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1. 发明授权

US06239134B1 Diazole derivatives as serotonergic agents 失效
标题翻译：二唑衍生物作为血清素能药剂
公开(公告)号：US06239134B1
公开(公告)日：2001-05-29
申请号：US09515049
申请日：2000-02-25
申请人： Annmarie L. Sabb , Robert L. Vogel , Michael G. Kelly , Yvette L. Palmer , Wayne E. Childers
发明人： Annmarie L. Sabb , Robert L. Vogel , Michael G. Kelly , Yvette L. Palmer , Wayne E. Childers
IPC分类号： A61K31496
CPC分类号： C07D285/10 , C07D417/12
摘要： The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.
摘要翻译：本发明提供通式（1）的化合物：其中X，Y或Z的两个原子是氮，第三个原子是硫或氧; R是H，卤素，OH，SH，C 1 -C 6烷基， C 1 -C 6烷氧基，C 1 -C 6硫代烷基，苯氧基，硫代苯氧基，苯基或取代的苯基; A是C，CH或N; R 1是芳基，杂芳基或环烷基，任选地被1至3个选自C1- C6烷基，C1-C6烷氧基; CF 3，Cl，Br，F，CN或CO 2 CH 3; R 2为H或烷基R 3为C 1 -C 6烷基，任选取代的芳基，任选取代的5或6元杂芳基，任选被C 1 -C 6烷基取代的C 3至C 8环烷基，含有一个或多个选自O，S或N的杂原子的3至8元杂环; 或其药学上可接受的盐，以及使用这些化合物治疗中枢神经系统疾病的药物组合物和方法。

2. 发明授权

US07271164B2 Cyclohepta[b][1,4]diazepino[6,7,1,-hi]indoles and derivatives 失效
标题翻译：环庚三烯[b] [1,4]二氮杂[6,7,1，-i]吲哚和衍生物
公开(公告)号：US07271164B2
公开(公告)日：2007-09-18
申请号：US10966227
申请日：2004-10-15
申请人： Annmarie L. Sabb , Robert L. Vogel
发明人： Annmarie L. Sabb , Robert L. Vogel
IPC分类号： A61K31/55 , A61P25/00 , A61P25/24 , C07D243/00
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，酰基或酚酰基或噻吩甲酰基; R 3和R 4各自独立地为H，烷基或环烷基; R 5是H或烷基; R 6是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。

3. 发明授权

US07271163B2 Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效
标题翻译：环戊基[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物
公开(公告)号：US07271163B2
公开(公告)日：2007-09-18
申请号：US10898029
申请日：2004-07-23
申请人： Annmarie L. Sabb , Robert L. Vogel , James A. Nelson , Sharon J. Rosenzweig-Lipson , Gregory S. Welmaker , Joan E. Sabalski
发明人： Annmarie L. Sabb , Robert L. Vogel , James A. Nelson , Sharon J. Rosenzweig-Lipson , Gregory S. Welmaker , Joan E. Sabalski
IPC分类号： A61K31/55 , A61P25/00 , A61P25/24 , C07D243/00
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各自独立地为氢，1-6个碳原子的烷基，环烷基，1-6个碳原子的烷氧基，-CH 2 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，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个碳原子的氟代烷氧基 -6个碳原子，2-7个碳原子的酰基，芳基或芳酰基; R 4和R 5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，氟烷基，-CN，烷基 1-6个碳原子的磺酰胺，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个碳原子或芳酰基; R 6和R 7各自独立地为氢，C 1 -C 6烷基或环烷基; 或其药学上可接受的盐，以及含有这些化合物的药物组合物及其使用方法，包括治疗强迫症，恐慌症，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，癫痫和脊髓损伤。

4. 发明授权

US07271162B2 Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效
标题翻译：环辛[b] [1,4]二氮杂[6,7,1-hi]吲哚和衍生物
公开(公告)号：US07271162B2
公开(公告)日：2007-09-18
申请号：US10872090
申请日：2004-06-18
申请人： Annmarie L. Sabb , Robert L. Vogel
发明人： Annmarie L. Sabb , Robert L. Vogel
IPC分类号： A61K31/55 , A61P25/00 , A61P25/24 , C07D243/00
CPC分类号： C07D487/06
摘要： This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated, acyl, or aroyl; R3, R4 are H, alkyl, cycloalkyl or —CH2-cycloalkyl; R5 is H or alkyl; R6 is H or alkyl; and wherein the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods for using these compounds to treat central nervous system 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：本发明提供具有以下结构的式I化合物：其中R 1和R 2均为H，烷基，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，酰基或芳酰基; R 3，R 4是H，烷基，环烷基或-CH 2 - 环烷基; R 5是H或烷基; R 6是H或烷基; 并且其中虚线表示任选的双键; 或其药学上可接受的盐，以及使用这些化合物治疗中枢神经系统疾病（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。

