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RU2003104981A - USE OF SOH-2 INHIBITORS TO PREVENT IMMUNO DEFICIENCY - Google Patents

USE OF SOH-2 INHIBITORS TO PREVENT IMMUNO DEFICIENCY

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Publication number
RU2003104981A
RU2003104981A RU2003104981/15A RU2003104981A RU2003104981A RU 2003104981 A RU2003104981 A RU 2003104981A RU 2003104981/15 A RU2003104981/15 A RU 2003104981/15A RU 2003104981 A RU2003104981 A RU 2003104981A RU 2003104981 A RU2003104981 A RU 2003104981A
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RU
Russia
Prior art keywords
cox
use according
inhibitor
group
pharmaceutically acceptable
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RU2003104981/15A
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Russian (ru)
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RU2303452C2 (en
Inventor
Хьетиль ТАСКЕН
Мишель МАУТСЕН
Суад РАМУНИ-ПЬЕТТ
Эйнар Мартин ОННАЛЬ
Поль ЭУКРУСТ
Стиг С. ФРЕЛАНН
Кристиан Карл ЙОХАНССОН
Видар ХАНССОН
Йо Клавенесс
Original Assignee
Леурас Ас
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Priority claimed from GB0017908A external-priority patent/GB0017908D0/en
Priority claimed from GB0109648A external-priority patent/GB0109648D0/en
Application filed by Леурас Ас filed Critical Леурас Ас
Publication of RU2003104981A publication Critical patent/RU2003104981A/en
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Claims (27)

