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Compounds that inhibit cholinesterase

A technology of acetylcholinesterase and compounds, applied in the direction of drug combination, organic chemistry, ester active ingredients, etc., can solve the problem that drugs cannot be targeted to specific cells or tissues, drug delivery cannot be delivered, and the interruption of single cell signal molecules cannot be effective Treatment of diseases or illnesses

Inactive Publication Date: 2010-01-20
COLUCID PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, currently available drugs usually cannot target the drug to specific cells or tissues, so that the drug cannot be delivered with a long-term sustained effect
In many cases, modification of the disruption of a single cell signaling molecule is not effective in treating the symptoms of the disease or disorder

Method used

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  • Compounds that inhibit cholinesterase
  • Compounds that inhibit cholinesterase
  • Compounds that inhibit cholinesterase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0546] Embodiment 1: the synthesis of compound

[0547] Compounds described in the present invention are subjected to R by methods known to those skilled in the art a - Prepared by the coupling reaction of phenol and Q-H. For example:

[0548]

[0549] where R a represents a suitable phenyl substituent of a Stigmine such as Rivastigmine or Physostigmine, and Q represents a pharmacologically active agent containing an amine. For example,

[0550]

[0551] Exemplary compounds are shown in Table A.

[0552] Table A

[0553] starting material

[0554] fluoxetine hydrochloride

[0555] Sertraline Maleate

[0556] Betahistine dihydrochloride

[0557] Gabapentin

[0558] fluvoxamine maleate

Embodiment 2

[0559] Embodiment 2: the preparation of hydrochloride

Embodiment 2A

[0560] Example 2A: Compounds described in the present invention were dissolved in chloroform (3 ml of chloroform per mmol of compound was used). Thereto was added dropwise a 1M diethyl ether solution of hydrochloric acid (1.5-2 molar equivalents) at 0°C. After the step of adding hydrochloric acid was completed, the mixture was warmed to room temperature. The solvent was removed by evaporation and the residue was dried under vacuum to obtain the hydrochloride salt of the compound.

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Abstract

Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Description

[0001] related application [0002] This application claims the benefit and priority of U.S. Patent Application No. 60 / 899,111 and No. 60 / 959,901. The filing date of the former is February 2, 2007, and the filing date of the latter is July 16, 2007. The disclosure of the application is hereby incorporated by reference. Background technique [0003] Many human disorders and diseases are accompanied by, or are the result of, disruption of cell signaling molecules. For example, the cell signaling molecule may be inappropriately synthesized, released, or reabsorbed, or receptor or non-receptor substrates may interrupt the mediation of cell signaling of the molecule, resulting in a disease or other condition. In many cases, clinical treatment regimens and currently available drugs are often associated with side effects in patients and must be carefully monitored. Current strategies for the development of drugs for the treatment of conditions and diseases that are accompanied by o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C271/44C07C271/48C07C271/52C07C271/56C07D211/86C07D223/24C07D403/14C07D413/04A61K31/27A61K31/496A61K31/4402A61K31/4422A61P25/28
Inventor 纳迪亚·M·J·鲁普尼克J·F·怀特潮崎和美J·D·利安德杜寿成D·J·考格林
Owner COLUCID PHARM INC
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