RU2450015C2 - Производные аминотиазола и их применение в качестве антибактериальных средств - Google Patents

Производные аминотиазола и их применение в качестве антибактериальных средств Download PDF

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RU2450015C2
RU2450015C2 RU2008150785/04A RU2008150785A RU2450015C2 RU 2450015 C2 RU2450015 C2 RU 2450015C2 RU 2008150785/04 A RU2008150785/04 A RU 2008150785/04A RU 2008150785 A RU2008150785 A RU 2008150785A RU 2450015 C2 RU2450015 C2 RU 2450015C2
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Маттью Дж. ЛАМАРШ (US)
Маттью Дж. ЛАМАРШ
Саймон БУШЕЛЛ (US)
Саймон Бушелл
Майкл А. ПАТЕЙН (US)
Майкл А. Патейн
Льюис УАЙТХЕД (US)
Льюис Уайтхед
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Новартис Аг
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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Abstract

Изобретение относится к соединениям общей формулы (VI), которые обладают антибактериальной активностью и могут использоваться для борьбы с бактериальными инфекциями. 3 н. и 3 з.п. ф-лы, 1 табл., 26 пр.

Description

Текст описания приведен в факсимильном виде.
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Claims (6)

1. Соединение формулы VI:
Figure 00000131

и его фармацевтически приемлемые соли, энантиомеры, стереоизомеры, поворотные изомеры, диастереоизомеры, атропоизомеры или рацематы;
в которой
R выбран из группы, включающей N(R1)2, N(R1)-A-G-Q-J;
А выбран из группы, включающей -С(O)-, -С(O)O-, -C(O)N(R8a)-, -S(O)2-;
G отсутствует или выбран из группы, включающей -[C(Ra)(Rb)]x-, -[C(Ra)(Rb)]x-O-[C(Ra)(Rb)y и -[C(Ra)(Rb)]x-N(R8a)-[C(Ra)(Rb)]y-, или выбран из группы, включающей (циклогексил)-, -(пирролидинил)-;
Q отсутствует или обозначает -С(O)-{N(R8a)-[C(Ra)(Rb)y}p-;
J выбран из группы, включающей Н, С14алкил, галоген, гидроксигруппу, аминогруппу, CO2H, CO214алкил, Р(O)(ОН)2;
Ra выбран из группы, включающей Н, С14алкил, F, -N(R1)2;
Rb выбран из группы, включающей Н, С14алкил и F;
р равно 1;
х и y независимо в каждом случае выбраны из целых чисел, равных 0-10;
R1 независимо в каждом случае выбран из группы, включающей -Н, С14алкил или С14алкил, замещенный J, и -R4b;
R2 обозначает остаток формулы:
Figure 00000132

R2a выбран из группы, включающей ОН, OC(O)R4a;
R2b обозначает Н;
R3 обозначает Н или С14алкил;
R12 обозначает СН2-O-СН3;
R4a обозначает Н или С14алкил;
R4b обозначает С14алкил;
R5 обозначает Н;
R8a обозначает Н.
2. Соединение по п.1, в котором R2a обозначает ОН или ОАс и R2b обозначает Н.
3. Соединение по п.1, в котором А обозначает С(O), С(O)O или C(O)NH;
G обозначает циклогексил;
Q отсутствует; и
J обозначает CO2H или CO2C1-C4алкил.
4. Соединение по п.1, в котором соединение формулы VI представляет собой соединение формулы VII:
Figure 00000133

и его фармацевтически приемлемые соли.
5. Способ борьбы с бактериальной инфекцией у субъекта, включающий введение нуждающемуся в этом субъекту соединения по любому из пп.1-4 в фармацевтически приемлемом количестве и фармацевтически приемлемый носитель, так что проводится борьба с бактериальной инфекцией.
6. Фармацевтическая композиция, обладающая антибактериальной активностью, включающая соединение по любому из пп.1-4 в фармацевтически приемлемом количестве и по меньшей мере один фармацевтически приемлемый носитель или разбавитель.
RU2008150785/04A 2006-05-31 2007-05-30 Производные аминотиазола и их применение в качестве антибактериальных средств RU2450015C2 (ru)

