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    Azacyclic compounds compositions containing them and their use as tachykinin antagonists
    1.
    发明授权
    Azacyclic compounds compositions containing them and their use as tachykinin antagonists 失效
    含有它们的氮环化合物组合物及其作为速激肽拮抗剂的用途

    公开(公告)号：US5633266A

    公开(公告)日：1997-05-27

    申请号：US495429

    申请日：1995-07-26

    Applicant: Raymond Baker ,  Christopher J. Swain ,  Brian J. Williams

    Inventor： Raymond Baker ,  Christopher J. Swain ,  Brian J. Williams

    IPC: A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P1/08 ,  A61P25/20 ,  A61P29/00 ,  A61P43/00 ,  C07D207/00 ,  C07D211/42 ,  C07D211/54 ,  C07D401/06

    CPC classification number: C07D401/06 ,  C07D211/42

    Abstract: The present invention relates to compounds of formula (I), and salts and prodrugs thereof, wherein n is 1 , 2 or 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents optionally substituted (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3; R.sup.2 represents optionally substituted aryl, heteroaryl, benzhydryl or benzyl; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.8 represents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a variety of substituents, or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.

    Abstract translation: PCT No.PCT / EP94 / 00412 Sec。 371日期：1995年7月26日 102（e）日期1995年7月26日PCT 1994年2月10日PCT PCT。 WO94 / 19323 PCT出版物 （I）的化合物本发明涉及式（I）化合物及其盐和前药，其中n为1,2或3，并且其中（CH 2）n的任何碳原子可以是 被R4和/或R5取代; X表示O或S; R 1表示任选取代的（CH 2）q苯基，其中q是0,1,2或3; R 2表示任选取代的芳基，杂芳基，二苯甲基或苄基; R 4和R 5各自独立地表示H，卤素，C 1-6烷基，氧代，CO 2 R a或CONR a R b; R 6表示H或C 1-6烷基; R 7表示C 1-6烷基或任选取代的苯基; R8表示H，CORa，CO 2 R a，COCONR a R b，COCO 2 R a，任选被各种取代基取代的C 1-6烷基，或任选被氧代取代的被任选取代的芳族杂环取代的C 1-6烷基。 这些化合物是可用于治疗疼痛或炎症，偏头痛或呕吐的速激肽拮抗剂。

    Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
    2.
    发明授权
    Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy 失效
    氮杂双环化合物，含有它们的药物组合物及其在治疗中的用途

    公开(公告)号：US5288730A

    公开(公告)日：1994-02-22

    申请号：US899205

    申请日：1992-06-16

    Applicant: Raymond Baker ,  Christopher J. Swain ,  Martin R. Teall ,  Brian J. Williams

    Inventor： Raymond Baker ,  Christopher J. Swain ,  Martin R. Teall ,  Brian J. Williams

    IPC: A61K31/40 ,  A61K31/435 ,  A61K31/55 ,  A61P1/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  C07F7/08 ,  C07D453/00

    CPC classification number: C07D453/02

    Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 represents phenyl or thienyl, either of which groups may be optionally substituted by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl;R.sup.2 represents benzyl which may be substituted in the benzyl ring by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, S0.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a C0.sub.2 R.sup.b, --C0.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.

    Abstract translation: 式（I）化合物及其盐和前药：（*化学结构*）（I）其中Q是任选取代的氮杂双环体系的残基; X表示氧杂或硫杂; Y表示H或羟基; R 1表示苯基或噻吩基，其中任一个可以任选被卤素，三氟甲基或C 1-3烷氧基或C 5-7环烷​​基取代; R 2表示可以在苄基环中被卤素，三氟甲基或C 1-3烷氧基取代的苄基或C 5-7环烷​​基; 并且R 3，R 4和R 5独立地表示H，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，SCH 3，SOCH 3，SO 2 CH 3，-NR a R b，-NR a COR b， -NR a CO 2 R b，-CO 2 R a或-CONR a R b; 并且R a和R b独立地表示H，C 1-6烷基，苯基或三氟甲基，是速激肽受体拮抗剂。 它们及其组合物可用于治疗。

    Substituted morpholine derivatives and their use as therapeutic agents
    3.
    发明授权
    Substituted morpholine derivatives and their use as therapeutic agents 失效
    取代的吗啉衍生物及其作为治疗剂的用途

