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1. 发明申请

WO2006047503A2 INHIBITORS OF C-FMS KINASE 审中-公开
标题翻译： C-FMS激酶抑制剂
公开(公告)号：WO2006047503A2
公开(公告)日：2006-05-04
申请号：PCT/US2005038340
申请日：2005-10-20
申请人： JANSSEN PHARMACEUTICA NV , PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
发明人： PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
IPC分类号： C07D307/68 , A61K31/16 , A61K31/195 , A61K31/381 , A61K31/452 , A61K31/4545 , C07D223/12 , C07D265/30 , C07D279/12 , C07D405/12 , C07D409/12
CPC分类号： C07D405/12 , C07D307/68 , C07D409/12
摘要： The invention relates to compounds of Formula (I) wherein A, R 1 , R 2 , X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
摘要翻译：本发明涉及式（I）的化合物，其中A，R 1，R 2，X，Y和W在说明书中阐述，以及溶剂合物，水合物，互变异构体或其药学上可接受的盐，其抑制蛋白酪氨酸激酶，特别是c-fms激酶。

2. 发明申请

WO2006047479A2 C-FMS KINASE INHIBITORS 审中-公开
标题翻译： C-FMS激酶抑制剂
公开(公告)号：WO2006047479A2
公开(公告)日：2006-05-04
申请号：PCT/US2005038307
申请日：2005-10-20
申请人： JANSSEN PHARMACEUTICA NV , PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
发明人： PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
IPC分类号： A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , C07D223/12 , C07D265/30 , C07D279/12 , C07D307/68 , C07D405/12 , C07D409/12
CPC分类号： C07D405/12 , C07D207/416 , C07D233/90 , C07D307/68 , C07D409/12
摘要： The invention is directed to compounds of Formula (I) wherein A, R 1 , R 2 , R 3 , R 4 , X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
摘要翻译：本发明涉及式（I）的化合物，其中A，R 1，R 2，R 3，R 4，说明书中列出了X，和W，以及其抑制蛋白酪氨酸激酶，特别是c-fms激酶的溶剂合物，水合物，互变异构体或其药学上可接受的盐。

3. 发明申请

WO2004096795A3 C-FMS KINASE INHIBITORS 审中-公开
标题翻译： C-FMS激酶抑制剂
公开(公告)号：WO2004096795A3
公开(公告)日：2005-03-10
申请号：PCT/US2004012729
申请日：2004-04-26
申请人： DIMENSIONAL PHARM INC , PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
发明人： PLAYER MARK R , BAINDUR NAND , BRANDT BENJAMIN M , CHADHA NARESH , PATCH RAYMOND J , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS
IPC分类号： A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , A61K31/55 , A61P35/00 , C07D207/34 , C07D207/42 , C07D213/81 , C07D223/12 , C07D231/16 , C07D231/38 , C07D261/18 , C07D265/02 , C07D265/30 , C07D279/12 , C07D295/14 , C07D307/68 , C07D307/71 , C07D307/72 , C07D401/12 , C07D405/00 , C07D405/12 , C07D491/04
CPC分类号： C07D213/81 , C07D231/38 , C07D265/02 , C07D307/68 , C07D307/71 , C07D405/12 , C07D491/04
摘要： The invention is directed to compounds of formulae (I), (II) and (III), wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
摘要翻译：本发明涉及式（I），（II）和（III）的化合物，其中A，R 1，R 2，R 3，R 4，X，Y和W在说明书中列出，以及溶剂化物，水合物，互变异构体或其药学上可接受的盐，其抑制蛋白酪氨酸激酶，特别是c-fms激酶。

4. 发明申请

WO2006047505A2 CRYSTAL STRUCTURE OF THE C-FMS KINASE DOMAIN 审中-公开
标题翻译： C-FMS激酶域的晶体结构
公开(公告)号：WO2006047505A2
公开(公告)日：2006-05-04
申请号：PCT/US2005038342
申请日：2005-10-20
申请人： JANSSEN PHARMACEUTICA NV , SCHUBERT CARSTEN , SPRINGER BARRY A , DECKMAN INGRID , PATCH RAYMOND J , STRUBLE GEOFFREY T , MA HONGCHANG , SCHALK-HIHI CELINE , BRANDT BENJAMIN M , PETROUNIA IOANNA
发明人： SCHUBERT CARSTEN , SPRINGER BARRY A , DECKMAN INGRID , PATCH RAYMOND J , STRUBLE GEOFFREY T , MA HONGCHANG , SCHALK-HIHI CELINE , BRANDT BENJAMIN M , PETROUNIA IOANNA
IPC分类号： G06F19/16 , G06F19/18 , G06F19/28
CPC分类号： C07K14/7153 , C07K2299/00 , C07K2319/00 , C30B7/00 , G06F19/16 , G06F19/18 , G06F19/28
摘要： The present invention includes a crystal structure of the kinase domain of c-fms and a methodology to produce diffraction quality crystals of the c-fms kinase domain by heterologous substitution of the kinase insert domain. Also included in the invention is the structure of the c-fms kinase domain in liganded form for use in the discovery of inhibitors of c-fms for the treatment of diseases caused by inappropriate activity of c-fms. The present invention includes descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of c-fms to be determined at atomic resolution so that ligand binding sites on can be identified and the interactions of ligands with amino acid residues can be modeled.
摘要翻译：本发明包括c-fms的激酶结构域的晶体结构和通过激酶插入结构域的异源取代产生c-fms激酶结构域的衍射质量晶体的方法。本发明还包括配体形式的c-fms激酶结构域用于发现c-fms抑制剂用于治疗由c-fms的不适当活性引起的疾病的结构。本发明包括晶体的X射线衍射图案的描述。衍射图允许以原子分辨率确定c-fms的三维结构，从而可以鉴定配体结合位点，并且可以建模与配体与氨基酸残基的相互作用。

