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1. 发明授权

US07196083B2 Heteropolycyclic inhibitors of protein kinases 失效
标题翻译：蛋白激酶的杂多环抑制剂
公开(公告)号：US07196083B2
公开(公告)日：2007-03-27
申请号：US10310600
申请日：2002-12-04
申请人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
发明人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
IPC分类号： A61K31/53
CPC分类号： C07D487/04 , C07D513/04
摘要： A method of inhibiting tumor growth is provided, comprising administering an effective dose of a compound of the formula wherein, independently at each occurrence, w is C or N, v and x are N with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to 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 R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic ring or a 5, 6 or 7-membered heterocyclic ring containing at least one atom selected from nitrogen, oxygen and sulfur.
摘要翻译：提供了一种抑制肿瘤生长的方法，包括施用有效剂量的下式的化合物

2. 发明授权

US06514972B2 Heteropolycyclic inhibitors of protein kinases 失效
标题翻译：蛋白激酶的杂多环抑制剂
公开(公告)号：US06514972B2
公开(公告)日：2003-02-04
申请号：US09900073
申请日：2001-07-06
申请人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
发明人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D513/04
摘要： A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to 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 R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 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：在每次出现时，v，w和x独立地选自C，N，O和S的化合物，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，根据需要进行H取代以满足开价值位置，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; 并且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以形成5,6或7-元碳环或杂环，条件是R 1，R 2，R 3和R 4中的每一个不是同时氢。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。

3. 发明申请

US20050272709A1 Immugenic compositions and diagnostic and therapeutic uses thereof 有权
标题翻译：传染性组合物及其诊断和治疗用途
公开(公告)号：US20050272709A1
公开(公告)日：2005-12-08
申请号：US10497046
申请日：2002-10-18
申请人： Zaihui Zhang , Tim Daynard , Mikhail Chafeev , Shisen Wang , Greg Chopiuk , Serguei Sviridov
发明人： Zaihui Zhang , Tim Daynard , Mikhail Chafeev , Shisen Wang , Greg Chopiuk , Serguei Sviridov
IPC分类号： C07D231/04 , A61K31/403 , A61K31/409 , A61K31/415 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/655 , A61K45/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/08 , 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 , C07D417/12
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, lymphoproliferative 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。该药物组合物可用于治疗过度增殖性疾病，该疾病包括肿瘤生长，淋巴组织增生性疾病，血管生成。本发明的化合物是取代的吡唑和吡唑啉。

4. 发明授权

US07745437B2 Compounds and compositions as protein kinase inhibitors 有权
标题翻译：化合物和组合物作为蛋白激酶抑制剂
公开(公告)号：US07745437B2
公开(公告)日：2010-06-29
申请号：US11628881
申请日：2005-06-09
申请人： Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shuli You , Qiong Zhang , Greg Chopiuk , Pamela A. Albaugh , Taebo Sim , Nathanael Schiander Gray
发明人： Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shuli You , Qiong Zhang , Greg Chopiuk , Pamela A. Albaugh , Taebo Sim , Nathanael Schiander Gray
IPC分类号： C07D403/04 , A61K31/4178
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, ΣΓK, Tιε2, Λχκ, θNK2α2, MKK4, c-RAF, MKK6, SAPK2α and SAPK2β 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，＆amp; Ggr; K，Tι＆egr; 2，Λχ＆kgr;; thetas;NK2α2，MKK4，c-RAF，MKK6，SAPK2α和SAPK2＆激酶。

5. 发明授权

US07893074B2 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders 有权
标题翻译： 2，4-嘧啶二胺可用于治疗肿瘤性疾病，炎症和免疫系统疾病
公开(公告)号：US07893074B2
公开(公告)日：2011-02-22
申请号：US10568367
申请日：2004-08-13
申请人： Carlos Garcia-Echeverria , Takanori Kanazawa , Eiji Kawahara , Keiichi Masuya , Naoko Matsuura , Takahiro Miyake , Osamu Ohmori , Ichiro Umemura , Ruo Steensma , Greg Chopiuk , Jiqing Jiang , Yongqin Wan , Qiang Ding , Qiong Zhang , Nathanael Schiander Gray , Donald Karanewsky
发明人： Carlos Garcia-Echeverria , Takanori Kanazawa , Eiji Kawahara , Keiichi Masuya , Naoko Matsuura , Takahiro Miyake , Osamu Ohmori , Ichiro Umemura , Ruo Steensma , Greg Chopiuk , Jiqing Jiang , Yongqin Wan , Qiang Ding , Qiong Zhang , Nathanael Schiander Gray , Donald Karanewsky
IPC分类号： C07D239/48 , A61K31/506
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 to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：式I的新型嘧啶衍生物用于其制备方法，它们作为药物的用途以及包含它们的药物组合物。

