RU2001132327A

RU2001132327A - APPLICATION OF MACROLIDE COMPOUNDS FOR THE TREATMENT OF EYE DRYNESS

Info

Publication number: RU2001132327A
Application number: RU2001132327/14A
Authority: RU
Inventors: Риудзи УЕНО
Original assignee: Сукампо Аг
Priority date: 1999-04-30
Filing date: 2000-04-26
Publication date: 2003-07-27

Claims

1. An agent for treating dry eye, comprising a macrolide compound as an active ingredient.

2. The tool according to claim 1, in which the macrolide compound is a tricyclic compound (I) of the following formula:

where adjacent pairs of R ¹ and R ² , R ³ and R ⁴ and R ⁵ and R ⁶ each independently a) consists of two adjacent hydrogen atoms, when R ² optionally represents alkyl, or (b) forms another bond between the atoms carbon bonded to members of each pair;

R ⁷ represents a hydrogen atom, hydroxyl, alkyloxy or protected hydroxyl, or may form oxo with R ¹ ;

R ⁸ and R ⁹ each independently represent a hydrogen atom or hydroxyl;

R ¹⁰ represents a hydrogen atom, alkyl, alkenyl, alkyl substituted with one or more hydroxyl, alkenyl substituted with one or more hydroxyl, or alkyl substituted with oxo;

X represents oxo, (hydrogen atom, hydroxyl), (hydrogen atom, hydrogen atom) or a group of the formula —CH ₂ O—;

Y represents oxo, (hydrogen atom, hydroxyl), (hydrogen atom, hydrogen atom) or a group of the formula N-NR ¹¹ R ¹² or N-OR ¹³ ;

R ¹¹ and R ¹² each independently represent a hydrogen atom, alkyl, aryl or tosyl;

R ¹³ , R ¹⁴ , R ¹⁵ , R ¹⁶ , R ¹⁷ , R ¹⁸ , R ¹⁹ , R ²² and R ²³ each independently represent a hydrogen atom or an alkyl;

R ²⁴ represents an optionally substituted ring, which optionally contains one or more heteroatoms; and

n = 1 or 2,

where Y, R ¹⁰ and R ²³ optionally form, together with the carbon atom to which they are attached, a saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom, a sulfur atom and / or an oxygen atom; said heterocyclic group may be substituted with one or more groups selected from the group consisting of alkyl, hydroxyl, alkyloxy, benzyl, a group of the formula —CH ₂ Se (C ₆ H ₅ ) and alkyl substituted with one or more hydroxyl,

or a pharmaceutically acceptable salt thereof.

3. The tool according to claim 1 or 2, in which the macrolide compound is FK506.

4. The tool according to any one of claims 1 to 3, which is in the form of a preparation for topical administration to the eye.

5. The tool according to any one of claims 1 to 4, which is intended to improve the tear time of the tear film.

6. A method for treating dry eye, comprising administering an effective amount of a macrolide compound to a subject who needs treatment for dry eye.

7. The use of macrolide compounds for the manufacture of pharmaceutical compositions for the treatment of dry eyes.