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RU2002111657A - HEXAHYDROFURO [2,3-b] FURAN-3-IL-N- {3 - [(1,3-BENZODIOXOL-5-ILSULFONIL) (Isobutyl) AMINO] -1-BENZYL-2-HYDROXYPROPYL} CARBAMRUS KARINOBI - Google Patents

HEXAHYDROFURO [2,3-b] FURAN-3-IL-N- {3 - [(1,3-BENZODIOXOL-5-ILSULFONIL) (Isobutyl) AMINO] -1-BENZYL-2-HYDROXYPROPYL} CARBAMRUS KARINOBI

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Publication number
RU2002111657A
RU2002111657A RU2002111657/04A RU2002111657A RU2002111657A RU 2002111657 A RU2002111657 A RU 2002111657A RU 2002111657/04 A RU2002111657/04 A RU 2002111657/04A RU 2002111657 A RU2002111657 A RU 2002111657A RU 2002111657 A RU2002111657 A RU 2002111657A
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RU
Russia
Prior art keywords
compound according
retrovirus
mammals
compound
inhibiting
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Application number
RU2002111657/04A
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Russian (ru)
Other versions
RU2247123C2 (en
Inventor
Пит Том Берт Поль Вигеринк
Гуангианг ВАНГ
Майкл ЭЙССЕНСТЭТ
Джон В. ЭРИКСОН
Original Assignee
Тиботек Фармасьютикалз Лтд.
ДЗЕ ГАВЕРМЕНТ ОФ ДЗЕ ЮНАЙТЕД СТЕЙТС ОФ АМЕРИКА, репрезентед бай ДЗЕ СЕКРЕТЭРИ, ДЕПАРТМЕНТ ОФ ХЕЛТ ЭНД ХЬЮМЭН СЕРВИСИЗ, НЭШНЛ ИНСТИТЬЮТС ОФ ХЕЛТ
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Application filed by Тиботек Фармасьютикалз Лтд., ДЗЕ ГАВЕРМЕНТ ОФ ДЗЕ ЮНАЙТЕД СТЕЙТС ОФ АМЕРИКА, репрезентед бай ДЗЕ СЕКРЕТЭРИ, ДЕПАРТМЕНТ ОФ ХЕЛТ ЭНД ХЬЮМЭН СЕРВИСИЗ, НЭШНЛ ИНСТИТЬЮТС ОФ ХЕЛТ filed Critical Тиботек Фармасьютикалз Лтд.
Publication of RU2002111657A publication Critical patent/RU2002111657A/en
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Publication of RU2247123C2 publication Critical patent/RU2247123C2/en

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Claims (18)

