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Antifungal macrocyclic polyene novel compound

An antifungal and compound technology, applied in the field of medicine, can solve the problems of difficult and uncertain synthesis, achieve the effects of easy preparation, convenient storage and transportation, and reduce manufacturing costs and costs

Pending Publication Date: 2021-01-05
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although medicinal chemistry and pharmacy are practical sciences that continue to develop, they constantly guide pharmaceutical progress through innovation, continuously improve drug safety to guide the development of drugs and preparations and guide clinical medication, and even though pharmaceuticals have reached the point of changing the physical state of raw materials However, due to the difficulty and uncertainty of the synthesis, so far, there are no published literature reports at home and abroad to conduct in-depth and innovative research on the new stable chemical state of amphotericin B And precise synthesis, new compounds with chemical molecular formula and molecular weight or structural formula that are easier to prepare or have better stability, such as ω-type crystal compounds and ν-type compounds, that is, new compounds with different molecular formulas or structural forms and their preparation methods and uses

Method used

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  • Antifungal macrocyclic polyene novel compound
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  • Antifungal macrocyclic polyene novel compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Preparation of Embodiment 1 Amphotericin B 2 Hydrate (Amphotericin B ω type compound)

[0117] Add 10g of amphotericin B to a 250ml flask, add 8ml of dimethyl sulfoxide, add 120ml of methanol, 10ml of isopropanol, and 50ml of water. Sodium hydroxide solution, adjust the pH value to about 7.4, stir until completely dissolved, add a small amount of activated carbon and stir for about 15 minutes to filter, add 60% lactic acid solution to the filtrate, adjust the pH value to about 5.5, add 8ml of dichloromethane, stir, Place between 0~-10°C, wait until the precipitate is fully separated, filter with suction, wash with a small amount of chloroform, water and ethanol three times, filter with suction, and dilute the obtained solid in an oven at about 50°C for 3 hours to obtain about 6.5g of a yellow solid; Identification: ①HPLC: the retention time of the main peak of HPLC in the determination of the content is consistent with the retention time of the main peak of the HPLC of ...

Embodiment 2

[0118] Preparation of embodiment 2 amphotericin B 2 hydrate (amphotericin B ω type compound)

[0119] Add 10g of amphotericin B to a 250ml flask, add 10ml of dimethylformamide, add 120ml of 95% ethanol, 50ml of acetone, 40ml of water, protect with nitrogen, stir, keep the temperature between 35-50°C, add 5% Potassium hydroxide solution, adjust the pH value to about 7.1, stir to dissolve, add a small amount of activated carbon and stir for about 20 minutes to filter, add 40% lactic acid solution to the filtrate, adjust the pH value to about 5.5, add 5ml of chloroform, stir, Place between 0~-10°C, wait for the precipitate to be fully resolved, filter with suction, wash with a small amount of water and ethanol four times, filter with suction, dilute the obtained solid in an oven at 40°C and blow dry for about 3 hours to obtain 7.3g of yellow crystalline solid; identification : 1. HPLC: the main peak retention time of its HPLC is consistent with the main peak retention time of the...

Embodiment 3

[0120] Example 3 Preparation of Amphotericin B 1.75 Hydrate (Amphotericin Bγ Type Compound)

[0121] Add 10g of amphotericin B to a 250ml flask, add 5ml of dimethyl sulfoxide, add 80ml of 95% ethanol, 30ml of isopropanol, and 40ml of water. 6% sodium hydroxide solution, adjust the pH value to about 7.5, stir until dissolved, add a small amount of activated carbon and stir for about 20 minutes to filter, add 40% lactic acid solution to the filtrate, adjust the pH value to about 5.5, add 5ml of dichloroethane , stirred, placed between 0~-10°C, waited for the precipitate to be fully analyzed, filtered with suction, washed with a small amount of water and ethanol four times, filtered with suction, and the obtained solid was diluted in an oven at 40°C for about 3 hours in vacuum to obtain a yellow crystalline solid of about 7.0 g; Identification: 1. HPLC: the retention time of the main peak of its HPLC in the determination of normalized content is consistent with the retention time...

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Abstract

The invention relates to a gamma-type, omega-type and nu-type novel compound of macrocyclic polyene antifungal amphotericin B. The gamma-type, omega-type and nu-type novel compound of the macrocyclicpolyene antifungal amphotericin B has less hygroscopicity and better storage stability, is more beneficial to quality control of drugs and preparations and the like, and is applicable to preparation of drugs for treating or preventing infections such as cryptococcosis, north American blastomycosis, disseminated candidiasis, coccidioidomycosis, histoplasmosis, mucormycosis, sporotrichosis, aspergillosis, chromomycosis, fungal infections cutaneous after burning, respiratory tract candida, aspergillus or cryptococcus infection, fungal corneal ulcer, black sickness, enterovirus infection, anti-depression and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide a compound with a new molecular formula and a new molecular structure and a pharmaceutical composition thereof with better stability of the macrocyclic polyene antifungal drug amphotericin B. Background technique [0002] Amphotericin B (Amphotericin B, CAS: 1397-89-3, molecular formula C 47 h 73 NO 17 , M=924.08) is a macrocyclic polyene broad-spectrum antifungal drug produced by Streptomyces nodosum, it is the drug of choice for the treatment of most deep fungal infections, and it is suitable for deep fungal infections caused by sensitive fungi and the condition Patients with progressive development, such as sepsis, endocarditis, meningitis (cryptococcus and other fungi), abdominal infection (including those related to dialysis), lung infection, urinary tract infection and endophthalmitis, etc., can also be treated Visceral Leishmaniasis (VL), etc. More specificall...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/06A61K31/7048A61P31/10A61P31/12A61P33/02A61P25/24
CPCC07H17/08C07H1/06A61P31/10A61P31/12A61P33/02A61P25/24C07B2200/13
Inventor 刘力
Owner 刘力