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71. 发明申请

WO2012142959A1 一种高纯度的卡泊芬净或其盐及其制备方法和用途审中-公开
公开(公告)号：WO2012142959A1
公开(公告)日：2012-10-26
申请号：PCT/CN2012/074420
申请日：2012-04-20
申请人：上海天伟生物制药有限公司 , 何兵明 , 李明 , 唐志军 , 季晓铭
发明人：何兵明 , 李明 , 唐志军 , 季晓铭
IPC分类号： C07K7/54 , A61K38/12 , A61P31/10
CPC分类号： A61K38/12 , A61K31/19 , A61K38/005 , C07K7/54 , C07K7/56
摘要：本发明公开了一种高纯度的卡泊芬净或其盐及其制备方法和用途。公开了一种低溶剂残留及低盐的卡泊芬净或其盐及其制备工艺；将卡泊芬净或其盐粗品溶于水和醋酸体系中，然后和第一有机溶剂乙醇混合，再和第二有机溶剂乙酸乙酯混合，再通过过滤和与水共同干燥得到具有良好稳定性的低溶剂残留及低盐的卡泊芬净或其盐。

72. 发明申请

WO2009151341A1 PROCESS FOR PREPARING CASPOFUNGIN AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备CASPOFUNGIN及其中间体的方法
公开(公告)号：WO2009151341A1
公开(公告)日：2009-12-17
申请号：PCT/NO2009/000218
申请日：2009-06-11
申请人： AXELLIA PHARMACEUTICALS APS , HEGGELUND, Audun , KVERNENES, Ole, Heine , BJØRNSTAD, Vidar
发明人： HEGGELUND, Audun , KVERNENES, Ole, Heine , BJØRNSTAD, Vidar
IPC分类号： C07K7/54
CPC分类号： C07K7/56
摘要： The present invention relates to novel intermediates of formula (VII), or an acid addition salt or a solvate thereof, wherein R 1 is -(CO)NH 2 , -CH 2 NH 2 or -CN; R 2 = R 3 = H or R 2 and R 3 together form a cyclic boronate or borate ester; X is a helping group selected from the group consisting of i) a five or six membered heterocyclic aromatic ring and derivatives thereof comprising at least one N-atom being a part of an imine-group, wherein said N-atom forms the point of connection to the cyclohexapeptide ring, and ii) tetrazolyl and derivatives thereof for which a nitrogen atom forms the point of connection to the cyclohexapeptide ring, and a process for the preparation of caspofungin utilizing said intermediates.
摘要翻译：本发明涉及式（Ⅶ）的新型中间体或其酸加成盐或其溶剂化物，其中R 1为 - （CO）NH 2，-CH 2 NH 2或-CN; R2 = R3 = H或R2和R3一起形成环状硼酸酯或硼酸酯; X是选自i）五元或六元杂环芳香环及其衍生物的辅助基团，其包含至少一个N-原子是亚胺基的一部分，其中所述N-原子形成连接点并且ii）其氮原子与环己肽环形成连接点的四唑基及其衍生物，以及利用所述中间体制备卡泊芬净的方法。

73. 发明申请

WO2009083663A3 CYCLIC PEPTIDES COMPRISING AT LEAST ONE AZA-?3-AMINOACYL RESIDUE AND USES THEREOF 审中-公开
标题翻译：包含至少一种AZA-？3-氨基酸残基的循环肽及其用途
公开(公告)号：WO2009083663A3
公开(公告)日：2009-08-27
申请号：PCT/FR2008001403
申请日：2008-10-08
申请人： CENTRE NAT RECH SCIENT , UNIV RENNES , LAURENCIN MATHIEU , ZATYLNY-GAUDIN CELINE , HENRY JOEL , BAUDY FLOC H MICHELE
发明人： LAURENCIN MATHIEU , ZATYLNY-GAUDIN CELINE , HENRY JOEL
IPC分类号： C07K7/54 , A61K38/12 , A61P31/00 , C07K5/12
CPC分类号： C07K7/56 , A61K38/00
摘要： Cyclic peptides having a random alternation of L-a-aminoacyl residues and of aza-ß3-aminoacyl residues and uses thereof.
摘要翻译：具有L-α-氨酰基残基和氮杂-β-氨酰基残基的随机交替的循环肽及其用途。

