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1. 发明申请

WO2009097287A9 COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2009097287A9
公开(公告)日：2009-08-06
申请号：PCT/US2009/032148
申请日：2009-01-27
申请人： IRM LLC , OKRAM, Barun , UNO, Tetsuo , DING, Qiang , LIU, Yahua , JIN, Yunho , JIN, Qihui , WU, Xu , CHE, Jianwei , YAN, S. Frank , HAO, Xueshi
发明人： OKRAM, Barun , UNO, Tetsuo , DING, Qiang , LIU, Yahua , JIN, Yunho , JIN, Qihui , WU, Xu , CHE, Jianwei , YAN, S. Frank , HAO, Xueshi
IPC分类号： C07D471/04 , A61K31/4375
摘要： The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity,particulary Syk,ZAP70,KDR,FMS,FLT*,c-Kit,RET,TrkA,TrkB,TrkC-GR-1R,Alk,c- FMS.or combinations thereof.

2. 发明申请

WO2005039486A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：WO2005039486A3
公开(公告)日：2006-03-16
申请号：PCT/US2004027997
申请日：2004-08-27
申请人： IRM LLC , DING QIANG , GRAY NATHANAEL SCHIANDER , LI BING , LIU YI , UNO TETSUO
发明人： DING QIANG , GRAY NATHANAEL SCHIANDER , LI BING , LIU YI , UNO TETSUO
IPC分类号： A61K20060101 , A61K31/4745 , A61K31/519 , A61K31/675 , C07D471/02 , C07D487/02 , C07D487/04 , C07D471/04 , A61K31/4355
CPC分类号： C07D487/04
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, CSK, TrkB, FGFR3, Fes, Lck, B-RAF, C-RAF, MKK6, SAPK2a and SAPK2ß kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，BCR-Abl异常活化的疾病或病症，Bmx，CSK，TrkB，FGFR3，Fes，Lck，B-RAF，C-RAF，MKK6，SAPK2a和SAPK2β激酶。

3. 发明申请

WO2006000420A1 PYRIMIDINE UREA DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的吡嗪类尿素衍生物
公开(公告)号：WO2006000420A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006815
申请日：2005-06-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , IRM LLC , DING, Qiang , GRAY, Nathanael, Schiander , LI, Bing , LIU, Yi , SIM, Taebo , UNO, Tetsuo , ZHANG, Guobao , PISSOT SOLDERMANN, Carole , BREITENSTEIN, Werner , BOLD, Guido , CARAVATTI, Giorgio , FURET, Pascal , GUAGNANO, Vito , LANG, Marc , MANLEY, Paul, W. , SCHOEPFER, Joseph , SPANKA, Carsten
发明人： DING, Qiang , GRAY, Nathanael, Schiander , LI, Bing , LIU, Yi , SIM, Taebo , UNO, Tetsuo , ZHANG, Guobao , PISSOT SOLDERMANN, Carole , BREITENSTEIN, Werner , BOLD, Guido , CARAVATTI, Giorgio , FURET, Pascal , GUAGNANO, Vito , LANG, Marc , MANLEY, Paul, W. , SCHOEPFER, Joseph , SPANKA, Carsten
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention relates to compounds of formula (I) wherein the substituents X 1 , R 1 , R 2 , R 3 and R 4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译：本发明涉及式（I）的化合物，其中取代基X 1，R 1，R 2，R 3， SUP＆gt;和R 4具有本发明的描述中阐述和解释的含义，这些化合物的制备方法，含有它们的药物组合物，其用途可任选地与一种或多种用于治疗对蛋白激酶活性的抑制作出反应的疾病的更多其它药物活性化合物，以及治疗这种疾病的方法。

4. 发明申请

WO2005034869A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：WO2005034869A3
公开(公告)日：2005-07-07
申请号：PCT/US2004033009
申请日：2004-10-08
申请人： IRM LLC , DING QIANG , XIE YONGPING , GRAY NATHANAEL SCHIANDER , YOU SHULI , CHOPIUK GREG , JIANG JIQING , LIU YI , STEENSMA RUO , WANG XING , SIM TAEBO
发明人： DING QIANG , XIE YONGPING , GRAY NATHANAEL SCHIANDER , YOU SHULI , CHOPIUK GREG , JIANG JIQING , LIU YI , STEENSMA RUO , WANG XING , SIM TAEBO
IPC分类号： A61K20060101 , A61K31/44 , A61K31/47 , A61K31/4706 , A61K31/4745 , A61K31/519 , C07D215/16 , C07D471/00 , C07D471/02 , A61K31/514
CPC分类号： C07D471/04
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGF beta , SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2 beta kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，BCR-Abl异常活化的疾病或病症，CSK，JNK1，JNK2，PDGF-R，p38，p70S6K，TGFβ，SRC，EGFR，c-Kit，trkB，FGFR3，Fes，Lck，Syk，RAF，MKK4，MKK6和SAPK2β激酶。

