利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

19 条记录 (耗时 0.014 秒)

    AZABICYCLO[3.2.1]OCTANE DERIVATIVES
    1.
    发明申请
    AZABICYCLO[3.2.1]OCTANE DERIVATIVES 审中-公开
    AZABICYCLO [3.2.1] OCTANE DERIVATIVES

    公开(公告)号：WO2009056520A1

    公开(公告)日：2009-05-07

    申请号：PCT/EP2008/064529

    申请日：2008-10-27

    申请人： GLAXO GROUP LIMITED ,  ANDREOTTI, Daniele ,  PROFETA, Roberto

    发明人： ANDREOTTI, Daniele ,  PROFETA, Roberto

    IPC分类号： C07D221/22

    CPC分类号： C07D221/22

    摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A or W, wherein A is formula (IA) wherein p is 0, 1, 2, 3, 4 or 5 and R 5 is halogen, cyano or C 1-4 alkyl, each of them being the same or different; and W is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 5 , each of them being the same or different; R 3 is a group (P) wherein R 6 is selected from the group consisting of hydrogen, C 1-4 alkyl, haloC 1-4 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl, and n is 1 or 2; R4 is hydrogen, linear or branched C 1-4 alkyl, hydroxyl or C 1-4 alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐，溶剂合物或前药，其中R 1是氢或C 1-4烷基; R2是A或W基团，其中A是式（IA），其中p是0,1,2,3,4或5，R 5是卤素，氰基或C 1-4烷基，它们各自相同或不同; 并且W是一个或者萘基，任选地被1或2个基团R 5取代，它们各自相同或不同; R3是一个基团（P），其中R6选自氢，C1-4烷基，卤代C 1-4烷基，C 3-6环烷基和C 3-6环烷基C 1-3烷基，n是1或2; R4是氢，直链或支链C 1-4烷基，羟基或C 1-4烷氧基; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的应用。

    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
    3.
    发明申请
    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    潜在的谷氨酸受体的化合物及其在医药中的应用

    公开(公告)号：WO2007090841A1

    公开(公告)日：2007-08-16

    申请号：PCT/EP2007/051136

    申请日：2007-02-06

    申请人： GLAXO GROUP LIMITED ,  ANDREOTTI, Daniele ,  WARD, Simon, Edward

    发明人： ANDREOTTI, Daniele ,  WARD, Simon, Edward

    IPC分类号： C07D307/22 ,  C07D401/10 ,  C07D409/10 ,  A61K31/34 ,  A61P25/00

    CPC分类号： C07D401/10 ,  C07D307/22 ,  C07D409/10

    摘要： Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl, furanyl and thienyl, each optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, cyano, C(O) C 1-4 alkyl, NHSO 2 C 1-4 alkyl, NMeSO2C 1-4 alkyl, NHCOC 1-4 alkyl, NMeCOC 1-4 aIkyl, SOC 1-4 alkyl, SO 2 C 1-4 alkyl, and CO 2 C 1-4 alkyl, or two Y groups together form a cyclic group -0(CH 2 )O-. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.

    摘要翻译： 提供式（I）化合物，其盐和溶剂化物：其中Ar选自苯基，吡啶基，呋喃基和噻吩基，各自任选被一个或多个Y基团取代; 并且每个Y基团独立地选自：卤素，C 1-4烷基，卤代C 1-4烷基，C 1-4烷基， 烷氧基，氰基，C（O）C 1-4烷基，NHSO 2 -C 1-4烷基，NMeSO 2 C 1 -4个烷基，NHCOC 1-4烷基，NMeCOC 1-4烷基，SO 1-4烷基，SO 2个C 1-4烷基，和C 2 -C 1-4烷基，或两个Y基团一起形成环状 基团-O（CH 2 CH 2）O-。 还公开了制备方法及其用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症的用途。

    CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS
    4.
    发明申请
    CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS 审中-公开
    简便的N-杂环化合物及其作为CRF受体拮抗剂的用途

