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1.发明授权公开(公告)号：US06795776B1
公开(公告)日：2004-09-21
申请号：US09687609
申请日：2000-10-13
申请人： Roberto Weinmann , Howard M. Einspahr , Stanley R. Krystek , John S. Sack , Mark E. Salvati , John S. Tokarski , Ricardo M. Attar , Chihuei Wang
发明人： Roberto Weinmann , Howard M. Einspahr , Stanley R. Krystek , John S. Sack , Mark E. Salvati , John S. Tokarski , Ricardo M. Attar , Chihuei Wang
IPC分类号： G01N3100
CPC分类号： C07K14/721 , G01N33/743 , G01N2333/723
摘要： The first crystal structure of the androgen receptor ligand binding domain has been determined to 2.0 angstrom resolution. Disclosed are the coordinates for the crystal structure, and methods for determining agonists, partial agonists, antagonists, partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor.
摘要翻译： 雄激素受体配体结合结构域的第一个晶体结构已经确定为2.0埃的分辨率。 公开了晶体结构的坐标，以及用于确定雄激素受体的激动剂，部分激动剂，拮抗剂，部分拮抗剂和选择性雄激素受体调节剂（SARM）的方法。
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2.发明授权公开(公告)号：US07225083B2
公开(公告)日：2007-05-29
申请号：US10878851
申请日：2004-06-28
申请人： Roberto Weinmann , Howard M. Einspahr , Stanley R. Krystek , John S. Sack , Mark E. Salvati , John S. Tokarski , Ricardo M. Attar , Chihuei Wang
发明人： Roberto Weinmann , Howard M. Einspahr , Stanley R. Krystek , John S. Sack , Mark E. Salvati , John S. Tokarski , Ricardo M. Attar , Chihuei Wang
CPC分类号： C07K14/721 , G01N33/743 , G01N2333/723
摘要： The first crystal structure of the androgen receptor ligand binding domain has been determined to 2.0 angstrom resolution. Disclosed are the coordinates for the crystal structure, and methods for determining agonists, partial agonists, antagonists, partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor.
摘要翻译： 雄激素受体配体结合结构域的第一个晶体结构已经确定为2.0埃的分辨率。 公开了晶体结构的坐标，以及用于确定雄激素受体的激动剂，部分激动剂，拮抗剂，部分拮抗剂和选择性雄激素受体调节剂（SARM）的方法。
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3.发明授权Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases 有权吡咯并哒嗪JAK3抑制剂及其用于治疗炎症和自身免疫疾病的用途公开(公告)号：US08921368B2
公开(公告)日：2014-12-30
申请号：US14005570
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07D471/04 , A01N43/58 , A61K31/50
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐。 式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。
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公开(公告)号：US07547782B2
公开(公告)日：2009-06-16
申请号：US11529875
申请日：2006-09-28
申请人： Robert M. Borzilleri , Xiao-Tao Chen , David K. Williams , John S. Tokarski , Robert F. Kaltenbach
发明人： Robert M. Borzilleri , Xiao-Tao Chen , David K. Williams , John S. Tokarski , Robert F. Kaltenbach
IPC分类号： C07D401/12 , C07D421/12 , C07D403/12 , C07D405/12 , C07D239/28 , C07D409/12 , C07D411/12 , C07D413/12 , C07D417/12 , C07D419/23 , A61P35/00 , C07D419/12 , C07D239/20 , C07D411/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07D515/04 , C07D213/46 , C07D413/10 , C07D211/74 , C07D211/86 , C07D211/78 , C07D211/90 , C07D211/81 , C07D213/56 , C07D213/63 , C01B15/14 , C01B33/12 , C07F7/10
CPC分类号： C07D401/12 , C07D213/82 , C07D471/04
摘要： The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
摘要翻译： 本发明涉及具有式I或II的化合物：包括其盐，以及用于治疗癌症的方法。
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公开(公告)号：US07084160B2
公开(公告)日：2006-08-01
申请号：US10464139
申请日：2003-06-18
申请人： Robert M. Borzilleri , Rajeev S. Bhide , John S. Tokarski , Peter Zheng , Ligang Qian , Zhen-Wei Cai
发明人： Robert M. Borzilleri , Rajeev S. Bhide , John S. Tokarski , Peter Zheng , Ligang Qian , Zhen-Wei Cai
IPC分类号： A61K31/44 , C07D417/12
CPC分类号： C07D277/42 , C07D417/12 , C07D417/14
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
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公开(公告)号：US20100029676A1
公开(公告)日：2010-02-04
申请号：US12092360
申请日：2006-11-03
申请人： Charles L. Sawyers , Michael Burgess , Neil Pravin Shah , Francis Y. Lee , John S. Tokarski , Herbert E. Klei
发明人： Charles L. Sawyers , Michael Burgess , Neil Pravin Shah , Francis Y. Lee , John S. Tokarski , Herbert E. Klei
IPC分类号： A61K31/497 , C12Q1/48 , G01N33/53 , C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/106 , C12Q2600/136
摘要： The present invention relates to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins.
摘要翻译： 本发明涉及突变型BCR-ABL激酶蛋白，以及可用于治疗病症（例如涉及表达这种突变型BCR-ABL激酶蛋白的细胞）的癌症的诊断和治疗方法和组合物。
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公开(公告)号：US07141571B2
公开(公告)日：2006-11-28
申请号：US11019901
申请日：2004-12-22
申请人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Ping Chen , Harold Mastalerz , Derek J. Norris , John S. Tokarski , Yufen Zhao , Wen-Ching Han
发明人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Ping Chen , Harold Mastalerz , Derek J. Norris , John S. Tokarski , Yufen Zhao , Wen-Ching Han
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其成为抗增殖剂。 式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。
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公开(公告)号：US07880004B2
公开(公告)日：2011-02-01
申请号：US11521035
申请日：2006-09-14
IPC分类号： A61K31/444 , A61K31/437 , C07D471/04 , C07D213/64
CPC分类号： C07D213/75 , C07D471/04
摘要： The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:
摘要翻译： 本发明涉及可用于治疗具有下式的癌症的化合物：
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公开(公告)号：US07297695B2
公开(公告)日：2007-11-20
申请号：US11426479
申请日：2006-06-26
申请人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Ping Chen , Harold Mastalerz , Derek J. Norris , John S. Tokarski , Yufen Zhao , Wen-Ching Han
发明人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Ping Chen , Harold Mastalerz , Derek J. Norris , John S. Tokarski , Yufen Zhao , Wen-Ching Han
IPC分类号： C07D487/04 , C07D401/06 , C07D401/14 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其成为抗增殖剂。 式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。
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10.发明申请PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 有权吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途公开(公告)号：US20140005146A1
公开(公告)日：2014-01-02
申请号：US14005572
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐。 式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。
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