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51. 发明申请

US20040001838A1 CYTOTOXIC AGENTS BEARING A REACTIVE POLYETHYLENE GLYCOL MOIETY, CYTOTOXIC CONJUGATES COMPRISING POLYETHYLENE GLYCOL LINKING GROUPS, AND METHODS OF MAKING AND USING THE SAME 有权
标题翻译：携带反应性聚乙烯甘油酸酯的细胞毒性试剂，包含聚乙烯甘油连接组的细胞因子，以及制备和使用它们的方法
公开(公告)号：US20040001838A1
公开(公告)日：2004-01-01
申请号：US10024290
申请日：2001-12-21
申请人： ImmunoGen, Inc.
发明人： Robert Yongxin Zhao , Michael Louis Miller , Wayne Charles Widdison , Ravi V.J. Chari
IPC分类号： A61K039/395 , A61K031/7024 , C07K016/46
CPC分类号： A61K47/60
摘要： Cytotoxic agents bearing a polyethylene glycol (PEG) linking group having a terminal active ester, cytotoxic conjugates comprising one or more cytotoxic agents linked to a cell-binding agent via PEG linking groups, and methods for producing both are disclosed. A therapeutic composition comprising a therapeutically-effective amount of one of the cytotoxic conjugates of the present invention, and a method of killing selected cell populations comprising contacting target cells, or tissue containing target cells, with an effective amount of one of the cytotoxic conjugates, are also disclosed.
摘要翻译：公开了具有末端活性酯的聚乙二醇（PEG）连接基团的细胞毒性剂，包含通过PEG连接基团与细胞结合剂连接的一种或多种细胞毒性剂的细胞毒性缀合物，以及用于生产两者的方法。一种治疗组合物，其包含治疗有效量的本发明的细胞毒性偶联物之一，以及杀死所选细胞群的方法，包括将靶细胞或含有组织的靶细胞与有效量的一种细胞毒性缀合物，也被披露。

52. 发明申请

US20030229148A1 2-aminotetralines, a process for their preparation, and pharmaceutical compositions, for the prevention and therapeutic treatment of inflammatory and/or autoimmune pathologies 审中-公开
公开(公告)号：US20030229148A1
公开(公告)日：2003-12-11
申请号：US10408122
申请日：2003-04-08
申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
发明人： Nicola Fanto , Gian Piero Moretti , Piero Foresta
IPC分类号： A61K031/7024 , A61K031/513 , A61K031/135 , A61K031/205 , C07C215/46
CPC分类号： C07C215/64 , C07C217/74 , C07C225/20
摘要： 2-Aminotetralines, a process for their preparation, and pharmaceutical compositions, for the prevention and therapeutic treatment of inflammatory pathologies (particularly septic shock) and/or autoimmune pathologies in which the aetiopathogenic role of inflammatory cytokines has been ascertained.

53. 发明申请

US20030220270A1 Mono-and disaccharide derivatives 审中-公开
公开(公告)号：US20030220270A1
公开(公告)日：2003-11-27
申请号：US10148441
申请日：2002-10-07
发明人： Lucas Alfonsus T. Hilgers , Anneke Georgine Blom
IPC分类号： A61K031/7024 , C07H013/02
CPC分类号： C07H13/06 , A61K9/0019 , A61K39/39 , A61K47/26
摘要： The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

54. 发明申请

US20030219494A1 Compositions and methods of using them 审中-公开
标题翻译：组合和使用方法
公开(公告)号：US20030219494A1
公开(公告)日：2003-11-27
申请号：US10393050
申请日：2003-03-20
发明人： Maree Therese Smith , Lindsay Charles Brown , Mark Bradford Pullar Harvey , Craig McKenzie Williams
IPC分类号： A61K033/00 , A61K031/704 , A61K031/7024 , A61K031/485 , A61K031/198 , A61K031/21
CPC分类号： C07D489/08 , A61K31/00 , A61K31/137 , A61K47/55 , C07D489/04
摘要： The present invention is directed to compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention relates to the use of a compound which either directly or indirectly prevents, attenuates or reverses the development of reduced opioid sensitivity, together with a compound which activates the opioid receptor that is the subject of the reduced opioid sensitivity, in methods and compositions for the prevention or alleviation of pain, especially in neuropathic conditions and even more especially in peripheral neuropathic conditions such as painful diabetic neuropathy (PDN).
摘要翻译：本发明涉及用于诱导，促进或以其它方式促进疼痛缓解的组合物和方法。更具体地说，本发明涉及直接或间接地防止，减弱或逆转阿片样物质降低敏感性的发展的化合物与激活作为降低的阿片样物质敏感性的受试者的阿片受体的化合物的用途，在用于预防或减轻疼痛的方法和组合物，特别是在神经病学条件下，甚至更特别是在周围神经病症状如疼痛性糖尿病性神经病变（PDN）中。

