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91. 发明申请

WO0232918A3 KETOLIDE ANTIBACTERIALS 审中-公开
标题翻译：卡介胶抗菌素
公开(公告)号：WO0232918A3
公开(公告)日：2003-01-03
申请号：PCT/US0132119
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC
发明人： HLASTA DENNIS , HENNINGER TODD C , GRANT EUGENE B , KHOSLA CHAITIN , CHU DANIEL T W , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08 , Y02P20/55
摘要： The present invention includes compounds of the formula wherein: X is hydrogen or halide; R is hydrogen, acyl, or a hydroxy protecting group; R is hydrogen, hydroxyl, or -OR wherein R is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.
摘要翻译：本发明包括下式的化合物其中：X是氢或卤化物; R 2是氢，酰基或羟基保护基; R 6是氢，羟基或-OR a，其中R a是选自C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基，杂环的取代或未取代的部分，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环（C 1 -C 10）烷基，杂环（C 2 -C 10）烯基和杂环（C 2 -C 10） R 13是氢或取代或未取代的部分，其中部分选自甲基; C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10），杂环基（C 2 -C 10）烯基和杂环基（C 2 -C 10）炔基;且R是氢或取代或未取代的部分，其中该部分选自C1-C10烷基，C2-C10链烯基，C2 -C 1 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环（C 1 -C 10）烷基，杂环（C 2 -C 10）（C 2 -C 10）炔基;及其药学上可接受的盐，酯和前药形式。这些化合物具有抗感染活性，可用于治疗细菌和原生动物感染。

92. 发明申请

WO2002077005A1 PESTICIDAL SPINOSYN DERIVATIVES 审中-公开
标题翻译：杀虫剂药物衍生物
公开(公告)号：WO2002077005A1
公开(公告)日：2002-10-03
申请号：PCT/US2002/008957
申请日：2002-03-21
申请人： DOW AgroSciences LLC , HAHN, Donald, R. , BALCER, Jesse, L. , LEWER, Paul , GILBERT, Jeffrey, R. , GRAUPNER, Paul, R.
发明人： HAHN, Donald, R. , BALCER, Jesse, L. , LEWER, Paul , GILBERT, Jeffrey, R. , GRAUPNER, Paul, R.
IPC分类号： C07H17/08
CPC分类号： A01N63/00 , A01N45/02 , A01N63/02 , C07H17/08 , C12P19/62 , Y02A50/356
摘要： Macrolide compounds produced by culturing novel mutant Saccharopolyspora sp. strains have insecticidal and acaricidal activity and are useful intermediates for preparing spinosyn analogs.
摘要翻译：通过培养新的突变体酿酒酵母菌株产生的大环内酯类化合物具有杀虫和杀螨活性，并且是制备多杀菌素类似物的有用中间体。

93. 发明申请

WO2002064608A1 SYNTHESIS AND SEPARATION OF OPTICALLY ACTIVE ISOMERS OF ERYTHROMYCIN AND THEIR BIOLOGICAL ACTIONS 审中-公开
标题翻译：红霉素的光学活性异构体及其生物学行为的合成与分离
公开(公告)号：WO2002064608A1
公开(公告)日：2002-08-22
申请号：PCT/US2001/044423
申请日：2001-11-27
申请人： ACADEMIC PHARMACEUTICALS, INC. , SOMBERG, John, C. , RANADE, Vasant
发明人： SOMBERG, John, C. , RANADE, Vasant
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention provides methods for purifying and using optically active isomers of erythromycin as well as compositions comprising such optically active isomers. Such optically active isomers having desired actions as an antibiotic substantially separable from undesirable effects on GI motility and the cardiac potassium channels such that the cardiac action potential is not prolonged and the QT interval on the surface EKG (electrocardiogram) is not increased, such that the erythromycin can be useful for more effective therapy of systemic infections. Also disclosed are methods for assaying the levels of such isomers present in the biological fluids.
摘要翻译：本发明提供了用于纯化和使用红霉素旋光异构体的方法以及包含这种旋光异构体的组合物。具有基本上不受GI运动性和心脏钾通道的不良影响的期望作用的具有期望作用的这种光学活性异构体，使得心脏动作电位不延长，并且表面EKG（心电图）上的QT间期不增加，使得红霉素可用于更有效地治疗全身感染。还公开了用于测定存在于生物流体中的这些异构体水平的方法。

