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1. 发明授权

US06369060B1 Indoline derivatives useful as 5-HT-2C receptor antagonists 失效
标题翻译：可用作5-HT-2C受体拮抗剂的二氢吲哚衍生物
公开(公告)号：US06369060B1
公开(公告)日：2002-04-09
申请号：US09202780
申请日：1998-12-21
申请人： Steven Mark Bromidge , Ian Thomson Forbes
发明人： Steven Mark Bromidge , Ian Thomson Forbes
IPC分类号： A61K31501
CPC分类号： C07D401/14
摘要： The invention relates to compounds of formula (I) or a salt thereof wherein X is CH or N; R1 is hydrogen or C1-6 alkyl; R2 and R3 groups are independently C1-6 alkyl, or trifluoromethyl, having pharmacological activity, processes for their preparation, compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
摘要翻译：本发明涉及式（I）化合物或其盐，其中X是CH或N; R1是氢或C1-6烷基; R 2和R 3基团独立地为具有药理学活性的C 1-6烷基或三氟甲基，其制备方法，含有它们的组合物及其在治疗CNS疾病如焦虑症中的应用。

2. 发明授权

US06548504B1 Compounds 失效
标题翻译：化合物
公开(公告)号：US06548504B1
公开(公告)日：2003-04-15
申请号：US09600558
申请日：2000-07-19
申请人： Steven Mark Bromidge , Stephen Frederick Moss
发明人： Steven Mark Bromidge , Stephen Frederick Moss
IPC分类号： A61K31495
CPC分类号： C07D295/096
摘要： The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms or is an arylC1-6alkyl group, and Rb is hydrogen or C1-6alkyl;
摘要翻译：因此，本发明在第一方面提供式（I）化合物或其盐：其中基团D选自下式（A），（B）或（C）中的基团：其中P 是环中含有至多20个碳原子的单环，双环或三环脂环; A是单键，C 1-6亚烷基或C 2-6亚烯基; R 1是卤素，任选地被一个或更多个氟原子，C 3-6环烷基，C 1-6烷氧基，OCF 3，羟基，羟基C 1-6烷基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷酰基，氨基，烷基氨基或二烷基氨基，SR 11，其中R 11是氢或C 1-6烷基或R 1为芳基，芳基C 1-6烷基，双环杂环或为各自含有1至4个选自氧，氮或硫的杂原子的5至7元杂环; n为0,1,2或3; 和R 2是氢，C 1-6烷基，芳基，芳基C 1-6烷基或C 3-6环烷基; 其中R a是含有1至20个碳原子的烷基或芳基C 1-6烷基，R b是氢或C 1-6烷基;

3. 发明授权

US5773619A Process for the preparation of azabicycloc derivatives 失效
标题翻译：制备氮杂双环衍生物的方法
公开(公告)号：US5773619A
公开(公告)日：1998-06-30
申请号：US439616
申请日：1995-05-12
申请人： Steven Mark Bromidge , Martyn Voyle , Erol Ali Faruk , Mark Jason Hughes , John Kitteringham , Gary Thomas Borrett
发明人： Steven Mark Bromidge , Martyn Voyle , Erol Ali Faruk , Mark Jason Hughes , John Kitteringham , Gary Thomas Borrett
IPC分类号： C07D487/18 , C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents ##STR2## in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl or a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4 ; and R.sub.3 is CN; said process comprising reacting a compound of formula (II): ##STR3## wherein R.sub.1 ' is R.sub.1 or a group convertible thereto, and R.sub.3 ' is an electron withdrawing group, with a source of nitrous acid, and thereafter converting the resulting .dbd.NOH group to .dbd.NR.sub.2 wherein R.sub.2 is as defined in formula (I), converting R.sub.1 ' and R.sub.3 ' when other than R.sub.1 and R.sub.3 to R.sub.1 and R.sub.3, and thereafter optionally forming a pharmaceutically acceptable salt.
摘要翻译：制备式（I）化合物或其药学上可接受的盐的方法：其中R 1表示，其中r表示2至4的整数，s表示1或2，t表示表示0或1; R2是OR4，其中R4是C1-4烷基，C2-4烯基或C2-4炔基或OCOR5，其中R5是氢或R4; R3为CN; 所述方法包括使式（II）化合物：其中R 1'为R 1或可转换的基团，并且R 3'为吸电子基团，并与亚硝酸源反应，然后将所得 = NOH基团= NR 2，其中R 2如式（I）中所定义，当R 1和R 3不同于R 1和R 3时，将R 1'和R 3'转化，然后任选形成药学上可接受的盐。

