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1. 发明授权

US5703087A Phenyl indole compounds 失效
标题翻译：苯基吲哚化合物
公开(公告)号：US5703087A
公开(公告)日：1997-12-30
申请号：US635905
申请日：1996-11-27
申请人： Jens Kristian Perregaard , Ejner Knud Moltzen , Kim Andersen , Henrik Pedersen , Klaus Peter B.o slashed.ges.o slashed. , Andre Pernet , Barbara Bopp , Darcy Mulford , Kiyoshi Sakamoto
发明人： Jens Kristian Perregaard , Ejner Knud Moltzen , Kim Andersen , Henrik Pedersen , Klaus Peter B.o slashed.ges.o slashed. , Andre Pernet , Barbara Bopp , Darcy Mulford , Kiyoshi Sakamoto
IPC分类号： A61K31/4427 , A61K31/445 , A61P9/12 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D401/14
CPC分类号： C07D401/14
摘要： The present invention relates to phenylindole compounds of formula I: ##STR1## related to atypical neuroleptic sertindole.
摘要翻译： PCT No.PCT / DK94 / 00407 Sec。 371日期：1996年11月27日 102（e）日期1996年11月27日PCT 1994年10月28日PCT公布。第WO95 / 12591号公报日期：1995年5月11日本发明涉及式I的苯基吲哚化合物：与非典型精神抑制索吲哚有关的（I）。

2. 发明授权

US06476035B1 Indole and 2,3-dihydroindole derivatives, their preparation and use 失效
标题翻译：吲哚和2,3-二氢吲哚衍生物，其制备和用途
公开(公告)号：US06476035B1
公开(公告)日：2002-11-05
申请号：US09491204
申请日：2000-01-25
申请人： Ejner Knud Moltzen , Jens Kristian Perregaard , Ivan Mikkelsen , Garrick Paul Smith
发明人： Ejner Knud Moltzen , Jens Kristian Perregaard , Ivan Mikkelsen , Garrick Paul Smith
IPC分类号： A61K31496
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12
摘要： The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.
摘要翻译：本发明涉及具有式（I）的吲哚和2,3-二氢吲哚衍生物或其任何对映体或其任何混合物或其酸加成盐，其中A，R 1，R 2，R 3，W，X ，Y和Z如说明书所述。该化合物是有效的5-羟色胺再摄取抑制剂，具有5-HT1A受体拮抗作用。

3. 发明授权

US06514993B1 Serotonin 5-HT1A and dopamin D2 receptor ligands 失效
标题翻译： 5-羟色胺5-HT1A和多巴胺D2受体配体
公开(公告)号：US06514993B1
公开(公告)日：2003-02-04
申请号：US09424930
申请日：1996-12-09
申请人： Jens Kristian Perregaard , Ejner Knud Moltzen
发明人： Jens Kristian Perregaard , Ejner Knud Moltzen
IPC分类号： A61K314439
CPC分类号： C07D401/06 , C07D233/32 , C07D233/36
摘要： The present invention relates to a novel series of 4-phenylpiperazines, 4-phenylpiperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compounds of general formula (I) wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R1 is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R2-R5 are optional substituents; R9 and R10 are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR6R7, or NR8 wherein R6, R7, and R8 are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R6 and R7 constitute a 3-7 membered spiro ring; Z is —(CH2)m—, m being 2 or 3 or Z is —CH═CH—; X is N, C or CH; show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.
摘要翻译：本发明涉及通式（I）的新一系列4-苯基哌嗪，4-苯基哌啶和4-苯基-1,2,3,6-四氢吡啶化合物，其中A是亚烷基，亚烯基，亚炔基和C3-7 亚环烷基 R 1是C 3-10烷基，烯基或炔基，环烷基（烯）基，环烷基（烯）基 - 烯（烯/炔）基，三氟甲磺酰基或烷基磺酰基，R 2 -R 5是任选的取代基; R9和R10是氢，烷基或一起形成乙烯或丙烯桥; W为O或S; V是O，S，CR 6 R 7或NR 8，其中R 6，R 7和R 8是氢或烷基，烯基，环烷基，环烷基烷基，任选取代的芳烷基或芳基，或R 6和R 7构成3-7元螺环; Z是 - （CH 2）m - ，m是2或3或Z是-CH = CH-; X为N，C或CH; 显示对中枢5-羟色胺5-HT1A和多巴胺D2受体的影响。因此，新化合物可用于治疗某些精神病和神经障碍，特别是精神病。

