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1. 发明申请

US20190389904A2 MALT1 INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：US20190389904A2
公开(公告)日：2019-12-26
申请号：US15755951
申请日：2016-08-26
申请人： Nathanael S. Gray , David A. Scott , John Hatcher , Spandan Chennamadhavuni , Ari M. Melnick , Lorena Fontan Gabas , Hao Wu , Qi Qiao , Guangyan Du
发明人： Nathanael S. Gray , David A. Scott , John Hatcher , Spandan Chennamadhavuni , Ari M. Melnick , Lorena Fontan Gabas , Hao Wu , Qi Qiao , Guangyan Du
IPC分类号： C07K5/11 , A61K38/07
摘要： Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, which may be useful as MALT1 inhibitors. Also provided are for the treatment of proliferative disorders (e.g., cancer (e.g., non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, MALT, lymphoma), benign neoplasm, a disease associated with angiogenesis, an autoimmune disease, an inflammatory disease, an autoinflammatory disease) by administering a compound of Formula (I).

2. 发明申请

US20120094999A1 EGFR INHIBITORS AND METHODS OF TREATING DISORDERS 有权
标题翻译： EGFR抑制剂和治疗疾病的方法
公开(公告)号：US20120094999A1
公开(公告)日：2012-04-19
申请号：US13319079
申请日：2010-05-05
申请人： Nathanael S. Gray , Pasi Janne , Michael J. Eck , Wenjun Zhou
发明人： Nathanael S. Gray , Pasi Janne , Michael J. Eck , Wenjun Zhou
IPC分类号： A61K31/52 , C07D403/12 , A61K31/506 , C07D487/04 , A61K31/519 , C07D401/12 , A61K31/53 , C07D471/04 , C07D239/48 , C07D413/12 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61P35/00 , C07D401/14 , C07D403/14 , C07D473/16
CPC分类号： C07D473/16 , C07D403/14
摘要： The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
摘要翻译：本发明涉及能够调节表皮生长因子受体（EGFR）的新型嘧啶，吡咯并 - 吡啶，吡啶，嘌呤和三嗪化合物，包括Her-激酶，以及这些化合物在治疗中的用途各种疾病，病症或病症。

3. 发明申请

US20110312908A1 SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE 有权
标题翻译： BCR-ABL的小分子麻醉抑制剂和使用方法
公开(公告)号：US20110312908A1
公开(公告)日：2011-12-22
申请号：US12745496
申请日：2008-11-28
申请人： Nathanael S. Gray , Jianming Zhang , Barun Okram , Xianming Deng , Jae Won Chang , Amy Wojciechowski
发明人： Nathanael S. Gray , Jianming Zhang , Barun Okram , Xianming Deng , Jae Won Chang , Amy Wojciechowski
IPC分类号： A61K31/7076 , C07D495/04 , C07D239/94 , C07D413/12 , A61P35/00 , C07H19/167 , A61K31/519 , A61K31/5377 , A61K31/517 , A61K31/506 , C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K31/7076 , A61K45/06 , C07D239/42 , C07D239/94 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04 , C07D473/34 , C07D495/04 , C07H19/16 , Y02A50/401
摘要： The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.
摘要翻译：本发明提供了通过胺连接基与芳基连接的新的杂芳基化合物。这些化合物可用于治疗癌症。

