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    Condensed indoline derivatives and their use as 5-HT, in particular 5-HT2C, receptor ligands
    1.
    发明授权
    Condensed indoline derivatives and their use as 5-HT, in particular 5-HT2C, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5-HT，特别是5-HT 2C受体配体

    公开(公告)号：US07323473B2

    公开(公告)日：2008-01-29

    申请号：US11637042

    申请日：2006-12-12

    申请人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    发明人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    IPC分类号： A61K31/437 ,  C07D471/14

    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, alkylsulfonyl, 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，烷基磺酰基，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
    4.
    发明授权
    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：US07323486B2

    公开(公告)日：2008-01-29

    申请号：US11637036

    申请日：2006-12-12

    申请人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    发明人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    IPC分类号： A61K31/407 ,  C07D491/048 ,  C07D495/04

    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
    5.
    发明授权
    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：US07173056B2

    公开(公告)日：2007-02-06

    申请号：US11117488

    申请日：2005-04-29

    申请人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    发明人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    IPC分类号： A61K31/407 ,  C07D209/56

    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 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
    8.
    发明授权
    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：US07323487B2

    公开(公告)日：2008-01-29

    申请号：US11637082

    申请日：2006-12-12

    申请人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    发明人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    IPC分类号： A61K31/407 ,  C07D209/56

    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
    9.
    发明授权
    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：US07166613B2

    公开(公告)日：2007-01-23

    申请号：US11117459

    申请日：2005-04-29

    申请人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    发明人： Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  David Reginald Adams

    IPC分类号： A61K31/437 ,  C07D471/14

    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。

    Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
    10.
    发明授权
    Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application 失效
    吲哚衍生物制备方法，含有它们的药物组合物及其药物应用

    公开(公告)号：US06706750B1

    公开(公告)日：2004-03-16

    申请号：US10009568

    申请日：2002-03-11

    申请人： Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  Ian Anthony Cliffe ,  David Reginald Adams ,  Nathaniel Julius Monck

    发明人： Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  Ian Anthony Cliffe ,  David Reginald Adams ,  Nathaniel Julius Monck

    IPC分类号： A61K3140

    CPC分类号： C07D495/04 ,  C07D209/94

    摘要： A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, 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; gastrointestinial 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独立地选自氢和烷基; R3是烷基; R4，R6和R7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，烷基磺酰基，烷基磺酰基，硝基，腈，碳 - 烷氧基，碳 - 芳氧基和羧基; R5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，烷基亚磺酰基，烷基磺酰基，硝基，腈，碳 - 烷氧基，碳 - 芳氧基和羧基; A是5或6元部分不饱和或芳族杂环或5或6元部分不饱和碳环，其中如果A是6元部分不饱和的碳环，则R 4至R 7中的至少一个 >不是氢，和其药学上可接受的盐，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，例如用于治疗中枢性疾病 神经系统; 损害中枢神经系统; 心血管疾病; 胃肠疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。