公开(公告)号：EP1569930B1

公开(公告)日：2007-01-03

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：EP1592687A1

公开(公告)日：2005-11-09

申请号：EP04701298.4

申请日：2004-01-10

申请人： Merck Patent GmbH

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

IPC分类号： C07D405/12 ,  A61K31/40 ,  A61P25/18

CPC分类号： C07D405/12

摘要： The invention relates to novel benzofurane derivatives of formula (I) wherein R1, R2, X, Y, Z and m have the designations cited in patent claim 1. Said compounds have a strong affinity towards 5-HT1A receptors, inhibit the resumption of serotonin, have serotonin-agonistic and serotonin-antagonistic characteristics, and are suitable for using as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics.

公开(公告)号：EP1366039B1

公开(公告)日：2005-09-07

申请号：EP01273302.8

申请日：2001-12-24

申请人： Merck Patent GmbH

发明人： BÖTTCHER, Henning ,  BARTOSZYK, Gerd ,  HARTING, Jürgen ,  VAN AMSTERDAM, Christoph ,  SEYFRIED, Christoph

IPC分类号： C07D403/06 ,  A61K31/495 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D215/48 ,  A61K31/495 ,  C07D217/26

公开(公告)号：EP1425008A1

公开(公告)日：2004-06-09

申请号：EP02767352.4

申请日：2002-08-09

申请人： MERCK PATENT GmbH

发明人： BARTOSZYK, Gerd ,  RUSS, Hermann ,  SEYFRIED, Christoph ,  BÖTTCHER, Henning ,  BOKEL, Heinz-Hermann ,  SCHMID-GROSSMANN, Uschi

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

CPC分类号： A61K31/353

摘要： Substituted aminomethyl chromans, one of their optical isomers or pharmaceutically acceptable salts, used for the manufacture of a medicament for the treatment of adverse effects of anti-Parkinsonian drugs in extrapyramidal movement disorders and/or for the manufacture of a medicament for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics. A preferred compound is (-)-(R)-2-{4-[[3,4-dihydro-2H-benzopyran-2-yl)-methyl!amino!butyl}-1,2-benzoisothiazol-3-(2H)-on-1,1-dioxide or a physiologically acceptable salt thereof.

公开(公告)号：EP1140898B1

公开(公告)日：2002-08-28

申请号：EP98966851.2

申请日：1998-12-22

申请人： MERCK PATENT GmbH

发明人： MATZEN, Lisa ,  BÖTTCHER, Henning ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  HARTING, Jürgen ,  RAUTENBERG, Wilfried

IPC分类号： C07D401/04 ,  A61K31/40 ,  C07D401/06 ,  C07D209/14 ,  C07D401/14 ,  C07D209/16

CPC分类号： C07D401/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/06 ,  C07D401/14

公开(公告)号：EP0931067A1

公开(公告)日：1999-07-28

申请号：EP97944823.0

申请日：1997-09-03

申请人： MERCK PATENT GmbH

发明人： ARLT, Michael ,  BÖTTCHER, Henning ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D295 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D213 ,  C07D239 ,  C07D241 ,  C07D307 ,  C07D401 ,  C07D405 ,  C07D409

CPC分类号： C07D213/74 ,  C07D213/38 ,  C07D239/42 ,  C07D295/073 ,  C07D295/096 ,  C07D295/155 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： Piperazine derivatives having formula (I), wherein R?1 and R2¿ have the meanings given in claim 1, are dopamine ligands with D4 receptor selectivity and are suited for treatment and prophylaxis of anxiety states, depression, schizophrenia, obsessive ideas, Parkinson's disease, tardive diskinesia, nausea and gastro-intestinal tract disorders.

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：EP1497279B1

公开(公告)日：2011-03-09

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.