137464-98-3Relevant academic research and scientific papers
NOVEL ORGANIC COMPOUND, NEAR-INFRARED FLUORESCENT CONSTANT MEDIUM CONTAINING SAME, AND METHOD FOR NANO-GRANULATING CONSTANT MEDIUM
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, (2018/12/04)
The present invention relates to a novel organic compound, a near-infrared fluorescent constant medium containing the same, and a method for nano-granulating the constant medium.
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria
O’ Neill, Paul M.,Stocks, Paul A.,Sabbani, Sunil,Roberts, Natalie L.,Amewu, Richard K.,Shore, Emma R.,Aljayyoussi, Ghaith,Angulo-Barturén, I?igo,Belén, María,Jiménez-Díaz,Bazaga, Santiago Ferrer,Martínez, María Santos,Campo, Brice,Sharma, Raman,Charman, Susan A.,Ryan, Eileen,Chen, Gong,Shackleford, David M.,Davies, Jill,Nixon, Gemma L.,Biagini, Giancarlo A.,Ward, Stephen A.
, p. 2996 - 3005 (2018/05/24)
A series of aryl carboxamide and benzylamino dispiro 1,2,4,5-tetraoxane analogues have been designed and synthesized in a short synthetic sequence from readily available starting materials. From this series of endoperoxides, molecules with in vitro IC50s versus Plasmodium falciparum (3D7) as low as 0.84 nM were identified. Based on an assessment of blood stability and in vitro microsomal stability, N205 (10a) was selected for rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models. The results indicate that the 4-benzylamino derivatives have excellent profiles with a representative of this series, N205, an excellent starting point for further lead optimization studies.
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
, p. 5577 - 5582 (2011/10/09)
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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Page/Page column 52, (2010/11/03)
The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
2-(ARYL)AZACYCLYLMETHYL CARBOXYLATES, SULFONATES, PHOSPHONATES, PHOSPHINATES AND HETEROCYCLES AS S1P RECEPTOR AGONISTS
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Page/Page column 51, (2008/06/13)
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by mo
A fischer-indole approach to pyrrolo[2,3-d]pyrimidines
Taylor, Edward C.,Hu, Baihua
, p. 323 - 338 (2007/10/03)
Several new 5,6-disubstituted pyrrolo[2,3-d]pyrimidines have been prepared by thermolysis of ketone hydrazones of 2-amino-6-hydrazino4(3H)-oxopyrimidine (8) (the Fischer-Indole Synthesis).
Liquid crystalline mixtures containing 3,4-difluorophenyl-substituted bicyclohexyls
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, (2008/06/13)
Compounds of formula STR1 wherein Z is a single covalent bond or --CH2 CH2 --, and R1 is 1E-alkenyl with 2-12 carbon atoms, liquid crystalline mixtures containing them and their use for electro-optical purposes.
Synthesis and antifolate properties of 5,10-ethano-5,10-dideazaaminopterin
DeGraw,Christie,Colwell,Sirotnak
, p. 320 - 324 (2007/10/02)
2-Carbomethoxy-4-(p-carbomethoxyphenyl)cyclohexanone was prepared in a four-step process and thermally condensed with 2,4,6-triaminopyrimidine to afford methyl 2,4-diamino-4-deoxy-7-hydroxy-5,10-ethano-5,10-dideazapteroate. Reduction of the 7-oxo function with borane gave the 7,8-dihydro pterin which was subsequently oxidized to the fully aromatic pteroate ester with dicyanodichlorobenzoquinone. Saponification of the benzoate ester, coupling with diethyl glutamate and final ester hydrolysis afforded the title compound. This novel deazaaminopterin analogue was approximately as potent as methotrexate in vitro in terms of DHFR and L1210 cell growth inhibition. There are indications of diastereomeric differences in the enzyme inhibition measurements. A significant transport advantage over MTX for influx into L1210 cells was observed. The compound was active against the E 0771 murine mammary solid tumor, but further investigation with individual diastereomers is required to define the ED50.
Bicyclohexyl derivatives
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, (2008/06/13)
Compounds of the formula STR1 wherein Z1 is a single covalent bond or --CH2 CH2 --, X1 is hydrogen, fluorine or chlorine and R1 is 1E-alkenyl with 2 to 12 carbon atoms, their preparation, liquid cryst
