IP Library › Granted Patent US 12,202,843
Granted Patent B2
US 12,202,843 · App. 17/345,557 · Granted Jan 21, 2025

Muscarinic receptor agonists

Inventors: Miles Stuart Congreve (Cambridge, GB); Giles Albert Brown (Cambridge, GB); Benjamin Gerald Tehan (Cambridge, GB); Mark Pickworth (Cambridge, GB); Julie Elaine Cansfield (Cambridge, GB)
Assignee: Nxera Pharma UK Limited
C07D519/00A61K31/438A61K31/439A61P25/00A61P25/18A61P25/28C07D471/10C07D498/10
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Quick Facts
Patent No.
US 12,202,843
App. No.
17/345,557
Granted
Jan 21, 2025
Kind
B2
Abstract

This invention relates to compounds that are agonists of the muscarinic M 1 receptor and which are useful in the treatment of muscarinic M 1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X 1 , X 2 , R 1 , R 2 , R 3 and R 4 are as defined herein.

Claims (21)

1. A compound, which is:

or a salt thereof.

2. The compound according to claim 1 , which is:

or a salt thereof.

3. The compound according to claim 1 , which is:

or a salt thereof.

4. A pharmaceutically acceptable salt of the compound according to claim 1 .

5. An acid addition salt of the compound according to claim 1 .

6. The acid addition salt according to claim 5 , wherein the acid is selected from: acetic, 2,2-dichloroacetic, adipic, alginic, ascorbic L-aspartic, benzenesulfonic, benzoic, 4-acetamidobenzoic, butanoic, (+) camphoric, camphor-sulfonic, (+)-(1S)-camphor-10-sulfonic, capric, caproic, caprylic, cinnamic, citric, cyclamic, dodecylsulfuric, ethane-1,2-disulfonic, ethanesulfonic, 2-hydroxyethanesulfonic, formic, fumaric, galactaric, gentisic, glucoheptonic, D-gluconic, glucuronic, glutamic, α-oxoglutaric, glycolic, hippuric, hydrohalic acids, isethionic, lactic, lactobionic, maleic, malic, (−)-L-malic, malonic, (±)-DL-mandelic, methanesulfonic, naphthalene-2-sulfonic, naphthalene-1,5-disulfonic, 1-hydroxy-2-naphthoic, nicotinic, nitric, oleic, orotic, oxalic, palmitic, pamoic, phosphoric, propionic, pyruvic, L-pyroglutamic, salicylic, 4-amino-salicylic, sebacic, stearic, succinic, sulfuric, tannic, (+)-L-tartaric, thiocyanic, p-toluenesulfonic, undecylenic, valeric acids, acylated amino acids, and cation exchange resins.

7. The acid addition salt according to claim 6 , wherein the acid is hydrochloric, hydrobromic, maleic, phosphoric, succinic, or (+)-L-tartaric acid.

8. The acid addition salt according to claim 7 , wherein the acid is hydrochloric acid.

9. A pharmaceutical composition comprising a compound according to claim 1 , or a salt thereof, and a pharmaceutically acceptable excipient.

10. A pharmaceutical composition comprising a pharmaceutically acceptable salt according to claim 4 and a pharmaceutically acceptable excipient.

11. A pharmaceutical composition comprising an acid addition salt according to claim 5 and a pharmaceutically acceptable excipient.

12. A pharmaceutical composition comprising an acid addition salt according to claim 6 and a pharmaceutically acceptable excipient.

13. A pharmaceutical composition comprising an acid addition salt according to claim 7 and a pharmaceutically acceptable excipient.

14. A pharmaceutical composition comprising an acid addition salt according to claim 8 and a pharmaceutically acceptable excipient.

15. A method of treating Alzheimer's disease, dementia with Lewy bodies or schizophrenia, comprising administering an effective amount of the compound according to claim 1 , or a salt thereof, to a patient in need thereof.

16. The method according to claim 15 , wherein the disorder is Alzheimer's disease.

17. The method according to claim 15 , wherein the disorder is dementia with Lewy bodies.

18. The method according to claim 15 , wherein the disorder is schizophrenia.

Assignments (2)
CHANGE OF NAME Recorded Sep 9, 2024
From: HEPTARES THERAPEUTICS LIMITED
To: NXERA PHARMA UK LIMITED
Reel/Frame 068529/0381 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2021
From: CONGREVE, MILES STUART; BROWN, GILES ALBERT; TEHAN, BENJAMIN GERALD; PICKWORTH, MARK; CANSFIELD, JULIE ELAINE
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 057011/0149 →
Priority Claims (1)
GB 1404922 · Mar 19, 2014 · national
Continuity (4)
Continuation 16584185 · Sep 26, 2019
Continuation 15987506 · May 23, 2018
Continuation 15126935
Related Publication 20220048928A1 · Feb 17, 2022
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