C07D491/22

Proteasome activity enhancing compounds

The present invention is directed to compounds having the Formulae (Ia), (Ib), (Ic), or (Id); or the Formulae (II), (IIa), (IIb), or (IIc); or the Formulae (III), (IIIa), (IIIb), (IIIc), (IIId), or (IIIe), and pharmaceutically acceptable salts, solvates, clathrates and prodrugs of any Formula thereof, compositions thereof, and methods for the treatment of a condition associated with a dysfunction in proteostasis.

POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE
20230227454 · 2023-07-20 · ·

The present invention provides a compound represented by Formula (I):

##STR00001##

wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R.sup.1 is halogen or the like; R.sup.2a and R.sup.2b are each independently hydrogen or the like; R.sup.3 is substituted or unsubstituted alkyl or the like; R.sup.4 is hydrogen or the like; and n is an integer of 1 to 3.

POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE
20230227454 · 2023-07-20 · ·

The present invention provides a compound represented by Formula (I):

##STR00001##

wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R.sup.1 is halogen or the like; R.sup.2a and R.sup.2b are each independently hydrogen or the like; R.sup.3 is substituted or unsubstituted alkyl or the like; R.sup.4 is hydrogen or the like; and n is an integer of 1 to 3.

Macrocyclic deaza-purinones for the treatment of viral infections

This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Macrocyclic deaza-purinones for the treatment of viral infections

This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

OXYNITIDINE DERIVATIVES USEFUL AS INHIBITORS OF TOPOISOMERASE IB (TOP1) AND TYROSYL-DNA PHOSPHODIESTERASE 1 (TDP1)

Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as Top1 and/or Tdp1 inhibitors. The disclosure provides pharmaceutical compositions containing a compound of Formula I as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula I to treat cancer are provided in this disclosure. The disclosed compounds of Formula I may be used alone to treat cancer, but may also be used in combination with another active agent, such as a Top1 inhibitor, for example, camptothecin or a camptothecin analogue.

OXYNITIDINE DERIVATIVES USEFUL AS INHIBITORS OF TOPOISOMERASE IB (TOP1) AND TYROSYL-DNA PHOSPHODIESTERASE 1 (TDP1)

Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as Top1 and/or Tdp1 inhibitors. The disclosure provides pharmaceutical compositions containing a compound of Formula I as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula I to treat cancer are provided in this disclosure. The disclosed compounds of Formula I may be used alone to treat cancer, but may also be used in combination with another active agent, such as a Top1 inhibitor, for example, camptothecin or a camptothecin analogue.

PARA-AMINO-BENZYL LINKERS, PROCESS FOR THEIR PREPARATION AND THEIR USE IN CONJUGATES

The present invention relates to para-amino-benzyl linker compounds useful for linking drug moieties to antibodies, to linker-drug compounds in which said para-amino-benzyl linker compounds are covalently linked to drug moieties, and to antibody-drug conjugates in which said para-amino-benzyl linker compounds are covalently linked to drug wherein said drug is enzymatically cleaved from the conjugate at a particular cell or tissue type targeted by said antibody.

ANTI-TUMOR COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

ANTI-TUMOR COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.