Patent classifications
C07C317/18
METHOD AND INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF MENAQUINONE MK-7
The invention relates to a method and intermediate compounds for the preparation of menaquinone MK-7. The method for the preparation of menaquinone MK-7 is characterized in that, it comprises coupling of a compound of formula (11) with a compound of formula (17) in the presence of a base, to obtain a compound of formula (18), which is subjected to desulfonylation reaction in the presence of a palladium catalyst, to obtain a compound of formula (19), which is subjected to oxidation reaction, to obtain menaquinone MK-7. The invention also relates to compound (8), preferably in a crystalline form, which is a convenient intermediate compound for the preparation of menaquinone MK-7.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), ##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), ##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Hydrogels with biodegradable crosslinking
Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.
Hydrogels with biodegradable crosslinking
Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.
Process of vitamin K.SUB.2 .derivatives preparation
Provided is an improved process of vitamin K2 derivatives preparation, represented by formula (I) wherein n is an integer from 3 to 13. ##STR00001##
Process of vitamin K.SUB.2 .derivatives preparation
Provided is an improved process of vitamin K2 derivatives preparation, represented by formula (I) wherein n is an integer from 3 to 13. ##STR00001##
PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
##STR00001##
PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
##STR00001##
PROCESS OF VITAMIN K2 DERIVATIVES PREPARATION
Provided is an improved process of vitamin K2 derivatives preparation, represented by formula (I) wherein n is an integer from 3 to 13.
##STR00001##