RU2346693C2 - Myocardial perfusion imaging using adenosine receptor agonists - Google Patents

Myocardial perfusion imaging using adenosine receptor agonists Download PDF

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RU2346693C2
RU2346693C2 RU2006127167/15A RU2006127167A RU2346693C2 RU 2346693 C2 RU2346693 C2 RU 2346693C2 RU 2006127167/15 A RU2006127167/15 A RU 2006127167/15A RU 2006127167 A RU2006127167 A RU 2006127167A RU 2346693 C2 RU2346693 C2 RU 2346693C2
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pharmaceutical composition
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buffer
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RU2006127167/15A
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RU2006127167A (en
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Луис БЕЛАРДИНЕЛЛИ (US)
Луис Белардинелли
Митчелл РОСНЕР (US)
Митчелл РОСНЕР
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Си Ви Терапьютикс, Инк.
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Abstract

FIELD: medicine; cardiology.
SUBSTANCE: pharmaceutical composition contains agonist A2A receptor and at least, one base oil, and, at least, one cosolvent.
EFFECT: fast and maximum coronary vasodilatation in mammals without invoking related peripheral vasodilatation, elimination of multiple introduction.
26 cl, 8 ex, 3 tbl, 18 dwg

Description

Текст описания приведен в факсимильном виде.

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The text of the description is given in facsimile form.
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Claims (26)

1. Фармацевтическая композиция, содержащая
а) агонист А2A рецептора CVT-3146, представляющий собой (1-{9-[(4S,2R,3R,5R)-3,4-дигидрокси-5-(гидроксиметил)оксолан-2-ил]-6-аминопурин-2-ил} пиразол-4-ил)-N-метилкарбоксамид, имеющий формулу
Figure 00000075

b) по меньшей мере один жидкий носитель, выбранный из группы, состоящей из воды, дистиллированной воды, деионизированной воды, физиологического раствора, буфера и их комбинаций, и
c) по меньшей мере один сорастворитель, включающий количество метилбороновой кислоты в растворе или количество боратного буфера,
и где величина рН указанной фармацевтической композиции составляет от приблизительно 8,5 до приблизительно 10.1. A pharmaceutical composition comprising
a) an agonist A 2A of the CVT-3146 receptor, which is (1- {9 - [(4S, 2R, 3R, 5R) -3,4-dihydroxy-5- (hydroxymethyl) oxolan-2-yl] -6-aminopurine -2-yl} pyrazol-4-yl) -N-methylcarboxamide having the formula
Figure 00000075

