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RU2317990C2 - СОЕДИНЕНИЯ ТРИАЗОЛО(4,5-d)ПИРИМИДИНА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ - Google Patents

СОЕДИНЕНИЯ ТРИАЗОЛО(4,5-d)ПИРИМИДИНА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ Download PDF

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RU2317990C2
RU2317990C2 RU2001118284/04A RU2001118284A RU2317990C2 RU 2317990 C2 RU2317990 C2 RU 2317990C2 RU 2001118284/04 A RU2001118284/04 A RU 2001118284/04A RU 2001118284 A RU2001118284 A RU 2001118284A RU 2317990 C2 RU2317990 C2 RU 2317990C2
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pyrimidin
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cyclopentan
cyclopropyl
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Саймон ГИЛ (GB)
Саймон ГИЛ
Дэвид ХАРДЕРН (GB)
Дэвид ХАРДЕРН
Энтони ИНГОЛЛ (GB)
Энтони ИНГОЛЛ
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Abstract

Описываются новые производные триазоло[4,5-d]пиримидина общей формулы I
Figure 00000001
где
R1 - С3-5алкил, возможно замещенный галогеном;
R2 - фенил, возможно замещен фтором;
R3 и R4 одинаковы и означают гидрокси;
R - ХОН, где Х обозначает СН2, ОСН2СН2 или связь;
или его фармацевтически приемлемая соль, или сольват, или сольват такой соли,
при условии, что:
когда Х-СН2 или связь, R1 не означает пропил,
когда Х обозначает СН2 и R1 обозначает СН2СН2CF3, бутил или пентил, фенильная группа на R2 должна быть замещена фтором,
когда Х обозначает ОСН2СН2 и R1-пропил, фенильная группа на R2 должна быть замещена фтором; фармацевтическая композиция на их основе, способ их получения, новые промежуточные продукты формул:
Figure 00000002
Figure 00000003
и [R-(R*, R*)-2,3-дигидроксибутандиоат (1:1) соединения III
Figure 00000004
и способ лечения заболеваний, опосредованных Р2T рецептором, таких как инфаркт миокарда, предотвращения или распространения опухоли и др. 9 н. и 6 з.п. ф-лы.

Description

Текст описания приведен в факсимильном виде.
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Claims (16)

