专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明公开

EP0079125A1 3-Substituted spectinomycin analogues and their preparation 失效
标题翻译： 3-Substituierte Spectinomycin-Analoge und ihre Herstellung。
公开(公告)号：EP0079125A1
公开(公告)日：1983-05-18
申请号：EP82305299.8
申请日：1982-10-05
申请人： THE UPJOHN COMPANY
发明人： Thomas, Richard Charles , Fritzen, Edward Lawrence
IPC分类号： C07D493/04 , C07H15/22 , C07D309/32
CPC分类号： C07H15/224
摘要： Novel C-3' analogues of spectinomycin and C-6' analogues thereof, including novel 3'-diazo-secospectinomycin compounds, can have antimicrobial properties.
摘要翻译：奇异霉素和C-6分子类似物的新型C-3分子类似物，包括新的3分钟 - 重氮 - 次视谱霉素化合物，可以具有抗微生物特性。

42. 发明公开

EP0044477A2 Process for production of antibiotics, and novel antibiotics produced thereby 失效
标题翻译：一种生产抗生素，和由此产生的抗生素处理。
公开(公告)号：EP0044477A2
公开(公告)日：1982-01-27
申请号：EP81105357.8
申请日：1981-07-09
申请人： KOWA COMPANY, LTD.
发明人： Iwasaki, Akio , Deushi, Takeo , Watanabe, Isamu , Mori, Toshihito
IPC分类号： C12P19/48 , C07H15/22
CPC分类号： C07H15/224 , C12P19/48 , C12R1/01 , Y10S435/822
摘要： Zur kontinuierlichen indirekten Warmebehandlung von rieselfähigem Gut ist ein drehbares Rohr geeignet, dessen Rohrmantel aus ebenen Flächen zusammengesetzt ist, und auf mindestens einer inneren Fläche Leitbleche vorhanden sind. Die Rohre konnen zu einem Rohrbündel zusammenge- schaltet werden. Solche Rohrbündel in Warmeaustauschern lassen sich aus gefalteten bzw. ebenen Blechen einfach fertigen.
摘要翻译：用于可倾倒的可旋转管的连续间接热处理是合适的，包覆管由平坦表面，并且导向板的存在的至少一个内表面上。所述管可以连接在一起以形成一个管束。在热交换器中，例如管束可以由折叠或平片被容易地制造。

43. 发明授权

EP0002680B1 4-Spectinomycylamin und seine physiologisch verträgliche Salze, Verfahren zur Herstellung und diese Stoffe enthaltende Arzneimittel 失效
标题翻译： 4-氨基丁酰胺及其生理接受的盐，其制备方法和含有这些物质的药物产品
公开(公告)号：EP0002680B1
公开(公告)日：1981-02-11
申请号：EP78101542.5
申请日：1978-12-04
申请人： Dr. Karl Thomae GmbH
发明人： Maier, Roland, Dipl.-Chem. Dr. , Woitun, Eberhard, Dipl.-Chem. Dr. , Reuter, Wolfgang, Dipl.-Chem. Dr. , Wetzel, Bernd, Dipl.-Chem. Dr. , Goeth, Hanns, Dr. , Lechner, Uwe, Dr.
IPC分类号： C07D493/04 , A61K31/335
CPC分类号： C07H15/224

44. 发明申请

WO2017037719A1 AMINOGLYCOSIDE DERIVATIVES AND USES THEREOF IN TREATING GENETIC DISORDERS 审中-公开
标题翻译：氨基丁糖衍生物及其在治疗遗传性疾病中的应用
公开(公告)号：WO2017037719A1
公开(公告)日：2017-03-09
申请号：PCT/IL2016/050968
申请日：2016-09-02
申请人： ELOXX PHARMACEUTICALS LTD.
发明人： BAASOV, Timor , TUVIA, Shmuel
IPC分类号： C07H15/23 , A61K31/7036 , A61P7/04 , A61P21/00 , A61P21/04 , C07H15/222 , C07H15/224
CPC分类号： C07H15/224 , C07H15/23
摘要： Novel aminoglycosides, represented by Formulae la and lb, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.
摘要翻译：提供了本发明说明书中定义的由式Ia和1b表示的新型氨基糖苷类，其设计为展现终止密码子突变读取活性。还提供了含有该组合物的药物组合物及其用于治疗遗传性疾病和病症例如与终止密码子突变相关的疾病和病症的用途。

