公开(公告)号：US08377896B2

公开(公告)日：2013-02-19

申请号：US13044226

申请日：2011-03-09

申请人： Michael T. Migawa ,  Xiaojing Wang ,  Eric E. Swayze ,  Richard H. Griffey

发明人： Michael T. Migawa ,  Xiaojing Wang ,  Eric E. Swayze ,  Richard H. Griffey

IPC分类号： A61K31/70 ,  C07H15/20

CPC分类号： C07H15/234

摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

摘要翻译： 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。

公开(公告)号：US07973147B2

公开(公告)日：2011-07-05

申请号：US12084878

申请日：2006-05-16

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Yong-pil Kim ,  Hideaki Hanaki ,  Atsuko Matsumoto ,  Yoko Takahashi

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Yong-pil Kim ,  Hideaki Hanaki ,  Atsuko Matsumoto ,  Yoko Takahashi

IPC分类号： C07H15/20 ,  C07H15/22 ,  C07C61/12

CPC分类号： C07H11/04 ,  C07C323/59 ,  C12P13/02 ,  C12P19/26 ,  C12P19/44 ,  C12R1/465

摘要： A microorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.

摘要翻译： 属于Streptomyces sp。的菌株K04-0144所代表的微生物 在培养基中培养生产K04-0144物质的能力，分离的K04-0144A物质，K04-0144B物质和K04-0144C物质对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））具有很强的抗菌活性， 因此，这些可用作由MRSA引起的感染性疾病的治疗剂以及由多种药物（包括β-内酰胺抗生素抗性细菌）引起的感染性疾病。 此外，类似地，由于从培养液中分离的新型K04-0144D物质具有增强作为抗菌剂的β-内酰胺抗生素与其组合的作用，因此可用作治疗剂 用于由耐甲氧西林金黄色葡萄球菌（MRSA）引起的感染性疾病和包含β-内酰胺抗生素抗性细菌的多药物。

公开(公告)号：US20080261895A1

公开(公告)日：2008-10-23

申请号：US11976413

申请日：2007-10-24

申请人： Matthew J. Hoffmann ,  William DeMaio ,  Jim Wang ,  John W. Ullrich

发明人： Matthew J. Hoffmann ,  William DeMaio ,  Jim Wang ,  John W. Ullrich

IPC分类号： A61K31/7032 ,  A61K31/138 ,  C07C215/46 ,  A61K31/14 ,  C07C211/63 ,  C07H15/20

CPC分类号： C07C215/64 ,  C07C291/04 ,  C07C2601/14

摘要： The present invention provides novel isolated compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy-DV metabolites, hydroxy-DV-glucuronide metabolites, N-oxide-DV metabolites, and benzyl-hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising any of the metabolites or derivatives of the invention in combination with a pharmaceutically acceptable carrier or excipient. The invention also includes a method of treating at least one central nervous system disorder in a mammal comprising providing to a mammal in need thereof an effective amount of the compounds of the invention.

摘要翻译： 本发明提供了新型分离的化合物，其特征在于代谢物或脱甲基蓝法的衍生物，包括羟基-DV代谢物，羟基-DV-葡糖苷酸代谢物，N-氧化物-DL代谢物和苄基羟基-DV代谢物。 本发明包括药物组合物，其包含本发明的任何代谢物或衍生物与药学上可接受的载体或赋形剂的组合。 本发明还包括治疗哺乳动物中的至少一种中枢神经系统病症的方法，其包括向有需要的哺乳动物提供有效量的本发明化合物。

公开(公告)号：US20070142631A1

公开(公告)日：2007-06-21

申请号：US11673180

申请日：2007-02-09

申请人： Mitali Ghoshal ,  Gerald Sigler ,  Raymond Hui ,  Ronald Hawley ,  Eva Hoess ,  Erasmus Huber ,  John Patterson ,  Salvatore Salamone ,  Allan Dorn

发明人： Mitali Ghoshal ,  Gerald Sigler ,  Raymond Hui ,  Ronald Hawley ,  Eva Hoess ,  Erasmus Huber ,  John Patterson ,  Salvatore Salamone ,  Allan Dorn