74. 发明申请

WO2006086012A3 ANTIBIOTIC COMPOUND 审中-公开
标题翻译：抗生素化合物
公开(公告)号：WO2006086012A3
公开(公告)日：2007-01-11
申请号：PCT/US2005033326
申请日：2005-09-16
申请人： MERCK & CO INC , BARRETT JOHN F , HERATH KITHSIRI B , JAYASURIYA HIRANTHI , MASUREKAR PRAKASH S , ONDEYKA JOHN G , SINGH SHEO BUX , ZHANG CHAOWEI
发明人： BARRETT JOHN F , HERATH KITHSIRI B , JAYASURIYA HIRANTHI , MASUREKAR PRAKASH S , ONDEYKA JOHN G , SINGH SHEO BUX , ZHANG CHAOWEI
IPC分类号： A61K31/00 , A61K38/12 , A61K38/14 , C07K7/50 , C07K7/54 , C07K7/58 , C07K9/00 , C12P21/02 , C12P21/04
CPC分类号： C07K9/008 , A61K38/00
摘要： Fermentation of a nutrient medium with a Nocardia spp. yields a novel broad spectrum antibiotic compound of structural formula (I) or a pharmaceutically acceptable salt, ester, enantiomer, diasteriomer or mixture.
摘要翻译：用诺卡氏菌发酵营养培养基产生结构式（I）的新型广谱抗生素化合物或其药学上可接受的盐，酯，对映异构体，非对映异构体或混合物。

75. 发明申请

WO2006094082A3 SEMI-SYNTHETIC DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开
公开(公告)号：WO2006094082A3
公开(公告)日：2006-09-08
申请号：PCT/US2006/007337
申请日：2006-02-27
申请人： CHIRON CORPORATION , NORTH CHINA PHARMACEUTICAL GROUP CORPORATION , CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
发明人： CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
IPC分类号： A61K38/04 , A61K38/14 , C07K7/50 , C07K7/54
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl- vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl- vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

76. 发明申请

WO2006078161A1 BINDING COMPOUNDS, IMMUNOGENIC COMPOUNDS AND PEPTIDOMIMETICS 审中-公开
标题翻译：结合化合物，免疫组化和蛋白质
公开(公告)号：WO2006078161A1
公开(公告)日：2006-07-27
申请号：PCT/NL2006/000036
申请日：2006-01-24
申请人： Pepscan Systems B.V. , TIMMERMAN, Peter , PUIJK, Wouter Cornelis , SLOOTSTRA, Jelle Wouter , VAN DIJK, Evert , MELOEN, Robbert Hans
发明人： TIMMERMAN, Peter , PUIJK, Wouter Cornelis , SLOOTSTRA, Jelle Wouter , VAN DIJK, Evert , MELOEN, Robbert Hans
IPC分类号： G01N33/68 , C07K14/48 , C07K14/49 , C07K14/495 , C07K14/61 , A61K47/42 , A61K39/00 , C07K14/52 , C07K14/59 , C07K1/04 , C07K7/54
CPC分类号： G01N33/6812 , C07K7/06 , C07K14/52 , C07K14/5409 , C07K14/59 , C07K14/7158
摘要： The invention provides means and methods for producing compounds suitable for testing for the presence and/or identification of an immunogenic compound and/or a binding compound of interest. Immunogenic compounds and compositions are also herewith provided, as well as peptidomimetics of members of the cystine-knot family.
摘要翻译：本发明提供了用于生产适于测试感兴趣的免疫原性化合物和/或结合化合物的存在和/或鉴定的化合物的方法和方法。还提供了免疫原性化合物和组合物，以及胱氨酸结构家族的成员的肽模拟物。

77. 发明申请

WO2006032457A1 PEPTIDE CYCLISATION 审中-公开
标题翻译：肽的循环
公开(公告)号：WO2006032457A1
公开(公告)日：2006-03-30
申请号：PCT/EP2005/010133
申请日：2005-09-20
申请人： LONZA AG , GIRAUD, Matthieu , WERBITZKY, Oleg , WILLINER, Michaela
发明人： GIRAUD, Matthieu , WERBITZKY, Oleg , WILLINER, Michaela
IPC分类号： C07K1/06 , C07K7/54 , C07C29/10 , C07C51/09 , C07C209/62
CPC分类号： C07K1/042 , C07K7/54 , C07K14/685
摘要： A novel method for side chain cyclisation of peptides by means of lactamization is provided.
摘要翻译：提供了通过内酰胺化进行肽侧链环化的新方法。

