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    Morpholine dopamine agonists
    1.
    发明授权
    Morpholine dopamine agonists 失效
    吗啉多巴胺激动剂

    公开(公告)号：US07576081B2

    公开(公告)日：2009-08-18

    申请号：US11425030

    申请日：2006-06-19

    Applicant: Charlotte Moira Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    Inventor： Charlotte Moira Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    IPC: A61K31/5377 ,  C07D413/04

    CPC classification number: C07D265/30 ,  C07D413/04

    Abstract: The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and (C1-C6)alkyl, R2 is selected from H and (C1-C6)alkyl, X is selected from H, HO, C(O)NH2, NH2 Y is selected from H, HO, NH2, Br, Cl and F Z is selected from H, HO F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (Ia) or (Ib), when A is C—X, B is C—Y, R1 is H or (C1-C6)alkyl and R2 is H or (C1-C6)alkyl at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C—X and B is C—Y, Y is H, Z is H, R1 is H and R2 is H, then X cannot be OH; these compounds are useful as a medicament.

    Abstract translation: 本发明提供式（I），（Ia）和（Ib）化合物，其中A选自CX和N，B选自CY和N，R 1选自H和（C 1 -C 6）烷基， R2选自H和（C1-C6）烷基，X选自H，HO，C（O）NH2，NH2Y选自H，HO，NH2，Br，Cl和FZ选自H，HOF ，CONH2和CN; 其药学上可接受的盐，溶剂合物和前药; 条件是：对于式（I），（Ia）或（Ib）的化合物，当A是CX时，B是CY，R 1是H或（C 1 -C 6）烷基，R 2是H或（C 1 -C 6） ）烷基，X，Y和Z中的至少一个必须是OH; 对于式（I）化合物，当A为C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

    New Amino Derivatives and Their Use as Pharmaceuticals
    3.
    发明申请
    New Amino Derivatives and Their Use as Pharmaceuticals 审中-公开
    新型氨基衍生物及其作为药物的用途

    公开(公告)号：US20090005354A1

    公开(公告)日：2009-01-01

    申请号：US12208148

    申请日：2008-09-10

    Applicant: Charlotte Moira Norfor Allerton ,  Andrew Simon Cook ,  David Hepworth ,  Duncan Charles Miller

    Inventor： Charlotte Moira Norfor Allerton ,  Andrew Simon Cook ,  David Hepworth ,  Duncan Charles Miller

    IPC: A61K31/397 ,  C07D413/02 ,  A61K31/5377 ,  A61P25/00 ,  A61P15/00 ,  C07D401/02

    CPC classification number: C07D413/04 ,  C07D401/04

    Abstract: The present invention provides for compounds of formula (I): which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.

    Abstract translation: 本发明提供了式（I）化合物：其是一类多巴胺激动剂，更特别的是在D2上对D3具有选择性的一类激动剂。 这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮 无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。 本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。 这些化合物也可用于治疗神经精神障碍和神经变性疾病。

    MORPHOLINE DOPAMINE AGONISTS
    6.
    发明申请
    MORPHOLINE DOPAMINE AGONISTS 有权
    吗啡多巴胺激动剂

    公开(公告)号：US20090270384A1

    公开(公告)日：2009-10-29

    申请号：US12496864

    申请日：2009-07-02

    Applicant: Charlotte Moria Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    Inventor： Charlotte Moria Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    IPC: A61K31/5375 ,  C07D265/30

    CPC classification number: C07D265/30 ,  C07D413/04

    Abstract: The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and (C1-C6)alkyl, R2 is selected from H and (C1-C6)alkyl, X is selected from H, HO, C(O)NH2, NH2 Y is selected from H, HO, NH2, Br, Cl and F Z is selected from H, HO, F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (Ia) or (Ib), when A is C—X, B is C—Y, R1 is H or (C1-C6)alkyl and R2 is H or (C1-C6)alkyl at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C—X and B is C—Y, Y is H, Z is H, R1 is H and R2 is H, then X cannot be OH; these compounds are useful as a medicament.

