Patent classifications
C07F9/65616
Nucleotide analogs
Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
SINGLE-STRANDED POLYNUCLEOTIDE
An object is to provide a technique that can enhance the binding properties of a single-stranded polynucleotide comprising a palindromic structure comprising an acyclic polynucleotide structural unit to target polynucleotides, such as miRNA, while suppressing self-duplex formation of the single-stranded polynucleotide. This object is achieved by a single-stranded polynucleotide comprising a palindromic structure comprising an acyclic polynucleotide structural unit, wherein adenine in the palindromic structure is replaced by diaminopurine, and thymine at a position complementary to the adenine is replaced by a thiouracil derivative.
Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
The present invention relates to Compounds of Formula (I) or Formula (II): ##STR00001##
or a pharmaceutically acceptable salt, solvate or enantiomer thereof, wherein A, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q and V are as defined herein. The present invention also relates to pharmaceutical compositions comprising a Compound of Formula (I) or Formula (II) and to their use in therapy.
SYNTHESIS OF BACKBONE MODIFIED MORPHOLINO OLIGONUCLEOTIDES AND CHIMERAS USING PHOSPHORAMIDITE CHEMISTRY
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.
INORGANIC POROUS SUBSTRATE, INORGANIC POROUS SUPPORT, AND NUCLEIC ACID PRODUCTION METHOD
An inorganic porous substrate having a silyl group represented by (i) and (ii) and having characteristics (iii) to (v), an inorganic porous support derived from the inorganic porous substrate, and a nucleic acid production method using the inorganic porous support: (i) a silyl group (A): a silyl group represented by the formula (i-1); (ii) a silyl group (B): at least one silyl group selected from the group consisting of silyl groups represented by (ii-1), (ii-2), and (ii-3); (iii) a particle diameter of 1 μm or more; (iv) a pore diameter of 20 nm or more; and (v) a cumulative pore volume in a pore diameter range of 40 nm to 1000 nm of more than 0.32 mL/g and 4 mL/g or less.
##STR00001##
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.
Functionally-Modified Oligonucleotides And Subunits Thereof
Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
PHOSPHOLIPIDATION OF IMIDAZOQUINOLINES AND OXOADENINES
The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)—active and toll-like receptor (TLR8)—active imidazoquinolines and oxoadenines.
PRODRUGS OF PHOSPHONAMIDE NUCLEOTIDE ANALOGUES AND THEIR PHARMACEUTICAL USE
Compounds, compositions, and method useful for treating a viral infection, such as human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, are disclosed. In particular, prodrugs of phosphonamide nucleotide analogues and methods for their preparation and use as therapeutic or prophylactic agents are disclosed.
PRODRUGS OF PHOSPHONAMIDE NUCLEOTIDE ANALOGUES AND THEIR PHARMACEUTICAL USE
Compounds, compositions, and method useful for treating a viral infection, such as human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, are disclosed. In particular, prodrugs of phosphonamide nucleotide analogues and methods for their preparation and use as therapeutic or prophylactic agents are disclosed.