Muscarinic receptor antagonists
AssigneeTheravance, Inc.
InventorsJames Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Abstract
Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
Claims11
A compound of the formula:
- La—X—Lb
- wherein:
- La is selected from the group consisting of:
- Lb is a group of formula (i):
- wherein:
- R46 is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, or heterocycle;
- R47 is alkyl, substituted alkyl, aryl, acyl, heterocycle, or —COOR49 where R49 is alkyl;
- or
- R46 and R47 together with the nitrogen atom to which they are attached form heterocycle;
- R48 is a covalent bond that attaches Lb to X;
- and
- X is a selected from the group consisting of —(CH2)8—, —(CH2)9— and —(CH2)10—;
- or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.