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41. 发明申请

US20060160906A1 Polyamine analogs as therapeutic agents for ocular diseases 审中-公开
标题翻译：多胺类似物作为眼部疾病的治疗剂
公开(公告)号：US20060160906A1
公开(公告)日：2006-07-20
申请号：US11244095
申请日：2005-10-04
申请人： Laurence Marton , Sterling Haidt , Peter Campochiaro
发明人： Laurence Marton , Sterling Haidt , Peter Campochiaro
IPC分类号： A61K31/13
CPC分类号： A61K31/132 , A61K31/13 , A61K31/133 , A61K31/135 , A61K31/198 , A61K31/395
摘要： This disclosure relates to methods of treating ocular diseases using polyamine analogs, particularly conformationally restricted polyamine analogs. The ocular diseases to be treated include a variety of ophthalmic disorders characterized by angiogenesis and/or neovascularization, including macular degeneration. Both wet macular degeneration and dry macular degeneration can be treated using the methods of the invention. The invention also provides ophthalmic formulations, including sustained release formulations and sustained release devices.
摘要翻译：本公开涉及使用多胺类似物，特别是构象限制的多胺类似物治疗眼部疾病的方法。待治疗的眼部疾病包括以血管生成和/或新血管形成为特征的各种眼科疾病，包括黄斑变性。可以使用本发明的方法治疗湿性黄斑变性和干性黄斑变性。本发明还提供眼用制剂，包括缓释制剂和持续释放装置。

42. 发明授权

US07045550B2 Polyamines and analogs for protecting cells during cancer chemotherapy and radiotherapy 有权
公开(公告)号：US07045550B2
公开(公告)日：2006-05-16
申请号：US10214917
申请日：2002-08-07
申请人： William E. Fahl , John Kink
发明人： William E. Fahl , John Kink
IPC分类号： A61K31/195 , A61K31/13
CPC分类号： A61Q7/00 , A61K8/41 , A61K9/127 , A61K31/132 , A61K31/198 , A61K45/06 , B82Y5/00 , A61K2300/00
摘要： Polyamine effectors are administered locally to provide protection against the adverse side-effects of chemotherapy or radiation therapy, such as alopecia, mucositis and dermatitis. Pharmaceutical preparations comprising one or more polyamine effectors formulated for topical or local delivery to epithelial or mucosal cells are disclosed. Methods of administering the pharmaceutical preparations are also disclosed.

43. 发明授权

US07026514B2 Compounds used to treat alcoholism 失效
标题翻译：用于治疗酒精中毒的化合物
公开(公告)号：US07026514B2
公开(公告)日：2006-04-11
申请号：US10482708
申请日：2002-07-01
申请人： Norberto Bilbeny Lojo , Hernan Garcia Madrid , Maria Belen Font Arellano
发明人： Norberto Bilbeny Lojo , Hernan Garcia Madrid , Maria Belen Font Arellano
IPC分类号： C07C211/36 , C07C233/08 , A61K31/132 , A61P25/32
CPC分类号： A61K31/132 , C07C211/36 , C07C2601/14
摘要： N,N′-bis(3-aminopropyl)cyclohexane-1,4-diamine, of formula (I), is a new compound that is prepared by hydrogenation with Raney nickel catalyst of N,N′-bis(2-cyanoethyl)-cyclohexane-1,4-diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of the tetrametanesulfonate monohydrate of (I) causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself. Therefore, the compounds of the invention are useful for the preparation of medicaments for the therapeutic and/or prophylactic treatment of alcoholism in mammals, including human beings
摘要翻译：式（I）的N，N'-双（3-氨基丙基）环己烷-1,4-二胺是一种新的化合物，其通过用阮内镍催化剂N，N'-双（2-氰基乙基） - 环己烷-1,4-二胺，后者通过1,4-环己烷二胺和丙烯腈之间的反应制备。对（I）的四磺酸一水合物的遗传酒精大鼠（来自智利大学的UCHB菌株）的口服给药导致酒精消耗的显着降低。治疗期间活动持续一段时间。此外，存在几乎无效的双硫仑样副作用，与某些抗酒精中毒药如氨基氰胺氰胺或双硫仑本身不利的使用相比，具有什么优势。因此，本发明的化合物可用于制备用于治疗和/或预防哺乳动物，包括人类中的酒精中毒的药物

