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    • 2. 发明申请
      WO1996005203A1 SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
    • SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
    • 螺旋取代的亚氨基衍生物及其作为治疗剂的用途
    • WO1996005203A1
    • 1996-02-22
    • PCT/GB1995001867
    • 1995-08-07
    • MERCK SHARP & DOHME LIMITED , LADDUWAHETTY, Tamara , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
    • MERCK SHARP & DOHME LIMITED
    • C07D471/10
    • C07D471/10
    • The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C1-6alkyl, C1-6alkoxy, hydroxy, halogen, cyano, trifluoromethyl, SO2C1-6alkyl, NR R , NR COR or CONR R , where R and R are each H, C1-6alkyl, phenyl or trifluoromethyl; R represents phenyl optionally substituted by 1, 2 or 3 of C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, -O(CH2)pO- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , SO2R , NR R , NR COR , NR CO2R , COR , CO2R or CONR R ; naphthyl; benzhydryl; or benzyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R represents hydrogen, a substituent as defined for R or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R and R are each H or C1-6alkyl or R and R together are linked so as to form a C1-3alkylene chain; R represents H, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenylC1-4alkyl, CO2R , CONR R , SOR or SO2R , wherein the phenyl moiety may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represent =O; and Z represents a bond, O, S, SO, SO2, NR , or -(CR R )- where R is H or C1-6alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    • 本发明涉及式（I）化合物，其中n为0,1,2或3; R表示C 1-6烷基，C 1-6烷氧基，羟基，卤素，氰基，三氟甲基，SO 2 C 1-6烷基，NR a R b，NR a COR b或CONR a R b，其中 R a和R b各自为H，C 1-6烷基，苯基或三氟甲基; R 1表示任选被1,2或3个C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，-O（CH 2）p O--（其中p为1或 2），卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a，SO 2 R a，NR a R b，NR a COR b， ，NR a CO 2 R b，COR a，CO 2 R a或CONR a R b; 萘; 二苯甲基; 或苄基，其中苄基和二苯甲基的萘基或每个苯基部分可被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 2表示氢，R 1所定义的取代基或选自吲唑基，噻吩基，呋喃基，吡啶基，噻唑基，四唑基和喹啉基的杂芳基; 其中每个杂芳基可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 3和R 4各自为H或C 1-6烷基或R 3和R 4一起连接形成C 1-3亚烷基链; R 5表示H，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基C 1-4烷基，CO 2 R a，CONR a R b，SOR a或SO 2 R a，其中 苯基部分可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; X和Y各自为H，或一起表示= O; 和Z表示键，O，S，SO，SO 2，NR 6或 - （CR 6 R 6） - ，其中R 6是H或C 1-6烷基; 或其药学上可接受的盐。 该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 发明申请
      WO1995004042A1 4-PHENYL-4-PHENYLPROPYL(ENYL)-PIPERIDINES AS TACHYKININ ANTAGONISTS 审中-公开
    • 4-PHENYL-4-PHENYLPROPYL(ENYL)-PIPERIDINES AS TACHYKININ ANTAGONISTS
    • 4-苯基-4-苯丙氨酸（ENYL）-PIPERIDINES作为TACHYKININ ANTAGONISTS
    • WO1995004042A1
    • 1995-02-09
    • PCT/GB1994001576
    • 1994-07-21
    • MERCK SHARP & DOHME LIMITED , MACLEOD, Angus, Murray , MERCHANT, Kevin, John , STEVENSON, Graeme, Irvine
    • MERCK SHARP & DOHME LIMITED
    • C07D211/22
    • C07D401/06 , C07D211/18 , C07D211/22 , C07D211/32
