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Compound with activity on muscarinic receptors

A compound, alkyl technology, applied in the treatment or alleviation of diseases in which improvement of muscarinic receptor activity has a beneficial effect, the field of activation of muscarinic receptors, can solve the lack of subtype selectivity, low efficacy, limitation problems of cognition

Inactive Publication Date: 2001-07-11
ACADIA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Therefore, m2 and / or m3 activity is the main disadvantage of the muscarinic agonists mentioned so far for the treatment of Alzheimer's disease, which severely limits the dose of the drug, so that the patient may always be given a suboptimal dose
Thus, lack of subtype selectivity and generally low potency of the cholinergic compounds tested increased peripheral side effects and limited cognitive effects due to weak and / or opposite effects in the brain

Method used

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  • Compound with activity on muscarinic receptors
  • Compound with activity on muscarinic receptors

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0067] When the preparation of the compounds of the present invention results in a mixture of stereoisomers, these isomers can be separated by conventional techniques such as preparative chiral chromatography. The compounds of the invention may be prepared in racemic form or may be prepared as individual enantiomers by stereoselective synthesis or by resolution. For example, formation may be by standard methods, for example by salt formation with optically active acids, such as (-)-di-p-toluoyl-d-tartaric acid and / or (+)-di-p-toluoyl-1-tartaric acid Diastereoisomeric pairs, followed by fractional crystallization followed by free base formation, resolve compounds into their component enantiomers. Compounds can also be resolved by formation of diastereomeric esters or amides followed by chromatographic separation followed by removal of the chiral auxiliary.

[0068] During the preparation of any of the compounds of the invention it may be necessary and / or required to protect se...

Embodiment

[0121] Embodiment XVII-R-SAT test

[0122] compound

Receptors and concentrations

m1

1.5M

m3

1.5M

m5

1.5M

A

(Example I)

107

+ / -

9

7

+ / -

8

3

+ / -

8

B

(Example IX)

76

+ / -

11

7

+ / -

9

-6

+ / -

10

C

(Example XV)

91

+ / -

9

4

+ / -

9

0

+ / -

12

D.

(Example X)

72

+ / -

9

13

+ / -

7

2

+ / -

15

E.

(Example Ⅺ)

42

+ / -

13

9

+ / -

3

-3

+ / -

2

f

(Example Ⅻ)

65

+ / -

9

9

+ / -

7

5

+ / -

11

G *

66

+ / -

19

16

+ / -

12

7

+ / -

11

[0123] * 4-n-Butyl-1-[4-phenyl-...

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PUM

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Abstract

Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a therapeutically effective amount of a selective muscarinic m1 agonist compound is administered to a patient in need of such treatment.

Description

field of invention [0001] The present invention relates to novel compounds that are selective for muscarinic acetylcholine receptor subtypes, as well as methods of activating muscarinic receptors and methods of treating or alleviating diseases in which improved muscarinic receptor activity has a beneficial effect . Background of the invention [0002] Muscarinic acetylcholine receptors play an important role in higher cognitive functions in the central nervous system as well as in the peripheral parasympathetic nervous system. Cloning has confirmed the existence of five different muscarinic receptor subtypes (called m1-m5) (see T.I.Bonner et al., Science 237, 1987, pp. 527-532; T.I.Bonner et al., Neuron 1, 1988, 403- 410 pages). m1 has been found to be the predominant subtype in the cerebral cortex and is thought to be involved in the control of cognitive functions, m2 predominates in the heart and is thought to be involved in the control of heart rat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/10A61K31/40A61K31/4427A61K31/445A61K31/454A61K31/4545A61K31/495A61P25/00A61P25/28A61P27/06A61P43/00C07D207/02C07D211/14C07D211/22C07D211/48C07D241/04C07D295/108C07D295/18C07D401/06C07D417/06
CPCC07D211/22C07D295/108A61P25/00A61P25/28A61P27/06A61P43/00C07D207/08C07D213/30C07D213/61C07D213/62C07D403/06
Inventor M·R·布兰恩T·梅斯尔E·A·库里尔K·L·杜根托M·弗里伯格N·斯克杰尔贝克T·斯帕丁格
Owner ACADIA PHARMA INC
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