专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08962622B2 Benzotriazole kinase modulators 有权
标题翻译：苯并三唑激酶调节剂
公开(公告)号：US08962622B2
公开(公告)日：2015-02-24
申请号：US11899758
申请日：2007-09-07
申请人： David Michael Goldstein , Levi Gong , Christophe Michoud , Wylie Solang Palmer , Achyutharao Sidduri
发明人： David Michael Goldstein , Levi Gong , Christophe Michoud , Wylie Solang Palmer , Achyutharao Sidduri
IPC分类号： C07D403/04 , A61K31/505 , C07D403/14
CPC分类号： C07D403/04 , C07D403/14
摘要： Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R1, R2, R3, and m are defined herein.
摘要翻译：式I的化合物调节jnk和cdk：或其药学上可接受的盐，其中R，R 1，R 2，R 3和m如本文所定义。

2. 发明申请

US20140221398A1 PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 有权
标题翻译：作为酪氨酸激酶抑制剂的吡唑并嘧啶衍生物
公开(公告)号：US20140221398A1
公开(公告)日：2014-08-07
申请号：US14117927
申请日：2012-05-16
申请人： David Michael Goldstein , Kenneth Albert Brameld
发明人： David Michael Goldstein , Kenneth Albert Brameld
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
摘要翻译：本公开提供了酪氨酸激酶抑制剂，特别是BLK，BMX，EGFR，HER2，HER4，ITK，Jak3，TEC，Btk和TXK的化合物和药学上可接受的盐，因此可用于治疗可通过抑制酪氨酸激酶如癌症和炎性疾病如关节炎等。还提供了含有这些化合物的药物组合物和药学上可接受的盐以及制备这些化合物和药学上可接受的盐的方法。

3. 发明申请

US20090270389A1 Pyrimidinyl pyridone inhibitors of kinases 失效
标题翻译：嘧啶嘧啶激酶抑制剂
公开(公告)号：US20090270389A1
公开(公告)日：2009-10-29
申请号：US12387181
申请日：2009-04-29
申请人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译：本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中A，R1，R2，R3和m如本文所述限定，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。

4. 发明授权

US06949560B2 Imidazo-substituted compounds as p38 kinase inhibitors 失效
标题翻译：咪唑取代的化合物作为p38激酶抑制剂
公开(公告)号：US06949560B2
公开(公告)日：2005-09-27
申请号：US10406364
申请日：2003-04-03
申请人： David Michael Goldstein , Ronald Charles Hawley , Alfred Sui-Ting Lui , Eric Brian Sjogren
发明人： David Michael Goldstein , Ronald Charles Hawley , Alfred Sui-Ting Lui , Eric Brian Sjogren
IPC分类号： A61P11/00 , A61P25/00 , A61P29/00 , C07D471/14 , C07D487/14 , A61K31/519 , A61P19/02 , A61P25/28
CPC分类号： C07D471/14 , C07D487/14
摘要： The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
摘要翻译：本发明公开了对应于式I的化合物：其中A，Z，Z 1，Y，R 1和R 2定义如说明书以及药物制剂，制备方法和用途。

5. 发明授权

US06451804B1 Heteroalkylamino-substituted bicyclic nitrogen heterocycles 失效
标题翻译：杂芳基氨基取代的双环氮杂环
公开(公告)号：US06451804B1
公开(公告)日：2002-09-17
申请号：US09693337
申请日：2000-10-20
申请人： James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
发明人： James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
IPC分类号： A61K31505
CPC分类号： C07D487/04
摘要： The invention provides compounds represented by the formula: wherein R1, R2, R3, R4, and n are as defined in the Summary of the Invention; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译：本发明提供由下式表示的化合物：其中R1，R2，R3，R4和n如发明概述中所定义; 和各异构体，异构体的外消旋或非外消旋混合物及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

6. 发明授权

US06444696B1 Pyrazole derivatives P38 MAP kinase inhibitors 失效
标题翻译：吡唑衍生物P38 MAP激酶抑制剂
公开(公告)号：US06444696B1
公开(公告)日：2002-09-03
申请号：US09909966
申请日：2001-07-19
申请人： David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
发明人： David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
IPC分类号： A61K314155
CPC分类号： C07D231/38 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/06
摘要： The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
摘要翻译：本发明涉及某些式（I）的吡唑衍生物：其为p-38MAP激酶抑制剂，含有它们的药物组合物，其使用方法和制备这些化合物的方法。

