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1. 发明申请

WO2006087722A1 BISPHOSPHONATES FOR TREATING ENDOMETRIOSIS 审中-公开
标题翻译：用于治疗子宫内膜异位症的二磷酸酯
公开(公告)号：WO2006087722A1
公开(公告)日：2006-08-24
申请号：PCT/IL2006/000209
申请日：2006-02-16
申请人： HADASIT MEDICAL RESEARCH SERVICES AND DEVELOPMENT LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , DANENBERG, Haim , SCHACHTER, Morey
发明人： GOLOMB, Gershon , DANENBERG, Haim , SCHACHTER, Morey
IPC分类号： A61K31/00 , A61K31/663 , A61P15/00
CPC分类号： A61K31/00 , A61K31/663
摘要： A novel method of treating endometriosis is disclosed. The method comprises administering to a female subject in need thereof a therapeutically effective amount of particles comprising an agent capable of inhibiting phagocytic cells of the female subject.
摘要翻译：公开了一种治疗子宫内膜异位症的新方法。该方法包括向有需要的女性受试者施用治疗有效量的包含能够抑制女性受试者的吞噬细胞的药剂的颗粒。

2. 发明申请

WO2006126208A2 COMPOSITIONS AND METHODS USING SAME FOR DELIVERING AGENTS INTO A TARGET ORGAN PROTECTED BY A BLOOD BARRIER 审中-公开
标题翻译：使用相同方式将组分和方法分送到由BLOOD BARRIER保护的目标组织
公开(公告)号：WO2006126208A2
公开(公告)日：2006-11-30
申请号：PCT/IL2006/000625
申请日：2006-05-25
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , EPSTEIN, Hila , AFERGAN, Eyal
发明人： GOLOMB, Gershon , EPSTEIN, Hila , AFERGAN, Eyal
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/0019
摘要： A method of delivering a pharmaceutical agent into a target organ protected by a blood barrier is provided. The method comprising administering to a subject in need thereof an amount of liposomes which comprise the pharmaceutical agent, the amount and the liposomes are selected such that the liposomes accumulate in cells of an immune system of the subject to thereby generate liposome loaded immune cells, the liposome loaded immune cells become activated and cross the blood barrier, and an effective amount of the pharmaceutical agent is released from the liposomes in the target organ of the subject.
摘要翻译：提供了将药剂递送到由血液屏障保护的靶器官中的方法。所述方法包括向有需要的受试者施用包含药剂的量的脂质体，选择量和脂质体使得脂质体积聚在受试者的免疫系统的细胞中，从而产生负载荷载脂质体的免疫细胞，加载脂质体的免疫细胞变得活化并穿过血液屏障，并且有效量的药剂从受试者的靶器官中的脂质体释放。

3. 发明申请

WO2003089568A3 METHOD OF INHIBITING RESTENOSIS 审中-公开
公开(公告)号：WO2003089568A3
公开(公告)日：2003-10-30
申请号：PCT/IB2003/001437
申请日：2003-04-16
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , DANENBERG, Haim
发明人： GOLOMB, Gershon , DANENBERG, Haim
IPC分类号： A61K9/127
摘要： A method of treating or preventing restenosis by administering to an individual an effective amount of an active compound which depletes and/or inhibits blood monocytes or macrophages thereby treating restenosis. A method of inhibiting the activity or production of cytokines or growth factors associated with vascular restenosis, by administering to an individual an effective amount of an active compound which depletes and/or inhibits blood monocytes or macrophages thereby treating restenosis. The cytokines and growth factors include, but are not limited to interleukin 1-β, matrix metalloproteinase-2, and platelet-derived growth factor β (PDGFβ). The active compound may be administered directly, encapsulated in a carrier particle, or in a particulate dosage form. The compound may be encapsulated, embedded or adsorbed within the particle, dispersed uniformly in the polymer matrix, adsorbed on the particle surface, or in combination of any of these forms. The particles include liposomes or inert polymeric particles, such as microcapsules, nanocapsules, nanoparticles, nanospheres, or microparticles. The particulates include any suspended or dispersed form of the compound which is not encapsulated, entrapped, or adsorbed within a polymeric particle. The particulates include suspended or dispersed colloids, aggregates, flocculates, insoluble salts and insoluble complexes of the active compound. The compound includes any intra-cellular toxin which depletes and/or inhibits blood monocytes or macrophages, such as, for example, a bisphosphonate.