4. 发明申请

US20090181991A1 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：US20090181991A1
公开(公告)日：2009-07-16
申请号：US12090844
申请日：2006-11-03
申请人： Qiong Zhang , Nathanael S. Gray , Yi Liu , Qiang Ding , Tetsuo Uno
发明人： Qiong Zhang , Nathanael S. Gray , Yi Liu , Qiang Ding , Tetsuo Uno
IPC分类号： A61K31/505 , C07D239/42 , C07D213/74 , A61K31/44
CPC分类号： C07D239/48 , C07D213/74 , C07D239/42 , C07D239/47 , C07D239/52
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 Lck, IR, IGF-1R, JNK1α, Flt3, Fes, EFGR (Her-1, erbB-1), cSRC, CDK1/cyclinB, c-RAF, BTK, Bmx, Axl, Aurora-A, Abl, BCR-Abl, TrkB, Tie2, Syk, SGK, SAPK2a, Rsk1 and Met 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Lck，IR，IGF异常活化的疾病或病症 -1R，JNK1alpha，Flt3，Fes，EFGR（Her-1，erbB-1），cSRC，CDK1 / cyclinB，c-RAF，BTK，Bmx，Ax1，Aurora-A，Abl，BCR-Abl，TrkB，Tie2， Syk，SGK，SAPK2a，Rsk1和Met激酶。

5. 发明授权

US07462629B2 Immunosuppressant compounds and compositions 有权
标题翻译：免疫抑制剂化合物和组合物
公开(公告)号：US07462629B2
公开(公告)日：2008-12-09
申请号：US10849450
申请日：2004-05-19
申请人： Shifeng Pan , Nathanael S. Gray , Yuan Mi , Yi Fan , Wenqi Gao
发明人： Shifeng Pan , Nathanael S. Gray , Yuan Mi , Yi Fan , Wenqi Gao
IPC分类号： A61K31/4725 , A61K31/4035 , A61K31/397 , C07D217/12 , C07D209/44 , C07D205/12
CPC分类号： C07C323/32 , C07C317/32 , C07C2601/14 , C07D205/04
摘要： The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
摘要翻译：本发明涉及免疫抑制剂，其生产方法及其用途和含有它们的药物组合物。本发明提供了一类新颖的化合物，其可用于治疗或预防由淋巴细胞相互作用介导的疾病或病症，特别是与EDG受体介导的信号转导相关的疾病。

6. 发明申请

US20080300267A1 Compounds and Compositions as Protein Kinase Inhibitors 审中-公开
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：US20080300267A1
公开(公告)日：2008-12-04
申请号：US11914210
申请日：2006-05-15
申请人： Barun Okram , Pingda Ren , Nathanael S. Gray
发明人： Barun Okram , Pingda Ren , Nathanael S. Gray
IPC分类号： A61K31/506 , C07D403/14 , A61P35/00 , A61P37/02 , A61P25/00
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 CDKs, Aurora, Jak2, Rock, CAMKII, FLT3, Tie2, TrkB, FGFR3 and KDR 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CDK异常激活的Aurora，Jak2的疾病或病症，Rock，CAMKII，FLT3，Tie2，TrkB，FGFR3和KDR激酶。

7. 发明授权

US07273864B2 Compositions and methods for inducing osteogenesis 失效
标题翻译：诱导成骨的组合物和方法
公开(公告)号：US07273864B2
公开(公告)日：2007-09-25
申请号：US10687220
申请日：2003-10-15
申请人： Xu Wu , Sheng Ding , Nathanael S. Gray
发明人： Xu Wu , Sheng Ding , Nathanael S. Gray
IPC分类号： C07D473/40 , C07D473/34 , C07D473/18 , A61K31/522 , A61K31/52
CPC分类号： C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40
摘要： The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: wherein R4 is a functional group including, for example, C1-4alkyl, C3-8cycloalkyl, hydroxyl-C1-4alkyl, aryl-C0-3alkyl, substituted with 0-2 R4a groups, and heterocyclo-C0-2alkyl, optionally substituted with C1-4alkyl; R5 is hydrogen and R6 is a functional group including, for example, halogen, C1-4alkyl, —C(O)—C1-4alkyl, —SO2—N(R2b R2b), halo—C1-4alkyl, —O-aryl and —N(R7 R8), or when R5 and R6 are on adjacent ring atoms they are optionally taken together to form —O—(CH2)1-2—O—; and all pharmaceutically acceptable salts and hydrates thereof.
摘要翻译：本发明提供了使用下式化合物将哺乳动物细胞分化和转分化成成骨细胞谱系细胞的组合物和方法：其中R 4是包括例如C 1 -C 6烷基的官能团， 1-4个碳原子的烷基，C 3-8环烷基，羟基-C 1-4烷基，芳基-C 0-3-3烷基，被0-2个R 4a取代的烷基和任选被C 1-4烷基取代的杂环-C 0-2-2烷基; R 5是氢，R 6是官能团，包括例如卤素，C 1-4烷基，-C（O） -C 1-4烷基，-SO 2 -N（R 2b，R 2b），卤代-C 1-4芳烷基，-O-芳基和-N（R 7 R 8），或当R 5 O >和R 6'在相邻的环原子上，它们任选地一起形成-O-（CH 2）2 - N 2 -O- ; 及其所有药学上可接受的盐和水合物。

