C07D473/18

SALICYL-ADENOSINEMONOSULFAMATE ANALOGS AND USES THEREOF

Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts or tautomers thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment and/or prevention of an infectious disease (e.g., bacterial infection (e.g., Mycobacterium infection (e.g., tuberculosis)). (I)

##STR00001##

SALICYL-ADENOSINEMONOSULFAMATE ANALOGS AND USES THEREOF

Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts or tautomers thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment and/or prevention of an infectious disease (e.g., bacterial infection (e.g., Mycobacterium infection (e.g., tuberculosis)). (I)

##STR00001##

COMPOUNDS FOR USES IN PHARMACOLOGICAL INDUCTION OF HBF FOR TREATMENT OF SICKLE CELL DISEASE AND ß-THALASSEMIA
20220152036 · 2022-05-19 ·

Provided herein are compounds of Formula (I). The compounds described herein are useful in treating a disease associated with the expression of endogenous embryonic/fetal globin (e.g., γ globin) in erythrocytes (e.g., treating β-thalassemia and/or sickle cell disease through at least the induction of the globin gene expression in erythrocytes), and/or anemia (β-thalassemia and/or sickle cell anemia). The compounds described herein are useful in treating, delaying, and/or preventing the adverse effects of β-thalassemia and/or sickle cell disease, inducing γ globin production, and/or inducing the expression of embryonic/fetal globin genes in a subject, cell, tissue, or biological sample. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for inducing γ globin production described herein and for treating any of the target diseases described herein.

##STR00001##

COMPOUNDS FOR USES IN PHARMACOLOGICAL INDUCTION OF HBF FOR TREATMENT OF SICKLE CELL DISEASE AND ß-THALASSEMIA
20220152036 · 2022-05-19 ·

Provided herein are compounds of Formula (I). The compounds described herein are useful in treating a disease associated with the expression of endogenous embryonic/fetal globin (e.g., γ globin) in erythrocytes (e.g., treating β-thalassemia and/or sickle cell disease through at least the induction of the globin gene expression in erythrocytes), and/or anemia (β-thalassemia and/or sickle cell anemia). The compounds described herein are useful in treating, delaying, and/or preventing the adverse effects of β-thalassemia and/or sickle cell disease, inducing γ globin production, and/or inducing the expression of embryonic/fetal globin genes in a subject, cell, tissue, or biological sample. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for inducing γ globin production described herein and for treating any of the target diseases described herein.

##STR00001##

SYNTHESIS OF BACKBONE MODIFIED MORPHOLINO OLIGONUCLEOTIDES AND CHIMERAS USING PHOSPHORAMIDITE CHEMISTRY
20220144867 · 2022-05-12 ·

Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

Substituted aryl ether compound, preparation method thereof, pharmaceutical composition and use thereof

The present invention relates to a compound having the following formula, or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, preparation method thereof, pharmaceutical composition comprising the same and use of the compound in the manufacture of a medicament for preventing or treating tumor, wherein the substituents are as defined in the specification. ##STR00001##

Substituted aryl ether compound, preparation method thereof, pharmaceutical composition and use thereof

The present invention relates to a compound having the following formula, or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, preparation method thereof, pharmaceutical composition comprising the same and use of the compound in the manufacture of a medicament for preventing or treating tumor, wherein the substituents are as defined in the specification. ##STR00001##

ASYMMETRIC AUXILIARY GROUP
20220127301 · 2022-04-28 ·

To provide a chiral reagent or a salt thereof.

The chiral reagent has following chemical formula (I). In the formula (I), G.sup.1 and G.sup.2 are independently a hydrogen atom, a nitro group (—NO.sub.2), a halogen atom, a cyano group (—CN), a group of formula (II) or (III), or both G.sup.1 and G.sup.2 taken together to form a group of formula (IV).

##STR00001##

ASYMMETRIC AUXILIARY GROUP
20220127301 · 2022-04-28 ·

To provide a chiral reagent or a salt thereof.

The chiral reagent has following chemical formula (I). In the formula (I), G.sup.1 and G.sup.2 are independently a hydrogen atom, a nitro group (—NO.sub.2), a halogen atom, a cyano group (—CN), a group of formula (II) or (III), or both G.sup.1 and G.sup.2 taken together to form a group of formula (IV).

##STR00001##

Antibody-immune agonist conjugate and applications thereof

The present disclosure relates to a linking unit molecule for targeting molecule-drug conjugate, and the corresponding conjugate, the preparation and use thereof, and in particular relates to an antibody-immune agonist conjugate (AIAC) as a novel type of cancer therapy.