公开(公告)号：US5030442A

公开(公告)日：1991-07-09

申请号：US333660

申请日：1989-04-04

申请人： Paul S. Uster ,  Yolanda P. Quinn

发明人： Paul S. Uster ,  Yolanda P. Quinn

IPC分类号： A61K8/14 ,  A61K8/49 ,  A61K9/107 ,  A61K9/127 ,  A61K31/505 ,  A61Q7/00

CPC分类号： A61K31/505 ,  A61K47/48038 ,  A61K47/48053 ,  A61K8/14 ,  A61K8/4953 ,  A61K9/1075 ,  A61K9/1272 ,  A61Q7/00 ,  Y10S514/88 ,  Y10S514/944 ,  Y10S514/947 ,  Y10S514/969 ,  Y10S514/975 ,  Y10T428/2984

摘要： An aqueous, noncrystalline minoxidil composition for topical use which has significantly improved flux of the drug through human cadaver skin. The composition contains minoxidil complexed with an amphipathic compound, oleic acid and with pharmaceutically acceptable excipients. The composition may be formulated in an aqueous vehicle, or dispersed in fluorochlorocarbon solvent for spray delivery from a self- propelled spray device.

摘要翻译： 用于局部使用的水性非结晶米诺地尔组合物，其通过人类尸体皮肤显着改善药物的通量。 组合物含有与两亲化合物，油酸和药学上可接受的赋形剂复合的米诺地尔。 组合物可以配制在水性载体中，或分散在氟氯化碳溶剂中，用于从自推进喷雾装置喷射输送。

公开(公告)号：US4780455A

公开(公告)日：1988-10-25

申请号：US722735

申请日：1985-04-12

申请人： Seymour Lieberman ,  V. V. K. Prasad ,  Laura Ponticorvo

发明人： Seymour Lieberman ,  V. V. K. Prasad ,  Laura Ponticorvo

IPC分类号： C07J31/00 ,  C07J51/00 ,  A61K31/685 ,  A61K31/56 ,  C07J9/00

CPC分类号： A61K47/48053 ,  C07J31/00 ,  C07J51/00

摘要： The present invention provides a composition with the structure(L).sub.m (E).sub.nwherein m and n are each integers, and m and n are different or the same; L is an ampholytic lipid or polymer, or a nonampholytic lipid with hydrophobic properties; E is a nonlipophilic ionic inorganic ester of an organic compound, E having the structural formulaZ.sup.+q R-Y-X-(O).sub.p.sup.-qwherein R is an organic moiety; Y is oxygen, sulfur or a substituted nitrogen, X is sulfur, phosphorus, nitrogen or boron; p is the integer 2 or the integer 3; Z is hydrogen or a metal, and Q is an integer indicating the elecrical charge.Suitable ampholytic lipids are phospholipids, sulfatides, and sphingomyelins. The esters can be sulfate or phosphate esters of steroid hormones. The compositions are useful for example, for altering the solubility properties of the esters, and for developing controlled-delivery systems for pharmaceuticals.

摘要翻译： 本发明提供具有结构（L）m（E）n的组合物，其中m和n各自是整数，m和n不同或相同; L是两性脂质或聚合物，或具有疏水性质的非溶血性脂质; E是有机化合物的非亲脂性离子无机酯，E具有结构式Z + qR-Y-X-（O）p-q，其中R是有机部分; Y是氧，硫或取代的氮，X是硫，磷，氮或硼; p是整数2或整数3; Z是氢或金属，Q是表示电荷的整数。 合适的两性脂质是磷脂，硫苷脂和鞘磷脂。 酯可以是类固醇激素的硫酸酯或磷酸酯。 组合物可用于例如用于改变酯的溶解性质和用于开发药物的受控递送系统。

公开(公告)号：US20120189571A1

公开(公告)日：2012-07-26

申请号：US13147751

申请日：2010-02-04

申请人： Shiladitya Sengupta ,  Abhimanyu Paraskar ,  Shivani Soni ,  Sudipta Basu ,  Poulomi Sengupta

发明人： Shiladitya Sengupta ,  Abhimanyu Paraskar ,  Shivani Soni ,  Sudipta Basu ,  Poulomi Sengupta

IPC分类号： A61K31/785 ,  A61K31/795 ,  A61P35/00 ,  A61P35/04 ,  C08F8/32 ,  C08F122/06 ,  C08F122/02 ,  C07J41/00 ,  C07F15/00 ,  B82Y5/00 ,  B82B1/00

CPC分类号： A61K47/489 ,  A61K31/282 ,  A61K31/382 ,  A61K33/24 ,  A61K47/16 ,  A61K47/24 ,  A61K47/48046 ,  A61K47/48053 ,  A61K47/48176 ,  A61K47/48215 ,  A61K47/543 ,  A61K47/544 ,  A61K47/58 ,  A61K47/60 ,  A61K47/6933 ,  C07J41/0055 ,  C08F8/32 ,  C08F22/06 ,  C08F222/06

摘要： The invention is directed to biocompatible conjugated polymer nanoparticles including a copolymer backbone, a plurality of sidechains covalently linked to said backbone, and a plurality of platinum compounds dissociably linked to said backbone. The invention is also directed to dicarbonyl-lipid compounds wherein a platinum compound is dissociably linked to the dicarbonyl compound. The invention is also directed to methods of treating cancer or metastasis. The methods includes selecting a subject in need of treatment for cancer or metastasis and administering to the subject an effective amount of any of the nanoparticles, compounds, or compositions of the invention.

