公开(公告)号：US07098338B2

公开(公告)日：2006-08-29

申请号：US10724844

申请日：2003-12-01

申请人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

发明人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

IPC分类号： C07D487/00 ,  A61K31/495

CPC分类号： C07D487/04 ,  A61K31/4985

摘要： This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1–6 carbon atoms; R′ is hydrogen, alkyl of 1–6 carbon atoms, acyl of 2–7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1–6 carbon atoms, alkoxy of 1–6 carbon atoms, halogen, trifluoroalkyl, or trifluoroalkoxy of 1–6 carbon atoms; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1–6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least two of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.

摘要翻译： 本发明提供式I化合物，其中R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R 1，R 2，R 3和R 4各自独立地为氢，烷基为1 -6个碳原子，1-6个碳原子的烷氧基，1-6个碳原子的卤素，三氟烷基或三氟烷氧基; X是CR 5 R 6或羰基; R 5和R 6各自独立地为氢或1-6个碳原子的烷基; 或其药学上可接受的盐，条件是R 1，R 2，R 3或R 3中的至少两个， 4不是氢; 其是可用于治疗涉及中枢神经系统的障碍（例如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖症，II型糖尿病）的5HT 2C受体激动剂 ，和癫痫。

公开(公告)号：US06706714B2

公开(公告)日：2004-03-16

申请号：US10244773

申请日：2002-09-16

申请人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

发明人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

IPC分类号： A61K31495

CPC分类号： C07D487/04 ,  A61K31/4985

摘要： This invention provides compounds of formula I, R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.

摘要翻译： 本发明提供式I化合物，R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R1，R2，R3， 和R 4各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，三氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺， 氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的三氟烷氧基，2-7个碳原子的酰基或芳酰基; X是CR5R6或羰基; R5和 R6各自独立地为氢或1-6个碳原子的烷基;或其药学上可接受的盐，条件是R 1，R 2，R 3或R 4中的至少一个不是氢;它们是5HT 2C受体激动剂，其可用于 治疗涉及中枢神经系统的障碍，如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，obesit y，II型糖尿病和癫痫。

公开(公告)号：US06777407B2

公开(公告)日：2004-08-17

申请号：US10016331

申请日：2001-11-02

申请人： Annmarie Louise Sabb ,  Robert Lewis Vogel ,  James Albert Nelson ,  Sharon Joy Rosenzweig-Lipson ,  Gregory Scott Welmaker ,  Joan Eileen Sabalski

发明人： Annmarie Louise Sabb ,  Robert Lewis Vogel ,  James Albert Nelson ,  Sharon Joy Rosenzweig-Lipson ,  Gregory Scott Welmaker ,  Joan Eileen Sabalski

IPC分类号： A61K3155

CPC分类号： C07D209/94 ,  A61K31/55 ,  C07D487/06

摘要： This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的化合物：其中：R 1是氢，-C（O）CH 3或1-6个碳原子的烷基; R 2和R 3各自独立地是氢，1-6个碳原子的烷基，环烷基，烷氧基 1-6个碳原子的-CH 2 OH，氟代烷基，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基 ，1-6个碳原子的氟烷氧基，2-7个碳原子的酰基，芳基或芳酰基; R4和R5各自独立地是氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素， 氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳的氟烷氧基 原子，2-7个碳原子的酰基或芳酰基; R6和R7各自独立地为氢，C1-C6烷基或环烷基;或其药学上可接受的盐，以及药物组合物conta 包括治疗强迫症，惊恐障碍，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓损伤的这些化合物和方法。

公开(公告)号：US06476032B2

公开(公告)日：2002-11-05

申请号：US09891593

申请日：2001-06-26

申请人： Sharon Joy Rosenzweig-Lipson ,  Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

发明人： Sharon Joy Rosenzweig-Lipson ,  Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  James Albert Nelson

IPC分类号： A61K314985

CPC分类号： C07D487/04 ,  A61K31/4985

摘要： This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.

