RU2225404C2 - ПРОИЗВОДНЫЕ ПИПЕРАЗИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ФАКТОРА Хa - Google Patents

ПРОИЗВОДНЫЕ ПИПЕРАЗИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ФАКТОРА Хa Download PDF

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RU2225404C2
RU2225404C2 RU2000104829/04A RU2000104829A RU2225404C2 RU 2225404 C2 RU2225404 C2 RU 2225404C2 RU 2000104829/04 A RU2000104829/04 A RU 2000104829/04A RU 2000104829 A RU2000104829 A RU 2000104829A RU 2225404 C2 RU2225404 C2 RU 2225404C2
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piperazine
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inhibitory activity
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Роджерс ДЖЕЙМС (GB)
Роджерс ДЖЕЙМС
Торстен НОВАК (GB)
Торстен Новак
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Abstract

Описываются производные пиперазина общей формулы I
Figure 00000001

в которой А представляет необязательно замещенное 5- или 6-членное моноциклическое ароматическое кольцо с 1, 2 или 3 атомами азота; B1, B2, В3 и В4 являются независимо СН или атомом азота, при условии, что по крайней мере один из B1, В2, В3 и В4 является азотом; X1 представляет СО; T1 представляет N; T2 представляет N; L1 представляет собой (1-4С)алкилен; R2 и R3 вместе образуют C1-4 алкиленовую группу, так что группа -T1(R2)-L1-Т2(R3)- образует пиперазиновое кольцо; Х2 представляет S(O)2; Q представляет собой фенил, нафтил, фенил(2-4С)алкенил, бензофуранил, индолил и Q является замещенным одним заместителем, выбранным из галогенов, фенила, замещенного галогеном. Описывается также фармацевтическая композиция, обладающая ингибирующей активностью в отношении фактора Ха. Технический результат заключается в получении производных пиперазина, проявляющих антитромболитические и антикоагуляционные свойства. 2 с. и 2 з.п. ф-лы, 1 табл.

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Claims (4)

  1. Производное пиперазина формулы I
    Figure 00000055
    в которой А представляет собой необязательно замещенное 5- или 6-членное моноциклическое ароматическое кольцо, содержащее в кольце 1, 2 или 3 азота;
    B1, В2, В3 и B4 являются независимо СН или атомом азота, при условии, что, по крайней мере, один из B1, B2, В3 и В4 является азотом,
    X1 представляет СО;
    T1 представляет собой N;
    Т2 представляет собой N;
    L1 представляет собой (1-4С)алкилен;
    R2 и R3 вместе образуют C1-4 алкиленовую группу; так что группа – T1(R2)-L1-Т2(R3) образует пиперазиновое кольцо,
    Х2 представляет собой S(O)2;
    Q представляет собой фенил, нафтил, фенил(2-4С)алкенил, бензофуранил, индолил и Q является замещенным одним заместителем, выбранным из галогенов, фенила, замещенного галогеном,
    и их фармацевтически приемлемые соли.
  2. 2. Соединение формулы I по любому из предшествующих пунктов, в которой А является незамещенным или замещенным одним радикалом, выбранным из (1-4С)алкила.
  3. 3. Соединение формулы I по любому из предшествующих пунктов, обладающее ингибирующей активностью в отношении фактора Ха, пригодное в терапии.
  4. 4. Фармацевтическая композиция, обладающая ингибирующей активностью в отношении фактора Ха, включающая в качестве активного компонента соединение формулы I, как определено в пп.1, 2 или 3, в эффективном количестве и фармацевтически приемлемый носитель.
RU2000104829/04A 1997-07-29 1998-07-23 ПРОИЗВОДНЫЕ ПИПЕРАЗИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ФАКТОРА Хa RU2225404C2 (ru)

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EP1000033B1 (en) 2004-05-06
US6458793B1 (en) 2002-10-01
WO1999006371A1 (en) 1999-02-11
AU8455798A (en) 1999-02-22
KR20010022108A (ko) 2001-03-15
CN1265098A (zh) 2000-08-30
SK1272000A3 (en) 2000-06-12
US20020193375A1 (en) 2002-12-19
DE69823665D1 (de) 2004-06-09
NO20000448L (no) 2000-03-16
NO317419B1 (no) 2004-10-25
JP2001512103A (ja) 2001-08-21
BR9811055A (pt) 2000-09-05
NZ501778A (en) 2001-09-28
NO20040520L (no) 2004-02-05
TR200000223T2 (tr) 2000-07-21
EP1000033A1 (en) 2000-05-17
NO20000448D0 (no) 2000-01-28
HUP0002528A3 (en) 2002-09-30
CA2295945A1 (en) 1999-02-11
HUP0002528A2 (hu) 2001-06-28
PT1000033E (pt) 2004-08-31
EP1367054A1 (en) 2003-12-03
DK1000033T3 (da) 2004-08-02
DE69823665T2 (de) 2005-04-28
ATE266007T1 (de) 2004-05-15
ES2219894T3 (es) 2004-12-01
AU754747B2 (en) 2002-11-21
PL338355A1 (en) 2000-10-23
GB9715894D0 (en) 1997-10-01

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