Muscarinic agonists
AssigneeHeptares Therapeutics Limited
InventorsGiles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
Life of this patent
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Abstract
This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.
Claims20
1-21. (canceled)
A method of treating a cognitive disorder or psychotic disorder or for treating or lessening the severity of acute, chronic, neuropathic, or inflammatory pain in a subject, comprising administering to the subject in need thereof an effective amount of a compound of formula (1a):
- or a salt thereof, wherein
- p is 1 or 2;
- g is 0, 1 or 2;
- r is 1 or 2;
- s is 0 or 1, where the total of r and s is 1 or 2;
- Q is CR1R2NR5R6, NR5R6, OR7 or SR7;
- R1 is selected from hydrogen and a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- R2 is selected from hydrogen and a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- R3 is selected from hydrogen;
- fluorine;
- cyano;
- hydroxy;
- amino;
- and a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one, two or three, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- R4 is a hydrogen or a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidised forms thereof;
- R5 is selected from hydroxy;
- OR7;
- COR7;
- COOR7;
- CH2COR7;
- CH2COOR7;
- a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- and a group W or CH2W where W is an optionally substituted 5- or 6-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof:
- R6 is selected from hydroxy;
- OR7;
- COR7;
- COOR7;
- CH2COR7;
- CH2COOR7;
- a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- and a group W or CH2W where W is an optionally substituted 5- or 6-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof;
- R7 is selected from hydrogen;
- a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidized forms thereof;
- and a group W or CH2W or C1-4 hydrocarbon group-W where W is an optionally substituted 5- or 6-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof;
- and
- the dotted line indicates an optional second carbon-carbon bond, provided that when a second carbon-carbon bond is present, then R3 is absent.
23-24. (canceled)
Dependencies are inferred from the claim text.