    公开(公告)号：US5612337A

    公开(公告)日：1997-03-18

    申请号：US663201

    申请日：1996-06-13

    Applicant: Raymond Baker ,  Timothy Harrison ,  Angus M. MacLeod ,  Andrew P. Owens ,  Eileen M. Seward ,  Christopher J. Swain ,  Martin R. Teall

    Inventor： Raymond Baker ,  Timothy Harrison ,  Angus M. MacLeod ,  Andrew P. Owens ,  Eileen M. Seward ,  Christopher J. Swain ,  Martin R. Teall

    IPC: C07D487/08 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07F9/6533 ,  C07F9/6558

    CPC classification number: C07D413/06 ,  C07D413/14 ,  C07F9/6533 ,  C07F9/65583

    Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 is hydrogen, halogen, C.sub.1-6 C alkyl, C.sub.1-6 alkoxy, CF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b are hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halogen, C .sub.1-6 alkyl, C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, halogen or CF.sub.3 ; R.sup.4 is selected from the definitions of R.sup.1 ; R.sup.5 is selected from the definitions of R.sup.2 ; R.sup.6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by .dbd.O, .dbd.S or a C.sub.1-4 alkyl group, and optionally substituted by an aminoalkyl group; R.sup.9a and R.sup.9b are hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined to form a C.sub.5-7 ring; X is C.sub.1-4 alkylene optionally substituted by oxo; and Y is a C.sub.1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C.sub.1-4 alkyl, R.sup.6 is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

    Abstract translation: PCT No.PCT / GB94 / 02819 Sec。 371日期：1996年6月13日 102（e）日期1996年6月13日PCT 1994年12月23日PCT公布。 公开号WO95 / 18124 日期：1995年7月6日（一）本发明涉及式（I）化合物，其中R 1为氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，NO 2，CN，SR a，SOR a ，SO 2 R a，CO 2 R a，CONR a R b，C 2-6烯基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b是氢或C 1-4烷基; R2是氢，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R3是氢，卤素或CF3; R4选自R1的定义; R5选自R2的定义; R6是含有2或3个氮原子的5元或6元杂环，任选被= O，= S或C 1-4烷基取代，并且任选被氨基烷基取代; R9a和R9b是氢或C1-4烷基，或R9a和R9b连接形成C5-7环; X是任选被氧代取代的C 1-4亚烷基; Y是任选被羟基取代的C 1-4烷基; 条件是如果Y是C 1-4烷基，则R6至少被氨基烷基取代; 及其药学上可接受的盐和前药。 该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

    Spiro-piperidine derivatives and their use as tachykinin antagonists
    9.
    发明授权
    Spiro-piperidine derivatives and their use as tachykinin antagonists 失效
    螺哌啶衍生物及其作为速激肽拮抗剂的用途

    公开(公告)号：US6060469A

    公开(公告)日：2000-05-09

    申请号：US77063

    申请日：1998-05-18

    Applicant: Raymond Baker ,  Timothy Harrison ,  Christopher John Swain ,  Brian John Williams

    Inventor： Raymond Baker ,  Timothy Harrison ,  Christopher John Swain ,  Brian John Williams

    IPC: A61K31/00 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/505 ,  A61K31/506 ,  A61P1/00 ,  A61P1/08 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  C07D491/10 ,  C07D491/107 ,  C07D471/10

    CPC classification number: C07D491/10

    Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.10 are a variety of substituents defined in the specification; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, emesis and postherpetic neuralgia.

    Abstract translation: PCT No.PCT / GB96 / 02853 Sec。 371日期1998年5月18日 102（e）日期1998年5月18日PCT提交1996年11月20日PCT公布。 公开号WO97 / 19084 日期：1997年5月29日本发明涉及式（I）化合物，其中R 1表示卤素，羟基，任选被一个或三个氟原子取代的C 1-6烷基，任选被一至三个氟原子取代的C 1-6烷氧基，或 任选被一至三个氟原子取代的C 1-6烷硫基; R 2表示氢，卤素，C 1-6烷基或C 1-6烷氧基; 或者当R 2与R 1相邻时，它们可以连接在一起，使得形成含有一个或两个氧原子的5-或6-元饱和或不饱和环; R3表示含有1,2,3或4个选自氮，氧和硫的杂原子的任选取代的5-或6-元芳族杂环基; m为0-3，n为0-3，条件是m + n的总和为2或3; p为零或1; q为1或2; 当m为1且n为1或2时，虚线表示任选的双键; R4，R5，R6，R9和R10是说明书中定义的各种取代基; 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，呕吐和带状疱疹后神经痛。

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