公开(公告)号：EP0898569A1

公开(公告)日：1999-03-03

申请号：EP97920673.0

申请日：1997-04-14

申请人： MERCK PATENT GmbH

发明人： MÄRZ, Joachim ,  BÖTTCHER, Henning ,  DEVANT, Ralf ,  GREINER, Hartmut ,  BARTOSZYK, Gerd ,  HARTING, Jürgen ,  SEYFRIED, Christoph ,  BENGT, Ronny, Andersson ,  HANSSON, Lars, Olov ,  SONESSON, Clas, Ake ,  STJERNLÖF, Nils, Peter

IPC分类号： C07D211 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D207 ,  C07D401 ,  C07D403 ,  C07D405

CPC分类号： C07D401/12 ,  A61K9/19 ,  A61K9/2018 ,  A61K9/2059 ,  C07D401/14 ,  C07D405/14

摘要： The invention relates to novel piperidine and pyrrolidine derivatives of formula (I) in which R?1, R2, R3¿, k, l, m and n have the meanings indicated in Claim 1, and their salts, novel intermediates and processes for the preparation of the compounds according to the invention. The compounds of formula (I) act as 5-HT¿1A? receptor antagonists and exhibit 5-HT reuptake-inhibiting actions and can be used for the production of medicaments.

公开(公告)号：EP0879234A1

公开(公告)日：1998-11-25

申请号：EP97901049.0

申请日：1997-01-17

申请人： MERCK PATENT GmbH

发明人： BÖTTCHER, Henning ,  MÄRZ, Joachim ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  HARTING, Jürgen ,  SEYFRIED, Christoph

IPC分类号： A61K31 ,  A61P25 ,  C07D401

CPC分类号： C07D401/14

摘要： The invention concerns new 1-pyrazol-3-yl-ethyl-4-indol-3-piperidine derivatives of formula (I) where R1 is H or A; R2 is H, a phenyl substituted 1 to 3 times by Hal, NO¿2?, CON(R?4)¿2, SO2N(R4)2, cyanogen, A or R4-O; R3 is H, Hal, A, A-O-, amino, cyanogen, carboxamide, NO¿2?, SO2N(R?4)¿2; R4 is H or A; A is (C¿1?-C6)alkyl or (C1-C6)alkyl containing one to three times substituted by fluorine; Hal is F, Cl, Br or J. The invention also concerns the salts of said derivatives. It has been shown that these compounds have an interesting pharmaceutical activity.

公开(公告)号：EP0281608A1

公开(公告)日：1988-09-14

申请号：EP87906082.0

申请日：1987-09-12

申请人： MERCK PATENT GmbH

发明人： HAUSBERG, Hans-Heinrich ,  BÖTTCHER, Henning ,  SEYFRIED, Christoph ,  BERGMANN, Rolf

IPC分类号： A61K31 ,  A61P5 ,  A61P25 ,  C07D209 ,  C07D401

CPC分类号： C07D401/06

摘要： On peut utiliser 3-[4-(4-phényl-1,2,3,6-tétrahydro-1-pyridyl)-butyl]-5-hydroxy-indol-méthansulfonate dans la thérapie de la maladie de Parkinson. Ces dérivés ont une solubilité particulièrement bonne.

摘要翻译： 3- [4-（4-苯基-1,2,3,6-四氢-1-吡啶基）丁基] -5-羟基吲哚 - 甲磺酸盐可用于治疗帕金森氏病。 这些衍生物具有特别好的溶解性。

公开(公告)号：EP0998474B1

公开(公告)日：2007-02-07

申请号：EP98938671.9

申请日：1998-06-29

申请人： Merck Patent GmbH

发明人： BÖTTCHER, Henning ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  SEYFRIED, Christoph

IPC分类号： C07D405/12 ,  A61K31/495

CPC分类号： C07D405/12

摘要： The invention relates to piperazine derivatives of formula (I), wherein R1, m, k and R2 have the meaning given in Claim 1. Said piperazine derivatives are potent 5-HT¿1A? agonists, have 5-HT-re-uptake inhibiting effects and are suitable for treating and preventing anxiety states, depression, schizophrenia, obsessive thoughts, tardive dyskensia, learning impairments and memory disturbances caused by age, for positively influencing compulsive behaviour, and for treating and combating the effects of cerebral infarctions, such as strokes and cerebral ischaemia.

