515813-02-2Relevant academic research and scientific papers
NEW FYN AND VEGFR2 KINASE INHIBITORS
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Page/Page column 32, (2021/06/22)
The invention relates to a N-phenylcarbamoyl compound of Formula (I) or a pharmaceutically acceptable salt thereof for use in the inhibition of at least one of tyrosine kinase selected from Fyn and VEGFR2 in the treatment of diseases and disorders involved with one or both kinases. (Formula)
ACYLAMINO BRIDGED HETEROCYCLIC COMPOUND, AND COMPOSITION AND APPLICATION THEREOF
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Paragraph 0132, (2021/11/04)
Provided are an acylamino bridged heterocyclic compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a solvate, a crystal, or a prodrug thereof, and a pharmaceutical composition comprising the compound, and an application of the compou
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity
Angell, Richard,Aston, Nicola M.,Bamborough, Paul,Buckton, Jacky B.,Cockerill, Stuart,deBoeck, Suzanne J.,Edwards, Chris D.,Holmes, Duncan S.,Jones, Katherine L.,Laine, Dramane I.,Patel, Shila,Smee, Penny A.,Smith, Kathryn J.,Somers, Don O.,Walker, Ann L.
scheme or table, p. 4428 - 4432 (2009/04/06)
The biphenyl amides (BPAs) are a novel series of p38α MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode.
BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C
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Page/Page column 87, (2008/06/13)
A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO2-, -CO-, -NR′-CO-NR′′-, -NR′-S(O)2-, -S(O)2-NR′-, -SO2-, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C1-C2 alkylene)-NR′- or -(C1-C2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C1-C4 alkyl; - R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′ , -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents -CO-, -SO- or -S(O)2-; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -(C1-C4 alkyl)-X1, -CO2R′, -SO2NR′R′′, -S(O)2-R′, -CONR′R′′, -NR′-CO-R′′′, -NR′-S(O)2-R′′′, -CO-NR′-(C1-C4 alkyl)-NR′R′′ and -CO-O-(C1-C4 alkyl)-NR′R′′ and/or (b) 1, 2 or 3 unsubstituted substituents selected from -(C1-C4 alkyl)-X2, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 hydroxyalkyl, hydroxy, cyano, nitro and -NR′R′′, wherein X1 is -CO2R′, -SO2-R′, -NR′-CO2-R′′, -NR′-S(O)2-R′′′, -CONR′R′′ or -SO2-NR′R′′, each X2 is the same or different and is cyano, nitro or -NR′R′′, each R′ and R′′ is the same or different and represents hydrogen or C1-C4 alkyl and each R′′′ is the same or different and represents C1-C4 alkyl.
NOVEL BIAROMATIC COMPOUNDS THAT ACTIVATE PPAR TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
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Page/Page column 46; 47, (2010/10/20)
The invention relates to novel biaromatic compounds that correspond to the general formula (I) and also to the method for preparing them, and to their use in pharmaceutical compositions for use in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or alternatively in cosmetic compositions.