4. 发明申请

WO2003048298A3 NANOPARTICLES CONTAINING POLYMERIC NUCLEIC ACID HOMOLOGS, PHARMACEUTICAL COMPOSITIONS AND ARTICLES OF MANUFACTURE CONTAINING SAME AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2003048298A3
公开(公告)日：2003-06-12
申请号：PCT/IL2002/000985
申请日：2002-12-05
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , SACKS, Hagit , NAJAREH, Yousef
发明人： GOLOMB, Gershon , SACKS, Hagit , NAJAREH, Yousef
IPC分类号： A61K31/70
摘要： A nanoparticle capable of delivery of an encapsulated molecule into a living cell. The nanoparticle includes an encapsulation media and an isolated nucleic acid homolog sequence. The encapsulation media is primarily polymeric. The nanoparticles release the encapsulated molecule over an extended period of time. Further disclosed are pharmaceutical compositions and articles of manufacture including nanoparticles and methods of preparing and using the nanoparticles.

5. 发明申请

WO2004089962A2 NEW CARBAMOYL-AND THIOCARBAMOYL-PHOSPHONATES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：新型碳水化合物和硫代磷酸酯和包含它们的药物组合物
公开(公告)号：WO2004089962A2
公开(公告)日：2004-10-21
申请号：PCT/IL2004/000302
申请日：2004-04-01
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , BREUER, Eli , REICH, Reuven , GOLOMB, Gershon , KATZ, Yiffat
发明人： BREUER, Eli , REICH, Reuven , GOLOMB, Gershon , KATZ, Yiffat
IPC分类号： C07F9/38
CPC分类号： C07F9/4065 , C07F9/3891
摘要： The present invention provides a compound of the following formula (I): R 3 -NH-C(=X)-P(=O)OR 1 OR 2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R' and R 2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R 1 and R 2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is 0 or S; and R 3 is selected, when X is 0, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R 3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that when X is O, R 3 is not cyclohexylmethyl, and when X is S, R 3 is not cyclohexyl. The invention further provides pharmaceutical compositions comprising the above compounds and their use in medicine.
摘要翻译：本发明提供下列化学式（I）的化合物：R 3 -NH-C（= X）-P（= O）OR 1或OR 2，包括其药学上可接受的盐，溶剂合物，水合物和多晶型物的式I化合物，以及式I化合物的几何异构体和光学活性形式以及所述异构体和形式的药学上可接受的盐，溶剂合物，水合物和多晶型物，其中R'和R 2可以相同或不同的，并且各自选自氢，酰氧基烷基和芳基，或者R 1和R 2可以与氧和磷原子一起形成二氧杂环磷杂环烷环; X为0或S; 当X为0时，R 3选自烷基，氨基，脒基和胍基中的至少一个来自双环烷基，环烷基烷基和取代的环烷基; 并且当X为S时，选自R 3选自二烷基，环烷基烷基和任选被烷基，氨基，脒基和胍基中的至少一个取代的环烷基; 条件是当X是O时，R 3不是环己基甲基，当X是S时，R 3不是环己基。本发明还提供了包含上述化合物及其在药物中的用途的药物组合物。