    • The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R , R , R and R ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R represents optionally substituted phenyl; R represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R represents H, COR , CO2R , COCONR R , COCO2R , SO2R , CONR SO2R , C1-6alkyl optionally substituted by a group selected from (CO2R , CONR R , hydroxy, cyano, COR , NR R , C(NOH)NR R , CONHphenyl(C1-4alkyl), COCO2R , COCONR R , SO2R , CONR SO2R and optionally substituted phenyl), Y-R or CO-Z-(CH2)q-R ; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy, or R and R together form a group =0; R and R each independently represents H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy or R and R together form a group =0; R represents an optionally substituted aromatic heterocycle; R represents H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, or phenyl; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl or C3-5cycloalkylmethyl; R represents NR R or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, optionally substituted phenyl or phenylC1-4alkyl; R represents C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH2, O, S or NR ; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
    • 本发明涉及式（I）化合物及其药学上可接受的盐和前药，其中X表示任选被一个或多个R 4，R 5，R 6和R 6取代的丙烯或亚丙烯基链 [R <7>; m为2,3或4; 当m为2或3时，n为0,1或2，m为4时，n为0或1; R 1表示任选取代的苯基; R 2表示任选取代的苯基，杂芳基，二苯甲基或苄基; R 3表示H，COR 9，CO 2 R 10，COCONR 10 R 11，COCO 2 R 10，SO 2 R 15，CONR 10 SO 2 R 15，任选取代的C 1-6烷基 通过选自（CO 2 R 10，CONR 10 R 11，羟基，氰基，COR 9，NR 10 R 11，C（NOH）NR 10 R 11， ，CONH苯基（C 1-4烷基），COCO 2 R 10，COCONR 10 R 11，SO 2 R 15，CONR 10 SO 2 R 15和任选取代的苯基），YR 8或CO-Z- （CH 2）q或r <12>; R 4和R 5各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，羟基或C 1-6烷氧基，或者R 4和R 5一起形成基团= 0; R 6和R 7各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，羟基或C 1-6烷氧基或R 6和R 7一起形成基团= 0; R 8表示任选取代的芳族杂环; R 9表示H，C 1-6烷基，C 3-6环烷基，C 3-5环烷基甲基或苯基; R 10和R 11各自独立地表示H，C 1-6烷基，C 3-6环烷基或C 3-5环烷基甲基; R 12表示NR 13 R 14或任选取代的芳族或非芳族氮杂环或氮杂双环基; R 13和R 14各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，任选取代的苯基或苯基C 1-4烷基; R 15表示C 1-6烷基，C 3-6环烷基，C 3-5环烷基甲基，三氟甲基或任选取代的苯基; Y表示可任选被氧代取代的1,2,3或4个碳原子的烃链; Z表示CH 2，O，S或NR 10; q表示0,1,2,3,4,5或6.化合物是用于治疗疼痛或炎症，偏头痛或呕吐的速激肽拮抗剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明申请
      WO1994001402A1 HETEROCYCLIC AMIDE DERIVATIVES AS TACHYKININ DERIVATIVES 审中-公开
    • HETEROCYCLIC AMIDE DERIVATIVES AS TACHYKININ DERIVATIVES
    • 作为TACHYKININ衍生物的杂环酰胺衍生物
    • WO1994001402A1
    • 1994-01-20
    • PCT/GB1993001415
    • 1993-07-06
    • MERCK SHARP & DOHME LIMITED , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
    • MERCK SHARP & DOHME LIMITED
    • C07D209/16
    • C07D213/81 , C07D209/14 , C07D295/15 , C07D401/12 , C07D403/12 , C07D409/12 , C07D453/02
    • Compounds of formula (I), and salts and prodrugs thereof, wherein Q is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional covalent bond; one of X and Y is H and the other is hydroxy or C1-6alkoxy, or X and Y together form a group =O or =NOR where R is H or C1-6alkyl; R is H or C1-6alkyl. R is CO-W-R where W represents a bond or a hydrocarbon chain of 1-6 carbon atoms and R is an azacyclic or azabicyclic group; R is H, C1-6alkyl or C2-6alkenyl; and R is phenyl optionally substituted by 1-3 of C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , NR R , NR COR , NR CO2R , CO2R or CONR R , where R and R are H, C1-6alkyl, phenyl or trifluoromethyl; are tachykinin antagonists useful in therapy.
