C07F9/535

Pentafluorophosphate derivative, its uses and an appropriate manufacturing method

It is provided a pentafluorophosphate derivative according to general formula (I): ##STR00001##
or a pharmaceutically acceptable salt or solvate thereof. Thereby, R.sup.1 and R.sup.2 denote independently from each other H or F; R.sup.3 denotes H, a C.sub.1-C.sub.10 alkyl optionally substituted by a hydrocarbon chain comprising an amide function and/or a carboxyl function, or by a substituent chosen from the group consisting of alkyl, alkylamino, alkylaminocarboxy, carboxy, alkoxycarbonyl, hydroxy, N-morpholino, N-morpholinoalkyl, N-morpholinocarbonyl, N-methyl-N-piperazinyl, N-methyl-N-piperazinylalkyl, N-methyl-N-piperazinylcarbonyl, and sulfo, an optionally substituted C.sub.3-C.sub.10 cycloalkyl, or an optionally substituted C.sub.6-C.sub.20 aryl, wherein a hydrocarbon chain of the alkyl, the cycloalkyl or the aryl can be interrupted by one or more oxygen, sulfur and/or nitrogen atoms; and M denotes any cation; with the proviso that at least one of R.sup.1 and R.sup.2 denotes F, if R.sup.3 denotes H.

HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME

Disclosed are chemical entities which are compounds of formula (I):

##STR00001##

or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a′, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Efficient phosphorous stabilizers based on diphenylamine and heterocyclic diphenylamine derivatives

The present invention relates to the use of efficient phosphorous substances, in particular based on diphenylamine and heterocyclic diphenylamine derivatives as stabilizers for organic materials, in particular for plastic materials, against oxidative, thermal and/or actinic degradation. The present invention additionally relates to an organic material that has been correspondingly stabilized as described above. The invention further relates to a method of stabilizing organic materials and to specific stabilizers.

Efficient phosphorous stabilizers based on diphenylamine and heterocyclic diphenylamine derivatives

The present invention relates to the use of efficient phosphorous substances, in particular based on diphenylamine and heterocyclic diphenylamine derivatives as stabilizers for organic materials, in particular for plastic materials, against oxidative, thermal and/or actinic degradation. The present invention additionally relates to an organic material that has been correspondingly stabilized as described above. The invention further relates to a method of stabilizing organic materials and to specific stabilizers.

Methods for the purification of L-glufosinate

Compositions and methods for isolating L-glufosinate from a composition comprising L-glufosinate and glutamate are provided. The method comprises converting the glutamate to pyroglutamate followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The composition comprising L-glufosinate and glutamate is subjected to an elevated temperature for a sufficient time to allow for the conversion of glutamate to pyroglutamate, followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The glutamate alternatively may be converted to pyroglutamate by enzymatic conversion. The purified L-glufosinate is present in a final composition at a concentration of 90% or greater of the sum of L-glufosinate, glutamate, and pyroglutamate. In some embodiments, a portion of the glutamate in the starting composition may be separated from the L-glufosinate using a crystallization step. Solid forms of L-glufosinate materials, including crystalline L-glufosinate ammonium, are also described.

Methods for the purification of L-glufosinate

Compositions and methods for isolating L-glufosinate from a composition comprising L-glufosinate and glutamate are provided. The method comprises converting the glutamate to pyroglutamate followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The composition comprising L-glufosinate and glutamate is subjected to an elevated temperature for a sufficient time to allow for the conversion of glutamate to pyroglutamate, followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The glutamate alternatively may be converted to pyroglutamate by enzymatic conversion. The purified L-glufosinate is present in a final composition at a concentration of 90% or greater of the sum of L-glufosinate, glutamate, and pyroglutamate. In some embodiments, a portion of the glutamate in the starting composition may be separated from the L-glufosinate using a crystallization step. Solid forms of L-glufosinate materials, including crystalline L-glufosinate ammonium, are also described.

Method for Preparing L-Glufosinate

Provided are a method for preparing L-glufosinate and the intermediate compounds of formula (V) and formula (III).

Method for Preparing L-Glufosinate

Provided are a method for preparing L-glufosinate and the intermediate compounds of formula (V) and formula (III).

COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH

The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.

COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH

The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.