KR940019712A - Purified streptogramine and its preparation - Google Patents

Purified streptogramine and its preparation Download PDF

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Publication number
KR940019712A
KR940019712A KR1019940002667A KR19940002667A KR940019712A KR 940019712 A KR940019712 A KR 940019712A KR 1019940002667 A KR1019940002667 A KR 1019940002667A KR 19940002667 A KR19940002667 A KR 19940002667A KR 940019712 A KR940019712 A KR 940019712A
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South Korea
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group
streptogramin
component
radical
subcomponent
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KR1019940002667A
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KR100333185B1 (en
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앤거 빠스칼
보나보 버트란
깔레 알랭
르페브르 빠뜨릭
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프랑소와즈 로브조아
로오느-푸우랜크 로레르 소시에테 아노님
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06182Dipeptides with the first amino acid being heterocyclic and Pristinamycin II; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids

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  • Chemical & Material Sciences (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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Abstract

하기 구조식의 스트렙토그라민의 하나 이상의 B군 성분 :At least one group B component of streptogramin of the formula:

(상기식에서, A1은 하기 구조식 :Wherein A 1 is the following structural formula:

의 라디칼이고, 이때 R'는 OH이며, Y는 H, 메틸아미노 라디칼 또는 디메틸아미노 라디칼이고, R은 에틸 라디칼이거나, R'가 수소 원자인 경우 R은 또한 -CH3일 수 있고 R1및 R2는 H이거나, 대안으로 A1은 하기 구조식 :Wherein R 'is OH, Y is H, methylamino radical or dimethylamino radical, R is an ethyl radical, or if R' is a hydrogen atom, R can also be -CH 3 and R 1 and R 2 is H, or alternatively A 1 is

의 라디칼이고, R은 이소부틸 라디칼이고, R1은 OH이며 R2는 -CH3임) 및 하기 구조식의 스트렙코그라민의 하나 이상의 A군 부성분 ;And R is an isobutyl radical, R 1 is OH and R 2 is -CH 3 ) and at least one group A subcomponent of strepcogramin of the following structural formula;

(상기식에서, R"는 H, 또는 메틸 또는 에틸 라디칼임)의 배합물로 구성된, 공결정물, 공침전물 또는 미쇄분쇄 물리적 혼합물 형태의 정제형 스트렙토그라민은 유용한 항균성 활성을 갖는다.Tablets of streptogramamine in the form of co-crystals, co-precipitates or pulverized physical mixtures, consisting of a combination of (wherein R '' is H, or methyl or ethyl radicals) have useful antimicrobial activity.

Description

정제형 스트렙토그라민 및 그의 제법Purified streptogramine and its preparation

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (10)

