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    • 1. 发明申请
    • PIPERIDINE AND PIPERAZINE DERIVATIVES POSSESSING AFFINITY AT 5HT-1 TYPE RECEPTORS
    • 5HT-1型受体的磷酸和哌嗪衍生物
    • WO2003068236A1
    • 2003-08-21
    • PCT/EP2003/001710
    • 2003-02-17
    • GLAXO GROUP LIMITEDFLYNN, Sean, ThomasSMITH, Paul, WTHEWLIS, Kevin, MichaelWARD, Simon, EWYMAN, Paul, Adrian
    • FLYNN, Sean, ThomasSMITH, Paul, WTHEWLIS, Kevin, MichaelWARD, Simon, EWYMAN, Paul, Adrian
    • A61K31/495
    • C07D401/12C07D215/20C07D401/14C07D405/12C07D405/14C07D413/12C07D413/14
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A is optionally substituted phenyl, indolyl, quinolinyl, quinazolinyl, indazolyl or isoquinolinyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH 2 or oxygen and is a single bond; or X is nitrogen, Y is CH 2 and is a single bond; R1 is halogen, cyano, nitro, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, C 3-7 heterocyclylC 1-6 alkyl, C 3-7 heterocyclyl C 1-6 alkoxy; a is 0, 1, 2, 3 or 4; R2 is either: halogen, -CN, an optionally substituted C 3-7 cycloalkyl, an optionally substituted aryl or an optionally substituted C-linked 3-7 membered heterocyclic group; or a group -(Z)b-B wherein: (i) Z is oxygen, CH 2 , C=O, SO 2 or C=N-OR3 wherein R3 is hydrogen or C 1-6 alkyl; b is 1, 2, or 3; and B is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkanoyl, fluoroC 1-6 alkanoyl, C 1-6 alkylsulfonyl, fluoroC¿ 1-6 alkylsulfonyl, carbamoyl or C 1-6 alkylcarbamoyl, or R4 and R5, together with the nitrogen atom to which they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group; or (ii) Z is oxygen, CH or CH 2 , b is 1, and B forms the rest of an aryl or a C 3-7 heterocyclic group fused to the phenyl ring; excluding 1-[2-[2-(phenylmethyl)phenoxy]ethyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine and pharmaceutically acceptable salts thereof, and N-[4-[2-[4-[(3,4-dimethoxyphenyl)methyl]-1-piperazinyl]ethoxy]phenyl]-ethanesulfonamide and pharmaceutically acceptable salts thereof. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.
    • 公开了式(I)化合物及其药学上可接受的盐:其中A是任选取代的苯基,吲哚基,喹啉基,喹唑啉基,吲唑基或异喹啉基; X是碳,Y是CH并且是双键; 或X是CH,Y是CH 2或氧并且是单键; 或X为氮,Y为CH 2且为单键; R 1是卤素,氰基,硝基,C 1-6烷基,卤代C 1-6烷基,C 1-6烷氧基,C 3-7杂环基C 1-6烷基,C 3-7杂环基C 1-6烷氧基; a是0,1,2,3或4; R 2是:卤素,-CN,任选取代的C 3-7环烷基,任选取代的芳基或任选取代的C-连接的3-7元杂环基; 或(Z)b-B基团,其中:(i)Z是氧,CH 2,C = O,SO 2或C = N-OR 3,其中R 3是氢或C 1-6烷基; b为1,2或3; 并且B是氢,C 1-6烷基,C 3-7环烷基,C 1-6烷氧基或NR 4 R 5,其中R 4和R 5独立地是氢,C 1-6烷基,C 3-7环烷基,C 1-6烷酰基,氟C 1-6烷酰基,C 1 -6烷基磺酰基,氟代C 1-6烷基磺酰基,氨基甲酰基或C 1-6烷基氨基甲酰基,或者R 4和R 5与它们所连接的氮原子一起形成任选取代的3至7元杂环基的一部分; 或(ii)Z是氧,CH或CH 2,b是1,B形成与苯环稠合的芳基或C 3-7杂环基的其余部分; 不包括1- [2- [2-(苯基甲基)苯氧基]乙基] -4 - [(2,3,4-三甲氧基苯基)甲基] - 哌嗪及其药学上可接受的盐,以及N- [4- [2- [4 - [(3,4-二甲氧基苯基)甲基] -1-哌嗪基]乙氧基]苯基] - 乙磺酰胺及其药学上可接受的盐。 还公开了制备化合物的方法和化合物在治疗中的用途,特别是CNS障碍如抑郁和焦虑。
    • 2. 发明申请
    • COMPOUNDS POSSESSING AFFINITY AT 5HT1-TYPE RECEPTORS AND USE THEREOF IN THERAPY
    • 化合物在5HT1型受体中的有益作用及其在治疗中的应用
    • WO2003068760A2
    • 2003-08-21
    • PCT/EP2003/001709
    • 2003-02-17
    • GLAXO GROUP LIMITEDSMITH, Paul, WTHEWLIS, Kevin, MichaelVONG, Antonio, Kuok, KeongWARD, Simon, E
    • SMITH, Paul, WTHEWLIS, Kevin, MichaelVONG, Antonio, Kuok, KeongWARD, Simon, E
    • C07D295/00
    • C07D401/12C07D215/20C07D401/14C07D405/14C07D409/14C07D413/14C07D417/14
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (I) wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R1 is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4 and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.
    • 公开了式(I)化合物及其药学上可接受的盐:(I)其中:A为任选取代的苯基,萘基,吲哚基,喹啉基,喹唑啉基,吲唑基,异喹啉基或苯并呋喃基; X是碳,Y是CH并且是双键; 或X是CH,Y是CH 2或氧并且是单键; 或X为氮,Y为CH 2且为单键; R 1是卤素,羟基,氰基,C 1-6烷基,卤代C 1-6烷基或C 1-6烷氧基; a是0,1,2,3或4; R2和R3与它们所连接的氮原子一起形成硝基或任选取代的3至7元杂环基,或者R 2和R 3独立地是氢,芳酰基,C 1-6烷基,C 1-6烷酰基,氟C 1-6烷基, C 1-6烷酰基,C 1-6烷基磺酰基,氟C 1-6烷基磺酰基,氨基甲酰基,C 1-6烷基氨基甲酰基,芳基C 1-6烷基或CO(CH 2)b NR 4 R 5基团,其中b为1,2,3或4,并且R 4和R 5独立地为氢或C 1-6烷基,或 R4和R5与它们连接的氮原子一起形成任选取代的3至7元杂环基的一部分。 还公开了制备化合物的方法和化合物在治疗中的用途,特别是CNS障碍如抑郁和焦虑。