6. 发明授权

US07189729B2 Methods and compositions as protein kinase inhibitors 有权
标题翻译：方法和组成作为蛋白激酶抑制剂
公开(公告)号：US07189729B2
公开(公告)日：2007-03-13
申请号：US10956412
申请日：2004-09-30
申请人： Greg Chopiuk , Pascal Furet , Nathanael Schiander Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
发明人： Greg Chopiuk , Pascal Furet , Nathanael Schiander Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
IPC分类号： C07D239/42 , C07D403/12 , A61K31/506 , A61P19/02 , A61P35/00
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. 发明授权

US07449582B2 Compounds and compositions as protein kinase inhibitors 失效
标题翻译：化合物和组合物作为蛋白激酶抑制剂
公开(公告)号：US07449582B2
公开(公告)日：2008-11-11
申请号：US10961646
申请日：2004-10-08
申请人： Qiang Ding , Yongping Xie , Nathanael S. Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
发明人： Qiang Ding , Yongping Xie , Nathanael S. Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
IPC分类号： C07D215/38 , C07D471/02 , C07D251/38
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，TGFbeta，SRC，EGFR，c-Kit，trkB，FGFR3，Fes，Lck，Syk，RAF，MKK4，MKK6和SAPK2β激酶。

8. 发明申请

US20070225286A1 Compounds and Compositions as Protein Kinase Inhibitors 有权
标题翻译：化合物和组合物作为蛋白激酶抑制剂
公开(公告)号：US20070225286A1
公开(公告)日：2007-09-27
申请号：US11628881
申请日：2005-06-09
申请人： Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shull You , Qiong Zhang , Greg Chopiuk , Pamela Albaugh , Taebo Sim , Nathanael Gray
发明人： Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shull You , Qiong Zhang , Greg Chopiuk , Pamela Albaugh , Taebo Sim , Nathanael Gray
IPC分类号： A61K31/496 , A61K31/497 , A61K31/5355 , C07D401/04 , 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, ΣΓK, Ttε2, Λχκ, ΘNK2α2, MKK4, c-RAF, MKK6, SAPK2α and SAPK2β 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，SigmaGammaK，Ttepsilon2，Lambdachikappa，ThetaNK2alpha2，MKK4，c-RAF，MKK6，SAPK2α和SAPK2β激酶。

9. 发明申请

US20110098280A1 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：US20110098280A1
公开(公告)日：2011-04-28
申请号：US12984519
申请日：2011-01-04
申请人： Carlos Garcia-Echeverria , Takanori Kanazawa , Eiji Kawahara , Keiichi Masuya , Naoko Matsuura , Takahiro Miyake , Osamu Ohmori , Ichiro Umemura , Ruo Steensma , Greg Chopiuk , Jiqing Jiang , Yongqin Wan , Qiang Ding , Qiong Zhang , Nathanael Schiander Gray , Donald Karanewsky
发明人： Carlos Garcia-Echeverria , Takanori Kanazawa , Eiji Kawahara , Keiichi Masuya , Naoko Matsuura , Takahiro Miyake , Osamu Ohmori , Ichiro Umemura , Ruo Steensma , Greg Chopiuk , Jiqing Jiang , Yongqin Wan , Qiang Ding , Qiong Zhang , Nathanael Schiander Gray , Donald Karanewsky
IPC分类号： A61K31/505 , C07D239/48 , C07D405/12 , A61K31/506 , C07D403/12 , C07D413/12 , A61K31/5377 , C07D401/12 , C07D417/14 , A61K31/541 , C07D401/14 , C07D498/04 , A61K31/5383 , C07D413/14 , A61K31/55 , A61P35/00
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 to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：式I的新型嘧啶衍生物用于其制备方法，它们作为药物的用途以及包含它们的药物组合物。

10. 发明申请

US20050171105A1 Methods and compositions as protein kinase inhibitors 有权
标题翻译：方法和组合物作为蛋白激酶抑制剂
公开(公告)号：US20050171105A1
公开(公告)日：2005-08-04
申请号：US10956412
申请日：2004-09-30
申请人： Greg Chopiuk , Pascal Furet , Nathanael Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
发明人： Greg Chopiuk , Pascal Furet , Nathanael Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
IPC分类号： A61K31/53 , A61P35/00 , C07D239/26 , C07D239/42 , C07D403/12 , C07D43/02
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。

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