C07C227/14

Prodrugs of glutamine analogs

The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Prodrugs of glutamine analogs

The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

CARBONIC ACID ADDUCTS
20200216384 · 2020-07-09 ·

The present invention relates to a carbonic acid adduct (CAA) comprising carbonic acid, at least one amine, and optionally at least one salt, said adduct being producible by a method comprising the following steps: a) providing a solution (A) comprising dissolved CO.sub.2; optionally b) dissolving a base (BA) not corresponding to the amine (AM) in the solution (A) so as to obtain the solution (A1); c) dissolving the at least one amine (AM) in the solution (A) or (A1) so as to obtain the solution (B); d) freezing the solution obtained after completion of step c); and e) storing the solution frozen in step d) at 100 to 0 C. for no longer than 4 days. The content of CO.sub.2 in the solution that is subjected to step c) is at least 6 g/l. The invention also relates to a method for producing the carbonic acid adduct (CAA), a pharmaceutical preparation (PP) comprising the carbonic acid adduct (CAA), and methods for the production thereof and use of the carbonic acid adduct (CAA) or the pharmaceutical preparation (PP) in therapy for a range of indications.

Composition made of amino acid or ester with polymer quality and methods for obtaining same

The present invention relates to a composition which comprises at least one ,-amino-alkanoic acid or ester and at least one alkanoic ester or acid, characterised in that: the ,-amino-alkanoic acid or ester has formula H.sub.2N(CH.sub.2).sub.n-COOR, wherein n=9 to 13 and R is an alkyl group or a hydrogen; the alkanoic ester or acid has formula R.sub.1COOR.sub.2, wherein R.sub.1 is a straight or branched alkyl group with formula C.sub.mH.sub.2m+1 or C.sub.mH.sub.2m3, wherein m=6 to 20 and R.sub.2 is an alkyl group or a hydrogen; the molar ratio between the alkanoic acid(s) or ester(s) and the ,-amino-alkanoic acid(s) or ester(s) is in the range from 0.001 to 0.4%. The present invention also relates to novel methods for obtaining such a composition.

Modified Conjugated Diene-Based Polymer And Method Of Preparing The Same

The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.

Modified Conjugated Diene-Based Polymer And Method Of Preparing The Same

The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.

Prodrugs of glutamine analogs

The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Prodrugs of glutamine analogs

The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

MANUFACTURE OF NITRILE COMPOUNDS

A process for manufacturing a nitrile compound through chain elongation of an alkylene amine compound containing three or more amine units in which at least two amine units are protected by a cyclic urea unit and at least one amine unit is not protected, includes reacting the at least one amine unit that is not protected with glycolonitrile or with the combination of formaldehyde and a cyanide compound selected from HCN and inorganic cyanide salts, to add at least one acetonitrile group to the at least one amine unit that is not protected.

MANUFACTURE OF NITRILE COMPOUNDS

A process for manufacturing a nitrile compound through chain elongation of an alkylene amine compound containing three or more amine units in which at least two amine units are protected by a cyclic urea unit and at least one amine unit is not protected, includes reacting the at least one amine unit that is not protected with glycolonitrile or with the combination of formaldehyde and a cyanide compound selected from HCN and inorganic cyanide salts, to add at least one acetonitrile group to the at least one amine unit that is not protected.