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    BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS
    1.
    发明申请
    BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS 审中-公开

    公开(公告)号：US20110124626A1

    公开(公告)日：2011-05-26

    申请号：US13054688

    申请日：2009-07-17

    申请人： Parminder Kaur Pooni ,  Kevin John Merchant ,  Catrina Morvern Kerr ,  Stuart Richard Crosby ,  Tomohiro Okawa ,  Mitsuru Sasaki ,  Mika Gotou ,  Graham Andrew Showell ,  Martin Richard Teall

    发明人： Parminder Kaur Pooni ,  Kevin John Merchant ,  Catrina Morvern Kerr ,  Stuart Richard Crosby ,  Tomohiro Okawa ,  Mitsuru Sasaki ,  Mika Gotou ,  Graham Andrew Showell ,  Martin Richard Teall

    IPC分类号： A61K31/397 ,  C07D403/12 ,  A61K31/55 ,  C07D401/12 ,  C07D223/16 ,  C07D413/10 ,  C07D403/14 ,  A61P25/28

    CPC分类号： C07D403/12 ,  C07D223/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

    摘要： 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)m— 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)(haloC1-6alkyl)-, C1-4 alkylene and —C(OR3)(haloC1-6alkyl)-; 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 C14 alkylene or C24 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, 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 ═O; 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.

    Gamma secretase inhibitors
    3.
    发明授权
    Gamma secretase inhibitors 失效
    γ分泌酶抑制剂

    公开(公告)号：US06448229B2

    公开(公告)日：2002-09-10

    申请号：US09896296

    申请日：2001-06-29

    申请人： Martin Richard Teall

    发明人： Martin Richard Teall

    IPC分类号： A61K315375

    CPC分类号： C07K5/06026 ,  A61K31/451 ,  A61K31/5375 ,  A61K31/54 ,  A61K38/00 ,  C07K5/06191

    摘要： The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein X is CH2, O or S. The compounds inhibit gamma secretase without affecting Notch signalling, and hence find use in the treatment or prevention of Alzheimer's disease.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐：其中X为CH 2，O或S.该化合物抑制γ分泌酶而不影响Notch信号传导，因此可用于治疗或预防阿尔茨海默氏病。

    Morpholine derivatives and their use as therapeutic agents
    5.
    发明授权
    Morpholine derivatives and their use as therapeutic agents 失效
    吗啉衍生物及其作为治疗剂的用途

    公开(公告)号：US5968934A

    公开(公告)日：1999-10-19

    申请号：US68818

    申请日：1998-05-14

    申请人： Christopher John Swain ,  Martin Richard Teall ,  Brian John Williams

    发明人： Christopher John Swain ,  Martin Richard Teall ,  Brian John Williams

    IPC分类号： A61K31/00 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D413/04 ,  C07D417/04

    摘要： The present invention relates to compounds of formula (I) ##STR1## wherein X is a 5- or 6-membered C-linked heteroaromatic ring containing 1 to 4 nitrogen atoms and optionally containing in the ring one oxygen or sulphur atom; Y is a group of the formula --(CH.sub.2).sub.n NR.sup.6 R.sup.7 or a methylene- or ethylene-linked imidazolyl group; Z is hydrogen or C.sub.1-4 alkyl optionally substituted by a hydroxy group; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9a and R.sup.9b are a variety of substituents; R.sup.6 is hydrogen, C.sub.1-6 akyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 akyl substituted by C.sub.1-4 alkoxy or hydroxy, R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or a 4-, 5- or 6-membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form a saturated or partially saturated heterocyclic ring or a non-aromatic azabicyclic ring system; and n is zero, 1 or 2; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherapeutic neuralgia.

    摘要翻译： PCT No.PCT / GB96 / 02766 Sec。 371日期：1998年5月14日 102（e）日期1998年5月14日PCT 1996年11月13日PCT公布。 WO97 / 18206 PCT公开号 日期：1997年5月22日本发明涉及式（I）化合物，其中X为含有1至4个氮原子且任选地在环中含有一个氧或硫原子的5-或6-元C-连接的杂芳环; Y是式 - （CH2）nNR6R7或亚甲基或乙烯连接的咪唑基的基团; Z是氢或任选被羟基取代的C 1-4烷基; R1，R2，R3，R4，R5，R9a和R9b是多种取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-4烷基，R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基， 苯基或被一个或两个选自C 1-4烷氧基，羟基或含有一个或两个选自N，O和S的杂原子的4-，5-或6-元杂脂肪族环取代的C 2-4烷基; 或R6和R7与它们所连接的氮原子一起形成饱和或部分饱和的杂环或非芳族氮杂双环体系; n为零，1或2; 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，呕吐和治疗后神经痛。