公开(公告)号：US20120164072A1

公开(公告)日：2012-06-28

申请号：US13318869

申请日：2010-05-04

申请人： Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

发明人： Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

IPC分类号： A61K51/08 ,  A61K9/14 ,  A61K47/42 ,  A61K9/133 ,  A61K38/08 ,  A61K38/28 ,  A61K38/11 ,  A61K38/23 ,  A61K38/22 ,  A61K38/24 ,  A61K38/20 ,  A61K38/21 ,  A61K38/19 ,  A61K38/34 ,  A61K38/44 ,  A61K38/06 ,  A61K48/00 ,  A61K31/713 ,  A61K38/18 ,  A61K38/13 ,  A61K31/704 ,  A61K38/14 ,  A61K33/24 ,  A61K31/28 ,  A61K31/475 ,  A61K31/337 ,  A61K31/365 ,  A61K31/4745 ,  A61K49/00 ,  A61K38/38 ,  C07C237/50 ,  C07C229/22 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P35/00 ,  A61P3/10 ,  A61P37/04 ,  A61P31/12 ,  A61P31/04 ,  A61K9/127 ,  B82Y5/00

CPC分类号： A61K9/1272 ,  A61K9/0019 ,  A61K9/127 ,  A61K9/51 ,  C07C229/22

摘要： Nano-sized particles are provided comprising at least one multi-headed amphiphilic compound, in which at least one headgroup of said multi-headed amphiphilic compound is selectively cleavable or contains a selectively cleavable group, and at least one biologically active agent, which is both encapsulated within the nano-particle and non-covalently associated thereto.

摘要翻译： 提供包含至少一种多头两亲化合物的纳米级颗粒，其中所述多头两亲化合物的至少一个头基可选择性切割或含有选择性可切割基团，以及至少一种生物活性剂，其均为 封装在纳米颗粒内并与其非共价缔合。

公开(公告)号：US20130172321A1

公开(公告)日：2013-07-04

申请号：US13593911

申请日：2012-08-24

申请人： Eliahu Heldman

发明人： Eliahu Heldman

IPC分类号： A61K31/55 ,  A61K31/167 ,  A61K31/27 ,  A61K31/465

CPC分类号： A61K31/465 ,  A61K9/0014 ,  A61K9/0053 ,  A61K31/136 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/55 ,  A61K2300/00

摘要： The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).

公开(公告)号：US08377469B2

公开(公告)日：2013-02-19

申请号：US11813311

申请日：2006-01-02

申请人： Jacob Zabicky ,  Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

发明人： Jacob Zabicky ,  Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

IPC分类号： A61K9/127

CPC分类号： A61K9/1272 ,  A61K9/127 ,  A61K9/1277

摘要： Method for the preparation of nano- and mesosized particles consisting of a lipid layer comprising at least one amphiphile and a core of an inorganic compound and/or a metal, comprising: (i) dissolving in a common solvent at least one self-aggregating amphiphile with at least one inorganic, organometallic or metallorganic precursor of said inorganic compound or metal; and (ii) either injecting the resulting solution into an aqueous solution or drying the resulting solution and re-hydrating it, so as to form particles in which the precursor is encapsulated by the amphiphile(s) and is converted therein to said inorganic compound and/or metallic solid form.

摘要翻译： 由包含至少一种无机化合物和/或金属的两亲物和核心的脂质层组成的纳米和中尺寸颗粒的制备方法，包括：（i）在普通溶剂中溶解至少一种自聚集的两亲物 与所述无机化合物或金属的至少一种无机，有机金属或金属有机前体; 和（ii）将所得溶液注入水溶液中或干燥所得溶液并对其进行再水化，以形成其中前体被两亲物包封并在其中转化为所述无机化合物的颗粒， /或金属固体形式。

公开(公告)号：US20060039962A1

公开(公告)日：2006-02-23

申请号：US10497705

申请日：2002-12-04

申请人： Eliahu Heldman ,  Charles Linder ,  Sarina Grinberg

发明人： Eliahu Heldman ,  Charles Linder ,  Sarina Grinberg

IPC分类号： A61K9/127 ,  C07C237/12

CPC分类号： C07D401/04 ,  A61K9/1272 ,  C07C219/06 ,  C07C233/36 ,  C07C235/28 ,  C07C237/10 ,  C07D303/46 ,  C07H7/00 ,  C07H15/10 ,  C07H15/26

摘要： An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine derivative, and at least one hydrogen-bonding group located either within said headgroup and/or in close proximity thereto. The cleavable group or moiety is cleaved under selective conditions including change of chemical, physical or biological environment and is preferably cleaved enzymatically in a biological environment such as the brain or the blood. Vesicles or liposomes made from said amphiphilic compounds are suitable for delivery of a therapeutic substance or a diagnostic agent specifically to a target organ or tissue, or for delivery of a nucleic acid for gene therapy.

