公开(公告)号：US5212170A

公开(公告)日：1993-05-18

申请号：US882405

申请日：1992-05-13

申请人： Gary P. Stack

发明人： Gary P. Stack

IPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

摘要： The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.

摘要翻译： 其中Z为的化合物其中R 4为-H或烷基; q是整数0,1或2之一; Y是H 2或O; 或Z以R1形式取代，如上所述，R 1为氢或烷基或与Z结合; R2和R3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，氨基甲酰基或亚磺酰氨基或R2和R3一起是亚甲二氧基，亚乙二氧基或亚丙二氧基; m是整数1,2或3之一; n是整数0或1之一; 或其药学上可接受的盐是可用于缓解这些疾病状态的症状的抗精神病药，抗抑郁药和抗焦虑剂。

公开(公告)号：US5189171A

公开(公告)日：1993-02-23

申请号：US822475

申请日：1992-01-17

申请人： Gary P. Stack ,  Terrance H. Andree ,  Noreen T. Scherer

发明人： Gary P. Stack ,  Terrance H. Andree ,  Noreen T. Scherer

IPC分类号： C07D319/20 ,  C07D405/12 ,  C07D407/12 ,  C07D493/04

CPC分类号： C07D405/12 ,  C07D319/20 ,  C07D407/12 ,  C07D493/04

摘要： A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; 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 O or NR.sup.4, in which R.sup.4 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

摘要翻译： 下式的化合物：其中虚线表示任选的不饱和度; 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，烷酰氨基或亚磺酰氨基或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O或NR4，其中R4是氢或烷基; 或其药学上可接受的盐是抗精神病药。

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：US07008944B2

公开(公告)日：2006-03-07

申请号：US10618947

申请日：2003-07-14

申请人： Jonathan L. Gross ,  Gary P. Stack

发明人： Jonathan L. Gross ,  Gary P. Stack

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50

CPC分类号： C07D491/04

摘要： Compounds of the formula: are 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： 下式的化合物可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，饮食失调，肥胖症，乙醇或可卡因滥用引起的成瘾性疾病及相关 疾病

公开(公告)号：US06700001B2

公开(公告)日：2004-03-02

申请号：US10264947

申请日：2002-10-04

申请人： Jonathan L. Gross ,  Gary P. Stack

发明人： Jonathan L. Gross ,  Gary P. Stack

IPC分类号： C07D31158

CPC分类号： C07D491/04 ,  C07D311/04 ,  C07D311/58

摘要： A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is provided where R, R1, R2 and R3 are as defined herein. The compound of formula (II) is prepared using an optically active benzene compound of formula (I) where R0 is as defined herein. The 2-hydroxymethyl-chroman compounds of formula (II) are useful as intermediates for preparing a variety of medicinal agents.

摘要翻译： 提供了立体选择性合成式（II）的2-羟甲基 - 苯并二氢吡喃酮的方法，其中R，R 1，R 2和R 3如本文所定义。 式（II）化合物使用式（I）的光学活性苯化合物制备，其中R 0如本文所定义。 式（II）的2-羟甲基 - 苯并二氢吡喃化合物可用作制备各种药剂的中间体。

公开(公告)号：US06656950B2

公开(公告)日：2003-12-02

申请号：US10127923

申请日：2002-04-23

申请人： Megan Tran ,  Gary P. Stack

发明人： Megan Tran ,  Gary P. Stack

IPC分类号： A61K31436

CPC分类号： C07D491/04

摘要： Compounds of the formula useful for the treatment of depression, 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 dysthymia.

摘要翻译： 治疗抑郁症，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以及精神抑制的化合物。

公开(公告)号：US06617327B2

公开(公告)日：2003-09-09

申请号：US10128722

申请日：2002-04-23

申请人： Jonathan L. Gross ,  Gary P. Stack

发明人： Jonathan L. Gross ,  Gary P. Stack

IPC分类号： A61K314985

CPC分类号： C07D491/04

摘要： Compounds of the formula: are 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： 下式的化合物可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，饮食失调，肥胖症，乙醇或可卡因滥用引起的成瘾性疾病及相关 疾病

公开(公告)号：US06599915B2

公开(公告)日：2003-07-29

申请号：US10228744

申请日：2002-08-27

申请人： Megan Tran ,  Gary P. Stack

发明人： Megan Tran ,  Gary P. Stack

IPC分类号： A61K314741

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：US06559169B2

公开(公告)日：2003-05-06

申请号：US10128447

申请日：2002-04-23

申请人： George E. M. Husbands ,  Gary P. Stack ,  Richard E. Mewshaw ,  Ian A. Cliffe

发明人： George E. M. Husbands ,  Gary P. Stack ,  Richard E. Mewshaw ,  Ian A. Cliffe

IPC分类号： C07D40104

CPC分类号： C07D405/14 ,  C07D471/04

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

摘要翻译： 用于治疗抑郁症和强迫症，恐慌发作，广泛性焦虑症，性功能障碍，饮食失调，乙醇或可卡因滥用引起的成瘾性疾病和相关疾病的其他疾病的组合物。

公开(公告)号：US5962465A

公开(公告)日：1999-10-05

申请号：US15149

申请日：1998-01-29

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 ,  A61K31/47

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。