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31. 发明申请

WO1987001289A1 BONE-SEEKING COMPLEXES OF TECHNETIUM-99m 审中-公开
标题翻译：骨科 - 99m技术复合物
公开(公告)号：WO1987001289A1
公开(公告)日：1987-03-12
申请号：PCT/GB1986000510
申请日：1986-08-28
申请人： AMERSHAM INTERNATIONAL PLC , KELLY, James, Duncan , GRIFFITHS, David, Vaughan
发明人： AMERSHAM INTERNATIONAL PLC
IPC分类号： A61K49/02
CPC分类号： A61K51/0478 , A61K51/0489 , A61K2123/00 , C07F9/3869 , C07F9/3873
摘要： A composition for use in the preparation of a bone-scanning agent comprises a mixture of a bis-phosphonic acid of formula (I), wherein R is H and R is -COOH or formula (II), or R is -NMe2 and R is -CH2OH, or a non-toxic salt thereof, with a reducing agent for pertechnetate. Technetium-99m, as an aqueous solution of pertechnetate ions, is added to the composition to form a complexe of Tc-99m and the bis-phosphonate. The complex is useful as a bone-scanning agent and is rapidly taken up in bone to give scans of high definition.
摘要翻译：用于制备骨扫描剂的组合物包含式（I）的双膦酸的混合物，其中R 1为H且R 2为-COOH或式（II），或 R 1是-NMe 2，R 2是-CH 2 OH，或其无毒盐，和高锝酸盐的还原剂。将锝-99m作为高锝酸盐离子的水溶液加入到组合物中以形成Tc-99m和双膦酸盐的络合物。该复合物作为骨扫描剂是有用的，并且被快速地吸收在骨中以给出高清晰度的扫描。

32. 发明申请

WO2016199111A1 AMIDE-LINKED EP4 AGONIST-BISPHOSPHONATE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：酰胺连接的EP4激发剂 - 二磷酸酯化合物及其用途
公开(公告)号：WO2016199111A1
公开(公告)日：2016-12-15
申请号：PCT/IB2016/053482
申请日：2016-06-13
申请人： SIMON FRASER UNIVERSITY
发明人： THÉVENIN, Marion , YOUNG, Robert N. , CHEN, Gang
IPC分类号： C07F9/572 , A61K47/48 , A61P19/08
CPC分类号： C07F9/5727 , A61K47/548 , A61P19/08 , C07F9/3873
摘要： The present invention relates to EP4 agonist-bisphosphonate conjugates or related compounds and uses thereof. Said conjugates or related compounds may be used to provide delivery of an EP4 agonist or related compound to a desired site of action, such as a bone. Bisphosphonate moieties, linked to the EP4 agonists via amide linkers, have been implicated in the inhibition of bone resorption and bone targeting.
摘要翻译：本发明涉及EP4激动剂 - 双膦酸盐缀合物或相关化合物及其用途。所述缀合物或相关化合物可以用于将EP4激动剂或相关化合物递送至期望的作用位点，例如骨。通过酰胺接头与EP4激动剂连接的双膦酸酯部分已经涉及抑制骨吸收和骨靶向。

33. 发明申请

WO2016094897A1 COMPOSITIONS AND METHODS RELATING TO THE TREATMENT OF CANCER, AUTOIMMUNE DISEASE, AND NEURODEGENERATIVE DISEASE 审中-公开
标题翻译：与治疗癌症，自身免疫性疾病和神经病变疾病相关的组合物和方法
公开(公告)号：WO2016094897A1
公开(公告)日：2016-06-16
申请号：PCT/US2015/065487
申请日：2015-12-14
申请人： THE JACKSON LABORATORY
发明人： MILLS, Kevin David , HASHAM, Muneer Gulamhusein
IPC分类号： A61K31/145 , C07C307/10 , C07C311/08
CPC分类号： C07C335/20 , C07C307/10 , C07C311/08 , C07C311/39 , C07C311/47 , C07C335/16 , C07C335/22 , C07D205/04 , C07D295/26 , C07F9/12 , C07F9/3873
摘要： Described herein are methods and compositions relating to the treatment of e.g., cancer, autoimmune disease, immune deficiency, and/or neurodegenerative disease. In some embodiments, the methods of treatment relate to administering a compound as described herein. In some embodiments, the subject treated according to the methods described herein is a subject determined to have an increased level of DNA damage.
摘要翻译：本文描述了与例如癌症，自身免疫疾病，免疫缺陷和/或神经变性疾病的治疗有关的方法和组合物。在一些实施方案中，治疗方法涉及施用如本文所述的化合物。在一些实施方案中，根据本文所述方法治疗的受试者被确定为具有增加的DNA损伤水平。