摘要翻译： 本发明提供了式I化合物，其中R是氢或1-6个碳原子的烷基; R'是氢，1-6个碳原子的烷基，2-7个碳原子的酰基或芳酰基; R1，R2，R3， 和R 4各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，三氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺， 氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的三氟烷氧基，2-7个碳原子的酰基或芳酰基; X是CR5R6或羰基; R5和 R6各自独立地为氢或1-6个碳原子的烷基;或其药学上可接受的盐，条件是R 1，R 2，R 3或R 4中的至少一个不是氢;它们是5HT 2C受体激动剂，其可用于 治疗涉及中枢神经系统的障碍，例如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍， 肥胖，II型糖尿病和癫痫。

公开(公告)号：US06503900B2

公开(公告)日：2003-01-07

申请号：US10017738

申请日：2001-11-02

申请人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  Robert Lewis Vogel ,  Joan Eileen Sabalski

发明人： Annmarie Louise Sabb ,  Gregory Scott Welmaker ,  Robert Lewis Vogel ,  Joan Eileen Sabalski

IPC分类号： A61K3155

CPC分类号： C07D487/06

摘要： This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: wherein: R1 and R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, phenoyl or thiophenoyl; R3, R4, R5 and R6 are H, alkyl, cycloalkyl, alkoxy or cycloalkoxy; R7 is H or alkyl; R8 is H or alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods and pharmaceutical compositions utilizing them for the treatment or prevention of disorders such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的[1,4]二氮杂[6,7,1-jk]咔唑化合物：其中：R1和R2是H，烷基，烷氧基，卤素，氟化烷基，-CN，-NH-SO2-烷基 ，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，苯甲酰基或噻吩甲酰基; R3，R4，R5和R6是H，烷基，环烷基，烷氧基或环烷氧基; R7是H或烷基; R8是H或烷基; 虚线表示可选的双键; 或其药学上可接受的盐，以及利用它们用于治疗或预防诸如强迫症，抑郁症，焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓障碍的疾病的方法和药物组合物 线损伤。

公开(公告)号：US06784172B2

公开(公告)日：2004-08-31

申请号：US10016420

申请日：2001-11-02

申请人： Annmarie Louise Sabb ,  Robert Lewis Vogel ,  Madelene Miyoko Antane ,  Panolil Raveendranath ,  Sreenivasulu Megati ,  Michael David Smith ,  James Albert Nelson

发明人： Annmarie Louise Sabb ,  Robert Lewis Vogel ,  Madelene Miyoko Antane ,  Panolil Raveendranath ,  Sreenivasulu Megati ,  Michael David Smith ,  James Albert Nelson

IPC分类号： A61K3155

CPC分类号： C07D487/06

摘要： This invention provides processes for synthesizing compounds of formula I: wherein R is H or alkyl; R1, R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or aroyl; R3 and R4 are H, alkyl or cycloalkyl; the dashed line indicates an optional double bond; as well as intermediates and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明提供了合成式I化合物的方法：其中R是H或烷基; R1，R2是H，烷基，烷氧基，卤素，氟化烷基，-CN，烷基磺酰胺，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基或芳酰基。 R3和R4是H，烷基或环烷基; 虚线表示可选的双键; 以及其中间体和药学上可接受的盐。

公开(公告)号：US06858604B2

公开(公告)日：2005-02-22

申请号：US10016743

申请日：2001-11-02

申请人： Annmarie Louise Sabb ,  Robert Lewis Vogel

发明人： Annmarie Louise Sabb ,  Robert Lewis Vogel

IPC分类号： A61K31/551 ,  A61K31/5517 ,  A61P3/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D209/00 ,  C07D243/00 ,  C07D487/06 ,  A61K31/55

CPC分类号： C07D487/06

摘要： This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; R3 and R4 are each, independently, H, alkyl or cycloalkyl; R5 is H or alkyl; R6 is H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的化合物：其中R 1和R 2各自独立地为H，烷基，环烷基，-CH 2 - 环烷基，烷氧基，卤素，氟化烷基，-CN，-NH-SO 2 - 烷基，-SO 2 -NH- 烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基或苯甲酰基或噻吩甲酰基; R 3和R 4各自独立地为H，烷基或环烷基; R5是H或烷基; R6为H或; 虚线表示可选的双键; 或其药学上可接受的盐，以及利用这些化合物治疗或预防包括强迫症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖症，癫痫症， 和脊髓损伤。

