FOR THE TREATMENT OF DEPRESSION 审中-公开
标题翻译：替代苯甲酸酯及其用于治疗呕吐的用途
公开(公告)号：WO1997040027A1
公开(公告)日：1997-10-30
申请号：PCT/EP1997001904
申请日：1997-04-15
申请人： AKZO NOBEL N.V. , LEYSEN, Dirk, Casimir, Maria , RUIGT, Gerardus, Stephanus, Franciscus , LINDERS, Joannes, Theodorus, Maria , DIJCKS, Fredericus, Antonius , GROVE, Simon, James, Anthony , RAE, Duncan, Robertson
发明人： AKZO NOBEL N.V.
IPC分类号： C07D261/20
CPC分类号： C07D413/10 , C07D231/56 , C07D261/20 , C07D413/12 , C07D417/12
摘要： The present invention relates to certain novel benzylamine derivatives of formula (I) wherein R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxy-C1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, carboxamide and C1-6alkylcarboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl and C1-6alkoxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, halogen, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl) or one of R and R are as hereinbefore defined and one is hydroxy; R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxyC1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, C1-6alkylcarboxamide and carboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-6alkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy-C1-6alkyl, haloC1-6alkyl, haloC2-6alkenyl, haloC2-6alkynyl, cyano, carboxyl, C1-6alkylcarboxy and carboxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl); or one of R or R together with one of R or R and the N atom to which it is attached form a 5- or 6-membered heterocyclic ring. R represents one or more ring substituents selected from halogen, hydrogen C1-6alkyl and C1-6alkoxy; and R represents a single ring substituent of formula (A) wherein the dotted line represents an optional bond; Y is oxygen or -NR (where R is hydrogen or C1-6alkyl) and R represents one or more substituents selected from hydrogen, halogen, haloC1-6alkyl, C1-6alkyl and C1-6alkoxy; or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
摘要翻译：本发明涉及一些式（I）的新型苄胺衍生物，其中R 1和R 2可以相同或不同，各自选自C 6-12芳基，C 2-4芳基，C 6-12芳基C 1-6烷基，其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基-C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，羧酰胺和C 1-6烷基羧酰胺），氢，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 2-6烯基，C 2-6炔基和C 1-6烷氧基C 1-6烷基（其中烷基，环烷基，环烯基，烯基，炔基或烷氧基烷基部分可以任选地被一个或多个选自氨基，卤素，羟基，C 1-6烷基羧酰胺，羧酰胺，羧基，C 1-6烷氧基羰基，C 1-6a 烷基羧基和羧基C 1-6烷基）或R 1和R 2中的一个如上文所定义，一个是羟基; R 3和R 4可以相同或不同，各自选自C 6-12芳基，C 2-14杂芳基，C 6-12芳基C 1-6烷基，C 2-4杂芳基C 1-6烷基（其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，C 1-6烷基羧酰胺和甲酰胺），氢，C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-6烷基，C 4-6环烯基， C 1-6烷氧基-C 1-6烷基，卤代C 1-6烷基，卤代C 2-6烯基，卤代C 2-6炔基，氰基，羧基，C 1-6烷基羧基和羧基C 1-6烷基（其中烷基，环烷基，环烯基，链烯基，炔基，或烷氧基烷基部分可以任选地被一个或多个选自氨基，羟基，C 1-6烷基羧酰胺，甲酰胺，羧基，C 1-6烷氧基羰基，C 1-6烷基羧基和羧基C 1-6烷基）; 或R 3或R 4中的一个与R 1或R 2中的一个以及与其连接的N原子形成5-或6-元杂环。 R 5表示一个或多个选自卤素，C 1-6烷基和C 1-6烷氧基的环取代基; 并且R 6表示式（A）的单环取代基，其中虚线表示任选的键; Y是氧或-NR 8（其中R 8是氢或C 1-6烷基），R 7代表一个或多个选自氢，卤素，卤代C 1-6烷基，C 1-6烷基和C 1-6烷氧基的取代基; 或其药学上可接受的盐或溶剂合物。本发明还涉及其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