    公开(公告)号：WO2004094420A1

    公开(公告)日：2004-11-04

    申请号：PCT/IB2004/001350

    申请日：2004-04-07

    申请人： SB PHARMCO PUERTO RICO INC ,  NEUROCRINE BIOSCIENCES INC ,  ANDREOTTI, Daniele ,  BERNASCONI, Giovanni ,  CASTIGLIONI, Emiliano ,  CONTINI, Stefania ,  DI FABIO, Romano ,  FAZZOLARI, Elettra ,  FERIANI, Aldo ,  GENTILE, Gabriella ,  MATTIOLI, Mario ,  MINGARDI, Anna ,  SABBATINI, Fabio ,  ST-DENIS, Yves

    发明人： ANDREOTTI, Daniele ,  BERNASCONI, Giovanni ,  CASTIGLIONI, Emiliano ,  CONTINI, Stefania ,  DI FABIO, Romano ,  FAZZOLARI, Elettra ,  FERIANI, Aldo ,  GENTILE, Gabriella ,  MATTIOLI, Mario ,  MINGARDI, Anna ,  SABBATINI, Fabio ,  ST-DENIS, Yves

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 2 , nitro, hydroxy, -NR 3 R 4 , cyano and or a group Z; R 1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo Cl­-C6 alkoxy, halogen, NR 3 R 4 or cyano; D, G is . -C- optionally substituted; X is carbon or nitrogen; Y is nitrogen or -C- optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which: - one carbon atom is replaced by a carbonyl or S(O) m ; and - one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR 12 , S(O) m , carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R 5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 2. to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    摘要翻译： 本发明提供了包括立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z; R 1是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或 氰基; D，G为-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环，其可以是饱和的或可以含有一至三个双键，其中： - 一个碳原子被羰基或S（O）m取代; 和 - 1-4个碳原子可以任选被氧，氮或NR 12，S（O）m，羰基取代，并且这样的环可进一步被1至8个取代基取代; Z是5-6元杂环，其可以被1至8个R5基团取代或可被1至4个取代基取代的苯基环; m为0至2的整数。其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

    PROCESS FOR PREPARING BICYCLIC COMPOUNDS
    5.
    发明申请
    PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
    制备双相化合物的方法

    公开(公告)号：WO2006108689A2

    公开(公告)日：2006-10-19

    申请号：PCT/EP2006/003480

    申请日：2006-04-06

    申请人： SB PHARMCO PUERTO RICO INC ,  NEUROCRINE BIOSCIENCES INC ,  ANDREOTTI, Daniele ,  BACCHI, Sergio ,  DELPOGETTO, Monica ,  GUELFI, Simone ,  PERBONI, Alcide ,  RIBECAI, Arianna ,  SPADA, Simone ,  STABILE, Paolo ,  TAMPIERI, Marsia

    发明人： ANDREOTTI, Daniele ,  BACCHI, Sergio ,  DELPOGETTO, Monica ,  GUELFI, Simone ,  PERBONI, Alcide ,  RIBECAI, Arianna ,  SPADA, Simone ,  STABILE, Paolo ,  TAMPIERI, Marsia

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P1/00 ,  A61P25/00

    CPC分类号： C07D471/04 ,  C07D207/22

    摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper (I) (Ia)wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C(O)R 5 , nitro, -NR 6 R 7 , cyano, and a group R 8 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 6 R 7 or cyano; R 5 is a C1-C4 alkyl, -OR 6 or -NR 6 R 7 ; R 6 is hydrogen or C1-C6 alkyl; R 7 is hydrogen or C1-C6 alkyl; R 8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R 11 groups; R 9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR 6 R 7 ; X is halogen; and R'' corresponds to R; R'' 1 corresponds to R 1 ; R 2 is hydrogen, C3-C7 cycloalkyl, or a group R 9 ; R 3 is C3-C7 cycloalkyl, or a group R 9 ; or R 2 and R 3 together with N form a 5-14 membered heterocycle, which may be substituted by 1 to 3 R 10 groups; R'' 4 is hydrogen; R'' 5 corresponds to R 5 ; R'' 6 corresponds to R 6 ; R'' 7 corresponds to R 7 ; R'' 8 corresponds to R 8 ; R'' 9 corresponds to R 9 ; R 10 is a group R 8 , C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR 6 R 7 , phenyl which may be substituted by 1 to 4 R 11 groups; R'' 11 corresponds to R 11 .

