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    Piperidone tachykinin antagonists
    11.
    发明授权
    Piperidone tachykinin antagonists 失效
    哌啶酮速激肽拮抗剂

    公开(公告)号：US06262075B1

    公开(公告)日：2001-07-17

    申请号：US09117011

    申请日：1998-07-20

    Applicant: Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Donald Stuart Middleton ,  Sandra Dora Meadows

    Inventor： Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Donald Stuart Middleton ,  Sandra Dora Meadows

    IPC: A61K31454

    CPC classification number: C07D401/14

    Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof, wherein X is a direct link or C1-C4 alkylene; and R is C3-C7 cycloalkyl optionally substituted by 1 or 2 substituents each independently selected from fluoro and C3-C7 cycloalkyl: with the proviso that X is not methylene when R is cyclopropyl, together with processes for the preparation of, intermediates used in the preparation of, compositions containing and uses of, such compounds. These compounds are useful as tachykinin antagonists.

    Abstract translation: 本发明提供式（I）化合物及其药学上可接受的酸加成盐，其中X为直链或C1-C4亚烷基; 并且R是任选被1或2个独立地选自氟和C 3 -C 7环烷基的取代基取代的C 3 -C 7环烷基：条件是当R是环丙基时，X不是亚甲基，以及制备用于 含有和使用这些化合物的组合物的制备。 这些化合物可用作速激肽拮抗剂。

    5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists
    12.
    发明授权
    5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists 失效
    5-氮杂二环（3.1.0）己基烷基-2-哌啶酮和γ-谷氨酰胺作为神经激肽受体拮抗剂

    公开(公告)号：US6034082A

    公开(公告)日：2000-03-07

    申请号：US74931

    申请日：1998-05-13

    Applicant: Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Donald Stuart Middleton ,  Sandra Dora Meadows

    Inventor： Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Donald Stuart Middleton ,  Sandra Dora Meadows

    IPC: A61K31/00 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/00 ,  A61P11/00 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P25/00 ,  A61P25/04 ,  A61P27/16 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D243/08 ,  C07D401/02 ,  C07D413/14

    CPC classification number: C07D401/06

    Abstract: Compounds of formula (I) ##STR1## and salts thereof, wherein: R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alky aryl or aryl(C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents or is indolyl, thienyl, benzothienyl or naphthyl; R.sup.3 is NH.sub.2,--NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 SO.sub.2 N(R.sup.4).sub.2, NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a group or formula (a) ##STR2## wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.6 alkyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.4 -C.sub.8 cycloalkanoly, C.sub.3 -C.sub.7 cycloalkyl(C.sub.2 -C.sub.6)alkanoyl, aryl CO--, C.sub.1 -C.sub.6 alkylSO.sub.2 --, (R.sup.4).sub.2 NSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkylSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl-SO.sub.2 --, or arylSO.sub.2 --; X is CH.sub.2 or C.dbd.O; m is 0, 1 or 2 with the proviso that m is not O when W is NR.sup.5, C.dbd.O, or O; and n is an integer of from 1 to 4. These compounds are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.

    Abstract translation: PCT No.PCT / EP96 / 05000 Sec。 371日期：1998年5月15日 102（e）日期1998年5月15日PCT 1996年11月11日PCT PCT。 公开号WO97 / 19942 日本时间1997年6月5日式（I）化合物及其盐，其中：R1为C1-C6烷基，C3-C7环烷基，C3-C7环烷基（C1-C4）烷基芳基或芳基（C1-C4）烷基; 其中C 1 -C 6烷基任选被氟取代，并且C 3 -C 7环烷基或C 3 -C 7环烷基（C 1 -C 4）烷基在环烷基环中任选被至多两个独立地选自卤素，C 1 -C 4烷氧基或卤代 （C 1 -C 4）烷氧基; R2是任选被一个或两个卤素取代基取代的苯基，或是吲哚基，噻吩基，苯并噻吩基或萘基; R3是NH2，-NR4SO2（C1-C6烷基），-NR4SO2芳基，-NR4SO2N（R4）2，NR4CO（C1-C6烷基），-NR4CO芳基或式（a）其中W是O，NR5，CH（ OH），CHCO 2 H，CHN（R 4）2，CHF，CF 2，C = O或CH 2; R4是H或C1-C6烷基; R 5是H，C 1 -C 6烷基，C 3 -C 7环烷基，C 3 -C 7环烷基（C 1 -C 6）烷基，C 2 -C 6烷酰基，C 4 -C 8环烷醇聚，C 3 -C 7环烷基（C 2 -C 6）烷酰基，芳基CO-，C 1 -C 6烷基SO 2 - （R 4）2 NSO 2 - ，C 3 -C 7环烷基SO 2 - ，C 3 -C 7环烷基（C 1 -C 6）烷基-SO 2 - 或芳基SO 2 - X是CH 2或C = O; m为0,1或2，条件是当W为NR5，C = O或O时，m不为O; 并且n为1至4的整数。这些化合物是用于治疗各种医学状况（包括尿失禁，哮喘和相关病症）的神经激肽受体拮抗剂。

