公开(公告)号：EP2607370A3

公开(公告)日：2014-03-12

申请号：EP12199225.9

申请日：2003-08-06

申请人： Novartis AG

发明人： Storer, Richard ,  Jonaitis, David

IPC分类号： C07H19/073 ,  A61K31/7072 ,  A61P31/12

CPC分类号： C07H19/073 ,  A61K31/7072 ,  C07H19/06

摘要： Amorphous forms of beta-L-2'-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2'-deoxythymidine can be used in the manufacture of other forms of beta-L-2'-deoxythymidine, or in pharmaceutical compositions. Particularly preferred use is the treatment of hepatitis B.

公开(公告)号：EP2558478A4

公开(公告)日：2013-10-23

申请号：EP11769451

申请日：2011-04-12

申请人： SOMALOGIC INC

发明人： ROHLOFF JOHN ,  JANJIC NEBOJSA ,  CARTER JEFFREY D ,  FOWLER CATHERINE

IPC分类号： C07H19/073 ,  C07H19/10 ,  C07H21/04

CPC分类号： C07H19/10 ,  C07H19/06 ,  C07H21/04 ,  C12N15/115 ,  C12N2310/335

摘要： The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.

摘要翻译： 本公开涉及核酸化学领域，具体涉及5位修饰的尿苷以及其亚磷酰胺和三磷酸衍生物。 本公开还涉及制备和使用该方法。

公开(公告)号：EP2578578A1

公开(公告)日：2013-04-10

申请号：EP11789564.9

申请日：2011-04-25

申请人： Central Glass Company, Limited

发明人： ISHII, Akihiro ,  NAGURA, Hirokatsu ,  TSURUTA, Hideyuki

IPC分类号： C07D317/30 ,  A61K31/7068 ,  C07B61/00 ,  C07H19/073

CPC分类号： C07D317/30 ,  Y02P20/55

摘要： In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SO 2 F 2 ) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is useful as an important intermediate for the synthesis of 2'-deoxy-2'-fluoro-2'-C-methylcytidine with antivirus activity.

摘要翻译： 在本发明的存在下，通过1,2-二醇与（II）二醇的反应制备开环氟化合物的形式的（2R）-2-氟-2-C-甲基-D-内酰基-3-内酯前体 硫酰氟（SO 2 F 2）在有机碱和任选的氟离子源存在下进行。 本发明的制造方法与以往的制造方法（缩短三个步骤：环状亚硫酸酯化，氧化和开环氟化至一步）相比，确保了较少的工艺步骤，并且满足了工业生产的要求（高产率 和高繁殖力）。 由此获得的（2R）-2-氟-2-C-甲基-D-内酰基-3-内酯前体可用作合成2'-脱氧-2'-氟-2'-基内酯前体的重要中间体 甲基胞苷具有抗病毒活性。

公开(公告)号：EP2562255A1

公开(公告)日：2013-02-27

申请号：EP11772132.4

申请日：2011-04-21

申请人： Riken ,  TagCyx Biotechnologies

发明人： HIRAO, Ichiro ,  HIRAO, Michiko ,  YOKOYAMA, Shigeyuki ,  MITSUI, Tsuneo ,  YAMASHIGE, Rie

IPC分类号： C12N15/09 ,  C07H19/044 ,  C07H19/073 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/542

CPC分类号： G01N21/6486 ,  C07H19/044 ,  C12Q1/6818 ,  C12Q2525/117

摘要： It is an object of the present invention to provide quenching or fluorescent nucleic acid base analogs and applications thereof. The quencher of the present invention has a 2-nitropyrrole structure represented by Formula I:

(in Formula I, R 1 and R 2 are groups independently selected from the group consisting of:
ribose and deoxyribose;
hydrogen, hydroxyl and SH groups, and halogens;
substituted or unsubstituted alkyl, alkenyl, and alkynyl groups each having 2 to 10 carbon atoms;
one or more five-membered heterocyclic rings, one or more six-membered heterocyclic rings, and one or more fused heterocyclic rings, these heterocylic rings containing nitrogen or sulfur, and one or more aromatic rings;
sugars, sugar chains, amino acids, and peptides; and
fluorescent molecules linked via linkers).

摘要翻译： 本发明的目的是提供淬灭或荧光核酸碱基类似物及其应用。 本发明的猝灭剂具有由式I表示的2-硝基吡咯结构：（式I中，R 1和R 2独立地选自：核糖和脱氧核糖;氢，羟基和SH基团以及卤素 取代或未取代的碳原子数为2〜10的烷基，链烯基和炔基;一个以上五元环，一个以上六元杂环，一个以上稠合杂环，这些杂环含有氮 或硫，以及一个或多个芳环;糖，糖链，氨基酸和肽;以及通过接头连接的荧光分子）。

公开(公告)号：EP2402358A3

公开(公告)日：2012-07-18

申请号：EP10172853.3

申请日：2010-08-15

申请人： Instytut Biochemii I Biofizyki Pan

发明人： ZIEMKOWSKI, Przemys?aw ,  MIAZGA, Agnieszka ,  KULIKOWSKI, Tadeusz ,  LOUVEL, Severine ,  KLIMKAIT, Thomas ,  VIDAL, Vincent

IPC分类号： C07H19/073 ,  A61K31/7068 ,  A61P31/18 ,  A61K31/7072

CPC分类号： C07H19/06

摘要： 4'-Ethynylostavudine derivatives according to the invention substituted at 4'-ethynylostavudine 5'-O-position with 12-tetradodecanoyl, 12-bromododecanoyl, 12-methoxydodecanoyl, 12-ethylothiododecanoyl, or 12-azidododecanoyl group (represented by the symbols WA37, WA38, WA40, WA42, WA39 ) in deClPhR™ cells exert very high antiviral activity against the wild type HIV-1 strain, as well as against its drug and multidrug resistant strains, without any citotoxicty at the therapeutic concentrations (CC 50 >200 µM).
These compounds, because of their very low toxicity may be applied at all phases of AIDS, even at the final phase when the T4 lymphocytes level in patients drops down below 200/µL of peripheral blood.
The 2',3'- didehydro-3'-deoxy-4'-ethynylothymidine derivatives, according to the invention, are synthesized by the transformation of the known compound 4'-ethynylostavudine ( WA32, wherein R represents hydrogen).

