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1. 发明申请

WO2008052734A1 HETEROCYCLIC COMPOUNDS AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译：杂环化合物作为抗炎药
公开(公告)号：WO2008052734A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/009382
申请日：2007-10-29
申请人： NOVARTIS AG , FERRAND, Sandrine , GLICKMAN, Fraser , LEBLANC, Catherine , RITCHIE, Cathy , SHAW, Duncan , STIEFL, Nikolaus Johannes , FURET, Pascal , IMBACH, Patricia , STAUFFER, Frédéric , CAPRARO, Hans-Georg , GESSIER, François , GAUL, Christoph , ALBAUGH, Pamela A. , CHOPIUK, Greg
发明人： FERRAND, Sandrine , GLICKMAN, Fraser , LEBLANC, Catherine , RITCHIE, Cathy , SHAW, Duncan , STIEFL, Nikolaus Johannes , FURET, Pascal , IMBACH, Patricia , STAUFFER, Frédéric , CAPRARO, Hans-Georg , GESSIER, François , GAUL, Christoph , ALBAUGH, Pamela A. , CHOPIUK, Greg
IPC分类号： C07D487/04 , A61K31/5025 , A61P9/00 , A61P19/00 , A61P25/00
CPC分类号： C07D487/04
摘要： A compound of Formula Ia or Ib in free or salt or solvate form, where R 1 , R 2 , R 3 , R 4 , R 5 R 20 , R 24 , R 25 , X, Y and Z have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. These compounds are also useful for treating diseases mediated by the Pi3k receptor, the JAK-2 receptor and the TRK receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式Ia或Ib的游离或盐或溶剂化物形式的化合物，其中R 1，R 2，R 3，R 3， 4，R 5，R 20，R 24，R 25，X，Y和Z 具有说明书中所示的含义，可用于治疗由ALK-5和/或ALK-4受体介导的疾病。这些化合物也可用于治疗由Pi3k受体，JAK-2受体和TRK受体介导的疾病。还描述了含有化合物的药物组合物和用于制备化合物的方法。

2. 发明申请

WO2005123719A1 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：WO2005123719A1
公开(公告)日：2005-12-29
申请号：PCT/US2005/020371
申请日：2005-06-09
申请人： IRM LLC , REN, Pingda , WANG, Xia , ZHANG, Guobao , DING, Qiang , YOU, Shuli , ZHANG, Qiong , CHOPIUK, Greg , ALBAUGH, Pamela, A. , SIM, Taebo , GRAY, Nathanael, Schiander
发明人： REN, Pingda , WANG, Xia , ZHANG, Guobao , DING, Qiang , YOU, Shuli , ZHANG, Qiong , CHOPIUK, Greg , ALBAUGH, Pamela, A. , SIM, Taebo , GRAY, Nathanael, Schiander
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , 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, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2 2, MKK4, c-RAF, MKK6, SAPK2 and SAPK2 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，PDGF-R，trkB，c-SRC，BMX，FGFR3，b-RAF，SGK，Tie2，Lck，JNK2 2，MKK4，c-RAF，MKK6，SAPK2和SAPK2激酶。

3. 发明申请

WO2003045379A1 HYDRAZONOPYRAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTICS 审中-公开
标题翻译：水合唑衍生物及其用作治疗药物
公开(公告)号：WO2003045379A1
公开(公告)日：2003-06-05
申请号：PCT/CA2002/001583
申请日：2002-10-18
申请人： KINETEK PHARMACEUTICALS, INC. , ZHANG, Zaihui , DAYNARD, Timothy, S. , CHAFEEV, Mikhail, A. , WANG, Shisen , CHOPIUK, Greg, B. , SVIRIDOV, Serguei, V.
发明人： ZHANG, Zaihui , DAYNARD, Timothy, S. , CHAFEEV, Mikhail, A. , WANG, Shisen , CHOPIUK, Greg, B. , SVIRIDOV, Serguei, V.
IPC分类号： A61K31/415
CPC分类号： C07D417/12 , A61K31/415 , A61K31/4155 , A61K31/655 , C07D231/04 , C07D231/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention deomonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, Iymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要翻译：提供药物组合物和化合物。本发明化合物具有抗增殖活性，可促进缺乏细胞周期和死亡正常调节的细胞凋亡。在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的药物组合物。药物组合物可用于治疗过度增殖性疾病，其中该疾病包括肿瘤生长，增生性增生性疾病，血管发生。本发明的化合物是取代的吡唑和吡唑啉。

4. 发明申请

WO2005034869A2 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：WO2005034869A2
公开(公告)日：2005-04-21
申请号：PCT/US2004/033009
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： A61K
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, TGFβ, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2β kinases.
摘要翻译：本发明提供了一类新化合物，包含此类化合物的药物组合物以及使用此类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，特别是涉及异常的疾病或病症的方法激活Abl，BCR-Abl，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

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。

6. 发明申请

WO2005033086A1 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：WO2005033086A1
公开(公告)日：2005-04-14
申请号：PCT/US2004/032473
申请日：2004-09-30
申请人： IRM LLC , CHOPIUK, Greg , FURET, Pascal , GRAY , Nathanael, Schiander , IMBACH, Patricia , LIU, YI , SCHOEPFER, Joseph , STEENSMA, Ruo
发明人： CHOPIUK, Greg , FURET, Pascal , GRAY , Nathanael, Schiander , IMBACH, Patricia , LIU, YI , SCHOEPFER, Joseph , STEENSMA, Ruo
IPC分类号： C07D251/48
CPC分类号： C07D239/26 , A61K31/5377 , C07D239/42 , C07D403/12
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, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGFβ , KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 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，EGF-R，c-erbB2激酶（HER-2），CHK2，FGFR3，p70S6K，PKC，PDGF-R，p38，TGFbeta，KDR，c-Kit，b-RAF，c-RAF，FLT1和/或FLT4 激酶。

7. 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。

8. 发明申请

WO0202562A3 HETEROPOLYCYCLIC INHIBITORS 审中-公开
标题翻译：杂环化合物抑制剂
公开(公告)号：WO0202562A3
公开(公告)日：2002-05-02
申请号：PCT/IB0101519
申请日：2001-07-06
申请人： KINETEK PHARMACEUTICALS INC , ZHANG ZAIHUI , XINYAO DU , CHOPIUK GREG
发明人： ZHANG ZAIHUI , DU XINYAO , CHOPIUK GREG
IPC分类号： A61P17/06 , A61P35/00 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： A compound of formula (I) wherein, independently at each occurence, v, w, and x are selected from C, N, O, and S, with H substitition as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R , R , R and R are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R , R , R and R may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R , R , R , and R is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.
摘要翻译：式（I）的化合物，其中在每次出现时，v，w和x独立地选自C，N，O和S，根据需要进行H取代以实现开价值位点; y和z选自N和C，H取代作为开放的价键位点，条件是w，v，x，y和z中的每一个不同时为C; 由v，w，x，y和z形成的环可以是饱和或不饱和的; R 1，R 2，R 3和R 4选自氢，烷基，芳基，烷芳基，芳烷基，杂烷基和杂芳基; 其中R 1，R 2，R 3和R 4中的任何相邻的两个可以连接在一起形成5,6或7元碳环或杂环，条件是R“ R 1，R 2，R 3和R 4不同时为氢。公开了所述化合物的药物组合物，以及用于治疗包括细胞过度增殖的生物学条件的方法。

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