    Compounds as delta opioid agonists
    14.
    发明授权
    Compounds as delta opioid agonists 失效
    化合物作为δ阿片激动剂

    公开(公告)号：US06200978B1

    公开(公告)日：2001-03-13

    申请号：US09261540

    申请日：1999-03-03

    Applicant: Graham Nigel Maw ,  Donald Stuart Middleton

    Inventor： Graham Nigel Maw ,  Donald Stuart Middleton

    IPC: A61K31496

    CPC classification number: C07D211/26 ,  C07D205/04 ,  C07D209/08 ,  C07D209/44 ,  C07D213/79 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D249/06 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D277/24 ,  C07D277/56 ,  C07D487/04

    Abstract: Compounds of the formula (I)—shown below—are described. The compounds are useful in the manufacture of a pharmaceutical composition for preventing or treating inflammatory diseases such as arthritis, psoriasis, asthma, or inflammatory bowel disease, disorders of respiratory function, gastrointestinal disorders such as functional bowel disease, functional GI disorders such as irritable bowel syndrome, functional diarrhoea, functional distension, functional pain, non-ulcerogenic dyspepsia or others associated with disorders of motility or secretion, urogenital tract disorders such as incontinence, as analgesics for treating pain including non-somatic pain, or as immunosuppressants to prevent rejection in organ transplant and skin graft.

    Abstract translation: 描述下式（I）的化合物。该化合物可用于制备用于预防或治疗炎性疾病如关节炎，牛皮癣，哮喘或炎性肠病，呼吸功能障碍，胃肠道疾病的药物组合物 诸如功能性肠病，功能性胃肠疾病如肠易激综合征，功能性腹泻，功能性膨胀，功能性疼痛，非溃疡性消化不良或与运动性或分泌性障碍相关的其它功能性肠病，泌尿生殖道疾病如失禁等疾病，作为治疗用止痛剂 疼痛包括非躯体疼痛，或作为免疫抑制剂，以防止器官移植和皮肤移植排斥反应。

    (Azetidin-1-ylalkyl) lactams as tachykinin antagonists
    16.
    发明授权
    (Azetidin-1-ylalkyl) lactams as tachykinin antagonists 失效
    （氮杂环丁烷-1-基烷基）内酰胺作为速激肽拮抗剂

    公开(公告)号：US5968923A

    公开(公告)日：1999-10-19

    申请号：US798534

    申请日：1997-02-10

    Applicant: Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Sandra Dora Meadows ,  Donald Stuart Middleton

    Inventor： Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Sandra Dora Meadows ,  Donald Stuart Middleton

    IPC: C07D205/08 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61P1/00 ,  A61P11/00 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P29/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D205/04 ,  C07D205/06 ,  C07D205/085 ,  C07D211/76 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/02 ,  C07D451/06 ,  C07D521/00 ,  A61K401/06 ,  A61K413/14 ,  A61K451/02

    CPC classification number: C07D231/12 ,  C07D211/76 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D451/02

    Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.3 R.sup.4, --NR.sup.5 CONR.sup.5 R.sup.6, (C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.4 alkyl)R.sup.5 N--, --NR.sup.5 COCF.sub.3, --NR.sup.5 SO.sub.2 CF.sub.3, --NR.sup.5 (SO.sub.2 C.sub.1 -C.sub.4 alkyl), --NR.sup.5 SO.sub.2 NR.sup.5 R.sup.6, --NR.sup.5 (SO.sub.2 aryl), --N(aryl) (SO.sub.2 C.sub.1 -C.sub.4 alkyl), --OR.sup.5, --O(C.sub.3 -C.sub.7 cycloalkyl), --SO.sub.2 NR.sup.5 R.sup.6, het.sup.3 or a group of formulas: (a), (b), (c), (d), (e), (f), (g) or (h); X is C.sub.1 -C.sub.4 alkylene; X.sup.1 is a direct link or C.sub.1 -C.sub.6 alkylene; X.sup.2 is a direct link, CO, SO.sub.2, or NR.sup.5 CO; and m is 0, 1 or 2; together with intermediates used in the preparation of compositions containing and the use as tachykinin angatonists of such derivatives. ##STR1##