公开(公告)号：US5770734A

公开(公告)日：1998-06-23

申请号：US902109

申请日：1992-06-22

申请人： Annmarie Louise Sabb

发明人： Annmarie Louise Sabb

IPC分类号： A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  C07D215/38 ,  C07D401/12 ,  C07D401/02

CPC分类号： C07D215/38 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  C07D401/12

摘要： R.sup.2 is H, alkyl of 1 to 6 carbon atoms, cyano, halo, nitro, amino or mono or dialkylamino in which the alkyl groups have 1 to 6 carbon atoms; R.sup.3 is H or alkyl of 1 to 6 carbon atoms; n is 1 to 5 and R.sup.4 and R.sup.5 taken with the nitrogen atom to which they are attached are polymethylene of 4 to 6 carbon atoms, morpholino, pyrrolidin-2-on-1-yl, or a piperazin-1-yl moiety in the 4-position of which is H, alkyl of 1 to 6 carbon atoms or unsubstituted or substituted pyrimidinyl, pyridinyl, or pyrazinyl wherein the substituents are alkyl of 1 to 6 carbon atoms, alkoxyl of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl and the pharmaceutically acceptable salts, hydrates and solvates thereof are M.sub.1 receptor agonists useful in treatment of dementias involving the cholinergic system.

摘要翻译： 其中R1是H，1-6个碳原子的烷基或环烷基; R2是H，具有1-6个碳原子的烷基，氰基，卤素，硝基，氨基或单或二烷基氨基，其中烷基具有1至6个碳原子; R3是H或1-6个碳原子的烷基; n为1至5，并且与其所连接的氮原子一起取代的R4和R5为4至6个碳原子的多亚甲基，吗啉代，吡咯烷-2-基-1-基或哌嗪-1-基部分 4位是H，1至6个碳原子的烷基或未取代或取代的嘧啶基，吡啶基或吡嗪基，其中取代基为1至6个碳原子的烷基，1至6个碳原子的烷氧基，卤素，氰基，硝基 或三氟甲基，其药学上可接受的盐，水合物和溶剂合物是可用于治疗涉及胆碱能系统的痴呆症的M1受体激动剂。

公开(公告)号：US5750522A

公开(公告)日：1998-05-12

申请号：US678851

申请日：1996-07-12

申请人： Annmarie Louise Sabb ,  William A. Kinney

发明人： Annmarie Louise Sabb ,  William A. Kinney

IPC分类号： C07D487/04 ,  C07D253/10 ,  A61K31/53

CPC分类号： C07D487/04

摘要： This invention provides compounds having the formula ##STR1## wherein R is azacycle or azabicycle; R.sub.1 is alkyl; R.sub.2 and R.sub.3 are each, independently, hydrogen, alkyl, alkoxy, or thioalkyl; n is 0-5; or a pharmaceutically acceptable salt thereof, which are useful in treating symptoms of cholinergic insufficiency involving cognitive disorders.

摘要翻译： 本发明提供具有式“IMAGE”的化合物，其中R是氮杂环或氮杂双环; R1是烷基; R2和R3各自独立地为氢，烷基，烷氧基或硫代烷基; n为0-5; 或其药学上可接受的盐，其可用于治疗涉及认知障碍的胆碱能功能不全症状。

公开(公告)号：US07608626B2

公开(公告)日：2009-10-27

申请号：US11260716

申请日：2005-10-27

申请人： Annmarie Louise Sabb ,  Robert Lewis Vogel

发明人： Annmarie Louise Sabb ,  Robert Lewis Vogel

IPC分类号： C07D221/02 ,  A01N43/42 ,  A61K31/44

CPC分类号： C07D471/04

摘要： Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

摘要翻译： 提供式1化合物或其药学上可接受的盐：其是脑5-羟色胺受体2C亚型的激动剂或部分激动剂。 化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。