C07C227/12

PROCESS FOR THE PREPARATION OF A QUELATING AGENT
20190002395 · 2019-01-03 ·

It is provided a compound of formula (I); wherein R.sup.5 is selected from the group consisting of H, OM, COOM, NH.sub.2, SO.sub.3M, (C.sub.1-C.sub.4)alkyl, and halogen; and A is a radical having at least 3 C atoms selected from the group consisting of: i) a radical of formula (i) wherein R.sup.7 is selected from the group consisting of OM, and COOM, and n is 0, 1 or 2; and ii) a radical of formula (ii) or of formula (iii) wherein R.sup.8 is selected from the group consisting of H, (C.sub.1-C.sub.4)alkyl; and wherein M is independently selected from the group consisting of H, an alkaly metal, and NH.sub.4.sup.+. It is also provided a process for the preparation thereof, a composition comprising it, and its use for correcting deficiencies of metals in plants.

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SUBSTITUTED TRICYCLIC HETEROCYCLIC COMPOUNDS AS METALLO-BETA-LACTAMASE INHIBITORS

The invention relates to substituted tricyclic heterocyclic compounds of formula (I), pharmaceutically acceptable salts thereof and pharmaceutical compositions wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X1, X2, X3, X4, X5 and n defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase (MBL) inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for reducing or overcoming antibiotic resistance.

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SUBSTITUTED TRICYCLIC HETEROCYCLIC COMPOUNDS AS METALLO-BETA-LACTAMASE INHIBITORS

The invention relates to substituted tricyclic heterocyclic compounds of formula (I), pharmaceutically acceptable salts thereof and pharmaceutical compositions wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X1, X2, X3, X4, X5 and n defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase (MBL) inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for reducing or overcoming antibiotic resistance.

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MEANS AND METHODS FOR MANUFACTURING RACEMIC ALANINE FOR THE MGDA SYNTHESIS

The present invention relates to the field of chemical manufacture. In particular, it relates to a method for manufacturing racemic methylglycinediacetic acid (MGDA) comprising the steps of contacting a solution comprising or being enriched in D-alanine or L-alanine to an alanine racemase at a temperature of at least 50? C. and alkaline conditions for a time sufficient to allow conversion of said solution into a racemic alanine solution, obtaining a racemic alanine solution, and chemically converting the racemic alanine into racemic MGDA. The invention further contemplates an alanine racemase which is capable of converting a solution comprising or being enriched in D-alanine or L-alanine into racemic alanine solution at a temperature of at least 50? C. and under alkaline conditions as well as the use of said alanine racemase for converting a solution comprising or being enriched in D-alanine or L-alanine into racemic alanine solution at a temperature of at least 50? C. and under alkaline conditions.

MEANS AND METHODS FOR MANUFACTURING RACEMIC ALANINE FOR THE MGDA SYNTHESIS

The present invention relates to the field of chemical manufacture. In particular, it relates to a method for manufacturing racemic methylglycinediacetic acid (MGDA) comprising the steps of contacting a solution comprising or being enriched in D-alanine or L-alanine to an alanine racemase at a temperature of at least 50? C. and alkaline conditions for a time sufficient to allow conversion of said solution into a racemic alanine solution, obtaining a racemic alanine solution, and chemically converting the racemic alanine into racemic MGDA. The invention further contemplates an alanine racemase which is capable of converting a solution comprising or being enriched in D-alanine or L-alanine into racemic alanine solution at a temperature of at least 50? C. and under alkaline conditions as well as the use of said alanine racemase for converting a solution comprising or being enriched in D-alanine or L-alanine into racemic alanine solution at a temperature of at least 50? C. and under alkaline conditions.

Process for the Synthesis of Melphalan and the Hydrochloride Salt

The present invention relates to an improved process for the preparation of Melphalan, more specifically the invention relates to an efficient process for the preparation of substantially pure Melphalan hydrochloride (I).

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Process for the Synthesis of Melphalan and the Hydrochloride Salt

The present invention relates to an improved process for the preparation of Melphalan, more specifically the invention relates to an efficient process for the preparation of substantially pure Melphalan hydrochloride (I).

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Process for the synthesis of melphalan and the hydrochloride salt

The present invention relates to an improved process for the preparation of Melphalan, more specifically the invention relates to an efficient process for the preparation of substantially pure Melphalan hydrochloride (I). ##STR00001##

Process for the synthesis of melphalan and the hydrochloride salt

The present invention relates to an improved process for the preparation of Melphalan, more specifically the invention relates to an efficient process for the preparation of substantially pure Melphalan hydrochloride (I). ##STR00001##

PHARMACEUTICALLY ACTIVE COMPOUNDS

The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

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