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1. 发明申请

WO2008083729A1 RADIOLABELLING VIA FLUORINATION OF AZIRIDINES 审中-公开
标题翻译：通过氟化钠的放射性辐射
公开(公告)号：WO2008083729A1
公开(公告)日：2008-07-17
申请号：PCT/EP2007/007968
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , SRINIVASAN, Ananth , BRUMBY, Thomas , STELLFELD, Timo , GRAHAM, Keith , VOIGTMANN, Ulrike , BECAUD, Jessica , MU, Linjing
发明人： SRINIVASAN, Ananth , BRUMBY, Thomas , STELLFELD, Timo , GRAHAM, Keith , VOIGTMANN, Ulrike , BECAUD, Jessica , MU, Linjing
IPC分类号： C07C311/19 , C07D203/08 , C07D203/24 , C07D207/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D487/04 , C07D487/22 , C07D491/04 , C07K7/02
CPC分类号： C07C311/19 , C07B59/001 , C07B2200/05 , C07D203/08 , C07D203/24 , C07D207/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D487/04 , C07D487/22 , C07D491/04 , C07K5/06191 , C07K7/02
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging.
摘要翻译：本发明涉及适用于或已经用<！ - SIPO - >已经放射性标记的新化合物，制备这些化合物的方法和用于诊断成像的这些化合物的用途。

2. 发明申请

WO2008040441A3 SILICON DERIVATIVES FOR PET IMAGING 审中-公开
公开(公告)号：WO2008040441A3
公开(公告)日：2008-04-10
申请号：PCT/EP2007/008044
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , SRINIVASAN, Ananth , LEHMANN, Lutz , VOIGTMANN, Ulrike , STELLFELD, Timo , AMETAMEY, Simon , KLAR, Ulrich , HÖHNE, Aileen , MU, Linjing
发明人： SRINIVASAN, Ananth , LEHMANN, Lutz , VOIGTMANN, Ulrike , STELLFELD, Timo , AMETAMEY, Simon , KLAR, Ulrich , HÖHNE, Aileen , MU, Linjing
IPC分类号： C07K1/13 , C07F7/02 , A61K51/08 , A61K51/04 , C07B59/00 , A61K31/695
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled vompounds are characerized by Formula II, wherein the moieties F, R 1 , R 2 , B 1,2, Y 1.2 ,, Z 1.2 and E have the meaning as defined in the specification and claims.

3. 发明申请

WO2008028688A2 COMPOUNDS AND METHODS FOR 18F LABELED AGENTS 审中-公开
标题翻译： 18F标签代理的化合物和方法
公开(公告)号：WO2008028688A2
公开(公告)日：2008-03-13
申请号：PCT/EP2007/008042
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , LEHMANN, Lutz , SRINIVASAN, Ananth , BRUMBY, Thomas , SÜLZLE, Detlef , STELLFELD, Timo , GRAHAM, Keith , KARRAMKAM, Mylène , AMETAMEY, Simon
发明人： LEHMANN, Lutz , SRINIVASAN, Ananth , BRUMBY, Thomas , SÜLZLE, Detlef , STELLFELD, Timo , GRAHAM, Keith , KARRAMKAM, Mylène , AMETAMEY, Simon
IPC分类号： A61K51/08 , C07K7/06 , A61K51/04 , C07C255/58
CPC分类号： C07K14/6555 , A61K51/088 , C07K14/57545
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characterized by Formula II, wherein the substituents G, Q, L, Y and U have the meaning as defined in the specification and claims.
摘要翻译：本发明涉及适用于或已经用<！ - SIPO - >已经放射性标记的新化合物，制备这些化合物的方法和用于诊断成像的这些化合物的用途。这些标记的化合物由式II表征，其中取代基G，Q，L，Y和U具有如说明书和权利要求书中所定义的含义。

