RU2001108500A - APPLICATION OF FUMARIC ACID DERIVATIVES IN TRANSPLANTATION MEDICINE - Google Patents

APPLICATION OF FUMARIC ACID DERIVATIVES IN TRANSPLANTATION MEDICINE

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Publication number
RU2001108500A
RU2001108500A RU2001108500/14A RU2001108500A RU2001108500A RU 2001108500 A RU2001108500 A RU 2001108500A RU 2001108500/14 A RU2001108500/14 A RU 2001108500/14A RU 2001108500 A RU2001108500 A RU 2001108500A RU 2001108500 A RU2001108500 A RU 2001108500A
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Russia
Prior art keywords
use according
fumaric acid
monoalkyl ester
paragraphs
biologically active
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RU2001108500/14A
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Russian (ru)
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RU2210364C2 (en
Inventor
Раджендра Кумар ДЖОШИ
Ханс-Петер ШТРЕБЕЛЬ
Original Assignee
Фумафарм Аг
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Priority claimed from DE19839566A external-priority patent/DE19839566C2/en
Application filed by Фумафарм Аг filed Critical Фумафарм Аг
Publication of RU2001108500A publication Critical patent/RU2001108500A/en
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Publication of RU2210364C2 publication Critical patent/RU2210364C2/en

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Claims (16)

1. Применение одного или нескольких моно-(C1-C5)-алкиловых эфиров фумаровой кислоты в форме соли с одно- или двухвалентными катионами или в форме свободной кислоты, индивидуально или в сочетании с ди-[(C1-C5-алкил] фумаратом, для терапии в отношении отторжения трансплантата (реакции "трансплантат против хозяина") при трансплантациях органов и клеток.1. The use of one or more mono- (C 1 -C 5 ) -alkyl esters of fumaric acid in the form of a salt with mono- or divalent cations or in the form of a free acid, individually or in combination with di - [(C 1 -C 5 - alkyl] fumarate, for treatment of transplant rejection (graft versus host reaction) in organ and cell transplantation. 2. Применение по п. 1, где одна или несколько солей одно- или двухвалентных катионов моноалкиловых эфиров фумаровой кислоты общей формулы
Figure 00000001

применяются, в случае необходимости, в смеси с диалкилфумаратом формулы
Figure 00000002

причем А означает двухвалентный катион из ряда Ca, Mg, Zn или Fe или одновалентный катион из ряда Li, Na или К, и n означает 1 или 2 в зависимости от рода катиона;
и/или один или несколько алкилгидрофумаратов общей формулы
Figure 00000003

в случае необходимости, в смеси с диалкилфумаратом формулы
Figure 00000004

и, в случае необходимости, с обычными фармацевтическими вспомогательными веществами и носителями.2. The use according to claim 1, where one or more salts of mono- or divalent cations of monoalkyl esters of fumaric acid of the general formula
Figure 00000001

are used, if necessary, in a mixture with dialkyl fumarate of the formula
Figure 00000002

moreover, A means a divalent cation from the series Ca, Mg, Zn or Fe or a monovalent cation from the series Li, Na or K, and n means 1 or 2, depending on the kind of cation;
and / or one or more alkyl hydrofumarates of the general formula
Figure 00000003

if necessary, in a mixture with a dialkyl fumarate of the formula
Figure 00000004

