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1. 发明公开

EP3237015A1 DERIVES HYDROXYBISPHOSPHONIQUES HYDROSOLUBLES DE LA DOXORUBICINE 审中-公开
标题翻译：衍生物羟基二硫代磷酸酯水合物DE LA DOXORUBICINE
公开(公告)号：EP3237015A1
公开(公告)日：2017-11-01
申请号：EP15801727.7
申请日：2015-11-20
申请人： Atlanthera
发明人： EGOROV, Maxim , GOUJON, Jean-Yves , LE BOT, Ronan , DAVID, Emmanuelle
IPC分类号： A61K47/50 , C07F9/38 , C07C335/04 , A61P19/00 , A61P35/00
CPC分类号： A61K31/663 , A61K47/548 , C07C335/40 , C07F9/6552 , C07H15/244
摘要： The invention relates to hydrosoluble hydroxybisphosphonic derivatives of doxorubicin of formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to the use of said compounds as a drug, especially in the treatment of a bone tumour. The invention further relates to the pharmaceutical compositions comprising such compounds, the methods for the synthesis thereof and synthesis intermediates.
摘要翻译：本发明涉及式（I）多柔比星的水溶性羟基双膦酸衍生物及其药学上可接受的盐。本发明还涉及所述化合物作为药物，特别是用于治疗骨肿瘤的用途。本发明进一步涉及包含此类化合物的药物组合物，其合成方法和合成中间体。

2. 发明授权

EP2000150B1 TITANIUM OXIDE COMPLEX PARTICLE, DISPERSION SOLUTION OF THE PARTICLE, AND PROCESS FOR PRODUCTION OF THE PARTICLE 有权
标题翻译：粒子颗粒的TITANOXIDKOMPLEXTEILCHEN分散液和方法
公开(公告)号：EP2000150B1
公开(公告)日：2016-07-13
申请号：EP07739321.3
申请日：2007-03-22
申请人： TOTO LTD.
发明人： KANEHIRA, Koki , SONEZAKI, Shuji , OGAMI, Yumi , NAKAMURA, Tomomi
IPC分类号： A61K41/00 , A61K9/08 , A61K33/24 , A61K47/32 , A61K47/34 , A61K47/36 , A61P35/00 , A61P43/00 , C01G23/047
CPC分类号： A61K47/48861 , A61K9/0009 , A61K9/167 , A61K33/24 , A61K41/0014 , A61K41/0019 , A61K41/0033 , A61K41/0057 , A61K47/54 , A61K47/542 , A61K47/548 , A61K47/58 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/6923 , A61K51/1244 , A61N5/062 , A61N7/00 , A61N2005/0661 , B82Y5/00 , C01G23/047 , C09C1/3676 , Y10T428/2982

3. 发明公开

EP2488208A4 COMPOUNDS HAVING PEPTIDES CONJUGATED TO BONE TARGETING MOIETIES AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译：连接，骨TARGET收缩单位结合肽和方法进行生产及其用途
公开(公告)号：EP2488208A4
公开(公告)日：2015-07-01
申请号：EP10823111
申请日：2010-10-12
申请人： UNIV ALBERTA
发明人： DOSCHAK MICHAEL R , KRISHNA BHANDARI HARI
IPC分类号： A61K47/48 , A61K38/23 , A61P19/08
CPC分类号： A61K47/48 , A61K38/23 , A61K47/50 , A61K47/548
摘要： Described herein are compositions having a peptide sequence that includes at least one bone targeting moiety, wherein the bone targeting moiety is bonded to the peptide sequence by a linker, wherein the peptide sequence is calcitonin, and wherein the composition is neutral or a pharmaceutically acceptable salt or ester thereof. In one aspect, calcitonin inhibits or slows osteoclast mediated resorptive bone loss. The compounds described herein can be used in a number of therapeutic applications including treating or preventing conditions associated with bone loss, which include, but are not limited to, osteoporosis, Paget's disease, osteolytic tumors, Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Osteoarthritis, osteopenia, and hypercalcemia. Also described herein are the methods of making these compositions that prevent or treat conditions associated with bone loss and methods of preventing bone fractures.
摘要翻译：描述中是具有肽序列的组合物确实包括至少一个骨靶向部分，worin骨靶向部分是由左结合到肽序列，worin肽序列是降钙素和worin所述组合物是中性或药学上可接受的盐或酯。在一个方面，降钙素抑制或减缓破骨细胞介导的骨吸收损失。中所述的化合物可以以多种治疗应用，包括治疗或预防与骨损失，这包括相关联的条件下使用，但不限于，骨质疏松症，佩吉特氏病，溶骨性肿瘤，类风湿关节炎，银屑病关节炎，强直性脊柱炎，骨关节炎，骨质疏松和高钙血症。如此描述的是使合成的组合物并预防或治疗与骨损失和预防骨折的方法相关条件的方法。

