公开(公告)号：US20170189376A1

公开(公告)日：2017-07-06

申请号：US15397780

申请日：2017-01-04

Applicant: MOR RESEARCH APPLICATIONS LTD. ,  BAR-ILAN UNIVERSITY

Inventor： Lilach Moyal ELCHARAR ,  Emmilia HODAK ,  Ada REPHAELI ,  Abraham NUDELMAN

IPC: A61K31/385 ,  A61K31/704 ,  A61K45/06

CPC classification number: A61K31/385 ,  A61K31/704 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods for treating ameliorating, reducing and/or preventing a cutaneous T-cell lymphoma in a subject in need thereof, comprising administration butyroyloxymethyl diethyl phosphate (AN-7) alone or combined with an additional anti-cancer therapy.

公开(公告)号：US20240216320A1

公开(公告)日：2024-07-04

申请号：US18605474

申请日：2024-03-14

Applicant: Augusta University Research Institute, Inc. ,  Bar Ilan University ,  Ramot at Tel-Aviv University Ltd.

Inventor： Betty S. PACE ,  Abraham NUDELMAN ,  Zvi MALIK ,  Ada REPHAELI

IPC: A61K31/22 ,  A61K9/00 ,  A61K31/17 ,  A61P7/06

CPC classification number: A61K31/22 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/17 ,  A61P7/06

Abstract: It has been found that the prodrug 1-(butyryloxy)ethyl-5-amino-4-oxopentanoate (AN-233), an oral active conjugate of BA (histone deacetylase inhibitor) and ALA (heme precursor), is useful for the treatment of hemoglobinopathies including but not limited to sickle cell disease and thalassemias. In one embodiment, AN-233 activates γ-globin transcription, induces HbF expression, produces an anti-sickling effect, or combinations thereof when administered to a subject in need thereof.

公开(公告)号：US20140371245A1

公开(公告)日：2014-12-18

申请号：US14339491

申请日：2014-07-24

Applicant: Ramot at Tel-Aviv University Ltd. ,  Bar-Ilan University

Inventor： Abraham NUDELMAN ,  Ada REPHAELI

IPC: C07D473/18

CPC classification number: C07D473/18

Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.

Abstract translation: 公开了嘌呤和嘧啶核苷类似物的新型N-酰化，O-酰化和（双或三）-N，O-酰化衍生物，含有它们的药物组合物及其用于治疗增殖性疾病或病症的用途。

公开(公告)号：US20210145783A1

公开(公告)日：2021-05-20

申请号：US17099455

申请日：2020-11-16

Applicant: Augusta University Research Institute, Inc. ,  Bar Ilan University ,  Ramot at Tel-Aviv University Ltd.

Inventor： Betty S. PACE ,  Abraham Nudelman ,  Zvi MALIK ,  Ada REPHAELI

IPC: A61K31/22 ,  A61K31/17 ,  A61K9/00 ,  A61P7/06

Abstract: It has been found that the prodrug 1-(butyryloxy)ethyl-5-amino-4-oxopentanoate (AN-233), an oral active conjugate of BA (histone deacetylase inhibitor) and ALA (heme precursor), is useful for the treatment of hemoglobinopathies including but not limited to sickle cell disease and thalassemias. In one embodiment, AN-233 activates γ-globin transcription, induces HbF expression, produces an anti-sickling effect, or combinations thereof when administered to a subject in need thereof.

公开(公告)号：US20150216830A1

公开(公告)日：2015-08-06

申请号：US14663767

申请日：2015-03-20

Applicant: BAR ILAN UNIVERSITY ,  RAMOT AT TEL AVIV UNIVERSITY LTD.

Inventor： Ada REPHAELI ,  Nataly TARASENKO ,  Zvi MALIK ,  Abraham NUDELMAN ,  Gili BERKOVITCH-LURIA ,  Dvir DORON

IPC: A61K31/221 ,  A61K45/06

CPC classification number: A61K31/221 ,  A61K31/197 ,  A61K31/225 ,  A61K41/0061 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K2300/00 ,  A61N5/062 ,  C07C229/22

Abstract: There are provided conjugates comprising 5-aminolevulinic acid (5-ALA), an aldehyde and a carboxylic acid (e.g., a histone deacetylase inhibitor), compositions comprising same, methods for their preparation and uses thereof for treatment of cancer and anemia, and for inducing erythropoiesis.

Abstract translation: 提供了包含5-氨基乙酰丙酸（5-ALA），醛和羧酸（例如组蛋白脱乙酰酶抑制剂）的组合物，包含其的组合物，其制备方法及其用于治疗癌症和贫血，以及用于 诱导红细胞生成。

公开(公告)号：US20130150352A1

公开(公告)日：2013-06-13

申请号：US13763815

申请日：2013-02-11

Applicant: Ramot at Tel-Aviv University Ltd. ,  Bar-Ilan University ,  BioLineRX Ltd.

Inventor： Abraham NUDELMAN ,  Ada REPHAELI ,  Irit GIL-AD ,  Abraham WEIZMAN ,  Mazal SHAUL ,  Efrat HALBFINGER

IPC: C07D417/06

CPC classification number: C07D417/06 ,  C07D279/28 ,  Y10T428/2982

Abstract: Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.

Abstract translation: 公开了4-氨基丁酸三苯甲磺隆的奋乃静化新型结晶形式及其生产方法。 新型结晶形式的特征在于独特的XRPD图案和DSC，其在相对较高的温度（例如高于209℃）下显示出吸热峰。 还公开了通过在单步合成中原位去保护和成盐，以及由此得到的高纯度的奋乃静4-氨基丁酸三苯甲磺酸盐，制备4-氨基丁酸三苯甲基奋乃静化物的方法。 还公开了所述所述的所述4-氨基丁酸三苯甲磺酸激素的用途。