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1.发明授权公开(公告)号：US06420413B2
公开(公告)日：2002-07-16
申请号：US09833827
申请日：2001-04-12
申请人： Jean-Louis Peglion , Aimée Dessinges , Bertrand Goument , Mark Millan , Françoise Lejeune , Mauricette Brocco
发明人： Jean-Louis Peglion , Aimée Dessinges , Bertrand Goument , Mark Millan , Françoise Lejeune , Mauricette Brocco
IPC分类号： C07D20970
CPC分类号： C07D407/12 , C07C215/42 , C07D209/16 , C07D209/40 , C07D307/93 , C07D317/70 , C07D319/14 , C07D333/78
摘要： A compound selected from those of formula (I): wherein: denotes single bond or double bond, n is integer from 1 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, linear or branched (C1-C6)-alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, X represents a group selected from —CH═CH—, oxygen, S(O)m wherein m is integer from 0 to 2 inclusive, and NR3 wherein R3 represents a group as defined in the description, Y represents CH or CH2 depending on whether denotes single bond or double bond, or may have the additional meaning of oxygen when X represents oxygen, T represents monocyclic or polycyclic (C3-C10)cycloalkyl optionally containing within the ring system oxygen, selenium, S(O)p, NR3, or SiR4R5 wherein p, R3, R4, and R5 are as defined in the description, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful in the treatment of CNS disorders.
摘要翻译： 选自式（I）的化合物：其中：表示单键或双键，n为1〜6的整数，R1和R2表示选自氢，直链或支链（C1-C6） - 烷基 ，芳基，芳基烷基，环烷基，环烷基烷基，烯基，炔基，杂环烷基，杂环烷基烷基，杂芳基和杂芳基烷基，X表示选自-CH = CH-，氧，S（O）m的基团，其中m为0至2的整数 和NR 3，其中R 3表示说明书中定义的基团，Y表示CH或CH 2，取决于是单键或双键，或当X表示氧时，可以具有氧的额外含义，T表示单环或多环（C 3 -C 10 ）环烷基，其任选地在环体系内含有氧，硒，S（O）p，NR 3或SiR 4 R 5，其中p，R 3，R 4和R 5如说明书中所定义，其异构体及其加成盐与药学上可接受的酸 或碱，以及含有其的药物 可用于治疗CNS疾病。
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公开(公告)号：US07465733B2
公开(公告)日：2008-12-16
申请号：US11395747
申请日：2006-03-31
申请人： Jean-Louis Peglion , Aimée Dessinges , Bertrand Goument , Mark Millan , Clotilde Mannoury La Cour
发明人： Jean-Louis Peglion , Aimée Dessinges , Bertrand Goument , Mark Millan , Clotilde Mannoury La Cour
IPC分类号： A61K31/495 , A61K31/496 , C07D295/096 , C07D215/08 , C07D311/68 , C07D319/08 , A61K31/551
CPC分类号： C07D313/08 , C07D211/22 , C07D213/81 , C07D215/42 , C07D243/08 , C07D249/12 , C07D295/096 , C07D295/155 , C07D311/68 , C07D319/20 , C07D405/04
摘要： A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, alkyl, alkoxy, phenyl and cyano, X represents a bond, an oxygen atom or a group selected from —(CH2)m—, —OCH2— and —NR5—, wherein m represents 1 or 2, and R5 is as defined in the description, Y represents an oxygen atom or a group selected from NR7 and CHR8, wherein R7 and R8 are as defined in the description, Z represents a nitrogen atom or a CH group, n represents 1 or 2, Ak represents an alkylene chain, Ar represents an aryl or heteroaryl group, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.
摘要翻译： 选自式（I）的化合物：其中：R 1，R 2，R 3和R 4可以相同或不同，表示选自氢，卤素，烷基，烷氧基，苯基和氰基的原子或基团，X 表示键，氧原子或选自 - （CH 2）m - ， - OCH 2 - 和-NR 5 - 的基团，其中m表示1或2，R 5如说明书中所定义，Y表示氧原子或 选自NR7和CHR8的基团，其中R7和R8如说明书中所定义，Z表示氮原子或CH基团，n表示1或2，Ak表示亚烷基链，Ar表示芳基或杂芳基，其光学 异构体及其与药学上可接受的酸的加成盐。 含有该药物的药物可用于治疗需要5-羟色胺再摄取抑制剂和/或NK1拮抗剂的病症。
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公开(公告)号：US06743818B2
公开(公告)日：2004-06-01
申请号：US10195009
申请日：2002-07-12
IPC分类号： A61K3140
CPC分类号： C07D401/12
摘要： A compound selected from those of formula (I): wherein: n represents integer from 0 to 6, R1 represents a group selected from hydrogen, hydroxy, cyano, alkoxy, alkoxycarbonyl, carboxy, optionally substituted aminocarbonyl, and NR4R5 wherein R4, and R5 are as defined in the description, R2 represents a group selected from hydrogen, alkyl, hydroxymethyl, and —U—V—W wherein T, U, V, and W are as defined in the description, and R3 represents a group selected from hydrogen, linear or branched (C1-C6)alkyl, aryl, and, heteroaryl, its isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful in the treatment of CNS disorders.
