896160-43-3

Upstream product

• 454-92-2 3-(trifluoromethyl)benzoic acid 
• 2840-04-2 5-amino-2-methylbenzoic acid 

Downstream Products

• 1630970-25-0 C₃₁H₂₉F₃N₆O₄ 
• 1431727-39-7 tert-butyl 3-(5-(2-methyl-5-(3-(trifluoromethyl)benzamido)benzamido)pyrimidin-2-ylamino)-phenylcarbamate 
• 1613228-43-5 2-methyl-N-(2-(3-propionamidophenylamino)pyrimidin-5-yl)-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-44-6 N-(2-(3-(3-(dimethylamino)propanamido)phenylamino)-pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-45-7 2-methyl-N-(2-(3-(N-propionylpropionamido)phenylamino)-pyrimidin-5-yl)-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1431727-00-2 N-(2-(3-acrylamidophenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-47-9 (E)-N-(2-(3-but-2-enamidophenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-48-0 (E)-N-(2-(3-(4-(dimethylamino)but-2-enamido)phenylamino)-pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)-benzamide 
• 1431727-02-4 2-methyl-5-(3-(trifluoromethyl)benzamido)-N-(2-(3-(vinylsulfonamido)phenylmino)pyrimidin-5-yl)benzamide 
• 1613228-49-1 N-(2-(3-(2-chloroacetamido)phenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-50-4 2-methyl-N-(2-(3-(2-(3-oxobenzo[d]isothiazol-2(3H)-yl)-acetamido)phenylamino)pyrimidin-5-yl)-5-(3-(trifluoromethyl)-benzamido)benzamide 
• 1431727-06-8 N-(2-(3-(N-acryloylacrylamido)phenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1431727-04-6 N-(2-(3-(2-acrylamidoacetamido)phenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 
• 1613228-42-4 N-(2-(4-aminophenylamino)pyrimidin-5-yl)-2-methyl-5-(3-(trifluoromethyl)benzamido)benzamide 

Relevant academic research and scientific papers

Bruton's tyrosine kinase inhibitor

The invention discloses a compound with a general formula (I), wherein the compound is capable of inhibiting Btk, and the groups are disclosed in the invention. The compound can be used for treating autoimmune diseases, heterologous immunization diseases, cancers, or thromboembolism diseases. The invention also discloses a pharmaceutical composition containing the compound represented by formula (I). The Bruton's tyrosine kinase inhibitor is capable of inhibiting the activity of Bruton's tyrosine kinas through covalent binding such as a covalent reversible mode.

Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity

Bruton's tyrosine kinase (Btk) is an attractive drug target for treating several B-cell lineage cancers. Ibrutinib is a first-in-class covalent irreversible Btk inhibitor and has demonstrated impressive effects in multiple clinical trials. Herein, we present a series of novel 2,5-diaminopyrimidine covalent irreversible inhibitors of Btk. Compared with ibrutinib, these inhibitors exhibited a different selectivity profile for the analyzed kinases as well as a dual-action mode of inhibition of both Btk activation and catalytic activity, which counteracts a negative regulation loop for Btk. Two compounds from this series, 31 and 38, showed potent antiproliferative activities toward multiple B-cell lymphoma cell lines, including germinal center B-cell-like diffuse large B cell lymphoma (GCB-DLBCL) cells. In addition, compound 31 significantly prevented tumor growth in a mouse xenograft model.

KINASE INHIBITOR AND METHOD FOR TREATMENT OF RELATED DISEASES

Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.

KINASE INHIBITOR AND METHOD FOR TREATMENT OF RELATED DISEASES

Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.

CHEMICAL COMPOUNDS

The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

PYRIDINE CARBOXAMIDE DERIVATIVES FOR USE AS ANTICANCER AGENTS

The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): (A chemical formula should be inserted here - please see paper copy enclosed herewith) (I) which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.