55. 发明申请

US20030211113A1 Induction of antigen specific immunologic tolerance 失效
公开(公告)号：US20030211113A1
公开(公告)日：2003-11-13
申请号：US10141668
申请日：2002-05-06
发明人： Emil D. Kakkis , Merry Passage , Thomas Lester , Rebecca Q Yang , Christopher Tanaka
IPC分类号： A61K039/00 , A61K031/522 , A61K038/13 , A61K031/7024
CPC分类号： A61K39/00 , A61K31/522 , A61K31/7024 , A61K38/00 , A61K38/11 , A61K38/13 , A61K2300/00
摘要： Antigen specific immune tolerance is induced in a mammalian host by administration of a toleragen in combination with a regimen of immunosuppression. The methods optionally include a preceding conditioning period, where immunosuppressive agents are administered in the absence of the toleragen. After the tolerizing regimen, the host is withdrawn from the suppressive agents, but is able to maintain specific immune tolerance to the immunogenic epitopes present on the toleragen. Optimally, the toleragen will have high uptake properties that allow uptake in vivo at low concentrations in a wide variety of tolerizing cell types.

56. 发明申请

US20030206895A1 Antioxidant composition comprising propionyl L-carnitine and a flavonoid against throm-bosis and atherosclerosis 审中-公开
标题翻译：抗氧化剂组合物包含丙酰基左旋肉碱和类黄酮抗血栓形成和动脉粥样硬化
公开(公告)号：US20030206895A1
公开(公告)日：2003-11-06
申请号：US10453787
申请日：2003-06-04
申请人： Sigma-Tau HealthScience S.p.A.
发明人： Claudio Cavazza
IPC分类号： A61K038/43 , A61K031/7048 , A61K031/7024 , A61K031/198
CPC分类号： A61K31/35 , A23L33/105 , A23L33/15 , A23L33/165 , A23V2002/00 , A61K31/70 , A61K2300/00 , A23V2250/0612 , A23V2250/2116 , A23V2250/70 , A23V2250/211 , A23V2250/1612 , A23V2250/156 , A23V2250/0622 , A23V2250/0632 , A23V2250/708 , A23V2250/314 , A23V2250/712
摘要： A composition is disclosed which comprises as characterizing active ingredients propionyl L-carnitine and a flavonoid, typically quercetin or its 3-rutinoside, rutin, for the prevention and/or therapeutic treatment of various alterations and pathological states induced by free radicals and by thrombotic or atherosclerotic abnormalities, that may take the form of a dietary supplement, dietetic support or of an actual medicine.
摘要翻译：公开了一种组合物，其包含作为表征活性成分丙酰L-肉毒碱和类黄酮，通常为槲皮素或其3-芸香苷，芦丁，用于预防和/或治疗治疗由自由基诱导的各种改变和病理状态以及血栓形成或/ 动脉粥样硬化异常，可能采取膳食补充剂，饮食支持或实际药物的形式。

57. 发明申请

US20030191070A1 Medical composition kit for treating lesioned abnormal tissue 有权
标题翻译：用于治疗病变异常组织的药物组合试剂盒
公开(公告)号：US20030191070A1
公开(公告)日：2003-10-09
申请号：US10297278
申请日：2002-12-31
发明人： Kinuko Oku , Takako Iwamoto , Takashi Ono
IPC分类号： A61K031/7024 , A61K031/24 , A61K033/06
CPC分类号： A61K33/06 , A61K9/0031 , A61K31/167 , A61K31/245 , A61K31/70 , A61K31/165 , A61K2300/00
摘要： Optimum compounding composition of a local injection preparation for treating rectal submucous lesioned abnormal tissue with local anesthetic is decided to provide a medical composition kit. In a composition kit for the treatment where respective containers are unsealed upon being used and respective contents are mixed to obtain a preparation for injection, a medical composition kit which is characterized in that respective single doses of a therapeutic preparation and local anesthetic are fractionally charged in containers, the said therapeutic preparation contains 1null10% of a water-soluble aluminum compound and 0.01null2% of tannic acid and the said local anesthetic contains 0.1null1% of lidocaine hydrochloride or 0.5null5% of procaine hydrochloride.
摘要翻译：决定用局部麻醉剂治疗直肠粘膜下损伤的异常组织的局部注射制剂的最佳配混组合物，以提供药物组合物试剂盒。在用于治疗的组合物试剂盒中，其中各个容器在使用时是非密封的，并且各自的内容物被混合以获得注射制剂，该药物组合物试剂盒的特征在于，将单个剂量的治疗制剂和局部麻醉剂分批装入容器，所述治疗剂含有1〜10％的水溶性铝化合物和0.01〜2％的单宁酸，所述局部麻醉剂含有0.1〜1％的盐酸利多卡因或0.5〜5％的盐酸普鲁卡因。

