Patent classifications
C07D213/57
AIEgens for cancer cell imaging
The present subject matter is directed to a luminogen exhibiting aggregation induced emission, wherein T1, T2, and T3 comprise one or more polyynes as a conjugated bridge. The present subject matter is also directed to an AIEgen comprising a hydrophilic pyridium group as a strong electron-withdrawing group; a piperazine group as an electron-donating group; and a α-Cyanostilbene; wherein the AIEgen exhibits aggregation induced emission. The present subject matter is directed to a method of synthesizing an AIEgen and is further directed to a method of labeling comprising incubating a subject having cells with a conjugate formed by conjugating an AIEgen with an antibody; and selectively labeling desired cells by turn-on imaging, wherein labeling occurs when the desired cells are selectively stained by fluorescent emission of the AIEgen upon degradation of the antibody after cellular internalization of the conjugate through endocytosis.
AIEgens for cancer cell imaging
The present subject matter is directed to a luminogen exhibiting aggregation induced emission, wherein T1, T2, and T3 comprise one or more polyynes as a conjugated bridge. The present subject matter is also directed to an AIEgen comprising a hydrophilic pyridium group as a strong electron-withdrawing group; a piperazine group as an electron-donating group; and a α-Cyanostilbene; wherein the AIEgen exhibits aggregation induced emission. The present subject matter is directed to a method of synthesizing an AIEgen and is further directed to a method of labeling comprising incubating a subject having cells with a conjugate formed by conjugating an AIEgen with an antibody; and selectively labeling desired cells by turn-on imaging, wherein labeling occurs when the desired cells are selectively stained by fluorescent emission of the AIEgen upon degradation of the antibody after cellular internalization of the conjugate through endocytosis.
SUBSTITUTED 2-[3-(1-METHYL-PIPERIDIN-4-YL)-PROPYLAMINO]-PYRIMIDINE-5-CARBOXYLIC ACIDS AND AMIDES AND METHODS OF MAKING THE SAME
The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including
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SUBSTITUTED 2-[3-(1-METHYL-PIPERIDIN-4-YL)-PROPYLAMINO]-PYRIMIDINE-5-CARBOXYLIC ACIDS AND AMIDES AND METHODS OF MAKING THE SAME
The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including
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HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
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HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
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Compounds for MYC inhibition
There is disclosed a compound, a pharmaceutical composition and a method of cancer treatment with an improved Myc inhibitor compound. More specifically, there is disclosed an improved compound having with improved solubility, improved binding characteristics and better efficacy and therapeutic activity inhibiting c-MYC wherein the improved compound comprises a tri-substituted pyridine having a thiazoyl moiety at position R.sup.1 versus an earlier disclosed genus of tri-substituted pyridine structures.
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
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PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
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COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME
Provided is a compound of Chemical Formula 1:
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wherein n is 0 or 1, when n is 0, at least one of R1 to R10 is a group of Chemical Formula A, and when n is 1, at least one of R1 to R12 is a group of Chemical Formula A:
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wherein L1 is a direct bond, or a substituted or unsubstituted arylene or heteroarylene group; l1 is an integer of 1 to 5; m is an integer of 1 to 3; when l1 is 2 or greater, the two or more L1s are the same as or different from each other, and an organic light emitting device including the same.