7. 发明授权

US08268840B2 Pyrimidinyl pyridone inhibitors of kinases 失效
标题翻译：嘧啶嘧啶激酶抑制剂
公开(公告)号：US08268840B2
公开(公告)日：2012-09-18
申请号：US12387181
申请日：2009-04-29
申请人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译：本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中A，R1，R2，R3和m如本文所述限定，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。

8. 发明授权

US08183254B2 Inhibitors of JNK 失效
标题翻译： JNK抑制剂
公开(公告)号：US08183254B2
公开(公告)日：2012-05-22
申请号：US12454210
申请日：2009-05-14
申请人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号： C07D401/14 , A61K31/506
CPC分类号： C07D401/14
摘要： The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译：本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。本申请公开了如下式I所述的JNK抑制剂的前药：其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5，Y1， Z1和Z2如本文所定义。本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

9. 发明授权

US08163906B2 Dihydroquinone and dihydronaphthridine inhibitors of JNK 有权
标题翻译：二氢醌和二氢萘并吡嗪类抑制剂
公开(公告)号：US08163906B2
公开(公告)日：2012-04-24
申请号：US12152432
申请日：2008-05-14
申请人： Sarah C. Abbot , Geneviève N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
发明人： Sarah C. Abbot , Geneviève N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
IPC分类号： C07D471/04
CPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04
摘要： Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl; Z is phenyl, cycloalkyl, heterocyclyl or heteroaryl, and is substituted with R1 and R2; R1 and R2 are each independently H, halo, CN, lower alkyl, or —Y1—Y2—Y3—R8, or R1 and R2 together form —O(CH2)nO—, where n is 1 or 2; Y1 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —S—, —SO2—, or a bond; Y2 is cycloalkylene, heterocycloalkylene, lower alkylene or a bond; Y3 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —SO2—, or a bond; R8 is H, lower alkyl, lower alkoxy, cycloalkyl, heterocycloalkyl, or —NR9R10, wherein R8 other than H is optionally substituted with lower alkyl, halo, —CF3, or —OH; R9 and R10 are each independently H or lower alkyl; R3 is OH, lower alkyl, lower alkoxy, (lower alkoxy)-lower alkoxy, or —NR9R10; R4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroxy, lower alkoxy, halo, nitro, amino, cyano, or halo-lower alkyl; R5 and R6 are each independently H, halo, cyano, lower alkyl, —CF3, lower alkoxy, —OCHF2, —NO2, or —NR9R10; R7 is H, F, Cl, methyl, or OH; R11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：式I化合物是JNK的有效调节剂：其中X是CR11或N; Y是-C（O）R 3，5元杂芳基或5元杂环基; Z是苯基，环烷基，杂环基或杂芳基，并被R1和R2取代; R1和R2各自独立地为H，卤素，CN，低级烷基或-Y1-Y2-Y3-R8，或R1和R2一起形成-O（CH 2）n O-，其中n为1或2; Y1是-O - ， - C（O） - ， - C（O）O - ， - C（O）NR 9 - ， - NR 9 C（O） - ， - S - ， - SO 2 - 或键; Y2是亚环烷基，杂环亚烷基，低级亚烷基或键; Y 3是-O - ， - C（O） - ， - C（O）O-，-C（O）NR 9 - ， - NR 9 C（O） - ， - SO 2 - 或键; R8是H，低级烷基，低级烷氧基，环烷基，杂环烷基或-NR9R10，其中R8以外的R8任选被低级烷基，卤素，-CF 3或-OH取代; R9和R10各自独立地为H或低级烷基; R3是OH，低级烷基，低级烷氧基，（低级烷氧基） - 低级烷氧基或-NR9R10; R 4是低级烷基，苯基，杂环基，环烷基，杂环烷基或杂芳基，并且任选被低级烷基，羟基，低级烷氧基，卤素，硝基，氨基，氰基或卤代低级烷基取代。 R 5和R 6各自独立地为H，卤素，氰基，低级烷基，-CF 3，低级烷氧基，-OCHF 2，-NO 2或-NR 9 R 10; R7是H，F，Cl，甲基或OH; R11是H，低级烷基，低级环烷基或苯基; 或其药学上可接受的盐。

10. 发明申请

US20090318484A1 Inhibitors of JNK 失效
标题翻译： JNK抑制剂
公开(公告)号：US20090318484A1
公开(公告)日：2009-12-24
申请号：US12454210
申请日：2009-05-14
申请人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号： A61K31/506 , C07D413/14 , A61P19/02 , A61P3/04 , A61P25/16 , A61P25/28
CPC分类号： C07D401/14
摘要： The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 areas defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译：本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。本申请公开了如下式I所述的JNK抑制剂的前药：其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5，Y1， Z1和Z2区域。本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式