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51. 发明申请

US20040180842A1 4"-substituted-9-deoxo-9A-AZA-9A-homoerythromycin a derivatives 有权
标题翻译： 4“ - 取代-9-脱氧-9A-AZA-9A-高红霉素a衍生物
公开(公告)号：US20040180842A1
公开(公告)日：2004-09-16
申请号：US10810922
申请日：2004-03-26
申请人： Pfizer Inc
发明人： Brian Scott Bronk , Michael Anthony Letavic , Takushi Kaneko , Bingwei Vera Yang , Edward Alan Glazer , Hengmiao Cheng
IPC分类号： C07H017/08 , A61K031/7052
CPC分类号： C07H17/08 , Y02P20/55
摘要： The invention relates to a method of preparing compounds of the formula 1 and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
摘要翻译：本发明涉及一种制备下式化合物及其药学上可接受的盐的方法。式1的化合物是可用于治疗各种细菌和原生动物感染的抗菌剂。本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌原生动物感染的方法。本发明还涉及制备式1化合物的方法和用于此类制备的中间体。

52. 发明申请

US20040132673A1 Clathrate of azithromycin hydrate with 1,2-propyleneglycol, method for the manufacture thereof and pharmaceutical composition comprising same 失效
标题翻译：阿奇霉素水合物与1,2-丙二醇的包合物，其制备方法和包含其的药物组合物
公开(公告)号：US20040132673A1
公开(公告)日：2004-07-08
申请号：US10476016
申请日：2003-10-23
发明人： Kwee-Hyun Suh , Gi-Jeong Kim , Sang-Min Yoon , Mi-Ra Seong , Gwan-Sun Lee
IPC分类号： A61K031/7052
CPC分类号： C07D413/14 , A61K31/7028
摘要： A clathrate of azithromycin hydrate with 1,2-propyleneglycol is much less hygroscopic than azithromycin hydrate or crystals known in the art, therefore, it can be useful for the preparation of a medicine for treating various microbial infections.
摘要翻译：具有1,2-丙二醇的阿奇霉素水合物的包合物比本领域已知的阿奇霉素水合物或晶体吸湿性好得多，因此可用于制备用于治疗各种微生物感染的药物。

53. 发明申请

US20040053857A1 Glycoalkaloid compositions and various uses thereof 审中-公开
标题翻译：糖类生物碱组合物及其各种用途
公开(公告)号：US20040053857A1
公开(公告)日：2004-03-18
申请号：US10607890
申请日：2003-06-27
申请人： SOLBEC PHARMACEUTICALS LIMITED
发明人： Stephen John Carter , Elizabeth Williams
IPC分类号： A61K031/7052 , A61K031/58
CPC分类号： A61K31/58 , A61K31/704 , A61K31/7052
摘要： A composition comprising at least two glycoalkaloids of formula I: 1 wherein: either one or both of the dotted lines represents a double bond, and the other a single bond, or both represent single bonds; A: represents a radical selected from the following radicals of general formulae (II) to (V): 2 each of R1 is a radical separately selected from the group consisting of hydrogen, amino, oxo and OR4; each of R2 is a radical separately selected from the group consisting of hydrogen, amino and OR4; each of R3 is a radical separately selected from the group consisting of hydrogen, carbohydrate and a carbohydrate derivative; nullXnull is a radical selected from the group comprising nullCH2null, nullOnull and nullNH2null; and wherein the compound includes at least one R4 group that is a carbohydrate or a derivative thereof selected from the group comprising glyceric aldehyde, glycerose, erythrose, threose, ribose, arabinose, xylose, lyxose, altrose, allose, gulose, mannose, glucose, idose, galactose, talose, rhamnose, dihydroxyactone, erythrulose, ribulose, xylulose, psicose, fructose, sorbose, tagatose, and other hexoses, heptoses, octoses, nanoses, decoses, deoxysugars with branched chains, (e.g. apiose, hamamelose, streptose, cordycepose, mycarose and cladinose), compounds wherein the aldehyde, ketone or hydroxyl groups have been substituted (e.g. N-acetyl, acetyl, methyl, replacement of CH2OH), sugar alcohols, sugar acids, benzimidazoles, the enol salts of the carbohydrates, saccharinic acids, sugar phosphates; wherein the ratio of said glycoalkaloids is between 6:1 and 1:6 and on the proviso that when the glycoalkaloids are solamargine and solasonine and they are present in a 1:1 ratio the solamargine and solasonine are isolated.
摘要翻译：一种组合物，其包含至少两种式I的生物碱：其中：虚线中的一个或两个表示双键，而另一个单键或两者均表示单键; A：表示选自以下通式（II）至（V）的基团的基团：R 1各自独立地选自氢，氨基，氧代和OR 4; R 2中的每一个是分别选自氢，氨基和OR 4的基团。 R 3中的每一个是分别选自氢，碳水化合物和碳水化合物衍生物的基团; “X”是选自-CH 2 - ， - O-和-NH 2 - 的基团; 并且其中所述化合物包括至少一个R 4基团，其为选自甘油醛，甘油糖，赤藓糖，苏糖，核糖，阿拉伯糖，木糖，莱克糖，阿卓糖，阿洛糖，古洛糖，甘露糖的碳水化合物或其衍生物，葡萄糖，偶氮，半乳糖，罗糖，鼠李糖，二羟基内酯，赤藓酮糖，核酮糖，木酮糖，灵芝蛋白，果糖，山梨糖，塔格糖和其他己糖，肝素，辛酸，纳米，脱衣剂，具有支链的脱氧糖（例如阿糖，链烷烃，冬虫夏草，麦考罗糖和分裂蛋白），其中醛，酮或羟基已经被取代的化合物（例如N-乙酰基，乙酰基，甲基，CH 2 OH的取代基），糖醇，糖酸，苯并咪唑，碳水化合物的烯醇盐，糖精，糖磷酸盐; 其中所述糖生物碱的比例在6:1至1:6之间，并且条件是当糖生物碱为solamargine和solasonine并且它们以1:1的比例存在时，分离出solamargine和solasonine。