6. 发明申请

WO2003089568A2 METHOD OF INHIBITING RESTENOSIS 审中-公开
标题翻译：抑制再狭窄的方法
公开(公告)号：WO2003089568A2
公开(公告)日：2003-10-30
申请号：PCT/IB2003/001437
申请日：2003-04-16
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , DANENBERG, Haim
发明人： GOLOMB, Gershon , DANENBERG, Haim
IPC分类号： C12N
CPC分类号： A61K9/5153 , A61K9/127 , A61K31/00 , A61K31/66 , A61K31/663 , A61K31/675 , A61K33/24 , Y10S514/824 , Y10S514/951
摘要： A method of treating or preventing restenosis by administering to an individual an effective amount of an active compound which depletes and/or inhibits blood monocytes or macrophages thereby treating restenosis. A method of inhibiting the activity or production of cytokines or growth factors associated with vascular restenosis, by administering to an individual an effective amount of an active compound which depletes and/or inhibits blood monocytes or macrophages thereby treating restenosis. The cytokines and growth factors include, but are not limited to interleukin 1-β, matrix metalloproteinase-2, and platelet-derived growth factor β (PDGFβ). The active compound may be administered directly, encapsulated in a carrier particle, or in a particulate dosage form. The compound may be encapsulated, embedded or adsorbed within the particle, dispersed uniformly in the polymer matrix, adsorbed on the particle surface, or in combination of any of these forms. The particles include liposomes or inert polymeric particles, such as microcapsules, nanocapsules, nanoparticles, nanospheres, or microparticles. The particulates include any suspended or dispersed form of the compound which is not encapsulated, entrapped, or adsorbed within a polymeric particle. The particulates include suspended or dispersed colloids, aggregates, flocculates, insoluble salts and insoluble complexes of the active compound. The compound includes any intra-cellular toxin which depletes and/or inhibits blood monocytes or macrophages, such as, for example, a bisphosphonate.
摘要翻译：通过向个体施用有效量的消耗和/或抑制血液单核细胞或巨噬细胞从而治疗再狭窄的活性化合物来治疗或预防再狭窄的方法。通过向个体施用有效量的消耗和/或抑制血液单核细胞或巨噬细胞从而治疗再狭窄的活性化合物来抑制与血管再狭窄相关的细胞因子或生长因子的活性或产生的方法。细胞因子和生长因子包括但不限于白细胞介素1-β，基质金属蛋白酶-2和血小板衍生生长因子β（PDGFβ）。活性化合物可以直接给药，包封在载体颗粒中或颗粒剂型中。该化合物可被包封，嵌入或吸附在颗粒内，均匀分散在聚合物基质中，吸附在颗粒表面上，或以任何这些形式的组合。颗粒包括脂质体或惰性聚合物颗粒，如微胶囊，纳米胶囊，纳米颗粒，纳米球或微粒。颗粒包括未被包封，包埋或吸附在聚合物颗粒内的任何悬浮或分散形式的化合物。颗粒包括活性化合物的悬浮或分散的胶体，聚集体，絮凝物，不溶性盐和不溶性复合物。该化合物包括消耗和/或抑制血液单核细胞或巨噬细胞的任何细胞内毒素，例如二膦酸盐。

7. 发明申请

WO2003048298A2 NANOPARTICLES CONTAINING POLYMERIC NUCLEIC ACID HOMOLOGS, PHARMACEUTICAL COMPOSITIONS AND ARTICLES OF MANUFACTURE CONTAINING SAME AND METHODS OF USE THEREOF 审中-公开
标题翻译：含有聚合物核酸同系物的纳米颗粒，药物组合物和含有该组合物的制品及其使用方法
公开(公告)号：WO2003048298A2
公开(公告)日：2003-06-12
申请号：PCT/IL2002/000985
申请日：2002-12-05
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GOLOMB, Gershon , SACKS, Hagit , NAJAREH, Yousef
发明人： GOLOMB, Gershon , SACKS, Hagit , NAJAREH, Yousef
IPC分类号： C12N
CPC分类号： A61K9/5153 , A61K9/1647 , A61K9/5031 , A61K9/5089 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K31/7125 , A61K31/713 , A61K47/34 , A61K48/00 , C12N15/88
摘要： A nanoparticle capable of delivery of an encapsulated molecule into a living cell. The nanoparticle includes an encapsulation media and an isolated nucleic acid homolog sequence. The encapsulation media is primarily polymeric. The nanoparticles release the encapsulated molecule over an extended period of time. Further disclosed are pharmaceutical compositions and articles of manufacture including nanoparticles and methods of preparing and using the nanoparticles.
摘要翻译：能够将包囊分子递送到活细胞中的纳米颗粒。纳米颗粒包括封装介质和分离的核酸同系物序列。封装介质主要是聚合物。纳米颗粒在延长的时间内释放包封的分子。还公开了包括纳米颗粒的药物组合物和制品以及制备和使用纳米颗粒的方法。

