Pharmion Corporation

Ash Stevens, Inc.

Celgene Corporation

US Government as Represented by the Secretary of the Army

Dana-Farber-Cancer Institute Inc.

Celgene International Sarl

Peter Blumbergs

Dumitru Ionescu

Gary Lee Silvey

Lee Alani Selvey

Andre Rosowsky

Maurice P LaMontagne

Mohammed Salahuddin Khan

Henry Bader

Ming-The Lin

Richard L Kalamas

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).

In one embodiment, the present invention relates to a new class of ammonium salts of N-acyl derivatives of N-(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to formula II-IV. Formula II has the structure of: The ammonium salts provided by the invention exhibit high inhibitory activity against the growth o methotrexate-resistant cells, and also exhibit superior chemical stability than corresponding acidic N-acyl derivatives of N-acyl derivatives of N(4-amino-4-deoxypteroyl)-L-ornithine compounds.

Pharmaceutically active ornithine derivatives, ammonium salts thereof and methods of making same

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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Royal Oak, MI, United States of America

Peter Blumbergs