5. 发明授权

US5571819A Imidazopyridines as muscarinic agents 失效
标题翻译：咪唑并吡啶类作为毒蕈碱药
公开(公告)号：US5571819A
公开(公告)日：1996-11-05
申请号：US343399
申请日：1994-11-22
申请人： Annmarie L. Sabb , Michael B. Webb
发明人： Annmarie L. Sabb , Michael B. Webb
IPC分类号： C07D471/04 , C07D519/00 , A61K31/435
CPC分类号： C07D471/04
摘要： The compound of the formula: ##STR1## where R.sub.1 is H, alkyl, perhaloalkyl, arylalkyl, alkenyl or alkynyl; R.sub.2 is H when R.sub.4 is other than H, and, when R.sub.4 is H, R.sub.2 is ##STR2## in which R.sub.5 is hydrogen or alkyl; R.sub.3 is hydrogen or halogen; R.sub.4 is H or ##STR3## X, Y and Z are, independently, nitrogen or carbon, at least one of X, Y or Z being nitrogen; n is 1 or 2; n.sub.1 is 0, 1, 2, 3, 4, or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.
摘要翻译：下式的化合物：其中R 1是H，烷基，全卤代烷基，芳基烷基，烯基或炔基; 当R4不为H时，R2为H，当R4为H时，R2为R5，其中R5为氢或烷基; R3是氢或卤素; R4是H或X，Y和Z独立地是氮或碳，X，Y或Z中的至少一个是氮; n为1或2; n1为0,1,2,3,4或5; 或其药学上可接受的盐是中枢活性毒蕈碱剂。

6. 发明授权

US06372745B1 2,3,4,4A-tetrahydro-1H-pyrazino[1,2-A]quinoxalin-5(6H)one derivatives 失效
标题翻译： 2,3,4,4-四氢-1H-吡嗪并[1,2-A]喹喔啉-5（6H）酮衍生物
公开(公告)号：US06372745B1
公开(公告)日：2002-04-16
申请号：US09455220
申请日：1999-12-06
申请人： Annmarie L. Sabb , Gregory S. Welmaker , James A. Nelson
发明人： Annmarie L. Sabb , Gregory S. Welmaker , James A. Nelson
IPC分类号： A61K315025
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。

7. 发明授权

US5712270A 2-arylamidothiazole derivatives with CNS activity 失效
标题翻译：具有CNS活性的2-芳基氨基噻唑衍生物
公开(公告)号：US5712270A
公开(公告)日：1998-01-27
申请号：US739559
申请日：1996-10-30
申请人： Annmarie L. Sabb
发明人： Annmarie L. Sabb
IPC分类号： C07D277/46 , C07D277/56 , C07D417/12 , C07D453/02 , C07D417/06 , C07D417/14
CPC分类号： C07D417/12 , C07D277/46 , C07D277/56 , C07D453/02
摘要： This invention relates to methods of treating neurological illnesses related to acetylcholine deficiency in the CNS including memory loss attending senility, Parkinson's disease, Down's syndrome or senile pugilistica by administering a therapeutically effective compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo�2.2.2!octyl or azabicyclo�2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo-�3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及通过给药治疗有效的化合物，其中R1，R2和R3是独立地是H，烷基，卤素，全卤代烷基，羟基，烷氧基，芳基或芳基烷基; n是0-5的整数; 当n1为零时，R为氮杂双环[2.2.2]辛基或氮杂双环[2.2.1]庚基，当n1为1,2,3,4或5时，R为NR4R5，其中R4和R5为烷基或R4， R5与其所连接的氮原子一起取代为其中所述取代基为烷氧基，卤素或全卤代烷基的N-（取代的芳基）哌嗪基; N-（吡啶基）哌嗪基; N-（嘧啶基）哌嗪基; 或3-氮杂双环[3.2.2]壬-3-基; X是氧或NH; n和n1独立地是整数0,1,2,3,4或5中的一个; 或其药学上可接受的盐。