54. 发明申请

US20040043990A1 Method of treatment 审中-公开
标题翻译：治疗方法
公开(公告)号：US20040043990A1
公开(公告)日：2004-03-04
申请号：US10410311
申请日：2003-04-09
发明人： Karen Jackson
IPC分类号： A61K031/7052 , A61K031/5513 , A61K031/485
CPC分类号： A61K31/485 , A61K31/5513 , A61K2300/00
摘要： There is described a method of treatment of a patient requiring analgesic therapy which comprises the administration of an analgesically effective amount of devazepide. There is also described the use of devazepide in the manufacture of an analgesically effective medicament.
摘要翻译：描述了需要镇痛治疗的患者的治疗方法，该方法包括给予镇痛有效量的他扎昔肽。还描述了devazepide在制造止痛有效药物中的用途。

55. 发明申请

US20040033962A1 Novel prodrugs von 6-hydroxy-2,3-dihydro-1h-indoles, 5-hydroxy-1,2-dihydro-3h-pyrrolo[3,2-e]indoles and 5-hydroxy-1,2-dihydro-3h-benzo(e)indoles as well as of 6-hydroxy-1,2,3,4-tetrahydro-benzo[f]quinoline derivatives for use in selective cancer therapy 失效
标题翻译：新型前药von 6-羟基-2,3-二氢-1H-吲哚，5-羟基-1,2-二氢-3H-吡咯并[3,2-e]吲哚和5-羟基-1,2-二氢-3h - 苯并（e）吲哚以及用于选择性癌症治疗的6-羟基-1,2,3,4-四氢 - 苯并[f]喹啉衍生物
公开(公告)号：US20040033962A1
公开(公告)日：2004-02-19
申请号：US10275415
申请日：2003-06-30
发明人： Lutz F. Tietze , Tobias Herzig , Anja Fecher
IPC分类号： A61K031/7052 , A61K031/407 , A61K031/404 , C07H017/02 , C07D209/52 , C07D209/04
CPC分类号： C07D487/04 , C07D209/60 , C07H17/02
摘要： The chemotherapy of malignant tumours is greatly restricted by the generally slight differentiation of the available cytostatic agents between normal and malignant tissue. In order to achieve an improvement of the selectivity in cancer therapy, novel prodrugs have been developed from 6-hydroxy-2,3-dihydro-1H-indolene, 5-hydroxy-1,2-dihydro-3H-pyrrolonull3,2-enullindolene and 5-hydroxy-1,2-dihydro-3H-benzonullenullindolene as well as from 6-hydroxy-1,2,3,4-tetrahydro-benzonullfnull-quinolines, that may be used within the framework of the ADEP therapy (antibody directed enzyme prodrug therapy). The new prodrugs are characterised by a high difference in toxicity between the prodrug and underlying drug and by a very high efficacy of the drug. The high selectivity of the new prodrugs is probably attributed to the fact that, in the new prodrugs, a secondary halide is present in contrast to the prodrugs of a similar type previously produced by us. The direct alkylation of the DNA or RNA by the prodrugs and thus the toxicity of the prodrugs is thereby reduced. After splitting off of the glycosidic and/or acetal group on the phenolic hydroxy groups of the prodrugs, a spirocyclopropacyclohexadiene is formed which, being a highly toxic group, effects an alkylation of the DNA or RNA.
摘要翻译：恶性肿瘤的化学疗法受到正常组织和恶性组织中可用的细胞生长抑制剂通常轻微分化的限制。为了实现癌症治疗中选择性的提高，已从6-羟基-2,3-二氢-1H-吲哚，5-羟基-1,2-二氢-3H-吡咯并[3,2 -e]吲哚烯和5-羟基-1,2-二氢-3H-苯并[e]吲哚以及6-羟基-1,2,3,4-四氢 - 苯并[f] - 喹啉，其可以是在ADEP治疗（抗体定向酶前药治疗）的框架内使用。新的前体药物的特征在于前药和潜在药物之间毒性的高度差异以及药物的非常高的功效。新前体药物的高选择性可能归因于以下事实：在新的前药中，与之前由我们生产的类似物质的前药相反，存在二卤化物。由前药直接烷基化DNA或RNA，从而减少前药的毒性。在前药的酚羟基上分离出糖苷和/或缩醛基团之后，形成螺环丙烯环己二烯，其是高毒性基团，从而影响DNA或RNA的烷基化。