摘要翻译： 本发明涉及生物相容的共轭聚合物纳米颗粒，其包括共聚物主链，与所述主链共价连接的多个侧链，以及与所述主链离解连接的多个铂化合物。 本发明还涉及其中铂化合物与二羰基化合物离解连接的二羰基 - 脂质化合物。 本发明还涉及治疗癌症或转移的方法。 所述方法包括选择需要治疗癌症或转移的受试者，并向受试者施用有效量的本发明的任何纳米颗粒，化合物或组合物。

公开(公告)号：US20120071442A1

公开(公告)日：2012-03-22

申请号：US13283020

申请日：2011-10-27

申请人： Saul Yedgar

发明人： Saul Yedgar

IPC分类号： A61K31/728 ,  A61P11/02

CPC分类号： A61K47/48053 ,  A61K31/685 ,  A61K31/717 ,  A61K31/721 ,  A61K31/726 ,  A61K31/727 ,  A61K31/728 ,  A61K31/737 ,  A61K47/544 ,  A61K47/61

摘要： This invention provides a method of treating, suppressing, inhibiting, or preventing chronic rhinosinusitis in a subject comprising the step of administering to a subject a compound comprising a lipid or phospholipid moiety bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a method of treating, suppressing, inhibiting, or preventing nasal polyps in a subject comprising the step of administering to a subject a compound comprising a lipid or phospholipid moiety bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.

摘要翻译： 本发明提供一种治疗，抑制或预防受试者慢性鼻鼻窦炎的方法，其包括向受试者施用包含脂质或磷脂部分键合到生理上可接受的单体，二聚体，低聚物或聚合物的化合物的步骤，以及 /或其药学上可接受的盐或其药物产品。 本发明还提供了治疗，抑制或预防受试者鼻息肉的方法，包括向受试者施用包含脂质或磷脂部分键合到生理上可接受的单体，二聚体，低聚物或聚合物的化合物的步骤， 和/或其药学上可接受的盐或药物产物。

公开(公告)号：US06127349A

公开(公告)日：2000-10-03

申请号：US49818

申请日：1998-03-27

申请人： Fred I. Chasalow

发明人： Fred I. Chasalow

IPC分类号： A61K47/48 ,  A61K31/335 ,  A61K31/66 ,  A61K31/675 ,  A61K31/685 ,  A61K31/70 ,  A61K38/00 ,  A61K45/00 ,  A61P43/00

CPC分类号： A61K47/48053

摘要： Disclosed herein are methods for increasing the bioavailability of pharmaceutical agents by conjugation to phospholipids. Also disclosed are phospholipid-derivatized steroids, peptides, antibiotics and other biologically active agents and pharmaceutical formulations comprising these compounds.

摘要翻译： 本文公开了通过与磷脂缀合来提高药剂的生物利用度的方法。 还公开了磷脂衍生的类固醇，肽，抗生素和其它生物活性剂和包含这些化合物的药物制剂。

公开(公告)号：US06092764A

公开(公告)日：2000-07-25

申请号：US897341

申请日：1997-07-21

申请人： Paul Francis Geders ,  Robert Henry Wille

发明人： Paul Francis Geders ,  Robert Henry Wille

IPC分类号： A61K38/00 ,  C07H21/00 ,  C07K14/52 ,  C12N15/115 ,  C12N15/88 ,  C12Q1/68 ,  B64C1/00

CPC分类号： C12N15/115 ,  A61K47/48053 ,  C07H21/00 ,  C07K14/52 ,  C12N15/88 ,  C12Q1/6811 ,  A61K38/00 ,  C12N2310/3515

摘要： An interface seal (52) for an aircraft (50) has a first rigid structural beam (60) attached to a first portion of the aircraft (50). A second rigid structural beam (64) is attached to a second portion of the aircraft (50). An elastomer skin (62) is connected to the first rigid structural beam (60) and attached to the second rigid structural beam (64).