摘要翻译： 提供能够形成囊泡或脂质体的两亲化合物，所述两亲化合物具有至少一个含有选择性可切割基团或部分的头基，例如胆碱或苯丙氨酸衍生物的残基，以及至少一个位于所述 头组和/或其附近。 可切割基团或部分在选择性条件下被切割，包括化学，物理或生物环境的变化，并且优选在诸如脑或血液的生物环境中酶促切割。 由所述两亲性化合物制成的囊泡或脂质体适于将治疗物质或诊断剂特异性递送至靶器官或组织，或用于递送用于基因治疗的核酸。

公开(公告)号：US08273731B2

公开(公告)日：2012-09-25

申请号：US12323779

申请日：2008-11-26

申请人： Eliahu Heldman

发明人： Eliahu Heldman

IPC分类号： A61K31/55 ,  A61K31/4439 ,  A61K31/465

CPC分类号： A61K31/465 ,  A61K9/0014 ,  A61K9/0053 ,  A61K31/136 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/55 ,  A61K2300/00

摘要： The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).

摘要翻译： 本公开至少部分地涉及包含用于治疗例如神经系统疾病的烟碱激动剂的组合物和方法，特别是涉及包括烟碱激动剂（例如尼古丁）和烟碱乙酰胆碱受体脱敏抑制剂的组合疗法（例如， ，opipramol）。

公开(公告)号：US06746688B1

公开(公告)日：2004-06-08

申请号：US09711709

申请日：2000-11-13

申请人： Moshe Kushnir ,  Eliahu Heldman

发明人： Moshe Kushnir ,  Eliahu Heldman

IPC分类号： A61K970

CPC分类号： A61K9/7023 ,  A61K31/198 ,  A61K31/216 ,  A61K47/10 ,  A61K47/12

摘要： A pharmaceutical composition for treatment of Parkinson's disease comprising a compound of levodopa dissolved in a non-degradative solvent which allows transdermal administrtion of levodopa. The compound of levodopa is an alkyl-ester of levodopa and the solvent is a formulation comprising a substantially non-aqueous solvent, a transdermal enchancer and a detergent. The alkyl-ester of levodopa is preferably levodopa-ethyl-ester (LDEE).

摘要翻译： 一种用于治疗帕金森病的药物组合物，其包含溶解在非降解溶剂中的左旋多巴的化合物，其允许透皮给药左旋多巴。 左旋多巴的化合物是左旋多巴的烷基酯，溶剂是包含基本上非水溶剂，透皮增强剂和洗涤剂的制剂。 左旋多巴的烷基酯优选为左旋多巴乙酯（LDO）。

公开(公告)号：US6166081A

公开(公告)日：2000-12-26

申请号：US287951

申请日：1999-04-07

申请人： Moshe Kushnir ,  Eliahu Heldman

发明人： Moshe Kushnir ,  Eliahu Heldman

IPC分类号： A61K9/70 ,  A61K31/195 ,  A61K31/198 ,  A61K31/135 ,  C07C271/06

CPC分类号： A61K31/198 ,  A61K9/7023 ,  A61K31/195 ,  A61K2300/00

摘要： A pharmaceutical composition for treatment of Parkinson's disease comprising a compound of levodopa dissolved in a non-degradative solvent which allows transdermal administrtion of levodopa. The compound of levodopa is an alkyl-ester of levodopa and the solvent is a formulation comprising a substantially non-aqueous solvent, a transdermal enhancer and a detergent. The alkyl-ester of levodopa is preferably levodopa-ethyl-ester (LDEE).

摘要翻译： 一种用于治疗帕金森病的药物组合物，其包含溶解在非降解溶剂中的左旋多巴的化合物，其允许透皮给药左旋多巴。 左旋多巴的化合物是左旋多巴的烷基酯，溶剂是包含基本上非水溶剂，透皮增强剂和洗涤剂的制剂。 左旋多巴的烷基酯优选为左旋多巴乙酯（LDO）。

公开(公告)号：US07887833B2

公开(公告)日：2011-02-15

申请号：US10497705

申请日：2002-12-04

申请人： Eliahu Heldman ,  Charles Linder ,  Sarina Grinberg ,  Victoria Kolot ,  Eleonora Shaubi

发明人： Eliahu Heldman ,  Charles Linder ,  Sarina Grinberg ,  Victoria Kolot ,  Eleonora Shaubi

IPC分类号： A61K9/127 ,  C07C231/00 ,  C07C229/00

CPC分类号： C07D401/04 ,  A61K9/1272 ,  C07C219/06 ,  C07C233/36 ,  C07C235/28 ,  C07C237/10 ,  C07D303/46 ,  C07H7/00 ,  C07H15/10 ,  C07H15/26

摘要： An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine derivative, and at least one hydrogen-bonding group located either within said headgroup and/or in close proximity thereto. The cleavable group or moiety is cleaved under selective conditions including change of chemical, physical or biological environment and is preferably cleaved enzymatically in a biological environment such as the brain or the blood. Vesicles or liposomes made from said amphiphilic compounds are suitable for delivery of a therapeutic substance or a diagnostic agent specifically to a target organ or tissue, or for delivery of a nucleic acid for gene therapy.

