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1. 发明授权

US10301280B2 Compounds and methods for kinase modulation, and indications therefor 有权
公开(公告)号：US10301280B2
公开(公告)日：2019-05-28
申请号：US15620396
申请日：2017-06-12
申请人： Plexxikon Inc.
发明人： Guoxian Wu , Katrina Chan , Todd Ewing , Prabha N. Ibrahim , Jack Lin , Marika Nespi , Wayne Spevak , Ying Zhang
IPC分类号： C07D403/12 , C07D401/12 , C07D471/04 , C07D487/04 , C07D513/04 , A61K31/519 , A61K31/506 , A61K31/437 , A61K31/675 , C07F5/02 , A61K31/5377 , C07F9/6561
摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

2. 发明授权

US10227357B2 Compounds and methods for kinase modulation, and indications therefor 有权
公开(公告)号：US10227357B2
公开(公告)日：2019-03-12
申请号：US14019442
申请日：2013-09-05
申请人： Plexxikon Inc.
发明人： Jack Lin , John Buell , Katrina Chan , Todd Ewing , Prabha Ibrahim , Marika Nespi , Phuongly Pham , Songyuan Shi , Wayne Spevak , Guoxian Wu , Jiazhong Zhang , Ying Zhang
IPC分类号： C07D495/04 , A61K31/519 , C07D401/12 , A61K31/52 , C07D239/74 , A61K31/5377 , C07D491/056 , C07D473/00 , C07D487/04 , A61K31/517 , C07D519/00
摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.

3. 发明申请

US20180002332A1 SYNTHESIS OF HETEROCYCLIC COMPOUNDS 有权
公开(公告)号：US20180002332A1
公开(公告)日：2018-01-04
申请号：US15705097
申请日：2017-09-14
申请人： Plexxikon Inc.
发明人： Prabha N. Ibrahim , Jack Lin , Wayne Spevak , Jiazhong Zhang
IPC分类号： C07D471/04 , C07D403/04
CPC分类号： C07D471/04 , C07D403/04
摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.

4. 发明申请

US20170349572A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
公开(公告)号：US20170349572A1
公开(公告)日：2017-12-07
申请号：US15620396
申请日：2017-06-12
申请人： Plexxikon Inc.
发明人： Guoxian Wu , Katrina Chan , Todd Ewing , Prabha N. Ibrahim , Jack Lin , Marika Nespi , Wayne Spevak , Ying Zhang
IPC分类号： C07D401/12 , C07F5/02 , C07D513/04 , C07D487/04 , C07D403/12 , A61K31/437 , A61K31/675 , A61K31/5377 , A61K31/519 , A61K31/506 , C07F9/6561 , C07D471/04
CPC分类号： C07D401/12 , A61K31/437 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/675 , C07D403/12 , C07D471/04 , C07D487/04 , C07D513/04 , C07F5/025 , C07F9/65616
摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

5. 发明授权

US09776998B2 Synthesis of heterocyclic compounds 有权
公开(公告)号：US09776998B2
公开(公告)日：2017-10-03
申请号：US15161103
申请日：2016-05-20
申请人： Plexxikon Inc.
发明人： Prabha N. Ibrahim , Jack Lin , Wayne Spevak , Jiazhong Zhang
IPC分类号： C07D471/04 , C07D403/04
CPC分类号： C07D471/04 , C07D403/04
摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.

