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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

    Piperidone tachykinin antagonists
    3.
    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
    4.
    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。

    Phenoxyphenylheterocyclyl derivatives as SSRIs
    7.
    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

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

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

    IPC: A61K3142

    CPC classification number: C07D207/09 ,  A61K31/40 ,  C07D207/08

    Abstract: 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.

    Abstract translation: 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

    N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
    10.
    发明授权
    N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase 失效
    N-苯丙基环戊基取代的戊二酰胺衍生物作为中性内肽酶的抑制剂

    公开(公告)号：US06660756B2

    公开(公告)日：2003-12-09

    申请号：US10096218

    申请日：2002-03-12

    Applicant: Stephen Challenger ,  Andrew Simon Cook ,  Adam Thomas Gillmore ,  Donald Stuart Middleton ,  David Cameron Pryde ,  Alan Stobie

    Inventor： Stephen Challenger ,  Andrew Simon Cook ,  Adam Thomas Gillmore ,  Donald Stuart Middleton ,  David Cameron Pryde ,  Alan Stobie

    IPC: A61K3144

    CPC classification number: C07D319/18 ,  C07C235/82 ,  C07C255/60 ,  C07C323/40 ,  C07C2601/08 ,  C07C2602/08 ,  C07D213/40 ,  C07D215/12 ,  C07D231/56 ,  C07D307/81 ,  C07D311/74 ,  C07D317/62

    Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

    Abstract translation: 本发明涉及用于治疗例如性功能障碍的式（I）化合物，其中R 1是任选取代的C 1-6烷基，任选取代的碳环基，任选取代的杂环基，氢，C 1-6烷氧基，-NR 2 R 3或-NR 4 SO 2 R 5; X是连接 - （CH 2）n - 或 - （CH 2）q -O-（其中Y连接到氧上）; 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基（C 1-3烷基）; C 3-7环烷基; 碳环基 杂环基 或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基，各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。

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