    Abstract translation: PCT No.PCT / EP95 / 03054 Sec。 371日期1997年2月10日 102（e）日期1997年2月10日PCT提交1995年7月29日PCT公布。 出版物WO96 / 05193 日期：1996年2月22日本发明提供式（I）化合物及其药学上可接受的盐，其中R为C 3 -C 7环烷基，芳基或C 1 -C 6烷基，所述C 1 -C 6烷基，所述C 1 -C 6烷基任选 被氟，COOH，-COO（C1-C4烷基），C3-C7环烷基，金刚烷基，芳基或het1取代，所述C3-C7环烷基任选被1或2个独立地选自C 1 -C 4烷基，C 3 C 1 -C 4烷氧基，羟基，氟，氟（C 1 -C 4）烷基和氟（C 1 -C 4）烷氧基; R1是苯基，萘基，噻吩基，苯并噻吩基或吲哚基，各自任选被1或2个独立地选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素和三氟甲基的取代基取代; R2是-CO2H，-CONR3R4，-CONR5（C3-C7环烷基），-NR5（C2-C5烷酰基），-NR3R4，-NR5CONR5R6，（C3-C7环烷基-C1-C4烷基）R5N-，-NR5COCF3， NR5SO2CF3，-NR5（SO2 C1-C4烷基），-NR5SO2NR5R6，-NR5（SO2芳基），-N（芳基）（SO2C1-C4烷基），-OR5，-O（C3-C7环烷基），-SO2NR5R6， 或（a），（b），（c），（d），（e），（f），（g）或（h） X是C 1 -C 4亚烷基; X1是直链或C1-C6亚烷基; X2是直接连接，CO，SO2或NR5CO; m为0,1或2; 以及用于制备含有这种衍生物的速激肽类似物的组合物中使用的中间体。

    3-aza and 3-oxa piperidone tachykinin antagonists
    17.
    发明授权
    3-aza and 3-oxa piperidone tachykinin antagonists 失效
    3-氮杂和3-氧杂哌啶酮速激肽拮抗剂

    公开(公告)号：US5846965A

    公开(公告)日：1998-12-08

    申请号：US788001

    申请日：1997-01-24

    Applicant: Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Sandra Dora Meadows ,  Donald Stuart Middleton

    Inventor： Alexander Roderick MacKenzie ,  Allan Patrick Marchington ,  Sandra Dora Meadows ,  Donald Stuart Middleton

    IPC: A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/5355 ,  A61P1/00 ,  A61P11/00 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D403/06 ,  C07D413/06 ,  A61K31/395 ,  C07D205/04 ,  C07D243/08 ,  C07D403/14

    CPC classification number: C07D403/06 ,  C07D413/06

    Abstract: Compounds of the formula: ##STR1## wherein: X is O, NH or NR.sup.1 ; R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl or aryl (C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R.sup.3 is NH.sub.2, --NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.6 alkyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.4 -C.sub.8 cycloalkanoyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.2 -C.sub.6)alkanoyl, aryl CO--, C.sub.1 -C.sub.6 alkyl SO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl SO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl SO.sub.2 --, aryl-SO.sub.2 -- or (R.sup.6).sub.2 NSO.sub.2 --, wherein each R.sup.6 is independently H or C.sub.1 -C.sub.4 alkyl or the two groups may be joined to form with the nitrogen atom to which they are attached, a pyrrolidinyl, piperidino, morphlino or piperazinyl group; m is 0, 1 or 2 with the proviso that m is not 0 when W is NR.sup.5, C.dbd.O, or O; and n is an integer of from 1 to 4; are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.

    Abstract translation: 下式的化合物：其中：X是O，NH或NR1; R1是C1-C6烷基，C3-C7环烷基，C3-C7环烷基（C1-C4）烷基，芳基或芳基（C1-C4）烷基; 其中C 1 -C 6烷基任选被氟取代，并且C 3 -C 7环烷基或C 3 -C 7环烷基（C 1 -C 4）烷基任选在环烷基环中被至多两个各自独立地选自卤素， C4烷氧基或卤代（C1-C4）烷氧基; R2是任选被一个或两个卤素取代基取代的苯基，吲哚基或噻吩基; R 3是NH 2，-NR 4 SO 2（C 1 -C 6烷基），-NR 4 SO 2芳基，-NR 4 CO（C 1 -C 6烷基），-NR 4 CO芳基或在其中W为W的5至7元N-连接的环状基团 O，NR 5，CH（OH），CHCO 2 H，CHN（R 4）2，CHF，CF 2，C = O或CH 2; R4是H或C1-C6烷基; R5是H，C1-C6烷基，C3-C7环烷基，C3-C7环烷基（C1-C6）烷基，C2-C6烷酰基，C4-C8环烷酰基，C3-C7环烷基（C2-C6）烷酰基，芳基CO-， C 1 -C 6烷基SO 2 - ，C 3 -C 7环烷基SO 2 - ，C 3 -C 7环烷基（C 1 -C 6）烷基SO 2 - ，芳基-SO 2 - 或（R 6）2 NSO 2 - ，其中每个R 6独立地是H或C 1 -C 4烷基或 两个基团可以与它们所连接的氮原子结合形成吡咯烷基，哌啶子基，吗啉基或哌嗪基; m为0,1或2，条件是当W为NR5，C = O或O时，m不为0; n为1〜4的整数， 是用于治疗各种医学状况（包括尿失禁，哮喘和相关病症）的神经激肽受体拮抗剂。

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