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公开(公告)号：US07534881B2
公开(公告)日：2009-05-19
申请号：US11168682
申请日：2005-06-28
申请人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen T. Wrobleski
发明人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen T. Wrobleski
IPC分类号： C07D487/04 , C07D207/30 , C07D207/50
CPC分类号： C07D487/04 , C07D487/14
摘要： A method for aminating pyrrole derivatives and for preparing pyrrolotriazine compounds having the formula V,
摘要翻译： 用于胺化吡咯衍生物和制备具有式V的吡咯并三嗪化合物的方法，
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2.发明授权Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 失效制备用作激酶抑制剂的吡咯并三嗪化合物的方法公开(公告)号：US06867300B2
公开(公告)日：2005-03-15
申请号：US10289010
申请日：2002-11-06
申请人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
发明人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
IPC分类号： A61P11/06 , A61P19/02 , A61P19/10 , C07D207/50 , C07D487/04 , C07D519/00 , A61K31/53
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译： 制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R1至R6和Z如说明书所述。 根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。 该步骤之后环化形成吡咯并三嗪核心。
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3.发明授权Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 有权制备用作激酶抑制剂的吡咯并三嗪化合物的方法公开(公告)号：US07211666B2
公开(公告)日：2007-05-01
申请号：US11019788
申请日：2004-12-22
申请人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
发明人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
IPC分类号： C07D487/04 , C07D207/36
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译： 制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R 1至R 6和Z如 规范。 根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。 该步骤之后环化形成吡咯并三嗪核心。
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4.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：US20140011800A1
公开(公告)日：2014-01-09
申请号：US14005568
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , JIngwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Hu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , JIngwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Hu , Bingwei Vera Yang
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
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JAK3的酪氨酸激酶活性，从而使其可用于治疗炎症和自身免疫性疾病。
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5.发明授权公开(公告)号：US07642257B2
公开(公告)日：2010-01-05
申请号：US12047550
申请日：2008-03-13
申请人： Jagabandhu Das , John Hynes , Katerina Leftheris , Shuqun Lin , Stephen T. Wrobleski , Hong Wu
发明人： Jagabandhu Das , John Hynes , Katerina Leftheris , Shuqun Lin , Stephen T. Wrobleski , Hong Wu
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.
摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R，R1，R2，R5，R6a，R6b，J，K，X和Z如 规范。
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6.发明授权公开(公告)号：US07419978B2
公开(公告)日：2008-09-02
申请号：US10970420
申请日：2004-10-21
申请人： Jagabandhu Das , John Hynes , Katerina Leftheris , Shuqun Lin , Stephen T. Wrobleski , Hong Wu
发明人： Jagabandhu Das , John Hynes , Katerina Leftheris , Shuqun Lin , Stephen T. Wrobleski , Hong Wu
IPC分类号： C07D487/04 , C07D487/14 , A61K31/53 , A61P19/02 , A61P19/10
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.
摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R 1，R 2，R 2，R 2， R 5，R 6a，R 6b，J，K，X和Z如说明书中所述。
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7.发明授权Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors 失效治疗p38激酶相关病症的方法和可用作激酶抑制剂的吡咯并三嗪化合物公开(公告)号：US06670357B2
公开(公告)日：2003-12-30
申请号：US10036293
申请日：2001-11-07
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups —ZR4R5 taken together comprise an —NH-substituted aryl.
摘要翻译： 公开了治疗与p38激酶活性相关的一种或多种病症的方法，包括向有需要的患者施用至少一种具有式（I）的化合物或其药学上可接受的盐，前药或溶剂化物，其中R 3是氢， 甲基，全氟甲基，甲氧基，卤素，氰基或NH 2，优选甲基，X，R 1至R 6和Z如说明书所述。 有利的是基团-ZR 4 R 5一起包含-NH-取代的芳基。
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8.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：US20080171741A1
公开(公告)日：2008-07-17
申请号：US11923760
申请日：2007-10-25
申请人： Stephen T. Wrobleski , Jagabandhu Das , T.G. Murali Dhar , Alaric J. Dyckman , John Hynes , Katerina Leftheris , James Lin , Shuqun Lin
发明人： Stephen T. Wrobleski , Jagabandhu Das , T.G. Murali Dhar , Alaric J. Dyckman , John Hynes , Katerina Leftheris , James Lin , Shuqun Lin
IPC分类号： A61K31/5377 , C07D261/06 , C07D271/10 , C07D271/06 , C07D211/86 , C07D253/06 , C07D333/06 , C07D413/10 , A61P29/00 , C07D413/06 , A61K31/42 , A61K31/4245 , A61K31/4412 , A61K31/53 , A61K31/381
CPC分类号： C07D261/18 , C07C237/42 , C07C2601/02 , C07D207/456 , C07D209/08 , C07D209/42 , C07D211/62 , C07D213/81 , C07D213/82 , C07D231/56 , C07D233/90 , C07D235/06 , C07D249/06 , C07D271/06 , C07D271/10 , C07D275/03 , C07D295/192 , C07D307/68 , C07D333/38 , C07D409/04 , C07D487/04 , C07D513/04
摘要： A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译： 式I化合物及其对映异构体，非对映异构体和药学上可接受的盐。 还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。
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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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