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.

The present disclosure relates generally, but not exclusively, to compounds and their use in therapy, to compositions and agents comprising said compounds, to methods of treatment using said compounds, and their use in the manufacture of medicaments. The disclosure further relates to inhibitors of IRAP and their use in the treatment or prevention of Alzheimer's disease and the treatment and prevention of memory and cognitive disorders.

The present disclosure relates generally, but not exclusively, to compounds and their use in therapy, to compositions and agents comprising said compounds, to methods of treatment using said compounds, and their use in the manufacture of medicaments. The disclosure further relates to inhibitors of IRAP and their use in the treatment or prevention of Alzheimer's disease and the treatment and prevention of memory and cognitive disorders.

Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).

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Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).

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Drug conjugates of formula [D-(X)b-(AA)w-(L)-]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: A is selected from (II) and (III) R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCO—OR.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.4 to 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.sup.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; A bis 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. ##STR00001##

Drug conjugates of formula [D-(X)b-(AA)w-(L)-]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: A is selected from (II) and (III) R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCO—OR.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.4 to 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.sup.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; A bis 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. ##STR00001##

Described herein are solvents and co-solvents comprising anhydromevalonolactone (aMVL) and various industrial applications for such solvents. aMVL has a number of advantageous properties for use in solvent, including high boiling point, low melting point, low viscosity, non-flammability, water solubility, exceptionally low volatility, and excellent solvation capability. Exemplary industrial applications for solvents comprising aMVL include polymer manufacturing, polymer recycling, mold production, fiber production, membrane manufacturing, thermosetting paint manufacturing, coating manufacturing, coating removal, paint strippers, cleaning products, degreasing products, nitrile synthesis, alkylation, production of syngas, carbon-carbon cross-coupling reactions, metal organic framework synthesis, halogenation reactions, formation of pharmaceuticals, formation of fungicides and/or herbicides, seed treatment products, bioregulators, and electrolytes in batteries or capacitors.

Described herein are solvents and co-solvents comprising anhydromevalonolactone (aMVL) and various industrial applications for such solvents. aMVL has a number of advantageous properties for use in solvent, including high boiling point, low melting point, low viscosity, non-flammability, water solubility, exceptionally low volatility, and excellent solvation capability. Exemplary industrial applications for solvents comprising aMVL include polymer manufacturing, polymer recycling, mold production, fiber production, membrane manufacturing, thermosetting paint manufacturing, coating manufacturing, coating removal, paint strippers, cleaning products, degreasing products, nitrile synthesis, alkylation, production of syngas, carbon-carbon cross-coupling reactions, metal organic framework synthesis, halogenation reactions, formation of pharmaceuticals, formation of fungicides and/or herbicides, seed treatment products, bioregulators, and electrolytes in batteries or capacitors.

Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL). ##STR00001##