5. 发明申请

WO2011076723A1 AMINO-HETEROARYL DERIVATIVES AS HCN BLOCKERS 审中-公开
标题翻译： AMINO-HETEROARYL DERIVATIVES作为HCN阻隔剂
公开(公告)号：WO2011076723A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070213
申请日：2010-12-20
申请人： N.V. Organon , GROVE, Simon James Anthony , MORRISON, Angus John , JAMIESON, Craig , PALIN, Ronald , MACLEAN, John Kinnaird Ferguson
发明人： GROVE, Simon James Anthony , MORRISON, Angus John , JAMIESON, Craig , PALIN, Ronald , MACLEAN, John Kinnaird Ferguson
IPC分类号： C07D213/73 , C07D239/42 , C07D401/12 , C07D403/12 , A61K31/435 , A61K31/497 , A61K31/506 , A61K31/53 , A61P25/00
CPC分类号： C07D239/42 , A61K31/435 , A61K31/497 , A61K31/506 , A61K31/53 , C07D213/73 , C07D401/12 , C07D403/12
摘要： The invention relates to amino-heteroaryl derivatives having the general Formula I 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的氨基 - 杂芳基衍生物或其药学上可接受的盐，其涉及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。

6. 发明申请

WO2007071638A1 COMPOUNDS WITH MEDICINAL EFFECTS DUE TO INTERACTION WITH THE GLUCOCORTICOID RECEPTOR 审中-公开
标题翻译：与葡萄糖激素受体相互作用的具有药物作用的化合物
公开(公告)号：WO2007071638A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/069814
申请日：2006-12-18
申请人： N.V. ORGANON , PHARMACOPEIA DRUG DISCOVERY, INC. , HAMILTON, Niall Morton , GROVE, Simon James Anthony , KICZUN, Michael John , MORPHY, John, Richard , SHERBORNE, Brad , LITTLEWOOD, Peter Thomas Albert , BROWN, Angus Richard , KINGSBURY, Celia , OHLMEYER, Michael , HO, Koc-Kan , KULTGEN, Steven G.
发明人： HAMILTON, Niall Morton , GROVE, Simon James Anthony , KICZUN, Michael John , MORPHY, John, Richard , SHERBORNE, Brad , LITTLEWOOD, Peter Thomas Albert , BROWN, Angus Richard , KINGSBURY, Celia , OHLMEYER, Michael , HO, Koc-Kan , KULTGEN, Steven G.
IPC分类号： A61K31/18 , A61K31/4439 , C07C311/17 , C07D401/12
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; R 1 is hydrogen, halogen, CN or (1 C-4C)alkyl; R 2 is hydrogen, halogen or optionally fluorinated (1 C-3C)alkoxy; R 3 and R 5 are independently hydrogen, optionally halogenated (1C- 4C)alkyl, optionally halogenated (1 C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1 C-4C)alkenyl or hydroxylmethyl; R 4 is hydrogen, halogen, optionally halogenated (1 C-4C)alkoxy or optionally halogenated aryl(1 C-4C)alkoxy; R 6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1 C-4C)alkyl, or R 6 is optionally halogenated (1 C-4C)alkyl; each R 7 independently is hydrogen, halogen, optionally halogenated (1 C-4C)alkyl or optionally halogenated (1 C-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; R 1是氢，卤素，CN或（C 1 -C 4）烷基; R 2是氢，卤素或任选氟化的（C 1 -C 3）烷氧基; 卤代（1C-4C）烷基，任选卤代（C 1 -C 4）烷氧基，任意卤代芳基（1C-4C）烷氧基，任选卤代（C 1 -C 4）烯基或羟甲基; R 4是氢，卤素，任选卤代（C 1 -C 4）烷氧基或任选卤代芳基（C 1 -C 4）烷氧基; R 6是氢，任选被一个或多个卤素或（C 1 -C 4）烷基取代的苄基，或R 6任选被卤代（C 1 -C 4）烷基 ; 每个R 7独立地是氢，卤素，任选卤代（C 1 -C 4）烷基或任选卤代（C 1 -C 4）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，用于特别用于治疗中枢神经系统疾病。

7. 发明申请

WO2010052198A1 ( PYRROLIDIN-2 -YL) PHENYL DERIVATIVES FOR USE IN THE TREATMENT OF PAIN 审中-公开
标题翻译：（吡咯烷-2-基）苯基衍生物用于治疗疼痛
公开(公告)号：WO2010052198A1
公开(公告)日：2010-05-14
申请号：PCT/EP2009/064490
申请日：2009-11-03
申请人： N.V. ORGANON , GROVE, Simon, James, Anthony , MISTRY, Ashvinkumar, Dhirubhai , PALIN, Ronald , MACLEAN, John, Kinnaird, Ferguson
发明人： GROVE, Simon, James, Anthony , MISTRY, Ashvinkumar, Dhirubhai , PALIN, Ronald , MACLEAN, John, Kinnaird, Ferguson
IPC分类号： C07D401/10 , A61K31/4439 , A61P25/02
CPC分类号： C07D401/10
摘要： The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula (I), wherein R 1 is (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, or halo(C 1-4 )alkyloxy; R 2 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; R 3 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 4 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 5 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C 3-6 )cycloalkyl group, optionally substituted with halogen; R 6 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl 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（吡咯烷-2-基）苯基衍生物，其中R 1为（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基或卤素 -4）烷氧基; R 2是H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; R3是H，（C1-4）烷基或卤代（C1-4）烷基; R4是H，（C1-4）烷基或卤代（C1-4）烷基; R5是H，（C1-4）烷基或卤代（C1-4）烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺（C 3-6）环烷基; R 6为H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; 或其药学上可接受的盐，包含其的药物组合物，以及这些（吡咯烷-2-基）苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

8. 发明申请

WO2002100865A1 BENZOXAZEPINE DERIVATIVES AND THEIR USE AS AMPA RECEPTOR STIMULATORS 审中-公开
标题翻译：苯并噻吩衍生物及其作为AMPA受体刺激物的用途
公开(公告)号：WO2002100865A1
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006185
申请日：2002-06-05
申请人： AKZO NOBEL N.V. , GROVE, Simon, James, Anthony , ZHANG, Mingqiang , SHAHID, Mohammad
发明人： GROVE, Simon, James, Anthony , ZHANG, Mingqiang , SHAHID, Mohammad
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 SO 2 ; R 1 , R 2 , R 3 and R 4 are independently selected from H, (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy(C 1-4 )alkyl, halogen, nitro, cyano, NR 8 R 9 , NR 8 COR 10 , and CONR 8 R 9 , R 5 , R 6 and R 7 are independently H or (C 1-4 )alkyl; R 8 and R 9 are independently H or (C 1-4 )alkyl; or R 8 and R 9 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 NR 11 ; R 10 is (C 1-4 )alkyl; R 11 is (C 1-4 )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 (C 1-4 )alkyl, (C 1-4 )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; R 1，R 2，R 3和R 4独立地选自H，（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，卤素，硝基，氰基，NR 8 R 9，NR 8 COR 10和CONR 8 R 9，R 5，R 6和R 7 独立地为H或（C 1-4）烷基; R 8和R 9独立地为H或（C 1-4）烷基; 或R 8和R 9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NR 11的杂原子; R 10是（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; 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。

9. 发明申请

WO9918941A3 Ih-MODULATORS 审中-公开
标题翻译： IH-调节剂
公开(公告)号：WO9918941A3
公开(公告)日：2000-01-13
申请号：PCT/EP9806651
申请日：1998-10-14
申请人： AKZO NOBEL NV , DIJCKS FREDERICUS ANTONIUS , GROVE SIMON JAMES ANTHONY , CARLYLE IAN CRAIG , THORN SIMON NICHOLAS , RAE DUNCAN ROBERTSON , RUIGT GERARDUS STEPHANUS FRANC , LEYSEN DIRK
发明人： DIJCKS FREDERICUS ANTONIUS , GROVE SIMON JAMES ANTHONY , CARLYLE IAN CRAIG , THORN SIMON NICHOLAS , RAE DUNCAN ROBERTSON , RUIGT GERARDUS STEPHANUS FRANC , LEYSEN DIRK
IPC分类号： G01N33/50 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/416 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/505 , A61K45/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07C47/55 , C07C47/575 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/48 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/56 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/56 , C07D333/58 , C07D413/04 , C07D498/04 , G01N33/15 , A61K31/34 , A61K31/38 , A61K31/425 , A61K31/435
CPC分类号： C07D413/04 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/137 , A61K31/15 , A61K31/381 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/437 , A61K31/472 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/58
摘要： The present invention relates to the use of an Ih channel modulator in the manufacture of a medicament for use in psychiatry. To certain novel methanamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly for use in psychiatry.
摘要翻译：本发明涉及Ih通道调节剂在制造用于精神病学的药物中的用途。某些新的甲胺衍生物，其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是用于精神病学。

10. 发明申请

WO2011003895A1 2-(1,2-BENZISOXAZOL-3-YL)BENZYLAMINE DERIVATIVES 审中-公开
标题翻译： 2-（1,2-BZZOXOX-Z-3-YL）苯甲酰胺衍生物
公开(公告)号：WO2011003895A1
公开(公告)日：2011-01-13
申请号：PCT/EP2010/059621
申请日：2010-07-06
申请人： N.V. ORGANON , GROVE, Simon James Anthony
发明人： GROVE, Simon James Anthony
IPC分类号： 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 R 1 represents the group CONR 2 R 3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R 2 and R 3 are independently H or (C 1-4 )alkyl; and R 4 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，该基团存在于5- 1,2-苯并异恶唑环; R2和R3独立地为H或（C1-4）烷基; 并且R 4是任选被一个或多个卤素取代的环丙基，2-吡啶基或苯基; 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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