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1.发明公开4-AMINO-5-OXO-8-PHENYL-5H-PYRIDO-[2,3-D]-PYRIMIDIN-DERIVATE ALS INHIBITOREN DER TYROSINKINASEN UND DER RAF-KINASEN ZUR BEHANDLUNG VON TUMOREN 有权4-氨基-5-氧代-8-苯基-5H-吡啶并[2,3-D]嘧啶衍生物作为酪氨酸激酶的肿瘤的治疗抑制剂和Raf激酶
公开(公告)号：EP1809630A1
公开(公告)日：2007-07-25
申请号：EP05800485.4
申请日：2005-10-20
申请人： Merck Patent GmbH
发明人： HOELZEMANN, Guenter , ACKERMANN, Karl-August , CRASSIER, Helene , JONCZYK, Alfred , RAUTENBERG, Wilfried , TARRASON, Gema , ROSELL-VIVES, Elisabet , ADAN, Jaume , CASES, Claudia
IPC分类号： C07D471/04 , C07C275/28 , A61K31/519 , A61P35/00 , A61P35/02
CPC分类号： C07D471/04
摘要： Compounds of formula (I), where R6, R7, R8, R9, Het1, X and X' have the meanings given in claim 1 are tyrosine kinase inhibitors, in particular, of TIE-2, and Raf kinases and can be used, amongst other things, for the treatment of tumours.
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公开(公告)号：EP1202966B1
公开(公告)日：2004-06-09
申请号：EP00964004.6
申请日：2000-08-08
申请人： MERCK PATENT GmbH
发明人： PRÜCHER, Helmut , BÖTTCHER, Henning , ACKERMANN, Karl-August , GOTTSCHLICH, Rudolf , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D211/18 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , A61K31/445 , A61K31/4523 , A61P25/00 , A61P25/16 , A61P25/18
CPC分类号： C07D401/06 , C07D211/22 , C07D405/06 , C07D409/06 , C07D417/06
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3.发明授权4-AMINO-5-OXO-8-PHENYL-5H-PYRIDO-[2,3-D]-PYRIMIDIN-DERIVATE ALS INHIBITOREN DER TYROSINKINASEN UND DER RAF-KINASEN ZUR BEHANDLUNG VON TUMOREN 有权4-氨基-5-氧代-8-苯基-5H-吡啶并[2,3-D]嘧啶衍生物作为酪氨酸激酶的肿瘤的治疗抑制剂和Raf激酶
公开(公告)号：EP1809630B1
公开(公告)日：2009-04-15
申请号：EP05800485.4
申请日：2005-10-20
申请人： Merck Patent GmbH
发明人： HOELZEMANN, Guenter , ACKERMANN, Karl-August , CRASSIER, Helene , JONCZYK, Alfred , RAUTENBERG, Wilfried , TARRASON, Gema , ROSELL-VIVES, Elisabet , ADAN, Jaume , CASES, Claudia
IPC分类号： C07D471/04 , C07C275/28 , A61K31/519 , A61P35/00 , A61P35/02
CPC分类号： C07D471/04
摘要： Compounds of formula (I), where R6, R7, R8, R9, Het1, X and X' have the meanings given in claim 1 are tyrosine kinase inhibitors, in particular, of TIE-2, and Raf kinases and can be used, amongst other things, for the treatment of tumours.
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公开(公告)号：EP1226143A2
公开(公告)日：2002-07-31
申请号：EP00975916.8
申请日：2000-10-25
申请人： MERCK PATENT GmbH
发明人： EGGENWEILER, Hans, Michael , ACKERMANN, Karl-August , JONAS, Rochus , WOLF, Michael , GASSEN, Michael , WELGE, Thomas
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I), wherein R1 means CONR4R5; R2 means H or A; R3 means Hal; R?4 and R5¿ each mean H or A1, independently of each other; Hal is F, Cl, Br or I, A means alkyl with 1-4 C atoms, A1 means alkyl with 1-10 C atoms; and X means alkylene with 1-4 C atoms, an ethylene group also being replaceable by a double or triple bond, and their physiologically compatible salts and/or solvates, used as phosphodiesterase VII inhibitors. The invention also relates to their use for producing a medicament.
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5.发明公开VERFAHREN ZUR HERSTELLUNG VON ENANTIOMERENREINEM N-METHYL- N- (1S)- 1-PHENYL- 2-((3S)-3- HYDROXYPYRROLIDIN- 1-YL)ETHYL]- 2,2- DIPHENYLACETAMID 有权N-（1S）-1-苯基-2 - （（3S）-3-羟基吡咯烷-1-基）乙基] -2,2-二苯基乙酰胺
公开(公告)号：EP1073634A1
公开(公告)日：2001-02-07
申请号：EP99923421.4
申请日：1999-04-16
申请人： MERCK PATENT GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , ACKERMANN, Karl-August , GOTTSCHLICH, Rudolf , STEIN, Ingeborg , BUDAK, Jens
IPC分类号： C07D207/12 , A61K31/40 , C07B43/06 , C07B35/02
CPC分类号： C07B35/02 , A61K31/40 , C07B43/06 , C07D207/12 , Y02P20/55
摘要： The invention relates to a new method for producing N-methyl-N- [(1S)- 1-phenyl-2- ((3S)-3- hydroxypyrrolidine- 1-yl)ethyl]- 2,2-diphenyl acetamide or N-methyl- N-[(1R)- 1-phenyl-2- ((3R)-3- hydroxypyrrolidine- 1-yl)ethyl]- 2,2-diphenyl acetamide and to the new compounds N-methyl- N-[(1S)- 1-phenyl- 2-((3S)- 3-hydroxypyrrolidine- 1-yl)- ethane] and N-methyl-N- [(1R)- 1-phenyl-2- ((3R)-3- hydroxypyrrolidine- 1-yl)- ethane] produced as intermediate products.
摘要翻译： 本发明涉及制备N-甲基-N - [（1S）-1-苯基-2 - （（3S）-3-羟基吡咯烷-1-基）乙基] -2,2-二苯基乙酰胺或N -N - [（1R）-1-苯基-2 - （（3R）-3-羟基吡咯烷-1-基）乙基] -2,2-二苯基乙酰胺和新化合物N-甲基-N- [ （1S）-1-苯基-2 - （（3S）-3-羟基吡咯烷-1-基） - 乙烷]和N-甲基-N - [（1R）-1-苯基-2 - （（3R）-3 - 羟基吡咯烷-1-基） - 乙烷]作为中间产物产生。
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公开(公告)号：EP1682548A1
公开(公告)日：2006-07-26
申请号：EP04790407.3
申请日：2004-10-14
申请人： Merck Patent GmbH
发明人： HÖLZEMANN, Günter , CRASSIER, Helene , ACKERMANN, Karl-August , STÄHLE, Wolfgang , JONCZYK, Alfred , RAUTENBERG, Wilfried , MITJANS, Francesc , ROSELL-VIVES, Elisabet , ADAN, Jaume , SOLER RIERA, Marta
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein R1, R2 , R3 , R4 , R5, R6 , R7 , R8, R9, X and X' have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumours.
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公开(公告)号：EP1626967A1
公开(公告)日：2006-02-22
申请号：EP04718277.9
申请日：2004-03-08
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , ACKERMANN, Karl-August , ARLT, Michael , FINSINGER, Dirk , SCHADT, Oliver , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D401/04 , A61K31/415 , A61P25/28
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： The invention relates to the compounds of formula (I) and the salts and solvates thereof, wherein X, R1, R2, R3, R4 and R5 are defined as in claim 1. The inventive compounds are suitable as ligands of 5 HT receptors.
摘要翻译： 本发明涉及式（I）化合物及其盐和溶剂化物，其中X，R 1，R 2，R 3，R 4和R 5如权利要求1中所定义。本发明化合物适合作为5HT受体的配体。
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公开(公告)号：EP1226143B1
公开(公告)日：2003-04-02
申请号：EP00975916.8
申请日：2000-10-25
申请人： MERCK PATENT GmbH
发明人： EGGENWEILER, Hans, Michael , ACKERMANN, Karl-August , JONAS, Rochus , WOLF, Michael , GASSEN, Michael , WELGE, Thomas
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I), wherein R1 means CONR4R5; R2 means H or A; R3 means Hal; R?4 and R5¿ each mean H or A1, independently of each other; Hal is F, Cl, Br or I, A means alkyl with 1-4 C atoms, A1 means alkyl with 1-10 C atoms; and X means alkylene with 1-4 C atoms, an ethylene group also being replaceable by a double or triple bond, and their physiologically compatible salts and/or solvates, used as phosphodiesterase VII inhibitors. The invention also relates to their use for producing a medicament.
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公开(公告)号：EP1656377A1
公开(公告)日：2006-05-17
申请号：EP04741135.0
申请日：2004-07-19
申请人： Merck Patent GmbH
发明人： HÖLZEMANN, Günter , CRASSIER, Helene , ACKERMANN, Karl-August , STÄHLE, Wolfgang , JONCZYK, Alfred , RAUTENBERG, Wilfried , MITJANS, Francesco , ROSELL-VIVES, Elisabet , ADAN, Jaume , SOLER, Marta
IPC分类号： C07D471/06 , C07D471/04 , C07D417/12 , C07D413/12 , C07D405/12 , C07D403/12 , C07D235/30 , A61K31/433 , A61K31/428 , A61K31/4245 , A61K31/4184
CPC分类号： C07D403/12 , C07D235/30 , C07D405/12 , C07D417/12 , C07D471/04 , C07D471/06
摘要： Novel compounds of formula (I) are disclosed, where R1, R1', L, Y, m and p have the meanings given in claim 1, which are inhibitors of tyrosine kinases, in particular, TIE-2 and Raf kinases and can be used for the treatment of tumours.
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10.发明公开CHROMENONDERIVATE UND IHRE VERWENDUNG ZUR BEHANDLUNG VON KRANKHEITEN IM ZUSAMMENHANG MIT 5-HTA1-REZEPTOREN UND /ODER DOPAMIN-D2-REZEPTOREN 审中-公开CHROMENONDERIVATE及其用于疾病治疗与5-HTA1受体和/或多巴胺D2受体有关的
公开(公告)号：EP1311503A1
公开(公告)日：2003-05-21
申请号：EP01969491.8
申请日：2001-07-24
申请人： MERCK PATENT GmbH
发明人： GOTTSCHLICH, Rudolf , ACKERMANN, Karl-August , PRÜCHER, Helmut , SEYFRIED, Christoph , BARTOSZYK, Gert , VAN AMSTERDAM, Christoph
IPC分类号： C07D405/14 , A61P25/18
CPC分类号： C07D405/12
摘要： The invention relates to novel chromenone derivatives of formula (I), wherein Y, X, R?1, R2, R3¿ and n have one of the meanings cited in Patent Claim No. 1, serving as inhibitors of the 5-HT¿1A? receptor and of the dopamine D2 receptor.
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