C07D309/32

ANTIBODY DRUG CONJUGATES

Drug conjugates of formula [D-(X).sub.b-(AA).sub.w-(L)-].sub.n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein:

##STR00001## A is selected from

##STR00002## R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCOOR.sub.a, alkyl, alkenyl, alkynyl, etc; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sub.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; Ab is a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer.

ANTIBODY DRUG CONJUGATES

Drug conjugates of formula [D-(X).sub.b-(AA).sub.w-(L)-].sub.n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein:

##STR00001## A is selected from

##STR00002## R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCOOR.sub.a, alkyl, alkenyl, alkynyl, etc; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sub.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; Ab is a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer.

N-CONTAINING CHROMEN-4-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The present invention provides the compounds having the general formula: (I) wherein R.sup.1 to R.sup.8, and X are as described herein, compositions including the compounds and methods of using the compounds.

##STR00001##

Compounds and methods of treating or ameliorating an IL-1R-mediated disease or disorder using same
11345696 · 2022-05-31 · ·

The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.

Compounds and methods of treating or ameliorating an IL-1R-mediated disease or disorder using same
11345696 · 2022-05-31 · ·

The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.

Spontaneous alignment assistant for liquid crystal compositions

The spontaneous orientation aid for a liquid crystal composition provides storage stability and allows liquid crystal molecules to be vertically aligned without a PI layer when added to a liquid crystal composition. When used in a liquid crystal composition, the spontaneous orientation aid can adsorb to substrates sandwiching a liquid crystal composition (liquid crystal layer) and keep the liquid crystal molecules aligned in a vertical direction. The spontaneous orientation aid makes it possible to align liquid crystal molecules without a PI layer (to induce vertical alignment of liquid crystal molecules under no applied voltage and to achieve horizontal alignment of the liquid crystal molecules under an applied voltage).

Spontaneous alignment assistant for liquid crystal compositions

The spontaneous orientation aid for a liquid crystal composition provides storage stability and allows liquid crystal molecules to be vertically aligned without a PI layer when added to a liquid crystal composition. When used in a liquid crystal composition, the spontaneous orientation aid can adsorb to substrates sandwiching a liquid crystal composition (liquid crystal layer) and keep the liquid crystal molecules aligned in a vertical direction. The spontaneous orientation aid makes it possible to align liquid crystal molecules without a PI layer (to induce vertical alignment of liquid crystal molecules under no applied voltage and to achieve horizontal alignment of the liquid crystal molecules under an applied voltage).

P62-ZZ chemical inhibitor

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

P62-ZZ chemical inhibitor

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

Small molecule stimulators of steroid receptor coactivator proteins and their use in the treatment of cancer

Small molecule stimulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing cancer. Also provided are methods for stimulating SRC family proteins in a cell.