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    Novel compounds
    1.
    发明申请
    Novel compounds 失效
    新型化合物

    公开(公告)号：US20060111429A1

    公开(公告)日：2006-05-25

    申请号：US11280128

    申请日：2005-11-15

    申请人： Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    发明人： Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC分类号： A61K31/40 ,  C07D207/10

    CPC分类号： C07D207/14 ,  C07D405/12

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is 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; provided that at least one of R1, R2 and R3 are other than H. 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）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5或6元碳环基团或第二个4-，5-或 其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性 和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

    N-Pyrrolidin-3YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors
    2.
    发明申请
    N-Pyrrolidin-3YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors 审中-公开

    公开(公告)号：US20090239928A1

    公开(公告)日：2009-09-24

    申请号：US11721352

    申请日：2005-12-02

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    IPC分类号： A61K31/40 ,  C07D207/14 ,  A61P13/00

    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(A)D, 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 C1-8allkyl, C1-8alkoxy, OH, halo, CF3, OCHF2, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; R2 represents aryl1 or het1, each of which is substituted by at least one substituent independently selected from B, provided that when R2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl2, het2, Oaryl2, Ohet2, Sarl2, Shet2, SC1-6alkyl, halogen, CHF2, OCHF2, CF2CF3, CH2CF3, CF2CH3, aryl2-C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, C3-6cycloalkylC1-4alkoxy, C3-6cycloalkyl-O—C1-4 alkyl, C3-6cycloalkyl-C1-4alkoxy-C1-4alkyl, OC3-6cycloalkyl, SC3-6cycloalkyl; wherein the aryl2 and het2 groups are optionally substituted by at least one group selected from C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, OC3-6cycloalkyl, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hydroxyC1$alkyl, C1-4alkoxy-C1-4alkyl, SC1-6alkyl and SCF3; 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 centre; R3 is H, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, aryl3, het3, aryl3-C1-4alkyl or het3-C1-4alkyl, wherein the C3-8cycloalkyl, aryl3 or het3 groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, CN, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; at each occurrence aryl, aryl1, aryl2 and aryl3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het1 represents an aromatic 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het2, and het3 independently represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, O or S heteroatom.

    Amides useful as monoamine re-uptake inhibitors
    3.
    发明授权
    Amides useful as monoamine re-uptake inhibitors 失效
    用作单胺再吸收抑制剂的酰胺

    公开(公告)号：US07122683B2

    公开(公告)日：2006-10-17

    申请号：US11280128

    申请日：2005-11-15

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

    IPC分类号： C07D207/14

    CPC分类号： C07D207/14 ,  C07D405/12

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is 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; provided that at least one of R1, R2 and R3 are other than H. 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）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5或6元碳环基团或第二个4-，5-或 其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性 和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

    N-Pyrrolidin-3-YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors
    4.
    发明申请
    N-Pyrrolidin-3-YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors 审中-公开

    公开(公告)号：US20090239929A1

    公开(公告)日：2009-09-24

    申请号：US11721359

    申请日：2005-12-02

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    IPC分类号： A61K31/40 ,  C07D207/14 ,  A61P13/00 ,  A61P25/24 ,  A61P25/00 ,  A61P15/12

    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(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; aryl represents phenyl, naphthyl, anthracyl or phenanthryl; het represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R2 is aryl1 or het1, each optionally substituted; 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 centre; R3 is (CH2)aE, wherein a is 0, 1 or 2 and E is a group selected from: Formula (i) wherein: X is O, S, NR12, (CH2)v or a bond; b is 1, 2, 3 or 4; c is 1, 2 or 3; v is 1 or 2; R10 and 11 are each independently H or C1-4 alkyl; and R12 is H, 1-6 alkyl, C(O)C1-6 alkyl, SO2—C1-6alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula (iii) wherein: d is 1, 2, 3 or 4; a is 1, 2 or 3; f is 1 or 2; and R30 is H or C1-4alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: g is 0, 1, 2 or 3; J is NR40; and R40 is C(O)C1-6 alkyl, S02-C1-6alkyl; Formula (v) wherein: h is 0, 1, 2 or 3; and R50 is H, C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; Formula (vi) —CH(cyclopropane)2; Formula (vii) C1-6alkyl, substituted by at least one substituent; and Formula (viii) C3-8cycloalkyl-C1-6alkyl; wherein the C1-6alkyl moiety is substituted at any point other than at the junction with the C3-8cycloalkyl moiety, by at least one substituent. The compounds exhibit activity as both serotonin and/or noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    Triazole derivatives which inhibit vasopressin antagonistic activity
    7.
    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