4. 发明公开

EP2303288A4 CONJUGATES OF A POLYMER, A BISPHOSPHONATE AND AN ANTI-ANGIOGENESIS AGENT AND USES THEREOF IN THE TREATMENT AND MONITORING OF BONE RELATED DISEASES 审中-公开
标题翻译：与骨相关联聚合物，双膦酸盐和抗血管生成的手段和它们的用途在治疗和疾病控制的缀合物
公开(公告)号：EP2303288A4
公开(公告)日：2015-04-22
申请号：EP09750275
申请日：2009-05-21
申请人： UNIV RAMOT
发明人： SATCHI-FAINARO RONIT , MILLER KEREN , SHABAT DORON , EREZ ROTEM
IPC分类号： A61K31/787 , A61K35/00 , A61K35/04 , A61K47/48 , A61K49/00
CPC分类号： A61K47/48084 , A61K9/1676 , A61K31/337 , A61K47/548 , A61K47/58 , A61K47/65 , A61K49/0017 , A61K49/0054 , A61K2800/57 , C07F9/3873 , C07F9/65517 , C07F9/65586 , C07K5/06078 , C07K5/1008
摘要： Conjugates of polymers or copolymers having attached thereto an anti-angiogenesis agent and a bisphosphonate bone targeting agent, and processes of preparing same, are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of bone related disorders are also disclosed.
摘要翻译：其上连接有抗血管生成剂和二膦酸盐骨靶向剂，以及制备相同的工艺的聚合物或共聚物的缀合物，是游离缺失盘。含论文缀合物和在骨相关疾病的治疗及其用途的药物组合物，从而游离缺失盘。

5. 发明公开

EP2859120A2 METHOD FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF LUNG CANCER METASTASIS 有权转让
标题翻译： VERFAHREN ZUR DIAGNOSE，PROGNOSE UND BEHANDLUNG VON LUNGENKREBSMETASTASEN
公开(公告)号：EP2859120A2
公开(公告)日：2015-04-15
申请号：EP13766663.2
申请日：2013-06-06
申请人： Fundació Institut de Recerca Biomèdica (IRB Barcelona) , Institució Catalana de Recerca i Estudis Avançats
发明人： GOMIS, Roger , PLANET, Evarist
IPC分类号： C12Q1/68 , G01N33/574
CPC分类号： C12Q1/6886 , A61K47/548 , C07K16/2875 , C12Q2600/106 , C12Q2600/112 , C12Q2600/118 , C12Q2600/156 , C12Q2600/158 , G01N33/57423 , G01N2333/82 , G01N2800/50 , G01N2800/52
摘要： The present invention relates to a method for the diagnosis or the prognosis of metastasis in lung cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in lung cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the lung cancer.
摘要翻译：本发明涉及一种用于诊断或预后的肺癌转移的方法，包括确定c-MAF基因是否在原发性肿瘤样品中扩增。同样，本发明还涉及用于诊断或预测肺癌转移的方法，以及用于确定相对于其他器官中转移的骨转移倾向的方法，其包括确定c-MAF 基因表达水平。最后，本发明涉及c-MAF抑制剂作为治疗肺癌的治疗靶标的用途。

6. 发明公开

EP2714024A4 ORAL FORMULATIONS OF MITOCHONDRIALLY-TARGETED ANTIOXIDANTS AND THEIR PREPARATION AND USE 有权
标题翻译：口服制剂OFF线粒体靶向抗氧化剂和生产及其用途
公开(公告)号：EP2714024A4
公开(公告)日：2014-12-31
申请号：EP12792111
申请日：2012-06-04
申请人： MITOTECH SA
发明人： SKULACHEV MAXIM V , SKULACHEV VLADIMIR P , ZAMYATNIN ANDREY A , EFREMOV EUGENY S , TASHLITSKY VADIM N , ZINOVKIN ROMAN A , EGOROV MAXIM V , FRIEDHOFF LAWRENCE T , PLETUSHKINA OLGA Y , ANDREEV-ANDRIEVSKY ALEXANDER A , ZINEVICH TATIANA V
IPC分类号： A61K31/122 , A61K9/00 , A61K31/352 , A61K31/4375 , A61K31/66 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/36 , A61P39/06 , C07F9/02 , C07F9/54
CPC分类号： A61K47/48084 , A61K9/0095 , A61K31/047 , A61K31/122 , A61K31/352 , A61K31/4375 , A61K31/66 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/36 , A61K47/545 , A61K47/548 , C07F9/5435 , C07F9/5442 , C07F9/5456
摘要： Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.
摘要翻译：本发明提供了稳定的液体和氧化和还原的固体配方和灰线粒体靶向的抗氧化剂，以及它们的制备和使用方法。