    摘要翻译： 本发明涉及由式（I）的中间体化合物通过铜催化的偶联反应制备式（IA）化合物的新方法，其为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂 I）（Ia）其中R是芳基或杂芳基，其各自可以被1至4个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，C（O）R 5，硝基，-NR 6 R 7，氰基和 基团R 8; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 6 R 7或氰基; R 5是C 1 -C 4烷基，-OR 6或-NR 6 R 7; R 6是氢或C 1 -C 6烷基; R 7是氢或C 1 -C 6烷基; R 8是5-6元杂环，其可以是饱和的或可以含有一至三个双键，并且其可以被1个或更多个R 11个基团取代; R 9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基：C 3 -C 7环烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基，卤代C 1 -C 6烷基; R 11是C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基或C（ O）NR 6 - [R 7 ; X是卤素; 并且R“对应于R; R“1 对应于R 1; R 2是氢，C 3 -C 7环烷基或基团R 9; R 3是C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环，其可以被1至3个R 10个基团取代; R“4是氢; R“5”对应于R 5; R“6”对应于R 6; R“7对应于R 7; R“8对应于R 8; R“9对应于R 9; R 10是基团R 8，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6链烯基， C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基，C（O）NR 6 R 7，可被1至4个R 11个组; R“”11“对应于R 11。

    ANTIBACTERIAL CONDENSED CARBAPENEMES
    6.
    发明申请
    ANTIBACTERIAL CONDENSED CARBAPENEMES 审中-公开
    抗菌剂凝聚的CARBAPENEMES

    公开(公告)号：WO1992015587A1

    公开(公告)日：1992-09-17

    申请号：PCT/EP1992000459

    申请日：1992-03-02

    申请人： GLAXO S.P.A. ,  BIONDI, Stefano ,  ANDREOTTI, Daniele ,  ROSSI, Tino ,  CARLESSO, Robert ,  TARZIA, Giorgio ,  PERBONI, Alcide

    发明人： GLAXO S.P.A.

    IPC分类号： C07D477/00

    CPC分类号： C07D477/00 ,  Y02P20/55

    摘要： Compounds of formula (I) in which R1 represents a hydrogen atom or a hydroxyl protecting group; R2 represents a hydrogen atom, a carboxyl protecting group or a cation derived from an inorganic base or an organic base; R3 represents the group O(CH2)nR4 in which n is an integer from 2 to 6 and R4 represents a halogen atom or a hydroxy, C1-3alkoxy, C1-3alkylthio, azido, cyano, nitro or quaternary ammonium group N+R5R6R7X- wherein R¿5? and R6 independently represent a C1-3alkyl group, R7 is a C1-2 alkyl group and X?-¿ is a pharmaceutically acceptable anion and metabolically labile esters, salts and solvates thereof, and processes for their production.

    摘要翻译： 其中R1代表氢原子或羟基保护基的式（I）化合物; R2表示氢原子，羧基保护基或衍生自无机碱或有机碱的阳离子; R3代表基团O（CH2）nR4，其中n是2-6的整数，R4代表卤素原子或羟基，C1-3烷氧基，C1-3烷硫基，叠氮基， 氰基，硝基或季铵基团N + R 5 R 6 R 7 X - ，其中R 5和R 6独立地为C 1-3烷基，R 7为C 1-2烷基并且X - 为药学上可接受的阴离子。 还描述了代谢不稳定的酯，它们的盐和溶剂化物，以及制备它们的方法。

    CYCLIC KETAL DERIVATIVES
    7.
    发明申请
    CYCLIC KETAL DERIVATIVES 审中-公开
    循环牙膏衍生物

