Patent classifications
C07D317/40
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 firth 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.
Treprostinil derivative compounds and methods of using same
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
Treprostinil derivative compounds and methods of using same
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
MONOETHYLENICALLY UNSATURATED MONOMERS AND USES THEREOF
The invention relates to a monoethylenically unsaturated monomer of formula (I), and to the use thereof for producing a polymer. The invention also relates to the polymer obtained by polymerising said monomer, and to the use thereof in a composition for producing coatings.
##STR00001##
MONOETHYLENICALLY UNSATURATED MONOMERS AND USES THEREOF
The invention relates to a monoethylenically unsaturated monomer of formula (I), and to the use thereof for producing a polymer. The invention also relates to the polymer obtained by polymerising said monomer, and to the use thereof in a composition for producing coatings.
##STR00001##
METHOD FOR PRODUCING CYCLIC CARBONATE HAVING UNSATURATED GROUP, AND NOVEL CYCLIC CARBONATE
A method for producing a cyclic carbonate represented by the following formula (1):
##STR00001##
wherein X.sup.1 and X.sup.2 are the same as or different from each other, and are each a hydrogen atom, a fluorine atom, or a monovalent organic group; and R is an organic group containing one or more carbon-carbon unsaturated bonds. The method includes reacting an unsaturated cyclic carbonate represented by the following formula (A):
##STR00002##
wherein X.sup.1 and X.sup.2 are defined as described above, and an alcohol represented by the formula (B): R—OH, wherein R is defined as described above, or an alkoxide thereof in the presence of a base, or reacting the unsaturated cyclic carbonate and the alkoxide. Also disclosed is a method for producing a cyclic carbonate.
METHOD FOR PRODUCING CYCLIC CARBONATE HAVING UNSATURATED GROUP, AND NOVEL CYCLIC CARBONATE
A method for producing a cyclic carbonate represented by the following formula (1):
##STR00001##
wherein X.sup.1 and X.sup.2 are the same as or different from each other, and are each a hydrogen atom, a fluorine atom, or a monovalent organic group; and R is an organic group containing one or more carbon-carbon unsaturated bonds. The method includes reacting an unsaturated cyclic carbonate represented by the following formula (A):
##STR00002##
wherein X.sup.1 and X.sup.2 are defined as described above, and an alcohol represented by the formula (B): R—OH, wherein R is defined as described above, or an alkoxide thereof in the presence of a base, or reacting the unsaturated cyclic carbonate and the alkoxide. Also disclosed is a method for producing a cyclic carbonate.
CONTINUOUS METHOD FOR PREPARING CARBONATE ESTERS
In one embodiment, a continuous process for preparing organic carbonate solvent of Formula (I) as described herein comprises contacting a first reactant (an alcohol) with a reactive carbonyl source (carbonyldiimidazole (CDI) or an alkylchloroformate) in the presence of a catalyst in reaction stream flowing through a continuous flow reactor at temperature 20° C. to about 160° C. and at a flow rate providing a residence time in the range of about 0.1 minute to about 24 hours; collecting a reactor effluent exiting from the continuous flow reactor; recovering a crude product from the reactor effluent; and distilling the crude product to obtain the organic carbonate compound of Formula (I). In another embodiment, the first reactant is an epoxide and the carbonyl source is carbon dioxide.
CONTINUOUS METHOD FOR PREPARING CARBONATE ESTERS
In one embodiment, a continuous process for preparing organic carbonate solvent of Formula (I) as described herein comprises contacting a first reactant (an alcohol) with a reactive carbonyl source (carbonyldiimidazole (CDI) or an alkylchloroformate) in the presence of a catalyst in reaction stream flowing through a continuous flow reactor at temperature 20° C. to about 160° C. and at a flow rate providing a residence time in the range of about 0.1 minute to about 24 hours; collecting a reactor effluent exiting from the continuous flow reactor; recovering a crude product from the reactor effluent; and distilling the crude product to obtain the organic carbonate compound of Formula (I). In another embodiment, the first reactant is an epoxide and the carbonyl source is carbon dioxide.
NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula:
##STR00001##
where R.sup.1-R.sup.6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.