8. 发明授权

US06255485B1 Purine inhibitors of protein kinases, G proteins and polymerases 有权
标题翻译：蛋白激酶，G蛋白和聚合酶的嘌呤抑制剂
公开(公告)号：US06255485B1
公开(公告)日：2001-07-03
申请号：US09130255
申请日：1998-08-06
申请人： Nathanael S. Gray , Peter Schultz , Sung-Hou Kim , Laurent Meijer
发明人： Nathanael S. Gray , Peter Schultz , Sung-Hou Kim , Laurent Meijer
IPC分类号： C07D47316
CPC分类号： A61K31/52 , C07D473/16
摘要： The present invention relates to purine analogs that inhibit, inter alia, protein kinases, G-proteins and polymerases. In addition, the present invention relates to methods of using such purine analogs to inhibit protein kinases, G-proteins, polymerases and other cellular processes and to treat cellular proliferative diseases.
摘要翻译：本发明涉及嘌呤类似物，其特别是抑制蛋白激酶，G蛋白和聚合酶。此外，本发明涉及使用这种嘌呤类似物来抑制蛋白激酶，G蛋白，聚合酶和其它细胞过程以及治疗细胞增殖性疾病的方法。

9. 发明授权

US09908884B2 EGFR inhibitors and methods of treating disorders 有权
公开(公告)号：US09908884B2
公开(公告)日：2018-03-06
申请号：US13319079
申请日：2010-05-05
申请人： Nathanael S. Gray , Pasi Janne , Michael J. Eck , Wenjun Zhou
发明人： Nathanael S. Gray , Pasi Janne , Michael J. Eck , Wenjun Zhou
IPC分类号： C07D403/12 , C07D473/16 , C07D403/14
CPC分类号： C07D473/16 , C07D403/14
摘要： The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

10. 发明申请

US20100298295A1 2-BIPHENYLAMINO-4-AMINOPYRIMIDINE DERIVATIVES AS KINASE INHIBITORS 失效
标题翻译：作为激酶抑制剂的2-联苯胺-4-氨基吡啶衍生物
公开(公告)号：US20100298295A1
公开(公告)日：2010-11-25
申请号：US12675379
申请日：2008-08-27
申请人： Thomas H. Marsilje , Wenshuo Lu , Bei Chen , Xiaohui He , Badry Bursulaya , Christian Cho-Hua Lee , Nathanael S. Gray
发明人： Thomas H. Marsilje , Wenshuo Lu , Bei Chen , Xiaohui He , Badry Bursulaya , Christian Cho-Hua Lee , Nathanael S. Gray
IPC分类号： A61K31/55 , C07D403/12 , A61K31/506 , C07D409/12 , C07D413/12 , C07D401/12 , C07D417/12 , C07D413/14 , A61K31/5377 , C07D239/48 , A61K31/505 , A61P35/00 , A61P31/00 , A61P37/06 , C12N5/02
CPC分类号： C07D403/12 , C07D239/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK).
摘要翻译：本发明提供式（1）的新型嘧啶衍生物及其药物组合物，以及使用这些化合物的方法。例如，本发明的嘧啶衍生物可用于治疗，改善或预防对胰岛素样生长因子（IGF-1R）或间变性淋巴瘤激酶（ALK）的抑制作出反应的病症。

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