C07D473/18

Synthesis of 2′,3′-dideoxynucleosides for automated DNA synthesis and pyrophosphorolysis activated polymerization

Methods for preparation of 2′,3′-dideoxynucleotides support structures, such as 2′,3′-dideoxyguanosine, 2′,3′-dideoxyadenosine, and 3′-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization.

Synthesis of 2′,3′-dideoxynucleosides for automated DNA synthesis and pyrophosphorolysis activated polymerization

Methods for preparation of 2′,3′-dideoxynucleotides support structures, such as 2′,3′-dideoxyguanosine, 2′,3′-dideoxyadenosine, and 3′-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization.

2, 6-Di-nitrogen-containing substituted purine derivative, and preparation method, pharmaceutical composition and use thereof

The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability. ##STR00001##

2, 6-Di-nitrogen-containing substituted purine derivative, and preparation method, pharmaceutical composition and use thereof

The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability. ##STR00001##

Amino-triazolopyridine Compounds and Their Use in Treating Cancer

The specification generally relates to compounds of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, where R.sup.1 and R.sup.2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Amino-triazolopyridine Compounds and Their Use in Treating Cancer

The specification generally relates to compounds of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, where R.sup.1 and R.sup.2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

COMPOSITIONS CONTAINING, METHODS AND USES OF ANTIBODY-TLR AGONIST CONJUGATES

Disclosed herein are Trastuzumab-linked TLR-agonist derivative analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The Trastuzumab-linked TLR-agonist derivative analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such Trastuzumab-linked TLR-agonist derivative analogs. Typically, the modified Trastuzumab-linked TLR-agonist derivative analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs and modified non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs, including therapeutic, diagnostic, and other biotechnology use.

COMPOSITIONS CONTAINING, METHODS AND USES OF ANTIBODY-TLR AGONIST CONJUGATES

Disclosed herein are Trastuzumab-linked TLR-agonist derivative analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The Trastuzumab-linked TLR-agonist derivative analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such Trastuzumab-linked TLR-agonist derivative analogs. Typically, the modified Trastuzumab-linked TLR-agonist derivative analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs and modified non-natural amino acid Trastuzumab-linked TLR-agonist derivative analogs, including therapeutic, diagnostic, and other biotechnology use.