58. 发明申请

US20030175834A1 Polyphenol inhibition of nucleoside diphosphate kinase-B activity and cancer metastasis 失效
标题翻译：多酚抑制核苷二磷酸激酶-B活性和癌转移
公开(公告)号：US20030175834A1
公开(公告)日：2003-09-18
申请号：US10331375
申请日：2002-12-30
发明人： Iain Buxton
IPC分类号： G01N033/574 , A61K031/7048 , A61K031/353 , A61K031/7024
CPC分类号： A61K31/353 , A61K31/366 , A61K31/7024 , A61K31/7048 , C12Q1/485 , G01N2333/91235 , G01N2500/02 , G01N2500/04
摘要： Aggressive human tumor cells from disparate tissues were found to secrete nucleoside diphosphate kinase-B (NDPK-B) as a phosphoprotein into the extracellular environment. The secreted enzyme was capable of trasphosphorylation activity in the absence of a phosphoryl donor, thereby producing elevated level of extracellular ATP that plays a significant role in angiogenesis required for the growth of cancer cells and cancer metastasis. A series of structurally related non-nucleotide anticancer compounds such as ellagic acid (EA), epigallocatechin gallate (EGCG), and epicatechin gallate (ECG) were found to inhibit the activity of secreted nucleoside diphosphate kinase-B as well as angiogenesis. The nucleoside diphosphate kinase-B inhibition data disclosed herein can be used in predicative models to design novel inhibitors of nucleoside diphosphate kinase-B activity.
摘要翻译：发现来自不同组织的侵袭性人肿瘤细胞将核苷二磷酸激酶-B（NDPK-B）作为磷蛋白分泌到细胞外环境中。分泌的酶能够在不存在磷酰基供体的情况下具有磷酸化活性，从而产生升高的细胞外ATP水平，其在癌细胞生长所需的血管发生和癌症转移中起重要作用。发现一系列结构相关的非核苷酸抗癌化合物如鞣花酸（EA），表没食子儿茶素没食子酸酯（EGCG）和表儿茶素没食子酸酯（ECG），抑制分泌的核苷二磷酸激酶B的活性以及血管生成。本文公开的核苷二磷酸激酶-B抑制数据可用于预测模型以设计核苷二磷酸激酶-B活性的新型抑制剂。

59. 发明申请

US20030147937A1 Use of compatible solutes as substances having free radical scavenging properties 审中-公开
标题翻译：使用相容性溶质作为具有自由基清除性质的物质
公开(公告)号：US20030147937A1
公开(公告)日：2003-08-07
申请号：US10257225
申请日：2003-01-21
发明人： Thomas Schwarz
IPC分类号： A61K048/00 , A61K038/00 , A61K031/7024 , A61K031/66
CPC分类号： A61K31/661 , A61K31/66 , A61K31/6615 , A61K2300/00
摘要： The invention relates to the use of compatible solutes selected from the group comprised of di-myo-inositol phosphate (DIP), cyclic 2,3 diphosphoglycerate (cDPG), 1,1-di-glyccrol phosphate (DGP), null-mannosylglycerate (firoin) null-mannosylglyceramide (firoin-A) and/or di-mannosyl-di-inositol phosphate (DMIP) and/or of derivatives of these compounds or combinations thereof for protecting organisms, organs, tissues, cells or the organic building blocks thereof from chemical radicals and oxidatively active compounds.
摘要翻译：本发明涉及使用选自二肌酸磷酸肌酸（DIP），环状2,3-二磷酸甘油酸（cDPG），1,1-二糖磷酸（DGP），β-甘露糖基甘油酸酯（DGP） firoin）β-甘露糖基甘油酰胺（firoin-A）和/或二 - 甘露糖基 - 二 - 肌醇磷酸酯（DMIP）和/或这些化合物的衍生物或其组合，用于保护生物，器官，组织，细胞或其有机结构单元来自化学自由基和氧化活性化合物。

60. 发明申请

US20030130207A1 Use of borate-polyol complexes in ophthalmic compositions 失效
公开(公告)号：US20030130207A1
公开(公告)日：2003-07-10
申请号：US10302294
申请日：2002-11-22
发明人： Masood Chowhan , Nissanke L. Dassanayake
IPC分类号： A61K031/7024 , A61K031/69
CPC分类号： A61K9/0048 , Y10S134/901 , Y10S514/812 , Y10S514/839 , Y10S514/84 , Y10S514/912 , Y10S514/915
摘要： Water-soluble borate-polyol complexes are useful as buffers and/or antimicrobials in aqueous ophthalmic compositions, including those containing polyvinyl alcohol. These compositions have greater antimicrobial activity than comparable compositions containing typical borate buffers and unexpectedly increase the antimicrobial efficacy of other antimicrobial agents when used in combination. In addition, use of the borate-polyol complexes avoids the incompatibility problem typically associated with the combination of borate buffer and polyvinyl alcohol; therefore, the compositions disclosed herein may also contain polyvinyl alcohol.

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