Patent classifications
C07C2603/22
PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
Emodin succinyl ester compound, preparation method therefor and application thereof
Disclosed in the present invention are an emodin succinyl ester compound, a preparation method therefor and a use thereof, the emodin succinyl ester compound having the structure as represented by formula I (R being a C.sub.1-5 alkyl group). The method provided in the present invention has a simple method course, and may effectively save time in synthesis and reduce costs, being simple to operate, being easy to implement, and being suitable for industrial production. Experiments show that the emodin succinyl ester compound of the present invention may better promote the healing of diabetic wounds than emodin, and may be used for preparing a drug for promoting the healing of diabetic wounds. Moreover, it has been confirmed by means of performing pharmacological experiments on rats suffering from experimentally mixed hyperlipidemia that the emodin succinyl ester compound of the present invention is superior to emodin, and has the advantages of having a remarkable blood fat lowering effect, being safe, being simple and convenient to administer, the raw materials being low cost and readily available, and being easy to transport and store.
Synthesis of a triangulene ring system and derivatives thereof
A three step synthesis of the 8,12-dihydro-4H-dibenzo[cd,mn]pyren-3a.sup.2-ylium cation (triangulenium cation) is effected by cascade cyclization of a tetra-benzyl alcohol precursor in triflic acid solution. This cation is easily observed by NMR and optical spectroscopy. Quenching of the cation into basic solutions or by hydride transfer from triethylsilane provides access to stable dihydro and tetrahydro[3]triangulenes. This route makes several [3]triangulene precursors more readily available for development of new applications in the field of molecular electronics.
SYNTHESIS OF A TRIANGULENE RING SYSTEM AND DERIVATIVES THEREOF
A three step synthesis of the 8,12-dihydro-4H-dibenzo[cd,mn]pyren-3a.sup.2-ylium cation (triangulenium cation) is effected by cascade cyclization of a tetra-benzyl alcohol precursor in triflic acid solution. This cation is easily observed by NMR and optical spectroscopy. Quenching of the cation into basic solutions or by hydride transfer from triethylsilane provides access to stable dihydro and tetrahydro[3]triangulenes. This route makes several [3]triangulene precursors more readily available for development of new applications in the field of molecular electronics.
EMODIN SUCCINYL ESTER COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Disclosed in the present invention are an emodin succinyl ester compound, a preparation method therefor and a use thereof, the emodin succinyl ester compound having the structure as represented by formula I (R being a C.sub.1-5 alkyl group). The method provided in the present invention has a simple method course, and may effectively save time in synthesis and reduce costs, being simple to operate, being easy to implement, and being suitable for industrial production. Experiments show that the emodin succinyl ester compound of the present invention may better promote the healing of diabetic wounds than emodin, and may be used for preparing a drug for promoting the healing of diabetic wounds. Moreover, it has been confirmed by means of performing pharmacological experiments on rats suffering from experimentally mixed hyperlipidemia that the emodin succinyl ester compound of the present invention is superior to emodin, and has the advantages of having a remarkable blood fat lowering effect, being safe, being simple and convenient to administer, the raw materials being low cost and readily available, and being easy to transport and store.
Pyrrolobenzodiazepines and conjugates thereof
The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
Octahydroanthracene compound, preparation method and application thereof
An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.
Preparation of 2,6- and 2,7-disubstituted anthraquinone derivates
A composition comprising a compound of formula (Va) wherein n is 1 or 2 and wherein m is 1 or 2, with n and m preferably both being 1 or both being 2, more preferably both being 1, and/or, preferably and, a compound of formula, wherein n is 1 or 2 and wherein m is 1 or 2, with n and m preferably both being 1 or both being 2, more preferably both being 1, and wherein at least 90 weight-% of the composition consist of compounds of formula (Va) and formula (Vb). ##STR00001##
Octahydroanthracene Compound, Preparation Method and Application Thereof
An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.
PREPARATION OF 2,6- AND 2,7-DISUBSTITUTED ANTHRAQUINONE DERIVATES
A composition comprising a compound of formula (Va) wherein n is 1 or 2 and wherein m is 1 or 2, with n and m preferably both being 1 or both being 2, more preferably both being 1, and/or, preferably and, a compound of formula, wherein n is 1 or 2 and wherein m is 1 or 2, with n and m preferably both being 1 or both being 2, more preferably both being 1, and wherein at least 90 weight-% of the composition consist of compounds of formula (Va) and formula (Vb).
##STR00001##