5. 发明申请

WO2005016894A1 2, 4-PYRIMIDINEDIAMINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS 审中-公开
标题翻译： 2，4-PYRIMININEDIAMINES有用的治疗神经疾病，炎症和免疫系统疾病
公开(公告)号：WO2005016894A1
公开(公告)日：2005-02-24
申请号：PCT/EP2004/009099
申请日：2004-08-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , IRM LLC , GARCIA-ECHEVERRIA, Carlos , KANAZAWA, Takanori , KAWAHARA, Eiji , MASUYA, Keiichi , MATSUURA, Naoko , MIYAKE, Takahiro , OHMORI, Osamu , UMEMURA, Ichiro , STEENSMA, Ruo , CHOPIUK, Greg , JIANG, Jiqing , WAN, Yongqin , DING, Qiang , ZHANG, Qiong , GRAY, Nathanael, Schiander , KARANEWSKY, Donald
发明人： GARCIA-ECHEVERRIA, Carlos , KANAZAWA, Takanori , KAWAHARA, Eiji , MASUYA, Keiichi , MATSUURA, Naoko , MIYAKE, Takahiro , OHMORI, Osamu , UMEMURA, Ichiro , STEENSMA, Ruo , CHOPIUK, Greg , JIANG, Jiqing , WAN, Yongqin , DING, Qiang , ZHANG, Qiong , GRAY, Nathanael, Schiander , KARANEWSKY, Donald
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14
摘要： Novel pyrimidine derivatives of formula (I) Wherein R is selected from C 16-10 aryl, C5-10 heteroaryl, C 3-12 cycloalkyl and C 3-10 heterocycloalkyl; R 0 -R 6 as described herein; and their use for the manufacture of a medicament for the treatment or prevention of a disease wich responds to inhibition of FAK and/or ALK and/or ZAP-70 and/or IGF-IR.
摘要翻译：式（I）的新型嘧啶衍生物其中R选自C16-10芳基，C5-10杂芳基，C3-12环烷基和C3-10杂环烷基; R 0 -R 6，如本文所述; 以及它们用于制备用于治疗或预防对FAK和/或ALK和/或ZAP-70和/或IGF-1R的抑制作出反应的疾病的药物的用途。

6. 发明申请

WO2005016528A2 COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF RECEPTOR TYROSINE KINASE ACTIVITY 审中-公开
标题翻译：作为受体酪氨酸激酶活性的抑制剂的化合物和组合物
公开(公告)号：WO2005016528A2
公开(公告)日：2005-02-24
申请号：PCT/US2004/026373
申请日：2004-08-13
申请人： IRM LLC , CHENG, Dai , DING, Qiang , HAN, Dong , GRAY, Nathanael Schiander , ZHANG, Guobao
发明人： CHENG, Dai , DING, Qiang , HAN, Dong , GRAY, Nathanael Schiander , ZHANG, Guobao
IPC分类号： B01L
CPC分类号： C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFRα kinase activity.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与cSRC，Lck，FGFR3，Flt3，TrkB，Bmx和/或PFGFRα激酶活性相关的疾病或病症的方法。

7. 发明申请

WO2009097287A1 COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS 审中-公开
标题翻译：化合物和组合物作为激酶抑制剂
公开(公告)号：WO2009097287A1
公开(公告)日：2009-08-06
申请号：PCT/US2009032148
申请日：2009-01-27
申请人： IRM LLC , OKRAM BARUN , UNO TETSUO , DING QIANG , LIU YAHUA , JIN YUNHO , JIN QIHUI , WU XU , CHE JIANWEI , YAN S FRANK
发明人： OKRAM BARUN , UNO TETSUO , DING QIANG , LIU YAHUA , JIN YUNHO , JIN QIHUI , WU XU , CHE JIANWEI , YAN S FRANK
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity,particulary Syk ZAP70,KDR,FMS,FLT*,c-Kit,RET,TrkA,TrkB,TrkC-GR-1R,Alk,c- FMS.or combinations thereof.
摘要翻译：本发明提供了一类新的2,7-萘啶衍生物; 包含这些化合物的药物组合物和使用这些化合物治疗的方法o预防与异常或失调的激酶活性相关的疾病或病症，特别是Syk ZAP70，KDR，FMS，FLT *，c-Kit，RET，TrkA，TrkB，TrkC-GR -1R，Alk，c-FMS或其组合。

