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31. 发明申请

US20020045607A1 Cholesterol and hedgehog signaling 审中-公开
标题翻译：胆固醇和刺猬信号
公开(公告)号：US20020045607A1
公开(公告)日：2002-04-18
申请号：US09954727
申请日：2001-09-11
申请人： The Johns Hopkins University School of Medicine
发明人： Philip A. Beachy , Jeffrey A. Porter , Michael K. Cooper
IPC分类号： A61K031/58
CPC分类号： A61K31/4355 , Y10S435/962 , Y10T436/141111
摘要： The present invention sterol-modified hedgehog polypeptides and functional fragments thereof. Methods of identifying compositions which affect hedgehog activity based on inhibition of cholesterol modification of hedgehog protein are described. In one aspect of the invention, the method provides a means for affecting cholesterol biosynthesis or transport in a cell comprising contacting a cell with an effective amount of a compound that affects hedgehog, thereby affecting cholesterol biosynthesis or transport. The effect may be inhibition or stimulation of cholesterol biosynthesis or transport.
摘要翻译：本发明固醇修饰的刺猬蛋白多肽及其功能片段。描述了基于对刺猬蛋白胆固醇修饰的抑制影响刺猬蛋白活性的组合物的方法。在本发明的一个方面，该方法提供了影响细胞中胆固醇生物合成或转运的方法，包括使细胞与有效量的影响刺猬蛋白的化合物接触，从而影响胆固醇生物合成或转运。该作用可能是抑制或刺激胆固醇生物合成或运输。

32. 发明申请

US20040248868A1 Phophylactic and therapeutic use of hydroxysteroids 有权
标题翻译：羟基类固醇的预防和治疗用途
公开(公告)号：US20040248868A1
公开(公告)日：2004-12-09
申请号：US10486499
申请日：2004-07-08
发明人： Ernst Wulfert
IPC分类号： A61K031/58 , A61K031/56
CPC分类号： A61K31/56
摘要： 3-Hydroxy-7-hydroxy steroids and 3-oxo-7-hydroxy steroids, especially the 7null-isomers thereof, and pharmaceutically acceptable esters thereof are useful for protection against ischaemia-induced damage to peripheral organs, such as the heart or kidneys, as well as treatment of spiral cord injury.
摘要翻译： 3-羟基-7-羟基甾族化合物和3-氧代-7-羟基甾族化合物，特别是其七乙酸异构体及其药学上可接受的酯可用于防止局部缺血诱发的对周围器官如心脏或肾脏的损伤，以及治疗螺旋线损伤。

33. 发明申请

US20040248866A1 Novel topical steroid cream formulations 失效
标题翻译：新型局部类固醇霜剂
公开(公告)号：US20040248866A1
公开(公告)日：2004-12-09
申请号：US10849282
申请日：2004-05-19
发明人： Maxine G. Moldenhauer
IPC分类号： A61K031/58
CPC分类号： A61K9/0014 , A61K31/58 , A61K47/06 , A61K47/10
摘要： Disclosed is a novel mometasone furoate cream formulation for topical administration in a oleaginous base containing propylene glycol. This cream is a cosmetically elegant preparation of mometasone that is both stable and bioeffective.
摘要翻译：公开了一种用于在含有丙二醇的含油基质中局部施用的新型莫拉米松糠酸霜剂。这种奶油是一种化妆品优美的莫米松的制剂，既稳定又具有生物有效性。

34. 发明申请

US20040220157A1 Compounds useful in the manufacture of an anti-inflammatory androstane derivative 有权
标题翻译：用于制造消炎雄甾烷衍生物的化合物
公开(公告)号：US20040220157A1
公开(公告)日：2004-11-04
申请号：US10862792
申请日：2004-06-07
发明人： Keith Biggadike , Steven John Coote , Rosalyn Kay Nice
IPC分类号： A61K031/58 , C07J071/00
CPC分类号： A61K31/58 , A61K9/0043 , A61K31/56
摘要： The present invention relates to, for example, compounds of formula (VI) 1 useful in the manufacture of anti-inflammatory androstane derivatives.
摘要翻译：本发明涉及例如可用于制造抗炎雄甾烷衍生物的式（VI）化合物。

35. 发明申请

US20040220115A1 Medicinal compositions and their method of preparation 审中-公开
标题翻译：药物组合物及其制备方法
公开(公告)号：US20040220115A1
公开(公告)日：2004-11-04
申请号：US10752095
申请日：2004-01-07
发明人： Bill E. Cham
IPC分类号： A61K031/7048 , A61K031/58
CPC分类号： A61K31/702 , A61K31/58 , A61K31/704 , A61K31/706
摘要： A medicinal composition comprising at least one compound which can interact with a target cell, the at least one compound being a glycoalkaloid of general formula (I) wherein: the composition is essentially without free sugars of the type which inhibit the interaction between the at least one glycoalkaloid and a target cell.

