公开(公告)号：US06689792B2

公开(公告)日：2004-02-10

申请号：US09976321

申请日：2001-10-12

申请人： Michael G. Kelly ,  Young H. Kang

发明人： Michael G. Kelly ,  Young H. Kang

IPC分类号： A61K31454

CPC分类号： C07D209/42 ,  C07D209/08 ,  C07D209/34 ,  C07D403/12

摘要： Compounds of formula (1) are provided: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by C, CR4, [[CHR4]] and CHCH2; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or A and B may be concatenated together to form indole, benzimidazole, indolone or indoline moieties; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders utilizing these compounds.

摘要翻译： 提供式（1）化合物：其中R 1和R 2是H，OH，F，Cl，Br，I，1至6碳烷基或烯基，1至6个碳烷氧基，芳基，OR 5，硝基，氨基，CF 3或R 1 并且R 2一起在2,3或3,4位上形成稠环，提供稠合苯基或苯并二恶烷基，或4-或7-取代的吲哚基，或5-或8-取代的吲哚基， 取代的喹啉基; R 3表示选自氢，1至6个碳烷基，1至4个碳烷氧基或卤素的基团; R 4表示选自氢，1至6个碳烷基或R 5的基团; R 5是CH 2 Ph，其中 苯环可任选被选自OMe，卤素，CF 3的基团取代; X选自C，CR 4，[[CHR]]和CHCH 2表示的基团; A选自N，NH， CH和CH 2; B选自由= O，= S，H和H 2表示的基团;或者A和B可以连接在一起形成吲哚，苯并咪唑，吲哚酮或二氢吲哚部分; 或其药学上可接受的盐，以及利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。

公开(公告)号：US06204274B1

公开(公告)日：2001-03-20

申请号：US09298200

申请日：1999-04-23

申请人： Michael G. Kelly ,  Young H. Kang

发明人： Michael G. Kelly ,  Young H. Kang

IPC分类号： A61K31445

CPC分类号： C07D401/14

摘要： The present invention provides compounds of the formula (1): wherein R1 and R2 each independently represent hydrogen, hydroxy, F, Cl, Br, I, CN, 1 to 6 carbon alkyl, 1 to 6 carbon alkoxy, nitro, CF3 and phenyloxy or benzyloxy, in which the aromatic ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; R3 and R4 are each independently a hydrogen, a 1 to 6 carbon alkyl or a CH2Ph in which the phenyl ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; Y is selected from CH2 or CH and, X is selected from a group represented by N, CR3, CHR3, CHCH; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds to treat central nervous system disorders, such as depression, anxiety, drug withdrawal, eating and sexual disorders and other conditions for which serotonin reuptake inhibitors are used.

摘要翻译： 本发明提供式（1）的化合物：其中R 1和R 2各自独立地表示氢，羟基，F，Cl，Br，I，CN，1至6个碳原子的烷基，1至6个碳烷氧基，硝基，CF 3和苯氧基或 苄氧基，其中芳环可以任选被1至3个选自C 1 -C 6烷氧基（优选OMe），F，Cl，Br，I和CF 3的基团取代; R 3和R 4各自独立地为氢， 至6碳烷基或CH 2 Ph，其中苯环可以任选被1至3个选自C 1 -C 6烷氧基（优选OMe），F，Cl，Br，I和CF 3的基团取代; Y选自CH 2或 CH，X选自由N，CR 3，CHR 3，CHCH表示的基团;或其药学上可接受的盐，以及使用该化合物治疗中枢神经系统疾病如抑郁症，焦虑症， 药物戒断，饮食和性障碍以及使用5-羟色胺再摄取抑制剂的其他条件。

公开(公告)号：US06432974B1

公开(公告)日：2002-08-13

申请号：US09771316

申请日：2001-01-26

申请人： Michael G. Kelly ,  Young H. Kang

发明人： Michael G. Kelly ,  Young H. Kang

IPC分类号： A61K314745

CPC分类号： C07D471/04

摘要： Compounds of the formula are useful in the treatment of anxiety, depression and related disorders of the central nervous system and other conditions such as schizophrenia, sleep disorders, including instances of circadian rhythm, the treatment of alcohol and drug withdrawal and sexual dysfunction.

摘要翻译： 该化合物可用于治疗中枢神经系统的焦虑，抑郁和相关疾病以及诸如精神分裂症，睡眠障碍，包括昼夜节律的事件，治疗酒精和药物戒断以及性功能障碍等其他病症。

公开(公告)号：US06310066B1

公开(公告)日：2001-10-30

申请号：US09504703

申请日：2000-02-16

申请人： Michael G. Kelly ,  Young H. Kang

发明人： Michael G. Kelly ,  Young H. Kang

IPC分类号： A61K31496

CPC分类号： C07D209/42 ,  C07D209/08 ,  C07D209/34 ,  C07D403/12

摘要： The present invention provides novel compounds of the general formula: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 4- or 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by N, CR4, CHR4 and CHCH; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders utilizing these compounds.

