C07D209/34

Methods and compounds for restoring mutant p53 function

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Methods and compounds for restoring mutant p53 function

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

METHOD FOR INTRODUCING DEUTERATED LOWER ALKYL INTO AMINE MOIETY OF COMPOUND CONTAINING SECONDARY AMINE

The present invention relates to a method of mono-deuterated-lower-alkylating the amine part in a compound having an amine protected with an aralkyl, which comprises introducing mono-deuterated lower-alkyl into the amine with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl group.

METHOD FOR INTRODUCING DEUTERATED LOWER ALKYL INTO AMINE MOIETY OF COMPOUND CONTAINING SECONDARY AMINE

The present invention relates to a method of mono-deuterated-lower-alkylating the amine part in a compound having an amine protected with an aralkyl, which comprises introducing mono-deuterated lower-alkyl into the amine with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl group.

SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA

Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.

SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA

Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.

COMPOSITION FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND AND POLYMER FOR FORMING ORGANIC FILM

A composition for forming an organic film, containing: a material for forming an organic film shown by the following general formula; and an organic solvent, where R.sub.1 represents a hydrogen atom, an allyl group, or a propargyl group, R.sub.2 represents a nitro group, a halogen atom, a hydroxy group, an alkyloxy group having 1 to 4 carbon atoms, an alkynyloxy group having 2 to 4 carbon atoms, an alkenyloxy group having 2 to 4 carbon atoms, a linear, branched, or cyclic alkyl group having 1 to 6 carbon atoms, a trifluoromethyl group, or a trifluoromethyloxy group, m = 0 or 1, n = 1 or 2, 1 = 0 or 1, k represents an integer of 0 to 2, W represents a divalent organic group having 1 to 40 carbon atoms, and each V independently represents a hydrogen atom or a linking moiety.

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COMPOSITION FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND AND POLYMER FOR FORMING ORGANIC FILM

A composition for forming an organic film, containing: a material for forming an organic film shown by the following general formula; and an organic solvent, where R.sub.1 represents a hydrogen atom, an allyl group, or a propargyl group, R.sub.2 represents a nitro group, a halogen atom, a hydroxy group, an alkyloxy group having 1 to 4 carbon atoms, an alkynyloxy group having 2 to 4 carbon atoms, an alkenyloxy group having 2 to 4 carbon atoms, a linear, branched, or cyclic alkyl group having 1 to 6 carbon atoms, a trifluoromethyl group, or a trifluoromethyloxy group, m = 0 or 1, n = 1 or 2, 1 = 0 or 1, k represents an integer of 0 to 2, W represents a divalent organic group having 1 to 40 carbon atoms, and each V independently represents a hydrogen atom or a linking moiety.

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Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase

Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.

ACTIVATORS OF THE UNFOLDED PROTEIN RESPONSE

A set of small molecules ERα biomodulators that kill therapy-resistant ERα positive breast, ovarian, and endometrial cancer cells. These small molecules have increased therapeutic potential because of an increased ability to kill therapy-resistant breast cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen and fulvestrant/ICI). The new compounds do not only inhibit proliferation of the cancer cells but actually kills them, which prevents reactivation of tumors years later.