    • 式（I）化合物及其盐和前药，其中Q 1是被一个或多个卤素取代的苯基; 任选取代的萘基，吲哚基，苯并噻吩基，苯并呋喃基，苄基或芴基; 虚线表示任选的共价键; X和Y之一是H，另一个是羟基或C 1-6烷氧基，或X和Y一起形成基团= O或= NOR 5，其中R 5是H或C 1-6烷基; R 1是H或C 1-6烷基。 R 2是CO-W-R 6，其中W表示1-6个碳原子的键或烃链，R 6是氮杂环或氮杂双环基; R 3是H，C 1-6烷基或C 2-6烯基; 并且R 4是任选被1-3个C 1-6烷基，C 2-6烯基，C 2-6炔基，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a ，NR a R b，NR a COR b，NR a CO 2 R b，CO 2 R a或CONR a R b，其中R a和R b， b是H，C 1-6烷基，苯基或三氟甲基; 是用于治疗的速激肽拮抗剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明申请
      WO1993018023A1 HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    • HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 杂环化合物，其制备方法和含有它们的药物组合物
    • WO1993018023A1
    • 1993-09-16
    • PCT/GB1993000411
    • 1993-02-26
    • MERCK SHARP & DOHME LIMITED , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
    • MERCK SHARP & DOHME LIMITED
    • C07D333/58
    • C07D333/58 , C07D209/16
    • Compounds of formula (I), and salts and prodrugs thereof, wherein Q is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; .... is an optional covalent bond; one of X and Y is H and the other is hydroxy or C1-6alkoxy, or X and Y are together =0 or =NOR ; R and R are H; C1-6alkyl optionally substituted by hydroxy, cyano, COR , CO2R , CONR R , or NR R (where R and R are H, C1-6 alkyl or phenyl (C0-4alkyl) optionally substituted by C1-6alkyl, C1-6alkoxy, halo and trifluoromethyl); phenyl (C1-4alkyl) (optionally substituted by C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl); COR ; CO2R ; CONR R ; COC1-6alkylNR R ; CONR COOR ; or SO2R ; R is H, C1-6alkyl or C2-6alkenyl; and R is phenyl optionally substituted by C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , NR R , NR COR , NR CO2R , CO2R or CONR R , where R and R are H, C1-6alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
    • 式（I）化合物及其盐和前药，其中Q 1是卤素取代的苯基; 萘; 吲哚基; 苯并噻吩基; 苯并呋喃基; 苄基; 或芴基; ....是可选的共价键; X和Y之一是H，另一个是羟基或C 1-6烷氧基，或X和Y一起= 0或= NOR 5。 R 1和R 2是H; 任选被羟基，氰基，COR c，CO 2 R c，CONR c R d或NR c R d取代的C 1-6烷基（其中R c和R d分别为 任选被C 1-6烷基，C 1-6烷氧基，卤素和三氟甲基取代的C 1-6烷基或苯基（C 0-4烷基）; 苯基（C 1-4烷基）（任选被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代）; COR ; CO 2 ; CONR - [R ; COC1-6alkylNR - [R ; CONR COOR ; 或SO2R ; R 3是H，C 1-6烷基或C 2-6烯基; R 4是任选被C 1-6烷基，C 2-6烯基，C 2-6炔基，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a，NR a取代的苯基 R b，NR a R c，NR a CO 2 R b，CO 2 R a或CONR a R b，其中R a和R b是H ，C 1-6烷基，苯基或三氟甲基; 速激肽拮抗剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO2010007382A8 BENZAZEPINE DERIVATIVES AND THEIR USE AS HSTAMINE H3 ANTAGONISTS 审中-公开
    • BENZAZEPINE DERIVATIVES AND THEIR USE AS HSTAMINE H3 ANTAGONISTS
    • 苯并噻吩衍生物及其作为HSTAMINE H3拮抗剂的用途
    • WO2010007382A8
    • 2010-03-18
    • PCT/GB2009001774
    • 2009-07-17
    • TAKEDA PHARMACEUTICAL , POONI PARMINDER KAUR , MERCHANT KEVIN JOHN , KERR CATRINA , CROSBY STUART RICHARD , OKAWA TOMOHIRO , SASAKI MITSURU , GOTOU MIKA , SHOWELL GRAHAM ANDREW , TEALL MARTIN RICHARD
    • POONI PARMINDER KAUR , MERCHANT KEVIN JOHN , KERR CATRINA , CROSBY STUART RICHARD , OKAWA TOMOHIRO , SASAKI MITSURU , GOTOU MIKA , SHOWELL GRAHAM ANDREW , TEALL MARTIN RICHARD
    • C07D223/16 , A61K31/55 , A61P25/18 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
    • C07D403/12 , C07D223/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
