Traitement en cours

Veuillez attendre...

Paramétrages

Paramétrages

Aller à Demande

1. WO2020117637 - PROMÉDICAMENTS AGONISTES MUSCARINIQUES CONTENANT UN CYCLE QUINUCLIDINE ET COMPOSITIONS ET MÉTHODES ASSOCIÉES

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

WHAT IS CLAIMED IS:

1. A compound of formula (I)


m, n, p and q are each independently an integer of 0 or 1 ;

X is C or S;

Y is C, N. O, S or
wherein when Y is C an alkyne is optionally formed, when Y is N an irnine or an oxime is formed, and when Y is O a carbonyl is formed;

R1 has the formula -CH-R3-0-R4;

R2 is an optionally substituted imine or oxime;

RJ is selected from H or an alkyl; and

R4 is selected from a phosphate, a sulfate, a trifluoroacetate or a polar amino acid, or any pharmaceutically acceptable salt, ester or prodrug thereof.

2. The compound of claim 1 wherein:

m, and n are 0;

p and q are 1 ;

X is C;

Y is N wherein an imine or an oxime is formed; and


3. The compound of claim 2 selected from

4. The compound of claim 1 wherein: m and p are 1 ;

n and q are 0;

X is C; and

Y is O.

5. The compound of claim 1 selected from


6. A compound of formula IL


or a pharmaceutically acceptable salt, ester or prodrug thereof.

7. An ophthalmologieal composition comprising a therapeutically effective amount of a compound of any of claims 1-8 wherein the pH of the composition is at least 3 log units less than the pKa of the compo und

8. The composition of claim 9 further comprising a cyclodextrin.

9. The composition of claim 10 wherein the cyclodextrin is selected from an alpha- cyclodextrin, a beta-cyclodextrin and a gamma-cyclodextrin.

10. A method of treating presbyopia or glaucoma comprising administering to a patient in need thereof a therapeutically effective amount of a compound of any of claims 1 -9.

11. A method of reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of any of claims 1-9.