    申请人： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    发明人： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    IPC分类号： A61K31/535

    CPC分类号： C07D401/14

    摘要： 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.

    摘要翻译： 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。

    Triazole derivatives which inhibit vasopressin antagonistic activity
    8.
    发明授权
    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：US07449462B2

    公开(公告)日：2008-11-11

    申请号：US10588876

    申请日：2005-01-11

    申请人： Justin S. Bryans ,  Patrick S. Johnson ,  Thomas Ryckmans ,  Alan Stobie

    发明人： Justin S. Bryans ,  Patrick S. Johnson ,  Thomas Ryckmans ,  Alan Stobie

    IPC分类号： C07D401/14 ,  A61K31/5517

    CPC分类号： C07D401/14

    摘要： 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.

    摘要翻译： 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。

    3-Heterocyclyl-4-Phenyl-Triazole Derivatives as Inhibitors of the Vasopressin Via Receptor
    10.
    发明申请
    3-Heterocyclyl-4-Phenyl-Triazole Derivatives as Inhibitors of the Vasopressin Via Receptor 审中-公开
    3-杂环基-4-苯基 - 三唑衍生物作为加压素通过受体的抑制剂

    公开(公告)号：US20070225333A1

    公开(公告)日：2007-09-27

    申请号：US10598840

    申请日：2005-04-18

    申请人： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    发明人： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04

    CPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

    摘要： Compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein R represents C1-6alkyl (optionally substituted by C1-6alkyloxy or Het) or C1-6alkyloxy; R1 and R2 independently represent hydrogen, halo or C1-6alkyl, ring A represents Het1; X represents O or NR3; R3 represents hydrogen or C1-6alkyl; ring B represents a phenyl group or Het2, either of which may be optionally substituted with one or more groups selected from halo, CN, C1-6alkyloxy, CF3, C1-6alkyl, NH2 and NO2; Het and Het1 independently represent a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic group comprising either (a) 1 to 4 nitrogen atoms, (b) one oxygen or one sulphur atom or (c) 1 oxygen atom or 1 sulphur atoms and 1 or 2 nitrogen atoms are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis) mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labour and Raynaud's disease.

    摘要翻译： 或式（I）化合物或其药学上可接受的衍生物，其中R表示C 1-6烷基（任选被C 1-6烷氧基或Het取代）或C 1-6烷基氧基; R 1和R 2独立地表示氢，卤素或C 1-6烷基，环A表示Het 1〜 ; X表示O或NR 3; R 3表示氢或C 1-6烷基; 环B表示苯基或Het 2，其中任一个可以任选被一个或多个选自卤素，CN，C 1-6烷氧基，CF 3， C 1〜C 6烷基，NH 2和NO 2; Het和Het 1独立地表示5-或6-元饱和，部分不饱和或芳族杂环基，其包含（a）1-4个氮原子，（b）一个氧或一个硫原子或（ c）1个氧原子或1个硫原子和1或2个氮原子可用于治疗焦虑症，心血管疾病（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（原发性和继发性），子宫内膜异位症，呕吐 包括运动病），子宫内生长迟缓，炎症（包括类风湿性关节炎）手段，先兆子痫，早泄，早产（早产）劳动和雷诺病。