851087-08-6Relevant academic research and scientific papers
TRIAZOLO-PYRIMIDINE COMPOUNDS AND USES THEREOF
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Page/Page column 132, (2020/05/07)
The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
Substituted arylamine compound as well as preparation method and purpose thereof
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Paragraph 0145-0150, (2019/10/01)
The invention relates to a substituted arylamine compound as well as a preparation method and a purpose thereof, and particularly relates to the substituted arylamine compound, a pharmacologically acceptable salt, a stereisomer, a polymorphic substance, a
PYRIDINONE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS
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Page/Page column 47-48, (2019/06/11)
The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PROCESS FOR PREPARING SPRAY DRIED SOLID DISPERSIONS OF (S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3- (METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE FOR PHARMACEUTICAL PREPARATIONS
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Page/Page column 6, (2017/03/28)
A process for preparing spray dried solid dispersions of (S)-N-(3-(6- isopropoxypyridin-3-yl)-lH4ndazol-5-yl)-l-(2-(4-(4-(l-methyl-lH-l,2,4-triazol-3-yl)phenyl)- 3,6-dihydropyridin-l(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base and hypromellose acetate succinate for pharmaceutical preparations including pharmaceutical capsule preparations.
(S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3- (METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE COMPOSITIONS FOR PHARMACEUTICAL PREPARATIONS
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Page/Page column 5; 8, (2016/07/05)
A composition comprising (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)- 1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3- (methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
Mild and Regioselective N-Alkylation of 2-Pyridones in Water
Hao, Xin,Xu, Zhongmiao,Lu, Hongfu,Dai, Xuedong,Yang, Ting,Lin, Xichen,Ren, Feng
supporting information, p. 3382 - 3385 (2015/07/28)
A mild and regioselective N-alkylation reaction of 2-pyridones in water has been developed. Tween 20 (2% w/w) was added to create a micellar system for improved solubility of starting materials, which leads to enhanced reaction rates. The protocol demonstrated a wide substrate scope with good isolated yields (40-94%) for all of the 24 examples evaluated. High regioselectivity favoring N-alkylation over O-alkylation was observed for benzyl halides (>5:1), primary alkyl halides (>6:1), and bulky and less reactive secondary alkyl halides (>2.4:1).
SUBSTITUTED N-[1-CYANO-2-(PHENYL)ETHYL] 1-AMINOCYCLOALK-1-YLCARBOXAMIDE COMPOUNDS - 760
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Page/Page column 103-104, (2012/01/05)
The present invention provides compounds of formula (I) in which, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
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Page/Page column 53-54, (2011/12/02)
The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various dis
COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
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Page/Page column 56-57, (2011/12/02)
The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I wherein the variables are as defined herein.
CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 78, (2011/01/05)
This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
