52088-10-5Relevant academic research and scientific papers
Synthesis of 3-aryl/heteroaryl-1-methyl-1H-indazoles and evaluation of their biological activities
Mohan, Arasavelli Ananda,Sharma, Ganapavarapu V. R.,Vidavalur, Siddaiah
, p. 287 - 294 (2018/09/14)
The synthesis of 3-aryl/heteroaryl-1-methyl-1H-indazole derivatives (5a-j) was achieved from commercially available 1H-indazole through the Suzuki cross-coupling reaction. The indazoles 5a-j were synthesized through two alternative routes (Route 1 and Route 2) from the same starting material and characterized using1H nuclear magnetic resonance (NMR),13C NMR, infrared, and liquid chromatography-mass spectrometry data. The first step which is common step to both routes involves conversion of 1H-3-iodo-1H-indazole (2). The antibacterial activity of 5a-j and intermediates 3a-j was evaluated against two Gram-positive and two Gram-negative bacterial strains and anticancer activity against HT-29 and MDA-MB-231cancer cell lines.
PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
-
Paragraph 0046-0047, (2017/09/19)
The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
Palladium complexes with 1-methyl-3-phenylindazole ligands
Bulygina,Khrushcheva,Ikonnikov,Sokolov
, p. 502 - 505 (2017/09/15)
1-Methyl-3-phenylindazole reacts with lithium tetrachloropalladate and palladium acetate to give new coordination and (C,N)-cyclometallated dimeric and monomeric palladium complexes.
SUBSTITUTED 2-ANILINOPYRIMIDINE DERIVATIVES AS EGFR MODULATORS
-
Page/Page column 35-36, (2016/07/05)
This application discloses novel substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, prodrugs, and compositions thereof, which are useful for the treatment or prevention of diseases or medical conditions mediated by epidermal growth factor receptors (EGFRs), including but not limited to a variety of cancers.
HISTONE DEMETHYLASE INHIBITORS
-
Paragraph 0190; 0191; 0192; 0193, (2014/06/25)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
PYRROLOPYRAZINE KINASE INHIBITORS
-
Page/Page column 59; 60, (2013/03/28)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome
Lynch, Stephen M.,Devicente, Javier,Hermann, Johannes C.,Jaime-Figueroa, Saul,Jin, Sue,Kuglstatter, Andreas,Li, Hongju,Lovey, Allen,Menke, John,Niu, Linghao,Patel, Vaishali,Roy, Douglas,Soth, Michael,Steiner, Sandra,Tivitmahaisoon, Parcharee,Vu, Minh Diem,Yee, Calvin
, p. 2793 - 2800 (2013/07/05)
Using a structure based design approach we have identified a series of indazole substituted pyrrolopyrazines, which are potent inhibitors of JAK3. Intramolecular electronic repulsion was used as a strategy to induce a strong conformational bias within the ligand. Compounds bearing this conformation participated in a favorable hydrophobic interaction with a cysteine residue in the JAK3 binding pocket, which imparted high selectivity versus the kinome and improved selectivity within the JAK family.
COMPOUNDS, COMPOSITIONS AND METHODS
-
Page/Page column 41; 15/23, (2008/06/13)
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells, and treating cell proliferating diseases or conditions.