56. 发明申请

US20040023898A1 Single dose azithromycin 失效
标题翻译：单次剂量阿奇霉素
公开(公告)号：US20040023898A1
公开(公告)日：2004-02-05
申请号：US10628102
申请日：2003-07-25
发明人： Michael William Dunne
IPC分类号： A61K031/7052
CPC分类号： A61K31/7052
摘要： The present invention relates to a method of treating infections in humans by administering a single dose of azithromycin.
摘要翻译：本发明涉及通过施用单次阿奇霉素来治疗人的感染的方法。

57. 发明申请

US20040018995A1 Derivatives of monosaccharides as cell adhesion inhibitors 审中-公开
公开(公告)号：US20040018995A1
公开(公告)日：2004-01-29
申请号：US10611091
申请日：2003-07-01
发明人： Sudershan K. Arora , Jang Bahadur Gupta , Vishwas D. Joshi
IPC分类号： A61K031/7052 , A61K031/7024 , C07H005/06
CPC分类号： C07H9/04
摘要： This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-null-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-null-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

58. 发明申请

US20040009930A1 Macrolide antibiotics 失效
标题翻译：大环内酯抗生素
公开(公告)号：US20040009930A1
公开(公告)日：2004-01-15
申请号：US10454354
申请日：2003-06-03
申请人： Pfizer Inc.
发明人： Wei-Guo Su , Yan Chen
IPC分类号： A61K031/7052 , A61K031/7048 , C07H017/08
CPC分类号： C07H17/08 , C07H17/00
摘要： A macrolide antibiotic of the formula 1 wherein the variables are defined as described herein.
摘要翻译：下式的大环内酯抗生素，其中变量如本文所述定义。

59. 发明申请

US20030220272A1 6-O-acyl ketolide antibacterials 有权
标题翻译： 6-O-酰基酮内酯抗菌剂
公开(公告)号：US20030220272A1
公开(公告)日：2003-11-27
申请号：US10301412
申请日：2002-11-21
发明人： Todd C. Henninger , Mark J. Macielag , Manomi A. Tennakoon , Xiaodong Xu
IPC分类号： A61K031/7048 , A61K031/7052 , C07H017/08
CPC分类号： C07D498/04 , C07H17/08
摘要： 6-O-Acyl ketolide antibacterials of the formula: 1 wherein R1, R2, R3, R4, W, X, Xnull, Y, and Ynull are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
摘要翻译：具有下式的6-O-酰基酮内酯抗菌剂：其中R 1，R 2，R 3，R 4，W，X，X'，Y和Y'如本文所述，其中取代基具有在说明书中指出。这些化合物可用作抗菌剂。

60. 发明申请

US20030203923A1 Method of inhibiting neurotrophin-receptor binding 审中-公开
标题翻译：抑制神经营养因子受体结合的方法
公开(公告)号：US20030203923A1
公开(公告)日：2003-10-30
申请号：US10205601
申请日：2002-07-26
发明人： Gregory M. Ross , Egor L. Shamovsky , Sandra Marone , Donald F. Weaver , Richard J. Riopelle
IPC分类号： A61K031/7052 , A61K031/519
CPC分类号： C07D221/14 , A61K31/00 , A61K31/473 , A61K31/4745
摘要： The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.
摘要翻译：本发明涉及抑制神经生长因子与p75 常见的神经营养因子受体的结合的组合物及其使用方法。在一个实施方案中，抑制神经生长因子与p75 的结合的化合物特别包括当与神经生长因子结合时，包含以下至少两种：（1）位于与Lys相互作用的第一电负性原子或官能团 <34>神经生长因子; （2）定位为与神经生长因子的Lys 95相互作用的第二电负性原子或官能团; （3）定位为与神经生长因子的Lys <88>相互作用的第三电负性原子或官能团; （4）定位为与神经生长因子的Lys 32相互作用的第四电负性原子或官能团; 和（5）疏水部分，其与由神经生长因子的Ile 31，Phe 101和Phe 86形成的疏水区相互作用。

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