摘要翻译： 选自式（I）的化合物：其中：n表示0至6的整数，R 1表示选自氢，羟基，氰基，烷氧基，烷氧基羰基，羧基，任选取代的氨基羰基和NR 4 R 5的基团，其中R 4和R 5 R 2表示选自氢，烷基，羟甲基和-UVW的基团，其中T，U，V和W如说明书中所定义，R 3表示选自氢，直链或支链（ C1-C6）烷基，芳基和杂芳基，其异构体，以及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用于治疗CNS疾病。
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公开(公告)号：US06452015B2
公开(公告)日：2002-09-17
申请号：US09833826
申请日：2001-04-12
IPC分类号： C07D40100
CPC分类号： C07D401/12
摘要： A compound selected from those of formula (I): wherein: n represents integer from 0 to 6, R1 represents a group selected from hydrogen, hydroxy, cyano, alkoxy, alkoxycarbonyl, carboxy, optionally substituted aminocarbonyl, and NR4R5 wherein R4, and R5 are as defined in the description, R2 represents a group selected from hydrogen, alkyl, hydroxymethyl, and -U-V-W wherein T, U, V, and W are as defined in the description, and R3 represents a group selected from hydrogen, linear or branched (C1-C6)alkyl, aryl, and, heteroaryl, its isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful in the treatment of CNS disorders.
摘要翻译： 选自式（I）的化合物：其中：n表示0至6的整数，R 1表示选自氢，羟基，氰基，烷氧基，烷氧基羰基，羧基，任选取代的氨基羰基和NR 4 R 5的基团，其中R 4和R 5 R 2表示选自氢，烷基，羟甲基和-UVW的基团，其中T，U，V和W如说明书中所定义，R 3表示选自氢，直链或支链（ C1-C6）烷基，芳基和杂芳基，其异构体，以及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用于治疗CNS疾病。
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公开(公告)号：US06486171B2
公开(公告)日：2002-11-26
申请号：US10105171
申请日：2002-03-25
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： A compound selected from those of formula (I): wherein: W represents optionally substituted naphthyl, or a group of formula Y (wherein) as defined in the description, n represents an integer from 1 to 6 inclusive, Z represents a single bond, oxygen, or optionally substituted nitrogen, A and Q each represent CH or nitrogen, it being understood that A or Q must be N and the other CH, M, together with a carbon of the phenyl to which it is bonded, represents thienyl, furyl, pyrrolyl, or oxopyrrolyl, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same, which are useful in the treatment of some CNS disorders.
摘要翻译： 选自式（I）的化合物：其中：W表示任选取代的萘基，或如说明书中所定义的式Y（其中）的基团，n表示1至6的整数，Z表示单键， 氧或任选取代的氮，A和Q各自表示CH或氮，应理解A或Q必须为N，另一个CH，M与其所键合的苯基的碳一起代表噻吩基，呋喃基 ，吡咯基或氧代吡咯基，其异构体及其药学上可接受的酸或碱加成盐，以及含有它们的药物，其可用于治疗一些CNS障碍。
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公开(公告)号：US07470683B2
公开(公告)日：2008-12-30
申请号：US11904006
申请日：2007-09-25
IPC分类号： C07D498/04 , A61K31/53
CPC分类号： C07D498/04
摘要： Compounds of formula I, of trans relative configuration: wherein: X represents an oxygen atom or an NR2 group, Y represents a group selected from —CH2—, —(CH2)2— and —CH═CH—, R1 and R2, which may be the same or different, each represents a hydrogen atom or a group selected from alkyl, cycloalkyl and cycloalkylalkyl, in racemic form or in the form of optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof. Medicinal products containing the same which are useful in the treatment of disorders of the central nervous system that involve the dopaminergic system.
摘要翻译： 式I化合物的反式相对构型：其中：X表示氧原子或NR 2基团，Y表示选自-CH 2 - ， - （CH 2）2 - 和-CH-CH-，R 1和R 2的基团，其中 可以相同或不同，各自表示氢原子或选自烷基，环烷基和环烷基烷基的基团，其为外消旋形式或旋光异构体形式，以及其与药学上可接受的酸及其水合物的加成盐。 含有该药物的药物可用于治疗涉及多巴胺能系统的中枢神经系统疾病。
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公开(公告)号：US6107345A
公开(公告)日：2000-08-22
申请号：US261803
申请日：1999-03-03
申请人： Jean-Louis Peglion , Aimee Dessinges , Jean-Christophe Harmange , Mark Millan , Adrian Newman-Tancredi , Mauricette Brocco
发明人： Jean-Louis Peglion , Aimee Dessinges , Jean-Christophe Harmange , Mark Millan , Adrian Newman-Tancredi , Mauricette Brocco
IPC分类号： C07D233/50 , A61K31/00 , A61K31/135 , A61K31/33 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P1/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/30 , A61P43/00 , C07C215/42 , C07C217/58 , C07C217/74 , C07D211/44 , C07D233/48 , C07D263/28 , C07D309/10 , C07D335/02 , C07D345/00 , A61K31/133
CPC分类号： C07D309/10 , C07C215/42 , C07C217/74 , C07D233/48 , C07D263/28 , C07D335/02
摘要： A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.
摘要翻译： 式（I）的化合物：其中：可以相同或不同的Z 1，Z 2，Z 3，Z 4表示如说明书中所定义的基团，X表示氧，S（O）p， - （CH 2）n - 或-CH 2 -Y-CH 2 - ，其中p，n和Y如说明书中所定义，A表示其中m，R 1，R 2和G如说明书中所定义，其异构体和加成盐与药学上可接受的酸 和含有它们的药用产品可用于治疗抑郁症，恐慌发作，强迫症，恐惧症，冲动性疾病，药物滥用或焦虑症等疾病。
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公开(公告)号：US06399616B1
公开(公告)日：2002-06-04
申请号：US09641777
申请日：2000-08-18
IPC分类号： A61K31496
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： A compound selected from those of formula (I): wherein: W represents optionally substituted naphthyl, n represents an integer from 2 to 3 inclusive, Z represents a single bond, A represents nitrogen, Q represents nitrogen, M, together with the carbon of pyridyl to which it is bonded, represents thieno, furo, pyrrolo or oxopyrrolo, Its optical isomers and pharmaceutically-acceptable acid or base additional salts thereof, and Medicinal products containing the same which are useful in the treatment of CNS disorders. It being understood that “aryl” is phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl.
摘要翻译： 选自式（I）的化合物：其中：W表示任选取代的萘基，n表示2〜3的整数，Z表示单键，A表示氮，Q表示氮，M表示与 吡咯基，吡咯基或氧吡咯，其光学异构体和药学上可接受的酸或碱的另外的盐，和含有它们的可用于治疗CNS病症的药物。可以理解的是“ 芳基“是苯基，萘基，二氢萘基或四氢萘基。
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公开(公告)号：US20080076765A1
公开(公告)日：2008-03-27
申请号：US11904006
申请日：2007-09-25
IPC分类号： A61K31/538 , A61P25/28 , C07D265/34
CPC分类号： C07D498/04
摘要： Compounds of formula I, of trans relative configuration: wherein: X represents an oxygen atom or an NR2 group, Y represents a group selected from —CH2—, —(CH2)2— and —CH═CH—, R1 and R2, which may be the same or different, each represents a hydrogen atom or a group selected from alkyl, cycloalkyl and cycloalkylalkyl, in racemic form or in the form of optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof. Medicinal products containing the same which are useful in the treatment of disorders of the central nervous system that involve the dopaminergic system.
摘要翻译： 式I化合物的反式相对构型：其中：X表示氧原子或NR 2基团，Y表示选自-CH 2 - ， - （ CH 2 - ）2 - 和-CH-CH-，R 1和R 2，其可以是 相同或不同，各自表示氢原子或选自烷基，环烷基和环烷基烷基的基团，其外消旋形式或旋光异构体形式，以及其与药学上可接受的酸及其水合物的加成盐。 含有该药物的药物可用于治疗涉及多巴胺能系统的中枢神经系统疾病。
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10.发明授权3-(piperid-4-yl)-1,2-benzisoxazole and 3-(piperazin-4-yl)-1,2-benzisoxazole compounds 失效3-（哌啶-4-基）-1,2-苯并异恶唑和3-（哌嗪-4-基）-1,2-苯并异恶唑化合物
公开(公告)号：US5780474A
公开(公告)日：1998-07-14
申请号：US868116
申请日：1997-06-03
IPC分类号： A61K31/445 , A61K31/495 , A61P25/18 , A61P25/20 , A61P43/00 , C07D413/12 , C07D413/14 , A61K31/44
CPC分类号： C07D413/12 , C07D413/14
摘要： Compounds of formula: ##STR1## wherein: A, m, n, E and Y are as defined in the description, the optical isomers thereof and the physiologically-tolerable salts thereof. These compounds, their optical isomers and their physiologically-tolerable salts, can be used as medicaments in the treatment of psychotic disorders, anxio-depressive disorders, and aggressiveness.
摘要翻译： 式：其中：A，m，n，E和Y如说明书中所定义，其光学异构体及其生理上可容忍的盐。 这些化合物，它们的光学异构体及其生理上可耐受的盐可以用作治疗精神病，焦虑抑郁症和侵略性的药物。
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