8. 发明公开

EP1888034A2 COMPOSITIONS AND METHODS USING SAME FOR DELIVERING AGENTS INTO A TARGET ORGAN PROTECTED BY A BLOOD BARRIER 审中-公开
标题翻译：组合物和分配的资金INTO的靶器官THIS使用的方法; 保护方式血液屏障
公开(公告)号：EP1888034A2
公开(公告)日：2008-02-20
申请号：EP06756179.5
申请日：2006-05-25
申请人： Yissum Research Development Company, of The Hebrew University of Jerusalem
发明人： GOLOMB, Gershon , EPSTEIN, Hila , AFERGAN, Eyal
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/0019
摘要： A liposome for use in delivering a pharmaceutical agent into a target organ protected by a blood barrier comprises a pharmaceutical agent targeted at an organ protected by said blood brain barrier, wherein said liposome is accumulated in a cell of an immune system of said subject to thereby generate a liposome loaded immune cell, said liposome loaded immune cell is capable of crossing the blood barrier, where an amount of the pharmaceutical agent is released from said liposome in the target organ of the subject.

9. 发明公开

EP1471870A2 USE OF LIPID CONJUGATES IN THE TREATMENT OF DISEASE 有权
标题翻译：脂质结合物的疾病中的治疗
公开(公告)号：EP1471870A2
公开(公告)日：2004-11-03
申请号：EP01900237.7
申请日：2001-01-10
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
发明人： YEDGAR, Saul , SHOSEYOV, David , GOLOMB, Gershon , REICH, Reuven , GINSBURG, Isaac , HIGAZI, Abd-Al-Roof , LIGUMSKI, Moshe , KRIMSKY, Miron , OJCIUS, David , YARD, Benito, Antonio , VAN DER WOUDE, Fokko, Johannes , SCHNITZER, Edit
IPC分类号： A61K6/00
CPC分类号： A61K47/544
摘要： The invention provides novel methods for treating disease based on the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and(tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels.

10. 发明授权

EP1228072B1 PDGF RECEPTOR KINASE INHIBITORY COMPOUNDS, THEIR PREPARATION, PURIFICATION AND PHARMACEUTICAL COMPOSITIONS INCLUDING SAME 有权
标题翻译： PDGF受体激酶抑制化合物，生产，对其进行清洁和药物组合物含
公开(公告)号：EP1228072B1
公开(公告)日：2005-09-28
申请号：EP00973192.8
申请日：2000-11-02
申请人： Yissum Research Development Company of the Hebrew University of Jerusalem
发明人： LEVITZKI, Alexander , GAZIT, Aviv , BANAI, Shmuel , GERTZ, David, S. , GOLOMB, Gershon , BOEHMER, Frank, D. , WALTENBERGER, Johannes
IPC分类号： C07D487/14 , A61K31/4188 , C07D487/04 , A61K31/4985 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： A preparation of a tyrphostin including a compound of a general formula (Compound I) or (Compound II), wherein, for (Compound I), the preparation is enriched either for R6 at position 6 or for R6 at position 7, or, for (Compound II), the preparation is enriched either for R6 at position 6 or for R6 at position 8.

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