- Arylamine compound, pharmaceutical composition containing arylamine compound as well as preparation method and application of arylamine compound
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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.
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Paragraph 0362-0363; 0366-0367
(2021/03/31)
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- Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators
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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.
- Kolari?, Anja,?vajger, Urban,Toma?i?, Tihomir,Brox, Regine,Frank, Theresa,Minovski, Nikola,Tschammer, Nuska,Anderluh, Marko
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- AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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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
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Paragraph 0297-0298
(2015/03/16)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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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
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Page/Page column 40
(2014/06/23)
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- AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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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
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Page/Page column 70; 72
(2013/04/10)
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- Efficient N-arylation catalyzed by a copper(I) pyrazolyl-nicotinic acid system
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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.
- Liu, Hai-Yang,Yu, Zhen-Tao,Yuan, Yong-Jun,Yu, Tao,Zou, Zhi-Gang
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body text
p. 9141 - 9144
(2011/01/12)
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- FUSED QUINOLINE DERIVATIVE AND USE THEREOF
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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.
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Page/Page column 125
(2008/06/13)
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