    公开(公告)号：WO1993002082A1

    公开(公告)日：1993-02-04

    申请号：PCT/EP1992001532

    申请日：1992-07-08

    申请人： GLAXO GROUP LIMITED ,  SIDEBOTTOM, Philip, James ,  WATSON, Nigel, Stephen ,  ROSS, Barry, Clive ,  PROCOPIOU, Panayiotis, Alexandrou ,  LESTER, Michael, George ,  CHAN, Chuen ,  ANDREOTTI, Daniele

    发明人： GLAXO GROUP LIMITED

    IPC分类号： C07D493/08

    CPC分类号： C07D493/08 ,  C07H19/01

    摘要： Compounds are described of formula (I) (wherein R1 represents a hydroxyl group or a group selected from -OCOCH=CHCH(CH¿3?)(CH2)3CH3, -OCOCH=CHC(CH3)=CHCH(CH3)CH2CH3 or -OCO-X-CH2CH(CH3)CH2CH3 [where X is -CH=CHCH(CH3)-, -CH2CH(OH)CH(CH3)-, -CH=CHC(OH)(CH3)-, -CH2CH(OH)CH2- or -CH2CH2CH(CH3)-]; R?2¿ represents a hydroxyl group or an acyloxy group selected from formyloxy and acetoxy; R3 represents a group selected from (a) (where R7 is a hydrogen atom or an acetyl group), -(CH¿3?)=CHCH(CH2R?8)CH¿2Ph (where R8 is a hydrogen or a hydroxyl group), -C(CH¿2?OH)=CHCH(CH3CH2Ph, -C(=CH2)CH(OH)CH(CH2OH)CH2Ph, -C(=CH2)CH(NHCOCH3)CH(CH3)CH2Ph, -C(CH2NHCOCH3)=CHCH(CH3)CH2Ph and (b); R?4, R5 and R6¿ may each independently represent a hydrogen atom or a methyl group; and salts thereof. These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

    3-TRIAZOLYLTHIOALKYL-3-AZABICYCLO (3 - 1 - O) HEXANES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS
    10.
    发明申请
    3-TRIAZOLYLTHIOALKYL-3-AZABICYCLO (3 - 1 - O) HEXANES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS 审中-公开
    3-三唑基三唑-3-基亚氨基（3 - 1 - O）HEXANES及其作为DOPAMINE D3受体配体使用

    公开(公告)号：WO2006108700A1

    公开(公告)日：2006-10-19

    申请号：PCT/EP2006/003553

    申请日：2006-04-12

    申请人： GLAXO GROUP LIMITED ,  ANDREOTTI, Daniele ,  CHECCHIA, Anna ,  HAMPRECHT, Dieter ,  MICHELI, Fabrizio

    发明人： ANDREOTTI, Daniele ,  CHECCHIA, Anna ,  HAMPRECHT, Dieter ,  MICHELI, Fabrizio

    IPC分类号： C07D403/12 ,  C07D413/12 ,  A61K31/4196 ,  A61K31/422 ,  A61P25/00

    CPC分类号： C07D413/12 ,  C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein • R 1 is hydrogen or C 1-4 alkyl; • R 2 is C 1-4 alkyl; • R 3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; • p is 0, 1 , 2, 3 or 4; and • R 4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy and C 1-4 alkanoyl; • n is 0 or 1 ; wherein when R 4 is chlorine and p is 1 , such R 4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R 3 comprises at least one SF 5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐：其中R 1是氢或C 1-4烷基; R 2是C 1-4烷基; R 3是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被 1,2,3或4个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1 -4个烷氧基，C 1-4烷酰基和SF 5; p是0，1，2，3或4; R 4和R 4独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基 C 1-4烷氧基，卤代C 1-4烷氧基和C 1-4烷酰基; n为0或1; 其中当R 4为氯且p为1时，相对于与分子的其余部分的连接键，该R 4不在邻位; 并且其中，如果n是0，则R 3 3包含至少一个SF 5基团作为取代基; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3受体的调节剂，例如。 治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。