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1. 发明申请

WO2004028443A2 LIPOPHILIC DIESTERS OF CHELATING AGENT FOR INHIBITION OF ENZYME ACTIVITY 审中-公开
标题翻译：用于抑制酶活性的螯合剂的锂离子电池
公开(公告)号：WO2004028443A2
公开(公告)日：2004-04-08
申请号：PCT/IL2003/000225
申请日：2003-03-16
申请人： D-PHARM LTD. , STRIEM, Sarina , FRIEDMAN, Jonathan, Eduard , REZNITSKY-COHEN, Dalia , KOZAK, Alexander
发明人： STRIEM, Sarina , FRIEDMAN, Jonathan, Eduard , REZNITSKY-COHEN, Dalia , KOZAK, Alexander
IPC分类号： A61K
CPC分类号： A61K31/225
摘要： The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA) for inhibition of proteolytic activities of certain metalloproteinases and of calpain. The invention further relates to methods for preventing, treating or managing MMP-related and calpain-related diseases or disorders in mammals comprising administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of said lipophilic diesters of the chelating agent BAPTA.
摘要翻译：本发明涉及螯合剂1,2-双（2-氨基苯氧基）乙烷-N，N，N'，N'-四乙酸（BAPTA）的亲脂性二酯用于抑制某些金属蛋白酶的蛋白水解活性和钙蛋白酶。本发明还涉及用于预防，治疗或管理哺乳动物中MMP-相关和钙蛋白酶相关疾病或病症的方法，其包括向有需要的哺乳动物施用包含治疗有效量的螯合剂BAPTA的所述亲脂性二酯的药物组合物。

2. 发明申请

WO9902120A2 COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES 审中-公开
标题翻译：可逆地提高生物膜渗透性的组合物和方法
公开(公告)号：WO9902120A2
公开(公告)日：1999-01-21
申请号：PCT/IL9800317
申请日：1998-07-07
申请人： DPHARM LTD , KOZAK ALEXANDER , VINIKOVA MARINA , SHAPIRO ISRAEL
发明人： VINIKOVA MARINA , SHAPIRO ISRAEL , KOZAK ALEXANDER
IPC分类号： A61K47/12 , A61K47/14 , A61K47/16 , A61K49/00 , C07C51/38 , C07C53/128 , A61K
CPC分类号： C07C53/128
摘要： The present invention provides a family of branched fatty acids and their derivatives, which improve and enable the penetration and absorption of active ingredients through biomembranes, such as the blood brain barrier. The invention further provides pharmaceutical compositions comprising these branched fatty acids and methods of using these compositions to permeabilize biological membranes thereby improving the administration of bioactive or therapeutic substances to cells or organs. According to a more preferred embodiment of this invention the methods are particularly useful to treat certain kinds of CNS lesions and diseases including tumors, infections, abscesses and degenerative and behavioral disorders.
摘要翻译：本发明提供了一类支链脂肪酸及其衍生物，其通过生物膜如血脑屏障改善并使得活性成分能够渗透和吸收。本发明进一步提供了包含这些支链脂肪酸的药物组合物以及使用这些组合物使生物膜透化从而改善生物活性或治疗性物质向细胞或器官的施用的方法。根据本发明更优选的实施方案，所述方法特别适用于治疗某些种类的CNS损伤和疾病，包括肿瘤，感染，脓肿以及退行性和行为障碍。

3. 发明申请

WO2003000173A2 USE OF BRANCHED-CHAIN FATTY ACIDS AND DERIVATIVES THEREOF FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：使用分支链脂肪酸及其衍生物治疗疼痛
公开(公告)号：WO2003000173A2
公开(公告)日：2003-01-03
申请号：PCT/IL2002/000502
申请日：2002-06-24
申请人： D-PHARM LIMITED , KOZAK, Alexander , DUVDEVANI, Revital , YOUNIS, Firas, M.
发明人： KOZAK, Alexander , DUVDEVANI, Revital , YOUNIS, Firas, M.
IPC分类号： A61K
CPC分类号： C07F9/11 , A61K31/16 , A61K31/20 , A61K31/22 , A61K31/66 , C07C53/128 , C07C69/30 , C07C233/05 , C07F9/10 , C07F9/12
摘要： The present invention relates to compounds and pharmaceutical compositions useful for treating pain. The invention also relates to methods of treating or alleviating pain in mammals, comprising administering to a mammal suffering from pain, a pain-alleviating amount of a compound of the general formula (I) or (II).
摘要翻译：本发明涉及可用于治疗疼痛的化合物和药物组合物。本发明还涉及治疗或减轻哺乳动物疼痛的方法，其包括向患有疼痛的哺乳动物施用减轻疼痛的量的通式（I）或（II）的化合物。