4. 发明申请

WO2008104203A3 18F FLUORO-BENZOYL LABELLED BIOLOGICAL ACTIVE COUMPOUNDS AS DIAGNOSITIC IMAGING AGENTS AS WELL AS BENZOTRIAZOL-1-YLOXY-BENZOYL, 2,5-DIOXO-PYRROLIDIN-1-YLOXY) BENZOYL AND TRIMETHYLAMMONIO-BENZOYL PRECURSERS 审中-公开
公开(公告)号：WO2008104203A3
公开(公告)日：2008-09-04
申请号：PCT/EP2007/007967
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , SRINIVASAN, Ananth , STELLFELD, Timo
发明人： SRINIVASAN, Ananth , STELLFELD, Timo
IPC分类号： A61K49/04 , A61K49/08 , A61K49/10 , A61K51/04 , C07D249/18 , C07D405/14 , C07D405/04 , C07D409/04 , A61K31/7072 , A61K38/08 , C07K7/06 , C07K1/13 , C07K5/023 , C07K5/02
摘要： The present invention relates to radiolabelled substitute benzene compounds for diagnostic imaging. The present invention provides methods for preparation of such compounds, in particular, preparation of novel compounds which serve as precursors for 18 F-labeling, and the use of thus 18 F-labe!ed compounds for diagnostic imaging. Formula (A), wherein one of -Y 1 , -Y 2 , -Y 3 Y 4 and -Y 5 is -A-B-D-P, wherein -A-B-D- is a bond or spacer, P is peptide, peptidomimetic, oligonucleotide or small molecule. K is LG-O or W, wherein: LG- is selected from the group comprising Formula (B), wherein T is H or Cl, Q is CH or N, K is absent or is C=O. W is radioactive or non-radioactive isotope of fluorine, more preferably 18 F.

5. 发明申请

WO2009127372A1 PURIFICATION STRATEGY FOR DIRECT NUCLEOPHILIC PROCEDURES 审中-公开
标题翻译：直接核子程序的纯化策略
公开(公告)号：WO2009127372A1
公开(公告)日：2009-10-22
申请号：PCT/EP2009/002674
申请日：2009-04-09
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , CYR, John , SRINIVASAN, Ananth , BERNDT, Mathias , GRAHAM, Keith , CHI, Dae, Yoon , LEE, Byoung, Se , CHU, So, Young , LIM, Song-Yi , LEE, Sang, Ju , RYU, Jin-Sook , OH, Seung, Jun
发明人： CYR, John , SRINIVASAN, Ananth , BERNDT, Mathias , GRAHAM, Keith , CHI, Dae, Yoon , LEE, Byoung, Se , CHU, So, Young , LIM, Song-Yi , LEE, Sang, Ju , RYU, Jin-Sook , OH, Seung, Jun
IPC分类号： C07B59/00 , C07B63/02
CPC分类号： C07B63/02 , C07B59/00 , C07B59/001 , C07B2200/11
摘要： The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and time-saving way to purify the desired product S-X from non-reacted precursors S-L-M and by-products L-M.
摘要翻译：本发明提供了制备和纯化化合物如药物的新颖且有利的方法。该方法包括与部分X的亲核取代反应，其中反应中的底物S的离去基团L共价连接到纯化部分M.该概念提供了一种方便和省时的方法，以从非极性纯化所需产物SX - 前体SLM和副产物LM。

6. 发明申请

WO2010000409A2 COMPOUNDS AND PROCESSES FOR PRODUCTION OF RADIOPHARMACEUTICALS 审中-公开
标题翻译：化合物和生产无机物的方法
公开(公告)号：WO2010000409A2
公开(公告)日：2010-01-07
申请号：PCT/EP2009/004537
申请日：2009-06-24
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , SRINIVASAN, Ananth , BERNDT, Mathias , GRAHAM, Keith , FRIEBE, Matthias , SCHMITT-WILLICH, Heribert
发明人： SRINIVASAN, Ananth , BERNDT, Mathias , GRAHAM, Keith , FRIEBE, Matthias , SCHMITT-WILLICH, Heribert
IPC分类号： C07B59/00 , C07C309/65 , C07C309/73 , C07C309/80 , C07C309/86
CPC分类号： C07B59/00 , C07B2200/05 , C07C309/65 , C07C309/73
摘要： The present invention relates to novel perfluorinated precursors for the production of F- 18 labeled radiotracers for Positron Emission Tomography (PET) and processes for radiolabeling and purification using these precursors. The invention also comprises radiopharmaceutical kits using these precursors and processes.
摘要翻译：本发明涉及用于生产用于正电子发射断层扫描（PET）的F-18标记放射性示踪剂的新型全氟化前体和使用这些前体进行放射性标记和纯化的方法。本发明还包括使用这些前体和方法的放射性药物试剂盒。

