公开(公告)号：US4140850A

公开(公告)日：1979-02-20

申请号：US828797

申请日：1977-08-29

申请人： Wendell Wierenga

发明人： Wendell Wierenga

IPC分类号： C07H9/06 ,  C07H19/12 ,  C07H23/00 ,  C07H17/00

CPC分类号： C07H9/06 ,  C07H19/12 ,  C07H23/00

摘要： Novel anhydroarabinofuranosyldihydrotriazine nucleosides and process for preparing the same. The compounds of formula I are useful as immunosuppressive agents in humans and are also active in vitro against various susceptible Herpes Viruses.

摘要翻译： 新型脱氢阿糖呋喃糖基二氢三嗪核苷及其制备方法。 式I的化合物可用作人的免疫抑制剂，并且在体外对各种易感的疱疹病毒也是活性的。

公开(公告)号：US4022889A

公开(公告)日：1977-05-10

申请号：US586232

申请日：1975-06-12

申请人： Brian Bannister ,  Clarence DeBoer ,  Harold E. Renis

发明人： Brian Bannister ,  Clarence DeBoer ,  Harold E. Renis

IPC分类号： C07H19/12 ,  A61K31/71

CPC分类号： C07H19/12

摘要： Pharmaceutical compositions of antibiotic U-44,590 and derivatives thereof which can be used to treat Gram-negative and Gram-positive bacterial and viral diseases in humans and animals.

摘要翻译： 抗生素U-44,590及其衍生物的药物组合物可用于治疗人和动物中的革兰氏阴性和革兰氏阳性细菌和病毒性疾病。

公开(公告)号：US3954752A

公开(公告)日：1976-05-04

申请号：US476459

申请日：1974-06-05

申请人： Alois Piskala ,  Frantisek Sorm

发明人： Alois Piskala ,  Frantisek Sorm

IPC分类号： C07H19/12 ,  C07D253/06

CPC分类号： C07H19/12

摘要： Process for preparing 2',3',5'-tri-0-acetyl-6-azauridine having the following formula ##SPC1##Which comprises reacting a crude anomeric mixture of methyl D-ribofuranosides having the formula ##SPC2##With anhydrous hydrogen chloride or anhydrous hydrogen bromide in the presence of acetic anhydride and acetic acid to thereby form the corresponding 2,3,5-tri-0-acetyl-D-ribofuranosyl halide having the formula ##SPC3##Wherein X is chloro or bromo, reacting the halide of formula III with 3,5-bis-trimethylsilyloxy-1,2,4-triazine having the following formula ##SPC4##In the presence of an inert solvent and a mercuric halide and recovering the 2',3',5'-tri-0-acetyl-6-azauridine.

摘要翻译： 制备具有下列结构式的2'，3'，5'-三-O-乙酰基-6-氮杂环丁烷的方法，其中包括反应具有下式的甲基D-呋喃核糖苷的原始反应混合物，其具有无机氢氯化物或无机氢溴化物 乙酸酐和乙酸的存在形成具有式WHEREIN X为氯或溴的相应的2,3,5-三-O-乙酰基-D-呋喃核糖基卤，使式III的卤化物与3,5-双 具有下式的三甲基甲硅烷氧基-1,2,4-三嗪在惰性溶剂和富马酸盐的存在下并恢复2'，3'，5'-三-O-乙酰基-6-氮杂环丁烷。

公开(公告)号：US3776899A

公开(公告)日：1973-12-04

申请号：US3776899D

申请日：1970-07-24

申请人： INST MICROBIOLOGII KIEW

发明人： CHERNETSKY V ,  ALEXEEVA I

IPC分类号： C07H19/12 ,  C07D51/52

CPC分类号： C07H19/12

摘要： A METHOD IN WHICH SOLUTIONS OF 2H, 3''-O-ALKYLIDENE-5''O-ACYL-4-THIO-6-AZAURIDINES OR 2'',3''-O-ALKYLIDENE-4-THIO6-AZAURIDINES IN ORGANIC SOLVENTS ARE TREATED WITH AMMONIA AT ATMOSPHERIC PRESSURE TO CONVER THE SUBSTITUTED AZAURIDINES TO 2'',3''-O-ALKYLIDENE-5-O-ACYL-6-AZACYTIDINES OR 2'',3''-O-ALKYLIDENE-6-AZACYTIDINES WHICH MAY THEN BE CONVERTED, IF DESIRED, TO FREE 6-AZACYTIDINE BY DISSOLVING THE ABOVE SUBSTITUTED-6-AZACYTIDINE IN AN ANHYDROUS SOLVENT AND TREATING SAME WITH A METAL ALCOHOLATE AT AN ALKALINE PH.