34. 发明申请

WO2015144282A1 ANORGANISCH-ORGANISCHE HYBRIDVERBINDUNG 审中-公开
标题翻译：无机复合有机化合物
公开(公告)号：WO2015144282A1
公开(公告)日：2015-10-01
申请号：PCT/EP2015/000454
申请日：2015-02-26
申请人： KARLSRUHER INSTITUT FÜR TECHNOLOGIE , MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFT E.V. , GEORG-AUGUST-UNIVERSITÄT GÖTTINGEN - STIFTUNG ÖFFENTLICHEN RECHTS UNIVERSITÄTSMEDIZIN
发明人： HECK, Joachim , POSS, Marieke , REICHARDT, Holger , NAPP, Joanna , ALVES, Frauke , STÜHMER, Walter , FELDMANN, Claus
IPC分类号： C07F7/00 , C07F9/58 , C07F9/6503 , C07F9/6506 , C07F9/6509 , C07F9/6533 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07F9/6574 , C07C309/47 , C07C309/50 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/12 , C07D413/04 , C07H19/00 , C07D417/10 , C07D417/12 , C07C237/26 , C07D493/10 , C07F5/06 , C07F9/09 , C07F9/117 , C07F9/12 , C07F9/30 , C07F9/38
CPC分类号： A61K49/0041 , A61K31/185 , A61K31/427 , A61K31/519 , A61K31/546 , A61K31/569 , A61K31/65 , A61K31/661 , A61K31/6615 , A61K31/662 , A61K31/663 , A61K31/665 , A61K31/675 , A61K31/683 , A61K31/7008 , A61K31/704 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K38/12 , A61K47/02 , A61K49/0021 , A61K49/0032 , A61K49/0034 , A61K49/0036 , C07C237/26 , C07C309/47 , C07C2603/46 , C07D251/50 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/12 , C07D413/04 , C07D417/10 , C07D417/12 , C07D493/10 , C07F5/069 , C07F7/006 , C07F9/091 , C07F9/117 , C07F9/12 , C07F9/301 , C07F9/3813 , C07F9/3873 , C07F9/582 , C07F9/65033 , C07F9/65061 , C07F9/650958 , C07F9/65335 , C07F9/65505 , C07F9/65515 , C07F9/65517 , C07F9/65522 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65744 , C07F9/65746 , C07J1/0033 , C07J51/00 , C09B1/02 , C09B1/52 , C09B11/08 , C09B19/00 , C09B23/06 , C09B23/086 , C09B29/16 , C09B31/072 , C09B31/08 , C09B35/023 , C09B55/006 , C09B55/009 , C09B57/00 , C09B57/02 , C09B57/08 , C09B62/085 , C09B63/005 , Y02A50/411
摘要： Die vorliegende Erfindung betrifft eine anorganisch-organische Hybridverbindung als lonenverbindung, aufgebaut aus einem anorganischen Kation und einem organischen Wirkstoffanion sowie gegebenenfalls einem organischen Fluoreszenzfarbstoffanion.
摘要翻译：本发明涉及一种有机 - 无机混合化合物作为无机阳离子组成的离子性化合物和有机Wirkstoffanion和任选的有机Fluoreszenzfarbstoffanion。