IPC分类号： C07J17/00 ,  C07H15/22 ,  C07D473/04 ,  C07H15/24 ,  C07H15/20

CPC分类号： C07D405/12 ,  C07D307/88 ,  C07D473/08 ,  C07H15/20 ,  C07H15/22 ,  C07H15/24 ,  C07J17/00 ,  C07J19/005 ,  C07J41/0005 ,  C07J41/0055 ,  C07J43/003 ,  G01N33/53 ,  G01N33/535 ,  G01N33/5735 ,  G01N33/581 ,  G01N33/78 ,  G01N33/9453 ,  G01N2333/904

摘要： The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or oligonucleotide. The present invention also provides novel compounds, assay reagents and packaged kits useful for performing such measurements.

摘要翻译： 本发明提供了一种用于测量生物样品中分析物的方法，由此使非竞争性抑制剂与配体偶联并用于均匀测定。 分析物可以是药物或药物衍生物，激素，多肽或寡核苷酸。 本发明还提供了可用于进行这种测量的新型化合物，测定试剂和包装的试剂盒。

公开(公告)号：US20050215491A1

公开(公告)日：2005-09-29

申请号：US11133018

申请日：2005-05-19

申请人： Manuel Martin-Lomas ,  Thomas Rademacher ,  Hugo Caro ,  Irene Francois

发明人： Manuel Martin-Lomas ,  Thomas Rademacher ,  Hugo Caro ,  Irene Francois

IPC分类号： C07H15/20 ,  C07H15/207 ,  C07H15/256 ,  C07H5/06 ,  A61K31/704

CPC分类号： C07H15/24 ,  C07H15/20 ,  C07H15/207

摘要： Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. In particular, the compounds are based on the 1,6 linkage of a sugar residue and a cyclitol.

摘要翻译： 公开了具有肌醇磷酸甘氨酸的模拟或拮抗性质的化合物，以及这些化合物的用途，以及其用途，例如， 治疗通过给予IPG第二信使或其IPG拮抗剂而改善的病症。 特别地，这些化合物基于糖残基和环醇的1,6-连接。

公开(公告)号：US20050100976A1

公开(公告)日：2005-05-12

申请号：US11015646

申请日：2004-12-20

申请人： Christopher Bieniarz ,  Michael Farrell

发明人： Christopher Bieniarz ,  Michael Farrell

IPC分类号： C07F9/09 ,  C07F9/655 ,  C07H15/20 ,  C07H15/24 ,  C07H15/26 ,  G01N33/58 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/537 ,  G01N33/543

CPC分类号： C07F9/093 ,  C07F9/65517 ,  C07F9/65522 ,  C07H15/20 ,  C07H15/24 ,  C07H15/26 ,  G01N33/581

摘要： The invention is directed to enhanced methods for detecting an analyte of interest in situ, by immunoassay, or by hybridization comprising binding an enzyme-labeled conjugate molecule to an analyte of interest in the presence of a redox-inactive reductive species and a soluble metal ion. The enzyme catalyzes the conversion of the inactive reductive species to an active reducing agent, which in turn reduces the metal ion to a metal atom thereby providing an enhanced means of detecting the analyte via metal deposition.

摘要翻译： 本发明涉及通过免疫测定或通过杂交来检测目的分析物的增强方法，包括在氧化还原惰性还原物质和可溶性金属离子存在下将酶标记的缀合物分子与目的分析物结合 。 酶催化无活性还原物质转化为活性还原剂，其又将金属离子还原成金属原子，从而提供通过金属沉积检测分析物的增强方法。

公开(公告)号：US5877296A

公开(公告)日：1999-03-02

申请号：US452164

申请日：1995-05-26

申请人： Philip Ross Hamann ,  Lois Hinman ,  Irwin Hollander ,  Ryan Holcomb ,  William Hallett ,  Hwei-Ru Tsou ,  Martin J. Weiss

发明人： Philip Ross Hamann ,  Lois Hinman ,  Irwin Hollander ,  Ryan Holcomb ,  William Hallett ,  Hwei-Ru Tsou ,  Martin J. Weiss

IPC分类号： C07H15/20 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K38/00 ,  A61K38/22 ,  A61K39/395 ,  A61K39/44 ,  A61K47/48 ,  A61P35/00 ,  C07H15/203 ,  C07K1/113 ,  C07K16/00 ,  A01N43/04 ,  C12P19/44

