- Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)
-
The invention discloses a benzoimidazo [2, 1-b] thiazole compound and application thereof, and belongs to the technical field of medicines. The inhibitory activity of the synthesized benzimidazo [2, 1-b] thiazole analogues on FLTT3 is more than 90%, wherein the compounds (compounds 2 , 4, 6, 8 and 10) are IC of FLTT3-ITD kinase. 50 Lower value, in particular compound 2, IC IC50 The value is only 5.60 nm, and therefore the compound of the present invention may be used as an inhibitor FLTT3, or for preparing a drug capable of modulating or suppressing diseases associated with abnormal cell proliferation by affecting the enzymatic activity of one or more tyrosine kinases and interfering with aberrant cell proliferation, having a wide application prospect. (by machine translation)
- -
-
-
- Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors
-
As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.
- Jiao, Xiaoyu,Tang, Chunlei,Zhang, Lixun,Zhang, Qing,Zhang, Yongjie,Zhao, Kuantao
-
-
- PROCESS FOR THE PREPARATION OF IMIDAZO[2,1-B][1,3]BENZOTHIAZOLE DERIVATIVES
-
Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)- N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-fe][l,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert- Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-and][l,3]benzo- thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers. N-(5-ferf-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl- ethoxy)imidazo[2,l-and][l,3]benzothiazol-2-yl]phenyl}urea is represented by the structure:
- -
-
-
- NEW AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY
-
The present invention concerns novel aminoacids derivatives, in particular some aminoacid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.
- -
-
-
- IMIDAZOLOTHIAZOLE COMPOUNDS AS MODULATORS OF PROTEIN KINASE
-
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
- -
-
Page/Page column 78-79
(2010/06/11)
-
- SOLID FORMS COMPRISING N-(5-TERT-BUTYL-ISOXAZOL-3-YL)-N'-{4-[7-(2-MORPHOLIN-4-YL-ETHOXY)IMIDAZO[2,1-B][1,3]BENZOTHIAZOL-2-YL]PHENYL}UREA, COMPOSITIONS THEREOF, AND USES THEREWITH
-
Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin- 4-yl-ethoxy)imidazo[2,l-b][l,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatmen
- -
-
Page/Page column 85
(2009/04/25)
-
- Identification of N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2- morpholin-4-yl-ethoxy)imidazo-[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor
-
Treatment of AML patients with small molecule inhibitors of FLT3 kinase has been explored as a viable therapy. However, these agents are found to be less than optimal for the treatment of AML because of lack of sufficient potency or suboptimal oral pharma
- Chao, Qi,Sprankle, Kelly G.,Grotzfeld, Robert M.,Lai, Andiliy G.,Carter, Todd A.,Velasco, Anne Marie,Gunawardane, Ruwanthi N.,Cramer, Merryl D.,Gardner, Michael F.,James, Joyce,Zarrinkar, Patrick P.,Patel, Hitesh K.,Bhagwat, Shripad S.
-
experimental part
p. 7808 - 7816
(2010/09/08)
-
- Imidazolothiazole compounds for the treatment of disease
-
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
- -
-
Page/Page column 39-40
(2008/06/13)
-