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1. 发明授权

US07323473B2 Condensed indoline derivatives and their use as 5-HT, in particular 5-HT2C, receptor ligands 失效
标题翻译：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。

2. 发明申请

US20080090858A1 Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 审中-公开
公开(公告)号：US20080090858A1
公开(公告)日：2008-04-17
申请号：US11987774
申请日：2007-12-04
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： A61K31/404 , A61K31/437 , A61P1/00 , A61P25/00 , A61P3/10 , A61P9/00
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.

3. 发明授权

US07098337B2 1,2,3,4,9,9a-hexahydro-2,4a,5-triaza-fluorene and 1,2,3,4-tetrahydro-2,4a,5-triaza-fluorene derivatives 失效
标题翻译： 1,2,3,4,9,9a-六氢-2,4a，5-三氮杂芴和1,2,3,4-四氢-2,4a，5-三唑 - 芴衍生物
公开(公告)号：US07098337B2
公开(公告)日：2006-08-29
申请号：US10350616
申请日：2003-01-24
申请人： David Reginald Adams , Jonathan Mark Bentley , Toby Jonathan Blench , Paul Hebeisen , Nathaniel Julius Thomas Monck , Hans Richter , Stephan Roever , Jonathan Richard Anthony Roffey , Sven Taylor
发明人： David Reginald Adams , Jonathan Mark Bentley , Toby Jonathan Blench , Paul Hebeisen , Nathaniel Julius Thomas Monck , Hans Richter , Stephan Roever , Jonathan Richard Anthony Roffey , Sven Taylor
IPC分类号： C07D471/14 , A61K31/4985 , A61P3/04
CPC分类号： C07D471/14
摘要： The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，溶剂化物和酯。这些化合物可用于制备用于治疗或预防中枢神经系统疾病，中枢神经系统损害，心血管疾病，胃肠道疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物组合物。

4. 发明申请

US20050197380A1 Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
公开(公告)号：US20050197380A1
公开(公告)日：2005-09-08
申请号：US11117460
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： 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 , C07D491/02 , C07D498/02
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.

5. 发明授权

US06380238B1 Indoline derivatives as 5-HT2B and or 5-HTC receptor ligands 失效
标题翻译：二氢吲哚衍生物作为5-HT2B和/或5-HTC受体配体
公开(公告)号：US06380238B1
公开(公告)日：2002-04-30
申请号：US09786154
申请日：2001-03-01
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , David Bebbington , Nathaniel Julius Monck , Claire Elizabeth Dawson , Robert Mark Pratt , Ashley Roger George
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , David Bebbington , Nathaniel Julius Monck , Claire Elizabeth Dawson , Robert Mark Pratt , Ashley Roger George
IPC分类号： C07D20908
CPC分类号： C07D401/04 , C07D209/08 , C07D401/12 , C07D409/04 , C07D409/12
摘要： For use in therapy a chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4 to R7 is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for 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 especially for the treatment of obesity; chemical compounds of formula (I) other than compounds wherein R7 is hydroxy.
摘要翻译：用于治疗式（I）化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，杂环基，烷氧基，芳氧基，烷硫基，芳硫基，烷基磺酰基，烷基磺酰基，芳基磺酰基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，甲醛，，氨基羰基，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基，其中R4至R7中的至少一个是氢以外的取代基，及其药学上可接受的盐和前药，特别是用于治疗中枢神经系统; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症，睡眠呼吸暂停，特别是治疗肥胖症; 式（I）的化合物，其中R 7是羟基的化合物。

6. 发明授权

US07323486B2 Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
标题翻译：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。

7. 发明授权

US07173056B2 Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
标题翻译：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。

8. 发明授权

US06962939B1 Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
标题翻译：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：US06962939B1
公开(公告)日：2005-11-08
申请号：US10009567
申请日：2000-08-04
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： 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
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, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, 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，烷基亚磺酰基，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。

9. 发明授权

US06552062B1 Indazole derivatives with 5-HT2 receptor activity 失效
标题翻译：具有5-HT2受体活性的吲唑衍生物
公开(公告)号：US06552062B1
公开(公告)日：2003-04-22
申请号：US09763886
申请日：2001-02-28
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Ashley Roger George
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Ashley Roger George
IPC分类号： A61K31416
CPC分类号： C07D231/56
摘要： A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for 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至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，氨基，单烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，芳基磺酰基，烷基亚砜基，烷基磺酰基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基; 并且R 8选自烷基和烷氧基及其药学上可接受的盐和前药，及其在治疗中的用途，特别是用于治疗中枢神经系统疾病的用途; 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。

10. 发明授权

US06365598B1 Pyrroloquinolines for treatment of obesity 失效
标题翻译：吡咯喹啉类治疗肥胖症
公开(公告)号：US06365598B1
公开(公告)日：2002-04-02
申请号：US09786159
申请日：2001-03-01
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Corinna Dagmar Bodkin , Howard Langham Mansell , Ashley Roger George , Ian Anthony Cliffe
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Corinna Dagmar Bodkin , Howard Langham Mansell , Ashley Roger George , Ian Anthony Cliffe
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： A chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 is selected from hydrogen, alkyl, alkoxy, formyl and cyano; X1 is selected from N and C—R7; X2 is selected from N and C—R8; X3 is selected from N and C—R9; X4 is selected from N and C—R10; wherein at least one of X1, X2, X3 and X4 is N; and R5 to R10 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and the use thereof in therapy, particularly for 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.

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