公开(公告)号：WO2005016228A2

公开(公告)日：2005-02-24

申请号：PCT/IL2004/000745

申请日：2004-08-12

Applicant: D-PHARM LTD. ,  ADVANCED NEUROPROTECTIVE SYSTEMS LTD. ,  DOLINA, Svetlana ,  SHTEIMAN, Vitaly ,  VINNIKOVA, Marina ,  SHAPIRO, Israel

Inventor： DOLINA, Svetlana ,  SHTEIMAN, Vitaly ,  VINNIKOVA, Marina ,  SHAPIRO, Israel

IPC: A61K

CPC classification number: C07D213/63 ,  C07D401/12

Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuroprotective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.

Abstract translation: 本发明涉及可用于降低癫痫发作风险和/或减轻患者癫痫现象的化合物和组合物。 根据本发明，化合物和组合物至少具有以下两种组分：a）选自吡哆醛，吡哆胺，吡哆醇，它们的药学上可接受的官能衍生物和盐的基于维生素B6的组分; 和b）至少一种抗癫痫药物（AED）或抗惊厥，神经保护药物或甘油三酯化合物或部分。 本发明进一步涉及预防癫痫发作和减轻癫痫发作的方法，以及减少抗癫痫药副作用的方法。

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

Applicant: DPHARM LTD ,  VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

Inventor： VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

IPC: A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K49/00 ,  C07C51/38 ,  C07C53/128 ,  C07C233/00 ,  C07F9/02

CPC classification number: C07C53/128

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2011086561A1

公开(公告)日：2011-07-21

申请号：PCT/IL2011/000050

申请日：2011-01-17

Applicant: D-PHARM LTD. ,  SHAPIRO, Israel ,  VISHKAUTSAN, Rosita ,  VINNIKOVA, Marina

Inventor： SHAPIRO, Israel ,  VISHKAUTSAN, Rosita ,  VINNIKOVA, Marina

IPC: C07D263/30 ,  C07D413/00

CPC classification number: C07C51/412 ,  A01N3/02 ,  A23B7/154 ,  A23L3/3508 ,  C07C51/09 ,  C07C67/343 ,  C07C2601/02 ,  C07C53/23 ,  C07C57/26 ,  C07C69/635

Abstract: The present invention relates to a process for the preparation of highly pure 3-(1-cyclopropenyl) propionic acid salt, particulary 3-(1-cyclopropenyl) propionic acid sodium salt, an ethylene receptor antagonist that may be used for inhibiting the abscission and ripening of plants and for prolonging the life of picked fruit, vegetable and cut flowers.

Abstract translation: 本发明涉及一种制备高纯度3-（1-环丙烯基）丙酸盐，特别是3-（1-环丙烯基）丙酸钠盐的方法，可用于抑制脱落的乙烯受体拮抗剂和 植物成熟和延长采摘水果，蔬菜和切花的寿命。

公开(公告)号：WO9916741A3

公开(公告)日：1999-07-01

申请号：PCT/IL9800468

申请日：1998-09-27

Applicant: PHARM LIMITED D ,  KOZAK ALEXANDER ,  SHAPIRO ISRAEL

Inventor： KOZAK ALEXANDER ,  SHAPIRO ISRAEL

IPC: A61K31/223 ,  A61K31/22 ,  A61P1/00 ,  A61P1/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P11/08 ,  A61P13/00 ,  A61P13/02 ,  A61P13/08 ,  A61P21/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  C07C229/00 ,  C07C229/16 ,  C07C229/76 ,  C09K3/00 ,  A61K31/225

CPC classification number: C07C229/16 ,  C07C229/76 ,  Y10S514/826 ,  Y10S514/836 ,  Y10S514/886

Abstract: The invention discloses stable diesters of chelating agents of divalent metal ions, processes for their preparation and pharmaceutical compositions thereof. Most preferred compounds according to the present invention are stable lipophilic diesters comprising a covalent conjugate of a BAPTA and a pharmaceutically acceptable alcohol. The diesters are useful in a method for treating a condition or disease related to an excess of divalent metal ions, and in particular for the treatment of a condition or disease related to elevated levels of intracellular calcium ions, such as in brain or cardiac ischemia, stroke, epilepsy, Alzheimer's disease or cardiac arrhythmia and in open heart surgery.

