Targeted drug rescue with novel compositions, combinations, and methods thereof

A composition and compound technology, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations containing active ingredients, etc., can solve the problem of disease-modifying therapy that has not yet been obtained

Active Publication Date: 2020-02-21
エクシーバゲーエムベーハー +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

An estimated 55 million people worldwide suffer from neurodegenerative diseases for which there are currently no approved disease-modifying therapies

Method used

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  • Targeted drug rescue with novel compositions, combinations, and methods thereof
  • Targeted drug rescue with novel compositions, combinations, and methods thereof
  • Targeted drug rescue with novel compositions, combinations, and methods thereof

Examples

Experimental program
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preparation example Construction

[0459] The preparation of enantiomerically pure molecules of biological interest can be efficiently achieved by asymmetric synthesis. This method involves the creation of one or more chiral centers from prochiral starting materials under the influence of a chiral host. The preparation of enantiomerically pure compounds involves the use of chiral auxiliaries, chiral reagents or catalysts, or combinations thereof.

[0460] In another example, compounds of the present disclosure can be prepared from (2R)-3-(dimethylamino)2-propanediol and (2S)-3-(dimethylamino)-1,2-propanediol (Scheme VIII )preparation.

[0461] A variety of versatile and convenient chiral carboxylic acid ligands can be found in the literature, such as mandelic acid, 2-methylmandelic acid, 2-chloromandelic acid, 3-chloromandelic acid, 4-methoxymandelic acid , O-acetyl mandelic acid, α-methoxyphenylacetic acid, malic acid, tartaric acid, etc. Chiral ligands can be prepared from readily available building blocks...

example 1

[0536] Example 1: Dextromethorphan has been synthesized from benzylisoquinoline (with a planar structure) by Grignard cyclization (Grewe'scyclization), giving the corresponding morphinan, wherein the 1,2,3,4,5 , 6,7,8-octahydro-1-(4-methoxybenzyl) isoquinoline is converted into N-formyl derivatives, crystallized into N-formyl morphinan, and the formyl group is reduced to N- Methyl, given 3-methoxy-17-methylmorphinan. Dextromethorphan is readily soluble in 96% ethanol and essentially insoluble in water. Dextromethorphan can be chlorobromide monohydrate or bound to a polystyrenesulfonic acid-based ion exchange resin. The specific optical rotation of dextromethorphan in water is +27.6° (20°C, sodium D-line).

example 2

[0537] Example 2: Equimolar amounts of sagrelate (429.506 g / mol) and dextromethorphan (271.40 g / mol) were mixed in a suitable solvent, stirred and allowed to crystallize. The compound of formula I and the dextromethorphan cation will form hydrogen bonds to form a complex and crystallize.

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Abstract

Compounds of Formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, metabolites thereof, derivatives thereof, prodrugs thereof, acid addition salts thereof, pharmaceutically acceptable salts thereof, or N-oxides thereof; or a combination thereof, processes and intermediates for preparation thereof, compositions thereof, and uses thereof, are provided. Pharmaceutical compositions comprising a compound of Formula I, or enantiomers thereof, metabolites thereof, derivatives thereof, prodrugs thereof, acid addition salts thereof, pharmaceutically acceptable salts thereof, or N-oxides thereof; or a combination thereof, wherein the compound is double and/or triple agent or ligand for CYP2D6, 5-HT2A, and/or 5HT2C receptors, and/or acetylcholinesterase are provided.

Description

technical field [0001] The present disclosure relates to Targeted Drug Rescue (TDR) with novel compositions, combinations, therapeutic formulations, symptom and disease modifying treatments, therapies, kits thereof TM and its methods. Background technique [0002] Excess weight alters the body, increasing levels of certain hormones and inflammation that contribute to metabolic disorders, cancer, and brain disorders, including developmental, psychiatric, and neurodegenerative diseases, which represent an enormous disease burden in terms of human suffering and economic cost, And lead to rapid growth in treatment and health care expenditures. Diseases affecting the brain and central nervous system represent one of the greatest global healthcare challenges and greatest treatment needs due to devastating personal and economic consequences for patients, caregivers and society. An estimated 55 million people worldwide suffer from neurodegenerative diseases for which there are cur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/135A61K31/138A61K31/215A61K31/485A61P25/00
CPCA61K31/13A61K31/225A61K31/439A61K31/485A61P25/00A61K31/195A61K45/06A61K2300/00A61K31/138A61K31/135A61K31/215
Inventor 斯瑞尼瓦萨饶·韦帕切杜汉斯·J·莫比乌斯安东·贝斯帕洛夫
Owner エクシーバゲーエムベーハー
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