    • A compound having the formula (1) wherein: R1 is a group selected from C3-8 cycloalkyl, C1-6 alkyl, C1-6 alkylene-C3-8 cycloalkyl, each of which groups may optionally be substituted with C1-6 alkyl, halogen, haloC1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C1-6 alkyl, haloC1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group -(CH2)n- formed thereby being optionally substituted with a group selected from C1-4 alkyl, C3-8 cycloalkyl and arylsulfonyl; A is a group selected from -N(R2)CO-, -CON(R2)-, -OC(O)-, -C(O)O-, -CO-, -C(R2)(OR3)-, -C(=N-O-R3)-, - C(=CR2R3)-, -C3-8 cycloalkylene-, -C(R2)(haloC1-6 alkyl)-, C1-4 alkylene and -C(OR3)(haloC1-6 alkyl)-; R2 and R3 are each independently selected from H, C1-6 alkyl, and C3-8 cycloalkyl, or, when A is -N(R2)CO- and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C1-4 alkylene or C2-4 alkenylene, each of which may optionally be substituted with one or more C1-4 alkyl groups, OR16, halogen or haloC1-6 alkyl; Z is selected from aryl, heteroaryl, C3-8 cycloalkyl, and heterocyclyl, each of which may optionally be substituted by a group selected from -Y-aryl, -Y-heteroaryl, -Y-C3-8 cycloalkyl and -Y-heterocyclyl, or, when X is present, Z may be H, or, when X is absent and A is -C(R2)(OR3)- or -N(R2)CO-, Z may be H, or, when A is -N(R2)CO- and X is absent, Z may form, together with the adjacent nitrogen atom and R2, an N-containing heterocyclyl group which may optionally be substituted, wherein, when A is -CO-, Z is linked to X or A via a carbon atom and wherein, when A is -N(R2)CO- and Z is H, R1 is C3-8 cycloalkyl; and Y represents a bond, C1-6 alkylene, CO, NR14, COC2-6 alkenylene, O, SO2 or NHCOC1-6 alkylene; wherein said cycloalkyl, aryl, heteroaryl and heterocyclyl groups Z may be optionally substituted by one or more substituents which may be the same or different, and which are selected from halogen, haloC1-6 alkyl, hydroxy, cyano, nitro, =O, -R4, -CO2R4, -COR4, -NR5R6, -C1-6 alkyl-NR5R6, -C3-8 cycloalkyl-NR5R6, - CONR12R13, -NR12COR13, -NR5SO2R6, -OCONR5R6, -NR5CO2R6, -NR4CONR5R6 or -SO2NR5R6- SHR8, -alkyl-OR8, -SOR8, -OR9, -SO2R9, -OSO2R9, -alkyl-SO2R9, -alkyl-CONHR9, -alkyl-SONHR9, -alkyl-COR10, -CO-alkyl-R10, -O-alkyl-R11 (wherein R4, R5 and R6 independently represent hydrogen, C1-6 alkyl, -C3-8 cycloalkyl, -C1-6 alkylene-C3-8 cycloalkyl, aryl, heterocyclyl or heteroaryl, wherein R8 represents C1-6 alkyl, wherein R9 represents C1-6 alkyl or aryl, wherein R10 represents aryl, wherein R11 represents C3-8 cycloalkyl or aryl, R12, R13, R14, R15 and R16 each independently represent H or C1-6 alkyl, and wherein -NR5R6 and -NR12R13 may represent a nitrogen containing heterocyclyl group); wherein said R4, R5, R6 R8, R9, R11 and R11 groups may be optionally substituted by one or more substituents which may be the same or different, and which are selected from the group consisting of halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, cyano, amino, =O or trifluoromethyl; and wherein substituents of Z selected from -Y-aryl, -Y-heteroaryl, -Y-C3-8cycloalkyl and -Y-heterocyclyl may be optionally substituted by one or more substituents selected from =O, hydroxy, cyano, nitro, halogen, haloC1-6 alkyl and C1-6alkyl; and wherein, when A is C1-4 alkylene, said cycloalkyl, aryl, heteroaryl or heterocyclyl group Z (such as a heterocyclyl group Z) is substituted at least with hydroxy, CF3, or =0; and wherein, when A is CON(R2) n is 1; or a pharmaceutically acceptable salt or ester thereof, provided that: when A is -CO-, R1 is CH3, C3-8 cycloalkyl-substituted C1-6 alkylene or n-butyl, n is 0 and X is -CH2CH2-, Z is not N-benzyl substituted 4-piperidinyl, N-(3-fluorobenzyl)-substituted 4-piperidinyl or N-acetyl substituted 4-piperidinyl; when A is -OC(O)-, R1 is cyclobutyl, n is 0 and X is -CH2CH2-, Z is not H; when A is -OC(O)-, R1 is n-propyl, n is 0 and X is -CH2-, Z is not H; and when A is -CO-, R1 is CH3, n is 0 and X is CH2, Z is not H.