45. 发明申请

WO2011124986A3 POLYOL MODIFIED AMINOGLYCOSIDE-LIPID CONJUGATES 审中-公开
标题翻译：多元醇改性氨基丁糖 - 脂质结合物
公开(公告)号：WO2011124986A3
公开(公告)日：2011-12-15
申请号：PCT/IB2011001226
申请日：2011-04-05
申请人： UNIV MANITOBA , SCHWEIZER FRANK , SMRITILEKHA BERA , ZHANEL GEORGE
发明人： SCHWEIZER FRANK , SMRITILEKHA BERA , ZHANEL GEORGE
IPC分类号： C07H15/00 , A61K31/7036 , A61P31/04 , C07H13/02 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18
CPC分类号： C07H15/224 , C07H17/04
摘要： In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof. Additionally, methods of treating and preventing bacterial infections using the aminoglycoside derivatives are also provided
摘要翻译：在某些方面，本发明提供具有抗菌活性的氨基糖苷衍生物。在一些方面，氨基糖苷衍生物包含由（a）氨基甙基和（b）氨基甙基的伯或仲羟基位置的至少一个疏水氨基甲酸酯和烷氧基及其盐组成的化合物。此外，还提供了使用氨基糖苷衍生物治疗和预防细菌感染的方法

46. 发明申请

WO2011124986A2 POLYOL MODIFIED AMINOGLYCOSIDE-LIPID CONJUGATES 审中-公开
标题翻译：多元醇改性氨基丁糖 - 脂质结合物
公开(公告)号：WO2011124986A2
公开(公告)日：2011-10-13
申请号：PCT/IB2011/001226
申请日：2011-04-05
申请人： UNIVERSITY OF MANITOBA , SCHWEIZER, Frank , SMRITILEKHA, Bera , ZHANEL, George
发明人： SCHWEIZER, Frank , SMRITILEKHA, Bera , ZHANEL, George
CPC分类号： C07H15/224 , C07H17/04
摘要： In some aspects, the present invention provides novel aminoglycoside derivatives that exhibit antibacterial activity. In some aspects, the aminoglycoside derivative comprising (a) an aminoglycoside group; and (b) at least one carbamate group or alkoxy group attached to a primary or secondary hydroxy position of the aminoglycoside group; or a salt thereof. In some embodiments, the hydrophobic group is a carbamate or an ether group. Additionally, methods of treating and preventing bacterial infections using these aminoglycoside derivatives are also provided.
摘要翻译：在某些方面，本发明提供具有抗菌活性的新型氨基糖苷衍生物。在一些方面，所述氨基糖苷衍生物包含（a）氨基糖苷类; 和（b）至少一个连接到氨基糖苷类的伯或仲羟基位置的氨基甲酸酯基或烷氧基; 或其盐。在一些实施方案中，疏水基团是氨基甲酸酯或醚基团。此外，还提供了使用这些氨基糖苷衍生物治疗和预防细菌感染的方法。

47. 发明申请

WO2010037179A1 ANIONIC CONJUGATES OF GLYCOSYLATED BACTERIAL METABOLITE 审中-公开
标题翻译：甘氨酸细菌代谢物的阴离子结合
公开(公告)号：WO2010037179A1
公开(公告)日：2010-04-08
申请号：PCT/AU2009/001313
申请日：2009-10-02
申请人： GLYCAN BIOSCIENCES PTY LTD , KETT, Warren, Charles , CHEN, Yugang
发明人： KETT, Warren, Charles , CHEN, Yugang
IPC分类号： C07H3/06 , A61K31/702 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K31/7056 , A61P7/02 , A61P11/00 , A61P11/06 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/04 , A61P37/00 , A61P37/08 , C07H5/06 , C07H15/12 , C07H15/203 , C07H15/22 , C07H15/224 , C07H15/232 , C07H15/234 , C07H15/26 , C07H19/056
CPC分类号： A61K47/4823 , A61K31/702 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K31/7056 , A61K47/48092 , A61K47/549 , A61K47/61 , C07H3/06 , C07H5/06 , C07H5/10 , C07H13/12 , C07H15/14 , C07H15/203 , C07H15/224 , C07H15/23 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H15/26 , C07H19/056
摘要： The invention relates to anionic conjugates of glycosylated bacterial metabolites that may be used to mimic the structure and/or activity of the anionic bioactive molecules known as glycosaminoglycans (GAGs). The invention also relates to processes for the preparation of the conjugates. Such conjugates are useful in the prophylaxis and/or treatment of disease conditions and in particular chronic disease conditions such as inflammatory (including allergic) diseases, metastatic cancers and infection by pathogenic agents including bacteria, viruses or parasites.
摘要翻译：本发明涉及可用于模拟称为糖胺聚糖（GAG）的阴离子生物活性分子的结构和/或活性的糖基化细菌代谢物的阴离子结合物。本发明还涉及制备缀合物的方法。这样的缀合物可用于预防和/或治疗疾病状况，特别是慢性疾病病症，例如炎症（包括过敏性）疾病，转移性癌症和包括细菌，病毒或寄生虫在内的病原体感染。