94. 发明申请

WO0248331A2 ACTIVE-SITE ENGINEERING OF NUCLEOTIDYLTRANSFERASES AND GENERAL ENZYMATIC METHODS FOR THE SYNTHESIS OF NATURAL AND "UNNATURAL" UDP-AND TDP-NUCLEOTIDE SUGARS 审中-公开
标题翻译： UDP和TDP核酸糖酵母合成的核苷酸转运蛋白的活性位点工程和一般合成方法
公开(公告)号：WO0248331A2
公开(公告)日：2002-06-20
申请号：PCT/US0147953
申请日：2001-12-13
申请人： SLOAN KETTERING INST CANCER , THORSON JON S , NIKILOV DIMITAR B
发明人： THORSON JON S , NIKILOV DIMITAR B
IPC分类号： C07B61/00 , C07H11/04 , C07H15/24 , C07H15/252 , C07H17/00 , C07H17/08 , C07H19/10 , C07H19/207 , C12N9/12 , C12N9/00
CPC分类号： C07H11/04 , C07H15/24 , C07H15/252 , C07H17/00 , C07H17/08 , C07H19/10 , C07H19/207 , C12N9/1241 , C40B40/00
摘要： The present invention provides mutant nucleotidylyltransferases, such as E>p
摘要翻译：本发明提供具有改变的底物特异性的突变体核苷酰基转移酶，例如E> p < 生产方法; 以及使用这些核苷酰基转移酶的产生核苷酸糖的方法。本发明还提供了使用天然和/或修饰的Ep或其它核苷酸转移酶合成所需核苷酸的方法; 和通过本方法研究的核苷酸外科手术。本发明还提供了新的糖基磷酸酯及其制备方法。

95. 发明申请

WO0200663A3 POLYCYCLIC XANTHONES AS ANTIBIOTICS 审中-公开
标题翻译：多环XANTHONES作为抗生素
公开(公告)号：WO0200663A3
公开(公告)日：2002-05-30
申请号：PCT/GB0102898
申请日：2001-06-29
申请人： INST BIOMAR SA , RUFFLES GRAHAM KEITH , PEREZ BAZ JULIA , CANEDO LIBRADA MARIA , GARCIA GRAVALOS DOLORES , ROMERO FRANCISCO , ESPLIEGO FERNANDO
发明人： PEREZ-BAZ JULIA , CANEDO LIBRADA MARIA , GARCIA GRAVALOS DOLORES , ROMERO FRANCISCO , ESPLIEGO FERNANDO
IPC分类号： A61K31/366 , A61P31/04 , A61P35/00 , C07D493/04 , C07H17/08 , C12N1/20 , C12P17/18 , C12P19/60 , C12R1/03 , A61K31/35 , A61K31/70
CPC分类号： C07D493/04 , C07H17/08 , C12P17/181 , C12R1/03
摘要： A novel class of antitumour compounds has been recognised based on the isolation from a new marine microbe, strain PO13-046, belonging to the genus Actinomadura sp. ), of a compound designated IB-00208. The class of the formulae (I) or (II) where R can be hydrogen, acyl, alkyl, alkenyl, aryl, benzyl, alkali metal, and/or sugar, and R and R can be hydrogen, alkyl, or together R and R form an unsaturated bond. Such compounds demonstrate an interesting activity several cancel cell lines and against Gram-positive bacteria.
摘要翻译：已经基于与命名为IB-00208的化合物的新型海洋微生物属于属Actinomadura sp。的菌株PO13-046的分离，已经认识到一类新的抗肿瘤化合物。式（I）或（II）的类别，其中R 1可以是氢，酰基，烷基，烯基，芳基，苄基，碱金属和/或糖，R 2和R 3可以是氢，烷基或一起R 2和R 3形成不饱和键。这些化合物表现出一些有趣的活性，一些取消细胞系和革兰氏阳性菌。

96. 发明申请

WO02038577A2 EXTENDED RELEASE ERYTHROMYCIN DERIVATIVES 审中-公开
标题翻译：延长释放的红霉素衍生物
公开(公告)号：WO02038577A2
公开(公告)日：2002-05-16
申请号：PCT/US2001/032055
申请日：2001-10-12
IPC分类号： A61K9/20 , A61K9/22 , A61K31/7048 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/30 , A61P31/04 , C07H17/08 , C07H
CPC分类号： C07H17/08
摘要： An extended release pharmaceutical composition comprised of an erythromycin derivative and non-polymer material for providing for extended release, in particular, a member selected from the group consisting of clays, long chain hydrocarbons, long chain carboxylic acids, long chain carboxylic acid esters, long chain alcohols, and mixtures thereof, with said member being present in an amount to provide for extended release of the erythromycin derivative.
摘要翻译：本发明涉及由红霉素衍生物和提供缓释的非聚合物材料组成的药物组合物，更具体地涉及选自粘土，长链烃，羧酸，长链长链羧酸酯，长链醇及其混合物; 所述元素的存在量足以提供红霉素衍生物的持续释放。