8. 发明申请

WO2007092531A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2007092531A3
公开(公告)日：2007-08-16
申请号：PCT/US2007/003319
申请日：2007-02-06
申请人： IRM LLC , DING, Qiang , REN, Pingda , ZHANG, Qiong , WANG, Xia , SIM, Taebo , ALBAUGH, Pamela A. , GRAY, Nathanael S.
发明人： DING, Qiang , REN, Pingda , ZHANG, Qiong , WANG, Xia , SIM, Taebo , ALBAUGH, Pamela A. , GRAY, Nathanael S.
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/4427 , A61K31/444 , A61K31/4468
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particulary diseases or disorders that involve abnormal activation of the Abl.Bcr-Abl, Bmx, b-RAF, c-RAFI c-SRC,KDR,CSKlFGFR3,JAK2ILck,Met,PKCalpha,SAPK2alpha)Tie2,TrkB and P70S6K kinases. These compounds have the following structure: (Formula I); in which: R 1 is selected from -NR 6 R 7 and -NR 6 C(O)R 8 ; wherein R 6 is selected from hydrogen and C 1-6 alkyl; R 7 is selected from hydrogen, C 1-6 alkyl. -NR 9 R 10 , C 6-10 aryl-C 0-4 alkyl, C 1-10 heteroaryl-C 0-4 alkyl, C 3-12 cycloalkyl-C 0-4 alkyl and C 3-8 heterocycloalkyl-C 0-4 alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R 7 can be optionally substituted by 1 to 3 radicals independently selected from C 1-6 alkyl, C 1-6 alkoxy, -QNR 9 R 10 and C 3-8 heterocycloalkyl-C 0-4 alkyl; wherein Q is selected from a bond and C 1-4 alkylene; R 8 is selected from hydrogen and C 1-4 alkyl; R 9 and R 10 are independently selected from hydrogen and C 1-6 alkyl; R 2 is selected from hydrogen and C 1-6 alkyl; R 3 is selected from hydrogen and C 1-6 alkyl; R 4 is selected from hydrogen, halo, C 1-6 alkyl, C 1-6 alkoxy, halosubstituted-C 1-6 alkyl and halosubsb'tuted-C 1-6 alkoxy; R 5 is selected from -C(O)NHR 11 and -NHC(O)R 11 ; wherein R 11 is selected from C 6-10 aryl and C 1-10 heteroaryl; wherein any aryl or heteroaryl of R 11 is optionally substituted with 1 to 3 radicals independently selected from halo, C 1-6 alkyl, C 1-6 alkoxy, halosubstituted-C 1-6 alkyl, halosubstituted-C 1-6 alkoxy, di-C 1-4 alkyl-amino-C 1-6 alkoxy, di-C 1-4 alkyl-amino-C 1-4 alkyl(C 1-4 alkyl)amino, C 1-10 heteroaiyl-C 0-4 alkyl, C 3-8 heterocycIoalkyl-C 0-4 alkyl and C 3-8 heterocycloalkyl-oxy; wherein any heteroaryl or heterocycloalkyl substituent of R 11 is further optionally substituted by 1 to 2 radicals independently selected from C 1-6 alkyl and hydroxy-C 1-6 alkyl; X and Y are independently selected from N and CH; and the pharmaceutically acceptable salts, hydrates, solvates and isomers thereof.

9. 发明申请

WO2007056151A3 PROTEIN KINASE INHBITORS 审中-公开
标题翻译：蛋白激酶抑制剂
公开(公告)号：WO2007056151A3
公开(公告)日：2007-08-02
申请号：PCT/US2006042975
申请日：2006-11-03
申请人： IRM LLC , ZHANG QIONG , GRAY NATHANAEL S , LIU YI , DING QIANG , UNO TETSUO
发明人： ZHANG QIONG , GRAY NATHANAEL S , LIU YI , DING QIANG , UNO TETSUO
IPC分类号： C07D239/42 , A61K31/44 , A61K31/505 , A61P35/00 , C07D213/74 , C07D239/47 , C07D239/48 , C07D239/52
CPC分类号： C07D239/48 , C07D213/74 , C07D239/42 , C07D239/47 , C07D239/52
摘要： The invention provides disubtituted pyrimidine or pyridine compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Lck, IR, IGF-IR, JNKl , Flt3, Fes, EFGR (Her-1, erbB-1) , cSRC, CDKl/cyclinB, c-RAF, BTK, Bmx, AxI, Aurora-A, AbI, BCR-AbI, TrkB, Tie2, Syk, SGK, SAPK2a, Rskl and Met kinases.
摘要翻译：本发明提供了取代的嘧啶或吡啶化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Lck，IR，IGF异常活化的疾病或病症 -IR，JNK1，Flt3，Fes，EFGR（Her-1，erbB-1），cSRC，CDK1 / cyclinB，c-RAF，BTK，Bmx，AxI，Aurora-A，AbI，BCR-AbI，TrkB，Tie2， Syk，SGK，SAPK2a，Rsk1和Met激酶。

10. 发明申请

WO2006081172A2 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：WO2006081172A2
公开(公告)日：2006-08-03
申请号：PCT/US2006002266
申请日：2006-01-19
申请人： IRM LLC , SIM TAEBO , GRAY NATHANAEL SCHIANDER , LEE HYUN SOO , LIU YI , REN PINGDA , YOU SHULI , ZHANG QIONG , DING QIANG , WANG XIA , JIANG SONGCHUN , ALBAUGH PAMELA A
发明人： SIM TAEBO , GRAY NATHANAEL SCHIANDER , LEE HYUN SOO , LIU YI , REN PINGDA , YOU SHULI , ZHANG QIONG , DING QIANG , WANG XIA , JIANG SONGCHUN , ALBAUGH PAMELA A
IPC分类号： A61K31/5377
CPC分类号： C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, FGFR3, PDGFRß and b-Raf kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，Bcr-Abl异常活化的疾病或病症，FGFR3，PDGFRβ和b-Raf激酶。

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