Azithromycin preparation in its noncryst alline and crystalline dihydrate forms

Patent 6451990 Issued on September 17, 2002. Estimated Expiration Date:

November 22, 2020. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Abstract Claims Description Full Text

Patent References

N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor
Patent #: 4474768
Issued on: 10/02/1984
Inventor: Bright

11-Methyl-11-aza-4-0-cladinosyl-6-0-desosaminyl-15-ethyl-7,1 3,14-trihydroxy-3,5,7,9,12,14-hexamethyl-oxacyclopentadecane-2-one and derivatives thereof
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Patent #: 5686587
Issued on: 11/11/1997
Inventor: Yang

Synthesis of 9-deoxo-9a-aza-11,12-deoxy-9a-methyl-9a-homoerythromycin A 11,12 Hydrogenorthoborate dihydrate and a process for the preparation of azitromicin dihydrate
Patent #: 5869629
Issued on: 02/09/1999
Inventor: Bayod Jasanda, et al.

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof Patent #: 6245903
Issued on: 06/12/2001
Inventor: Karimian , et al.

Inventors

Assignee

Astur-Pharma, S.A.

Application

No. 718833 filed on 11/22/2000

US Classes:

536/7.4, Additional nitrogen containing536/18.5Processes

Examiners

Primary: Peselev, Elli

Attorney, Agent or Firm

Knobbe, Martens, Olson & Bear, LLP

Foreign Patent References

SP 95-1389 EC. 05/13/1995
0 941 999 EP. 09/13/1999
WO 89/00576 WO. 01/13/1989

International Class

C07H 001/00

Foreign Application Priority Data

1999-11-26 ES

Abstract

The present invention describes new procedures for the preparation of the macrolide azithromycin in its non-crystalline and crystalline dihydrate forms, which are characterized and clearly differentiated by means of the following methods and techniques:1. IR Spectroscopy.2. Differential Scan Calorimetry (DSC).3. X-Ray Diffraction.4. Hygroscopicity.5. Crystallinity test (Light Polarized Microscopy) ##STR1##

Other References

Chemical Abstracts--26--Biomolecules and Their Synthetic Analogs, vol. 124, No. 3, 1996, 29525q, Q. Song, et al. "Preparation of crystals of azithromycin via crystalization from various solvents.
J. Chem. Research (S), 1988, 152-153, "Erythromycin Series. Part 13. Synthesis and Structure Elucidation of 10-Dihydro-10-deoxo-11-methyl-11-azaerythromycin A", Slobodan Djokic, et al
J. Org. Chem , American Chemical Society, 1997, "Synthesis of 9-deoxo-9a-aza-9a-homoerythromycin A 11, 12-Hydrogen Borate and Azithromycin 11, 12-Hydrogen Borate. A new Procedure to Obtain Azithromycin Dihydrate" by M. Bayod-Jasanada, et a