公开(公告)号：US4539407A

公开(公告)日：1985-09-03

申请号：US696820

申请日：1985-01-31

申请人： Gary P. Stack ,  John A. Moyer

发明人： Gary P. Stack ,  John A. Moyer

IPC分类号： C07D471/04 ,  C07D209/56

CPC分类号： C07D471/04

摘要： There are disclosed compounds of the formula ##STR1## wherein X is O, S or NHR.sup.3, wherein R.sup.3 is hydrogen, lower alkyl or cycloalkyl;R is loweralkyl, loweralkoxy, aralkoxy of up to 10 carbon atoms or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are, independently, hydrogen, lower alkyl, cycloalkyl or aminoalkyl; or R is alkoxymethyl or hydroxymethyl;n is one of the integers 2, 3 or 4;R.sup.1 and R.sup.2 are, independently, hydrogen, halo, nitro, cyano, SCH.sub.3, or NR.sup.6 R.sup.7, NHCOR.sup.6, COOR.sup.6, OR.sup.6 or SO.sub.2 NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 are independently hydrogen or loweralkyl;and their activity as anticonvulsants, having use in the treatment of epileptic conditions.

摘要翻译： 公开了下式的化合物，其中X是O，S或NHR 3，其中R 3是氢，低级烷基或环烷基; R为至多10个碳原子的低级烷基，低级烷氧基，芳烷氧基或NR4R5，其中R4和R5独立地为氢，低级烷基，环烷基或氨基烷基; 或R为烷氧基甲基或羟甲基; n是整数2,3或4之一; R 1和R 2独立地是氢，卤素，硝基，氰基，SCH 3或NR 6 R 7，NHCOR 6，COOR 6，OR 6或SO 2 NR 6 R 7，其中R 6和R 7独立地是氢或低级烷基; 及其作为抗惊厥药的活性，用于治疗癫痫病症。

公开(公告)号：US5134141A

公开(公告)日：1992-07-28

申请号：US755721

申请日：1991-09-06

申请人： John A. Moyer ,  Gary P. Stack

发明人： John A. Moyer ,  Gary P. Stack

IPC分类号： A61K31/435 ,  A61K31/55 ,  A61P25/00 ,  A61P25/20 ,  C07D401/12

CPC分类号： A61K31/55

摘要： A method for relieving depression with decahydro-3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,5-methano-6,7,9-metheno-2H-pentaleno[1,2-d]azepine-2,4(3H)-dione, or a pharmaceutically acceptable salt thereof.

摘要翻译： 用十氢-3- [4- [4-（2-嘧啶基）-1-哌嗪基]丁基] -1,5-亚甲基-6,7,9-亚氨基-2H-苯并[[1,2] -d]吖庚因-2,4（3H） - 二酮或其药学上可接受的盐。

公开(公告)号：US07381723B2

公开(公告)日：2008-06-03

申请号：US10878715

申请日：2004-06-28

申请人： Gary P. Stack ,  Megan Tran ,  Adam M. Gilbert

发明人： Gary P. Stack ,  Megan Tran ,  Adam M. Gilbert

IPC分类号： A01N43/66 ,  A01N43/54 ,  A01N43/42 ,  A61K31/53 ,  A61K31/44 ,  C07D239/42 ,  C07D401/04 ,  C07D403/00 ,  C07D401/00 ,  C07D405/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07C409/00

CPC分类号： C07D519/00

摘要： Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and are also useful for the treatment of disorders such as anxiety, aggression and stress, and for the control of various physiological phenomena, such eating disorders, disorders of thermoregulation, and sleep and sexual dysfunction.

摘要翻译： 式的化合物可用于治疗由于老化，中风，头部创伤，阿尔茨海默病或其他神经变性疾病或精神分裂症引起的认知缺陷，并且还可用于治疗诸如焦虑，侵袭和应激等疾病以及用于控制 的各种生理现象，这种进食障碍，体温调节障碍，以及睡眠和性功能障碍。

公开(公告)号：US06613913B2

公开(公告)日：2003-09-02

申请号：US10340413

申请日：2003-01-10

申请人： Megan Tran ,  Gary P. Stack

发明人： Megan Tran ,  Gary P. Stack

IPC分类号： C07D49806

CPC分类号： C07D498/04 ,  C07D519/00

摘要： Compounds of the formula: useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse and related illnesses.

