RU2208613C2 - Оксазолидиноновые антибактериальные агенты, содержащие тиокарбонильную функциональную группу - Google Patents

Оксазолидиноновые антибактериальные агенты, содержащие тиокарбонильную функциональную группу Download PDF

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RU2208613C2
RU2208613C2 RU99128083/04A RU99128083A RU2208613C2 RU 2208613 C2 RU2208613 C2 RU 2208613C2 RU 99128083/04 A RU99128083/04 A RU 99128083/04A RU 99128083 A RU99128083 A RU 99128083A RU 2208613 C2 RU2208613 C2 RU 2208613C2
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methyl
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Джексон Б. Мл. ХЕСТЕР
Элдон Джордж НАЙДИ
Сальваторе Чарльз ПЕРРИКОН
Тони-Джо ПОЕЛ
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Abstract

Описываются производные оксазолидинона формулы (I)
Figure 00000001

или их фармакологически приемлемые соли,
где G представляет собой
Figure 00000002

R1 представляет Н, NH2, NH-C1-4алкил, -C1-4алкил, -OC1-4алкил, -SC1-4алкил, А представляет собой
Figure 00000003

6-членную гетероароматическую группу, содержащую, по крайней мере, один атом азота, Q представляет собой
Figure 00000004

Figure 00000005

Figure 00000006

Figure 00000007

где Z2 представляет собой -SO2-, -O-, -S, -N(R107)-, -SO-; М представляет собой Н; Y и Х представляют собой Н. Описывается также способ лечения микробной инфекции у пациентов. Технический результат заключается в получении антимикробных средств, эффективных против большинства патогенов человека и животных. 2 с. и 1 з.п.ф-лы, 2 табл.

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Текст описания в факсимильном виде (см. графическую часть).

Claims (3)

1. Производное оксазолидинона формулы I
Figure 00000012

или его фармакологически приемлемые соли,
где G представляет собой;
Figure 00000013

R1 представляет собой a) Н; b) NH2; c) NH-C1-4 алкил; d) -C1-4 алкил; e) -OC1-4 алкил; f) -SC1-4 алкил; д) -C1-4 алкил, замещенный 1-3 F, 1-2 Cl, CN или -COOC1-4 алкилом;
А представляет собой
Figure 00000014

е) 6-членную гетероароматическую группу, содержащую, по крайней мере, один атом азота, где гетероароматическая группа замещена одним R55; где R23 и R24 в каждом случае являются одинаковыми или различными и представляют собой a) Н, b) F;
Q представляет собой
Figure 00000015