公开(公告)号：EP1408964B1

公开(公告)日：2007-01-24

申请号：EP02790172.7

申请日：2002-07-10

申请人： Merck Patent GmbH

发明人： BARTOSZYK, Gerd ,  RUSS, Hermann ,  SEYFRIED, Christoph ,  WEBER, Frank

IPC分类号： A61K31/4433 ,  A61P25/16 ,  A61P25/00

CPC分类号： A61K31/4433

摘要： (R/S)-(-/+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof and/or (S)-(+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof are used for the manufacture of a medicament for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders.

公开(公告)号：EP1611107A1

公开(公告)日：2006-01-04

申请号：EP04718264.7

申请日：2004-03-08

申请人： Merck Patent GmbH

发明人： SCHIEMANN, Kai ,  SCHADT, Oliver ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D231/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/4155 ,  A61P25/18

CPC分类号： C07D231/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14

摘要： The invention relates to the compounds of formula (I), and to the salts and solvates thereof, wherein X, R1, R2, R5 and Q are defined as in claim 1, and to the intermediate compounds of formula (IA). The inventive compounds are suitable as ligands of 5 HT receptors.

公开(公告)号：EP1611094A1

公开(公告)日：2006-01-04

申请号：EP04718288.6

申请日：2004-03-08

申请人： Merck Patent GmbH

发明人： SCHADT, Oliver ,  SCHIEMANN, Kai ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D201/00

CPC分类号： C07D231/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14

摘要： The invention relates to compounds of formula (I), in addition to their salts and solvates. In said formula, X, R1, R2, R3, R4, R5 and R6 are defined as cited in claim 1. Said compounds are suitable for use as ligands of 5 HT receptors.

公开(公告)号：EP1299099B1

公开(公告)日：2005-10-26

申请号：EP01902375.3

申请日：2001-02-01

申请人： Merck Patent GmbH

发明人： BARTOSZYK, Gerd ,  RUSS, Hermann ,  SEYFRIED, Christoph ,  WEBER, Frank

IPC分类号： A61K31/353 ,  A61P25/14 ,  A61P25/16

CPC分类号： A61K31/353 ,  A61K31/4433 ,  A61K45/06 ,  A61K2300/00

摘要： (R)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders. A preferred salt is (R)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane hydrochloride.

公开(公告)号：EP1569930A1

公开(公告)日：2005-09-07

申请号：EP03779945.9

申请日：2003-11-17

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  CRASSIER, Helene ,  BÖTTCHER, Henning ,  HEINRICH, Timo ,  SCHIEMANN, Kai ,  LEIBROCK, Joachim ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D417/12 ,  A61K31/433 ,  A61K31/4245 ,  A61P43/00 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.

公开(公告)号：EP1497279A2

公开(公告)日：2005-01-19

申请号：EP03720455.9

申请日：2003-04-11

申请人： MERCK PATENT GmbH

发明人： SCHADT, Oliver ,  BÖTTCHER, Henning ,  LEIBROCK, Joachim ,  SCHIEMANN, Kai ,  HEINRICH, Timo ,  HÖLZEMANN, Günter ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D401/06 ,  A61K31/404 ,  A61P43/00 ,  C07D405/12 ,  C07D209/42 ,  C07D471/04 ,  C07D417/12 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D231/12 ,  C07D209/42 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The invention relates to substituted indoles of formula (I) and to their physiologically safe derivatives and salts, wherein R1, D, E, R12, p, X1, E, G, X2 and Z have the meanings as cited in Claim 1. These substituted indoles and their physiologically safe derivatives and salts have particular effects on the central nervous system, above all, effects that inhibit 5HT-resumption and 5 HTx-agonistic and/or antagonistic effects and, in particular, serotonin, agonistic and antagonistic properties, and can be used as antipsychotics, antidepressants, anxiolytics and/or antihypertensives. These compositions can also be used as excitatory amino acid antagonists for fighting neurodegenerative diseases including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, cerebral ischemias, infarcts or psychoses.