44. 发明申请

US20050159364A1 Copper antagonist compounds 审中-公开
标题翻译：铜拮抗剂化合物
公开(公告)号：US20050159364A1
公开(公告)日：2005-07-21
申请号：US11018720
申请日：2004-12-20
申请人： Garth Cooper
发明人： Garth Cooper
IPC分类号： A61K9/70 , A61K31/00 , A61K31/132 , A61K31/195 , A61K31/47 , A61K31/66 , A61K38/04
CPC分类号： A61K31/00 , A61K9/7023 , A61K31/132
摘要： Copper antagonist compounds and the use of such compounds in methods for the treatment, prevention, or amelioration of various disorders that would be benefited by reduction in copper, for example copper (II), including neurodegenerative and other disorders.
摘要翻译：铜拮抗剂化合物以及这些化合物在治疗，预防或改善可通过还原铜（例如铜（II））而受益的各种疾病的方法中的应用，包括神经退行性疾病和其他疾病。

45. 发明申请

US20040162287A1 Substituted cyclohexane-1,4-diamine compounds 有权
标题翻译：取代的环己烷-1,4-二胺化合物
公开(公告)号：US20040162287A1
公开(公告)日：2004-08-19
申请号：US10704329
申请日：2003-11-10
申请人： GRUENENTHAL GmbH
发明人： Bernd Sundermann , Hagen-Heinrich Hennies , Werner Englberger , Babette-Yvonne Koegel
IPC分类号： A61K031/537 , A61K031/495 , A61K031/445 , A61K031/40
CPC分类号： A61K31/38 , A61K31/13 , A61K31/132 , A61K31/165 , A61K31/404 , A61K31/425
摘要： Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
摘要翻译：取代的环己烷-1,4-二胺化合物，其制备方法，包含这些化合物的药物组合物和使用这些化合物的治疗方法。

46. 发明授权

US06656912B2 Methods to treat &agr;1-antitrypsin deficiency 有权
公开(公告)号：US06656912B2
公开(公告)日：2003-12-02
申请号：US09768029
申请日：2001-01-22
申请人： David H. Perlmutter , Nancy Marcus
发明人： David H. Perlmutter , Nancy Marcus
IPC分类号： A61K3170
CPC分类号： A61K31/00 , A61K31/132 , A61K31/192 , A61K31/437 , A61K31/70 , A61K31/7008
摘要： Inhibitors of glucosidase, especially those related to castanospermine, are effective in preventing or ameliorating conditions such as liver damage and emphysema that are present in individuals who produce a mutant form of antitrypsin, &agr;1-ATZ. Also effective in the method of the invention are imino sugars and their reduced forms in general as well as phenylbutyric acid. These compounds enhance the secretion of the mutant form, which retains substantial biological activity, and do not impair its degradation in the endoplasmic reticulum.

47. 发明申请

US20030195377A1 Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor 失效
标题翻译：用于癌症治疗的环烷基取代多胺及其合成方法
公开(公告)号：US20030195377A1
公开(公告)日：2003-10-16
申请号：US10313530
申请日：2002-12-06
申请人： SLIL Biomedical Corporation
发明人： Benjamin Frydman , Aldonia L. Valasinas , Andrei V. Blokhin , Aparajita Sarkar , Hirak S. Basu , Venodhar K. Reddy , Laurence J. Marton , Yu Wang
IPC分类号： C07C211/17
CPC分类号： A61K31/132 , C07C211/18 , C07C2601/02
摘要： Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
摘要翻译：公开了可用于治疗由异常细胞增殖表现的癌症和其它疾病的构象限制性多胺化合物。还公开了合成这些化合物的改进方法。在本发明的一种方法中，含有含碳或含碳原子的化合物与烯烃化合物的双键反应形成环丙基环作为合成中的第一步。