Figure 00000016

Figure 00000017

Figure 00000018

или Q и R24, взятые вместе, представляют собой
Figure 00000019

где Z2 представляет собой a) -SО2-; b) -О-; с) -N(R107)-; d) -SO- или e) -S;
где R106 представляет собой НОСН2-С(О)-;
где R107 представляет собой НО-СН2-С (О)-;
М представляет собой Н;
Y представляет собой Н;
Х представляет собой Н;
где Е представляет собой -S(=О)i;
R38 представляет собой Н;
где R55 представляет собой 5-членную ненасыщенную гетероциклическую группу, содержащую три атома, выбранные из группы, включающей S, N, замещенную одним R58;
R58 обозначает C1-6 алкил;
i=1 или 2;
m=1;
n=1;
р=1 или n и p вместе равны 1.
2. Производное оксазолидинона по п.1, которое представляет собой
a) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]тиоацетамид;
b) (S)-N-[[3-[3-фтор-4-[4-(5-метил-1,3,4-тиадиазол-2-ил)-1-пиперазинил] фенил]-2-оксо-5-оксазолидинил]метил]-тиоацетамид;
d) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]тиоацетамид;
e) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]тиомочевину;
f) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил-N'-метилтиомочевину;
g) (3)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]тиоформамид;
h) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]тиопропионамид;
i) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил-2-хлортиоацетамид;
j) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]-α, α, α-трифтортиоацетамид;
k) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]-α-фтортиоацетамид;
l) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]-α, α-дифтортиоацетамид;
m) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]-α-циантиоацетамид;
n) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил-α,α-дихлортиоацетамид;
о) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил] -2-оксо-5-оксазолидинил]метил]-α-(метоксикарбонил)тиоацетамид;
p) (S)-N-[[3-[4-[1-[1,2,4]триазолил]фенил]-2-оксо-5-оксазолидинил]метил] тиоацетамид;
q) (S)-N-[[3-[4-[1-[1,2,4]триазолил]фенил]-2-оксо-5-оксазолидинил]метил] тиоацетамид;
r) (S)-N-[[3-[1-(гидроксиацетил)-5-индолинил]-2-оксо-5-оксазолидинил]метил]тиоацетамид;
s) (S)-N-[[3-[3-фтор-4-[4-(гидроксиацетил)-1-пиперазинил] фенил] -2-оксо-5-оксазолидинил]метил]тиоацетамид;
t) (S)-N-[[3-[3-фтор-4-(4-тиоморфолинил)фенил] -2-оксо-5-оксазолидинил] метил]тиоацетамид;
u) (S)-N-[[3-[3-фтор-4-(4-тиоморфолинил)фенил] -2-оксо-5-оксазолидинил] метил]тиоацетамид, тиоморфолин S-оксид;
v) (3)-N-[[3-[3-фтор-4-(4-тиоморфолинил)фенил] -2-оксо-5-оксазолидинил] метил]тиоацетамид, тиоморфолин S,S-диоксид;
w) (S)-N-[[3-[3,5-дифтор-4-[4-(гидроксиацетил)-1-пиперазинил]фенил]-2-оксо-5-оксазолидинил]метил]тиоацетамид;
x) (S)-N-[[3-[4-[1,2,4] триазолил] фенил]-2-оксо-5-оксазолидинил]метил] тиомочевину;
y) (S)-N-[[3-[3-фтор-4-[4-(гидроксиацетил)-1-пиперазинил] фенил] -2-оксо-5-оксазолидинил]метил]тиомочевину;
z) (S)-N-[[3-[1-(гидроксиацетил)-5-индолинил] -2-оксо-5-оксазолидинил] метил]тиомочевину;
aa) (S)-N-[[3-[3-фтор-4-(4-тиоморфолинил)фенил-2-оксо-5-оксазолидинил] метил]тиомочевину, тиоморфолин S-оксид;
bb) (S)-N-[[3-[3-фтор-4-(4-морфолинил)фенил]-2-оксо-5-оксазолидинил]метил-3-метилдитиокарбамат.
3. Способ лечения микробной инфекции у пациентов, включающий введение пациенту, если необходимо, эффективного количества соединения формулы I.
RU99128083/04A 1997-05-30 1998-05-18 Оксазолидиноновые антибактериальные агенты, содержащие тиокарбонильную функциональную группу RU2208613C2 (ru)

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CA2288750A1 (en) 1998-12-03
EP0984947B8 (en) 2005-06-15
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NZ501412A (en) 2001-11-30
HUP0001393A2 (hu) 2001-06-28
ATE293609T1 (de) 2005-05-15
WO1998054161A1 (en) 1998-12-03
KR20010013192A (ko) 2001-02-26
WO1998054161A9 (en) 1999-04-08
HUP0001393A3 (en) 2001-07-30
ES2242280T3 (es) 2005-11-01
PL337329A1 (en) 2000-08-14
SK156499A3 (en) 2000-06-12
EP0984947A1 (en) 2000-03-15
NO315798B1 (no) 2003-10-27
AU737995B2 (en) 2001-09-06
CN1138765C (zh) 2004-02-18
DE69829846T2 (de) 2006-02-23
AU7488398A (en) 1998-12-30
HK1027569A1 (en) 2001-01-19
DE69829846D1 (de) 2005-05-25
NO995846D0 (no) 1999-11-29
JP2002501530A (ja) 2002-01-15
BR9815518A (pt) 2000-11-21
CN1257486A (zh) 2000-06-21
FI19992555A (fi) 1999-11-30

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