摘要翻译： 用于治疗抑郁症和其他疾病如强迫症，恐慌发作，广泛性焦虑症，社会焦虑症，性功能障碍，进食障碍，肥胖症，乙醇或可卡因滥用引起的成瘾性疾病和相关疾病的化合物 。

公开(公告)号：US06555560B2

公开(公告)日：2003-04-29

申请号：US10132238

申请日：2002-04-25

申请人： Megan Tran ,  Gary P. Stack

发明人： Megan Tran ,  Gary P. Stack

IPC分类号： A61K314433

CPC分类号： C07D493/04

摘要： Compounds of the formula useful for the treatment of diseases such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 治疗疾病如抑郁症（包括但不限于严重抑郁障碍，儿童抑郁症和心境恶劣），焦虑症，恐慌症，创伤后应激障碍，经前焦虑障碍注意力缺陷障碍（伴有或不伴有多动症）的化合物 ），强迫症（包括头发性躁狂症），社会焦虑症，广泛性焦虑症，肥胖症，神经性厌食症，神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾等饮食障碍，性功能障碍及相关疾病。

公开(公告)号：US06552049B2

公开(公告)日：2003-04-22

申请号：US10131340

申请日：2002-04-24

申请人： Gary P. Stack ,  Hong Gao ,  Elizabeth S. Gildersleeve

发明人： Gary P. Stack ,  Hong Gao ,  Elizabeth S. Gildersleeve

IPC分类号： C07D40104

CPC分类号： C07D493/04

摘要： Compounds of the formula useful for the treatment of depression such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse and related illnesses.

摘要翻译： 治疗抑郁症如强迫症，惊恐发作，广泛性焦虑症，社会焦虑症，性功能障碍，进食障碍，肥胖症，乙醇或可卡因滥用引起的成瘾性疾病以及相关疾病的化合物。

公开(公告)号：US06458802B1

公开(公告)日：2002-10-01

申请号：US10095505

申请日：2002-03-12

申请人： Megan Tran ,  Gary P. Stack

发明人： Megan Tran ,  Gary P. Stack

IPC分类号： A61K34741

CPC分类号： C07D491/04

摘要： Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 下式的化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和心境恶劣），焦虑症，惊恐障碍，创伤后应激障碍，经前焦虑症（也称为月经前综合征 ），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症，神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍和相关疾病。

公开(公告)号：US5756532A

公开(公告)日：1998-05-26

申请号：US730267

申请日：1996-10-15

申请人： Gary P. Stack ,  Richard E. Mewshaw ,  Byron A. Bravo ,  Young H. Kang

发明人： Gary P. Stack ,  Richard E. Mewshaw ,  Byron A. Bravo ,  Young H. Kang

IPC分类号： A61K31/357 ,  A61K31/40 ,  A61K31/407 ,  A61K31/4439 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P43/00 ,  C07D209/60 ,  C07D405/14 ,  C07D409/14 ,  C07D491/04 ,  C07D491/056 ,  C07D491/113 ,  C07D49/02

CPC分类号： C07D491/04

摘要： The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R.sup.3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic system.

摘要翻译： 式I的化合物：其中R 1和R 2独立地是氢，烷基，苯基或苄基; 或者R 1和R 2一起是可以被如下定义的R 3取代的亚苄基或亚烷基，或者R 1和R 2与它们所连接的碳一起形成羰基部分或环烷基; R 3是氢，羟基，卤素，三氟甲基，三氟甲氧基，烷基，烷氧基，芳烷氧基，烷酰氧基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷磺酰氨基; R4是氢或烷基; m是整数0,1或2; n为0〜6的整数，包括0和6; Z是氢，羟基，烷基，烯基，炔基，烷氧基，环烷基，多环烷基，任选被如上所定义的R 3取代的苯基，任选被如上所定义的R 3取代的苯氧基，任选被如上定义的R 3取代的萘基， 其中杂芳基或杂芳氧基的杂环选自噻吩，呋喃，吡啶，吡嗪，嘧啶，吲哚，吲唑，咪唑，苯并二氢吡喃，香豆素，喹诺酮，喹啉，苯并异恶唑， 苯并恶唑，吡唑，吡咯，噻唑，恶唑或异恶唑，杂环任选被如上定义的R 3取代; 或其药学上可接受的盐可用于治疗多巴胺能系统的病症。