48. 发明申请

WO2009095588A2 SYNTHESE DE NOUVEAUX DERIVES DE NEAMINE ET LEUR UTILISATION COMME AGENTS ANTIBACTERIENS 审中-公开
标题翻译：新型胺衍生物的合成及其作为抗菌剂的用途
公开(公告)号：WO2009095588A2
公开(公告)日：2009-08-06
申请号：PCT/FR2009/050088
申请日：2009-01-22
申请人： UNIVERSITE JOSEPH FOURIER , DECOUT, Jean-Luc , BAUSSANE, Isabelle , DESIRE, Jérôme , PARIS, Jean-Marc
发明人： DECOUT, Jean-Luc , BAUSSANE, Isabelle , DESIRE, Jérôme , PARIS, Jean-Marc
IPC分类号： C07H15/224 , A61K31/7036 , A61P31/04 , A61K31/7028 , A61K31/4704
CPC分类号： C07H15/224
摘要： La présente invention concerne des composés de formule (I) dans laquelle : R 1 = OH ou NH 2 ; OR 2 , OR 3 , OR 4 et OR 5 forment des fonctions alcool, éther, ester, carbonate, carbamate, sulfonate ou sulfamate; et si R 5 = H, si R 2 =R 3 =R 4 , alors R 2 , R 3 et R 4 ≠ H; si R 2 = H, alors R3 ≠ H et R4 ≠ H; si R 3 = H, alors R 2 ≠ H et R 4 ≠ H; si R 4 = H, alors R 2 ≠ H et R 3 ≠ H; si R 5 ≠ H, si R 2 = H, alors R 3 ≠ H et R 4 ≠ H; si R 3 = H, alors R 2 ≠ H et R 4 ≠ H; si R 4 = H, alors R 2 ≠ H et R 3 ≠ H, leur utilisation en tant qu'agents antibiotiques et leur procédé de synthèse.
摘要翻译：本发明涉及式（I）化合物，其中：R1 = OH或NH2; OR2，OR3，OR4和OR5形成醇，醚，酯，碳酸酯，氨基甲酸酯，磺酸酯或氨基磺酸酯官能团; 并且如果R5 = H，如果R2 = R3 = R4，则R2，R3和R4？ H; 如果R2 = H，则R3 H和R4？ H; 如果R3 = H，则R2 H和R4？ H; 如果R4 = H，则R2 H和R3？ H; 如果R5？ H，如果R2 = H，则R3 H和R4？ H; 如果R3 = H，则R2 H和R4？ H; 如果R4 = H，则R2 H和R3？本发明还涉及其作为抗生素剂的用途及其合成方法。