公开(公告)号：US3708469A

公开(公告)日：1973-01-02

申请号：US3708469D

申请日：1969-09-15

申请人： SCHERING AG

发明人： VORBRUGGEN H ,  STREHLKE P

IPC分类号： C07D239/46 ,  C07D239/56 ,  C07D239/60 ,  C07D253/075 ,  C07F7/08 ,  C07H19/06 ,  C07H19/12 ,  C07H19/16 ,  C07D51/52

CPC分类号： C07D239/47 ,  C07D239/56 ,  C07D239/60 ,  C07D253/075 ,  C07F7/0898 ,  C07H19/06 ,  C07H19/12 ,  C07H19/16

摘要： 2-THIOPYRIMIDINE NUCLEOSIDES EXHIBITING CYTOTOXIC, ANTIVIRAL, ENZYME-INHIBITING AS WELL AS ANTIHYPERTHYROID EFFECTS ARE OBTAINED BY A NOVEL PROCESS COMPRISING REACTING A SILYL COMPOUND OF THE FORMULA

A1-SI(-A2)(-A3)-S-C
WITH A MASKED HALOGEN SUGAR AND THEN SPLITTING OFF THE BLOCKING GROUPS, THE FINAL COMPOUNDS BEING OF THE FORMULA

Z-N
WHEREIN X IS O OR NH, Y IS N OR CH, R IS H, ALKYL OF 1-4 CARBON ATOMS, HALOGEN, NITRO, NITRILE LOWER ALKYLAMINO LOWER ALKOXY, OR THE GROUP

-(CH2)N-CO-A

WHEREIN N IS O, 1 OR 2 IS O-ALKYL OF 1-5 CARBON ATOMS NH2 OR LOWER ALKYLAMINO, AND Z IS A SUGAR RESIDUE, AND WHEREIN IN FORMULA I A1, A2 AND A3 REPRESENT LOWER ALKYL.

公开(公告)号：US3282921A

公开(公告)日：1966-11-01

申请号：US37271264

申请日：1964-06-04

申请人： SYNTEX CORP

发明人： VERHEYDEN JULIEN P H ,  MOFFATT JOHN G

IPC分类号： C07H19/06 ,  C07H19/12

CPC分类号： C07H19/06 ,  C07H19/12

公开(公告)号：US20230416294A1

公开(公告)日：2023-12-28

申请号：US18041124

申请日：2021-08-10

申请人： The Johns Hopkins University ,  Institute of Organic Chemistry and Biochemistry AS CR v.v.i.

发明人： Barbara Slusher ,  Rana Rais ,  Franco D'Alessio ,  Pavel Majer ,  Marcela Krecmerova ,  Srinivasan Yegnasubramanian

IPC分类号： C07H19/12 ,  A61P37/06 ,  A61P29/00 ,  A61K45/06 ,  A61K31/706

CPC分类号： C07H19/12 ,  A61P37/06 ,  A61K31/706 ,  A61K45/06 ,  A61P29/00

摘要： Novel N4-substituted decitabine analogs are disclosed that exhibit promising in vitro and in vivo therapeutic activity. These novel compounds were shown to be resistant to deamination via cytidine deaminase (CDA) metabolism and provide a unique pharmacokinetic profile versus decitabine, while retaining the ability to induce DNA demethylation in target cells. These novel compounds can be used for treating hematological cancers, as well for new therapeutic interventions, including bacterial or viral pneumonia, acute respiratory distress syndrome, pulmonary fibrosis, transplantation and checkpoint inhibitor-induced adverse events, including pneumonitis.

公开(公告)号：US20210361777A1

公开(公告)日：2021-11-25

申请号：US17384350

申请日：2021-07-23

申请人： CEPHALON, INC.

发明人： Anthony S. DRAGER ,  Paritosh WATTAMWAR

IPC分类号： A61K47/69 ,  A61K47/54 ,  C07H19/12 ,  C07H15/24 ,  C07H15/26 ,  A61K9/51 ,  A61K9/00 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/704

摘要： The disclosure provides compounds of Formula (I), wherein X, Y, and Z are defined herein. The disclosure also provides particles comprising one or more compounds described herein, compositions comprising one or more compounds or particles described herein and a pharmaceutically acceptable carrier, and methods of treating a subject in need thereof comprising administering one or more compounds, particles, or compositions described herein to the subject. X—Y—Z  (I)

公开(公告)号：US10738073B2

公开(公告)日：2020-08-11

申请号：US16024221

申请日：2018-06-29

申请人： Geron Corporation

发明人： Sergei M. Gryaznov ,  Krisztina Pongracz ,  Daria Zielinska

IPC分类号： C07H19/16 ,  C07H19/06 ,  C07H19/12 ,  C07H19/10

摘要： Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base.

公开(公告)号：US10513534B2

公开(公告)日：2019-12-24

申请号：US14047862

申请日：2013-10-07

申请人： IDENIX PHARMACEUTICALS LLC ,  Centre National De La Recherche Scientifique ,  UNIVERSITE DE MONTPELLIER

发明人： Gilles Gosselin ,  Christophe Claude Parsy ,  Francois-Rene Alexandre ,  Houcine Rahali ,  Jean-Francois Griffon ,  Dominique Surleraux ,  Cyril B. Dousson ,  Claire Pierra ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC分类号： C07H19/06 ,  C07H19/073 ,  C07H19/10 ,  C07H19/11 ,  C07H19/16 ,  C07H19/173 ,  C07H19/20 ,  C07H19/213 ,  A61K31/7072 ,  A61K45/06 ,  A61K38/21 ,  A61K31/7076 ,  C07H19/14 ,  A61K31/7064 ,  C07H19/12 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/708 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7105 ,  C07H19/23

摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.