    • 具有式（1）的化合物，其中：R 1是选自C 3-8环烷基，C 1-6烷基，C 1-6亚烷基-C 3-8环烷基，其各自可以任选被C 1-6烷基取代， 卤素，卤代C 1-6烷基或OR 15，或R 1是任选被C 1-6烷基，卤代C 1-6烷基或OR 15取代的杂环基; n为0,1,2,3或4，由此形成的亚烷基 - （CH 2）n任选被选自C 1-4烷基，C 3-8环烷基和芳基磺酰基的基团取代; A是选自-N（R2）CO-，-CON（R2） - ，-OC（O） - ， - （O）O-，-CO-，-C（R2）（OR3） -C（= NO-R 3） - ， - C（= CR 2 R 3） - ， - C 3-8亚环烷基 - ， - C（R 2）（卤代C 1-6烷基） - ，C 1-4亚烷基和-C（OR 3） -6烷基） - ; R2和R3各自独立地选自H，C1-6烷基和C3-8环烷基，或当A是-N（R2）CO-且X不存在时，R2可以与相邻的氮原子和Z ，可以任选被取代的含N的杂环基; X不存在或是C 1-4亚烷基或C 2-4亚烯基，其各自可以任选被一个或多个C 1-4烷基，OR 16，卤素或卤代C 1-6烷基取代; Z选自芳基，杂芳基，C 3-8环烷基和杂环基，其各自可任选被选自-Y-芳基，-Y-杂芳基，-Y-C 3-8环烷基和-Y-杂环基 或当X存在时，Z可以是H，或者当X不存在且A是-C（R 2）（OR 3） - 或-N（R 2）CO-时，Z可以是H，或者当A是 -N（R2）CO-和X不存在，Z可以与相邻的氮原子一起形成，R 2可以任选被取代的含N的杂环基，其中当A是-CO-时，Z连接到 X或A通过碳原子，并且其中当A是-N（R 2）CO-且Z是H时，R 1是C 3-8环烷基; Y表示键，C 1-6亚烷基，CO，NR 14，COC 2-6亚烯基，O，SO 2或NHCOC 1-6亚烷基; 其中所述环烷基，芳基，杂芳基和杂环基基团Z可以任选地被一个或多个可以相同或不同的取代基取代，并且选自卤素，卤代C 1-6烷基，羟基，氰基，硝基，= O - R4，-CO 2 R 4，-COR 4，-NR 5 R 6，-C 1-6烷基-NR 5 R 6，-C 3-8环烷基-NR 5 R 6，-CONR 12 R 13，-NR 12 COR 13，-NR 5 SO 2 R 6，-OCONR 5 R 6，-NR 5 CO 2 R 6，-NR 4 CONR 5 R 6或-SO 2 NR 5 R 6 -SHR 8， - 烷基-OR 8，-SOR 8，-OR 9，-SO 2 R 9，-OSO 2 R 9， - 烷基-SO 2 R 9 - - 烷基-CONHR 9 - - 烷基-SHHR 9， - 烷基-CON10，-CO-烷基-R10，-O-烷基-R11 （其中R 4，R 5和R 6独立地表示氢，C 1-6烷基，-C 3-8环烷基，-C 1-6亚烷基-C 3-8环烷基，芳基，杂环基或杂芳基，其中R 8表示C 1-6烷基， C 1-6烷基或芳基，其中R 10表示芳基，其中R 11表示C 3-8环烷基或芳基，R 12，R 13，R 14，R 15和R 16各自独立地表示H或C 1-6烷基，并且其中-NR 5 R 6和-NR 12 R 13可以表示 含氮杂环基）; 其中所述R 4，R 5，R 6，R 8，R 9，R 11和R 11基团可以任选地被一个或多个可以相同或不同的取代基取代，并且选自卤素，羟基，C 1-6烷基， C 1-6烷氧基，氰基，氨基，= O或三氟甲基; 并且其中选自-Y-芳基，-Y-杂芳基，-Y-C3-8环烷基和-Y-杂环基的Z的取代基可以任选地被一个或多个选自以下的取代基取代：选自= O，羟基，氰基，硝基，卤素， 卤代C 1-6烷基和C 1-6烷基; 并且其中当A为C 1-4亚烷基时，所述环烷基，芳基，杂芳基或杂环基Z（例如杂环基Z）至少被羟基，CF 3或= 0取代; 并且其中当A是CON（R2）时，n是1; 或其药学上可接受的盐或酯，条件是：当A为-CO-时，R 1为CH 3，C 3-8环烷基取代的C 1-6亚烷基或正丁基，n为0且X为-CH 2 CH 2 - ，Z为 不是N-苄基取代的4-哌啶基，N-（3-氟苄基）取代的4-哌啶基或N-乙酰基取代的4-哌啶基; 当A为-OC（O） - 时，R1为环丁基，n为0，X为-CH2CH2-，Z为H; 当A为-OC（O） - 时，R 1为正丙基，n为0且X为-CH 2 - ，Z不为H; 当A为-CO-时，R 1为CH 3，n为0，X为CH 2，Z为H。
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