C07C271/02

Retinoid derivatives with antitumor activity

The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: ##STR00001##
wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

Process for stripping carbamate from ion exchange resin
10898891 · 2021-01-26 · ·

In a preferred embodiment, there is provided a process for separating an amine compound or a conjugate acid thereof and a carbamate compound or a conjugate acid thereof from a mixture having the amine compound, the carbamate compound, carbon dioxide and at least one anionic contaminant salt using an anionic exchange column, the process including passing the mixture through the column to obtain a first effluent and passing through the column an extraction fluid to obtain a second effluent, where the extraction fluid most preferably includes carbonic acid.

Process for stripping carbamate from ion exchange resin
10898891 · 2021-01-26 · ·

In a preferred embodiment, there is provided a process for separating an amine compound or a conjugate acid thereof and a carbamate compound or a conjugate acid thereof from a mixture having the amine compound, the carbamate compound, carbon dioxide and at least one anionic contaminant salt using an anionic exchange column, the process including passing the mixture through the column to obtain a first effluent and passing through the column an extraction fluid to obtain a second effluent, where the extraction fluid most preferably includes carbonic acid.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)
20210009511 · 2021-01-14 ·

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)
20210009511 · 2021-01-14 ·

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

CROSSLINKABLE COATING COMPOSITIONS FORMULATED WITH DORMANT CARBAMATE INITIATOR

A crosslinkable coating composition comprising: ingredient A that has at least two protons that can be activated to form a Michael carbanion donor; ingredient B that functions as a Michael acceptor having at least two ethylenically unsaturated functionalities each activated by an electron-withdrawing group; and a dormant carbamate initiator of Formula (1)

##STR00001##

wherein R.sub.1 and R.sub.2 can be independently selected from hydrogen, a linear or branched substituted or unsubstituted alkyl group having 1 to 22 carbon atoms; 1 to 8 carbon atoms; and A.sup.n+ is a cationic species or polymer and n is an integer equal or greater than 1 with the proviso that A.sup.n+ is not an acidic hydrogen; and optionally further comprising ammonium carbamate (H.sub.2NR.sub.1R.sub.2.sup.+OCONR.sub.1R.sub.2). The crosslinkable coating composition can be used for a variety of coating applications including nail coating compositions.

CROSSLINKABLE COATING COMPOSITIONS FORMULATED WITH DORMANT CARBAMATE INITIATOR

A crosslinkable coating composition comprising: ingredient A that has at least two protons that can be activated to form a Michael carbanion donor; ingredient B that functions as a Michael acceptor having at least two ethylenically unsaturated functionalities each activated by an electron-withdrawing group; and a dormant carbamate initiator of Formula (1)

##STR00001##

wherein R.sub.1 and R.sub.2 can be independently selected from hydrogen, a linear or branched substituted or unsubstituted alkyl group having 1 to 22 carbon atoms; 1 to 8 carbon atoms; and A.sup.n+ is a cationic species or polymer and n is an integer equal or greater than 1 with the proviso that A.sup.n+ is not an acidic hydrogen; and optionally further comprising ammonium carbamate (H.sub.2NR.sub.1R.sub.2.sup.+OCONR.sub.1R.sub.2). The crosslinkable coating composition can be used for a variety of coating applications including nail coating compositions.

AMINO DIACIDS CONTAINING PEPTIDE MODIFIERS

The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.

##STR00001##

AMINO DIACIDS CONTAINING PEPTIDE MODIFIERS

The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.

##STR00001##

Gossypol isocyanate ester compounds with antileukemic activities and a method of preparing the same

A compound of Formula I: ##STR00001##
is disclosed. A method of preparing the compound of Formula I is also disclosed. R is alkyl, haloalkyl, aryl, or substituted aryl. Preferably, R is CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2CH.sub.2CH.sub.3, CH(CH.sub.3).sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.3, CF.sub.3, CHF.sub.2, CH.sub.2CF.sub.3, ##STR00002##