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.

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.

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.

公开(公告)号：EP2167128B1

公开(公告)日：2012-10-24

申请号：EP08784834.7

申请日：2008-07-17

申请人： Merck Patent GmbH

发明人： GOODMAN, Simon ,  HAHN, Diane ,  MITJANS, Francesc ,  ADAN, Jaume ,  LO, Kin-Ming

IPC分类号： A61K39/395 ,  A61P35/00 ,  C07K16/28

CPC分类号： C07K16/2842 ,  A61K39/3955 ,  A61K2039/505 ,  A61K2039/507 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/72 ,  C07K2317/76 ,  C07K2317/90 ,  C07K2317/92 ,  A61K2300/00

公开(公告)号：EP2167128A2

公开(公告)日：2010-03-31

申请号：EP08784834.7

申请日：2008-07-17

申请人： Merck Patent GmbH

发明人： GOODMAN, Simon ,  HAHN, Diane ,  MITJANS, Francesc ,  ADAN, Jaume ,  LO, Kin-Ming

IPC分类号： A61K39/395 ,  A61P35/00 ,  C07K16/28

CPC分类号： C07K16/2842 ,  A61K39/3955 ,  A61K2039/505 ,  A61K2039/507 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/72 ,  C07K2317/76 ,  C07K2317/90 ,  C07K2317/92 ,  A61K2300/00

摘要： The invention relates to engineered antibodies which specifically bind to integrin receptors, especially the alpha V integrin receptor subunit. The antibodies comprise the antigen binding sites (CDRs) of a known mouse anti-integrin antibody, as well as hybrid light chain variable sequences, mutated heavy chain variable sequences (Frs) and modified heavy chain constant sequences. The novel antibodies have improved immunogenic and expression properties and elicit excellent anti-angiogenic as well as anti-tumor activities in humans in monotherapy but also and above all in combination with other angiogenesis and tumor inhibiting agents.

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.

公开(公告)号：EP1682548B1

公开(公告)日：2009-09-23

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.

公开(公告)号：EP1761503A2

公开(公告)日：2007-03-14

申请号：EP05716076.4

申请日：2005-03-15

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  CRASSIER, Helene ,  JONCZYK, Alfred ,  STÄHLE, Wolfgang ,  SUTTER, Arne ,  RAUTENBERG, Wilfried ,  MITJANS, Francesc ,  ROSELL-VIVES, Elisabet ,  ADAN, Jaume ,  SOLER RIERA, Marta

IPC分类号： C07D233/90 ,  A61K31/4164 ,  A61P35/00

CPC分类号： C07D233/90

摘要： The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X and X' which have the meaning cited in claim 1, are tyrosine kinase inhibitors, in particular TIE-2, and Raf-kinases, and can also be used in the treatment of tumours.

公开(公告)号：EP1651626A1

公开(公告)日：2006-05-03

申请号：EP04763077.7

申请日：2004-07-02

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  ACKERMANN, Karl-August ,  STÄHLE, Wolfgang ,  JONCZYK, Alfred ,  RAUTENBERG, Wilfried ,  MITJANS, Francesc ,  ROSELL-VIVES, Elisabet ,  ADAN, Jaume ,  SOLER, Marta ,  CRASSIER, Helene

IPC分类号： C07D285/14 ,  C07D213/81 ,  C07D213/70 ,  C07D319/18 ,  C07D277/64 ,  C07D307/86 ,  C07D317/64 ,  C07D213/69 ,  C07D235/32 ,  C07D471/04 ,  C07D209/08 ,  A61P35/00 ,  A61K31/435 ,  A61K31/4745 ,  A61K31/4184

CPC分类号： C07D213/69 ,  C07D209/08 ,  C07D213/70 ,  C07D213/81 ,  C07D235/32 ,  C07D277/64 ,  C07D277/82 ,  C07D285/14 ,  C07D307/86 ,  C07D317/64 ,  C07D319/18 ,  C07D471/04

摘要： The invention relates to novel urea derivatives which inhibit tyrosinkinases, especially TIE-2, and Raf kinases and which are used in the treatment of tumors.