5. 发明专利

CA2649512A1 C-FMS KINASE INHIBITORS 未知
公开(公告)号：CA2649512A1
公开(公告)日：2007-11-01
申请号：CA2649512
申请日：2006-04-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： BRANDT BENJAMIN M , BAINDUR NAND , PLAYER MARK R , ASGARI DAVOUD , PATCH RAYMOND J , CHADHA NARESH , GEORGIADIS TAXIARCHIS M
IPC分类号： C07D233/90 , A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , A61K31/501 , A61P35/00 , C07D223/12 , C07D265/30 , C07D279/12 , C07D307/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12

6. 发明专利

AU2005299476A1 c-fms kinase inhibitors 未知
公开(公告)号：AU2005299476A1
公开(公告)日：2006-05-04
申请号：AU2005299476
申请日：2005-10-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： BRANDT BENJAMIN M , PATCH RAYMOND J , PLAYER MARK R , CHADHA NARESH , GEORGIADIS TAXIARCHIS , ASGARI DAVOUD , BAINDUR NAND
IPC分类号： C07D405/12 , A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4525 , A61K31/4545 , A61P9/00 , A61P35/00 , C07D207/40 , C07D223/12 , C07D233/90 , C07D265/30 , C07D279/12 , C07D307/68 , C07D409/12
摘要： The invention is directed to compounds of Formulae I: wherein A, R 1 , R 2 , R 3 , R 4 , X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

7. 发明专利

AU2006342509A1 c-fms kinase inhibitors 未知
公开(公告)号：AU2006342509A1
公开(公告)日：2007-11-01
申请号：AU2006342509
申请日：2006-04-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： GEORGIADIS TAXIARCHIS , CHADHA NARESH , ASGARI DAVOUD , PLAYER MARK R , PATCH RAYMOND J , BAINDUR NAND , BRANDT BENJAMIN M
IPC分类号： C07D233/90 , A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , A61K31/501 , A61P35/00 , C07D223/12 , C07D265/30 , C07D279/12 , C07D307/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention is directed to compounds of Formula II: wherein A, R 1 , R 2 , R 3 , R 4 , X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

8. 发明专利

AU2005299500A1 Inhibitors of c-fms kinase 未知
公开(公告)号：AU2005299500A1
公开(公告)日：2006-05-04
申请号：AU2005299500
申请日：2005-10-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAINDUR NAND , CHADHA NARESH , ASGARI DAVOUD , GEORGIADIS TAXIARCHIS , BRANDT BENJAMIN M , PLAYER MARK R , PATCH RAYMOND J
IPC分类号： C07D307/68 , A61K31/16 , A61K31/195 , A61K31/381 , A61K31/452 , A61K31/4545 , C07D223/12 , C07D265/30 , C07D279/12 , C07D405/12 , C07D409/12
摘要： The invention relates to compounds of Formula I: wherein A is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of -C 1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, -CF 3 , alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, -OCF 3 , -OCO-alkyl, -CORA, -CN, -C(NH)NH 2 , -COOR a , -CONR a R b , -N(R a )COR b , -NO 2 , -SO 2 R a , -SO 3 R a or -SO 2 NR a R b ; or a 5- to 7-membered mono- or a 8- to 10-membered bicyclic heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with one or more of -C 1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, -CF 3 , alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, -OCF 3 , -OCO-alkyl, -COR a , -CN, -C(NH)NH 2 , -COOR a , -CONR a R b , -N(R a )COR b , -NO 2 , -SO 2 R a , -SO 3 R a or -SO 2 NR a R b ; R 1 is -H, aryl, -COR a , -COR a , -COOR a , -CONR a R b , -SO 2 R a or -SO 2 NR a R b ; X is -CO-, -C(-NH)-, -CS-, -CON(R a )-, -CS(NR a )-, -SO 2 - or -CR a R b -; Y is -S-, -SO-, -SO 2 -, -O- or direct link; R 2 is alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, each of which may be optionally substituted with one or more halogens; and W is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of C 1-4 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, halogen, hydroxy, -CF 3 , alkoxy, aryloxy, arylalkoxy, -OCF 3 , -COR a , -CN, -C(NH)NH 2 , -COOR a , -CONR a R b , -NHCOR a R b , -NHSO 2 R a , -NO 2 , -SOR a , -SO 3 R a or -SO 2 NR a R b ; or a 5- to 6-membered mono- or a 8- to 10-membered bicyclic heterocyclic or heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with -C 1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, heteroaryl, halogen, hydroxy, -CF 3 , alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, -OCF 3 , -OCO-alkyl, -OCO-alkylamino, -OCO-alkylamido, COR a , -CN, -C(NH)NH 2 , -COOR a , -CONR a R b , -N(R a )COR b , -NO 2 , -SO 2 R a , -SO 3 R a or -SO 2 NR a R b ; as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

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