公开(公告)号：US5541179A

公开(公告)日：1996-07-30

申请号：US433639

申请日：1995-05-02

申请人： Reinhardt B. Baudy ,  Scott C. Berta ,  Gary P. Stack

发明人： Reinhardt B. Baudy ,  Scott C. Berta ,  Gary P. Stack

IPC分类号： C07D213/74 ,  C07D295/185 ,  A61K31/55 ,  A61K31/495 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D295/185 ,  C07D213/74 ,  C07C2101/18

摘要： This invention relates to compounds useful as anxiolytic agents having the formula: ##STR1## where A is ##STR2## wherein X is O or S;R.sup.1 is selected from H, --CN, --OR.sup.3, --NO.sub.2, --NR.sup.3 R.sup.4, --NR.sup.3 COR.sup.4, --NR.sup.3 COOR.sup.4, --COR.sup.3, --COOR.sup.3, --CONR.sup.3 R.sup.4, --SR.sup.3, --SOR.sup.3, --SO.sub.2 R.sup.3, --SO.sub.2 NR.sup.3 R.sup.4, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, -perhalo-C.sub.1 -C.sub.6 -alkyl, F, Cl, Br, and I;R.sup.2 is selected from H, --COR.sup.3, --COOR.sup.3, --CONR.sup.3 R.sup.4, --CONHR.sup.3, --COCHR.sup.3 R.sup.4, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 alkenyl, and C.sub.2 -C.sub.6 -alkynyl;R.sup.3 and R.sup.4 are independently selected from C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 alkynyl, benzyl, or phenyl which may be optionally substituted by one to three groups selected from F, Cl, Br, I, --NO.sub.2, --CN, and --C.sub.1 -C.sub.6 alkoxy; or R.sup.3 and R.sup.4 together with the intervening nitrogen form a saturated or unsaturated ring having 4 to 6 carbons and one nitrogen; andor a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及可用作抗焦虑剂的化合物，其具有下式：其中A为X或O;或其中X为O或S; R1选自H，-CN，-OR3，-NO2，-NR3R4，-NR3COR4，-NR3COOR4，-COR3，-COOR3，-CONR3R4，-SR3，-SOR3，-SO2R3，-SO2NR3R4，C1-C6烷基， C 2 -C 6烯基，C 2 -C 6炔基， - 卤代-C 1 -C 6 - 烷基，F，Cl，Br和I; R2选自H，-COR3，-COOR3，-CONR3R4，-CONHR3，-COCHR3R4，C1-C6-烷基，C2-C6烯基和C2-C6-炔基; R 3和R 4独立地选自C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，苄基或苯基，其可任选被一至三个选自F，Cl，Br，I，-NO 2 ，-CN和-C 1 -C 6烷氧基; 或者R3和R4与中间的氮一起形成具有4-6个碳原子的饱和或不饱和的环和一个氮; 和/或其药学上可接受的盐。

公开(公告)号：US5245051A

公开(公告)日：1993-09-14

申请号：US939807

申请日：1992-09-03

申请人： Gary P. Stack ,  Young H. Kang

发明人： Gary P. Stack ,  Young H. Kang

IPC分类号： C07D407/12 ,  C07D493/04

CPC分类号： C07D407/12 ,  C07D493/04

摘要： A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2,3 or 4; X is --C(.dbd.O)-- or --(CH.sub.2).sub.m --, in which m is the integer 0 or 1; Y is methylene, ethylene or ethenylene, or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

摘要翻译： 下式的化合物，其中R 1和R 2独立地是氢，烷基，烷氧基，芳烷氧基，烷酰氧基，羟基，卤素，氨基，单或二烷基氨基，烷酰胺基或亚磺酰氨基，或者R 1和R 2一起是亚甲二氧基， 亚乙二氧基或亚丙二氧基; R3是氢或烷基; n是整数2,3或4之一; X是-C（= O） - 或 - （CH 2）m - ，其中m是整数0或1; Y是亚甲基，亚乙基或亚乙基或其药学上可接受的盐是抗精神病药。