    Abstract translation: 本发明提供式（I），（Ia）和（Ib）化合物，其中A选自CX和N，B选自CY和N，R 1选自H和（C 1 -C 6）烷基， R2选自H和（C1-C6）烷基，X选自H，HO，C（O）NH2，NH2Y选自H，HO，NH2，Br，Cl和FZ选自H，HO， F，CONH 2和CN; 其药学上可接受的盐，溶剂合物和前药; 条件是：对于式（I），（Ia）或（Ib）的化合物，当A是CX时，B是CY，R 1是H或（C 1 -C 6）烷基，R 2是H或（C 1 -C 6） ）烷基，X，Y和Z中的至少一个必须是OH; 对于式（I）化合物，当A为C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

    New aminopyridine derivatives and their use as pharmaceuticals
    7.
    发明申请
    New aminopyridine derivatives and their use as pharmaceuticals 审中-公开
    新的氨基吡啶衍生物及其作为药物的用途

    公开(公告)号：US20050288270A1

    公开(公告)日：2005-12-29

    申请号：US11138708

    申请日：2005-05-26

    Applicant: Charlotte Moira Norfor Allerton ,  Andrew Simon Cook ,  David Hepworth ,  Duncan Charles Miller

    Inventor： Charlotte Moira Norfor Allerton ,  Andrew Simon Cook ,  David Hepworth ,  Duncan Charles Miller

    IPC: A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/541 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

    CPC classification number: C07D413/04 ,  C07D401/04

    Abstract: The present invention provides for compounds of formula (I): which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.

    Abstract translation: 本发明提供了式（I）化合物：其是一类多巴胺激动剂，更特别的是在D2上对D3具有选择性的一类激动剂。 这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮 无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。 本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。 这些化合物也可用于治疗神经精神障碍和神经变性疾病。

    Morpholine dopamine agonists
    9.
    发明授权
    Morpholine dopamine agonists 有权
    吗啉多巴胺激动剂

    公开(公告)号：US07902188B2

    公开(公告)日：2011-03-08

    申请号：US12496864

    申请日：2009-07-02

    Applicant: Charlotte Moira Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    Inventor： Charlotte Moira Norfor Allerton ,  Andrew Douglas Baxter ,  Andrew Simon Cook ,  David Hepworth ,  Stephen Kwok-Fung Wong

    IPC: A61K31/5375 ,  C07D265/30

    CPC classification number: C07D265/30 ,  C07D413/04

    Abstract: The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and (C1-C6)alkyl, R2 is selected from H and (C1-C6)alkyl, X is selected from H, HO, C(O)NH2, NH2 Y is selected from H, HO, NH2, Br, Cl and F Z is selected from H, HO, F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (Ia) or (Ib), when A is C—X, B is C—Y, R1 is H or (C1-C6)alkyl and R2 is H or (C1-C6)alkyl at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C—X and B is C—Y, Y is H, Z is H, R1 is H and R2 is H, then X cannot be OH; these compounds are useful as a medicament.

    Abstract translation: 本发明提供式（I），（Ia）和（Ib）的化合物，其中A选自C-X和N，B选自C-Y和N，R 1选自H和（C1- C6）烷基，R2选自H和（C1-C6）烷基，X选自H，HO，C（O）NH 2，NH 2 Y选自H，HO，NH 2，Br，Cl和FZ选自 H，HO，F，CONH 2和CN; 其药学上可接受的盐，溶剂合物和前药; 条件是：对于式（I），（Ia）或（Ib）的化合物，当A是C-X时，B是C-Y，R1是H或（C1-C6）烷基，R2是H或 （C1-C6）烷基，X，Y和Z中的至少一个必须是OH; 对于式（I）化合物，当A为C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

    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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