1. Применение ингибитора СОХ-2, который ингибирует ферментативную активность СОХ-2, или его производного, или фармацевтически приемлемой соли для изготовления лекарственного средства для лечения или предупреждения ВИЧ-инфекций или инфекций, вызываемых родственным вирусом, или СПИДа.1. The use of an inhibitor of COX-2, which inhibits the enzymatic activity of COX-2, or its derivative, or a pharmaceutically acceptable salt for the manufacture of a medicament for the treatment or prevention of HIV infections or infections caused by a related virus or AIDS. 2. Применение по п.1, где указанное лекарственное средство предназначено для введения человеку, домашним питомцам или сельскохозяйственным животным.2. The use according to claim 1, where the specified drug is intended for administration to humans, pets or farm animals. 3. Применение по п.1 или 2, где указанный ингибитор СОХ-2 имеет отношение селективностей СОХ-1:СОХ-2, составляющее >5, предпочтительно >50 в соответствии с анализом WHMA при IC80.3. The use according to claim 1 or 2, wherein said COX-2 inhibitor has a COX-1: COX-2 selectivity ratio of> 5, preferably> 50, according to the WHMA assay at IC 80 . 4. Применение по любому из пп.1-3, где указанным ингибитором СОХ-2 является простой эфир метансульфонамида, тиоэфир метансульфонамида или диарилгетероцикл.4. The use according to any one of claims 1 to 3, wherein said COX-2 inhibitor is methanesulfonamide ether, methanesulfonamide thioether or diarylheterocycle. 5. Применение по любому из пп.1-4, где указанным ингибитором СОХ-2 является соединение общей формулы А5. The use according to any one of claims 1 to 4, wherein said COX-2 inhibitor is a compound of general formula A
Figure 00000001
Figure 00000001
где Х представляет атом кислорода или серы или алкильную группу, предпочтительно группу -СН2-;where X represents an oxygen or sulfur atom or an alkyl group, preferably a —CH 2 - group; R1 представляет циклоалкильную или арильную группу, которые могут быть, но необязательно, замещены одной или более группами или атомами, предпочтительно одним или более атомами галогена; иR 1 represents a cycloalkyl or aryl group which may be, but is not necessarily, substituted by one or more groups or atoms, preferably one or more halogen atoms; and R2, R3, R4 и R5 независимо представляют атом водорода, нитро- или ацильную группу или алкильную группу, которая может быть, но необязательно, замещена одной или более группами или атомами, либо, альтернативно, R2 и R3, R3 и R4, или R4 и R5, взятые вместе с атомом углерода, с которым они связаны, образуют циклопентаноновую группу,R 2 , R 3 , R 4 and R 5 independently represent a hydrogen atom, a nitro or acyl group or an alkyl group which may, but is not necessarily, substituted by one or more groups or atoms, or, alternatively, R 2 and R 3 , R 3 and R 4 , or R 4 and R 5 , taken together with the carbon atom to which they are attached, form a cyclopentanone group, или его производное, или фармацевтически приемлемая соль.or a derivative thereof, or a pharmaceutically acceptable salt.
6. Применение по п.5, где Х представляет атом кислорода.6. The use according to claim 5, where X represents an oxygen atom. 7. Применение по п.5 или 6, где R1 представляет арильную группу или арильную группу, замещенную одним или несколькими атомами фтора, или циклоалкильную группу.7. The use according to claim 5 or 6, where R 1 represents an aryl group or an aryl group substituted by one or more fluorine atoms, or a cycloalkyl group. 8. Применение по любому из пп.5-7, где R2 и R3 представляют атомы водорода, и R4 представляет группу -NO2 или -СОСН3.8. The use according to any one of claims 5 to 7, where R 2 and R 3 represent hydrogen atoms, and R 4 represents a group —NO 2 or —COCH 3 . 9. Применение по любому из пп.5-8, где R2 представляет атом водорода, и R3 и R4, взятые вместе, образуют циклопентаноновую группу.9. The use according to any one of claims 5 to 8, where R 2 represents a hydrogen atom, and R 3 and R 4 taken together form a cyclopentanone group. 10. Применение по любому из пп.5-9, где указанными ингибиторами СОХ-2 являются флозулид, NS-398, нимезулид, FK 3311 и L-745337.10. The use according to any one of claims 5 to 9, wherein said COX-2 inhibitors are flosulide, NS-398, nimesulide, FK 3311 and L-745337. 11. Применение по любому из пп.1-4, где указанным ингибитором СОХ-2 является соединение общей формулы В11. The use according to any one of claims 1 to 4, wherein said COX-2 inhibitor is a compound of general formula B
Figure 00000002
Figure 00000002
где Y представляет циклическую группу, предпочтительно оксазолильную, изоксазолильную, тиенильную, дигидрофурильную, фурильную, пирролильную, пиразолильную, тиазолильную, имидазолильную, изотиазолильную, циклопентенильную, фенильную и пиридильную группу;where Y represents a cyclic group, preferably an oxazolyl, isoxazolyl, thienyl, dihydrofuryl, furyl, pyrrolyl, pyrazolyl, thiazolyl, imidazolyl, isothiazolyl, cyclopentenyl, phenyl and pyridyl group; n = 0 - 3;n is 0 to 3; m = 0 - 4;m is 0 to 4; R6 представляет кетоциклильную, циклоалкильную или арильную группу, которая может быть, но необязательно, замещена одной или более группами или атомами, предпочтительно одним или более атомами галогена;R 6 represents a ketocyclyl, cycloalkyl or aryl group, which may be, but is not necessarily, substituted by one or more groups or atoms, preferably one or more halogen atoms; R7 каждый независимо представляет заместитель, которым может быть любая функциональная группа, предпочтительно, атом водорода или галогена или алкильная группа, которая может быть замещена одной или более группами или атомами;R 7 each independently represents a substituent, which may be any functional group, preferably a hydrogen or halogen atom or an alkyl group which may be substituted by one or more groups or atoms; R8 представляет алкильную группу;R 8 represents an alkyl group; R9 представляет атом галогена;R 9 represents a halogen atom; R10 представляет атом водорода или алкильную группу, необязательно замещенную одной или более группами или атомами, предпочтительно, ацильной группой,R 10 represents a hydrogen atom or an alkyl group optionally substituted with one or more groups or atoms, preferably an acyl group, или его производное, или фармацевтически приемлемая соль.or a derivative thereof, or a pharmaceutically acceptable salt.