4. 发明申请

US20100004452A1 5-QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIRMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
标题翻译： 5-Quinolinone衍生物作为5HT1A受体调节剂，用于治疗性功能障碍，认知障碍，心理障碍，异常，呕吐等。
公开(公告)号：US20100004452A1
公开(公告)日：2010-01-07
申请号：US12442148
申请日：2007-09-24
申请人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
发明人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
IPC分类号： C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D487/08
摘要： Disclosed are compounds of formula (I) wherein R1 is C1-6alkyl, halo or haloC1-6alkyl; R2 is hydrogen or C1-6alkyl; is a single or double bond; each R3 and R4, which may be the same or different, are hydrogen, C1-6alkyl or haloC1-6alkyl; wherein i) when is a double bond p and q are 1, and ii) when is a single bond, p and q are 2, and one of R3 and one of R4, together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R5, which may be the same or different, is C1-6alkyl or halo; or two R5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R6 which may be the same or different, is C1-6alkyl or halo; and m is 0, 1, 2 or 3.
摘要翻译：公开了式（I）的化合物，其中R 1是C 1-6烷基，卤素或卤代C 1-6烷基; R2是氢或C1-6烷基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US20100004452A1-20100107-P00001.TIF“img-content =”character“img-format =”tif“/> 是单键或双键; 每个R 3和R 4可以相同或不同，是氢，C 1-6烷基或卤代C 1-6烷基; 其中i）当是双键p，q是1，ii）当是单键，p和q是2，R 3和R 4中的一个连同它们的互连原子一起形成环丙烷环，被一个或两个卤素或甲基取代，这些基团可以相同或不同; X是CH或N; 当存在时，每个可以相同或不同的R 5是C 1-6烷基或卤素; 或两个R5基团可以连接形成桥，该桥包含一个或两个原子; n为0,1,2或3; 当存在每个可以相同或不同的R 6是C 1-6烷基或卤素时; m为0,1,2或3。

5. 发明授权

US06313145B1 Indoline derivatives useful as 5-HT-2C receptor antagonists 失效
标题翻译：可用作5-HT-2C受体拮抗剂的二氢吲哚衍生物
公开(公告)号：US06313145B1
公开(公告)日：2001-11-06
申请号：US09202772
申请日：1998-12-21
申请人： Steven Mark Bromidge
发明人： Steven Mark Bromidge
IPC分类号： A61K314439
CPC分类号： C07D401/14
摘要： Indoline derivatives useful as 5HT2C receptor antagonists and methods of using them to treat various CNS disorders are provided.
摘要翻译：提供了可用作5HT2C受体拮抗剂的二氢吲哚衍生物和使用它们治疗各种CNS疾病的方法。

