cas 943541-40-0, ethyl2,2-difluoro-2-(quinolin-6-yl)acetate

Articles about 943541-40-0Total 9 be found

Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors
Herein, we report a novel series of highly potent and selective triazolothiadiazole c-Met inhibitors. Starting with molecule 5, we have applied structure-based drug design principles to identify the triazolothiadiazole ring system. We successfully replaced the metabolically unstable phenolic moiety with a quinoline group. Further optimization around the 5,6 bicyclic moiety led to the identification of 21. Compound 21 suffered from PDE3 selectivity issues and subsequent, structurally informed design led to the discovery of compound 23. Compound 23 has exquisite kinase selectivity, excellent potency, favorable ADME profile, and showed dose-dependent antitumor efficacy in a SNU-5 gastric cancer xenograft model.
Aronov, Alex M.,Boucher, Diane,Deininger, David D.,Ford, Pamella J.,Giroux, Simon,Lauffer, David J.,Li, Pan,Liang, Jianglin,McGinty, Kira,Moody, Cameron S.,Ronkin, Steven,Swett, Rebecca,Tang, Qing,Waal, Nathan
supporting information
p. 955 - 960
(2021/06/25)

3. 4 - dihydro - 1H - benzo [c] [1, 2] oxa boric acid compound or a pharmaceutically acceptable salt thereof and its preparation and use
The invention relates to 3,4-dihydro-1H-benzo[c][1,2]oxaboric acid compounds or pharmaceutically acceptable salts thereof, a preparation method of the compounds and application of the compounds and the salts. Concretely, the invention relates to the compound with the general formula (I) and the pharmaceutically acceptable salts, and the preparation method of the compounds. The invention also relates to a pharmaceutical composition containing the compounds or the pharmaceutically acceptable salts as a receptor tyrosine kinase inhibitor, especially as a c-Met inhibitor. The invention also relates to application of the compounds or the pharmaceutical composition to prepare medicines for preventing and/or treating diseases related to c-Met abnormity. The compounds have obvious propagation inhibition activity on SNU-5 cells, and have obvious inhibition effect on c-Met kinases activity.
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(2017/08/14)

HETEROCYCLIC HYDRAZONE COMPOUNDS AND THEIR USES TO TREAT CANCER AND INFLAMMATION
The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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(2011/02/24)

HETEROCYCLIC OXIME COMPOUNDS
The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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(2011/04/13)

AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE
The present invention relates to anhydrous and hydrated forms of Compound 1, which qre useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders.
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Page/Page column 8

(2011/12/13)

AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITORS OF C-MET PROTEIN KINASE
The present invention relates to compounds of formula (I), which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula (I) and methods of using the compositions in the treatment of proliferative disorders
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Page/Page column 28-29

(2010/12/26)

SUBSTITUTED PYRAZOLE INHIBITORS OF C-MET PROTEIN KINASE
The present invention relates to compounds of formula (I), which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula (I) and methods of using the compositions in the treatment of proliferative disorders.
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Page/Page column 25-26

(2010/12/26)

POLYMORPHIC AND HYDRATE FORMS, SALTS AND PROCESS FOR PREPARING 6-{DIFLUORO[6-(1-METHYL-1H-PYRAZOL-4-YL)[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-3-YL]METHYL}QUINOLINE
The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.
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(2009/01/23)