C07C211/36

ANIMAL AND HUMAN ANTI-MALARIAL AGENTS
20170348316 · 2017-12-07 ·

Provided herein are Purine Comounds of Formula (I)

##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.

ANIMAL AND HUMAN ANTI-TRYPANOSOMONAL AND ANTI-LEISHMANIA AGENTS

Provided herein are Aminopurine compounds of Formula I:

##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.

ANIMAL AND HUMAN ANTI-TRYPANOSOMONAL AND ANTI-LEISHMANIA AGENTS

Provided herein are Aminopurine compounds of Formula I:

##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.

Cyclopropylamines as LSD1 inhibitors

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

Cyclopropylamines as LSD1 inhibitors

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

COUPLING OF DISTILLATIVE PURIFICATION WITH A PARTIAL CONDENSER FOR PRE-PURIFICATION OF ISOPHORONEDIAMINE

A process for fine purification of isophoronediamine (IPDA), including producing IPDA by aminating hydrogenation of isophorone nitrile in the presence of at least ammonia, hydrogen, a a hydrogenation catalyst and optionally further additions to obtain a crude IPDA, and subjecting the crude IPDA to a fine purification via two vacuum distillation columns, wherein in the first vacuum distillation column the removal of any remaining relatively low-boiling byproducts is effected and in the second vacuum distillation column the IPDA is obtained in pure form as tops and thus separated from the organic residues, and wherein the first vacuum distillation column has vacuum distillation column has a partial condenser fitted to it.

COUPLING OF DISTILLATIVE PURIFICATION WITH A PARTIAL CONDENSER FOR PRE-PURIFICATION OF ISOPHORONEDIAMINE

A process for fine purification of isophoronediamine (IPDA), including producing IPDA by aminating hydrogenation of isophorone nitrile in the presence of at least ammonia, hydrogen, a a hydrogenation catalyst and optionally further additions to obtain a crude IPDA, and subjecting the crude IPDA to a fine purification via two vacuum distillation columns, wherein in the first vacuum distillation column the removal of any remaining relatively low-boiling byproducts is effected and in the second vacuum distillation column the IPDA is obtained in pure form as tops and thus separated from the organic residues, and wherein the first vacuum distillation column has vacuum distillation column has a partial condenser fitted to it.

COUPLING OF DISTILLATIVE PURIFICATION WITH A PARTIAL CONDENSER FOR PRE-PURIFICATION OF ISOPHORONEDIAMINE

A process for fine purification of isophoronediamine (IPDA), including producing IPDA by aminating hydrogenation of isophorone nitrile in the presence of at least ammonia, hydrogen, a a hydrogenation catalyst and optionally further additions to obtain a crude IPDA, and subjecting the crude IPDA to a fine purification via two vacuum distillation columns, wherein in the first vacuum distillation column the removal of any remaining relatively low-boiling byproducts is effected and in the second vacuum distillation column the IPDA is obtained in pure form as tops and thus separated from the organic residues, and wherein the first vacuum distillation column has vacuum distillation column has a partial condenser fitted to it.

CHIRAL BINUCLEAR METAL COMPLEXES FOR STEREOSELECTIVE GLYCOSIDE HYDROLYSIS OF SACCHARIDES
20170275303 · 2017-09-28 ·

Disclosed herein is a class of chiral binuclear metal complexes for stereoselective glycoside hydrolysis of saccharides, and more particular chiral binuclear transition metal complex catalysts that discriminate epimeric glycosides and α- and β-glycosidic bonds of saccharides in aqueous solutions at near physiological pHs. The chiral binuclear metal complexes include a Schiff-base-type ligand derived from a chiral diamino building block, and a binuclear transition metal core, each which can be varied for selectivity. The metal core is a Lewis-acidic metal ion, such as copper, zinc, lanthanum, iron and nickel. The Schiff-base may be a reduced or non-reduced Schiff-base derived from aliphatic linear, aliphatic cyclic diamino alcohols or aromatic aldehydes. The ligand can be a penta- or heptadentate ligand derived from pyridinecarbaldehydes, benzaldehydes, linear or cyclic diamines or diamino alcohols.

METHOD FOR PRODUCING CIS- AND TRANS-ENRICHED MDACH

A process for preparing trans-enriched MDACH, including: distilling an MDACH starting mixture in the presence of an auxiliary, which is an organic compound having a molar mass of 62 to 500 g/mol, a boiling point at least 5° C. above the boiling point of cis,cis-2,6-diamino-1-methylcyclohexane, and 2 to 4 functional groups, each of which is independently an alcohol group or a primary, secondary or tertiary amino group. The MDACH starting mixture includes 0 to 100% by weight of 2,4-MDACH and 0 to 100% by weight of 2,6-MDACH, based on the total amount of MDACH present in the MDACH starting mixture. The MDACH starting mixture includes both trans and cis isomers. Trans-enriched MDACH includes 0 to 100% by weight of 2,4-MDACH and 0 to 100% by weight of 2,6-MDACH, where the proportion of trans isomers in the mixture is higher than the proportion of trans isomers in the MDACH starting mixture.