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1. 发明授权

US5968954A 2-aminoindan compounds as 5HT.sub.1B antagonists 失效
标题翻译： 2-氨基茚满化合物作为5HT1B拮抗剂
公开(公告)号：US5968954A
公开(公告)日：1999-10-19
申请号：US31490
申请日：1998-02-26
申请人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Alain Gobert
发明人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Alain Gobert
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P3/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D405/04 , C07D405/14 , C07D409/04 , C07D411/04 , C07D413/14 , C07D491/056 , C07D405/12
CPC分类号： C07D405/04 , C07D409/04 , C07D411/04
摘要： New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.
摘要翻译：新的2-氨基茚满化合物其中：n，Ar，R，E，X 1，X 2，X 3和X 4如说明书中所定义，以外消旋混合物的形式，以旋光异构体的形式和生理学上其耐受酸加成盐。本发明的产品可用作药物并且显示出对5HT1B受体的选择性结合亲和力。

2. 发明授权

US5753662A Piperazine compounds 失效
标题翻译：哌嗪化合物
公开(公告)号：US5753662A
公开(公告)日：1998-05-19
申请号：US655457
申请日：1996-05-30
申请人： Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
发明人： Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
IPC分类号： A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D307/79 , C07D307/81 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12 , C07D405/00 , C07D407/00
CPC分类号： C07D307/79 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12
摘要： A compound selected from those of formula: ##STR1## wherein: A--B, n, D and E are as defined in the specification, their racemic mixtures, and their optical isomers, and also the physiologically tolerable salts thereof with appropriate acids. The products of the invention may be used therapeutically.
摘要翻译：选自下式的化合物：其中：A-B，n，D和E如说明书中所定义，它们的外消旋混合物及其旋光异构体，以及其与适当的酸的生理上可耐受的盐。本发明的产品可以在治疗上使用。

3. 发明授权

US5464834A N-substituted N'-heterobicyclic piperazines having pharmaceutical activity 失效
标题翻译：具有药物活性的N-取代的N'-杂双环哌嗪
公开(公告)号：US5464834A
公开(公告)日：1995-11-07
申请号：US75679
申请日：1993-06-11
申请人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Jean-Michel Rivet
发明人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Jean-Michel Rivet
IPC分类号： A61K31/495 , A61P3/08 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D307/79 , C07D311/18 , C07D319/18 , C07D321/10 , C07D333/24 , C07D333/60 , C07D409/12 , C07D495/04 , C07D405/10 , C07D407/14
CPC分类号： C07D409/12
摘要： New N-substituted N'-heterobicyclic piperazines corresponding to the general formula I: ##STR1## wherein: R represents: ##STR2## D represents a single bond, except when R represents naphthyl, or a hydrocarbon chain having 1 to 8 carbon atoms inclusive which is straight-chain or branched by a gem-dimethyl; andA-B represents: --(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.3 --O--, or --CO--CH.dbd.CH--,as well as their possible stereoisomers, epimers, and pharmaceutically-acceptable acid addition salts thereof; and medicinal products containing the same, useful in the treatment of a disorder requiring a 5-HT.sub.1A receptor antagonist.
摘要翻译：对应于通式I的新的N-取代的N'-杂双环哌嗪：其中：R表示：除了当R表示萘基时，D表示单键，或具有1-8个碳原子的烃链，其由偕二甲基直链或支链; 并且A-B表示： - （CH 2）2 -O - ， - （CH 2）3 -O-或-CO-CH = CH-，以及它们可能的立体异构体，差向异构体及其药学上可接受的酸加成盐; 和含有该药物的药物，可用于治疗需要5-HT 1A受体拮抗剂的病症。

