# US 7,410,952 B2 · Derivatives of azithromycin

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- Number: US 7,410,952 B2
- Document ID: US7410952B2
- Status: Granted
- Kind: B2
- Application number: 10/552,318
- Filed: 2004-04-16
- Published: 2007-02-22
- Granted: 2008-08-12
- Earliest claimed: 2003-04-17
- Assignees: Sandoz Ltd.
- Inventors: Albert Codony; José Diago; Rafael Garcia; Jordi Rifa
- Web page: https://patentgrep.com/patent/US7410952B2

## CPC

- C07H 17/08: Hetero rings containing eight or more ring members, e.g. erythromycins
- A61K 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The invention relates to derivatives of azithromycin, processes for the manufacture thereof and pharmaceutical compositions thereof preferably together with azithromycin.

## Claims

### Claim 1

A derivative of azithromycin as base or in the form of an acid addition salt which is
3′-(N,N-didemethyl)-3′-N-formylazithromycin of formula 2.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising the derivative of azithromycin according to claim 1.

### Claim 3 (depends on 1)

A pharmaceutical composition according to claim 1 comprising a mixture of
i) the derivative of azithromycin according to claim 1, and
ii) any azithromycin base or salt in any crystalline, polymorphic or amorphous form,
wherein the weight ratio of the at least one derivative described in i) and azithromycin as described in ii) is between 0.1 and 99.

### Claim 4

A process for preparing 3′-(N,N-didemethyl)-3′-N-formylazithromycin of formula 2 comprising formylation of 3′-aminoazithromycin of formula 6.

### Claim 5 (depends on 4)

A process according to claim 4 wherein the formylation of 3′-aminoazithromycin is carried out by using formic acetic anhydride.