Patent classifications
C07H1/02
Methods for the preparation of ribosides
- Steven Donald Axt ,
- Pavel Robertovich Badalov ,
- Katrien Brak ,
- Silvio Campagna ,
- Andrei Chtchemelinine ,
- Edward Doerffler ,
- Morin Mae Frick ,
- Detian Gao ,
- Lars V. Heumann ,
- Brittanie Hoang ,
- Willard Lew ,
- Robert Ronald MILBURN ,
- Sean Timothy Neville ,
- Bruce Ross ,
- Erik Rueden ,
- Robert William Scott ,
- Dustin Siegel ,
- Andrew C. Stevens ,
- Clarissa Tadeus ,
- Tiago Vieira ,
- Andrew W. Waltman ,
- Xianghong Wang ,
- Mark Charles Whitcomb ,
- Lydia Wolfe ,
- Chia-Yun Yu
Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE
The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE
The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
CD73 INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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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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.
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PHOSPHOROUS (V)-BASED REAGENTS, PROCESSES FOR THE PREPARATION THEREOF, AND THEIR USE IN MAKING STEREO-DEFINED ORGANOPHOSHOROUS (V) COMPOUNDS
The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
PYRIDINIUM SALTS AS ACTIVATORS IN THE SYNTHESIS OF STEREODEFINED OLIGONUCLEOTIDES
The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.
PYRIDINIUM SALTS AS ACTIVATORS IN THE SYNTHESIS OF STEREODEFINED OLIGONUCLEOTIDES
The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.
A METHOD FOR GENERATING RANDOM OLIGONUCLEOTIDES AND DETERMINING THEIR SEQUENCE
Random oligonucleotides are generated with incomplete information about the sequence of the nucleic acid bases present in the newly generated molecules. The sequences of the oligonucleotides are subsequently determined and then these oligonucleotides can be processed for various potential uses.
A METHOD FOR GENERATING RANDOM OLIGONUCLEOTIDES AND DETERMINING THEIR SEQUENCE
Random oligonucleotides are generated with incomplete information about the sequence of the nucleic acid bases present in the newly generated molecules. The sequences of the oligonucleotides are subsequently determined and then these oligonucleotides can be processed for various potential uses.