36. 发明申请

US20040152701A1 Novel anhydrous crystalline form of Levofloxacin and process for preparation there of 审中-公开
标题翻译：左氧氟沙星的新型无水结晶形式及其制备方法
公开(公告)号：US20040152701A1
公开(公告)日：2004-08-05
申请号：US10716207
申请日：2003-11-18
申请人： DR. REDDY'S LABORATORIES LIMITED , DR. REDDY'S LABORATORIES, INC.
发明人： Manne Satyanarayana Reddy , Sajja Eswaraiah , Koppera Ravinder Reddy , Maram Reddy Sahadeva Reddy , Pitta Jaya Prakash
IPC分类号： A61K031/58 , C07D491/02
CPC分类号： C07D498/04
摘要： The present invention is directed to novel anhydrous crystalline form of Levofloxacin is depicted as Formula (I), further more its process for preparation thereof. The process for the preparation of novel anhydrous crystalline form of Levofloxacin comprises the condensation of N-Methyl piperazine with S(null)-9,10-difluoro-7-oxo 2,3-dihydro 7H-pyridonull1,2,3-DEnull null1,4null Benzoxazine-6-carboxylic acid in Acetonitrile followed by distillation of solvent to afford the residue, the resultant residue is refluxed with toluene and the solid is filtered at room temperature to afford the Levofloxacin. Thus resulted Levofloxacin is further refluxed in Acetonitrile and filtered the Novel anhydrous crystalline form of Levofloxacin as undissolved material. The anhydrous crystalline form of Levofloxacin is characterized by X-ray diffractogram, Differential Scanning Calorimetry thermogram and Infrared Spectra. 1
摘要翻译：本发明涉及左氧氟沙星的新型无水结晶形式如式（I）所示，其进一步制备其制备方法。制备新型无水结晶形式的左氧氟沙星的方法包括N-甲基哌嗪与S（ - ） - 9,10-二氟-7-氧代2,3-二氢-7-吡啶并[1,2,3- DE] [1,4]苯并恶嗪-6-羧酸，然后蒸馏除去溶剂，得到残留物，所得残余物与甲苯一起回流，固体在室温下过滤，得到左氧氟沙星。由此导致左氧氟沙星在乙腈中进一步回流，并以新溶剂的形式过滤了左氧氟沙星的新型无水结晶形式。无水结晶形式的左氧氟沙星的特征在于X射线衍射图，差示扫描量热法和红外光谱。

37. 发明申请

US20040152683A1 Use of mometasone furoate for treating airway passage and lung diseases 失效
公开(公告)号：US20040152683A1
公开(公告)日：2004-08-05
申请号：US10763295
申请日：2004-01-22
发明人： Joel A. Sequeira , Francis M. Cuss , Keith B. Nolop , Imtiaz A. Chaudry , Nagamani Nagabhushan , James E. Patrick , Mitchell Cayen
IPC分类号： A61K031/58
CPC分类号： A61K9/008 , A61K9/0043 , A61K9/0075 , A61K31/57 , A61K31/58 , Y10S514/826 , Y10S514/828 , Y10S514/958
摘要： The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