b) at least one liquid carrier selected from the group consisting of water, distilled water, deionized water, saline, buffer, and combinations thereof, and
c) at least one co-solvent, including the amount of methylboronic acid in the solution or the amount of borate buffer,
and where the pH of said pharmaceutical composition is from about 8.5 to about 10. 2. Фармацевтическая композиция по п.1, где величина рН составляет от около 9,1 до около 9,4.2. The pharmaceutical composition according to claim 1, where the pH is from about 9.1 to about 9.4. 3. Фармацевтическая композиция по п.2, где сорастворитель включает количество метилбороновой кислоты в растворе.3. The pharmaceutical composition according to claim 2, where the co-solvent includes the amount of methylboronic acid in the solution. 4. Фармацевтическая композиция по п.3, где жидкий носитель включает, по меньшей мере, один буфер.4. The pharmaceutical composition according to claim 3, where the liquid carrier includes at least one buffer. 5. Фармацевтическая композиция по п.4 дополнительно включающая приблизительно 0,55% (вес:объем) хлорида натрия и приблизительно 50 ммоль бикарбоната натрия.5. The pharmaceutical composition according to claim 4 further comprising approximately 0.55% (weight: volume) of sodium chloride and approximately 50 mmol of sodium bicarbonate. 6. Фармацевтическая композиция по п.4, в которой CVT-3146 присутствует в количестве, варьирующем от приблизительно 50 до приблизительно 250 мкг/мл, и метилбороновая кислота присутствует в количестве от приблизительно 0,4 до приблизительно 0,6% (вес:объем).6. The pharmaceutical composition according to claim 4, in which CVT-3146 is present in an amount ranging from about 50 to about 250 μg / ml, and methylboronic acid is present in an amount from about 0.4 to about 0.6% (weight: volume ) 7. Фармацевтическая композиция по п.6, в которой количество метилбороновой кислоты в растворе составляет приблизительно 0,5% (вес:объем) метилбороновой кислоты.7. The pharmaceutical composition according to claim 6, in which the amount of methylboronic acid in the solution is approximately 0.5% (weight: volume) of methylboronic acid. 8. Фармацевтическая композиция по п.7, где CVT-3146 присутствует в количестве от приблизительно 50 до приблизительно 250 мкг/мл.8. The pharmaceutical composition according to claim 7, where CVT-3146 is present in an amount of from about 50 to about 250 μg / ml. 9. Фармацевтическая композиция по п.2 в которой сорастворитель содержит боратный буфер.9. The pharmaceutical composition according to claim 2, wherein the co-solvent comprises borate buffer. 10. Фармацевтическая композиция по п.9, где величина рН составляет приблизительно 9,3 и композиция дополнительно включает буфер.10. The pharmaceutical composition according to claim 9, where the pH is approximately 9.3 and the composition further comprises a buffer. 11. Фармацевтическая композиция, содержащая
а) агонист А2A рецептора CVT-3146, представляющий собой (1-{9-[(4S,2R,3R,5R)-3,4-дигидрокси-5-(гидроксиметил)оксолан-2-ил]-6-аминопурин-2-ил}пиразол-4-ил)-N-метилкарбоксамид, имеющий формулу
Figure 00000076

b) по меньшей мере, один жидкий носитель, выбранный из группы, состоящей из воды, дистиллированной воды, деионизированной воды, физиологического раствора, буфера и их комбинаций, и
c) по меньшей мере, один сорастворитель, включающий пропиленгликоль или полиэтиленгликоль,
и где величина рН указанной фармацевтической композиции составляет от приблизительно 6 до приблизительно 8.11. A pharmaceutical composition comprising
a) an agonist A 2A of the CVT-3146 receptor, which is (1- {9 - [(4S, 2R, 3R, 5R) -3,4-dihydroxy-5- (hydroxymethyl) oxolan-2-yl] -6-aminopurine -2-yl} pyrazol-4-yl) -N-methylcarboxamide having the formula
Figure 00000076