4. 发明申请

WO9902120A8 COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES 审中-公开
标题翻译：反应性增加生物膜渗透性的组合物和方法
公开(公告)号：WO9902120A8
公开(公告)日：2002-06-06
申请号：PCT/IL9800317
申请日：1998-07-07
申请人： DPHARM LTD , VINIKOVA MARINA , SHAPIRO ISRAEL , KOZAK ALEXANDER
发明人： VINIKOVA MARINA , SHAPIRO ISRAEL , KOZAK ALEXANDER
IPC分类号： A61K47/12 , A61K47/14 , A61K47/16 , A61K49/00 , C07C51/38 , C07C53/128 , C07C233/00 , C07F9/02
CPC分类号： C07C53/128
摘要： The present invention provides a family of branched fatty acids and their derivatives, which improve and enable the penetration and absorption of active ingredients through biomembranes, such as the blood brain barrier. The invention further provides pharmaceutical compositions comprising these branched fatty acids and methods of using these compositions to permeabilize biological membranes thereby improving the administration of bioactive or therapeutic substances to cells or organs. According to a more preferred embodiment of this invention the methods are particularly useful to treat certain kinds of CNS lesions and diseases including tumors, infections, abscesses and degenerative and behavioral disorders.
摘要翻译：本发明提供了一种支链脂肪酸及其衍生物，其改善并且能够通过生物膜如血脑屏障渗透和吸收活性成分。本发明进一步提供包含这些支链脂肪酸的药物组合物和使用这些组合物使生物膜透化从而改善对细胞或器官的生物活性或治疗物质的给药的方法。根据本发明的一个更优选的实施方案，该方法特别适用于治疗某些种类的CNS病变和疾病，包括肿瘤，感染，脓肿和退行性和行为障碍。

5. 发明申请

WO9422483A3 PRODRUGS WITH ENHANCED PENETRATION INTO CELLS 审中-公开
标题翻译：具有增强渗透入细胞的产品
公开(公告)号：WO9422483A3
公开(公告)日：1994-12-22
申请号：PCT/GB9400669
申请日：1994-03-30
申请人： KOSM GERALD EMMANUEL , DPHARM LTD , KOZAK ALEXANDER
发明人： KOZAK ALEXANDER
IPC分类号： C12P17/18 , A61K31/19 , A61K31/215 , A61K31/47 , A61K31/66 , A61K31/70 , A61K38/00 , A61K45/00 , A61K47/48 , A61P43/00 , C07F9/10 , C07F9/62 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/10 , A61K47/54 , A61K47/542 , A61K47/544
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 human related to supranormal intracellular enzyme (.e.g. phospholipase and/or esterase) 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 accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.
摘要翻译：本发明涉及药学上可接受的前体药物，其是药理学活性化合物和细胞内运输佐剂的共价缀合物，其特征在于存在对细胞内酶活性具有断裂敏感性的共价键。前药可用于治疗与超细胞内酶（“磷脂酶和/或酯酶”）活动相关的人的病症或疾病的技术，由此在将其施用于具有这种病症或疾病的人时，该结合被破坏响应于这种活性，并且药理活性化合物选择性地在具有这种超常规细胞内酶活性的细胞内积累。共轭物是式中羧基官能团的酯，庚酰基-sn-3-甘油磷酰胆碱或辛酰基-sn-3-甘油磷酰胆碱。

6. 发明申请

WO1994022483A2 PRODRUGS WITH ENHANCED PENETRATION INTO CELLS 审中-公开
标题翻译：具有增强渗透入细胞的产品
公开(公告)号：WO1994022483A2
公开(公告)日：1994-10-13
申请号：PCT/GB1994000669
申请日：1994-03-30
申请人： KOSMIN, Gerald, Emmanuel , D-PHARM, LTD. , KOZAK, Alexander
发明人： KOSMIN, Gerald, Emmanuel , D-PHARM, LTD.
IPC分类号： A61K47/48
CPC分类号： C07F9/10 , A61K47/54 , A61K47/542 , A61K47/544
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 human related to supranormal intracellular enzyme (e.g. phospholipase and/or esterase) 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 accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.
摘要翻译：本发明涉及药学上可接受的前体药物，其是药理学活性化合物和细胞内运输佐剂的共价缀合物，其特征在于存在对细胞内酶活性具有断裂敏感性的共价键。该前体药物可用于治疗与超细胞内酶（例如磷脂酶和/或酯酶）活性相关的人的病症或疾病的技术，由此在将其施用于具有这种病症或疾病的人时，该结合被破坏对这种活性的反应，并且药理活性化合物选择性地在具有这种超常规细胞内酶活性的细胞内积累。共轭物是式中羧基官能团的酯，庚酰基-sn-3-甘油磷酰胆碱或辛酰基-sn-3-甘油磷酰胆碱。

