2-- 2-Deoxy-scyllo-inosamine containing aminocyclitol compounds method for the preparation thereof and pharmaceutical compositions comprising the same

The present invention relates to an aminocyclitol compound containing 2-deoxy-schyloinosamine, a preparing method thereof, an antibiotic composition containing the compound as an active ingredient, and a pharmaceutical composition for preventing or treating nonsense mutation-related genetic diseases...

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Bibliographische Detailangaben
Hauptverfasser:	KIM CHANG RAE, RYU HWI SO, LEEJOON, WI JAE BOK, LEE JI YOON, KIM HYE JI, PARK JE WON
Format:	Patent
Sprache:	eng ; kor
Schlagworte:	AGRICULTURE ANIMAL HUSBANDRY BEER BIOCHEMISTRY BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES CHEMISTRY COMPOSITIONS THEREOF CULTURE MEDIA DERIVATIVES THEREOF ENZYMOLOGY FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE FISHING FORESTRY HUMAN NECESSITIES HUNTING HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY MICROBIOLOGY MICROORGANISMS OR ENZYMES MUTATION OR GENETIC ENGINEERING NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PEST REPELLANTS OR ATTRACTANTS PLANT GROWTH REGULATORS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SPIRITS SUGARS TRAPPING VINEGAR WINE
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Beschreibung
Zusammenfassung:	The present invention relates to an aminocyclitol compound containing 2-deoxy-schyloinosamine, a preparing method thereof, an antibiotic composition containing the compound as an active ingredient, and a pharmaceutical composition for preventing or treating nonsense mutation-related genetic diseases containing the compound as an active ingredient. The aminocyclitol compound containing 2-deoxy-schyloinosamine of the present invention is a novel compound prepared by applying a semi-synthetic method to the structure of istamycin and has excellent antibacterial activity against gram-negative pathogens containing Escherichia coli and Pseudomonas aeruginosa, and gram-negative resistant bacteria that are resistant to aminoglycoside antibiotics. In addition, the compound of the present invention has a relatively improved read-through induction activity compared to conventional aminoglycosides in an in vitro experiment targeting a cell line derived from a cystic fibrosis patient. Therefore, the compound of the present invention can be usefully used as antibiotic and therapeutic agents for nonsense mutation-related genetic diseases. 본 발명은 2-데옥시-스킬로이노사민을 포함하는 아미노사이클리톨 화합물, 이의 제조방법, 상기 화합물을 유효성분으로 포함하는 항생제 조성물, 및 상기 화합물을 유효성분으로 포함하는 넌센스 돌연변이 관련 유전질환의 예방 또는 치료용 약학 조성물에 관한 것이다. 본 발명의 2-데옥시-스킬로이노사민을 포함하는 아미노사이클리톨 화합물은 이스타마이신 구조에 반합성법을 적용하여 제조된 신규 화합물로서, 대장균과 녹농균을 포함하는 그람음성 병원균과 아미노글리코사이드계 항생제에 내성을 나타내는 그람음성 내성균에 대한 우수한 항세균 활성을 갖는다. 또한, 본 발명의 상기 화합물은 낭성 섬유증 환자 적출 세포주를 대상으로 한 인비트로(in vitro) 실험에서 기존 아미노글리코사이드 대비 상대적으로 향상된 리드 스루(read through) 유도 활성을 갖는다. 따라서 본 발명의 상기 화합물은 항생제 및 넌센스 돌연변이 관련 유전질환 치료제의 용도로 유용하게 사용될 수 있다.