摘要翻译： 用于飞机（50）的接口密封件（52）具有附接到飞行器（50）的第一部分的第一刚性结构梁（60）。 第二刚性结构梁（64）附接到飞行器（50）的第二部分。 弹性体皮肤（62）连接到第一刚性结构梁（60）并且附接到第二刚性结构梁（64）。

公开(公告)号：US6087325A

公开(公告)日：2000-07-11

申请号：US950618

申请日：1997-10-15

申请人： Paul R. Meers ,  Charles Pak ,  Shaukat Ali ,  Andrew Janoff ,  J. Craig Franklin ,  Ravi K. Erukulla ,  Donna Cabral-Lilly

发明人： Paul R. Meers ,  Charles Pak ,  Shaukat Ali ,  Andrew Janoff ,  J. Craig Franklin ,  Ravi K. Erukulla ,  Donna Cabral-Lilly

IPC分类号： A61K9/127 ,  A61K38/00 ,  A61K47/48 ,  C07K1/107 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/093 ,  C07K5/097 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K9/00 ,  C07K5/00 ,  C07K7/00

CPC分类号： C07K7/06 ,  A61K47/48053 ,  A61K47/48238 ,  A61K47/48815 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  C07K1/1077 ,  C07K5/06026 ,  C07K5/06191 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0819 ,  C07K5/0823 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/1013 ,  C07K5/1027 ,  C07K9/001 ,  A61K38/00

摘要： Peptide-lipid conjugates are incorporated into liposomes so as to selectively destabilize the liposomes in the vicinity of target peptidase-secreting cells, and hence, to deliver the liposomes to the vicinity of the target cells, or directly into the cells. The liposomes can thus be used to treat mammals for diseases, disorders or conditions, e.g., tumors, microbial infection and inflammations, characterized by the occurrence of peptidase-secreting cells.

摘要翻译： 将肽 - 脂质缀合物掺入脂质体中，以选择性地使目标肽酶分泌细胞附近的脂质体不稳定，从而将脂质体递送至靶细胞附近或直接进入细胞。 因此，脂质体可用于治疗哺乳动物疾病，病症或病症，例如肿瘤，微生物感染和炎症，其特征在于发生肽酶分泌细胞。

公开(公告)号：US6077837A

公开(公告)日：2000-06-20

申请号：US178210

申请日：1998-10-23

申请人： Alexander Kozak

发明人： Alexander Kozak

IPC分类号： A61K31/352 ,  C07F9/10 ,  A61K31/685

CPC分类号： A61K47/48038 ,  A61K31/352 ,  A61K47/48053 ,  C07F9/10 ,  Y10S514/826

摘要： The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

公开(公告)号：US6024977A

公开(公告)日：2000-02-15

申请号：US923015

申请日：1997-09-03

申请人： Milton B. Yatvin ,  Michael H. B. Stowell ,  Michael J. Meredith

发明人： Milton B. Yatvin ,  Michael H. B. Stowell ,  Michael J. Meredith

IPC分类号： A61K47/48 ,  A61K31/00 ,  A61K31/196 ,  A61K31/198 ,  A61K31/513 ,  A61K31/519 ,  A61K31/55 ,  A61P25/00 ,  A61P43/00 ,  C07H19/06 ,  C07H19/10 ,  A61K9/127 ,  A61K31/135 ,  A61K31/54 ,  A61K38/00

CPC分类号： C07H19/06 ,  A61K31/00 ,  A61K47/48046 ,  A61K47/48053 ,  B82Y5/00 ,  C07H19/10

摘要： This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.

公开(公告)号：US6015564A

公开(公告)日：2000-01-18

申请号：US248082

申请日：1999-02-10

申请人： Christophe Boutillon ,  Frederic Martinon ,  Christian Sergheraert ,  Remy Magne ,  Helene Gras-Masse ,  Elisabeth Gomard ,  Andre Tartar ,  Jean-Paul Levy

发明人： Christophe Boutillon ,  Frederic Martinon ,  Christian Sergheraert ,  Remy Magne ,  Helene Gras-Masse ,  Elisabeth Gomard ,  Andre Tartar ,  Jean-Paul Levy

IPC分类号： A61K39/00 ,  A61K47/48 ,  A61P31/00 ,  A61P37/04 ,  C07K14/16 ,  A61K39/21 ,  A61K39/12 ,  C07K1/00

CPC分类号： C07K14/005 ,  A61K47/48023 ,  A61K47/48038 ,  A61K47/48053 ,  A61K47/48123 ,  A61K39/00 ,  C12N2740/16122 ,  C12N2740/16222 ,  C12N2740/16322

摘要： Cytotoxic lymphocyte-inducing lipopeptides comprising a peptide part having between 10 and 40 amino acids approximately and comprising at least one tigenic determinant. The lipopeptides also comprise one or more chains derived from fatty acids and one or more modified steroid groups. Said lipopeptides may be used for immunizing the human or animal body against pathogenic agents such as viruses or parasites. The peptide part may, in particular, be a fragment of the protein encoded by the ENV gene, by the NEF gene or by the GAG gene of HIV viruses.

摘要翻译： 细胞毒性淋巴细胞诱导脂肽包含约10至40个氨基酸的肽部分，并且包含至少一个抗原决定簇。 脂肽还包含一种或多种衍生自脂肪酸和一种或多种修饰类固醇基团的链。 所述脂肽可以用于免疫人体或动物体内的病原体如病毒或寄生虫。 肽部分尤其可以是由ENV基因，NEF基因或HIV病毒的GAG基因编码的蛋白质的片段。