- Substituted heteroaryl compounds and compositions and uses thereof
-
The invention provides a substituted heteroaryl compound and a composition thereof, and applications of the compound and the composition. The compound is a compound as shown in a formula I, or stereoisomer, tautomer, oxynitride, solvate, metabolite, pharmaceutically-acceptable salt or prodrug of the compound as shown in the formula I. The invention also provides a pharmaceutical composition containing the above-mentioned compound; and the above-mentioned compound and the pharmaceutical composition are capable of adjusting the activity of JAK kinases and are applied in prevention, treatment, therapy and alleviation of JAK kinase mediated diseases or disorders.
- -
-
Paragraph 0514; 0515; 0516; 0517
(2017/12/27)
-
- 2 - amino-pyrrolo [1, 2 - f] [1, 2, 4] triazine compounds, synthetic method and application
-
The invention discloses 2-aminopyrrolo[1,2-f][1,2,4]triazine compounds, and a synthesis method and application thereof, particularly 2-aminopyrrolo[1,2-f][1,2,4]triazine compounds, or pharmaceutically acceptable salts, hydrate, solvate or prodrug thereof.
- -
-
Paragraph 0066; 0069; 0070
(2017/07/01)
-
- Synthesis and medical application of pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound
-
The invention discloses a synthesis and medical application of pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound. The compound belongs to a novel-structure compound. The synthesis method is high in operating safety, mild in reaction condition and suitable for industrial production. The activity and the selectivity of BTK kinase and the in-vitro proliferation activity of a leukemia cell line are test, it is verified that the compound has the selective and irreversible inhibition effect on the BTK kinase, and has the different-degree inhibition effect on leukemia cells. According to measurement, the compound also has the good anti-arthritic activity on a collagen-induced arthritis (rCIA) model. The pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound can be used for preparing medicine for treating arthritis and leukemia.
- -
-
Paragraph 0030; 0031; 0034; 0035; 0038; 0039; 0042; 0043
(2017/07/31)
-
- Heterocyclic amines Hedgehog signal pathway inhibitor
-
The invention relates to the field of biological medicine, in particular to a heterocyclic amine compound and an application thereof, namely a general formula (I) compound and acceptable salt in the pharmaceutical field. The compound can be used in the Hedgehog signal transduction inhibitor application and various medical applications (please see the formula in the specification). The invention further relates to a preparation method with the general formula (I).
- -
-
Paragraph 0131; 0135; 0136
(2017/10/06)
-
- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
-
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a JAK-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated disease.
- -
-
Paragraph 0341
(2016/12/22)
-
- Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors
-
A novel series of Hh signaling pathway inhibitors were designed by replacing the pyrimidine skeleton of our earlier reported lead compound 1 with pyrrolo[2,1-f][1,2,4]triazine scaffold. Starting from this new scaffold, SAR exploration was investigated based on structural modification on A-ring, C-ring and D-ring. And several much potent compounds were studies in vivo to profile their pharmacokinetic properties. Finally, optimization leads to the identification of compound 19a, a potent Hh signaling pathway inhibitor with superior potency in vitro and satisfactory pharmacokinetic properties in vivo.
- Xin, Minhang,Zhang, Liandi,Tang, Feng,Tu, Chongxing,Wen, Jun,Zhao, Xinge,Liu, Zhaoyu,Cheng, Lingfei,Shen, Han
-
p. 1429 - 1440
(2014/03/21)
-
- JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF
-
Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
- -
-
Page/Page column 88-89
(2010/04/03)
-
- AURORA KINASE MODULATORS AND METHOD OF USE
-
The present invention relates to chemical compounds having a general formula (I) wherein A1-5 and 7-8, D', L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
- -
-
Page/Page column 47
(2009/10/22)
-
- HCV INHIBITING BI-CYCLIC PYRIMIDINES
-
The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for pre
- -
-
Page/Page column 50; 51
(2010/10/20)
-
- Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template
-
The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochemical inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biological activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochemical. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.
- Hunt, John T.,Mitt, Toomas,Borzilleri, Robert,Gullo-Brown, Johnni,Fargnoli, Joseph,Fink, Brian,Han, Wen-Ching,Mortillo, Steven,Vite, Gregory,Wautlet, Barri,Wong, Tai,Yu, Chiang,Zheng, Xiaoping,Bhide, Rajeev
-
p. 4054 - 4059
(2007/10/03)
-
- Synthesis of pyrrolo[2,1-f][1,2,4]triazine congeners of nucleic acid purines via the N-amination of 2-substituted pyrroles
-
The synthesis of several new 4-mono- and 2,4-disubstituted pyrrolo[2,1-f][1,2,4]triazines is described. Key 1-aminopyrrole-2-carbonitrile intermediates 3 and 15 were obtained by N-amination of the corresponding pyrrole-2-carboxaldehyde followed by CHO → CN conversion with either hydroxylamine-O-sulfonic acid for 3 or O-mesitylenesulfonylhydroxylamine for 15. Cyclization of 3 or 15 with a variety of amidine reagents or, after conversion of 3 to its corresponding amide, base-catalyzed annulation completed the synthesis of the title products.
- Patil,Otter,Klein
-
p. 781 - 786
(2007/10/02)
-