7. 发明申请

WO2008028530A1 COMPOUNDS AS APTAMER-DIMERS AND THEIR USES IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译：化合物作为APTAMER-DIMERS及其在诊断和治疗中的用途
公开(公告)号：WO2008028530A1
公开(公告)日：2008-03-13
申请号：PCT/EP2007/005875
申请日：2007-07-03
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , FRIEBE, Matthias , STEPHENS, Andrew , SRINIVASAN, Ananth , HECHT, Maren
发明人： FRIEBE, Matthias , STEPHENS, Andrew , SRINIVASAN, Ananth , HECHT, Maren
IPC分类号： C07K7/00 , C07K14/00 , A61K38/04 , A61K38/16 , A61K47/48
CPC分类号： C07K14/001 , A61K38/00 , A61K47/65 , A61K51/088 , C07K7/02
摘要： The object of the present invention is solved by compositions of peptide linkers and their use for synthesis and annealing of aptamer oligonucleotides in form of dimers. The present invention in particularly provides said compositions for the use as a diagnostic and/or therapeutic agent. In another preferred embodiment the present invention relates to a kit for preparing a radio pharmaceutical preparation, said kit comprising a vial comprising a quantity of the compound according to the invention. A further preferred embodiment of the present invention relates to methods of producing said compounds, comprising synthesis of said compound in an automated peptide synthesizer. In another preferred embodiment the present invention concerns the use of said compounds according to the present invention for the manufacture of a medicament, preferably for diagnosis or therapy of proliferative diseases. In a further preferred embodiment the present invention concerns methods for treating or diagnosing patients administering or utilizing the compounds according to the present invention.
摘要翻译：本发明的目的通过肽接头的组合物及其用于以二聚体的形式合成和退火适体寡核苷酸的用途来解决。本发明特别提供了用作诊断和/或治疗剂的所述组合物。在另一个优选的实施方案中，本发明涉及用于制备放射性药物制剂的试剂盒，所述试剂盒包含一定量的包含本发明化合物的小瓶。本发明的另一优选实施方案涉及产生所述化合物的方法，包括在自动肽合成仪中合成所述化合物。在另一个优选的实施方案中，本发明涉及根据本发明的所述化合物在制备药物中的用途，优选用于诊断或治疗增殖性疾病。在另一优选实施方案中，本发明涉及用于治疗或诊断施用或使用本发明化合物的患者的方法。

8. 发明申请

WO2008049644A1 THYMIDINE ANALOGS FOR IMAGING 审中-公开
标题翻译：用于成像的THYMIDINE模拟
公开(公告)号：WO2008049644A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/009408
申请日：2007-10-24
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
发明人： SRINIVASAN, Ananth , VOIGTMANN, Ulrike , BERNDT, Mathias , GRAHAM, Keith , ZITZMANN, Sabine , LEHMANN, Lutz , FITZNER, Ansgar
IPC分类号： A61K49/08 , A61K49/10 , C07H19/06 , A61K51/04 , A61P35/00 , A61K31/7064
CPC分类号： C07H19/06 , A61K47/60 , A61K51/0491
摘要： The present invention relates to nucleoside analogues and more particularly to labeled nucleoside analogues. It has been found new thymidine analogues can be stably labeled with a detectable label moiety. Further the present invention relates to methods of making above compounds and use of such compounds for diagnostic imaging of tumor cells and / or treatment of proliferative diseases. In addition, the present invention relates to the preparation and use of positron emitting compounds for positron emission tomography (PET). A kit is also disclosed.
摘要翻译：本发明涉及核苷类似物，更具体地涉及标记的核苷类似物。已经发现新的胸苷类似物可以用可检测的标记部分稳定地标记。此外，本发明涉及制备上述化合物的方法以及这些化合物用于肿瘤细胞诊断成像和/或治疗增殖性疾病的方法。此外，本发明涉及用于正电子发射断层摄影（PET）的正电子发射化合物的制备和应用。还披露了一个套件。

