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US 10,329,278 B2Granted
Pharmaceutical compounds
AssigneeHeptares Therapeutics Limited
InventorsGiles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Benjamin Gerald Tehan, Barry John Teobald
Life of this patent
Estimating the term…
Abstract
This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.
Claims17
A compound of the formula (1):
- or a salt thereof, wherein:
- X1 and X2 are saturated hydrocarbon groups which together contain a total of five to nine carbon atoms and zero or one oxygen atoms and which link together such that the moiety:
- forms a monocyclic or bicyclic ring system optionally substituted with one or more fluorine atoms;
- R1 is selected from OR5;
- NR5R6;
- COR5;
- COOR5;
- CONR5R6;
- CONR5OR6;
- C(═NR5)R6;
- C(═NOR5)R6;
- OCOR5;
- NR7COR5;
- NR7CONR5R6;
- NR7COOR5;
- OCONR5R6;
- CH2OR5;
- CH2NR5R6;
- CH2COR5;
- CH2COOR5;
- CH2CONR5R6;
- CH2CONR5OR6;
- CH2C(═NR5)R6;
- CH2C(═NOR5)R6;
- CH2OCOR5;
- CH2NR7COR5;
- CH2NR7CONR5R6;
- CH2NR7COOR5;
- CH2OCONR5R6;
- 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 an optionally substituted 4, 5- or 6-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof;
- R4 is H 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;
- and
- R5, R6 and R7 are the same or different and each is independently selected from hydrogen, a non-aromatic C1-6 hydrocarbon group optionally substituted with one or more fluorine atoms or optionally substituted with a 4, 5- or 6-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof, or R5 and R6 can be joined together to form an optionally substituted monocyclic or bicyclic ring containing 0, 1, 2 or 3 heteroatoms selected from O, N and S and oxidized forms thereof.
31 more elements
Dependencies are inferred from the claim text.