Patent classifications
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.
Process for the preparation of Ivacaftor and its intermediates
The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.
Process for the preparation of Ivacaftor and its intermediates
The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.
Process for the preparation of Ivacaftor and its intermediates
The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.
Carbonic acid adducts
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.
Carbonic acid adducts
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.
NITROGEN-CONTAINING CHAIN COMPOUND, PREPARATION METHOD, COMPOSITION CONTAINING SAID COMPOUND, AND USE THEREOF
Disclosed are a nitrogen-containing chain compound, a preparation method, a composition containing said compound, and a use thereof. Provided is a nitrogen-containing chain compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The nitrogen-containing chain compound represented by formula (I) may be used for preparing a lipid carrier. The prepared lipid carrier can encapsulate a nucleic acid drug, and may be used for delivering a nucleic acid prophylactic agent and/or therapeutic agent to mammalian cells and organs and producing an effect.