C07H19/173

2' AND/OR 5' AMINO-ACID ESTER PHOSPHORAMIDATE 3'-DEOXY ADENOSINE DERIVATIVES AS ANTI-CANCER COMPOUNDS

Disclosed are chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in homo sapiens. The compounds are derivatives of cordycepin (3′-deoxyadenosine) having a 2′ and/or 5′-amino-acid ester phosphoramidate moiety.

INHIBITORS OF ADENYLATE-FORMING ENZYME MENE

Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts or tautomers thereof which may inhibit adenylate-forming enzymes. Also provided are pharmaceutical compositions, kits, uses, and methods involving the inventive compounds for the treatment and/or prevention of an infectious disease (e.g., bacterial infection (e.g., tuberculosis, methicillin-resistant Staphylococcus aureus)).

INHIBITORS OF ADENYLATE-FORMING ENZYME MENE

Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts or tautomers thereof which may inhibit adenylate-forming enzymes. Also provided are pharmaceutical compositions, kits, uses, and methods involving the inventive compounds for the treatment and/or prevention of an infectious disease (e.g., bacterial infection (e.g., tuberculosis, methicillin-resistant Staphylococcus aureus)).

NUCLEOSIDES AND NUCLEOTIDES WITH 3' ACETAL BLOCKING GROUP

Embodiments of the present disclosure relate to nucleotide and nucleoside molecules with acetal 3′-OH blocking groups. Also provided herein are methods to prepare such nucleotide and nucleoside molecules, and the uses of fully functionalized nucleotides containing the 3′ acetal blocking group for sequencing applications.

NUCLEOSIDES AND NUCLEOTIDES WITH 3' ACETAL BLOCKING GROUP

Embodiments of the present disclosure relate to nucleotide and nucleoside molecules with acetal 3′-OH blocking groups. Also provided herein are methods to prepare such nucleotide and nucleoside molecules, and the uses of fully functionalized nucleotides containing the 3′ acetal blocking group for sequencing applications.

COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO.sub.2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

6-MERCAPTOPURINE NUCLEOSIDE ANALOGUES
20210380628 · 2021-12-09 ·

A compound has the following formula (I) or formula (II), an isomer thereof, a tautomer thereof, a pharmaceutical acceptable solvate thereof, or a pharmaceutical acceptable prodrug thereof.

##STR00001##

NUCLEOSIDE DERIVATIVE AND USE THEREOF
20210371447 · 2021-12-02 · ·

A nucleoside derivative represented below, or a salt thereof.

##STR00001##

(In (1), R.sup.1 represents a hydrogen atom, a hydroxyl group or a protected group, and in (2), X represent a halogen atom. In (1) and (2), R.sup.2 and R.sup.4 each represent a hydrogen atom, a hydroxyl protecting, phosphate, or protected phosphate group, or —P(═O).sub.nR.sup.5R.sup.6 (n is 0 or 1, R.sup.5 and R.sup.6 each representing a hydrogen atom, hydroxyl, protected hydroxyl, mercapto, protected mercapto, lower alkoxy, cyano lower alkoxy, amino or substituted amino group, when n is 1, R.sup.5 and R.sup.6 are not both hydrogen atoms), R.sup.3 represents NHR.sup.7 (R.sup.7 represents a hydrogen atom, alkyl, alkenyl or protecting group for an amino group), an azide, amidino or guanidino group, each having a linking group (when R.sup.7 is hydrogen atom, the linking group is an alkylene group), and B represents any of a purine-9-yl, 2-oxo-pyrimidin-1-yl, substituted purine-9-yl or substituted 2-oxo-pyrimidin-1-yl group.)

2′ and/or 5′ amino-acid ester phosphoramidate 3′-deoxy adenosine derivatives as anti-cancer compounds

Disclosed are chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in Homo sapiens. The compounds are derivatives of cordycepin (3′-deoxyadenosine) having a 2′ and/or 5′-amino-acid ester phosphoramidate moiety.

2′ and/or 5′ amino-acid ester phosphoramidate 3′-deoxy adenosine derivatives as anti-cancer compounds

Disclosed are chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in Homo sapiens. The compounds are derivatives of cordycepin (3′-deoxyadenosine) having a 2′ and/or 5′-amino-acid ester phosphoramidate moiety.