公开(公告)号：US20120302553A1

公开(公告)日：2012-11-29

申请号：US13367065

申请日：2012-02-06

Applicant: Thomas Ruhland ,  Garrick P. Smith ,  Benny Bang-Anderson ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

Inventor： Thomas Ruhland ,  Garrick P. Smith ,  Benny Bang-Anderson ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: 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 classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08110567B2

公开(公告)日：2012-02-07

申请号：US12700521

申请日：2010-02-04

Applicant: Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ejner Knud Moltzen ,  Kim Andersen ,  Ask Puschl

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ejner Knud Moltzen ,  Kim Andersen ,  Ask Puschl

IPC: A61P25/22 ,  A61K31/55 ,  C07D403/00 ,  C07D243/00

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06391882B1

公开(公告)日：2002-05-21

申请号：US09719849

申请日：2001-02-02

Applicant: Ejner Knud Moltzen ,  Ivan Mikkelsen ,  Christian Korg-Jensen

Inventor： Ejner Knud Moltzen ,  Ivan Mikkelsen ,  Christian Korg-Jensen

IPC: A61K31495

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3 to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.

Abstract translation: 其中A是具有式（IIA），（IIB），（IIC）的基团的取代的4-，5-，6-和7-吲哚衍生物，其中X，U，Y，R 3至R 12， Z，W，n和m如上所定义。 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。

公开(公告)号：US5703087A

公开(公告)日：1997-12-30

申请号：US635905

申请日：1996-11-27

Applicant: 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

Inventor： 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: A61K31/4427 ,  A61K31/445 ,  A61P9/12 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D401/14

CPC classification number: C07D401/14

Abstract: The present invention relates to phenylindole compounds of formula I: ##STR1## related to atypical neuroleptic sertindole.

Abstract translation: 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）。

公开(公告)号：US07342015B2

公开(公告)日：2008-03-11

申请号：US10482762

申请日：2002-06-27

Applicant: Mario Rottländer ,  Ejner Knud Moltzen ,  Ivan Mikkelsen ,  Thomas Ruhland ,  Kim Andersen ,  Christian Krog-Jensen

Inventor： Mario Rottländer ,  Ejner Knud Moltzen ,  Ivan Mikkelsen ,  Thomas Ruhland ,  Kim Andersen ,  Christian Krog-Jensen

IPC: A61K31/497 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D401/12 ,  C07D403/12 ,  C07D409/14

Abstract: 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

Abstract translation: 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

公开(公告)号：US06514993B1

公开(公告)日：2003-02-04

申请号：US09424930

申请日：1996-12-09

Applicant: Jens Kristian Perregaard ,  Ejner Knud Moltzen

Inventor： Jens Kristian Perregaard ,  Ejner Knud Moltzen

IPC: A61K314439

CPC classification number: C07D401/06 ,  C07D233/32 ,  C07D233/36

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07138407B2

公开(公告)日：2006-11-21

申请号：US11296835

申请日：2005-12-06

Applicant: Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: A61K31/4409 ,  C07D211/70

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: 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.

公开(公告)号：US06476035B1

公开(公告)日：2002-11-05

申请号：US09491204

申请日：2000-01-25

Applicant: Ejner Knud Moltzen ,  Jens Kristian Perregaard ,  Ivan Mikkelsen ,  Garrick Paul Smith

Inventor： Ejner Knud Moltzen ,  Jens Kristian Perregaard ,  Ivan Mikkelsen ,  Garrick Paul Smith

IPC: A61K31496

CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07683053B2

公开(公告)日：2010-03-23

申请号：US11551188

申请日：2006-10-19

Applicant: Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ejner Knud Moltzen ,  Kim Andersen

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: A61P25/00 ,  A61K31/55 ,  C07D243/08

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07144884B2

公开(公告)日：2006-12-05

申请号：US10488280

申请日：2002-10-02

Applicant: Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: A61K31/495 ,  C07D295/096 ,  C07D241/04 ,  C07D211/54 ,  C07D211/70

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: 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

Abstract translation: 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，包括一般焦虑症和恐慌症以及强迫症