49. 发明申请

WO01080863A1 BIFUNCTIONAL ANTIBIOTICS 审中-公开
标题翻译：双功能抗体
公开(公告)号：WO01080863A1
公开(公告)日：2001-11-01
申请号：PCT/US2001/040611
申请日：2001-04-27
IPC分类号： A61K31/70 , A61K31/704 , C07H15/224 , C07H15/232 , C07H15/234
CPC分类号： C07H15/234 , A61K31/70 , A61K31/704 , A61K47/552 , C07H15/224 , C07H15/232 , Y02A50/473
摘要： Bifunctional antibiotics that target both bacterial RNA and resistance-causing enzymes are disclosed. The A-site of bacterial 16S rRNA serves as the target site for most aminoglycoside antibiotics. Resistance to this class of antibiotics is frequently developed by microbial enzymatic acetylation, phosphorylation or ribosylation of aminoglycosides, modifications that weaken their interactions with the target RNA. Using surface plasmon resonance (SPR), the binding affinity and stoichiometry of various aminoglycosides have been investigated and it was found that neamine, the key pharmacophore of the deoxystreptamine class of aminoglycosides, binds to the A-site in a two to one stoichiometry with a K >d K >d -fold increase in affinity). Antibiotic activities of the dimers were determined for several bacterial strains by the Kirby-Bauer method. The most active dimer, based on antibiotic activity, also showed the highest inhibition of in vitro translation (IC50 = 0.055 mu M). The latter assay was developed in order to correlate the relationship between SPR-based affinity and translation inhibition. By these combined methods, transport limitations for the semisynthetic aminoglycosides as well as non-ribosomally based antibiotic activity could be determined. Further analysis of these dimers as substrates for aminoglycoside modifying-enzymes identified a neamine dimer that was a potent inhibitor (Kis = 0.1 mu M) of the APH(2'') activity of the bifunctional enzyme AAC(6'')-APH(2''), the primary enzyme responsible for high level gentamicin C resistance in several bacterial strains.
摘要翻译：公开了靶向细菌RNA和产生抗性的酶的双功能抗生素。细菌16S rRNA的A位点作为大多数氨基糖苷类抗生素的靶位点。通常通过微生物酶促乙酰化，氨基糖苷类磷酸化或核糖基化，削弱其与靶RNA的相互作用的修饰来发展抗这类抗生素的抗性。使用表面等离子体共振（SPR），已经研究了各种氨基糖苷类的结合亲和力和化学计量学，并且发现神经胺是氨基糖苷类的脱氧链霉胺类的关键药效团，以2比1的化学计量与A位点结合每个结合位点的K > d <10μM。制备了一种神经胺二聚体文库，并通过SPR测定了它们对16S rRNA A位点的亲和力，对于最佳的二聚体（相似的10 3 3倍）增加了KI <= 40nM 亲和力）。通过Kirby-Bauer方法测定了几种细菌菌株对二聚体的抗生素活性。基于抗生素活性的最活跃的二聚体也显示了体外翻译的最高抑制（IC50 =0.055μM）。开发了后一种测定法，以便将基于SPR的亲和力和翻译抑制之间的关系相关联。通过这些组合方法，可以确定半合成氨基糖苷类的运输限制以及非核糖体基抗生素活性。作为氨基糖苷修饰酶的底物的这些二聚体的进一步分析鉴定了二胺，其是双功能酶AAC（6“）-APH的APH（2”）活性的有效抑制剂（Kis =0.1μM） 2“），是几种细菌菌株中高水平庆大霉素C抗性的主要酶。

50. 发明申请

WO1992003460A1 4-O-(AMINOGLYCOSYL)- OR 4,6-DI-O-(AMINOGLYCOSYL)-2,5-DIDEOXY-5,5-DIFLUOROSTREPTAMINE DERIVATIVE AND PRODUCTION THEREOF 审中-公开
标题翻译： 4-O-（氨基甲酰基） - 或4,6-DI-O-（氨基甲酰基）-2,5-二脱氧-5,5-二氟哌啶胺衍生物及其生产物
公开(公告)号：WO1992003460A1
公开(公告)日：1992-03-05
申请号：PCT/JP1991001115
申请日：1991-08-22
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI , TAKEUCHI, Tomio , UMEZAWA, Sumio , TSUCHIYA, Tsutomu , SHITARA, Tetsuo , FUKATSU, Shunzo , UMEMURA, Eijiro
发明人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
IPC分类号： C07H15/234
CPC分类号： C07H15/224 , C07H15/234 , C07H15/236 , Y02P20/55
摘要： The invention provides 5-deoxy-5,5-difluoro derivatives of aminoglycoside antibiotics of neamine, kanamycin A, kanamycin B, gentamicin and seldomycin, each synthesized as a novel compound, and also 1-N-(α-hydroxy-φ-aminoalkanoyl) derivatives synthesized from the newly obtained 5-deoxy-5,5-difluorokanamycins A and B and analogs thereof. The 5-deoxy-5,5-difluoro derivatives thus obtained have antibacterial activities superior or substantially equivalent to those of the amino-glycoside antibiotics from which they are derived and further have a remarkably improved median lethal dose (LD50) when intravenously administered to mice and a remarkably reduced toxicity on mammals.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式