Patent classifications
C07C403/14
TOTAL SYNTHESIS METHOD FOR VITAMIN A AND DERIVATIVE THEREOF AND DEUTERATED COMPOUND THEREOF
Disclosed in the present invention is a total synthesis method for vitamin A and derivative thereof and deuterated compound thereof. ?-cyclocitral is used as a starting material to produce alkenyl boronate, then the alkenyl boronate (or hydrolyzed alkenyl boric acid) is subjected to a series of reactions to produce retinal or retinal with substituent, and the retinal or retinal with substituent is further subjected to a reduction reaction to obtain vitamin A or vitamin A with substituent; the vitamin A or vitamin A with substituent is subjected to an esterification reaction to obtain vitamin A ester or vitamin A ester with substituent; or said retinal or retinal with substituent is subjected to an oxidation reaction to obtain vitamin A acid or vitamin A acid with substituent. When deuterated allenol is used, deuterated vitamin A and derivative thereof are obtained. The present invention has the advantages of short synthetic route, simple operation, readily available raw materials and reagents, and modularization and divergence, and can synthesize the deuterated vitamin A and derivative thereof which are difficult to synthesize in the prior art.
Compounds for the treatment of HIV
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus. ##STR00001##
RETINAL DERIVATIVES AND METHODS FOR THE USE THEREOF FOR THE TREATMENT OF VISUAL DISORDERS
Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.
RETINAL DERIVATIVES AND METHODS FOR THE USE THEREOF FOR THE TREATMENT OF VISUAL DISORDERS
Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.
Compositions and methods for the delivery of nucleic acids
A nanosized complex includes a nucleic acid and a compound comprising formula (I): ##STR00001## wherein R.sup.1 is an alkylamino group or a group containing at least one aromatic group; R.sup.2 and R.sup.3 are independently an aliphatic group or hydrophobic group; R.sup.4 and R.sup.5 are independently H, a substituted or unsubstituted alkyl group, an alkenyl group, an acyl group, or an aromatic group, or a polymer, a targeting group, a detectable moiety, or a linker, or a combination thereof, and at least one of R.sup.4 and R.sup.5 includes a retinoid or retinoid derivative that targets and/or binds to an interphotoreceptor retinoid binding protein; a, b, c, and d are independently an integer from 1 to 10; and pharmaceutically acceptable salts thereof.
Compositions and methods for the delivery of nucleic acids
A nanosized complex includes a nucleic acid and a compound comprising formula (I): ##STR00001## wherein R.sup.1 is an alkylamino group or a group containing at least one aromatic group; R.sup.2 and R.sup.3 are independently an aliphatic group or hydrophobic group; R.sup.4 and R.sup.5 are independently H, a substituted or unsubstituted alkyl group, an alkenyl group, an acyl group, or an aromatic group, or a polymer, a targeting group, a detectable moiety, or a linker, or a combination thereof, and at least one of R.sup.4 and R.sup.5 includes a retinoid or retinoid derivative that targets and/or binds to an interphotoreceptor retinoid binding protein; a, b, c, and d are independently an integer from 1 to 10; and pharmaceutically acceptable salts thereof.
Retinal derivatives and methods for the use thereof for the treatment of visual disorders
Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.
Retinal derivatives and methods for the use thereof for the treatment of visual disorders
Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.
Compounds For the Treatment of HIV
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
##STR00001##
METHODS OF TREATMENT USING PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS
Compounds useful for the treatment of pain or cancer in a mammal.