C07H19/23

MODULATORS OF 5'-NUCLEOTIDASE, ECTO AND THE USE THEREOF

Compounds that modulate the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided.

DERIVATIVES OF GYLCERO-MANNO-HEPTOSE ADP FOR USE IN MODULATING IMMUNE RESPONSE
20220177510 · 2022-06-09 ·

The disclosure provides compounds, compositions and methods related to activating alpha-kinase 1 (ALPK1) for modulating an immune response and treating or preventing cancer, infection, inflammation and related diseases and disorders as well as potentiating an immune response to a target antigen. The disclosure also provides heterocyclic compounds of formula (I) as agonists of alpha protein kinase 1 (ALPK1) and their use in activating ALPK1, modulating an immune response and treating diseases such as cancer, wherein A.sup.1, A.sup.2, L.sup.1, L.sup.2, L.sup.3, Z.sup.1, Z.sup.2, W.sup.1, W.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined herein.

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CD73 INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20220162253 · 2022-05-26 ·

A CD73 inhibitor having the structure represented by formula (I), a preparation method therefor and an application thereof are provided. The series of compounds can be widely applied in the preparation of drugs for treating cancers or tumors that are at least partially mediated by CD73, autoimmune diseases and disorders and metabolic diseases, in particular drugs for treating melanoma, colon cancer, pancreatic cancer, breast cancer, prostate cancer, lung cancer, leukemia, brain tumor, lymphoma, ovarian cancer and Kaposi's sarcoma. A new generation of CD73 inhibitor drugs is expected to be developed.

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CD73 inhibitors

Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

CD73 inhibitors

Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Cyclic Di-Nucleotide Compounds as STING Agonists

A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Y.sup.a, X.sup.a, X.sup.a1, X.sup.b, X.sup.b1, X.sup.c, X.sup.c1, X.sup.d, X.sup.d1, R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.5a, R.sup.6, R.sup.6a, R.sup.7, R.sup.7a, R.sup.8, R.sup.8a, and R.sup.9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds (I).

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Cyclic Di-Nucleotide Compounds as STING Agonists

A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Y.sup.a, X.sup.a, X.sup.a1, X.sup.b, X.sup.b1, X.sup.c, X.sup.c1, X.sup.d, X.sup.d1, R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.5a, R.sup.6, R.sup.6a, R.sup.7, R.sup.7a, R.sup.8, R.sup.8a, and R.sup.9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds (I).

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NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)

The disclosure is directed to compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, or Formula VI: Methods of their use in inhibiting a protein arginine methyltransferase 5 (PRMT5) enzyme and treating disease, as well as methods of their preparation are also described. ##STR00001## ##STR00002##