35. 发明申请

WO2015120531A1 PHOSPHONATE FUNCTIONAL ANTIMICROBIAL COATINGS FOR METAL SURFACES 审中-公开
标题翻译：用于金属表面的磷酸盐功能抗微生物涂料
公开(公告)号：WO2015120531A1
公开(公告)日：2015-08-20
申请号：PCT/CA2014/050796
申请日：2014-08-20
申请人： NANO SAFE COATINGS INCORPORATED , FOUCHER, Daniel
发明人： FOUCHER, Daniel , POROSA, Lukasz , WOLFAARDT, Gideon
IPC分类号： C07F9/40 , A01N57/18 , A01P1/00 , A61L2/16 , A61L2/232 , C07F9/38 , C09D5/14
CPC分类号： A01N57/20 , A01N57/12 , B05D3/0272 , C07F9/3808 , C07F9/3817 , C07F9/3873 , C07F9/4006 , C07F9/4009 , C07F9/5728 , C07F9/6552 , C09D5/14 , C09D5/1625 , A01N33/12
摘要： The present invention relates to antimicrobial compositions containing mono-, bis-, tri- or tetra- phosphonate quaternary ammonium compounds and surfaces coated with such compositions which demonstrate antimicrobial activity against a variety of gram positive and gram negative bacteria including, but not limited to, Staphylococcus , Pseudomonas,Klebsiella, Salmonella, Listeria, Arthrobacte r and Escherichia .
摘要翻译：本发明涉及含有单 - ，双 - ，三 - 或四 - 膦酸季铵化合物的抗微生物组合物和涂覆有这些组合物的表面，其显示针对各种革兰氏阳性和革兰氏阴性菌的抗微生物活性，包括但不限于，葡萄球菌属，假单胞菌属，克雷伯菌属，沙门氏菌属，利斯特氏菌属，节杆菌属和大肠杆菌属。

36. 发明申请

WO2008128056A1 BISPHOSPHONATE COMPOUNDS AND METHODS WITH ENHANCED POTENCY FOR MULTIPLE TARGETS INCLUDING FPPS, GGPPS, AND DPPS 审中-公开
标题翻译：双膦酸盐化合物和具有增强靶点的方法，包括FPPS，GGPPS和DPPS
公开(公告)号：WO2008128056A1
公开(公告)日：2008-10-23
申请号：PCT/US2008/060051
申请日：2008-04-11
申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS , OLDFIELD, Eric , ZHANG, Yonghui
发明人： OLDFIELD, Eric , ZHANG, Yonghui
IPC分类号： C07F9/576 , C07F9/6503
CPC分类号： C07F9/3865 , C07F9/386 , C07F9/3873 , C07F9/5414 , C07F9/581 , C07F9/587 , C07F9/65061 , C07F9/65517 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/723 , G01N33/5011
摘要： The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.
摘要翻译：本公开尤其提供了新的双膦酸盐化合物以及制备和使用这些化合物的方法。在某些实施方案中，本发明的化合物包括能够选择性抑制法呢基二磷酸合成酶（FPPS），香叶基香叶基二磷酸合成酶（GGPPS）和癸酰焦磷酸合酶（DPPS）中的一种或多种的双膦酸盐。在优选的实施方案中，本发明的化合物能够选择性地抑制FPPS，GGPPS和DPPS中的两种或更多种。在实施方案中，本发明的化合物和方法表现出优异的活性水平，例如在抗癌情境，免疫刺激背景和其他情况下，其在若干情况下超过前一代二膦酸药物的活性水平达数量级。在实施方案中，本发明提供了与研究和治疗应用相关的化合物和方法，例如用于肿瘤或癌细胞生长抑制，Gammadelta T细胞的活化，与甲羟戊酸代谢途径相关的某些酶的抑制，骨吸收疾病，癌症，免疫疾病，免疫治疗和传染病。

37. 发明申请

WO2008035367B1 PROCESS FOR THE SYNTHESIS OF IBANDRONATE SODIUM 审中-公开
标题翻译：用于合成IBANDRONATE SODIUM的方法
公开(公告)号：WO2008035367B1
公开(公告)日：2008-08-07
申请号：PCT/IN2007000255
申请日：2007-06-22
申请人： CIPLA LTD , RAO DHARAMARAJ RAMCHANDRA , KANKAN RAJENDRA NARAYANRAO , GHAGARE MARUTI GANPATI
发明人： RAO DHARAMARAJ RAMCHANDRA , KANKAN RAJENDRA NARAYANRAO , GHAGARE MARUTI GANPATI
IPC分类号： C07F9/38
CPC分类号： C07F9/3873
摘要： The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N- (methylpentyl) amino] propionic acid (III).
摘要翻译：本发明涉及合成式（I）的伊班膦酸钠的改进方法。本发明还提供了合成3- [N-（甲基戊基）氨基]丙酸（III）的新方法。

