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    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands
    3.
    发明申请
    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5HT，特别是5HT2C受体配体

    公开(公告)号：US20070099980A1

    公开(公告)日：2007-05-03

    申请号：US11637036

    申请日：2006-12-12

    申请人： Jonathan Roffey ,  James Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    发明人： Jonathan Roffey ,  James Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    IPC分类号： A61K31/407

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4745 ,  C07D209/60 ,  C07D209/70 ,  C07D209/90 ,  C07D471/06 ,  C07D491/04 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中R 1和R 2各自独立地选自氢和烷基; R 3是烷基; R 4和R 5选自氢和烷基; R 6和R 7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚砜基，硝基，腈 ，碳 - 烷氧基，碳 - 芳氧基和羧基; 并且A是任选地含有一个或多个杂原子的5-或6-元环，其中除了环A稠合的苯环的不饱和碳原子之外的环A的原子是饱和或不饱和的， 可接受的盐，加成化合物和前药; 以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。

    Condensed indoline derivatives and their use as 5HT , in particular 5hHT2c, receptor ligands
    5.
    发明申请
    Condensed indoline derivatives and their use as 5HT , in particular 5hHT2c, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5HT，特别是5hHT2c受体配体

    公开(公告)号：US20070105889A1

    公开(公告)日：2007-05-10

    申请号：US11637042

    申请日：2006-12-12

    申请人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    发明人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    IPC分类号： A61K31/4745 ,  A61K31/403

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4745 ,  C07D209/60 ,  C07D209/70 ,  C07D209/90 ,  C07D471/06 ,  C07D491/04 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中R 1和R 2各自独立地选自氢和烷基; R 3是烷基; R 4和R 5选自氢和烷基; R 6和R 7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚砜基，硝基，腈 ，碳 - 烷氧基，碳 - 芳氧基和羧基; 并且A是任选地含有一个或多个杂原子的5-或6-元环，其中除了环A稠合的苯环的不饱和碳原子之外的环A的原子是饱和或不饱和的， 可接受的盐，加成化合物和前药; 以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。

    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands
    6.
    发明申请
    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5HT，特别是5HT2C受体配体

    公开(公告)号：US20070099981A1

    公开(公告)日：2007-05-03

    申请号：US11637082

    申请日：2006-12-12

    申请人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn

    发明人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn

    IPC分类号： A61K31/403

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4745 ,  C07D209/60 ,  C07D209/70 ,  C07D209/90 ,  C07D471/06 ,  C07D491/04 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2c receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中R 1和R 2各自独立地选自氢和烷基; R 3是烷基; R 4和R 5选自氢和烷基; R 6和R 7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚砜基，硝基，腈 ，碳 - 烷氧基，碳 - 芳氧基和羧基; 并且A是任选地含有一个或多个杂原子的5-或6-元环，其中除了环A稠合的苯环的不饱和碳原子之外的环A的原子是饱和或不饱和的， 其可接受的盐，加成化合物和前药; 以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。

    AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS
    7.
    发明申请
    AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS 审中-公开

    公开(公告)号：US20100204224A1

    公开(公告)日：2010-08-12

    申请号：US11993557

    申请日：2006-07-07

    申请人： Richard Hamlyn ,  Glyn Addison ,  Christopher Geoffrey Earnshaw ,  Harry Finch ,  Mike Huckstep ,  Rosemary Lynch ,  Sarah Mellor

    发明人： Richard Hamlyn ,  Glyn Addison ,  Christopher Geoffrey Earnshaw ,  Harry Finch ,  Mike Huckstep ,  Rosemary Lynch ,  Sarah Mellor

