Patent classifications
C07D309/34
Pharmacophores, compounds and methods having application in the treatment of cancer through inhibition of CYP17A1 and CYP19A1
The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH.sub.3; and NH.sub.2; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.
Pharmacophores, compounds and methods having application in the treatment of cancer through inhibition of CYP17A1 and CYP19A1
The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH.sub.3; and NH.sub.2; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.
ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE
An organic electroluminescence device includes an anode, a cathode, a first emitting layer, and a second emitting layer provided between the first emitting layer and the cathode, in which the first emitting layer contains a first compound represented by a formula (101) below as a first host material, the second emitting layer contains a second compound represented by a formula (2) below as a second host material, and the first emitting layer is in direct contact with the second emitting layer.
##STR00001##
ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE
An organic electroluminescence device includes an anode, a cathode, a first emitting layer, and a second emitting layer provided between the first emitting layer and the cathode, in which the first emitting layer contains a first compound represented by a formula (101) below as a first host material, the second emitting layer contains a second compound represented by a formula (2) below as a second host material, and the first emitting layer is in direct contact with the second emitting layer.
##STR00001##
Process for the preparation of pyrylium salts
The present invention relates to the process for the preparation of Pyrylium salts having the formula represented below. Present invention provide a simplified method of producing symmetrical and unsymmetrical pyrylium salts. The invention explores readily available starting materials with reaction conditions which are suitable for industrial scale applications. All the synthesized compounds were confirmed by various spectroscopic techniques such as Fourier transform infrared spectroscopy, 1H NMR, 13C NMR, 19F NMR spectroscopy, and single-crystal X-ray analysis. Mass of the compounds confirmed by HRMS analysis. ##STR00001##
Process for the preparation of pyrylium salts
The present invention relates to the process for the preparation of Pyrylium salts having the formula represented below. Present invention provide a simplified method of producing symmetrical and unsymmetrical pyrylium salts. The invention explores readily available starting materials with reaction conditions which are suitable for industrial scale applications. All the synthesized compounds were confirmed by various spectroscopic techniques such as Fourier transform infrared spectroscopy, 1H NMR, 13C NMR, 19F NMR spectroscopy, and single-crystal X-ray analysis. Mass of the compounds confirmed by HRMS analysis. ##STR00001##
HOST MATERIAL, COMPOSITION, AND ORGANIC ELECTROLUMINESCENT ELEMENT
To improve the emission efficiency, the driving voltage and the lifetime of an organic light-emitting device using a delayed fluorescent material. A host material for a delayed fluorescent material, containing a compound represented by the following general formula: R.sup.1 to R.sup.5 each are a substituent not containing a cyano group. n1 to n5 each are 0 to 4, Ar is a monocyclic arylene group or a monocyclic heteroarylene group.
##STR00001##
ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT
The present disclosure provides an organic compound that has a mother skeleton with a fused-ring structure, an electron-withdrawing group bonded to the mother skeleton, and an electron-donating group bonded to the mother skeleton, wherein the electron-withdrawing group is bonded at a position satisfying the following relationship in the mother skeleton.
Σ|C.sub.H|>Σ|C.sub.L| (1)
(C.sub.H: 2PZ atomic orbital coefficient of a carbon at a substitution site in the HOMO of the mother skeleton)
(C.sub.L: 2PZ atomic orbital coefficient of the carbon at the substitution site in the LUMO of the mother skeleton)
ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT
The present disclosure provides an organic compound that has a mother skeleton with a fused-ring structure, an electron-withdrawing group bonded to the mother skeleton, and an electron-donating group bonded to the mother skeleton, wherein the electron-withdrawing group is bonded at a position satisfying the following relationship in the mother skeleton.
Σ|C.sub.H|>Σ|C.sub.L| (1)
(C.sub.H: 2PZ atomic orbital coefficient of a carbon at a substitution site in the HOMO of the mother skeleton)
(C.sub.L: 2PZ atomic orbital coefficient of the carbon at the substitution site in the LUMO of the mother skeleton)
Compositions and methods for visible-light-controlled ruthenium-catalyzed olefin metathesis
The present disclosure provides compositions and methods for metathesizing a first alkenyl or alkynyl group with a second alkenyl or alkynyl group, the composition comprising a ruthenium metathesis catalyst and a photoredox catalyst that is activated by visible light.