4. 发明授权

US06727263B2 Indole and 2,3-dihydroindole derivatives, their preparation and use 失效
标题翻译：吲哚和2,3-二氢吲哚衍生物，其制备和用途
公开(公告)号：US06727263B2
公开(公告)日：2004-04-27
申请号：US10223046
申请日：2002-08-16
申请人： Ejner Knud Moltzen , Jens Kristian Perregaard , Ivan Mikkelsen , Garrick Paul Smith
发明人： Ejner Knud Moltzen , Jens Kristian Perregaard , Ivan Mikkelsen , Garrick Paul Smith
IPC分类号： A61K314439
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12
摘要： The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.
摘要翻译：本发明涉及具有式（I）的吲哚和2,3-二氢吲哚衍生物或其任何对映体或其任何混合物或其酸加成盐，其中A，R 1，R 2， R 3，W，X，Y和Z如说明书所述。该化合物是有效的5-羟色胺再摄取抑制剂，具有5-HT1A受体拮抗作用。

5. 再颁专利

USRE36374E 1,2,3-triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists 失效
公开(公告)号：USRE36374E
公开(公告)日：1999-11-02
申请号：US648240
申请日：1996-05-13
申请人： Klaus Peter Bogeso , Klaus Gundertofte , Ejner Knud Moltzen , Henrik Pedersen
发明人： Klaus Peter Bogeso , Klaus Gundertofte , Ejner Knud Moltzen , Henrik Pedersen
IPC分类号： A61K31/4427 , A61K31/445 , A61P21/00 , A61P25/02 , A61P25/28 , C07D401/04 , C07D413/04 , C07D417/04
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to novel compounds of the following formula, where the dotted line designates in optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,4- or 1,3,4-oxadiazole,R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifuoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula 1, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.

6. 发明申请

US20120302553A1 PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS 有权
标题翻译：作为丝氨酸还原抑制剂的苯基哌嗪衍生物
公开(公告)号：US20120302553A1
公开(公告)日：2012-11-29
申请号：US13367065
申请日：2012-02-06
申请人： Thomas Ruhland , Garrick P. Smith , Benny Bang-Anderson , Ask Puschl , Ejner Knud Moltzen , Kim Andersen
发明人： Thomas Ruhland , Garrick P. Smith , Benny Bang-Anderson , Ask Puschl , Ejner Knud Moltzen , Kim Andersen
IPC分类号： A61K31/551 , A61K31/495 , C07D243/08 , C07D213/32 , C07D241/04 , C07D211/20 , A61K31/451 , A61P25/24 , A61P25/22 , A61P25/00 , C07D295/096 , A61K31/4418
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

7. 发明授权

US08110567B2 Phenyl-piperazine derivatives as serotonin reuptake inhibitors 有权
标题翻译：苯基哌嗪衍生物作为血清素再摄取抑制剂
公开(公告)号：US08110567B2
公开(公告)日：2012-02-07
申请号：US12700521
申请日：2010-02-04
申请人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen , Ask Puschl
发明人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen , Ask Puschl
IPC分类号： A61P25/22 , A61K31/55 , C07D403/00 , C07D243/00
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

8. 发明授权

US07342015B2 Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US07342015B2
公开(公告)日：2008-03-11
申请号：US10482762
申请日：2002-06-27
申请人： Mario Rottländer , Ejner Knud Moltzen , Ivan Mikkelsen , Thomas Ruhland , Kim Andersen , Christian Krog-Jensen
发明人： Mario Rottländer , Ejner Knud Moltzen , Ivan Mikkelsen , Thomas Ruhland , Kim Andersen , Christian Krog-Jensen
IPC分类号： A61K31/497 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12 , C07D409/14
摘要： A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disorders, and neurological disorders such as psychosis
摘要翻译：具有式（I）的杂芳基衍生物。本发明的化合物被认为可用于治疗情绪障碍，例如一般性焦虑障碍，恐慌症，强迫症，抑郁症，社会恐惧症和进食障碍，以及神经系统疾病如精神病

9. 发明授权

US07138407B2 Phenyl-piperazine derivatives as serotonin reuptake inhibitors 有权
公开(公告)号：US07138407B2
公开(公告)日：2006-11-21
申请号：US11296835
申请日：2005-12-06
申请人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ask Puschl , Ejner Knud Moltzen , Kim Andersen
发明人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ask Puschl , Ejner Knud Moltzen , Kim Andersen
IPC分类号： A61K31/4409 , C07D211/70
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

10. 发明授权

US07683053B2 Phenyl-piperazine derivatives as serotonin reuptake inhibitors 有权
标题翻译：苯基哌嗪衍生物作为血清素再摄取抑制剂
公开(公告)号：US07683053B2
公开(公告)日：2010-03-23
申请号：US11551188
申请日：2006-10-19
申请人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen
发明人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen
IPC分类号： A61P25/00 , A61K31/55 , C07D243/08
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

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