IP Library Granted Patent US 11,793,817
Granted Patent B2
US 11,793,817 · App. 17/226,523 · Granted Oct 24, 2023

Muscarinic M1 receptor agonists

Inventors: Miles Stuart Congreve (Cambridge, GB); Giles Albert Brown (Cambridge, GB); Julie Elaine Cansfield (Cambridge, GB); Benjamin Gerald Tehan (Cambridge, GB)
Assignee: Heptares Therapeutics Limited
A61K31/55A61K31/4545C07D211/06C07D401/04C07D401/14
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Quick Facts
Patent No.
US 11,793,817
App. No.
17/226,523
Granted
Oct 24, 2023
Kind
B2
Abstract

This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R 1 -R 6 are as defined herein.

Claims (13)

1. A compound:

or a salt thereof.

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

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

4. The acid addition salt according to claim 3 , wherein the acid is selected from the group consisting of acetic, 2,2-dichloroacetic, adipic, alginic, ascorbic (e.g. L-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 (e.g. D-glucuronic), glutamic (e.g. L-glutamic), α-oxoglutaric, glycolic, hippuric, hydrohalic acids (e.g. hydrobromic, hydrochloric, hydriodic), isethionic, lactic (e.g. (+)-L-lactic, (+)-DL-lactic), lactobionic, acetyl leucine, 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, (−)-D-tartaric, (−)-dibenzoyltartaric, thiocyanic, p-toluenesulfonic, undecylenic and valeric acids, as well as acylated amino acids and cation exchange resins.

5. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable excipient.

6. A pharmaceutical composition comprising a pharmaceutically acceptable salt according to claim 2 and a pharmaceutically acceptable excipient.

7. A pharmaceutical composition comprising an acid addition salt according to claim 3 and a pharmaceutically acceptable excipient.

8. A pharmaceutical composition comprising an acid addition salt according to claim 4 and a pharmaceutically acceptable excipient.

9. 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 to a patient in need thereof.

10. The method according to claim 9 , wherein the disorder is Alzheimer's disease.

11. The method according to claim 9 , wherein the disorder is dementia with Lewy bodies.

12. The method according to claim 9 , 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 068524/0400 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 2, 2021
From: CONGREVE, MILES STUART; BROWN, GILES ALBERT; CANSFIELD, JULIE ELAINE; TEHAN, BENJAMIN GERALD
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 057371/0295 →
Continuity (7)
Continuation 16560529 · Sep 4, 2019
Continuation 15886249 · Feb 1, 2018
Continuation 15436224 · Feb 17, 2017
Division 14941328 · Nov 13, 2015
Continuation 14358984
Provisional Application 61632813 · Nov 18, 2011
Related Publication 20210353637A1 · Nov 18, 2021