- Dynamic kinetic resolution method for tail chain of Remdesivir phosphoric acid intermediate
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The invention relates to a drug intermediate of an RNA polymerase inhibitor, in particular to an intermediate of Remdesivir phosphate and a preparation method of the intermediate. According to the method, a compound Sp/Rp epimerization mixture in a formula (I) is crystallized under a dynamic kinetic resolution condition, so that the Rp single configuration isomer, in a formula (I'), of the Remdesivir intermediate is obtained. In the synthesis process, an epimerization mixture of the compound shown in the formula (I) is finally converted into a single-configuration I'compound through crystallization-induced epimerization under the dynamic kinetic resolution condition, so that the total yield of the reaction is increased, the utilization rate of raw materials is increased, and the process is more environmentally friendly and efficient.
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Paragraph 0049-0052
(2021/09/21)
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- Preparation method of (by machine translation)
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To the method disclosed by the invention, compound, compound, and compound V react IV; through acid hydrolysis to obtain compound IV compound III; compound III is subjected to further resolution under the action of a base, and the method disclosed by the invention is suitable for industrialized large-scale production II by avoiding the use, of genotoxic nitro substituent to reduce the risk I. of genotoxic impurities. (by machine translation)
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Paragraph 0008; 0018-0019; 0023-0024; 0027-0028
(2020/05/30)
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- THIARABINE- AND THIARABINE PRODRUG-BASED TREATMENTS
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The present disclosure is concerned with combination therapies that include sulfur- based nucleotide and nucleoside compounds for the treatment of various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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- 2,4,7-SUBSTITUTED-7-DEAZA-2'-DEOXY-2'-FLUOROARABINOSYL NUCLEOSIDE AND NUCLEOTIDE PRO-DRUGS AND USES THEREOF
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The present disclosure is concerned with 2,4,7-substituted-7-deaza-2'-deoxy-2'- fluoroarabinosyl nucleoside and nucleotide prodrugs that are capable of inhibiting viral infections and methods of treating viral infections such as, for example, human immunodeficiency virus (HIV), human papillomavirus (HPV), herpes simplex virus (HSV), human cytomegalovirus (HCMV), chicken pox, infectious mononucleosis, mumps, measles, rubella, shingles, ebola, viral gastroenteritis, viral hepatitis, viral meningitis, human metapneumovirus, human parainfluenza virus type 1, parainfluenza virus type 2, parainfluenza virus type 3, respiratory syncytial virus, viral pneumonia, Chikungunya virus (CHIKV), Venezuelan equine encephalitis (VEEV), dengue (DENV), influenza, West Nile virus (WNV), zika (ZIKV), 229E, NL63, OC43, HKU1, Middle East respiratory syndrome coronavirus (MERS-CoV), severe acute respiratory syndrome coronavirus (SARS-CoV), and severe acute respiratory syndrome coronavirus disease 2019 (SARS-CoV-2), using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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- Ribavirin side chain intermediate and preparation method thereof (by machine translation)
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To the method, the intermediate state is obtained by reaction of phenyl diphenyl phosphate and pentafluorophenol in an organic solvent under basic conditions, and an alanine (2 - ethyl butyl) ester hydrochloride is added to carry out butt-joint reaction, and then an organic solvent is used for refining to obtain high-purity target product N - [(S) (2,n-alanine) - L L-alanine (2 - ethylbutyl) ester. The method has great help for the current severe novel coronavirus 2019 - nCoV (?datdatdatas) epidemic situation control work. (by machine translation)
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Paragraph 0047-0057
(2020/07/02)
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- 4'-THIO-NUCLEOTIDE AND -NUCLEOSIDE PRODRUGS FOR THE TREATMENT OF CANCER
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The present disclosure is concerned with 4'-thio nucleotide and nucleoside compounds for the treatment of various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Paragraph 00424; 00432
(2019/11/12)
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- HCV POLYMERASE INHIBITORS
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The invention provides compounds of the formula:wherein B is a nucleobase selected from the groups (a) to (d):and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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Page/Page column 81; 82
(2020/02/14)
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- METHODS FOR TREATING ARENAVIRIDAE AND CORONAVIRIDAE VIRUS INFECTIONS
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Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
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Paragraph 0662-0663
(2017/04/04)
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- METHODS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS
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Provided are methods for treating Flaviviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I:, wherein the 1' position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Zika virus infections.
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Paragraph 0259
(2017/11/15)
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- METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
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Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae vims infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula (IV): The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
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Paragraph 0248
(2016/05/19)
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- DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
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The invention provides compounds of formula (I), wherein: R1 is OR11, or NR5R5'; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(=O)R6, O(C=O)R6 or O(C=O)OR6; R5′ is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.
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Page/Page column 49
(2016/03/22)
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- HCV POLYMERASE INHIBITORS
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The invention provides compounds of the formula:(I) wherein B is a nucleobase selected from the groups (a) to (d) and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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Page/Page column 67; 68
(2015/03/28)
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- HCV POLYMERASE INHIBITORS
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The invention provides compounds of the formula (I) wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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Page/Page column 69; 70
(2015/05/05)
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