8. 发明授权

US4985560A Pyridazino(4,5-b)indolizines 失效
标题翻译：哒嗪（4,5-b）中氮茚
公开(公告)号：US4985560A
公开(公告)日：1991-01-15
申请号：US464468
申请日：1990-01-12
申请人： Annmarie L. Sabb , Magid A. Abou-Gharbia , Gervais Dionne
发明人： Annmarie L. Sabb , Magid A. Abou-Gharbia , Gervais Dionne
IPC分类号： C07D471/14 , C07D519/00
CPC分类号： C07D471/14
摘要： The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.2]nonan-3-yl, pyrrol-1-yl, pyrrolidin-2-on-1-ytl, pyrrolidin-2-thion-1-yl, imidazol-1-yl, alkyl-piperidin-1-yl or a piperazin-1-yl moiety in the 4-position of which is hydrogen, --CHO, alkyl or unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, alkoxy, halo, cyano, nitro or trifluoromethyl; or (c) n is 1 to 5, and R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, 3-quinuclidinyl, 2-adamantyl, bicyclo[3.2.1]octan-1-yl, bicyclo[3.3.1]nonan-9-yl or 2-,3- or 4- pyridinyl; or a pharmaceutically acceptable salt thereof are M.sub.1 receptor agonists useful in treatment of dementias involving the cholinergic system. dd
摘要翻译：下式的化合物：其中R 1是氢，烷氧基，氰基，卤素，硝基，氨基或单或二烷基氨基; R2是氢，烷基，苯基，苄基，2-噻吩基，3-噻吩基或2-，3-或4-吡啶基; R3是氢，烷基或苯基; R4是N-甲基 - 吡咯烷-2-基，2-，3-或4-吡啶基，3-奎宁环基或其中n为1至5; m为0〜3; 和R8是氢或1至6个碳原子的烷基; 其中：（a）n为2，R5取R5为乙烯，R6为-CHO，烷基，未取代或取代的苯基，嘧啶基，吡啶基或吡嗪基，其中取代基为烷基，烷氧基，卤素，氰基，硝基或三氟甲基; （b）n为1至5，R 5和R 6一起为可被烷基取代的多亚甲基或R 5和R 6为吗啉代，3-氮杂双环[3.2.2]壬烷-3-基，吡咯-1-基，吡咯烷 -2-对-1-基，吡咯烷-2-硫基-1-基，咪唑-1-基，烷基 - 哌啶-1-基或哌嗪-1-基部分，其4-位是氢， -CHO，烷基或未取代或取代的苯基，嘧啶基，吡啶基或吡嗪基，烷氧基，卤素，氰基，硝基或三氟甲基; 或（c）n为1至5，并且R 5和R 6独立地为氢，烷基，苯基，3-奎宁环基，2-金刚烷基，双环[3.2.1]辛-1-基，双环[3.3.1] 壬-9-基或2-，3-或4-吡啶基; 或其药学上可接受的盐是可用于治疗涉及胆碱能系统的痴呆症的M1受体激动剂。

9. 发明授权

US07012089B2 [1,4]Diazocino[7,8,1-hi]indole derivatives as antipsychotic and antiobesity agents 失效
标题翻译： [1,4] Diazocino [7,8,1-hi]吲哚衍生物作为抗精神病药和抗肥胖剂
公开(公告)号：US07012089B2
公开(公告)日：2006-03-14
申请号：US10422657
申请日：2003-04-24
申请人： Hong Gao , Gary P. Stack , Annmarie L. Sabb
发明人： Hong Gao , Gary P. Stack , Annmarie L. Sabb
IPC分类号： C07D245/04 , C07D487/06 , A61K31/395 , A61P25/18 , A61P25/24
CPC分类号： C07D487/06
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: where R1 through R7 are defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
摘要翻译：提供式（I）化合物或其药学上可接受的盐：其中R 1至R 7在本文中定义。式（I）化合物是5HT 2C激动剂或部分激动剂，并且可用于治疗多种疾病。

10. 发明授权

US5773458A 1-azabicycloheptane derivatives 失效
公开(公告)号：US5773458A
公开(公告)日：1998-06-30
申请号：US953601
申请日：1997-10-17
申请人： Annmarie L. Sabb , Reinhardt P. Stein
发明人： Annmarie L. Sabb , Reinhardt P. Stein
IPC分类号： C07D487/08 , A61K31/40 , C07D487/04
CPC分类号： C07D487/08
摘要： The compound of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are centrally active muscarinic agents.

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