Abstract translation: 本发明公开了二价金属离子螯合剂的稳定二酯，其制备方法及其药物组合物。 根据本发明的最优选的化合物是包含BAPTA和药学上可接受的醇的共价缀合物的稳定的亲脂性二酯。 二酯可用于治疗与过量的二价金属离子有关的病症或疾病，特别是用于治疗与细胞内钙离子水平升高相关的病症或疾病，例如脑或心脏局部缺血， 中风，癫痫，阿尔茨海默病或心律失常以及心脏直视手术。

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

Applicant: DPHARM LTD ,  KOZAK ALEXANDER ,  VINIKOVA MARINA ,  SHAPIRO ISRAEL

Inventor： VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

IPC: A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K49/00 ,  C07C51/38 ,  C07C53/128 ,  A61K

CPC classification number: C07C53/128

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2005016228A3

公开(公告)日：2005-05-19

申请号：PCT/IL2004000745

申请日：2004-08-12

Applicant: DPHARM LTD ,  ADVANCED NEUROPROTECTIVE SYSTE ,  DOLINA SVETLANA ,  SHTEIMAN VITALY ,  VINNIKOVA MARINA ,  SHAPIRO ISRAEL

Inventor： DOLINA SVETLANA ,  SHTEIMAN VITALY ,  VINNIKOVA MARINA ,  SHAPIRO ISRAEL

IPC: A61K20060101 ,  A61K31/44 ,  A61P25/08 ,  C07D20060101 ,  C07D213/02

CPC classification number: C07D213/63 ,  C07D401/12

Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuroprotective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.

Abstract translation: 本发明涉及用于降低患者癫痫发作风险和/或缓解患者癫痫现象的化合物和组合物。 根据本发明，化合物和组合物至少具有以下两个组分：a）选自吡哆醛，吡哆胺，吡哆醇及其药学上可接受的官能衍生物和盐的维生素B6基成分; 和b）至少一种抗癫痫药物（AED）或抗惊厥，神经保护药物或指头化合物或部分。 本发明还涉及用于预防癫痫发作和减轻癫痫发作的方法以及减少抗癫痫药物的副作用的方法。

公开(公告)号：WO0119320A2

公开(公告)日：2001-03-22

申请号：PCT/IL0000562

申请日：2000-09-13

Applicant: DPHARM LTD ,  KOZAK ALEXANDER ,  SHAPIRO ISRAEL ,  VINNIKOVA MARINA ,  ERSHOV LEONID ,  SENDERIKHIN ALEXANDER ,  AYALON ORAN

Inventor： KOZAK ALEXANDER ,  SHAPIRO ISRAEL ,  VINNIKOVA MARINA ,  ERSHOV LEONID ,  SENDERIKHIN ALEXANDER ,  AYALON ORAN

IPC: A61K47/48 ,  A61K20060101 ,  A61K9/02 ,  A61K9/06 ,  A61K9/08 ,  A61K9/10 ,  A61K9/12 ,  A61K9/20 ,  A61K9/48 ,  A61K9/72 ,  A61K31/56 ,  A61K31/661 ,  A61K45/00 ,  A61P1/04 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07F20060101 ,  C07F9/6512 ,  C07F9/6524 ,  A61K

CPC classification number: A61K47/544

Abstract: The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via a bridging group, to a phospholipid moiety such that the active species is preferentially released, preferably by enzymatic cleavage, at the required site of action. The invention further discloses pharmaceutical compositions comprising said prodrugs and the uses thereof for the treatment of diseases and disorders related to inflammatory, to degenerative or atrophic conditions, and to uncontrolled cell growth.

Abstract translation: 本发明公开了包含通过桥连基团共价连接到磷脂部分的抗增殖药物的前药，使得活性物质优选通过酶裂解在所需的作用位点释放。 本发明进一步公开了包含所述前体药物及其用途的药物组合物，用于治疗与炎性，退行性或萎缩状态相关的疾病和病症以及不受控制的细胞生长。