9. 发明申请

WO2007039318A2 NEUROPEPTIDE Y ANALOGS 审中-公开
标题翻译：神经元Y模拟
公开(公告)号：WO2007039318A2
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009812
申请日：2006-10-05
申请人： SCHERING AKTIENGESELLSCHAFT , SRINIVASAN, Ananth
发明人： SRINIVASAN, Ananth
IPC分类号： C07K14/575 , G01N33/68 , A61K38/22
CPC分类号： C07K14/57545
摘要： The neuropeptideY(NPY)-receptor-subtype Y 1 is expressed differentially from breast tumor cells and is therefore an advantageous target molecule for the molecular imaging of breast cancer. Peptide analogs were synthesized, whose sequence is reduced to the receptor-binding sections of the natural ligand NPY. These Y 1 receptor-selective peptide analogs contain unnatural amino acids that increase the receptor affinity and are to ensure the stability of the greatly shortened peptide. New NPY analogs, which are to be used as radioligands, were tested for their binding affinity and selectivity for the Y 1 receptor. To this end, in-vitro binding tests with Y 1 - or Y 2 receptor-expressing cell lines were established and optimized. Then, the binding affinities of the NPY analogs were determined. In this case, a peptide (P2489) was identified, whose highest binding affinity was determined with a K i of 42.8 nmol of Y 1 receptor-expressing SK-N-MC cells and whose selectivity for the Y 1 receptor could be detected by the fact that there is no binding toY 2 receptor-expressing MHH-NB-11 cells. As an additional NPY analog, peptide fW7 contained the unnatural amino acid ?-aminocyclopropanecarboxylic acid on positions 32 and 34, by which the binding to the Y 1 receptor was influenced in a positive manner. A direct coupling of the chelating agent DOTA, which is necessary for the radiometal labeling of the peptides, to the N-terminal end of the peptides resulted in the loss of the binding affinity. By indirect coupling of the DOTA to the peptide fW7 via a spacer, this loss could be reduced, and fW7(DOTA) had a high binding affinity (K i = 62.8 nmol) similar to P2489.
摘要翻译：神经肽Y（NPY） - 受体亚型Y 1'与乳腺肿瘤细胞差异表达，因此是乳腺癌分子成像的有利靶分子。合成肽类似物，其序列被还原成天然配体NPY的受体结合部分。这些Y 1受体选择性肽类似物含有增加受体亲和力的非天然氨基酸，并确保大大缩短的肽的稳定性。测试其用作放射性配体的新NPY类似物对Y 1受体的结合亲和力和选择性。为此，建立并优化了与Y 1 - 或Y 2受体表达细胞系的体外结合试验。然后，确定了NPY类似物的结合亲和力。在这种情况下，鉴定出肽（P2489），其最高结合亲和力用42.8nmol的表达Y 1 / L受体的SK-N-MC的K < 可以通过不存在与表达Y 2受体的MHH-NB-11细胞结合的事实来检测细胞并且其对Y 1受体的选择性。作为另外的NPY类似物，肽fW7在位置32和34上含有非天然氨基酸的α-氨基环丙烷羧酸，通过它们与Y 1受体的结合受到积极的影响。将肽的放射性金属标记所必需的螯合剂DOTA与肽的N-末端的直接偶联导致结合亲和力的丧失。通过经由间隔物将DOTA与肽fW7间接偶联，可以降低该损失，并且fW7（DOTA）具有与P2489类似的高结合亲和力（KIII = 62.8nmol）。

10. 发明申请

WO2012129029A4 MULTIPLE LINER HANGER ASSEMBLY 审中-公开
公开(公告)号：WO2012129029A4
公开(公告)日：2012-09-27
申请号：PCT/US2012/029075
申请日：2012-03-14
申请人： BAKER HUGHES INCORPORATED , SRINIVASAN, Ananth , HARRIS, Alex, D. , TALBOT, Todd, J.
发明人： SRINIVASAN, Ananth , HARRIS, Alex, D. , TALBOT, Todd, J.
IPC分类号： E21B43/08 , E21B11/02 , E21B23/00
摘要： A hanger assembly provided for multiple hanging opportunities. If liner is being run and the primary hanger doesn't work then a backup hanger is available to set near the nonfunctional primary hanger. In drilling with casing applications when there is a steering equipment malfunction or an MWD breakdown or bit wear requiring the BHA to be pulled, the liner can be hung where it is and the BHA pulled. Upon running back in with the BHA on a running tool the initial hanger can be released and the running tool configured to only set a different hanger when the total depth is reached in drilling with the liner. The running tool is then retrieved and the completion can go on.

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