公开(公告)号：US20070173486A1

公开(公告)日：2007-07-26

申请号：US10554447

申请日：2004-04-29

申请人： James Davidson ,  Jonathan Bentley ,  Claire Dawson ,  Kerry Harrison ,  Howard Mansell ,  Alan Pither ,  Robert Pratt ,  Jonathan Roffey ,  Victoria Ruston

发明人： James Davidson ,  Jonathan Bentley ,  Claire Dawson ,  Kerry Harrison ,  Howard Mansell ,  Alan Pither ,  Robert Pratt ,  Jonathan Roffey ,  Victoria Ruston

IPC分类号： A61K31/397 ,  A61K31/551 ,  A61K31/454 ,  C07D403/02

CPC分类号： C07D401/12 ,  C07D205/04 ,  C07D211/46 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

摘要： Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR15, or NR16C(O)R17; Y is C═O, C═S, SO2, or (CR7R8); m=1 or 2; n=1 or 2; and p=1, 2, 3 or 4, R7 to R17 being as defined in the specification; wherein if —Y—R3 is —C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroaryl; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.

摘要翻译： 式（I）化合物及其在治疗中的用途，特别是用于治疗CB 1受体介导的病症，例如肥胖症，其中：R 1是芳基或 杂芳基; R 2是烷基，芳基或杂芳基; R 3是烷基，芳基，杂芳基，NR 9 R 10，或15，或NR 15， 16 C（O）R 17; Y是C-O，C-S，SO 2，或（CR 7 R 8）。 m = 1或2; n = 1或2; 和p = 1,2,3或4，R 7至R 17如说明书中所定义; 其中如果-Y-R 3为-C（O）NH（烷基），那么：R 1和/或R 2选自杂芳基; 和/或m和/或n为2; 和/或R 11和/或R 12是低级烷基或其药学上可接受的盐或前药。

公开(公告)号：US20070054891A1

公开(公告)日：2007-03-08

申请号：US10552575

申请日：2004-04-29

申请人： James Davidson ,  Claire Dawson ,  Kerry Harrison ,  Howard Mansell ,  Robert Pratt ,  Suhkjit Sohal ,  Victoria Ruston

发明人： James Davidson ,  Claire Dawson ,  Kerry Harrison ,  Howard Mansell ,  Robert Pratt ,  Suhkjit Sohal ,  Victoria Ruston

IPC分类号： A61K31/397 ,  C07D205/02

CPC分类号： C07D405/12 ,  C07D205/04 ,  C07D409/12

摘要： Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH-0-] group.

摘要翻译： 式（I）化合物及其在治疗中的用途，特别是用于治疗由CB1受体介导的病症，例如肥胖症：式（I）其中：R 1〜 和R 2独立地选自芳基; 和R 3是氢或烷基; 或其药学上可接受的盐或前药，其中R 1和R 2中的至少一个在其相邻位置具有非氢取代基相对于 与[-CH-O-]基团的连接点。

公开(公告)号：US20050187282A1

公开(公告)日：2005-08-25

申请号：US11117459

申请日：2005-04-29

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： C07D491/048 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4745 ,  A61P1/04 ,  A61P3/04 ,  A61P7/02 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D209/60 ,  C07D209/70 ,  C07D471/04 ,  C07D491/04 ,  C07D491/056 ,  C07D495/04 ,  A61K31/403 ,  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。

公开(公告)号：US20050192334A1

公开(公告)日：2005-09-01

申请号：US11117488

申请日：2005-04-29

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： C07D491/048 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4745 ,  A61P1/04 ,  A61P3/04 ,  A61P7/02 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D209/60 ,  C07D209/70 ,  C07D471/04 ,  C07D491/04 ,  C07D491/056 ,  C07D495/04 ,  A61K31/403 ,  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。

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。

公开(公告)号：US20080114018A1

公开(公告)日：2008-05-15

申请号：US11984735

申请日：2007-11-21

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： A61K31/437 ,  A61K31/403 ,  A61P9/00 ,  A61P25/00 ,  A61P3/00 ,  A61P15/00

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.

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。

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。