97. 发明申请

WO00078772A3 ANTIBIOTIC AGENTS 审中-公开
标题翻译：抗生素
公开(公告)号：WO00078772A3
公开(公告)日：2002-03-21
申请号：PCT/GB2000/002217
申请日：2000-06-19
IPC分类号： A61K9/08 , A61K9/10 , A61K9/20 , A61K9/48 , A61K31/7048 , A61P31/00 , A61P31/04 , A61P31/06 , C07H17/08
CPC分类号： C07H17/08
摘要： Methods of treating a microbial infection comprising administering to a patient in need of such treatment are disclosed. In one aspect the method comprises administering to a patient in need of such treatment a therapeutically effective amount of Erythromycin B (or a pharmaceutically acceptable derivative thereof). In another aspect the method comprises a pharmaceutical composition comprising at least 50 % by weight of Erythromycin B (or a pharmaceutically acceptable derivative thereof) of the total weight of antibiotic present in the composition. Also disclosed are 2'-esters of Erythromycin B and Erythromycin B enol ether.
摘要翻译：公开了治疗微生物感染的方法，包括对需要这种治疗的患者施用。在一个方面，该方法包括向需要这种治疗的患者施用治疗有效量的红霉素B（或其药学上可接受的衍生物）。在另一方面，该方法包括药物组合物，其包含至少50重量％的组合物中存在的抗生素总重量的红霉素B（或其药学上可接受的衍生物）。还公开了红霉素B和红霉素B烯醇醚的2'-酯。

98. 发明申请

WO02012260A1 MACROLIDE ANTIBIOTICS 审中-公开
标题翻译：抗坏血酸
公开(公告)号：WO02012260A1
公开(公告)日：2002-02-14
申请号：PCT/IB2001/001403
申请日：2001-08-06
IPC分类号： A61K31/7048 , A61P31/04 , A61P33/02 , A61P43/00 , C07H17/00 , C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： A macrolide antibiotic of formula (I) wherein the variables are defined as described herein.
摘要翻译：式（I）的大环内酯抗生素，其中变量如本文所述定义。

99. 发明申请

WO02012256A1 METHOD FOR PURIFICATION OF ACARBOSE 审中-公开
标题翻译：乙醛净化方法
公开(公告)号：WO02012256A1
公开(公告)日：2002-02-14
申请号：PCT/US2001/024729
申请日：2001-08-07
IPC分类号： C07H1/08 , C07H17/08 , C07H1/06 , C07H5/04 , C07H15/22 , C07H15/232
CPC分类号： C07H17/08 , C07H1/08
摘要： The present invention relates to a novel process for the preparation of acarbose. Said process comprises the steps of: 1) acidifying a fermentation broth containing an acarbose; 2) removing particulates from the fermentation broth; 3) adsorbing the acarbose on a cation-exchanger in the presence of an anion of a weak acid; 4) eluting the acarbose from the cation-exchanger with at least one of hydrochloric acid and the weak acid; 5) precipitating the acarbose with a solvent; and 6) separating the acarbose.
摘要翻译：本发明涉及一种制备阿卡波糖的新方法。所述方法包括以下步骤：1）酸化含有阿卡波糖的发酵液; 2）从发酵液中除去微粒; 3）在弱酸阴离子存在下将阿卡波糖吸附在阳离子交换器上; 4）用盐酸和弱酸中的至少一种从阳离子交换器洗脱阿卡波糖; 5）用溶剂沉淀阿卡波糖; 和6）分离阿卡波糖。

100. 发明申请

WO02010181A1 AZITHROMOCIN MONOHYDRATE WITH LOWER HYGROSCOPICITY, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS WHICH INCLUDE IT 审中-公开
标题翻译：具有较低水平的AZITHROMOCIN MONOHYDRATE，制备方法和包括其中的药物组合物
公开(公告)号：WO02010181A1
公开(公告)日：2002-02-07
申请号：PCT/IB2001/001327
申请日：2001-07-25
IPC分类号： A61P31/04 , C07H17/08 , A61K31/7052
CPC分类号： C07H17/08
摘要： The improved form of azitromycin monohydrate of lower hydroscopicity and greater density and hardness that presents values of: apparent filling density not lower than 0.35 g/ml; and apparent knocked density not lower than 0.50 g/ml. The method for preparation of an improved form of azitromycin monohydrate is characterised in that the hydroscopic azitromycin monohydrate is subjected to a procession of compaction by pressure. The invention also refers to a pharmaceutical composition that includes a therapeutically effective quantity of improved form of azitromycin monohydrate in association with at least one pharmaceutically acceptable suitable inert diluent.
摘要翻译：具有较低吸水性和较高密度和硬度的改进形式的azitromycin一水合物具有以下值：表观填充密度不低于0.35g / ml; 明显的敲击密度不低于0.50g / ml。制备改性形式的阿霉素一水合物的方法的特征在于，通过压力对吸湿性阿霉素一水合物进行压实加压。本发明还涉及一种药物组合物，其包含与至少一种药学上可接受的合适的惰性稀释剂相关的治疗有效量的改进形式的阿霉素一水合物。

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