78. 发明申请

WO02055545A1 ANTIMICROBIAL PSEUDOPEPTIDES 审中-公开
标题翻译：抗菌药物
公开(公告)号：WO02055545A1
公开(公告)日：2002-07-18
申请号：PCT/FR2002/000032
申请日：2002-01-07
IPC分类号： A01N43/72 , A01N63/02 , A61K38/00 , A61P31/00 , C07K7/02 , C07K7/54 , C12P17/14 , C12P21/02 , C12P21/04 , A61K38/08
CPC分类号： A01N63/02 , A01N43/72 , A61K38/00 , C07K7/02 , C07K7/54 , C12P17/14 , C12P21/02
摘要： The invention relates to antimicrobial molecules with a pseudopeptide structure. In particular, said molecules are isolated from Xenorhabdus bacteria. They are particularly suitable for the protection of crops, in the form of pesticides, used to combat plant diseases caused by microbial agents and in the pharmaceutical and veterinary fields as antimicrobial agents, used to combat human and animal diseases of microbial origin.
摘要翻译：本发明涉及具有假肽结构的抗微生物分子。特别地，所述分子与Xenorhabdus细菌分离。它们特别适用于以农药的形式，用于防治由微生物剂引起的植物病害和作为抗微生物剂的药剂和兽医领域的作物，用于对抗微生物来源的人类和动物疾病。

79. 发明申请

WO0170930A3 GROWTH FACTOR BINDING MOLECULES 审中-公开
标题翻译：生长因子结合分子
公开(公告)号：WO0170930A3
公开(公告)日：2002-01-10
申请号：PCT/US0108920
申请日：2001-03-21
申请人： UNIV SOUTH FLORIDA , SEBTI SAID M , HAMILTON ANDREW D
发明人： SEBTI SAID M , HAMILTON ANDREW D
IPC分类号： A61K38/00 , C07K7/56 , C07K14/00 , A61K38/02 , A61K38/12 , C07K2/00 , C07K7/54 , G01N33/68
CPC分类号： C07K7/56 , A61K38/00 , C07K14/001
摘要： Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold such as a calixarene, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.
摘要翻译：具有多个肽环的生长因子结合分子，其连接于非肽有机支架如杯芳烃，优选具有具有四个氨基酸侧链的假六氨基酸肽环。生长因子结合分子特异性结合各种生长因子并且适用于治疗具有肿瘤或再狭窄的受试者。在一个实施方案中，公开了用于抑制实体瘤中肿瘤生长和血管生成的血小板衍生生长因子结合分子。

80. 发明申请

WO00011023A2 RING MODIFIED CYCLIC PEPTIDE ANALOGS 审中-公开
标题翻译：环改性循环肽模拟
公开(公告)号：WO00011023A2
公开(公告)日：2000-03-02
申请号：PCT/US1999/018908
申请日：1999-08-18
IPC分类号： A61K9/08 , A61K9/72 , A61K38/00 , A61P31/10 , A61P33/00 , C07K1/06 , C07K7/50 , C07K7/54 , C07K7/56 , C07K7/64 , A61K38/12
CPC分类号： C07K7/50 , A61K38/00 , C07K7/56 , Y02A50/409
摘要： A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal ornithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.
摘要翻译：提供了一种用于改变棘球in素型化合物的环肽环体系以产生具有抗真菌活性的新类似物的方法。本发明的方法包括打开环肽环，切割末端鸟氨酸单元，插入至少一个新的氨基酸或其它合成单元并封闭环以产生新的环肽环结构。该方法允许将诸如水溶性的特征结合到环肽环核中，用于进一步修饰的位点，增加或减少环核内的氨基酸或肽单元的数目，并且增加或减少环核内的成员总数戒指。本发明还提供新颖的棘白菌素类化合物及其作为抗真菌剂或抗寄生虫剂的用途。

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