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    NOVEL COMPOUNDS
    1.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    新型化合物

    公开(公告)号：US20080306123A1

    公开(公告)日：2008-12-11

    申请号：US12124755

    申请日：2008-05-21

    申请人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    发明人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    IPC分类号： A61K31/4468 ,  A61P13/00 ,  A61P29/00 ,  A61P15/00 ,  A61P25/24

    CPC分类号： C07D207/14

    摘要： 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.

    摘要翻译： 式（I）化合物及其药学上和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，het，芳基-C 1-4烷基或叔丁基 其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基 - C 1-6烷基和C 1-4烷基-S-C 1-4烷基; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1 -4-烷基-S-C 1-4烷基; R 3为C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个取代基取代 独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。 本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

    Compounds
    2.
    发明授权
    Compounds 失效

    公开(公告)号：US07378436B2

    公开(公告)日：2008-05-27

    申请号：US10872160

    申请日：2004-06-17

    申请人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    发明人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    IPC分类号： A61K31/40 ,  C07D295/10

    CPC分类号： C07D207/14

    摘要： 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.

    Diphenyl ether compounds useful in therapy
    6.
    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

    申请人： Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    发明人： Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    IPC分类号： C07C21758

    CPC分类号： 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

    摘要： 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.

    摘要翻译： 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

    Phenoxybenzylamine derivatives as SSRIs
    7.
    发明授权
    Phenoxybenzylamine derivatives as SSRIs 失效
    苯氧基苄胺衍生物作为SSRIs

    公开(公告)号：US06610747B2

    公开(公告)日：2003-08-26

    申请号：US09941177

    申请日：2001-08-27

    申请人： Mavis Diane Adam ,  Mark David Andrews ,  Mark Leonard Elliott ,  Geoffrey Edward Gymer ,  David Hepworth ,  Harry Ralph Howard, Jr. ,  Donald Stuart Middleton ,  Alan Stobie

    发明人： Mavis Diane Adam ,  Mark David Andrews ,  Mark Leonard Elliott ,  Geoffrey Edward Gymer ,  David Hepworth ,  Harry Ralph Howard, Jr. ,  Donald Stuart Middleton ,  Alan Stobie

    IPC分类号： A61K3118

    CPC分类号： C07D277/62 ,  A61K31/135 ,  A61K31/343 ,  A61K31/381 ,  A61K31/39 ,  A61K31/47 ,  C07C311/08 ,  C07C323/20 ,  C07C2602/08 ,  C07D215/20 ,  C07D239/74 ,  C07D307/87 ,  C07D327/06 ,  C07D333/54 ,  C07D333/72

    摘要： A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; 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; 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.

    摘要翻译： 通式（I）的化合物，其中R 1和R 2是H，C 1 -C 6烷基或（CH 2）d（C 3 -C 6环烷基），其中d = 0,1,2或3; 或R 1和R 2与它们所连接的氮一起形成氮杂环丁烷环; Z或Y是-SR 3，另一个Z或Y是卤素或-R 3; 其中R 3是任选被氟取代的C 1 -C 4烷基; 除了R3不是CF3; 或Z和Y连接，使得与互连原子一起形成稠合的5至7元碳环或杂环，并且其中当Z和Y除碳原子之外形成杂环时，连接 含有一个或两个独立地选自氧，硫和氮的杂原子; 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 ; 或含有1,2或3个选自N，S和O的杂原子的5-或6-元杂环，任选被一个或多个R 13独立地取代; 其中R 13是羟基，C 1 -C 4烷氧基，F，C 1 -C 6烷基，卤代烷基，卤代烷氧基，-NH 2，-NH（C 1 -C 6烷基）或-N（C 1 -C 6烷基）2。

    Phenoxyphenylheterocyclyl derivatives as SSRIs
    8.
    发明授权
    Phenoxyphenylheterocyclyl derivatives as SSRIs 失效
    苯氧基苯杂环基衍生物作为SSRIs

    公开(公告)号：US06630504B2

    公开(公告)日：2003-10-07

    申请号：US09939475

    申请日：2001-08-24

    申请人： Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    发明人： Mark David Andrews ,  David Hepworth ,  Donald Stuart Middleton ,  Alan Stobie

    IPC分类号： A61K3142

    CPC分类号： C07D207/09 ,  A61K31/40 ,  C07D207/08

    摘要： The invention provides compounds of general formula (I) wherein R1 is H or C1-C6 alkyl; R2 and R3, together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R2 is attached) wherein a second heteroatom, if present, is selected from oxygen, nitrogen and sulfur, with the proviso that said ring cannot contain two adjacent heteroatoms; Z is CF3, OCF3, C1-C6alkylthio or C1-C6alkoxy; Y is hydrogen, halogen, —ORa, Ra or C1-C6alkylthio, and wherein Ra is C1-C4 alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; and Z and Y together do not form a fused phenyl ring; 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; 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.

    摘要翻译： 本发明提供通式（I）的化合物，其中R 1是H或C 1 -C 6烷基; R 2和R 3连同互连原子形成含有一个或两个杂原子（包括R 2连接的氮）的4至8元饱和环，其中如果存在第二杂原子， 选自氧，氮和硫，条件是所述环不能含有两个相邻的杂原子; Z是CF 3，OCF 3，C 1 -C 6烷硫基或C 1 -C 6烷氧基; Y是氢，卤素，-OR a，R 5c或C 1 -C 6烷硫基，并且其中R 5'是任选被氟原子取代的C 1 -C 4烷基; 或者当Z和Y连接到连接环A和B的醚键时，Z和Y被连接，使得Z和Y连接，使得与互连原子一起形成稠合的5至7元碳环或杂环， 可以是饱和的，不饱和的或芳族的，并且其中当Z和Y形成杂环时，除了碳原子之外，所述键含有一个或两个独立地选自氧，硫和氮的杂原子; 并且Z和Y一起不形成稠合的苯环; 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，CONR 6 R 7，SO 2 NR 6 R 7，SO 2 NHC（= O）R 6，OH，C 1-4烷氧基，NR 8 SO 2 R 9，NO 2，NR 6 R 11，CN，CO 2 R 10，CHO，SR 10，S（O）R 9或SO 2 R 10; 或含有1,2或3个选自N，S和O的杂原子的5-或6-元杂环，任选被一个或多个R 13独立地取代; 其中R 13是羟基，C 1 -C 4烷氧基，F，C 1 -C 6烷基，卤代烷基，卤代烷氧基，-NH 2，-NH（C 1 -C 6烷基）或-N（C