公开(公告)号：EP2055711B1

公开(公告)日：2011-08-17

申请号：EP09152764.8

申请日：2005-06-23

申请人： Centre National de la Recherche Scientifique ,  Université Paris Sud (Paris 11) ,  Rocco, Flavio

发明人： Rosilio, Véronique ,  Renoir, Jack-Michel ,  Couvreur, Patrick ,  Rocco, Flavio ,  Cattel, Luigi ,  Stella, Barbara

IPC分类号： C07H19/073 ,  A61K31/706

CPC分类号： C07H19/06 ,  A61K47/542 ,  B82Y30/00 ,  C07H19/073 ,  C07H19/16

公开(公告)号：EP2344513A2

公开(公告)日：2011-07-20

申请号：EP09741728.1

申请日：2009-04-08

申请人： Vorbrüggen, Helmut

发明人： Vorbrüggen, Helmut

IPC分类号： C07H19/073 ,  C07D239/47

CPC分类号： C07D239/47 ,  C07H19/073 ,  C07H23/00 ,  Y02P20/55

摘要： The invention relates to methods for producing gemcitabine derivatives of the general formula 6, or gemcitabine hydrochloride 7 (2'-desoxy-2',2'-difluorocytidine hydrochloride), to the silylated cytosine analogs 4c and 4d as intermediate products, and to the use thereof for reactions with 3,5-protected sugars of the general formula 5 into the corresponding protected 2’-desoxycytidines. The subsequent saponification of the protected cytidines removes not only the 3’,5’-O-benzoate protecting groups, but also the N
4 -amidyl group, or the N
4 -guanidyl group, thereby obtaining the desired free cytidines 6. The subsequent treatment of gemcitabine derivatives of the general formula 6 with acids results in 2’-desoxy-2’,2’-difluorocytidine hydrochloride (gemcitabine hydrochloride) 7.

公开(公告)号：EP2303906A1

公开(公告)日：2011-04-06

申请号：EP09763709.4

申请日：2009-06-12

申请人： ScinoPharm Taiwan, Ltd.

发明人： CHEN, Shu-ping ,  SHIEH, Chia-lin

IPC分类号： C07H19/073 ,  A61K31/522

CPC分类号： C07H19/073

摘要： The present application provides several crystalline forms of gemcitabine base and methods of making the same.

公开(公告)号：EP1831238A4

公开(公告)日：2011-04-06

申请号：EP05857267

申请日：2005-12-29

申请人： BERRY & ASSOCIATES INC

发明人： BERRY DAVID A ,  PEARSON WILLIAM H

IPC分类号： C40B40/06 ,  C07B61/00 ,  C07C1/00 ,  C07D207/00 ,  C07F9/06 ,  C07F9/117 ,  C07H19/067 ,  C07H19/073 ,  C07H19/167 ,  C07H19/173 ,  C07H21/00 ,  C07H23/00 ,  G01N33/00

CPC分类号： C07H21/00 ,  C07B63/00 ,  C07B2200/11 ,  C07C245/08 ,  C07F9/2408 ,  C07F9/6561 ,  C07H19/067 ,  C07H19/073 ,  C07H19/167 ,  C07H19/173 ,  C07H21/04 ,  C07H23/00

公开(公告)号：EP2279194A1

公开(公告)日：2011-02-02

申请号：EP09739272.4

申请日：2009-01-16

申请人： Life Technologies

发明人： MENCHEN, Steven, M. ,  ROSENBLUM, Barnett ,  KENNEY, Paul ,  KHAN, Shoeb, I. ,  MA, Zhaochun ,  CHEN, Jer-kang ,  LAM, Joseph ,  HUANG, Boli

IPC分类号： C07H19/073 ,  C07H21/04 ,  C12Q1/68 ,  C07H19/173

CPC分类号： C07H21/04 ,  C07H19/073 ,  C07H19/173 ,  C12Q1/6874 ,  C12Q2523/107 ,  C12Q2525/186 ,  C12Q2525/197

摘要： Nucleotide analogs that can sustain the enzymatic synthesis of double-stranded nucleic acid from a nucleic template are described. The nucleotide analogs include: (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine, uracil and their analogs; (ii) a label attached to the base or analog of the base via a cleavable linker; (iii) a deoxyribose; and (iv) one or more phosphate groups. The linker and/or the label inhibits template directed polymerase incorporation of a further nucleotide substrate onto an extended primer strand. In addition, cleavage of the linker leaves a residue attached to the base which is not present in the natural nucleotide and which does not inhibit extension of the primer strand. The nucleotide analogs can therefore be used as reversible terminators in sequencing by synthesis methods without blocking the 3' hydroxyl group. Methods of sequencing DNA using the substrates are also described.