摘要翻译： 提供能够形成囊泡或脂质体的两亲化合物，所述两亲化合物具有至少一个含有选择性可切割基团或部分的头基，例如胆碱或苯丙氨酸衍生物的残基，以及至少一个位于所述 头组和/或其附近。 可切割基团或部分在选择性条件下被切割，包括化学，物理或生物环境的变化，并且优选在诸如脑或血液的生物环境中酶促切割。 由所述两亲性化合物制成的囊泡或脂质体适于将治疗物质或诊断剂特异性递送至靶器官或组织，或用于递送用于基因治疗的核酸。

公开(公告)号：US20090011002A1

公开(公告)日：2009-01-08

申请号：US11813311

申请日：2006-01-02

申请人： Jacob Zabicky ,  Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

发明人： Jacob Zabicky ,  Charles Linder ,  Sarina Grinberg ,  Eliahu Heldman

IPC分类号： A61K9/127 ,  A61K9/14

CPC分类号： A61K9/1272 ,  A61K9/127 ,  A61K9/1277

摘要： Method for the preparation of nano- and mesosized particles consisting of a lipid layer comprising at least one amphiphile and a core of an inorganic compound and/or a metal, comprising: (i) dissolving in a common solvent at least one self-aggregating amphiphile with at least one inorganic, organometallic or metallorganic precursor of said inorganic compound or metal; and (ii) either injecting the resulting solution into an aqueous solution or drying the resulting solution and re-hydrating it, so as to form particles in which the precursor is encapsulated by the amphiphile(s) and is converted therein to said inorganic compound and/or metallic solid form.

摘要翻译： 由包含至少一种无机化合物和/或金属的两亲物和核心的脂质层组成的纳米和中尺寸颗粒的制备方法，包括：（i）在普通溶剂中溶解至少一种自聚集的两亲物 与所述无机化合物或金属的至少一种无机，有机金属或金属有机前体; 和（ii）将所得溶液注入水溶液中或干燥所得溶液并对其进行再水化，以形成其中前体被两亲物包封并在其中转化为所述无机化合物的颗粒， /或金属固体形式。

公开(公告)号：US5106831A

公开(公告)日：1992-04-21

申请号：US599977

申请日：1990-10-19

申请人： Abraham Fisher ,  Ishai Karton ,  Eliahu Heldman ,  Yona Grunfeld ,  Aharon Levy

发明人： Abraham Fisher ,  Ishai Karton ,  Eliahu Heldman ,  Yona Grunfeld ,  Aharon Levy

IPC分类号： C07D497/20

CPC分类号： C07D497/20

摘要： A pharmaceutical composition is disclosed comprising (-)-cis-2-methylspiro(1,3-oxathiolan-5,3')quinuclidine, and/or the pharmaceutically compatible acid addition salts thereof, together with at least one of physostigmine, tetrahydroaminoacridine, choline, lecithin, piracetam, aniracetam, pramiracetam, oxiracetam, 4-aminopyridine, 3,4-diaminopyridine, somatostatin, pirenzepine, N-methylatropine, N-butylscopolamine, scopolamine, clonidine, quanfamicine and Nerve Growth Factor. Also disclosed is a method for treating senile dementia of Alzheimer's type, which comprises coadministering to a patient in need thereof an effective dose of the spiro compound together with at least one other compound selected from those listed above.

摘要翻译： 公开了一种药物组合物，其包含（ - ） - 顺式-2-甲基螺旋（1,3-氧硫杂环戊烷-5,3'）奎宁环和/或其药学上相容的酸加成盐，以及至少一种毒扁豆素，四氢氨基吖啶， 胆碱，卵磷脂，吡拉西坦，阿拉西坦，普拉西坦，奥拉西坦，4-氨基吡啶，3,4-二氨基吡啶，生长抑素，哌仑西平，N-甲基阿托品，N-丁基东莨菪碱，东莨菪碱，可乐定，喹唑啉和神经生长因子。 还公开了一种治疗阿尔茨海默氏型老年痴呆症的方法，其包括将有效剂量的螺环化合物与选自上述列举的至少一种其它化合物共同施用于有需要的患者。