7. 发明申请

WO2005016229A2 USE OF LIPOPHILIC DIESTERS OF CHELATING AGENT FOR THE TREATMENT OF AMYLOIDOSIS AND ATHEROSCLEROSIS 审中-公开
标题翻译：麻醉药物治疗青光眼病和甲状腺功能亢进症的使用
公开(公告)号：WO2005016229A2
公开(公告)日：2005-02-24
申请号：PCT/IL2004/000746
申请日：2004-08-12
申请人： D-PHARM LTD. , ROSENBERG, Gilad, Israel , FRIEDMAN, Jonathan, Eduard , ANGEL, Itzchak , KOZAK, Alexander
发明人： ROSENBERG, Gilad, Israel , FRIEDMAN, Jonathan, Eduard , ANGEL, Itzchak , KOZAK, Alexander
IPC分类号： A61K
CPC分类号： A61K31/24
摘要： The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N’,N’-tetraacetic acid (BAPTA) for preventing, treating or managing atherosclerosis, amyloidosis-related diseases and disorders and other pathologies associated with proteins aggregations. In particular, these compounds are useful in treating cardiac and vascular amyloidosis, neurodegenerative diseases and disorders and cerebral amyloid angiopathy (CAA).
摘要翻译：本发明涉及螯合剂1,2-双（2-氨基苯氧基）乙烷-N，N，N'，N'-四乙酸（BAPTA）的亲脂性二酯用于预防，治疗或控制动脉粥样硬化，淀粉样变性 - 相关疾病和病症以及与蛋白质聚集相关的其他病理学。特别地，这些化合物可用于治疗心脏和血管淀粉样变性，神经变性疾病和病症以及脑淀粉样血管病（CAA）。

8. 发明申请

WO2004028443A3 LIPOPHILIC DIESTERS OF CHELATING AGENT FOR INHIBITION OF ENZYME ACTIVITY 审中-公开
标题翻译：用于抑制酶活性的螯合剂脂溶性二酯
公开(公告)号：WO2004028443A3
公开(公告)日：2004-05-27
申请号：PCT/IL0300225
申请日：2003-03-16
申请人： DPHARM LTD , STRIEM SARINA , FRIEDMAN JONATHAN EDUARD , REZNITSKY-COHEN DALIA , KOZAK ALEXANDER
发明人： STRIEM SARINA , FRIEDMAN JONATHAN EDUARD , REZNITSKY-COHEN DALIA , KOZAK ALEXANDER
IPC分类号： A61K31/225 , C07C229/00 , C07C205/00 , C07C211/00 , C07C233/00 , C07C249/00 , C07C291/00 , C07C335/00 , C07C381/00
CPC分类号： A61K31/225
摘要： The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA) for inhibition of proteolytic activities of certain metalloproteinases and of calpain. The invention further relates to methods for preventing, treating or managing MMP-related and calpain-related diseases or disorders in mammals comprising administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of said lipophilic diesters of the chelating agent BAPTA.
摘要翻译：本发明涉及螯合剂1,2-二（2-氨基苯氧基）乙烷-N，N，N'，N'-四乙酸（BAPTA）的亲脂二酯用于抑制某些金属蛋白酶的蛋白水解活性和钙蛋白酶。本发明进一步涉及用于预防，治疗或控制哺乳动物中的MMP-相关和钙蛋白酶相关疾病或病症的方法，其包括向需要其的哺乳动物施用药物组合物，所述药物组合物包含治疗有效量的螯合剂BAPTA的所述亲脂二酯。

9. 发明申请

WO0207669A3 PHOSPHOLIPID DERIVATIVES OF VALPROIC ACID AND MIXTURES THEREOF 审中-公开
标题翻译：磷酸及其混合物的磷脂衍生物
公开(公告)号：WO0207669A3
公开(公告)日：2003-01-09
申请号：PCT/IL0100629
申请日：2001-07-10
申请人： DPHARM LTD , KOZAK ALEXANDER
发明人： KOZAK ALEXANDER
IPC分类号： A61K31/683 , A61K31/19 , A61K31/352 , A61P25/00 , A61P25/06 , A61P25/08 , C07F9/10 , A61K31/685 , C07F9/02
CPC分类号： A61K31/352 , A61K31/19 , A61K47/544 , C07F9/10
摘要： The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.
摘要翻译：本发明涉及作为丙戊酸的磷脂衍生物的化合物，涉及包含所述化合物的组合物及其用于治疗癫痫，偏头痛，双相性精神障碍和疼痛的用途。

10. 发明申请

WO0211666A3 DERIVATIVES OF BRANCHED-CHAIN LIPOPHILIC MOLECULES AND USES THEREOF 审中-公开
标题翻译：支链亲脂性分子的衍生物及其用途
公开(公告)号：WO0211666A3
公开(公告)日：2002-07-11
申请号：PCT/IL0100713
申请日：2001-08-01
申请人： DPHARM LTD , KOZAK ALEXANDER , VINNIKOVA MARINA , POLYAK MICHAEL , BEIT-YANNAI ELIEZER , REZNITSKY-COHEN DALIA
发明人： KOZAK ALEXANDER , VINNIKOVA MARINA , POLYAK MICHAEL , BEIT-YANNAI ELIEZER , REZNITSKY-COHEN DALIA
IPC分类号： A61K47/06 , A61K38/00 , A61K45/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/02 , C07F9/09 , C07F9/10 , C07F9/11
CPC分类号： C07F9/11 , C07F9/091 , C07F9/10
摘要： The present invention discloses novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth. The invention further discloses pharmaceutical compositions comprising said molecules and their uses.
摘要翻译：本发明公开了用于透化生物屏障和抑制肿瘤生长的支链亲脂性分子的新型磷酸衍生物。本发明进一步公开了包含所述分子及其用途的药物组合物。

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