b) at least one liquid carrier selected from the group consisting of water, distilled water, deionized water, saline, buffer, and combinations thereof, and
c) at least one cosolvent, including propylene glycol or polyethylene glycol,
and where the pH of said pharmaceutical composition is from about 6 to about 8. 12. Фармацевтическая композиция по п.11, в которой сорастворитель включает пропиленгликоль.12. The pharmaceutical composition according to claim 11, in which the co-solvent includes propylene glycol. 13. Фармацевтическая композиция по п.12, в которой сорастворителем является пропиленгликоль и пропиленгликоль присутствует в количестве от приблизительно 5 до приблизительно 25% (вес: объем).13. The pharmaceutical composition according to item 12, in which the co-solvent is propylene glycol and propylene glycol is present in an amount of from about 5 to about 25% (weight: volume). 14. Фармацевтическая композиция по п.13, в которой пропиленгликоль присутствует в количестве от около 8 до около 20% (вес: объем).14. The pharmaceutical composition of claim 13, wherein the propylene glycol is present in an amount of from about 8 to about 20% (weight: volume). 15. Фармацевтическая композиция по п.11, в которой указанная композиция дополнительно содержит ЭДТА.15. The pharmaceutical composition according to claim 11, in which the composition further comprises EDTA. 16. Фармацевтическая композиция по п.15 в которой CVT-3146 присутствует в количестве от приблизительно 50 до приблизительно 150 мкг/мл.16. The pharmaceutical composition of claim 15, wherein CVT-3146 is present in an amount of from about 50 to about 150 μg / ml. 17. Способ осуществления расширения коронарных сосудов без существенного расширения периферических сосудов у человека, включающий введение человеку фармацевтической композиции по п.1 или 11, где указанная композиция содержит от приблизительно 10 до приблизительно 600 мкг, по меньшей мере, одного агониста А2А рецептора.17. A method for effecting the expansion of coronary vessels without significant expansion of peripheral vessels in humans, comprising administering to a human a pharmaceutical composition according to claim 1 or 11, wherein said composition contains from about 10 to about 600 μg of at least one A 2A receptor agonist. 18. Способ по п.17, в котором указанную фармацевтическую композицию вводят внутривенно (в/в) путем болюса.18. The method according to 17, in which the specified pharmaceutical composition is administered intravenously (iv) by bolus. 19. Способ по п.18, в котором указанную фармацевтическую композицию вводят в течение от приблизительно 10 до приблизительно 20 с.19. The method of claim 18, wherein said pharmaceutical composition is administered for a period of from about 10 to about 20 seconds. 20. Способ визуализации перфузии миокарда у человека, включающий введение человеку радионуклида и композиции по п.1 или 11 или одновременно, или последовательно при исследовании миокарда на выявление областей недостаточного кровотока после введения радионуклида и композиции.20. A method for visualizing myocardial perfusion in humans, comprising administering to a human a radionuclide and a composition according to claim 1 or 11, either simultaneously or sequentially when examining the myocardium to identify areas of insufficient blood flow after administration of the radionuclide and the composition. 21. Способ по п.20, в котором исследование миокарда начинают в пределах около 1 мин после введения радионуклида и композиции.21. The method according to claim 20, in which the myocardial examination is started within about 1 minute after the introduction of the radionuclide and composition. 22. Способ по п.21, в котором агонист А2А рецептора вызывает увеличение коронарного кровотока по меньшей мере в 2,5 раза и такое увеличение кровотока достигается меньше чем приблизительно за 5 мин.22. The method according to item 21, in which the agonist A 2A receptor causes an increase in coronary blood flow by at least 2.5 times and such an increase in blood flow is achieved in less than about 5 minutes 23. Способ по п.22, в котором CVT-3146 вводят в количестве от приблизительно 10 до приблизительно 600 мкг в виде единственного в/в болюса.23. The method according to item 22, in which CVT-3146 is administered in an amount of from about 10 to about 600 μg as a single IV bolus. 24. Способ по п.23, в котором количество CVT-3146 составляет от приблизительно 100 до приблизительно 500 мкг.24. The method of claim 23, wherein the amount of CVT-3146 is from about 100 to about 500 mcg. 25. Способ по п.24, в котором количество CVT-3146 составляет приблизительно 400 мкг.25. The method according to paragraph 24, in which the amount of CVT-3146 is approximately 400 μg. 26. Способ по п.25, в котором указанную композицию вводят в течение приблизительно от 10 до приблизительно 30 с или меньше. 26. The method according A.25, in which the specified composition is administered for about 10 to about 30 s or less.
RU2006127167/15A 2004-01-27 2004-01-27 Myocardial perfusion imaging using adenosine receptor agonists RU2346693C2 (en)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Gao Z et. al "Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists.", J Pharmacol Exp Ther. 2001 Jul; 298(1):209-18. *
Zhao G et. al. " Comparative profile of vasodilation by CVT-3146, a novel A2A receptor agonist, and adenosine in conscious dogs.", J Pharmacol Exp Ther. 2003 Oct; 307(1): 182-9. Epub 2003 Sep 3. Trochu JN et. al. "Selective A2A adenosine receptor agonist as a coronary vasodilator in conscious dogs: potential for use in myocardial perfusion imaging." J Cardiovasc Pharmacol. 2003 Jan; 41(1): 132-9. *

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