253315-22-9Relevant articles and documents
Arylamine compound, pharmaceutical composition containing arylamine compound as well as preparation method and application of arylamine compound
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Paragraph 0362-0363; 0366-0367, (2021/03/31)
The present invention relates to an arylamine compound of a formula (I), a pharmaceutical composition comprising the same, a preparation method of the arylamine compound and application of the pharmaceutical composition in the prevention or treatment of diseases or conditions associated with RET activity.
Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators
Kolari?, Anja,?vajger, Urban,Toma?i?, Tihomir,Brox, Regine,Frank, Theresa,Minovski, Nikola,Tschammer, Nuska,Anderluh, Marko
, p. 68 - 90 (2018/05/26)
Based on the previously published pyrazolopyridine-based hit compound for which negative allosteric modulation of both CXCR3 and CXCR4 receptors was disclosed, we designed, synthesized and biologically evaluated a set of novel, not only negative, but also positive allosteric modulators with preserved pyrazolopyridine core. Compound 9e is a dual negative modulator, inhibiting G protein activity of both receptors. For CXCR4 receptor para-substituted aromatic group of compounds distinguishes between negative and positive modulation. Para-methoxy substitution leads to functional antagonism, while para-chloro triggers agonism. Additionally, we discovered that chemotaxis is not completely correlated with G protein pathways. This is the first work in which we have on a series of compounds successfully demonstrated that it is possible to produce selective as well as dual-acting modulators of chemokine receptors, which is very promising for future research in the field of discovery of selective or dual modulators of chemokine receptors.
AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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Paragraph 0297-0298, (2015/03/16)
The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions cont
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 40, (2014/06/23)
The present invention provides compounds of Formula (I), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophyla
AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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Page/Page column 70; 72, (2013/04/10)
The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions cont
Efficient N-arylation catalyzed by a copper(I) pyrazolyl-nicotinic acid system
Liu, Hai-Yang,Yu, Zhen-Tao,Yuan, Yong-Jun,Yu, Tao,Zou, Zhi-Gang
body text, p. 9141 - 9144 (2011/01/12)
Catalyst 6-(1H-pyrazol-1-yl)nicotinic acid L-CuCl behaves as a very active promoter of the N-arylation reactions, as it has been demonstrated with varieties of substrates under mild reaction conditions. A Cu(I) complex based on L of precatalyst has been isolated by a hydrothermal method and structurally characterized.
FUSED QUINOLINE DERIVATIVE AND USE THEREOF
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Page/Page column 125, (2008/06/13)
The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Rl is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6is (cyclic group optionally having substituent(s)) -carbonyl, and the like; R7, R8,R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7and R8,R8 and R9,and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; --- represents unsubstituted (i.e., absence) or a single bond; and --- represents a single bond or a double bond, or a salt thereof, and the like.