Compositions and methods for treatment of neuromuscular disorders and neurodegenerative disorders

A composition and compound technology, applied in neuromuscular system diseases, muscular system diseases, nervous system diseases, etc., can solve problems such as pessimism

Inactive Publication Date: 2015-05-06
CELLIXBIO PTE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once dopaminergic compounds are excluded from the development pipeline, the situation is far from optimistic
This dopaminergic treatment approach involves reformulation of existing drugs, yet is more likely to provide incremental rather than profound improvements over existing treatments

Method used

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  • Compositions and methods for treatment of neuromuscular disorders and neurodegenerative disorders
  • Compositions and methods for treatment of neuromuscular disorders and neurodegenerative disorders
  • Compositions and methods for treatment of neuromuscular disorders and neurodegenerative disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0161]

[0162] Synthesis of Compound-2:

[0163]

[0164] To compound 1 (50 mmol) in 1:1 THF / H at 0 °C 2 To a solution in O mixture (300 mL), NaHCO was added continuously 3 (150mmol) and Boc 2 O (110 mmol). After 30 minutes, the solution was stirred at room temperature overnight. with Et 2 O extracted the resulting cloudy solution (2 x 200 mL). Half-saturated citric acid was added carefully at 0°C, the aqueous layer was acidified to pH=4-5, then washed with CH 2 Cl 2 Extraction (3 x 200 mL). The combined organic phases were dried (Na 2 SO 4 ) and evaporated under reduced pressure to give high-purity Boc-amino acid in the form of a solid or hard colorless oil, which was allowed to crystallize on standing. These Boc-amino acids were used in the next step without purification. M.F: C 20 H 30 N 2 O 8 ; Mol. Wt: 426.46.

[0165] Synthesis of Compound-3:

[0166]

[0167] Compound 2 (50 mmol), 2,2-dimethoxypropane (200 mmol) and anhydrous toluene (20 vol) ...

Embodiment 2

[0175]

[0176] Synthesis of Compound-2:

[0177]

[0178] Compound 1 (50 mmol), 2,2-dimethoxypropane (200 mmol) and anhydrous toluene (20 vol) were added to a 500 mL two-necked flask. One neck of the flask is equipped with a Soxhlet extractor, the cannula of which is filled with granular anhydrous CaCl 2 (75g) to capture MeOH and H 2 O. The other neck of the flask was sealed with a sampling septum. After the system was flushed with argon for 5 minutes and heated to reflux for 5 minutes, p-toluenesulfonic acid monohydrate (430 mg, 4.5 mol%) was added and left to reflux for 12 hours. The reaction mixture was concentrated under reduced pressure. The reaction residue was diluted with ethyl acetate (10 Vol) and washed with saturated sodium bicarbonate solution followed by brine. The organic layer was dried over sodium sulfate, filtered and concentrated in vacuo to yield compound 2. M.F: C 16 H 22 N 2 O 4 ; Mol. Wt: 306.36.

[0179] Synthesis of Compound-4:

[0180]...

Embodiment 3

[0188]

[0189] Synthesis of Compound-2:

[0190]

[0191] To a solution of compound 1 (50 mmol) in dichloromethane (10 mL) at 0°C were successively added diisopropylethylamine (150 mmol) and methoxyethoxymethyl chloride (MEM-Cl) (110 mmol). The reaction mixture was stirred for 3.0 hours, monitored by TLC for completion, and washed with water (10 Vol) and brine. The organic phase was dried (Na 2 SO 4 ) and evaporated under reduced pressure to form the benzaldehyde derivative 2. M.F: C 19 H 30 O 10 ; Mol. Wt: 418.44.

[0192] Synthesis of Compound-3:

[0193]

[0194] A Soxhlet extractor was filled with 20 g molecular sieves and the benzaldehyde derivative (5 mmol) and hydrazine hydrate (75 mmol) were refluxed in ethanol (10 vol) overnight (16-24 hours). The hot alcoholic solution was filtered and the solvent was evaporated to yield (73%) crude product-3. Compound 3 was formed after one recrystallization from ethanol. M.F: C 19 H 32 N 2 O 9 ; Mol. Wt: 43...

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Abstract

The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for treating or preventing neuromuscular disorders and neurodegenerative diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosaf intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of neuromuscular disorders and neurodegenerative diseases such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension.

Description

[0001] priority [0002] This application claims the benefit of Indian Provisional Patent Application No. 1779 / CHE / 2012 filed on May 7, 2012 and International Application No. PCT / IB2012 / 053555 filed on July 12, 2012, relied upon for all purposes The entire disclosures of these applications are incorporated herein by reference. technical field [0003] The present disclosure generally relates to compounds and compositions for the treatment of neuromuscular disorders, metabolic conditions, and neurodegenerative diseases. More specifically, the present invention relates to the treatment of a subject with a pharmaceutically acceptable dose of a compound, crystal, solvate, enantiomer or stereoisomer, ester, salt, hydrate, prodrug or mixtures thereof . Background technique [0004] Intercellular communication in the central nervous system requires precise control of the duration and intensity of neurotransmitter action on specific molecular targets. Plasma membrane neurotransmi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/48C07C233/49C07C233/87C07D339/04A61K31/16A61K31/385A61K31/185A61P25/16A61P25/28
CPCA61K31/165A61K31/198A61K31/202A61K31/385A61K31/405C07C243/18C07C271/18C07C281/02C07D209/16C07D209/20C07D339/04C07D495/04A61K2300/00A61K47/542A61K47/545A61P17/00A61P21/00A61P25/00A61P25/16A61P25/28A61P9/12
Inventor M·坎杜拉
Owner CELLIXBIO PTE LTD
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