Chinese Academy of Sciences

Tarapeutics Science Inc.

Precedo Pharmaceuticals Co., Ltd

Anhui New Star Pharmaceutical Development Co., Ltd.

Hefei Gracevo Bio-medicine Co., Ltd

Hefei Cosource Pharmaceutical Co., Ltd.

Beilei Wang

Yi Yang

Cheng Chen

Jing Liu

Qingsong Liu

Li Wang

Wenchao Wang

Chen Hu

Aoli Wang

Wei Wang

Ziping Qi

Hong Wu

Kailin Yu

Fengming Zou

Shuang Qi

Junjie Wang

Jiaxin Wu

Xixiang Li

Yongfei Chen

Zongru Jiang

Qingwang Liu

Wenliang Wang

Yun Wu

Zhenquan Hu

Zheng Zhao

Xiaofei Liang

Tao Ren

Juan Liu

Qiang Wang

Feng Li

Xuesong Liu

Qianmao Liang

Ziping Q

Taoshan Jiang

Feiyang Liu

Xiaochuan Liu

Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The compound and composition above can inhibit wild-type KIT and/or mutant KIT tyrosine kinase activity and treat, prevent, or alleviate diseases, disorders, or conditions associated with wild-type KIT and/or mutant KIT kinase activity.

Pan-KIT kinase inhibitor having quinoline structure and application thereof

Disclosed is a kinase inhibitor, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. Also disclosed are a pharmaceutical composition comprising the kinase inhibitor and uses and methods for inhibiting the activity of one or more tyrosine kinases selected from MST1 and a mutant thereof in a cell or subject and for preventing or treating a disease related to MST1 or a mutant thereof in a subject by using the compound or composition.

MST1 kinase inhibitor and use thereof

The present application relates to a compound serving as a selective PI3Kδ kinase inhibitor, comprising the compound shown in formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof, wherein X, R, R, R, R, Rand Rare as defined in the description. The present application also relates to a method for using the kinase inhibitor to inhibit PI3Kδ kinase activity or to treat or prevent diseases or conditions associated with tyrosine kinase activity of PI3Kδ, as well as a use thereof.

Selective PI3Kδ inhibitor and use thereof

Described herein is a kinase inhibitor compound represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug of the compound. Further described herein is a pharmaceutical composition containing the kinase inhibitor compound, as well as methods of using the compound to inhibit cKIT (especially mutant cKIT/T670I), FLT3 (comprising mutant FLT3-ITD), PDGFRα, PDGFRβ, and/or VEGFR2 kinase activity in cells or a subject, and methods for preventing or treating disorders related to cKIT (especially mutant cKIT/T670I), FLT3 (comprising mutant FLT3-ITD), PDGFRα, PDGFRβ, and/or VEGFR2 activity in a subject.

Indazole kinase inhibitor and use thereof

The present invention relates to a kinase inhibitor, comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. The present invention also relates to a pharmaceutical composition comprising the kinase inhibitor, and to uses and methods for using these compounds and compositions to inhibit the activity of wild-type FLT3, mutant FLT3-ITD, PDGFR&#x3b1; and/or PDGFR&#x3b2; kinase in a cell or a subject, as well as uses and methods of these compounds and compositions to preventing or treating kinase-associated conditions in a subject. 

Pyrimidine derivative kinase inhibitors

The present invention provides a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound of formula (I), as well as the use and method for preventing or treating FLT3-related conditions, especially conditions related to mutant FLT3 kinase (particularly, FLT3/ITD mutant kinase). 

Inhibitor of FLT3 kinase and use thereof

The present invention provides a compound represented by formula (I), or a pharmaceutically acceptable salt, a solvate, an ester, an acid, a metabolite or a prodrug thereof. The compound itself in the present invention or in combination with at least one therapeutic agent can be used for preventing or treating diseases, disorders or symptoms caused by the adjustment of the activity of tyrosine kinase C-KIT, or affected by the activity of the tyrosine kinase C-KIT or involving in the activity of the tyrosine kinase C-KIT, especially cancers or other cell proliferation diseases. 

Selective C-KIT kinase inhibitor

The present application provides a compound of Formula (I) as an inhibitor against wild-type EGFR and/or mutant EGFR, which may be used for treating human non-small cell lung cancer individually or in combination with other therapeutic agent(s). The compound of Formula (I) of the present application may be used for treating patients of drug-resistant human non-small cell lung cancer harboring wild-type EGFR and/or EGFR T790M mutation and/or EGFR L858R mutation and/or EGFR delE746_A750 mutation. 

Kinase inhibitor against wild-type and mutant EGFR

The present invention provides an inhibitor of Bruton's tyrosine kinase, which is a compound of formula (I), or its pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method for inhibiting the activity of tyrosine kinase activity or for treating a disease, disorder, or condition, which would benefit from the inhibition of Bruton's tyrosine kinase(s), by using the Bruton's tyrosine kinase inhibitor, as well application of the Bruton's tyrosine kinase inhibitor for the same. 

Irreversible bruton's tyrosine kinase inhibitor

The present application provides a compound of formula I, which is a EGFR and ALK dual inhibitor and can be used alone or in combination with other therapeutic agents to treat diseases such as non-small cell lung cancer. The compounds of the present application are useful in the treatment of diseases carrying the EGFR wild-type gene, or carrying the EGFR T790M mutant gene and/or the EGFR L858R mutant gene and/or the EGFR delE746_A750 mutant gene, or in the treatment of diseases carrying the ALK wild-type gene, ALK F1174L mutant gene and/or ALK F1196M gene and/or EML4-ALK mutant gene and/or NPM-ALK mutant gene, and can be used in the first-line treatment of anaplastic lymphoma kinase (ALK) positive late-stage non-small cell Lung cancer. 

EGFR and ALK dual inhibitor

Provided in the present invention is a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. Also provided in the present invention are a pharmaceutical composition comprising a compound of formula (I) and a use and method for preventing or treating cell proliferative conditions and/or FLT3-related conditions, in particular for conditions responding to the inhibition of FLT3 kinase (especially FLT3/ITD mutant kinases). 

The present invention provides a Bruton's tyrosine kinase inhibitor, which is a compound represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method and use of using the Bruton's tyrosine kinase inhibitor to inhibit the tyrosine kinase activity or treat diseases, disorders or symptoms benefiting from the inhibition of the Bruton's tyrosine kinase (Btk) activity. 

Bruton's tyrosine kinase inhibitor

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Anhui, China

Beilei Wang