38. 发明申请

US20040138179A1 Antifungal formulations 有权
标题翻译：抗真菌配方
公开(公告)号：US20040138179A1
公开(公告)日：2004-07-15
申请号：US10691928
申请日：2003-10-23
发明人： Jay A. Goldstein , Michael Rothman , Whe-Yong Lo
IPC分类号： A61K031/675 , A61K031/58 , A61K031/4196
CPC分类号： A61Q17/005 , A61K8/63 , A61K9/0014 , A61K31/00 , A61K31/4174 , A61K31/57 , A61K45/06 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/44 , A61Q19/00 , A61K2300/00
摘要： A topical composition and the method using the composition, which contains an antifungal agent and a low potency anti-inflammatory steroid which is safe and effective such as desonide or its derivative. The low potency steroid agent does not cause side effects such as skin atrophy, striae and hypopigmentation. In a representative example, the low potency anti-inflammatory steroid has the following structure: 1 wherein R1, R2, R3, and R4 taken independently can be H, C1-C10 alkyl, C1-C10 alkenyl, C3-C10 cycloalkyl, and phenyl groups; R1 and R2 taken together can be C3-C10 cycloalkyl; and R3, and R4 taken independently can be H, C1-C10 alkyl, C1-C10 alkenyl, C3-C10 cycloalkyl, phenyl, C7-C10 phenylalkyl, carboxylate, sulfonyl, phosphoryl, and phosphonyl groups. The composition can be formulated in a dosage form such as a cream, ointment, gel, lotion, foam, powder, aerosol, spray, shampoo, or liquid solution. The composition can be used to treat a fungal disease such as tinea pedis, tinea capitis, tinea corporis, tinea versicolor, tinea cruris, and candidiasis as well as intertriginous dermatitis complicated by candidiasis.
摘要翻译：一种外用组合物和使用该组合物的方法，其含有抗真菌剂和安全有效的低效抗炎类固醇，例如去氧化物或其衍生物。低效甾类药物不会引起副作用，如皮肤萎缩，皮肤色素沉着和色素沉着不足。在代表性的例子中，低效抗炎类固醇具有以下结构：其中独立地取代的R 1，R 2，R 3和R 4可以是H，C 1 -C 10烷基，C 1 -C 10烯基，C 3 -C 10环烷基和苯基 ; R 1和R 2一起可以是C 3 -C 10环烷基; R 3和R 4独立地可以是H，C 1 -C 10烷基，C 1 -C 10烯基，C 3 -C 10环烷基，苯基，C 7 -C 10苯基烷基，羧酸酯，磺酰基，磷酰基和膦酰基。组合物可以配制成剂型，例如霜剂，软膏剂，凝胶剂，洗剂，泡沫剂，粉剂，气雾剂，喷雾剂，洗发剂或液体溶液。该组合物可用于治疗真菌性疾病，例如足癣，头癣，体癣，花斑斑，斑癣和念珠菌病以及由念珠菌病复杂的间质性皮炎。

39. 发明申请

US20040127702A1 Novel crystal form 失效
标题翻译：新型晶体
公开(公告)号：US20040127702A1
公开(公告)日：2004-07-01
申请号：US10666175
申请日：2003-09-19
发明人： Bruce Allen Pearlman , Frederick J. Antosz
IPC分类号： C07J021/00 , A61K031/58
CPC分类号： C07J1/00 , C07J21/00
摘要： The present invention involves a novel crystal form of 17null-hydroxy-7null-(5null-methyl-2null-furyl)-pregna-4,9(11)-dien-3-one-21-carboxylic acid, null-lactone, having the formula 1 which is an intermediate useful in preparation of an important pharmaceutical, eplerenone.
摘要翻译：本发明涉及17β-羟基-7α-（5'-甲基-2'-呋喃基） - 孕甾-4,9（11） - 二烯-3-酮-21-羧酸，γ-内酯的新晶体形式具有下式，其为可用于制备重要药物依普利酮的中间体。

40. 发明申请

US20040120997A1 Amphoteric sterols and the use thereof 有权
标题翻译：两性甾醇及其用途
公开(公告)号：US20040120997A1
公开(公告)日：2004-06-24
申请号：US10468654
申请日：2004-02-11
发明人： Steffan Panzner , Gerold Endert , Stefan Fankhnullnel , Nasr El-Mokdad
IPC分类号： C07J043/00 , A61K031/58 , A61K009/127
CPC分类号： C07J43/00 , A61K9/1272 , A61K31/58 , C07J41/0055 , C07J43/003
摘要： The invention relates to a sterol skeleton based compound wherein one or several amphoteric groups with an isoelectric point of between 4 and 9 are substituted on the 3rd position of the ring system, in addition to liposomes containing said compounds.
摘要翻译：本发明涉及一种基于甾醇骨架的化合物，其中除了含有所述化合物的脂质体之外，其中一个或几个具有4至9个等电点的两性基团在环系统的第3位上被取代。

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