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US 11,306,090 B2Granted
Azabicyclo and diazepine derivatives
AssigneeAlcon Inc.
InventorsDavid Ellis, Howard Allen Ketelson
Life of this patent
Estimating the term…
Abstract
The present invention provides in one aspect azabicyclo and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator.
Claims14
A compound or a pharmaceutically acceptable salt thereof, wherein the compound is presented by formula (I):
- wherein
- Me=CH3;
- A=NR5;
- X=—OH, —O—Y—Z, —S—Y—Z, or —NR5—Y—Z;
- R1 and R2 are independently H, D, hydroxyl, alkoxy, nitrile, halogen atoms, C1-C20 straight, branched or cyclo alkyl groups optionally substituted with halogen atoms;
- or
- R1 and R2 are independently phenyl or benzyl groups being optionally substituted with one or more substituents selected from C1-C20 straight, branched or cyclo alkyl groups, halo alkyl groups, hydroxyl, alkoxy, nitrile, nitro, amino, amide, ester, sulfone, sulfoxide, sulfonamide, and halogen atoms;
- or
- R1 and R2 are independently a heterocyclic saturated, unsaturated or aromatic 5- or 6-member ring containing one or more heteroatoms selected from nitrogen, oxygen and sulfur and being optionally substituted with one or more substituents selected from C1-C20 straight, branched or cyclo alkyl, halo alkyl groups, hydroxyl, alkoxy, nitrile, nitro, amino, amide, ester, sulfone, sulfoxide or halogen atoms;
- R3 and R4 are independently hydrogen, C1-C10 straight or branched or cyclo alkyl or halo alkyl groups or
- R3 and R4 can combine to form 3- to 6-membered rings;
- R5═H, a C1-C20 straight or branched alkyl groups, or a C1-C10 straight or branched haloalkyl groups;
- Y is a bivalent radical having the following meaning:
- a) Straight or branched C1-C20 alkyl, being optionally substituted with one or more of the substituents selected from the group consisting of:
- halogen atoms and hydroxyl;
- b) —C(O)(C1-C10 alkyl)- or —C(O)(CH2)nC(O)O—(C1-C10 alkyl)- or —(C1-C10 alkyl)-;
- c)
- d)
- e)
- or
- f)
- wherein n is an integer from 0 to 20;
- R6 and R7 are independently H or C1-C10, straight or branched alkyl groups, C1-C10 straight or branched haloalkyl groups;
- or
- R6 and R7 can combine to form 3- to 6-membered rings;
- and
- Z is H, —OH, C1-6 alkoxy, —COOH, —NR8R9;
- R8 and R9 are independently C1-C20 alkyl, being optionally substituted with one or more substituents selected from hydroxyl, amino, ester, carboxylic acid, and halogen atoms;
- or
- R8 and R9 can combine to form 3- to 6-membered rings containing one or more heteroatoms which are selected from the group consisting of:
27 more elements
Dependencies are inferred from the claim text.