摘要翻译： 本发明提供了下列通式的新化合物：其中R 1和R 2是H，OH，F，Cl，Br，I，1至6碳烷基或烯基，1至6个碳烷氧基，芳基，OR 5，硝基，氨基， CF 3或R 1和R 2一起形成在2,3或3,4位上的稠环，提供稠合的苯基或苯并二恶烷基，或4-或7-取代的吲哚基，或4- 或5-或8-取代的喹啉基; R 3表示选自氢，1至6个碳烷基，1至4个碳烷氧基或卤素的基团; R 4表示选自氢，1至6个碳烷基或R 5 R 5是CH 2 Ph，其中苯环可以任选地被选自OMe，卤素，CF 3的基团取代; X选自由N，CR 4，CHR 4和CHCH表示的基团; A选自N， NH，CH和CH 2; B选自由= O，= S，H和H 2表示的基团;或其药学上可接受的盐，以及药物组合物和治疗方法 使用这些化合物的中枢神经系统疾病。

公开(公告)号：US6066637A

公开(公告)日：2000-05-23

申请号：US298202

申请日：1999-04-23

申请人： Michael G. Kelly ,  Young H. Kang

发明人： Michael G. Kelly ,  Young H. Kang

IPC分类号： B01D3/14 ,  C07C7/04 ,  C07D401/06 ,  C07D401/14 ,  A61K31/495 ,  A61K31/445

CPC分类号： C07D401/06 ,  C07D401/14

摘要： The present invention provides compounds represented by the general formula (1) whereinR.sub.1 is selected from H, OH, OR.sub.2 or halogen (F, Cl, Br, I);R.sub.2 is lower alkyl (C.sub.1 to C.sub.6);n is selected from 0, 1 or 2;X is CH or CH.sub.2 ;m is selected from 2, 3 or 4;Y is N or CH.sub.2 ;Ar is aryl or heteroaryl, both optionally substituted;or pharmaceutically acceptable salts thereof, as well as methods and pharmaceutical compositions utilizing these compounds for the inhibition of serotonin uptake and the treatment of CNS disorders, particularly depression.

摘要翻译： 本发明提供由通式（1）表示的化合物，其中R 1选自H，OH，OR 2或卤素（F，Cl，Br，I）; R2是低级烷基（C1-C6）; n选自0,1或2; X是CH或CH 2; m选自2,3或4; Y为N或CH2; Ar为芳基或杂芳基，均为任选取代的; 或其药学上可接受的盐，以及利用这些化合物抑制5-羟色胺摄取和治疗CNS障碍，特别是抑郁症的方法和药物组合物。

公开(公告)号：US4587738A

公开(公告)日：1986-05-13

申请号：US664494

申请日：1984-10-25

申请人： Young H. Kang

发明人： Young H. Kang

IPC分类号： G01B3/10 ,  G01B3/11 ,  G01B5/02 ,  G01B3/12

CPC分类号： G01B5/025 ,  G01B3/1005 ,  G01B3/11 ,  G01B2003/1038 ,  G01B2003/1069

摘要： A measuring rule including a numerical counter with a tapered knurled shaft mounted for rotation, a rotating spool having an elongated cord wound around it and spring bias means for rewinding the cord around the spool. Stop means are provided for automatically preventing rewinding of the cord about the spool until the stop means is disengaged by the user of the rule, while permitting the cord to be freely pulled off the spool. The cord passes from the spool around the knurled shaft to turn it and the counter as the cord is pulled off the spool, through the stop means and out of the housing so that the length of cord pulled out of the rule and passing around the knurled shaft is indicated by the numerical counter. Error correcting means are further provided for adjusting the location where the cord passes around the tapered shaft along its length.

摘要翻译： 包括具有安装用于旋转的锥形滚花轴的数字计数器的测量规则，具有缠绕在其上的细长绳索的旋转线轴和用于将绳索绕线轴重绕的弹簧偏压装置。 提供止动装置，用于自动防止绳索围绕卷轴重绕，直到停止装置由规则用户脱开，同时允许绳索被自由地从卷轴上拉出。 绳索从卷轴周围绕着滚花轴旋转，使其与计数器相连，因为线缆通过止动装置从线轴上脱出，从而将绳索的长度拉出规则并绕过滚花 轴由数字计数器指示。 进一步提供误差校正装置，用于调节绳索沿其长度绕过锥形轴的位置。

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。

公开(公告)号：US5750724A

公开(公告)日：1998-05-12

申请号：US739912

申请日：1996-10-30

申请人： Young H. Kang ,  Gary P. Stack

发明人： Young H. Kang ,  Gary P. Stack

IPC分类号： A61K20060101 ,  A61K31/00 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D20060101 ,  C07D405/12 ,  C07D493/04 ,  C07D405/00

CPC分类号： C07D493/04 ,  C07D405/12

摘要： The compounds of formula I: ##STR1## wherein R.sup.1, R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; or, R.sup.1 is defined as above and R.sup.4 and R.sup.5, taken together, are ortho substituted methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl; n is 3 or 4; or pharmaceutically acceptable salts thereof, are useful in the treatment of depression and related disorders.

摘要翻译： 式I的化合物：其中R 1，R 4和R 5独立地是氢，烷基，烷氧基，芳烷氧基，烷酰氧基，羟基，卤素，三氟甲基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷磺酰氨基; 或者，R1如上所定义，R 4和R 5一起是邻位取代的亚甲二氧基，亚乙二氧基或亚丙二氧基; R2和R3独立地是氢或烷基; n为3或4; 或其药学上可接受的盐可用于治疗抑郁症和相关疾病。

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：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。