C07D319/06

Diamine compound with Meldrum's acid group and related polymer thereof

The present disclosure provides a diamine compound, which includes a structure represented by formula (I). Formula (I) is defined as in the specification. The present disclosure further provides an amide bond-containing polymer, a polyimide, a polybenzoxazine, a thermosetting resin and a copolymerized thermosetting resin prepared by the diamine compound including the structure represented by formula (I).

Diamine compound with Meldrum's acid group and related polymer thereof

The present disclosure provides a diamine compound, which includes a structure represented by formula (I). Formula (I) is defined as in the specification. The present disclosure further provides an amide bond-containing polymer, a polyimide, a polybenzoxazine, a thermosetting resin and a copolymerized thermosetting resin prepared by the diamine compound including the structure represented by formula (I).

Substituted esters containing polyols and saccharides for treating hepatotoxicity and fatty liver diseases

The present invention relates to compounds effective in treating hepatotoxicity and fatty liver diseases and uses thereof. The present compound is represented by Formula (II), which has the formula: R.sub.1—O—X—(CH.sub.2).sub.m—X—O—R.sub.2, wherein: each X is —C(═O)—; R.sub.1 is a C.sub.1-C.sub.18 alkyl polyol: R.sub.2 is a saccharide group of formula (G).sub.p; G is a monosaccharide residue, where (i) at least one of the —OH groups in (G).sub.p is substituted by a halogen atom, and (ii) the saccharide group of formula (G).sub.p is linked to —O— through a —CH.sub.2 group; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

Substituted esters containing polyols and saccharides for treating hepatotoxicity and fatty liver diseases

The present invention relates to compounds effective in treating hepatotoxicity and fatty liver diseases and uses thereof. The present compound is represented by Formula (II), which has the formula: R.sub.1—O—X—(CH.sub.2).sub.m—X—O—R.sub.2, wherein: each X is —C(═O)—; R.sub.1 is a C.sub.1-C.sub.18 alkyl polyol: R.sub.2 is a saccharide group of formula (G).sub.p; G is a monosaccharide residue, where (i) at least one of the —OH groups in (G).sub.p is substituted by a halogen atom, and (ii) the saccharide group of formula (G).sub.p is linked to —O— through a —CH.sub.2 group; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

STRUCTURALLY MODIFIED OPIOIDS FOR PREVENTION AND TREATMENT OF DISEASES AND CONDITIONS

Aspects of the present invention are directed to structurally modified opioids (SMOs) that result in improved modulating activity at the NMDAR and improved PK and PD parameters over existing drugs with NMDAR modulating activity. The structural modifications of an opioid or opioid enantiomer that result in the SMOs can be obtained by starting the synthetic process de novo; by modifying the synthetic process for the opioid at any intermediate step during the synthesis of the racemate or of one enantiomer; or by modifying the structure of the opioid or opioid enantiomer after the synthesis. The nitric acid ester substitutions are of particular relevance, especially when associated to deuterated substitutions and/or halogen substitutions.

STRUCTURALLY MODIFIED OPIOIDS FOR PREVENTION AND TREATMENT OF DISEASES AND CONDITIONS

Aspects of the present invention are directed to structurally modified opioids (SMOs) that result in improved modulating activity at the NMDAR and improved PK and PD parameters over existing drugs with NMDAR modulating activity. The structural modifications of an opioid or opioid enantiomer that result in the SMOs can be obtained by starting the synthetic process de novo; by modifying the synthetic process for the opioid at any intermediate step during the synthesis of the racemate or of one enantiomer; or by modifying the structure of the opioid or opioid enantiomer after the synthesis. The nitric acid ester substitutions are of particular relevance, especially when associated to deuterated substitutions and/or halogen substitutions.

Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. ##STR00001##

Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. ##STR00001##

Facile and selective perfluoro- and polyfluoroarylation of Meldrum's acid

This disclosure relates generally to the facile and selective mono-perfluoro and poly-fluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics.

Facile and selective perfluoro- and polyfluoroarylation of Meldrum's acid

This disclosure relates generally to the facile and selective mono-perfluoro and poly-fluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics.