公开(公告)号：EP2078018B1

公开(公告)日：2012-03-14

申请号：EP07861468.2

申请日：2007-10-18

申请人： Signal Pharmaceuticals LLC

发明人： MORTENSEN, Deborah Sue ,  MEDEROS, Maria Mercedes Delgado ,  SAPIENZA, John Joseph ,  ALBERS, Ronald J. ,  LEE, Branden G. ,  HUANG, Dehua ,  SCHWARZ, Kimberly Lyn ,  PARNES, Jason Simon ,  RIGGS, Jennifer R. ,  PAPA, Patrick William

IPC分类号： C07D473/00 ,  C07D475/00 ,  A61K31/519 ,  A61K31/522 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D473/00 ,  C07D473/28 ,  C07D473/32 ,  C07D475/00

摘要： Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

公开(公告)号：EP2215091A2

公开(公告)日：2010-08-11

申请号：EP08856914.0

申请日：2008-11-26

申请人： Nerviano Medical Sciences S.r.l.

发明人： CARUSO, Michele ,  BERIA, Italo ,  BRASCA, Maria, Gabriella ,  POSTERI, Helena ,  FACHIN, Gabriele

IPC分类号： C07D475/00 ,  A61K31/519 ,  A61P35/00 ,  A61P31/00

CPC分类号： C07D475/00

摘要： Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

公开(公告)号：EP1765820A4

公开(公告)日：2010-07-21

申请号：EP05763510

申请日：2005-06-23

申请人： IRM LLC

发明人： REN PINGDA ,  WANG XIA ,  GRAY NATHANAEL SCHIANDER ,  LIU YI ,  SIM TAEBO

IPC分类号： C07D475/00

CPC分类号： C07D475/00

公开(公告)号：EP1866311A4

公开(公告)日：2010-03-31

申请号：EP06748656

申请日：2006-03-24

申请人： GLAXO GROUP LTD

发明人： CALLAHAN JAMES FRANCIS ,  WAN ZEHONG ,  YAN HONGXING

IPC分类号： C07D475/00 ,  A61K31/19 ,  A61K31/535 ,  A61K31/55 ,  A61K31/5513 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D239/47 ,  C07D243/08 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D487/04

公开(公告)号：EP2079743A1

公开(公告)日：2009-07-22

申请号：EP07824247.6

申请日：2007-10-19

申请人： Chroma Therapeutics Limited

发明人： MOFFAT, David Festus Charles ,  PATEL, Sanjay Ratilal ,  DAVIES, Stephen John ,  BAKER, Kenneth William John ,  PHILPS, Oliver James

IPC分类号： C07D475/00 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D475/00

摘要： Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: wherein R1 and R2 are hydrogen, or an optionally substituted (C1-C6)alkyl, (C2- C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 and R3' are independently selected from hydrogen, -CN, hydroxyl, halogen, optionally substituted (C1-C6) alkyl, (C2- C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, -NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1 -Y1- wherein R is an alpha amino acid or alpha amino acid ester motif, linked to ring A by linker R-L1-Y1- as defined in the claims.

公开(公告)号：EP2078018A1

公开(公告)日：2009-07-15

申请号：EP07861468.2

申请日：2007-10-18

申请人： Signal Pharmaceuticals LLC

发明人： MORTENSEN, Deborah Sue ,  MEDEROS, Maria Mercedes Delgado ,  SAPIENZA, John Joseph ,  ALBERS, Ronald J. ,  LEE, Branden G. ,  HUANG, Dehua ,  SCHWARZ, Kimberly Lyn ,  PARNES, Jason Simon ,  RIGGS, Jennifer R. ,  PAPA, Patrick William

IPC分类号： C07D473/00 ,  C07D475/00 ,  A61K31/519 ,  A61K31/522 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D473/00 ,  C07D473/28 ,  C07D473/32 ,  C07D475/00

摘要： Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

公开(公告)号：EP1866311A2

公开(公告)日：2007-12-19

申请号：EP06748656.3

申请日：2006-03-24

申请人： GLAXO GROUP LIMITED

发明人： CALLAHAN, James Francis ,  WAN, Zehong ,  YAN, Hongxing

IPC分类号： C07D475/00 ,  C07D413/12 ,  C07D413/14 ,  C07D243/08 ,  A61K31/19 ,  A61K31/535 ,  A61K31/55 ,  A61K31/5513 ,  C07D239/47

CPC分类号： C07D487/04

摘要： Novel substituted l,5,7-trisubstituted-354-dihydro-pyriinido[4,5-(flpyrimidin- 2-(2H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