6. 发明授权

US5981545A N-linked azabicyclic heterocycles useful for treating dementia 失效
标题翻译：用于治疗痴呆的N-连接的氮杂双环杂环
公开(公告)号：US5981545A
公开(公告)日：1999-11-09
申请号：US594034
申请日：1990-10-04
申请人： Sarah Margaret Jenkins , Harry John Wadsworth , Barry Sidney Orlek , Steven Mark Bromidge
发明人： Sarah Margaret Jenkins , Harry John Wadsworth , Barry Sidney Orlek , Steven Mark Bromidge
IPC分类号： C07D487/08 , A61K31/41 , A61K31/435 , A61P25/28 , C07D453/02 , C07D471/08 , C07D221/22
CPC分类号： C07D471/08 , C07D453/02
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises zero, one or two nitrogen atoms, Q being optionally C-substituted by a group R.sub.1 selected from halogen, CN, OR.sub.2, SR.sub.2, N(R.sub.2).sub.2, NHCOR.sub.2, NHCOOCH.sub.3, NHCOOC.sub.2 H.sub.5, NHOR.sub.2, N.sub.3, NHNH.sub.2, NO.sub.2, COR.sub.2, COR.sub.3, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, cyclopropyl or C.sub.1-2 alkyl optionally substituted with OR.sub.2, N(R.sub.2).sub.2, SR.sub.2, CO.sub.2 R.sub.2, CON(R.sub.2).sub.2 or one, two or three halogen atoms, in which each R.sub.2 is independently hydrogen or C.sub.1-2 alkyl and R.sub.3 is OR.sub.2, NH.sub.2 or NHR.sub.2 ; r represents an integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0 or 1; R.sub.a and R.sub.b each represent hydrogen or, when X is hydrogen, optionally together represent a bond; with the proviso that when Y is hydrogen s is 1.
摘要翻译：式（I）化合物或其药学上可接受的盐：其中X和Y中的一个代表氢，另一个表示Z，其中Z是其中Q表示完成5元芳族的3元二价残基的基团并且包含0,1或2个氮原子，Q任选被选自卤素，CN，OR2，SR2，N（R2）2，NHCOR2，NHCOOCH3，NHCOOC2H5，NHOR2，N3，NHNH2，NO2的基团R1取代的Q。，COR2，COR3，C2-4烯基，C2-4炔基，环丙基或任选被OR2，N（R2）2，SR2，CO2R2，CON（R2）2或一个，两个或三个卤素原子取代的C 1-2烷基，其中每个R 2独立地是氢或C 1-2烷基，R 3是OR 2，NH 2或NHR 2; r表示2或3的整数，s表示1或2的整数，t表示0或1; Ra和Rb各自表示氢，或当X为氢时，可选地一起表示键; 条件是当Y为氢时，s为1。

7. 发明申请

US20100286152A1 N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译：作为GHRELIN受体的调节剂的N-苯基水杨酸
公开(公告)号：US20100286152A1
公开(公告)日：2010-11-11
申请号：US12602829
申请日：2008-06-05
申请人： Giovanni Bernasconi , Steven Mark Bromidge , Andrew James Carpenter , Lucilla D'Adamo , Romano Di Fabio , Sebastien Guery , Francesca Pavone , Alfonso Pozzan , Marilisa Rinaldi , Fabio Maria Sabbatini , Yves St-Denis
发明人： Giovanni Bernasconi , Steven Mark Bromidge , Andrew James Carpenter , Lucilla D'Adamo , Romano Di Fabio , Sebastien Guery , Francesca Pavone , Alfonso Pozzan , Marilisa Rinaldi , Fabio Maria Sabbatini , Yves St-Denis
IPC分类号： A61K31/495 , C07D409/06 , C07D405/06 , C07D295/13 , C07D401/06 , C07D403/06 , C07D211/28 , A61K31/496 , A61K31/4525 , A61K31/445 , A61K31/506 , A61P3/00
CPC分类号： C07D333/76 , C07D211/34 , C07D213/56 , C07D213/61 , C07D239/26 , C07D295/15 , C07D307/81 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/60 , C07D405/06 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂合物，

