Chemagis Ltd.

Ramot at Tel-aviv University Ltd.

Vladimir Naddaka

Oded Arad

Shady Saeed

Joseph Kaspi

Eyal Klopfer

Stephen Cherkez

Ofer Sharon

Shen Jingshan

Shadi Saeed

Fernando Patolsky

Vadim Krivitsky

Ori Lerman

Itai Adin

Guo Hongli

Dionne Montviliski

Lior Zelikovitch

Guy Davidi

Carmen Iustain

Le-Chang Hsiung

Jael Lexner

Naim Menashe

Systems and methods for sensing target molecules such as redox reactive agents, comprising a sample compartment and a sensing compartment being in fluid communication, are disclosed. A sensing compartment which comprises nanostructures to which a functional moiety is covalently attached and which is such that upon contacting a redox reactive agent a change in electrical property of the nanostructure occurs, and integration of such a sensing compartment with sensing systems as described herein are also disclosed. Methods of monitoring a metabolic activity of cells, and uses thereof, are also disclosed.

Method and system for sensing

The present invention provides novel isoquinolinium compounds, methods of producing the isoquinolinium compounds, and methods for converting them into cisatracurium, e.g., cisatracurium besylate. The isoquinolinium compounds of the present invention can be obtained in the form of solids, which can be purified using simple techniques and can be used to afford pure cisatracurium besylate without HPLC purification.

Isoquinolinium compounds useful in the preparation of cisatracurium and associated intermediates

The present invention provides processes for producing isoquinolinium compounds, and for converting them into cisatracurium salts, e.g., cisatracurium besylate

Process for producing cisatracurium compounds and associated intermediates

Provided is a process for producing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod), which includes reacting 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline with a non-gaseous amine precursor. Also provided are methods for isolating highly pure imiquimod. Further provided are intermediates useful in the production of imiquimod, methods for producing such intermediates, and methods for obtaining imiquimod from such intermediates.

Imiquimod production process

Derivatives of 1,2-benzisoxazole-3-methanesulfonic acid, which are non-hygroscopic and non-hydrated and their use as intermediates from the preparation of zonisamide are disclosed. Further disclosed are processes of preparing zonisamide from these 1,2-benzisoxazole-3-methanesulfonic acid derivatives, processes of preparing exemplary 1,2-benzisoxazole-3-methanesulfonic acid derivatives and crystalline forms of exemplary 2-benzisoxazole-3-methanesulfonic acid derivatives. A novel process of preparing zonisamide is also disclosed.

Derivatives of 1,2-benzisoxazole-3-methane sulfonic acid as novel intermediates for the synthesis of zonisamide

The present invention provides a process for preparing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod). The process preferably includes heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with ammonia in a polar aprotic solvent at relatively moderate pressure to produce imiquimod, and optionally purifying the imiquimod. The process of the present invention can produce highly pure imiquimod in high yield.

A novel process for preparing highly pure cilostazol, effected by reacting 6-hydroxy-3,4-dihydroquinolinone and 5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole in the presence of a hydrated inorganic base, is disclosed. Further disclosed is highly pure cilostazol, and particularly highly pure cilostazol that is substantially free of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butoxy]-1-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butyl ]-3,4-dihydro-1H-quinolin-2-one.

Highly pure cilostazol and an improved process for obtaining same

The present invention provides a process for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (Imiquimod) of formula (I). The process comprises heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with formamide, and optionally with bubbling of gaseous ammonia to afford Imiquimod of formula (I). According to the present invention, by using this process and novel purification methods, essentially as described herein, highly pure Imiquimod is obtained.

Process for preparing Imiquimod

The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): which comprises reacting a methylating agent with indazole-3-carboxylic acid of formula (VI): in the presence of an alkaline earth metal oxide or alkoxide in an appropriate solvent. Also provided is a process for producing Granisetron, using the method of the present invention for producing 1-methylindazole-3-carboxylic acid.

Process for preparing 1-methylindazole-3-carboxylic acid

The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH CONH , wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100&deg; C.

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Lod, Israel

Vladimir Naddaka