CPC分类号： A61K47/48238 ,  A61K47/48407

摘要： This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

摘要翻译： 本发明描述由强效抗肿瘤抗生素及其衍生物的加利车霉素家族的二硫化物类似物制备的载体 - 药物偶联物，以及来自相关抗肿瘤抗生素如精蛋白的类似类似物。 载体可以是靶向不想要的细胞群的抗体，生长因子或类固醇，例如肿瘤的细胞。 全蛋白质载体以及它们的抗原识别片段及其化学或遗传操作的对应物可用于缀合物的靶向部分。 本发明包括合成这些缀合物所需的化合物，载体 - 药物共轭物的合适药物组合物及其使用方法。

公开(公告)号：US5763586A

公开(公告)日：1998-06-09

申请号：US747670

申请日：1996-11-12

申请人： Don N. Gray

发明人： Don N. Gray

IPC分类号： C07H15/20 ,  C07H15/207 ,  C11D3/22 ,  C07H1/00 ,  C07K1/14

CPC分类号： C07H15/20 ,  C07H15/207 ,  C11D3/221

摘要： The extraction of proteins from selected naturally occurring membranes without any harmful, adverse, or other deleterious effect(s). In one preferred embodiment the detergent is prepared from the reaction of a cycloalkyl aliphatic alcohol and a saccharide.

摘要翻译： 从选定的天然存在的膜中提取蛋白质而没有任何有害的，不利的或其他有害的作用。 在一个优选的实施方案中，洗涤剂由环烷基脂族醇和糖的反应制备。

公开(公告)号：US5710133A

公开(公告)日：1998-01-20

申请号：US483263

申请日：1995-06-07

申请人： Tetsuya Nakada ,  Michio Kubota

发明人： Tetsuya Nakada ,  Michio Kubota

IPC分类号： C07H15/203 ,  C08B37/00 ,  A61K31/70 ,  C07H15/20 ,  C12P19/44

CPC分类号： C07H15/203 ,  C08B37/0015

摘要： Disclosed is a novel .alpha.-glycosyl derivative of a catecholamine or its salt, said .alpha.-glycosyl derivative being prepared by allowing a saccharide-transferring enzyme together with or without glucoamylase to act on a solution containing an .alpha.-glucosyl saccharide and one of catecholamines in order to form an .alpha.-glycosyl derivative of said catecholamines, and recovering the resultant .alpha.-glycosyl derivative. The .alpha.-glycosyl derivative overcomes conventional drawbacks of catecholamines, and does not substantially exhibit or have a reducing activity and undesirable toxicity, but has a relatively-high stability and exerts the inherent physiological activities of catecholamines in vivo. Thus, the .alpha.-glycosyl derivative is advantageously used as a variety of pharmaceuticals in the form of an injection, tablet, etc.

公开(公告)号：US5693767A

公开(公告)日：1997-12-02

申请号：US251869

申请日：1994-06-01

申请人： R. -Erich Klemke ,  Masato Koreeda ,  Todd A. Houston ,  Brian K. Shull ,  Roeland J. Tuinman

发明人： R. -Erich Klemke ,  Masato Koreeda ,  Todd A. Houston ,  Brian K. Shull ,  Roeland J. Tuinman

IPC分类号： C07H15/18 ,  C07H15/256 ,  C07H17/04 ,  C07J9/00 ,  C07J17/00 ,  C07H15/20 ,  A61K31/70

CPC分类号： C07H15/18 ,  C07H15/256 ,  C07H17/04 ,  C07J17/005 ,  C07J9/00 ,  C07J9/005

摘要： Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.

摘要翻译： 提供新的糖苷，特别是甾体和非甾体糖苷。 甾体和非甾体糖苷优选由具有有价值性质如药理学性质的糖苷配制剂制备。 糖苷由有用的糖苷配制而成，具有与它们各自的未糖基化糖苷基相同的有用性质。 糖苷以酰化和脱酰基形式提供。 酰基水解后的酰化糖苷具有增强的水溶性，如糖苷配基是乙酰氨基酚的情况所示。