C07D263/04

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.

Annulation catalysts via direct C—H bond amination

Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. CH bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield CN bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.

Annulation catalysts via direct C—H bond amination

Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. CH bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield CN bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.

TERPINEOL AND PREPARATION METHOD AND APPLICATION THEREOF

The present invention discloses a terpinenol compound as well as its preparation method and application. The structure of such terpinenol compound is as shown in Formula (I) or (II). In Formula (I), R is independently selected from C.sub.12-C.sub.16 alkyl, NR.sup.1R.sup.2, SR.sup.3 or OR.sup.4; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from C.sub.1-C.sub.6 alkyl or NO.sub.2; the C.sub.1-C.sub.6 alkyl can be substituted by OH; Alternatively, the R.sup.1 and R.sup.2 form a five-member ring or six-member ring in together with N used to link up them; the five-member or six-member ring may contain one O or CO. As indicated by results of activity test, such terpinenol compound has satisfactory effect in prevention of asthma, inflammation and pulmonary artery hypertension, which also has high pharmaceutical significance.

##STR00001##

TERPINEOL AND PREPARATION METHOD AND APPLICATION THEREOF

The present invention discloses a terpinenol compound as well as its preparation method and application. The structure of such terpinenol compound is as shown in Formula (I) or (II). In Formula (I), R is independently selected from C.sub.12-C.sub.16 alkyl, NR.sup.1R.sup.2, SR.sup.3 or OR.sup.4; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from C.sub.1-C.sub.6 alkyl or NO.sub.2; the C.sub.1-C.sub.6 alkyl can be substituted by OH; Alternatively, the R.sup.1 and R.sup.2 form a five-member ring or six-member ring in together with N used to link up them; the five-member or six-member ring may contain one O or CO. As indicated by results of activity test, such terpinenol compound has satisfactory effect in prevention of asthma, inflammation and pulmonary artery hypertension, which also has high pharmaceutical significance.

##STR00001##

Moisture-curing polyurethane composition containing oxazolidine
11952493 · 2024-04-09 · ·

A polyurethane composition, which contains at least one isocyanate-group-containing polymer, obtained from the reaction of at least one polyol with at least one diisocyanate, and at least one oxazolidine of the formula (I). The polyurethane composition allows one-component moisture-curing adhesives, sealants or coatings that have good storage stability, long open times and cure quickly to give a surprisingly non-tacky material having pronounced high-resilient properties.

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.

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.