公开(公告)号：EP1658081B1

公开(公告)日：2007-10-24

申请号：EP04761485.4

申请日：2004-08-27

申请人： 4 AZA IP NV

发明人： WAER, Mark, Jozef, Albert ,  HERDEWIJN, Piet, André, Maurits, Maria ,  PFLEIDERER, Wolfgang, Eugen ,  MARCHAND, Arnaud, Didier, Marie ,  DE JONGHE, Steven, Cesar, Alfons

IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D475/04 ,  C07D475/08 ,  C07D475/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D475/10 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D475/04 ,  C07D475/08 ,  A61K2300/00

摘要： This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro- derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

公开(公告)号：EP1658081A2

公开(公告)日：2006-05-24

申请号：EP04761485.4

申请日：2004-08-27

申请人： 4 AZA Bioscience nv

发明人： WAER, Mark, Jozef, Albert ,  HERDEWIJN, Piet, André, Maurits, Maria ,  PFLEIDERER, Wolfgang, Eugen ,  MARCHAND, Arnaud, Didier, Marie ,  DE JONGHE, Steven, Cesar, Alfons

IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D475/04 ,  C07D475/08 ,  C07D475/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D475/10 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D475/04 ,  C07D475/08 ,  A61K2300/00

摘要： This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro- derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

公开(公告)号：EP1222189B1

公开(公告)日：2004-11-17

申请号：EP00992437.4

申请日：2000-10-12

申请人： Ciba Specialty Chemicals Holding Inc.

发明人： EICHENBERGER, Thomas ,  HÜGIN, Max ,  MÜLLER, Karl-Heinz

IPC分类号： C07D475/00

CPC分类号： C07D487/14 ,  C09B17/00 ,  C09B57/00

摘要： Preparation of pyrimido[5,4-g]pteridine of formula (I) wherein A1, A2, A3 and A4 are each independently of the others -NR1R2, wherein R1 and R2 are hydrogen, C1-C8alkyl, -CO-C1-C8alkyl, -CO-C6-C14aryl, -COO-C1-C8alkyl, -COO-C6-C14aryl, -CONH-C1-C8alkyl or -CONH-C6-C14aryl, or -OH, -SH, hydrogen, C1-C8alkyl, C1-C8alkoxy, or C6-C14aryl or -O-C6-C14aryl each unsubstituted or mono- or poly- substituted by halogen, nitro, cyano, -OR10, -SR10, -NR10R11, -CONR10R11, -COOR10, -SO2R10, -SO2NR10R11, -SO3R10, -NR11COR10 or by -NR11COOR10, wherein R10 and R11 are each independently of the other hydrogen, C1-C8alkyl, C5-C12cycloalkyl or C2-C8alkenyl, by a) reacting the pyrimidine of formula (II) with the pyrimidine of formula (III) in the presence of an acid and, if desired, of a solvent, the molar ratio of the acid to the compound of formula (II) being in the range of from 100:1 to 1:1, and b) subsequently treating the resulting reaction mixture with a base, and novel pyrimido[5,4-g]pteridine salts and their use.

摘要翻译： 式（I）的嘧啶并[5,4-g]蝶啶的制备其中A 1，A 2，A 3和A 4各自独立地为-NR 1 R 2，其中R 1和R 2为氢，C 1 -C 8烷基，-CO-C 1 -C 8烷基 ，-CO-C 6 -C 14芳基，-COO-C 1 -C 8烷基，-COO-C 6 -C 14芳基，-CONH-C 1 -C 8烷基或-CONH-C 6 -C 14芳基，或-OH，-SH，氢，C 1 -C 8烷基， C8烷氧基或C6-C14芳基或-OC 6 -C 14芳基各自未被取代或被卤素，硝基，氰基，-OR 10，-SR 10，-NR 10 R 11，-CONR 10 R 11，-COOR 10，-SO 2 R 10，-SO 2 NR 10 R 11单取代或多取代 其中R 10和R 11各自独立地为氢，C 1 -C 8烷基，C 5 -C 12环烷基或C 2 -C 8烯基，其中a）使式（II）的嘧啶与下式的嘧啶反应：其中R 10和R 11各自独立地为氢，C 1 -C 8烷基， （III）化合物在酸和如果需要时的溶剂存在下反应，酸与式（II）化合物的摩尔比在100:1至1:1的范围内，和b） 随后用碱处理所得反应混合物，得到新的嘧啶并[5,4-g]蝶啶盐 s和它们的使用。