12. Применение по п.11, где R8 представляет NH2- или -СН3.12. The use according to claim 11, where R 8 represents NH 2 - or-CH 3 . 13. Применение по п.11 или 12, где Y представляет пиразолильную, фурильную или тиенильную группу.13. The use according to claim 11 or 12, where Y represents a pyrazolyl, furyl or thienyl group. 14. Применение по любому из пп.11-13, где R6 представляет арильную группу, необязательно замещенную одним или более атомами фтора.14. The use according to any one of claims 11 to 13, wherein R 6 is an aryl group optionally substituted with one or more fluorine atoms. 15. Применение по любому из пп.11-14, где n = 1 или 2.15. The use according to any one of paragraphs.11-14, where n = 1 or 2. 16. Применение по любому из пп.11-15, где R7 предпочтительно представляет атом брома, ацильную группу или замещенную алкильную группу.16. The use according to any one of claims 11 to 15, where R 7 preferably represents a bromine atom, an acyl group or a substituted alkyl group. 17. Применение по любому из пп.11-16, где указанным ингибитором СОХ-2 является целекоксиб, рофекоксиб, DuP-697, SC-58125, DFP, DFU, CGP 28232 или трициклический MF.17. The use according to any one of claims 11-16, wherein said COX-2 inhibitor is celecoxib, rofecoxib, DuP-697, SC-58125, DFP, DFU, CGP 28232 or tricyclic MF. 18. Применение по любому из пп.1-4, где указанным ингибитором СОХ-2 является производное нестероидного противовоспалительного лекарственного средства (НСПВС).18. The use according to any one of claims 1 to 4, wherein said COX-2 inhibitor is a derivative of a non-steroidal anti-inflammatory drug (NSAID). 19. Применение по любому из пп.1-18, где указанным ингибитором СОХ-2 является диизопропилфторфосфат, L-745337, рофекоксиб, NS398, SC58125, этодолак, мелоксикам, целекоксиб или нимезулид.19. The use according to any one of claims 1 to 18, wherein said COX-2 inhibitor is diisopropyl fluorophosphate, L-745337, rofecoxib, NS398, SC58125, etodolac, meloxicam, celecoxib or nimesulide. 20. Применение по п.19, где указанным ингибитором СОХ-2 является рофекоксиб.20. The use according to claim 19, where the specified COX-2 inhibitor is rofecoxib. 21. Применение по п.19, где указанным ингибитором СОХ-2 является целекоксиб.21. The use according to claim 19, where the specified COX-2 inhibitor is celecoxib. 22. Применение по п.19, где указанным ингибитором СОХ-2 является мелоксикам.22. The use according to claim 19, where the specified COX-2 inhibitor is meloxicam. 23. Фармацевтическая композиция, включающая ингибитор СОХ-2, который ингибирует ферментативную активность СОХ-2, или его производное, или фармацевтически приемлемую соль, определенные в любом из пп.1-22, и фармацевтически приемлемый разбавитель, носитель или наполнитель для использования в качестве лекарственного средства, предпочтительно для лечения или предупреждения расстройства, определенного в п.1 или 2.23. A pharmaceutical composition comprising a COX-2 inhibitor that inhibits the enzymatic activity of COX-2, or a derivative thereof, or a pharmaceutically acceptable salt, as defined in any one of claims 1 to 22, and a pharmaceutically acceptable diluent, carrier or excipient for use as a medicament, preferably for treating or preventing a disorder as defined in claim 1 or 2. 24. Фармацевтическая композиция по п.23, которая дополнительно содержит один или более дополнительных ингибиторов СОХ-2, его производные или фармацевтически приемлемые соли и/или один или более дополнительных активных ингредиентов.24. The pharmaceutical composition according to claim 23, which further comprises one or more additional COX-2 inhibitors, its derivatives or pharmaceutically acceptable salts and / or one or more additional active ingredients. 25. Продукт, включающий ингибитор СОХ-2, который ингибирует ферментативную активность СОХ-2, или его производное или фармацевтически приемлемую соль, определенные в любом из пп.1-22, и один или более дополнительных ингибиторов СОХ-2, его производные или фармацевтически приемлемые соли и/или один или несколько дополнительных активных ингредиентов в виде комбинированного препарата для одновременного, раздельного или последовательного применения для лечения или предупреждения расстройства, определенного в п.1 или 2.25. A product comprising a COX-2 inhibitor that inhibits the enzymatic activity of COX-2, or a derivative or pharmaceutically acceptable salt thereof, as defined in any one of claims 1 to 22, and one or more additional COX-2 inhibitors, its derivatives or pharmaceutically acceptable salts and / or one or more additional active ingredients in the form of a combined preparation for simultaneous, separate or sequential use for the treatment or prevention of the disorder defined in claim 1 or 2. 26. Применение фармацевтической композиции, определенной в п.23 или 24, для изготовления лекарственного средства для лечения или предупреждения расстройства, определенного в п.1 или 2.26. The use of a pharmaceutical composition as defined in claim 23 or 24 for the manufacture of a medicament for the treatment or prevention of a disorder as defined in claim 1 or 2. 27. Способ лечения или предупреждения расстройства определенного в п.1 или 2 у человека или животного, где указанному человеку или животному вводят ингибитор СОХ-2, который ингибирует ферментативную активность СОХ-2, или его производное, или фармацевтически приемлемую соль, определенные в любом из пп.1-22, или вводят фармацевтическую композицию, определенную в п.23 или 24.27. A method of treating or preventing a disorder as defined in claim 1 or 2 in a human or animal, wherein a COX-2 inhibitor that inhibits the enzymatic activity of COX-2, or a derivative thereof, or a pharmaceutically acceptable salt, as defined in any from claims 1 to 22, or enter the pharmaceutical composition defined in paragraph 23 or 24.
RU2003104981/15A 2000-07-20 2001-07-20 Using cox-2 inhibitors for prophylaxis of immunodeficiency RU2303452C2 (en)

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GB0017908A GB0017908D0 (en) 2000-07-20 2000-07-20 Method
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GB0109648A GB0109648D0 (en) 2001-04-19 2001-04-19 Method
GB0109648.6 2001-04-19

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