48. 发明申请

US20030194746A1 Methods and means relating to atherosclerosis 失效
标题翻译：与动脉粥样硬化有关的方法和手段
公开(公告)号：US20030194746A1
公开(公告)日：2003-10-16
申请号：US10225461
申请日：2002-08-22
发明人： Ivan Petyaev
IPC分类号： G01N033/53
CPC分类号： G01N33/92 , A61K31/047 , A61K31/132 , A61K31/145 , A61K31/16 , A61K31/166 , A61K31/185 , A61K31/195 , A61K31/198 , A61K31/222 , A61K31/341 , A61K31/351 , A61K31/352 , A61K31/355 , A61K31/4025 , A61K31/409 , A61K31/4709 , A61K31/5383 , A61K31/7048 , A61K39/118 , C07K16/18 , C12N9/0002 , C12Q1/25 , G01N33/56927 , G01N33/6854 , G01N33/6893 , G01N2500/00 , G01N2500/04 , G01N2800/323
摘要： The present invention relates to the identification of lipid oxidising antibodies as a key pathogenic factor in atherosclerotic disorders. The presence of such antibodies is a important marker for the diagnosis and prognosis of such disorders and methods and means for the assessment of athersclerotic conditions are provided herein.
摘要翻译：本发明涉及将脂质氧化抗体鉴定为动脉粥样硬化性疾病中的关键致病因子。这种抗体的存在是这种疾病的诊断和预后的重要标志物，本文提供了用于评估非衰老病症的方法和手段。

49. 发明申请

US20020142995A1 Ammonium salts of hemoglobin allosteric effectors, and uses thereof 审中-公开
标题翻译：血红蛋白变构效应物的铵盐及其用途
公开(公告)号：US20020142995A1
公开(公告)日：2002-10-03
申请号：US09920310
申请日：2001-08-01
发明人： Yves Claude Nicolau , Jaime E. Lazarte , Dennis R. Alford
IPC分类号： A61K031/663 , C07F009/02
CPC分类号： C07F9/117 , A61K31/132 , A61K31/661 , A61K31/6615 , A61K31/663 , C07F9/093 , A61K2300/00
摘要： The present invention comprises compounds, compositions thereof, and methods capable of delivering a broad range of anionic molecules to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering a ligand for the allosteric site of hemoglobin to the cytoplasm of the red blood cells.
摘要翻译：本发明包括化合物，其组合物和能够将广泛范围的阴离子分子递送至哺乳动物细胞的细胞质的方法。在某些实施方案中，本发明涉及通过将血红蛋白的变构位点的配体递送至红细胞的细胞质来提高哺乳动物红细胞传递氧的能力的化合物，其组合物和方法。

50. 发明授权

US06274630B1 Method of inhibiting biosynthesis of EIf5A 失效
标题翻译：抑制EIf5A生物合成的方法
公开(公告)号：US06274630B1
公开(公告)日：2001-08-14
申请号：US08928492
申请日：1997-09-12
申请人： Raymond J. Bergeron, Jr.
发明人： Raymond J. Bergeron, Jr.
IPC分类号： A61K3113
CPC分类号： A61K31/506 , A61K31/131 , A61K31/132 , A61K31/785
摘要： A method and pharmaceutical composition for inhibiting or preventing the intracellular biosynthesis of EIf5A by the administration to a human or non-human mammal in need thereof an amount of a polyamine analogue or salt thereof sufficient to deplete the supply of intracellular spermidine required for EIf5A biosynthesis.
摘要翻译：一种用于通过向有需要的人或非人哺乳动物给药来抑制或预防EIf5A的细胞内生物合成的方法和药物组合物，其量足以耗尽EIf5A生物合成所需的细胞内亚精胺的供应。

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