1352244-77-9Relevant academic research and scientific papers
NOVEL PROTEIN KINASE INHIBITORS
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Page/Page column 51; 53-54, (2021/10/30)
The present disclosure describes novel protein kinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such protein kinase inhibitors and methods of using them for treating cancer and other diseases, conditions, or disorders, which respond to the inhibition of epidermal growth factor receptor (EGFR), anaplastic lymphoma kinase (ALK) activity, or a combination thereof, are also described.
Compound used as EGFR kinase inhibitor and application thereof
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Paragraph 0422; 0425-0428, (2021/05/22)
The invention relates to a compound used as an EGFR kinase inhibitor and application thereof, the compound has a structure as shown in a formula I, and the compound can be used for adjusting EGFR kinase activity or treating related diseases, especially non-small cell lung cancer.
THERAPEUTIC COMPOUNDS AND METHODS OF USE
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Paragraph 0612; 0613; 0614, (2021/05/21)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
Novel pyrimidine derivative showing growth inhibition of cancer cell and pharmaceutical composition comprising the same
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, (2020/12/05)
The present invention provides a novel compound represented by chemical formula 1 or a salt thereof, and a pharmaceutical composition for treating lung cancer containing the same. Since the pyrimidine derivative compound represented by the chemical formul
CARBOXAMIDE AND SULFONAMIDE DERIVATIVES USEFUL AS TEAD MODULATORS
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Page/Page column 0395-0400, (2020/03/29)
The invention is concerned with the compounds of formula (I) and formula (II): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.
Pyridine N-oxidation derivative as well as preparation method and application thereof
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Paragraph 1030-1035, (2019/08/06)
The invention relates to a pyridine N-oxidation derivative as well as a preparation method and an application thereof, in particular to a compound shown in a general formula (I), a preparation methodof the compound, pharmaceutical composition containing the compound and an application of the compound as a BRD4 inhibitor in treating related diseases such as cancer, inflammation, chronic liver diseases, diabetes, cardiovascular diseases, AIDS and the like, wherein in the general formula (I), all substituent groups are the same as definitions in the description.
6-5 FUSED RINGS AS C5a INHIBITORS
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Paragraph 0232, (2019/01/05)
The present disclosure provides, inter alia, Compounds of Formula (I) (I) or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
Spiro aryl phosphorus oxide or sulfide
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Paragraph 0566; 0567; 0568; 0569, (2016/10/08)
The invention discloses a spiro aryl phosphorus oxide or sulfide as ALK inhibitor, and in particular discloses a compound shown in a formula (I) as an ALK inhibitor or a pharmaceutically acceptable salt thereof.
BROMODOMAIN INHIBITORS
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Paragraph 0510; 0511, (2015/04/28)
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.13,7.1 9,13]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles
Breslin, Henry J.,Lane, Brandon M.,Ott, Gregory R.,Ghose, Arup K.,Angeles, Thelma S.,Albom, Mark S.,Cheng, Mangeng,Wan, Weihua,Haltiwanger, R. Curtis,Wells-Knecht, Kevin J.,Dorsey, Bruce D.
experimental part, p. 449 - 464 (2012/03/10)
A novel set of 2,4,8,22-tetraazatetracyclo[14.3.1.13,7.1 9,13]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles were prepared as potential anaplastic lymphoma kinase (ALK) inhibitors, designed to rigidly lock an energy-minimized bioactive conformation of the diaminopyrimidine (DAP) scaffold, a well-documented kinase platform. From 13 analogues prepared, macrocycle 2m showed the most promising in vitro ALK enzymatic (IC50 = 0.5 nM) and cellular (IC50 = 10 nM) activities. In addition, macrocycle 2m exhibited a favorable kinase selectivity preference for inhibition of ALK relative to the highly homologous insulin receptor (IR) kinase (IR/ALK ratio of 173). The inclusive in vitro biological results for this set of macrocycles validate this scaffold as a viable kinase template and further corroborate recent DAP/ALK solid state studies indicating that the inverted "U" shaped conformation of the acyclic DAPs is a preferred bioactive conformation.