1. Соединения триазоло[4,5-d]пиримидина общей формулы I
Figure 00000069
где R1 обозначает неразветвленный С3-5алкил, необязательно замещенный одним или большим числом атомов галогена;
R2 обозначает фенильную группу, необязательно замещенную одним или большим числом атомов фтора;
R3 и R4 являются оба гидроксигруппами;
R обозначает ХОН, где Х обозначает CH2, OCH2CH2 или связь;
или их фармацевтически приемлемая соль, или сольват, или сольват такой соли,
при условии, что:
когда X обозначает СН2 или связь, R1 не может быть пропилом,
когда Х обозначает СН2 и R1 обозначает СН2СН2CF3, бутил или пентил, фенильная группа на R2 должна быть замещена фтором,
когда Х обозначает ОСН2СН2 и R1 - пропил, фенильная группа на R2 должна быть замещена фтором.
2. Соединение по п.1, в котором R1 обозначает 3,3,3-трифторпропил, неразветвленный бутил или неразветвленный пропил.
3. Соединение по п.1 или 2, в котором R2 обозначает фенил или 4-фторфенил или 3,4-дифторфенил.
4. Соединение по любому одному из пп.1-3, в котором R обозначает СН2OH или ОСН2СН2OH.
5. Соединение по п.1, которое представляет собой:
[1R-[1α,2а,3β(1R*,2S*),5β]]-3-[7-[[2-(4-фторфенил)-циклопропил]амино]-5-[(3,3,3-трифторпропил)тио]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-5-(гидроксиметил)-циклопентан-1,2-диол;
[1R-[1α,2α,3β(1R*,2S*),5β]]-3-[7-[[2-(3,4-дифторфенил)-циклопропил]амино]-5-[(3,3,3-трифторпропил)тио]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-5-(гидроксиметил)циклопентан-1,2-диол;
[1S-(1α,2α,3β(1S*,2R*),5β]]-3-[7-[[2-(3,4-дифторфенил)-циклопропил]амино]-5-(пропилтио)-3Н-1,2,3-триазоло-[4,5-d]пиримидин-3-ил]-5-(2-гидроксиэтокси)-циклопентан-1,2-диол;
[1R-[1α,2α,3β(1R*,2S*),5β]]-3-[5-(бутилтио)-7-[[2-(3,4-дифторфенил)циклопропил]амино]-3Н-1,2,3-триазоло[4,5-d]-пиримидин-3-ил]-5-(гидроксиметил)-циклопентан-1,2-диол;
[1S-[1α,2β,3β,4α(1S*,2R*)]]-4-[5-(бутилтио)-7-[[2-(4-фторфенил)циклопропил]амино]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-циклопентан-1,2,3-триол;
[1S-(1α,2α,3β(1S*,2R*),5β]-3-[7-[[2-(3,4-дифторфенил)-циклопропил]амино]-5-[(3,3,3-трифторпропил)тио]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-5-(гидроксиэтокси)-циклопентан-1,2-диол;
[1S-[1α,2α,3β,5β(1S*,2R*)]]-3-(2-гидроксиэтокси)-5-[7-(2-фенилциклопропил)амино]-5-[(3,3,3-трифторпропил)тио]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-циклопентан-1,2-диол;
[1S-[1α,2β,3β,4α(1S*,2R*)]]-4-[5-(бутилтио)-7-[[2-(3,4-дифторфенил)циклопропил]амино]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]циклопентан-1,2,3-триол;
[1S-[1α,2α,3β(1S*,2R*),5β]]-3-[5-(бутилтио)-7-[(2-фенилциклопропил)амино]-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-5-(2-гидроксиэтокси)-циклопентан-1,2-диол; где алкильные группы являются неразветвленными;
или их фармацевтически приемлемые соли, или их сольваты, или сольваты таких солей.
6. [1S-[1α,2α,3β(1S*,2R*),5β]]-3-[7-[2-(3,4-дифторфенил)циклопропил)амино]-5-(н-пропилтио)-3Н-1,2,3-триазоло[4,5-d]пиримидин-3-ил]-5-(2-гидроксиэтокси)-циклопентан-1,2-диол.
7. Фармацевтическая композиция, обладающая антагонистической/агонистической активностью в отношении Р2T рецептора, включающая соединение по любому одному из пп.1-6 в сочетании с фармацевтически приемлемым разбавителем, адъювантом и/или носителем.
8. Фармацевтическая композиция, включающая соединение по любому одному из пп.1-6, предназначенная для лечения или профилактики инфаркта миокарда, кровоизлияния тромботической природы, преходящего нарушения мозгового кровообращения и/или болезней периферических сосудов или предотвращения роста или распространения опухоли.
9. Соединение по любому одному из пп.1-6, предназначенное для лечения или профилактики инфаркта миокарда, кровоизлияния тромботической природы, преходящего нарушения мозгового кровообращения и/или болезней периферических сосудов или предотвращения роста или распространения опухоли.
10. Соединение по любому одному из пп.1-6 в качестве активного ингредиента при производстве лекарственного средства, предназначенного для лечения или профилактики инфаркта миокарда, кровоизлияния тромботической природы, преходящего нарушения мозгового кровообращения и/или болезней периферических сосудов или предотвращения роста или распространения опухоли.
11. Способ лечения или профилактики нарушений, опосредованных Р2T рецептором, выбранных из инфаркта миокарда, кровоизлияния тромботической природы, преходящего нарушения мозгового кровообращения и/или болезней периферических сосудов или предотвращения роста или распространения опухоли, который включает введение субъекту, страдающему от такого нарушения или восприимчивому к такому состоянию, терапевтически эффективного количества соединения по любому одному из пп.1-6.
12. Способ получения соединения формулы (I) по п.1, при котором соединение формулы (II):
Figure 00000070
где R и R1 определены в п.1 и L обозначает уходящую группу,
подвергают взаимодействию с [R-(R*,R*)-2,3-дигидроксибутандиоатом (1:1) соединения формулы (III):
Figure 00000071
где R2 определен в п.1,
в присутствии основания в инертном растворителе при температуре окружающей среды.
13. Соединение формулы (II):
Figure 00000070
где R и R1 определены в п.1 и L обозначает уходящую группу.
14. Соединение формулы (V):
Figure 00000072
где R1 и R определены в п.1 и L представляет уходящую группу.
Приоритет по пунктам:
04.12.1998 по пп.1-4, 6-14;
09.04.1999 по п.5.
RU2001118284/04A 1998-12-04 1999-12-02 СОЕДИНЕНИЯ ТРИАЗОЛО(4,5-d)ПИРИМИДИНА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ RU2317990C2 (ru)

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SE9901271A SE9901271D0 (sv) 1999-04-09 1999-04-09 Novel compounds

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