6. 发明申请

US20170056382A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20170056382A1
公开(公告)日：2017-03-02
申请号：US15260042
申请日：2016-09-08
申请人： Plexxikon Inc.
发明人： Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
IPC分类号： A61K31/44 , A61K31/505 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/437 , A61K31/47 , A61K31/42 , A61K31/415 , A61K31/433 , A61K31/549 , A61K31/4436 , A61K31/4439
CPC分类号： A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

7. 发明申请

US20160326162A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20160326162A1
公开(公告)日：2016-11-10
申请号：US15093660
申请日：2016-04-07
申请人： Plexxikon Inc.
发明人： Jack Lin , Phuongly Pham , John Buell , Ken Dong , Prabha Ibrahim , Wayne Spevak , Garson Tsang , Guoxian Wu , Ying Zhang
IPC分类号： C07D471/04 , A61K31/437 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , C07D487/04 , A61K31/4985 , A61K31/541 , A61K45/06 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K45/06 , C07D487/04 , C07D519/00
摘要： Compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R1, R2, Q1, Q2, and Q3, are described in this disclosure, compositions thereof, and methods and uses thereof.
摘要翻译：或其药学上可接受的盐，溶剂化物，互变异构体，异构体或氘代类似物，其中R1，R2，Q1，Q2和Q3在本公开内容中描述，其组合物，及其方法和用途。

8. 发明授权

US09096593B2 Compounds and methods for kinase modulation, and indications therefor 有权
标题翻译：用于激酶调节的化合物和方法及其适应症
公开(公告)号：US09096593B2
公开(公告)日：2015-08-04
申请号：US14033291
申请日：2013-09-20
申请人： Plexxikon Inc.
发明人： Jiazhong Zhang , Prabha N. Ibrahim , Ryan Bremer , Wayne Spevak , Hanna Cho
IPC分类号： C07D401/14 , A61K31/4427 , C07D471/04 , A61K31/437 , A61K31/506 , C07D401/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4427 , A61K31/506 , C07D401/04 , C07D401/14
摘要： Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors.
摘要翻译：其化合物及其盐，其制剂，其缀合物，其衍生物，其形式及用途。在某些方面和实施方案中，所述的化合物或其盐，其制剂，其缀合物，其衍生物或其形式在Fms蛋白激酶或Fms和Kit蛋白激酶或Fms和Flt-3蛋白激酶上具有活性。还描述了其用于治疗疾病和病症的方法，包括与Fms蛋白激酶，Kit蛋白激酶或Flt-3蛋白激酶（包括类风湿性关节炎，骨关节炎，多发性硬化症，阿尔茨海默病，帕金森氏病，肾小球性肾炎，间质性肾炎，狼疮性肾炎，肾小管坏死，糖尿病性肾病，肾肥大，急性骨髓性白血病，黑素瘤，多发性骨髓瘤，转移性乳腺癌，前列腺癌，胰腺癌，神经纤维瘤病，脑转移瘤和胃肠道间质瘤。

9. 发明申请

US20140303187A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20140303187A1
公开(公告)日：2014-10-09
申请号：US14245770
申请日：2014-04-04
申请人： Plexxikon Inc.
发明人： Guoxian Wu , Jiazhong Zhang , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , James Tsai
IPC分类号： C07D417/04 , A61K31/506
CPC分类号： A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

10. 发明申请

US20140213554A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20140213554A1
公开(公告)日：2014-07-31
申请号：US14137438
申请日：2013-12-20
申请人： Plexxikon Inc.
发明人： Guoxian Wu , Katrina Chan , Todd Ewing , Prabha N. Ibrahim , Jack Lin , Marika Nespi , Wayne Spevak , Ying Zhang
IPC分类号： C07D401/12 , A61K31/437 , C07F5/02 , C07D487/04 , C07D513/04 , C07D403/12 , A61K31/506 , A61K31/5377 , C07F9/6561 , A61K31/675 , C07D471/04 , A61K31/519
CPC分类号： C07D401/12 , A61K31/437 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/675 , C07D403/12 , C07D471/04 , C07D487/04 , C07D513/04 , C07F5/025 , C07F9/65616
摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.
摘要翻译：描述了对具有任何突变的c-kit蛋白激酶或突变c-kit蛋白激酶有活性的化合物，以及制备和使用这些化合物治疗与c-kit蛋白激酶异常活性相关的疾病和病症的方法和/或突变c-kit蛋白激酶。

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