and, if necessary, with conventional pharmaceutical excipients and carriers. 3. Применение по п. 1 или 2, отличающееся тем, что применяется кальциевая соль монометилового или моноэтиловый эфир фумаровой кислоты. 3. The use according to claim 1 or 2, characterized in that the calcium salt of monomethyl or monoethyl ester of fumaric acid is used. 4. Применение по п. 1 или 2, отличающееся тем, что применяется одна или несколько солей кальция, магния и/или цинка моноэтилового эфира фумаровой кислоты в смеси с диметилфумаратом. 4. The use according to claim 1 or 2, characterized in that one or more salts of calcium, magnesium and / or zinc monoethyl ester of fumaric acid are used in a mixture with dimethyl fumarate. 5. Применение по любому из пп. 1-4, при котором биологически активные вещества применяются перорально в виде таблеток, микротаблеток, пилюль или гранулятов в капсулах или капсул. 5. The use according to any one of paragraphs. 1-4, in which the biologically active substances are administered orally in the form of tablets, microtablets, pills or granules in capsules or capsules. 6. Применение по п. 5, отличающееся тем, что применяется кальциевая соль моноалкилового эфира фумаровой кислоты в количестве 10 - 300 мг, причем общая масса биологически активных веществ составляет 10-300 мг. 6. The use according to claim 5, characterized in that the calcium salt of fumaric acid monoalkyl ester is used in an amount of 10 to 300 mg, the total weight of biologically active substances being 10-300 mg. 7. Применение по п. 5, отличающееся тем, что применяется 10-290 мас. ч. кальциевой соли моноалкилового эфира фумаровой кислоты и 290-10 мас. ч. диметилфумарата, причем общая масса биологически активных веществ составляет 20-300 мг. 7. The use according to claim 5, characterized in that 10-290 wt. including the calcium salt of monoalkyl ester of fumaric acid and 290-10 wt. including dimethyl fumarate, and the total mass of biologically active substances is 20-300 mg. 8. Применение по п. 5, отличающееся тем, что применяется 10-250 мас. ч. кальциевой соли моноалкилового эфира фумаровой кислоты, 1-50 мас. ч. диметилфумарата и 1-50 мас. ч. цинковой соли моноалкилового эфира фумаровой кислоты, причем общая масса биологически активных веществ составляет 20-300 мг. 8. The use according to claim 5, characterized in that 10-250 wt. including calcium salt of monoalkyl ester of fumaric acid, 1-50 wt. including dimethyl fumarate and 1-50 wt. including zinc salt of monoalkyl ester of fumaric acid, and the total weight of biologically active substances is 20-300 mg. 9. Применение по п. 5, отличающееся тем, что применяется 10-250 мас. ч. кальциевой если моноалкилового эфира фумаровой кислоты, 250-10 мас. ч. диметилфумарата, 1-50 мас. ч. магниевой соли моноалкилового эфира фумаровой кислоты и 1-50 мас. ч. цинковой соли моноалкилового эфира фумаровой кислоты, причем общая масса биологически активных веществ составляет 30-300 мг. 9. The use according to claim 5, characterized in that 10-250 wt. including calcium if monoalkyl ester of fumaric acid, 250-10 wt. including dimethyl fumarate, 1-50 wt. including magnesium salt of monoalkyl ester of fumaric acid and 1-50 wt. including zinc salt of monoalkyl ester of fumaric acid, and the total weight of biologically active substances is 30-300 mg. 10. Применение по любому из пп. 1-9, отличающееся тем, что терапия осуществляется в сочетании с иммуносупрессором. 10. The use according to any one of paragraphs. 1-9, characterized in that the therapy is carried out in combination with an immunosuppressant. 11. Применение по п. 10, отличающееся тем, что осуществляется последовательное или чередующееся введение циклоспорина с введением производных фумаровой кислоты. 11. The use according to claim 10, characterized in that the sequential or alternating administration of cyclosporine with the introduction of fumaric acid derivatives is carried out. 12. Применение по любому из пп. 1-9, отличающееся тем, что терапия осуществляется в сочетании с одним или несколькими препаратами трансплантационной медицины. 12. The use according to any one of paragraphs. 1-9, characterized in that the therapy is carried out in combination with one or more transplant medicine. 13. Применение по любому из пп. 5-12, отличающееся тем, что размер или средний диаметр пилюль или микротаблеток находится в пределах 300-2000 мкм, в особенности в области 500 - 1500 мкм или 1000 мкм. 13. The use according to any one of paragraphs. 5-12, characterized in that the size or average diameter of the pills or microtablets is in the range of 300-2000 microns, in particular in the range of 500 - 1500 microns or 1000 microns. 14. Применение по п. 5, отличающееся тем, что лекарственные средства используются в форме мягких или твердых желатиновых капсул. 14. The use according to claim 5, characterized in that the drugs are used in the form of soft or hard gelatin capsules. 15. Применение по пп. 1-14, отличающееся тем, что разовые дозы лекарственных средств снабжены устойчивым к действию желудочного сока покрытием. 15. The use of PP. 1-14, characterized in that the single dose of the drug is provided with a coating resistant to the action of gastric juice. 16. Применение по любому из пп. 1-4, отличающееся тем, что лекарственные средства используются в форме препаратов для кожного и чрескожного введения, препаратов для парентерального и для ректального введения. 16. The use according to any one of paragraphs. 1-4, characterized in that the drugs are used in the form of preparations for skin and percutaneous administration, preparations for parenteral and rectal administration.
RU2001108500/14A 1998-08-31 1999-08-20 Application of derivatives of fumaric acid in transplantation medicine RU2210364C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19839566A DE19839566C2 (en) 1998-08-31 1998-08-31 Use of fumaric acid derivatives in transplant medicine
DE19839566.3 1998-08-31

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JP (1) JP3553883B2 (en)
CN (1) CN1195511C (en)
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AU (1) AU746958B2 (en)
BG (1) BG64435B1 (en)
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CA (1) CA2322188C (en)
DE (2) DE19839566C2 (en)
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EE (1) EE05025B1 (en)
ES (1) ES2195609T3 (en)
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IL (1) IL138110A0 (en)
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