Tel Aviv University

Bar-ilan University

Biolinerx Ltd.

Ada Rephaeli

Abraham Nudelman

Irit Gil-Ad

Abraham Weizman

Efrat Halbfinger

Mazal Shaul

Gideon Stein

Zvi Malik

Avraham Weizman

Gili Berkovitch-Luria

Ilan Winkler

Ran Lifshitz

Kinneret Savitsky

Yona Geffen

Dvir Doron

Nataly Tarasenko

Shlomit Halachmi

Eran J Benjamin

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.

Derivatives of purinic and pyrimidinic antiviral agents and use thereof as potent anticancer agents

The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

5-aminolevulinic acid derivatives, methods for their preparation and uses thereof

Methods and articles of manufacture for use in improving a cognitive function, utilizing a conjugate comprising a first moiety having GABA agonist activity and a second moiety having CNS activity being covalently linked to the first moiety, are disclosed. Also disclosed are methods and articles of manufacture of preventing onset or inhibiting progression of a cognitive impairment or dysfunction utilizing the disclosed conjugate.

Methods of improving cognitive functions

An acid addition salt of a nortriptyline-GABA conjugate, a novel crystalline form of a fumaric acid addition salt of a nortriptyline-GABA conjugate, and processes of preparing the forgoing are disclosed. Uses of the above-indicated forms of a nortriptyline-GABA conjugate in the treatment of CNS disorders, and in the treatment of pain in particular, are also disclosed. Further disclosed in a large-scale process of preparing a nortriptyline-GABA conjugate.

Acid addition salt of a nortriptyline-GABA conjugate and a process of preparing same

A conjugate comprising L-DOPA covalently linked to at least one &#x3b3;-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Conjugates for treating neurodegenerative diseases and disorders

A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.

Conjugates comprising a psychotropic drug or a GABA agonist and an organic acid and their use in treating pain and other CNS disorders

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&#xb0; 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.

Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same

Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Conjugated psychotropic drugs and uses thereof

Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.

Growing community of inventors

Herzlia, Israel

Ada Rephaeli