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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.

    Aminocyclohexane derivatives as 5-HT receptor agonists
    3.
    发明授权
    Aminocyclohexane derivatives as 5-HT receptor agonists 失效
    氨基环己烷衍生物作为5-HT受体激动剂

    公开(公告)号：US06211219B1

    公开(公告)日：2001-04-03

    申请号：US09214343

    申请日：1999-01-04

    申请人： Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    发明人： Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    IPC分类号： C07D40306

    CPC分类号： C07D231/12 ,  C07D209/14 ,  C07D233/56 ,  C07D249/08

    摘要： A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.

    摘要翻译： 一类取代的氨基环己烷衍生物是5-HT1样受体的选择性激动剂，它是人类5-HT1Dalpha受体亚型的有效激动剂，同时对5-HT1Dalpha受体亚型具有至少10倍的选择性亲和力， HT1Dbeta亚型; 因此，它们可用于治疗和/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起更少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。

    Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists
    5.
    发明授权
    Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists 失效
    哌嗪，哌啶和四氢吡啶衍生物作为5-HT受体激动剂

    公开(公告)号：US5998416A

    公开(公告)日：1999-12-07

    申请号：US171930

    申请日：1998-10-26

    申请人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    发明人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    IPC分类号： C07D405/04 ,  C07D405/14 ,  A61K31/495 ,  A61K31/505

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

    摘要翻译： PCT No.PCT / GB97 / 01329 Sec。 371日期：1998年10月26日 102（e）日期1998年10月26日PCT提交1997年5月15日PCT公布。 出版物WO97 / 45432 PCT 日期1997年12月4日一类N-取代的哌嗪，哌啶和四氢吡啶衍生物，通过任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分进一步在4-位上被取代为5-HT1- 作为人5-HT1Dα受体亚型的有效激动剂，同时相对于5-HT1Dβ亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。

    Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists
    6.
    发明授权
    Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists 失效
    吲哚-3-烷基的哌嗪，哌啶和四氢吡啶衍生物作为5-HT1D-α激动剂

    公开(公告)号：US5807857A

    公开(公告)日：1998-09-15

    申请号：US737769

    申请日：1996-11-15

    申请人： Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Austin John Reeve ,  Graham Andrew Showell ,  Leslie Joseph Street ,  Victor Giulio Matassa

    发明人： Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Austin John Reeve ,  Graham Andrew Showell ,  Leslie Joseph Street ,  Victor Giulio Matassa

    IPC分类号： C07D401/14 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/495 ,  A61P9/00 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D471/04

    摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT1D receptors, being potent agonists of the human 5-HT1Dalpha receptor subtype, while possessing at least a 10-fold selective affinity for the 5-HT1Dalpha receptor subtype, relative to the 5-HT1Dbeta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.

    摘要翻译： PCT No.PCT / GB95 / 01129 Sec。 371日期1996年11月15日 102（e）日期1996年11月15日PCT提交1995年5月18日PCT公布。 公开号WO95 / 32196 （I）式（I）化合物或其盐或前药，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑的任选取代的五元杂芳环 ，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1至4个碳原子的直链或支链亚烷基链; Q表示任选被羟基取代的含有1至6个碳原子的直链或支链亚烷基链; T表示氮或CH; U表示氮或C-R2; V表示氧，硫或N-R3; -F-G-表示-CH 2 -N，-CH 2 -CH-或-CH = C-; R 1表示C 3-6烯基，C 3-6炔基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何基团可以任选被取代; 并且R 2和R 3独立地表示氢或C 1-6烷基是5-HT1D受体的选择性激动剂，它是人5-HT1Dalpha受体亚型的有效激动剂，同时对5-HT1Dalpha受体亚型具有至少10倍的选择性亲和力， 相对于5-HT1Dbeta亚型; 因此，它们可用于治疗和/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。