Patent classifications
C07F9/22
POLYHYDROXYLATED CYCLOPENTANE DERIVATIVES AND METHODS OF USE
The present disclosure provides linker compounds of Formula (I) or (II): pharmaceutically acceptable salts thereof, and related scaffolds and conjugates. The present disclosure also relates to uses of the linker compounds, scaffolds, and conjugates, e.g., in delivering nucleic acid and/or treating or preventing diseases.
Liquid Formulations of Urease Inhibitors for Fertilizers
An improved solvent system for the formulation and application of N-alkyl thiophosphoric triamide urease inhibitors. These formulations provide safety and performance benefits relative to existing alternatives and enable storage, transport and subsequent coating or blending with urea based or organic based fertilizers. These formulations are comprised primarily of environmentally friendly aprotic and protic solvents (particularly dimethyl sulfoxide and alcohols/polyols) to stabilize the urease inhibitor.
Artificial single guide RNA and use thereof
The invention provides an artificial sgRNA and a CRISPR/Cas9 system by combining the artificial sgRNA and Cas9. Activity of the sgRNA can be retained even when a nucleotide linker region for forming a single strand by linking the 3′-terminal of crRNA and the 5′-terminal of tracrRNA in sgRNA is substituted with an amino acid derivative linker, when the linker region existing between stem-loop 1 and stem-loop 2 of tracrRNA and/or the loop portion of stem-loop 2 are/is substituted with an amino acid derivative linker, or when an amino acid derivative linker is added/inserted into the vicinity of the 5′-terminal and/or the 3′-terminal of sgRNA. Stability in vivo can be improved by introducing one or more amino acid derivative linkers into the sgRNA.
Diastereoselective synthesis of phosphate derivatives
The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.
Small molecule inhibitors selective for polo-like kinase proteins
Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of ##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.
COMPOSITIONS WITH IMPROVED UREASE-INHIBITING EFFECT COMPRISING (THIO)PHOSPHORIC ACID TRIAMIDE AND FURTHER COMPOUNDS SUCH AS AMINES AND COLORANTS
A composition comprising: (A) a mixture comprising at least one (thio)phosphoric acid triamide according to the general formula (I) R.sup.1R.sup.2N—P(X)(NH.sub.2).sub.2, wherein X is oxygen or sulfur; R.sup.1 is a C.sub.1 to C.sub.20 alkyl, C.sub.3 to C.sub.20 cycloalkyl, C.sub.6 to C.sub.20 aryl, or dialkylaminocarbonyl group; R.sup.2 is H, or R.sup.1 and R.sup.2 together with the nitrogen atom linking them define a 5- or 6-membered saturated or unsaturated heterocyclic radical, which optionally comprises 1 or 2 further heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur, and (L1) at least one amine selected from the group consisting of (L10), (L11), (L12), (L13), (L14), (L15), (L16), (L17), (L18), (L19), (L20), (L21), (L22), (L23), (L24), and (L29).
SOLVENT FOR THIOPHOSPHORIC TRIAMIDE OR DICYANDIAMIDE SOLUTIONS, AND RELATED METHODS
Solvents useful with thiophosphoric triamide urease inhibitors, that provide stable solution of a thiophosphoric triamide, such as for distribution (in low or high concentrations) onto a fertilizer or other liquid or solid material that contains urea.
Highly luminescent color-selective nanocrystalline materials
A nanocrystal capable of light emission includes a nanoparticle having photoluminescence having quantum yields of greater than 30%.
Capsaicinoid prodrug compounds and their use in treating medical conditions
The invention provides capsaicinoid prodrug compounds (e.g., prodrugs of resiniferatoxin, tinyatoxin, iodoresiniferatoxin, and related compounds), pharmaceutical compositions, and their use in the treatment of medical conditions, such as pain, and in agonizing TRPV1 activity.
Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of
##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.