Patent classifications
C07C275/20
METABOLICALLY ROBUST ANALOGS OF CYP-EICOSANOIDS FOR THE TREATMENT OF CARDIAC DISEASE
The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of cardiovascular diseases.
METHOD FOR PRODUCING URACIL COMPOUND
An object of the present invention is to provide an industrially advantageous method for producing uracil compound, which is a production intermediate of a 2,6-dioxo-3,6-dihydropyrimidine compound, and ureidomethylene compound applicable as a raw material for uracil compounds. The present invention is characterized in that uracil compound, which is a production intermediate of a 2,6-dioxo-3,6-dihydropyrimidine compound, is produced by subjecting a compound of formula (II) below or a salt thereof to chemical reaction in the presence of an organic base or an inorganic base. In formula (II), X.sup.1 represents a hydrogen atom or a substituted or unsubstituted C1-6 alkyl group, X.sup.2 represents a hydrogen atom or a substituted or unsubstituted linear C1-6 alkyl group, etc., R.sup.1 represents a hydrogen atom or a substituted or unsubstituted C1-6 alkyl group, etc., R.sup.2 represents a hydrogen atom or a substituted or unsubstituted C1-6 alkyl group, and R.sup.3 represents a substituted or unsubstituted C1-6 alkyl group, etc.
##STR00001##
Amino acid derivatives
There are provided pyrrolysine analogs of the formulae (X), (I), (II), (V), (VI), (VII) and (VIII), in which the a, b, d, X, Y, Z, FG, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the claims, which are useful in bioconjugation processes and mutant proteins containing them.
Amino acid derivatives
There are provided pyrrolysine analogs of the formulae (X), (I), (II), (V), (VI), (VII) and (VIII), in which the a, b, d, X, Y, Z, FG, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the claims, which are useful in bioconjugation processes and mutant proteins containing them.
COMPOUNDS AND METHOD OF USE THEREOF FOR TREATING BACTERIAL DISEASES
The present disclosure provides compounds that can inhibit the type III secretion system (TTSS) to decrease the pathogenesis of gram-negative bacteria. These compounds may have wide applications for treating bacteria diseases caused by gram-negative bacteria in a host species, including but not limited to, plants and animals. The present invention further relates to compositions that inhibit pathogenesis of gram-negative bacteria without killing the bacteria. Methods relating to preventing and/or treating infection of a host species by bacterial pathogens are also provided herein.
COMPOUNDS AND METHOD OF USE THEREOF FOR TREATING BACTERIAL DISEASES
The present disclosure provides compounds that can inhibit the type III secretion system (TTSS) to decrease the pathogenesis of gram-negative bacteria. These compounds may have wide applications for treating bacteria diseases caused by gram-negative bacteria in a host species, including but not limited to, plants and animals. The present invention further relates to compositions that inhibit pathogenesis of gram-negative bacteria without killing the bacteria. Methods relating to preventing and/or treating infection of a host species by bacterial pathogens are also provided herein.
LIPID COMPOUND AND USE THEREOF
The present application provides a novel lipid compound, a lipid nanoparticle comprising the same, and use thereof in targeted delivery of a drug. Specifically, the present application provides a compound of Formula I
##STR00001## or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof. Furthermore, the present application provides a lipid nanoparticle comprising the compound of Formula I or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof; still further, the lipid nanoparticle may further comprise a cationic lipid; yet still further, the lipid nanoparticle may further comprise a helper lipid. A composition comprising the above compound or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof, or the lipid nanoparticle can achieve the organ-targeted delivery of a therapeutic/prophylactic agent.
LIPID COMPOUND AND USE THEREOF
The present application provides a novel lipid compound, a lipid nanoparticle comprising the same, and use thereof in targeted delivery of a drug. Specifically, the present application provides a compound of Formula I
##STR00001## or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof. Furthermore, the present application provides a lipid nanoparticle comprising the compound of Formula I or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof; still further, the lipid nanoparticle may further comprise a cationic lipid; yet still further, the lipid nanoparticle may further comprise a helper lipid. A composition comprising the above compound or a pharmaceutically acceptable salt, a prodrug, or a stereoisomer thereof, or the lipid nanoparticle can achieve the organ-targeted delivery of a therapeutic/prophylactic agent.
COMPOSITION FOR ORGAN-SPECIFIC DELIVERY OF NUCLEIC ACID
The present application provides a composition for organ-specific delivery of nucleic acids, which comprises a guided on-target lipid delivery lipid; further, the composition may comprise a helper lipid; still further, the composition may comprise a cationic lipid. The guided on-target lipid delivery lipid may be selected from one or more of an ionizable anionic steroid and/or an ionizable anionic polymer conjugated lipid; the helper lipid is optionally one or more of a phospholipid, a steroid, a polymer conjugated lipid, and a modifiable lipid; and the cationic lipid may be selected from one or more of a permanently cationic lipid and/or an ionizable cationic lipid. The delivery composition is capable of specifically delivering a prophylactic/therapeutic agent, particularly a nucleic acid component, to a target organ.
Cationic lipid compound, and preparation method therefor and use thereof
A cationic lipid compound, and a preparation method therefor and use thereof are provided. The cationic lipid compound features a hydroxyl group at the head part, and its overall structure resembles a cone with a small head and a large tail. The LNPs prepared using the cationic lipid compounds with the aforementioned optimal structure usually exhibit enhanced biocompatibility and higher in vivo mRNA transfection efficiency, achieving unexpected technical effects. The synthesis route of the cationic lipid compounds is straightforward and practicable, with inexpensive and readily available raw materials, facilitating industrial production. Furthermore, the LNPs produced from the cationic lipid compounds possess a stable nanostructure that can be stored at low temperatures for a long time, thereby prolonging the shelf life of the pharmaceutical products while reducing the transportation requirements.