Pharmion Corporation

Celgene Corporation

Ash Stevens, Inc.

Lixte Biotechnology, Inc.

Celgene International Sarl

Dumitru Ionescu

Peter Blumbergs

Gary Lee Silvey

Lee Alani Selvey

Jason J Piotrowski

The present invention provides a process for producing the compound having the structure: comprising  

Process of synthesizing 3-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1] heptane-2-carboxylic acid

The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacyditine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.

Pharmaceutical compositions comprising forms of 5-azacytidine

The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

Methods for isolating crystalline form I of 5-azacytidine

Provided herein are pharmaceutical compositions or dosage forms comprising crystalline 5-azacytidine monohydrate. The pharmaceutical compositions or dosage forms provided herein may be used for oral administration in the treatment of diseases, including the treatment of myelodysplastic syndromes (MDS).

Pharmaceutical compositions comprising 5-azacytidine monohydrate

The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula:  The invention also includes pharmaceutical compositions comprising said forms.

Pharmaceutical compositions comprising crystal forms of 5-azacytidine

The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure:  The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected &#x3b2;-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

Synthesis of 5-azacytidine

The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.

Forms of 5-azacytidine

The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure also includes pharmaceutical compositions comprising said forms.

Forms of 5-Azacytidine

The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected &#x3b2;-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula:The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

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Ann Arbor, MI, United States of America

Dumitru Ionescu