38. 发明申请

WO2008070960A1 IBANDRONATE SODIUM PROPYLENE GLYCOL SOLVATE AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译： IBANDRONATE SODIUM丙烯甘油溶剂及其制备方法
公开(公告)号：WO2008070960A1
公开(公告)日：2008-06-19
申请号：PCT/CA2007/002093
申请日：2007-11-21
申请人： APOTEX PHARMACHEM INC. , REY, Allan, W. , STRADIOTTO, David, A. , DATTA, Probal, Kanti , TRAYNOR, Krista, Lyn , McPHAIL, Cameron, L.
发明人： REY, Allan, W. , STRADIOTTO, David, A. , DATTA, Probal, Kanti , TRAYNOR, Krista, Lyn , McPHAIL, Cameron, L.
IPC分类号： C07F9/38 , A61P19/10 , A61K31/663
CPC分类号： C07F9/3873 , A61K31/663
摘要： Ibandronate sodium and propylene glycol readily forms a free-flowing crystalline solvate. The novel solvate is non-hygroscopic, free-flowing, chemically and polymorphically stable, and easily dried even on industrial scale. Thus, it is particularly suitable for pharmaceutical applications. A process for preparing said novel solvate is further disclosed. Formula (I).
摘要翻译：伊班膦酸钠和丙二醇容易形成自由流动的结晶溶剂合物。新型溶剂化物是非吸湿性，自由流动性，化学性和多晶型稳定性，即使在工业规模上也容易干燥。因此，它特别适用于药物应用。进一步公开了制备所述新型溶剂合物的方法。式（I）。

39. 发明申请

WO2008017339A1 α-AMINO ACID PHOSPHONIC ACID COMPOUNDS, METHOD OF PREPARATION AND USE THEREOF 审中-公开
标题翻译： α-氨基酸磷酸化合物，其制备方法及其用途
公开(公告)号：WO2008017339A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/004683
申请日：2007-05-25
申请人： THERMPHOS TRADING GMBH , NOTTE, Patrick , DEVAUX, Albert, Firmin
发明人： NOTTE, Patrick , DEVAUX, Albert, Firmin
IPC分类号： C07F9/38 , C07F9/6506 , C02F5/14
CPC分类号： C02F5/14 , C02F5/12 , C02F2103/10 , C07F9/3873 , C07F9/65067
摘要： Novel aminoacid alkylphosphonic acid compounds are disclosed. These compounds can be used in multiple applications, in particular in a scale inhibitor functionality in aqueous systems, including in marine oil recovery.
摘要翻译：公开了新的氨基酸烷基膦酸化合物。这些化合物可以在多种应用中使用，特别是在含水体系中的阻垢剂官能度中，包括在海水中回收。

40. 发明申请

WO2007013097A8 IMPROVED PROCESS FOR THE PREPARATION OF IBANDRONATE SODIUM 审中-公开
标题翻译：改进IBANDRONATE SODIUM的制备方法
公开(公告)号：WO2007013097A8
公开(公告)日：2007-12-06
申请号：PCT/IN2006000251
申请日：2006-07-17
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , USHARANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , USHARANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07F9/38
CPC分类号： C07F9/3873
摘要： Present invention discloses an improved and commercial process for the preparation of ibandronic acid or its monosodium salt. According to the process 3-N-methylaminopropionitrile is reacted with n-pentylbromide to get the tertiary amine of formula-II. Hydrolysis of the nitrile compound of formula-II with hydrochloric acid gave the b-alanine derivative of formula-X. Bis-phosphonylation of the acid compound of formula-X with phorphorous trichloride and phosphorous acid, followed by water hydrolysis gave aqueous ibandronic acid. Treatment of this with sodium hydroxide, followed by dilution of the aqueous solution with methanol gave ibandronate monosodium of formula-Ia as white crystalline solid. Present process utilizes simple raw materials and avoids the column chromatography technique used in the prior art process for isolation of ibandronic acid. Overall yield of ibandronate is more than 60% from the nitrile intermediate of formula-II. Ibandronate is widely used as bone resorption inhibitor.
摘要翻译：本发明公开了用于制备伊班膦酸或其单钠盐的改进和商业化方法。根据方法，将3-N-甲基氨基丙腈与正戊基溴反应得到式II的叔胺。用盐酸水解式II的腈化合物得到式-X的β-丙氨酸衍生物。将式-X的酸化合物与无色三氯化磷和亚磷酸二膦酰化，随后进行水解，得到伊班膦酸水溶液。用氢氧化钠处理，然后用甲醇稀释水溶液，得到式Ia的伊班膦酸钠单钠为白色结晶固体。本发明方法使用简单的原料，并避免了用于分离伊班膦酸的现有技术方法中使用的柱色谱技术。伊班膦酸钠的总收率高于式Ⅱ的腈中间体的60％以上。伊班膦酸盐被广泛用作骨吸收抑制剂。

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