7. 发明公开

EP2187965A4 PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING 有权转让
标题翻译： PSMA-BINDUNGSLIGANDEN-LINKS-KONJUGATE UND ANWENDUNGSVERFAHREN
公开(公告)号：EP2187965A4
公开(公告)日：2014-11-26
申请号：EP08798020
申请日：2008-08-15
申请人： PURDUE RESEARCH FOUNDATION
发明人： LOW PHILIP STEWART , KULARATNE SUMITH A
IPC分类号： A61K39/395 , C12P21/00
CPC分类号： A61K47/64 , A61K31/426 , A61K31/4745 , A61K31/475 , A61K47/48023 , A61K47/48038 , A61K47/48084 , A61K47/54 , A61K47/542 , A61K47/547 , A61K47/548 , A61K49/0041 , A61K49/0043 , A61K49/0052 , A61K49/0056 , A61K51/04 , A61K51/0402 , A61K51/0489 , A61K51/088 , C07C323/52 , C07D207/416 , C07K5/08
摘要： Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
摘要翻译：本文描述了可用于递送治疗剂，诊断剂和成像剂的前列腺特异性膜抗原（PSMA）结合缀合物。本文还描述了含有它们的药物组合物和使用缀合物和组合物的方法。还描述了制备缀合物和含有它们的组合物的方法。

8. 发明公开

EP2678039A1 BISPHOSPHONATE-PRODRUGS 审中-公开
标题翻译：双膦酸盐前药
公开(公告)号：EP2678039A1
公开(公告)日：2014-01-01
申请号：EP12707980.4
申请日：2012-02-24
申请人： KTB Tumorforschungsgesellschaft mbH
发明人： KRATZ, Felix , HOCHDOERFFER, Katrin
IPC分类号： A61K47/48 , A61P35/00 , A61P19/08
CPC分类号： A61K47/48084 , A61K31/35 , A61K31/40 , A61K31/704 , A61K38/00 , A61K47/548 , A61K47/65 , C07D405/00 , C07H15/252 , C07K5/06026 , C07K5/06052 , C07K5/06139
摘要： The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

9. 发明公开

EP2585066A2 PRODRUGS OF NH-ACIDIC COMPOUNDS: ESTER, CARBONATE, CARBAMATE AND PHOSPHONATE DERIVATIVES 有权
标题翻译： PRODRUGS AUS NH-SÄUREVERBINDUNGEN：ESTER-，CARBONAT-，CARBAMAT- UND PHOSPHONAT-DERIVATE
公开(公告)号：EP2585066A2
公开(公告)日：2013-05-01
申请号：EP11798995.4
申请日：2011-06-24
申请人： Alkermes Pharma Ireland Limited
发明人： BLUMBERG, Laura, Cook , REMENAR, Julius, F. , ALMARRSON, Orn , ZEIDAN, Tarek, A.
IPC分类号： A61K31/496 , C07D401/12
CPC分类号： A61K31/454 , A61K31/496 , A61K47/54 , A61K47/545 , A61K47/548 , C07D215/227
摘要： The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

10. 发明公开

EP2576575A1 PROSTAGLANDIN-BISPHOSPHONATE CONJUGATE COMPOUNDS, METHODS OF MAKING SAME, AND USES THEREOF 有权
标题翻译：前列腺素双膦酸酯缀合物的化合物，PROCESS FOR THEREOF AND USE PRODUCING
公开(公告)号：EP2576575A1
公开(公告)日：2013-04-10
申请号：EP11785955.3
申请日：2011-05-30
申请人： Simon Fraser University
发明人： YOUNG, Robert N. , ARNS, Stephen , MOREAU, Anne , MORSHED, Monzur , GIBE, Romelo
IPC分类号： C07F9/6558 , A61K31/675 , A61K47/48 , A61P19/08 , C07F9/547
CPC分类号： C07F9/572 , A61K47/548 , C07F9/3873 , C07F9/59 , C07F9/6512 , C07F9/65583
摘要： The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.

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