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AR060977A1 (es) * 2006-05-31 2008-07-23 Novartis Ag Aminotiazoles y sus usos
EA200900816A1 (ru) 2006-12-20 2009-12-30 Новартис Аг Антибактериальные соединения и способы их получения
CA2688621A1 (en) 2007-06-04 2008-12-11 Novartis Ag Macrocycles and their uses
AU2012261611B2 (en) * 2007-12-12 2014-05-15 Novartis Ag Aminothiazoles and their uses
PE20091108A1 (es) 2007-12-12 2009-08-24 Novartis Ag Aminotiazoles y sus usos
WO2014167371A1 (en) * 2013-04-12 2014-10-16 Naicons S.C.A.R.L. Analogs of the antibiotic aminothiazole ge2270
CN106366168B (zh) * 2016-08-26 2020-09-15 上海交通大学 羊毛硫肽类抗菌肽及其脱氢衍生物的制备方法
CN107243008B (zh) * 2017-04-13 2021-03-30 中国科学院广州生物医药与健康研究院 吡唑并[1,5-a]吡啶类化合物的新应用及一种治疗脓肿分枝杆菌感染的组合物
CN113219078B (zh) * 2021-03-25 2022-12-16 广东产品质量监督检验研究院(国家质量技术监督局广州电气安全检验所、广东省试验认证研究院、华安实验室) 一种生活用纸制品中17种有机抗菌剂快速筛查方法

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WO1997030078A1 (en) * 1996-02-14 1997-08-21 Biosearch Italia S.P.A. DERIVATIVES OF ANTIBIOTIC GE2270 FACTORS C2a, D2 AND E
EP0825194A2 (en) * 1996-08-22 1998-02-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai An amide derivative of amythiamicin
WO2003105881A1 (en) * 2002-06-17 2003-12-24 Vicuron Pharmaceuticals Inc. Use of amide derivative of ge 2270 factor a3 for the treatment of acne

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EP0451486B1 (en) * 1990-03-08 1995-04-19 GRUPPO LEPETIT S.p.A. Antibiotic GE 2270 factors B1, B2, C1, C2, D1, D2,E and T
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US5882900A (en) * 1992-09-10 1999-03-16 Gruppo Lepetit S.P.A. Process for the selective increase of production of antibiotic GE 2270 factor a by adding vitamin B12 to nutrient medium
AU679202B2 (en) 1992-12-22 1997-06-26 Gruppo Lepetit S.P.A. Antibiotics GE 37468 A, B and C
JPH10508476A (ja) 1994-11-08 1998-08-25 グルポ・レペチツト・エス・ピー・エイ 抗生物質ge2270因子d▲下2▼を得るための微生物変換法
ATE205505T1 (de) * 1995-02-07 2001-09-15 Biosearch Italia Spa Basische oxazolinamid-derivate von ge2270 und ge2270-änlichen antibiotika
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WO1997030078A1 (en) * 1996-02-14 1997-08-21 Biosearch Italia S.P.A. DERIVATIVES OF ANTIBIOTIC GE2270 FACTORS C2a, D2 AND E
EP0825194A2 (en) * 1996-08-22 1998-02-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai An amide derivative of amythiamicin
WO2003105881A1 (en) * 2002-06-17 2003-12-24 Vicuron Pharmaceuticals Inc. Use of amide derivative of ge 2270 factor a3 for the treatment of acne

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BRPI0711885A2 (pt) 2012-03-06
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US20080221142A1 (en) 2008-09-11
ES2441993T3 (es) 2014-02-07
MA30485B1 (fr) 2009-06-01
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US20100267757A1 (en) 2010-10-21
IL194880A (en) 2015-02-26
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CA2650133A1 (en) 2007-12-13
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JP5351014B2 (ja) 2013-11-27
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MY146920A (en) 2012-10-15
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