Patent classifications
C07D473/22
PURINE COMPOUNDS FOR TREATING DISORDERS
Substituted purine compounds of formula (I)-(III) and salts thereof act as adenosine A2a receptor (A2aR) antagonists for cancer immunotherapy, depression, anxiety, multiple sclerosis, NASH, scleroderma, ADHD, Alzheimer's 5 and Parkinsons. Pharmaceutical compositions comprising such compounds, and methods of their use in treating depression are also taught.
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PURINE COMPOUNDS FOR TREATING DISORDERS
Substituted purine compounds of formula (I)-(III) and salts thereof act as adenosine A2a receptor (A2aR) antagonists for cancer immunotherapy, depression, anxiety, multiple sclerosis, NASH, scleroderma, ADHD, Alzheimer's 5 and Parkinsons. Pharmaceutical compositions comprising such compounds, and methods of their use in treating depression are also taught.
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SMALL MOLECULE PARG INHIBITORS AND METHODS OF USE THEREOF
The present disclosure provides methods of inhibiting PARG in cancer cells, including methods comprising administering a PARG inhibitor that modulates position Tyr795 in PARG. Also provided herein are methods of treating and/or preventing cancer comprising administering a PARG inhibitor. In some embodiments, the PARG inhibitors are of the formula: wherein the variables are defined herein.
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BROAD SPECTRUM ANTI-CANCER COMPOUNDS
Described herein, inter alia, are compounds for treating cancer and methods of use. This disclosure features chemical entities (e.g., small hairpin RNAs (shRNAs), micro RNA (miRNAs), small interfering RNA (siRNAs), small molecule inhibitors, antisense nucleic acids, peptides, viruses, CRISPR-sgRNAs, or combinations thereof) that inhibit one or more of m6A writers (e.g., methyltransferase like 3 (Mettl3 or MT-A70) or methyltransferase like-14 (Mettl14)), m6Am writers (e.g., phosphorylated CTD interacting factor I (PCIF 1), or Mettl3/14), m6A erasers (e.g., fat-mass and obesity-associated protein (FTO) or ALKB homolog 5 (ALKBH5)), m6Am erasers (e.g., FTO), m6A readers (e.g., YTH domain-containing family proteins (YTHs)), YTF domain family member 1 (YTHDF 1), YTF domain family member 2 (YTHDF 2), YTF domain family member 3 (YTHDF 3), or tyrosine-protein phosphatase non-receptor type 2 (PTPN2).
BROAD SPECTRUM ANTI-CANCER COMPOUNDS
Described herein, inter alia, are compounds for treating cancer and methods of use. This disclosure features chemical entities (e.g., small hairpin RNAs (shRNAs), micro RNA (miRNAs), small interfering RNA (siRNAs), small molecule inhibitors, antisense nucleic acids, peptides, viruses, CRISPR-sgRNAs, or combinations thereof) that inhibit one or more of m6A writers (e.g., methyltransferase like 3 (Mettl3 or MT-A70) or methyltransferase like-14 (Mettl14)), m6Am writers (e.g., phosphorylated CTD interacting factor I (PCIF 1), or Mettl3/14), m6A erasers (e.g., fat-mass and obesity-associated protein (FTO) or ALKB homolog 5 (ALKBH5)), m6Am erasers (e.g., FTO), m6A readers (e.g., YTH domain-containing family proteins (YTHs)), YTF domain family member 1 (YTHDF 1), YTF domain family member 2 (YTHDF 2), YTF domain family member 3 (YTHDF 3), or tyrosine-protein phosphatase non-receptor type 2 (PTPN2).
PAPD5 INHIBITORS AND METHODS OF USE THEREOF
The disclosure relates to compounds that are, e.g., PAP Associated Domain Containing 5 (PAPD5) inhibitors and methods of use thereof.
Nitrogen-Containing Heterocyclic Compound, Preparation Method, Intermediate, Pharmaceutical Composition and use
Disclosed are a nitrogen-containing heterocyclic compound, preparation method, intermediate, pharmaceutical composition and use. The nitrogen-containing heterocyclic compound of the present invention has a novel structure, relatively high TLR7 agonist activity, high selectivity and good safety.
Nitrogen-Containing Heterocyclic Compound, Preparation Method, Intermediate, Pharmaceutical Composition and use
Disclosed are a nitrogen-containing heterocyclic compound, preparation method, intermediate, pharmaceutical composition and use. The nitrogen-containing heterocyclic compound of the present invention has a novel structure, relatively high TLR7 agonist activity, high selectivity and good safety.
POLY(ADP-RIBOSE) GLYCOHYDROLASE (PARG) INHIBITORS AGAINST COVID MACRODOMAIN AND METHODS OF USING THE SAME
The present disclosure provides compounds of Formula (Ia) and Formula (Ib) and the pharmaceutically acceptable salts and solvates thereof, wherein A.sup.1, A.sup.2, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined as set forth in the specification. The present disclosure also provides the use of compounds of Formula (Ia) or Formula (Ib) to treat a coronavirus infection in a subject.
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POLY(ADP-RIBOSE) GLYCOHYDROLASE (PARG) INHIBITORS AGAINST COVID MACRODOMAIN AND METHODS OF USING THE SAME
The present disclosure provides compounds of Formula (Ia) and Formula (Ib) and the pharmaceutically acceptable salts and solvates thereof, wherein A.sup.1, A.sup.2, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined as set forth in the specification. The present disclosure also provides the use of compounds of Formula (Ia) or Formula (Ib) to treat a coronavirus infection in a subject.
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