4. 发明授权

US08076325B2 1,2,4,5-tetrahydro-3H-benzazepine compounds, a process for their preparation and pharmaceutical compositions containing them 有权
标题翻译： 1,2,4,5-四氢-3H-苯并氮杂化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08076325B2
公开(公告)日：2011-12-13
申请号：US12283110
申请日：2008-09-09
申请人： Jean-Louis Peglion , Bertrand Goument , Aimee Dessinges , Pascal Caignard , Jean-Paul Vilaine , Catherine Thollon , Nicole Villeneuve , Stefano Chimenti
发明人： Jean-Louis Peglion , Bertrand Goument , Aimee Dessinges , Pascal Caignard , Jean-Paul Vilaine , Catherine Thollon , Nicole Villeneuve , Stefano Chimenti
IPC分类号： A01N43/00 , A61K31/55 , C07D223/16
CPC分类号： C07D223/16
摘要： Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group selected from cycloalkyl, benzyl and optionally substituted alkyl, R2, R3, R4 and R5 each represent a hydrogen atom or a hydroxy, methyl, —OSO2R10, —OCOR10 or optionally substituted alkoxy group, or R2 and R3, or R3 and R4, or R4 and R5 together form a group —O—(CH2)q—O—, —O—CH═CH—O— or —O—CH═CH—, R6, R7, R8 and R9 each represent a hydrogen atom or an alkoxy group, or R6 and R7, or R7 and R8, or R8 and R9 together form a group —O—(CH2)q—O—, R10 represents a group selected from linear or branched C1-C6alkoxy, NR11R′11 and optionally substituted alkyl, R11 and R′11 each represent a hydrogen atom or an alkyl group, or R11 and R′11 together with the nitrogen atom carrying them form an optionally substituted, monocyclic or bicyclic, nitrogen-containing heterocycle, X represents O, NH or CH2, m and p each represent 0 or 1, n and q each represent 1 or 2, in racemic form or in the form of optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating various pathologies.
摘要翻译：式（I）化合物：其中：R 1表示氢原子或选自环烷基，苄基和任选取代的烷基的基团，R 2，R 3，R 4和R 5各自表示氢原子或羟基，甲基，-OSO 2 R 10，-OCOR 10 或任选取代的烷氧基，或R 2和R 3，或R 3和R 4，或R 4和R 5一起形成基团-O-（CH 2）q -O-，-O-CH = CH-O-或-O-CH = CH-，R6，R7，R8和R9各自表示氢原子或烷氧基，或R6和R7，或R7和R8，或R8和R9一起形成-O-（CH 2）q -O-，R 10基团表示选自直链或支链C 1 -C 6烷氧基，NR 11 R 11和任选取代的烷基的基团，R 11和R 11各自表示氢原子或烷基，或者R 11和R 11与携带它们的氮原子一起形成任选取代的单环或双环含氮杂环，X表示O，NH或CH 2，m和p各自表示0或1，n和q各自表示1或2，以外消旋形式或i n是光学异构体的形式，以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各种病症。

5. 发明授权

US07612061B2 Piperazine compounds 失效
公开(公告)号：US07612061B2
公开(公告)日：2009-11-03
申请号：US12291485
申请日：2008-11-10
申请人： Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Clotilde Mannoury La Cour
发明人： Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Clotilde Mannoury La Cour
IPC分类号： A61K31/551 , C07D295/081
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.

6. 发明申请

US20090069296A1 1,2,4,5-Tetrahydro-3H-benzazepine compounds, a process for their preparation and pharmaceutical compositions containing them 有权
标题翻译： 1,2,4,5-四氢-3H-苯并氮杂化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US20090069296A1
公开(公告)日：2009-03-12
申请号：US12283110
申请日：2008-09-09
申请人： Jean-Louis Peglion , Bertrand Goument , Aimee Dessinges , Pascal Caignard , Jean-Paul Vilaine , Catherine Thollon , Nicole Villeneuve , Stefano Chimenti
发明人： Jean-Louis Peglion , Bertrand Goument , Aimee Dessinges , Pascal Caignard , Jean-Paul Vilaine , Catherine Thollon , Nicole Villeneuve , Stefano Chimenti
IPC分类号： C07D223/16 , A61K31/55
CPC分类号： C07D223/16
摘要： Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group selected from cycloalkyl, benzyl and optionally substituted alkyl, R2, R3, R4 and R5 each represent a hydrogen atom or a hydroxy, methyl, —OSO2R10, —OCOR10 or optionally substituted alkoxy group, or R2 and R3, or R3 and R4, or R4 and R5 together form a group —O—(CH2)q—O—, —O—CH═CH—O— or —O—CH═CH—, R6, R7, R8 and R9 each represent a hydrogen atom or an alkoxy group, or R6 and R7, or R7 and R8, or R8 and R9 together form a group —O—(CH2)q—O—-, R10 represents a group selected from linear or branched C1-C6alkoxy, NR11R′11 and optionally substituted alkyl, R11 and R′11 each represent a hydrogen atom or an alkyl group, or R11 and R′1 together with the nitrogen atom carrying them form an optionally substituted, monocyclic or bicyclic, nitrogen-containing heterocycle, X represents O, NH or CH2, m and p each represent 0 or 1, n and q each represent 1 or 2, in racemic form or in the form of optical isomers,and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating various pathologies.
摘要翻译：式（I）化合物：其中：R 1表示氢原子或选自环烷基，苄基和任选取代的烷基的基团，R 2，R 3，R 4和R 5各自表示氢原子或羟基，甲基，-OSO 2 R 10，-OCOR 10 或任选取代的烷氧基，或R 2和R 3，或R 3和R 4或R 4和R 5一起形成基团-O-（CH 2）q O - ， - O-CH-CH-O-或-O-CH-CH- ，R6，R7，R8和R9各自表示氢原子或烷氧基，或R6和R7，或R7和R8，或R8和R9一起形成-O-（CH2）qO-基，R10表示基团选自直链或支链C 1 -C 6烷氧基，NR 11 R 11和任选取代的烷基，R 11和R 11各自表示氢原子或烷基，或者R 11和R 11与携带它们的氮原子一起形成任选取代的，单环或双环，含氮杂环，X表示O，NH或CH 2，m和p各自表示0或1，n和q各自表示1或2，以外消旋形式或以旋光异构体的形式，其离子盐与药学上可接受的酸。含有该药物的药物可用于治疗各种病症。

