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    Diphenyl ether compounds useful in therapy
    2.
    发明授权
    Diphenyl ether compounds useful in therapy 失效
    用于治疗的二苯醚化合物

    公开(公告)号：US06448293B1

    公开(公告)日：2002-09-10

    申请号：US09810378

    申请日：2001-03-16

    Applicant: Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    Inventor： Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    IPC: C07C21758

    CPC classification number: C07D231/38 ,  C07C45/71 ,  C07C47/55 ,  C07C47/575 ,  C07C205/44 ,  C07C217/58 ,  C07C229/38 ,  C07C237/28 ,  C07C255/43 ,  C07C255/59 ,  C07C311/05 ,  C07C311/08 ,  C07C311/37 ,  C07C317/32 ,  C07C323/20 ,  C07C323/32 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/06 ,  C07D249/08 ,  C07D295/096 ,  C07D295/192

    Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O)R6, CO2R9, C(O)NHR6 or SO2NR6R7; R12 is F, OH, CO2H, C3-6cycloalkyl, NH2, CONH2, C1-6alkoxy, C1-6alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R13; or R6 and R7, together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R13; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, —NH2, —NH(C1-C6alkyl) or —N(C1-C6alkyl)2; wherein when R1 and R2 are methyl, R4 and R5 are hydrogen and n is 1, R3is not a —SMe group para to the ether linkage linking rings A and B.

    Abstract translation: 通式（I）的化合物或其药学上可接受的盐，溶剂化物或多晶型物; 其中; R 1和R 2可以相同或不同，为氢，C 1 -C 6烷基，（CH 2）m（C 3 -C 6环烷基），其中m = 0,1,2或3，或R 1和R 2与它们 连接形成氮杂环丁烷环; 每个R 3独立地为CF 3，OCF 3，C 1-4烷硫基或C 1 -C 4烷氧基; n为1,2或3; 并且R 4和R 5可以相同或不同，为：A-X，其中A = -CH = CH-或 - （CH 2）p - ，其中p为0,1或2; X是氢，F，Cl，Br，I，CONR6R7，SO2NR6R7，SO2NHC（= O）R6，OH，C1-4烷氧基，NR8SO2R9，NO2，NR6R11，CN，CO2R10，CHO，SR10，S（O）R9或SO2R10 ; R 6，R 7，R 8和R 10可以相同或不同，是氢或被一个或多个R 12独立地取代的C 1-6烷基; R9是任选被一个或多个R 12独立地取代的C 1-6烷基; R 11是氢，任选地被一个或多个R 12，C（O）R 6，CO 2 R 9，C（O）NHR 6或SO 2 NR 6 R 7取代的C 1-6烷基; R 12是F，OH，CO 2 H，C 3-6环烷基，NH 2，CONH 2，C 1-6烷氧基，C

    Triazole derivatives which inhibit vasopressin antagonistic activity
    5.
    发明申请
    Triazole derivatives which inhibit vasopressin antagonistic activity 失效
    抑制加压素拮抗活性的三唑衍生物

    公开(公告)号：US20070203132A1

    公开(公告)日：2007-08-30

    申请号：US10588876

    申请日：2005-01-11

    Applicant: Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    Inventor： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    IPC: A61K31/535

    CPC classification number: C07D401/14

    Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: Het represents 2-pyridinyl or 2-pyrimidinyl; R1 represents H, C1-3 alkyl or a nitrogen-containing heterocyclic ring having 5 or 6 ring atoms; R2 represents H, benzyl or C1-3 alkyl; and R3 represents H, methyl, methoxy or chloro; are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.

    Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中：Het表示2-吡啶基或2-嘧啶基; R 1表示H，C 1-3烷基或具有5或6个环原子的含氮杂环; R 2表示H，苄基或C 1-3烷基; R 3表示H，甲基，甲氧基或氯; （包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），痛经 早泄，过早（早产）劳动和雷诺氏病。

    Novel compounds
    8.
    发明申请
    Novel compounds 失效

    公开(公告)号：US20050137229A1

    公开(公告)日：2005-06-23

    申请号：US10872160

    申请日：2004-06-17

    Applicant: Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    Inventor： Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC: A61P13/00 ,  A61P25/24 ,  A61P29/00 ,  C07D207/14 ,  C07D211/06 ,  A61K31/445 ,  C07D211/56

    CPC classification number: C07D207/14

    Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    Quinoxaline derivatives useful in therapy
    10.
    发明授权
    Quinoxaline derivatives useful in therapy 失效
    喹喔啉衍生物可用于治疗

    公开(公告)号：US5863917A

    公开(公告)日：1999-01-26

    申请号：US938230

    申请日：1997-09-26

    Applicant: Charles Eric Mowbray ,  Alan Stobie

    Inventor： Charles Eric Mowbray ,  Alan Stobie

    IPC: A61K31/495 ,  A61K31/498 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  C07D241/44 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12 ,  C07D241/52

    CPC classification number: C07D403/12 ,  A61K31/498 ,  C07D241/44 ,  C07D413/06 ,  Y02P20/55

    Abstract: The invention provides compounds of formula I, ##STR1## wherein R.sup.1 and R.sup.2 independently represent Cl or C.sub.1-6 alkyl;R.sup.3 represents XCO.sub.2 R.sup.4, XCONHSO.sub.2 R.sup.5, YNHSO.sub.2 R.sup.5 or XR.sup.6 ;R.sup.4 represents H or C.sub.1-6 alkyl (optionally substituted by aryl or heterocyclyl);R.sup.5 represents CF.sub.3, heterocyclyl or C.sub.1-6 alkyl (optionally substituted by aryl or heterocyclyl);R.sup.6 represents an acidic heterocycle;X represents a C.sub.1-6 alkyl diradical (optionally subsituted by aryl or heterocyclyl); andY represents a C.sub.2-6 alkyl diradical (optionally substituted by aryl or heterocyclyl); provided that when R.sup.1 and R.sup.2 each represent Cl, then R.sup.3 does not represent CH.sub.2 CO.sub.2 H, CH.sub.2 CO.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 or 5-tetrazolylmethyl; and pharmaceutically acceptable salts thereof.The compounds are indicated as anxiolytics, anticonvulsants, analgesics and neuroprotectives.

    Abstract translation: 本发明提供式I化合物，其中R 1和R 2独立地表示C 1或C 1-6烷基; R3表示XCO2R4，XCONHSO2R5，YNHSO2R5或XR6; R 4表示H或C 1-6烷基（任选被芳基或杂环基取代）; R5代表CF3，杂环基或C1-6烷基（任选被芳基或杂环基取代）; R6表示酸性杂环; X表示C 1-6烷基双基（任选被芳基或杂环基取代）; Y代表二价C 2-6烷基（任选被芳基或杂环基取代）; 条件是当R 1和R 2各自表示Cl时，则R 3不表示CH 2 CO 2 H，CH 2 CO 2 CH 3，CH 2 CH 2 NHSO 2 CF 3或5-四唑基甲基; 及其药学上可接受的盐。 化合物表示为抗焦虑药，抗惊厥药，止痛剂和神经保护剂。

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