8. 发明申请

US20090076274A1 BENZOXAZINONE DERIVATIVES, PREPARATION THEREOF AND USES IN THE TREATMENT OF CNS AND OTHER DISORDERS 审中-公开
标题翻译：苄唑胺酮衍生物，其制备方法和用于治疗CNS和其他疾病的用途
公开(公告)号：US20090076274A1
公开(公告)日：2009-03-19
申请号：US12269313
申请日：2008-11-12
申请人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Mark Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
发明人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Mark Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
IPC分类号： C07D405/02
CPC分类号： C07D413/12 , C07D265/36 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Intermediates useful in the preparation of compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A, R1, R2, R3, , p, q, and X are as defined in the specification.
摘要翻译：公开了可用于制备式（I）化合物及其可药用盐的中间体：其中A，R1，R2，R3，，p，q和X如规范中所定义。

9. 发明申请

US20080280919A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 失效
标题翻译：具有5HT1型受体亲和力的喹啉和喹唑啉衍生物
公开(公告)号：US20080280919A1
公开(公告)日：2008-11-13
申请号：US12166547
申请日：2008-07-02
申请人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Mark Bromidge , Alessandro Falchi , Colin Philip Leslie , Giancarlo Merlo , Domenica Antonia Pizzi , Marilisa Rinaldi , Luigi Piero Stasi , Jessica Tibasco , Antonio Kuok Keong Vong , Simon Edward Ward
发明人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Mark Bromidge , Alessandro Falchi , Colin Philip Leslie , Giancarlo Merlo , Domenica Antonia Pizzi , Marilisa Rinaldi , Luigi Piero Stasi , Jessica Tibasco , Antonio Kuok Keong Vong , Simon Edward Ward
IPC分类号： A61K31/496 , A61P25/24 , A61P25/22
CPC分类号： C07D401/12 , C04B35/632
摘要： Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety. wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
摘要翻译：公开的是使用式（I）化合物与其它活性物质组合用于治疗CNS疾病如抑郁症或焦虑症的方法。其中R 1，m，X，R 2，n，W，p，Y，Z，R 3，R 4 R 5和q具有如在说明书中定义的含义。

10. 发明授权

US5808075A Process for the preparation of azabicyclic derivatives 失效
标题翻译：制备氮杂双环衍生物的方法
公开(公告)号：US5808075A
公开(公告)日：1998-09-15
申请号：US737427
申请日：1996-11-12
申请人： Steven Mark Bromidge , Martyn Voyle , Erol Ali Faruk , Mark Jason Hughes , John Kitteringham , Gary Thomas Borrett
发明人： Steven Mark Bromidge , Martyn Voyle , Erol Ali Faruk , Mark Jason Hughes , John Kitteringham , Gary Thomas Borrett
IPC分类号： C07D487/18 , C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R.sub.1 represents (a) in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl or a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4 ; and R.sub.3 is CN; said process comprising reacting a compound of formula (II) wherein R.sub.1 ' is R.sub.1 or a group convertible thereto, and R.sub.3 ' is an electron withdrawing group, with a source of nitrous acid, and thereafter converting the resulting .dbd.NOH group to .dbd.NR.sub.2 wherein R.sub.2 is as defined in formula (I), converting R.sub.1 ' and R.sub.3 ' when other than R.sub.1 and R.sub.3 to R.sub.1 and R.sub.3, and thereafter optionally forming a pharmaceutically acceptable salt.
摘要翻译： PCT No.PCT / EP95 / 01757 Sec。 371日期：1996年11月12日 102（e）日期1996年11月12日PCT提交1995年5月9日PCT公布。公开号WO95 / 31456 （I）制备式（I）化合物或其药学上可接受的盐的方法，其中R1表示（a）在其中r表示2〜4的整数，s表示1或2，t表示0或1; R2是OR4，其中R4是C1-4烷基，C2-4链烯基或C2-4炔基或OCOR5，其中R5是氢或R4; R3为CN; 所述方法包括使式（II）化合物（其中R 1'为R 1或可转化的基团）和R 3'为吸电子基团，与亚硝酸源反应，然后将所得= NOH基团转化为= NR2，其中 R 2如式（I）中所定义，当R 1和R 3不同于R 1和R 3时，将R 1'和R 3'转化，然后任选形成药学上可接受的盐。

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