7. 发明授权

US5593989A Tetracyclic 1,4-oxazine compounds 失效
标题翻译：四环1,4-恶嗪化合物
公开(公告)号：US5593989A
公开(公告)日：1997-01-14
申请号：US456504
申请日：1995-06-01
申请人： Jean-Louis Peglion , Joel Vian , Bertrand Goument , Mark Millan , Val erie Audinot , Jean-Charles Schwartz , Pierre Sokoloff
发明人： Jean-Louis Peglion , Joel Vian , Bertrand Goument , Mark Millan , Val erie Audinot , Jean-Charles Schwartz , Pierre Sokoloff
IPC分类号： A61K31/435 , A61K31/4741 , A61K31/535 , A61K31/5383 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , C07D491/04 , C07D491/048 , C07D491/153 , C07D498/04 , C07D498/14
CPC分类号： C07D491/04
摘要： New compounds of formula: ##STR1## wherein A--B, X, Y, R and n are as defined in the description. The geometric isomers, racemate and optical isomers thereof and the addition salts with pharmaceutically acceptable acids, and medicinal products containing the same are useful for treating psychotic disorders, depression, Parkinson's disease, memory disorders and disorders associated with drug abuse.
摘要翻译：新化合物：其中A-B，X，Y，R和n如说明书中所定义。其几何异构体，外消旋物和旋光异构体以及与药学上可接受的酸的加成盐以及含有它们的药物可用于治疗精神病，抑郁症，帕金森病，记忆障碍和与药物滥用相关的病症。

8. 发明授权

US06743818B2 Cyclobutaindolecarboxamide compounds 失效
标题翻译：环丁二酰胺化合物
公开(公告)号：US06743818B2
公开(公告)日：2004-06-01
申请号：US10195009
申请日：2002-07-12
申请人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Françoise Lejeune , Didier Cussac
发明人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Françoise Lejeune , Didier Cussac
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。

9. 发明授权

US06420413B2 Heterocycloalkylbenzocyclobutane and heteroarylbenzocyclobutane compounds 失效
标题翻译：杂环烷基苯并环丁烷和杂芳基苯并环丁烷化合物
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。

10. 发明授权

US6153625A Indan-1-ol compounds 失效
标题翻译：茚满-1-醇化合物
公开(公告)号：US6153625A
公开(公告)日：2000-11-28
申请号：US374161
申请日：1999-08-13
申请人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi
发明人： Jean-Louis Peglion , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi
IPC分类号： C07D211/58 , A61K31/00 , A61K31/443 , A61K31/445 , A61P3/00 , A61P3/04 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D405/04 , C07D405/12 , C07D409/12 , C07D411/12
CPC分类号： C07D405/04
摘要： A compound selected from those of formula (I): ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy, alkoxy, trihaloalkyl, or any pair may form a heterocycle,R.sub.5 represents hydrogen, alkyl, or arylalkyl,R.sub.6 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, or trihaloalkyl,A, together with the carbons of the phenyl, represents a heterocycle,their isomers and addition pharmaceutically-acceptable acid or base salts thereof, and medicinal products containing the same which are useful in the treatment of pathologies in which 5HT.sub.1B receptors are involved.
摘要翻译：选自式（I）的化合物的化合物：其中：R 1，R 2，R 3和R 4可以相同或不同，表示氢，卤素，烷基，烯基，炔基，羟基，烷氧基，三卤代烷基或任何一对可形成杂环，R 5表示氢，烷基或芳烷基，R 6表示氢，卤素，烷基，羟基，烷氧基或三卤代烷基，A与苯基的碳一起代表杂环，其异构体和加成药学上可接受的酸或其盐类和含有该物质的药物可用于治疗涉及5HT1B受体的病理学。

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