    IPC分类号： A61K31/5377 ,  C07D471/08 ,  A61K31/4995 ,  C07D487/10 ,  A61K31/407 ,  C07D487/04 ,  A61P13/10 ,  A61P25/00

    CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/10

    摘要： Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents; wherein (1) represents (A), (B) or (C); R1 represents: (a) -L-A or L′-A′ wherein L represents a bond or a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, A represents a phenyl, 5- to 10-membered heteroaryl, C3-C6 carbocyclyl or 5- to 10 membered heterocyclyl group, L′ represents a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, and A′ represents -Het-A or —X-A wherein Het represents —O—, —S— or NR′, and X represents —CO—, —SO—, SO2—, —CO—O—, CO—S, CONR′, —O—CO—, —S—CO— or NR′—CO—, wherein R′ represents hydrogen or C1-C6 alkyl; (b) -L-A-A′ or -L-A-L-A wherein A′ is as defined above, each A is the same or different and is as defined above and each L is the same or different and is as defined above; (c) -A-Z-A wherein Z is -Het-L′, —X-L′, -L′-Het- or L′-X, wherein Het, L′ and X are as defined above and each A is the same or different and is as defined above; (d) -A-Het-Y or -A-X—Y wherein is [L′-Het]n-L′, [L′-Het]n-L′, -[L′-Het]n-A, -L′-B-L′, -L′-B-A or -A-L-A wherein n is from 1 to 4 and B is —X—, —NR′—CO—NR′, —O—CO—NR′— or —NR′—CO—O, and wherein X and L are as defined above, each A is the same or different and is as defined above, each L′ is the same or different and is as defined above, each R′ is the same or different and is as defined above and each Het is the same or different and is as defined above; or (e) -L-CR(A)(A′) or L-CR(A)(L-A) wherein R is hydrogen or C1-C4 alkyl, A′ is as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above; R2 represents -L-A-, L′-A′, -L-A-A′ or L-A-L-A wherein L′ and A′ are as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above J represents —NR3—, —O— or a direct bond wherein R3 represent s hydrogen C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; p is an integer from 1 to 3; q is 1 or 2; and one of E and E′ is —CH2— and the other is a direct bond.

    ANTAGONISTS OF SNS SODIUM CHANNELS
    8.
    发明申请
    ANTAGONISTS OF SNS SODIUM CHANNELS 审中-公开

    公开(公告)号：US20100105651A1

    公开(公告)日：2010-04-29

    申请号：US11993515

    申请日：2006-07-07

    申请人： Richard Hamlyn ,  David Callis ,  Christopher Geoffrey Earnshaw ,  Harry Finch ,  Mike Huckstep ,  Rosemary Lynch ,  Sarah Mellor

    发明人： Richard Hamlyn ,  David Callis ,  Christopher Geoffrey Earnshaw ,  Harry Finch ,  Mike Huckstep ,  Rosemary Lynch ,  Sarah Mellor

    IPC分类号： A61K31/397 ,  C07D205/04 ,  C07D401/02 ,  A61P1/00 ,  A61P13/10 ,  A61P25/00

    CPC分类号： A61K31/397

    摘要： Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents, formula (I): R1 represents: (a) -L-A or -L′-A′ wherein L represents a bond or a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, A represents a phenyl, 5- to 10-membered heteroaryl, C3-C6 carbocyclyl or 5- to 10-membered heterocyclyl group, L′ represents a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, and A′ represents -Het-A or —X-A wherein Het represents —O—, —S— or —NR1—, and X represents —CO—, —SO—, —SO2—, —CO—O—, —CO—S—, —CONR1—, —O—CO—, —S—CO— or —NR1—CO—, wherein R1 represents hydrogen or C1-C6 alkyl; (b) -L-CR(A)(A′) or -L-CR(A)(L-A) wherein R is hydrogen or C1-C4 alkyl, A′ is as defined above, each L is the same or different and is as defined above and each A′ is the same or different and is as defined above; (c) -L-A-A′ or -L-A-L-A wherein A′ and L are as defined above and each A is the same or different and is as defined above; or (d) -A-Z-A wherein Z is -Het-L′-, —X-L′-, -L′-Het- or -L′-X—, wherein Het, L′ and X are as defined above and each A is the same or different and is as defined above; J represents —NRS—, —O— or a direct bond; R5 represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; R4 is represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; and either R represents -L-A, -L-A′, -L-A-A′, -L-A-L-A, -L-CR(A)(L-A), -L-CR(A)(A′) or -L-CR(A)(L″) wherein L″ is -Het-L′, —CONH2 or —CO2H, and wherein A′, Het, X and R are as defined above, each L is the same or different and is as defined above, each A is the same or different and is as defined above and R3 represents hydrogen, C1-C6 alkyl C2-C6 alkynyl or (CO)-L′, wherein L is as defined above or R2 and R3 form, together with the nitrogen to which they are attached, a 5- to 10-membered heteroaryl or 5- to 10-membered heterocyclyl ring.