하기 구조식의 스트렙토그라민의 하나 이상의 B군 성분 :At least one group B component of streptogramin of the formula: (상기식에서, A1은 하기 구조식 :Wherein A 1 is the following structural formula: 의 라디칼이고, 이때 R'는 수소원자 또는 히드록시 라디칼이며, Y는 수소원자, 메틸아미노 라디칼 또는 디메틸아미노 라디칼이고, R은 에틸 라디칼이거나, R'가 수소 원자인 경우 R은 또한 메틸 라디칼이고, R1및 R2는 각각 수소원자이거나, 또는 A1은 하기 구조식 :Wherein R 'is a hydrogen atom or a hydroxy radical, Y is a hydrogen atom, a methylamino radical or a dimethylamino radical, R is an ethyl radical or when R' is a hydrogen atom, R is also a methyl radical, R 1 and R 2 are each hydrogen or A 1 is the following structural formula: 의 라디칼이고, R은 이소 부틸 라디칼이고, R1은 히드록실 라디칼이며 R2는 메틸 라디칼임) 및 하기 구조식의 스트렙토그라민의 하나 이상의 A군 부성분;And R is an isobutyl radical, R 1 is a hydroxyl radical and R 2 is a methyl radical) and at least one group A subcomponent of streptogamine of the formula: 상기식에서, R"는 수소 원자, 또는 메틸 또는 에틸 라디칼임)의 배합물로 구성된, 공결정물, 공침전물 또는 미세 분쇄 물리적 혼합물 형태의 정제형 스트렙토그라민.Wherein R '' is a hydrogen atom, or a mixture of methyl or ethyl radicals), tableted streptogramin in the form of a co-crystal, co-precipitate or finely ground physical mixture. 제1항에 있어서, 6% 이하의 불순물을 함유하는 정제형 스트렙토 그라민.The tablet streptogramamine according to claim 1, which contains up to 6% impurities. 제1항 또는 2항에 있어서, 스트렙토그라민의 상기 B군 성분 및 스트렙토그라민의 상기 A군 부성분의 상대비가 10:90 내지 90:10 중량비인 정제형 스트렙토그라민.The tablet type streptogramamine according to claim 1 or 2, wherein the relative ratio of the Group B component of streptogamine and the Group A subcomponent of streptogramin is 10:90 to 90:10 by weight. 제3항에 있어서, 스트렙토그라민의 상기 B군 성분 및 스트렙토 그라민의 상기 A군 부성분의 상대비가 20:80 내지 80:20 중량비인, 공침전 또는 미세 분쇄 물리적 혼합물 형태의 정제형 스트렙토그라민.4. The tablet streptogramin according to claim 3, wherein the relative ratio of the Group B component of streptogramin and the Group A subcomponent of streptogramin is in a 20:80 to 80:20 weight ratio. 제1 또는 2항에 있어서, 1:2 정도의 몰비의 스트렙토그라민의 하나 이상의 상기 B군 성분 및 스트렙토그라민의 하나 이상의 상기 A군 부성분의 공결성 화합물 형태의 정제형 스트렙토그라민.The tablet streptogramamine according to claim 1 or 2, in the form of a covalent compound of at least one of the Group B components of streptogramin at a molar ratio of about 1: 2 and at least one Group A subcomponent of streptogramine. 스트렙토그라민의 상기 B군 성분(들)과 스트렙토그라민의 상기 A군 성분(들)을 공결정화하고, 만일 필요하다면 얻어진 공결정 화합물을 적당한 A군 또는 B군 성분(들)과 배합하여 원하는 비의 배합물을 얻는 것으로 구성된, 제 1 항에 따른 정제형 스트랩토그라민의 제조 방법.Co-crystallizing the Group B component (s) of streptogamine and the Group A component (s) of streptogramin, and if necessary combining the obtained co-crystal compound with a suitable Group A or Group B component (s) A process for the preparation of tablets of straptogramin according to claim 1, consisting of obtaining a blend. 스트렙토그라민의 하나 이상의 B군 성분과 스트렙토그라민의 A군 부성분의 공결성 화합물을 제조하고 산 매질내에서 처리하므로써 B군 성분(들)을 제거하는 것으로 구성된, 제1항에서 청구된 바의 스트렙토그라민의 A군 부성분의 정제 방법.Streptogra as claimed in claim 1, consisting of removing the group B component (s) by preparing a covalent compound of at least one group B component of streptogramin and a group A subcomponent of streptogramin and treating in an acid medium. Purification method of Min group A subcomponent. 정제형의 하기 구조식의 스트렙토그라민의 A군 성분 :Group A component of streptogramin of the following structural formula in tablet form: 상기식에서, R"는 수소원자 또는 에틸 라디칼이다.Wherein R ″ is a hydrogen atom or an ethyl radical. 제1항에서 청구된 바의 스트렙토그라민 또는 이들의 유도체의 하나 이상의 B군 성분 및 스트렙토그라민의 하나 이상의 A군 부성분으로 구성된 공결정화 화합물.A co-crystallization compound consisting of at least one group B component of streptogramin or a derivative thereof as claimed in claim 1 and at least one group A subcomponent of streptogramin. 제1 또는 2항에 따른 정제형 스트렙토그라민으로 구성된 항균성 제약학적 조성물.An antimicrobial pharmaceutical composition consisting of tablet streptogamine according to claim 1. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940002667A 1993-02-17 1994-02-15 Purified form of streptogramins and its preparation KR100333185B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9301787 1993-02-17
FR9301787A FR2701709B1 (en) 1993-02-17 1993-02-17 Purified form of streptogramins, its preparation and the pharmaceutical compositions containing it.

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KR940019712A true KR940019712A (en) 1994-09-14
KR100333185B1 KR100333185B1 (en) 2002-08-21

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PE (1) PE11395A1 (en)
UY (1) UY23821A1 (en)

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JP2016055278A (en) * 2014-09-12 2016-04-21 竹上 敬三 Dividing method of cocrystal

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JP2005132849A (en) 2005-05-26
UY23821A1 (en) 1995-02-17
KR100333185B1 (en) 2002-08-21
PE11395A1 (en) 1995-07-14

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