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

Applicant: D-PHARM LTD. ,  ROSENBERG, Gilad, Israel ,  FRIEDMAN, Jonathan, Eduard ,  ANGEL, Itzchak ,  KOZAK, Alexander

Inventor： ROSENBERG, Gilad, Israel ,  FRIEDMAN, Jonathan, Eduard ,  ANGEL, Itzchak ,  KOZAK, Alexander

IPC: A61K

CPC classification number: A61K31/24

Abstract: 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).

Abstract translation: 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）。

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

Applicant: DPHARM LTD ,  STRIEM SARINA ,  FRIEDMAN JONATHAN EDUARD ,  REZNITSKY-COHEN DALIA ,  KOZAK ALEXANDER

Inventor： STRIEM SARINA ,  FRIEDMAN JONATHAN EDUARD ,  REZNITSKY-COHEN DALIA ,  KOZAK ALEXANDER

IPC: A61K31/225 ,  C07C229/00 ,  C07C205/00 ,  C07C211/00 ,  C07C233/00 ,  C07C249/00 ,  C07C291/00 ,  C07C335/00 ,  C07C381/00

CPC classification number: A61K31/225

Abstract: 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.

Abstract translation: 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 。

公开(公告)号：WO2005016229A3

公开(公告)日：2005-04-21

申请号：PCT/IL2004000746

申请日：2004-08-12

Applicant: DPHARM LTD ,  ROSENBERG GILAD ISRAEL ,  FRIEDMAN JONATHAN EDUARD ,  ANGEL ITZCHAK ,  KOZAK ALEXANDER

Inventor： ROSENBERG GILAD ISRAEL ,  FRIEDMAN JONATHAN EDUARD ,  ANGEL ITZCHAK ,  KOZAK ALEXANDER

IPC: A61K20060101 ,  A61K31/24 ,  C07C20060101

CPC classification number: A61K31/24

Abstract: 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).

Abstract translation: 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）的亲脂二酯用于预防，治疗或控制动脉粥样硬化，淀粉样变性 - 相关的疾病和障碍以及与蛋白质聚集相关的其他病症。 具体而言，这些化合物可用于治疗心脏和血管淀粉样变性病，神经变性疾病和病症以及脑淀粉样血管病（CAA）。

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

Applicant: D-PHARM LTD. ,  STRIEM, Sarina ,  FRIEDMAN, Jonathan, Eduard ,  REZNITSKY-COHEN, Dalia ,  KOZAK, Alexander

Inventor： STRIEM, Sarina ,  FRIEDMAN, Jonathan, Eduard ,  REZNITSKY-COHEN, Dalia ,  KOZAK, Alexander

IPC: A61K

CPC classification number: A61K31/225

Abstract: 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.

Abstract translation: 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 。