1. Соединение, представленное формулой1. The compound represented by formula
Figure 00000001
Figure 00000001
его N-оксид, соль, сложный эфир, стереоизомерная форма, рацемическая смесь, пролекарство или метаболит.its N-oxide, salt, ester, stereoisomeric form, racemic mixture, prodrug or metabolite.
2. Соединение по п.1 в энантиомерно чистой форме.2. The compound according to claim 1 in enantiomerically pure form. 3. Соединение по п.1 или 2, отличающееся тем, что соединение представляет собой3. The compound according to claim 1 or 2, characterized in that the compound is a
Figure 00000002
Figure 00000002
его N-оксид, соль, сложный эфир, пролекарство или метаболит.its N-oxide, salt, ester, prodrug or metabolite.
4. Соединение по любому из пп.1-3 в форме фармацевтически переносимой соли.4. The compound according to any one of claims 1 to 3 in the form of a pharmaceutically tolerated salt. 5. Соединение по любому из пп.1-4 в форме пролекарства.5. The compound according to any one of claims 1 to 4 in the form of a prodrug. 6. Фармацевтическая композиция, содержащая эффективное количество, по крайней мере, одного соединения по любому из пп.1-5 и фармацевтически переносимый наполнитель.6. A pharmaceutical composition comprising an effective amount of at least one compound according to any one of claims 1 to 5 and a pharmaceutically acceptable excipient. 7. Способ ингибирования ретровирусной протеазы у млекопитающих, инфицированных указанным ретровирусом, включающий введение соединения по любому из пп.1-5 в количестве, ингибирующем протеазу, указанным нуждающимся в этом млекопитающим.7. A method of inhibiting a retroviral protease in mammals infected with said retrovirus, comprising administering a compound according to any one of claims 1 to 5 in an amount that inhibits the protease indicated by the mammal in need. 8. Способ лечения или борьбы с инфекцией или заболеванием, связанным с ретровирусной инфекцией, у млекопитающих, включающий введение эффективного количества, по крайней мере, одного соединения по любому из пп.1-5 указанным млекопитающим.8. A method of treating or combating an infection or disease associated with a retroviral infection in mammals, comprising administering an effective amount of at least one compound according to any one of claims 1 to 5 to said mammals. 9. Способ по п.7 или 8, отличающийся тем, что указанным млекопитающим является человек.9. The method according to claim 7 or 8, characterized in that said mammal is a human. 10. Способ ингибирования репликации ретровируса, включающий воздействие на ретровирус эффективным количеством, по крайней мере, одного соединения по любому из пп.1-5.10. A method of inhibiting retrovirus replication, comprising exposing the retrovirus to an effective amount of at least one compound according to any one of claims 1-5. 11. Способ по п.7 или 8, или 10, отличающийся тем, что ретровирус представляет собой вирус иммунодефицита человека (ВИЧ).11. The method according to claim 7 or 8, or 10, characterized in that the retrovirus is a human immunodeficiency virus (HIV). 12. Способ по п.11, отличающийся тем, что вирус ВИЧ представляет собой штамм, резистентный ко многим лекарственным препаратам.12. The method according to claim 11, characterized in that the HIV virus is a strain resistant to many drugs. 13. Соединение по любому из пп.1-5, для применения в качестве лекарства.13. The compound according to any one of claims 1 to 5, for use as a medicine. 14. Соединения по любому из пп.1-5 в качестве активного ингредиента лекарственного препарата для лечения или борьбы с инфекцией или заболеванием, связанным с ретровирусной инфекцией, у млекопитающих.14. Compounds according to any one of claims 1 to 5 as an active ingredient of a medicament for treating or combating an infection or disease associated with a retroviral infection in mammals. 15. Соединения по любому из пп.1-5 в качестве активного ингредиента лекарственного препарата для ингибирования ретровирусной протеазы у млекопитающих, инфицированных указанным ретровирусом.15. Compounds according to any one of claims 1 to 5 as an active ingredient of a medicament for inhibiting a retroviral protease in mammals infected with said retrovirus. 16. Соединения по любому из пп.1-5 в качестве активного ингредиента лекарственного препарата для ингибирования репликации ретровируса.16. Compounds according to any one of claims 1 to 5 as an active ingredient of a medicament for inhibiting retrovirus replication. 17. Применение по любому из пп.14-16, отличающееся тем, что ретровирус представляет собой вирус иммунодефицита человека (ВИЧ).17. The use according to any one of paragraphs.14-16, characterized in that the retrovirus is a human immunodeficiency virus (HIV). 18. Применение по любому из пп. 14-16, отличающееся тем, что вирус ВИЧ представляет собой штамм, резистентный ко многим лекарственным препаратам.18. The use according to any one of paragraphs. 14-16, characterized in that the HIV virus is a strain resistant to many drugs.
RU2002111657/04A 1999-10-06 2000-10-06 Hexahydrofuro[2,3-b]furan-3-yl-n-{3-[(1,3-benzodioxol-5- yl- sulfonyl)(isobu tyl)amino]-1-benzyl-2-hydroxypropyl}carbamate, pharmaceutical composition based on thereof, methods for inhibition and method for treatment RU2247123C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15785099P 1999-10-06 1999-10-06
US60/157,850 1999-10-06

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RU2002111657A true RU2002111657A (en) 2003-12-10
RU2247123C2 RU2247123C2 (en) 2005-02-27

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US (2) US6649651B1 (en)
EP (1) EP1222192B8 (en)
JP (1) JP4951179B2 (en)
KR (1) KR100792391B1 (en)
CN (1) CN1191256C (en)
AP (1) AP1459A (en)
AT (1) ATE398623T1 (en)
AU (1) AU781656B2 (en)
BR (1) BR0014602A (en)
CA (1) CA2386850C (en)
CZ (1) CZ300031B6 (en)
DE (1) DE60039244D1 (en)
DK (1) DK1222192T3 (en)
ES (1) ES2307533T3 (en)
HU (1) HU228938B1 (en)
IL (2) IL149005A0 (en)
MX (1) MXPA02003607A (en)
NO (1) NO327996B1 (en)
NZ (1) NZ518580A (en)
OA (1) OA12053A (en)
PL (1) PL204924B1 (en)
RU (1) RU2247123C2 (en)
SK (1) SK287153B6 (en)
WO (1) WO2001025240A1 (en)
ZA (1) ZA200202655B (en)

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