A heterobifunctional monodisperse polyethylene glycol with two adjacent monodisperse polyethylene glycol side chains, in which a peptide linker is degraded by intracellular enzymes to release a drug slowly and effectively mask the hydrophobicity of the drug, and an antibody-drug conjugate in which the antibody and the drug are bound using same is provided. A heterobifunctional monodisperse polyethylene glycol represented by the formula (1):

##STR00001##

wherein each symbol in the formula (1) is as defined in the DESCRIPTION.

A heterobifunctional monodisperse polyethylene glycol with two adjacent monodisperse polyethylene glycol side chains, in which a peptide linker is degraded by intracellular enzymes to release a drug slowly and effectively mask the hydrophobicity of the drug, and an antibody-drug conjugate in which the antibody and the drug are bound using same is provided. A heterobifunctional monodisperse polyethylene glycol represented by the formula (1):

##STR00001##

wherein each symbol in the formula (1) is as defined in the DESCRIPTION.

The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

##STR00001##

The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

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Provided is a novel fluorescent probe which can be used in a spray manner, has an outstandingly high sensitivity-specificity with instantaneousness, and enables detection of a brain tumor.

A fluorescent probe for detecting a brain tumor, including a compound of the following formula (I) or a salt thereof:

##STR00001##

wherein P1 represents an arginine residue, a histidine residue or a tyrosine residue, P2 represents a proline residue or a glycine residue, where P1 is linked to an adjacent N atom by forming an amide bond, and P2 is linked to P1 by forming an amide bond; R.sup.1 represents a hydrogen atom, or 1 to 4 identical or different substituents each independently selected from the group consisting of an optionally substituted alkyl group, a carboxyl group, an ester group, an alkoxy group, an amide group and an azide group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an optionally substituted alkyl group or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group;

X represents O, Si(R.sup.a)(R.sup.b), Ge(R.sup.a)(R.sup.b), Sn(R.sup.a)(R.sup.b), C(R.sup.a) (R.sup.b) or P(═O)(R.sup.a); R.sup.a and R.sup.b each independently represent a hydrogen atom, an alkyl group or an aryl group; and Y represents a C.sub.1-C.sub.3 alkylene group.

Provided is a novel fluorescent probe which can be used in a spray manner, has an outstandingly high sensitivity-specificity with instantaneousness, and enables detection of a brain tumor.

A fluorescent probe for detecting a brain tumor, including a compound of the following formula (I) or a salt thereof:

##STR00001##

wherein P1 represents an arginine residue, a histidine residue or a tyrosine residue, P2 represents a proline residue or a glycine residue, where P1 is linked to an adjacent N atom by forming an amide bond, and P2 is linked to P1 by forming an amide bond; R.sup.1 represents a hydrogen atom, or 1 to 4 identical or different substituents each independently selected from the group consisting of an optionally substituted alkyl group, a carboxyl group, an ester group, an alkoxy group, an amide group and an azide group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an optionally substituted alkyl group or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group;

X represents O, Si(R.sup.a)(R.sup.b), Ge(R.sup.a)(R.sup.b), Sn(R.sup.a)(R.sup.b), C(R.sup.a) (R.sup.b) or P(═O)(R.sup.a); R.sup.a and R.sup.b each independently represent a hydrogen atom, an alkyl group or an aryl group; and Y represents a C.sub.1-C.sub.3 alkylene group.

The invention provides a new oligopeptide linker intermediate and a preparation method thereof. The preparation method of the oligopeptide intermediate is easily carried out under mild reaction conditions, and since almost no side reactions occur in the reaction, the method produces a high-purity product with fewer impurities and easy to be purified, achieving unexpected technical effects.

The present disclosure provides compounds of Formula I for use in the treatment of medical disorders by the inhibition of human epididymal protein 4 (HE4).

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The present disclosure provides compounds of Formula I for use in the treatment of medical disorders by the inhibition of human epididymal protein 4 (HE4).

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Dual HDAC6/proteasome inhibitors, and methods of using the same, are provided for treating disease.