RU98119312A - APPLICATION OF DERIVATIVES OF RAPAMYCIN IN VASOPATHIES AND XENOTRANSPLANTATION - Google Patents

APPLICATION OF DERIVATIVES OF RAPAMYCIN IN VASOPATHIES AND XENOTRANSPLANTATION

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Publication number
RU98119312A
RU98119312A RU98119312/14A RU98119312A RU98119312A RU 98119312 A RU98119312 A RU 98119312A RU 98119312/14 A RU98119312/14 A RU 98119312/14A RU 98119312 A RU98119312 A RU 98119312A RU 98119312 A RU98119312 A RU 98119312A
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RU
Russia
Prior art keywords
recipient
formula
compound
chronic rejection
tissue
Prior art date
Application number
RU98119312/14A
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Russian (ru)
Other versions
RU2214247C2 (en
Inventor
Шулер Вальтер
Шуурман Хендрик
Векбеккер Гизберг
Цервес Ханс-Гюнтер
Original Assignee
Новартис Аг
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Publication date
Priority claimed from GBGB9606452.2A external-priority patent/GB9606452D0/en
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU98119312A publication Critical patent/RU98119312A/en
Application granted granted Critical
Publication of RU2214247C2 publication Critical patent/RU2214247C2/en

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Claims (10)

1. Применение соединения формулы I
Figure 00000001

где X обозначает (Н,Н) или О;
Y обозначает (Н,ОН) или О;
R1 и R2 независимо друг от друга выбирают из группы, включающей Н, алкил, арилалкил, гидроксиалкил, дигидроксиалкил, гидроксиалкоксикарбонилалкил, гидроксиалкиларилалкил, дигидроксиалкиларилалкил, ацилоксиалкил, аминоалкил, алкиламиноалкил, алкоксикарбониламиноалкил, ациламиноалкил, арилсульфонамидоалкил, аллил, дигидроксиалкилаллил, диоксоланилаллил, диалкилдиоксоланилалкил, ди(алкоксикарбон-ил)триазолилалкил и гидроксиалкоксиалкил, где "алк-" или "алкил" обозначает разветвленный или линейный С1-C6алкил, "арил" обозначает фенил или толил и "ацил" обозначает радикал, являющийся производным карбоновой кислоты;
R4 обозначает метил или R4 и R1 вместе образуют C2-C6алкил;
при условии, что R1 и R2 вместе не могут обозначать Н, а гидроксиалкоксиалкил не обозначает гидроксиалкоксиметил, при изготовлении фармацевтической композиции, предназначенной для предупреждения или лечения пролиферации и утолщения новой внутренней оболочки.
1. The use of the compounds of formula I
Figure 00000001

where X denotes (H, H) or O;
Y represents (H, OH) or O;
R 1 and R 2 are independently selected from the group consisting of H, alkyl, arylalkyl, hydroxyalkyl, digidroksialkil, gidroksialkoksikarbonilalkil, gidroksialkilarilalkil, digidroksialkilarilalkil, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, arilsulfonamidoalkil, allyl, digidroksialkilallil, dioksolanilallil, dialkildioksolanilalkil, di (alkoxycarbonyl) triazolylalkyl and hydroxyalkoxyalkyl, where “alk-” or “alkyl” means branched or linear C 1 -C 6 alkyl, “aryl” means phenyl or tolyl and "acyl" means a radical derived from a carboxylic acid;
R 4 is methyl or R 4 and R 1 together form a C 2 -C 6 alkyl;
provided that R 1 and R 2 together cannot designate H, and hydroxyalkoxyalkyl does not mean hydroxyalkoxymethyl, in the manufacture of a pharmaceutical composition intended to prevent or treat the proliferation and thickening of a new inner shell.
2. Применение соединения формулы I по п. 1 при изготовлении фармацевтической композиции, предназначенной для предупреждения или уменьшения симптомов хронического отторжения трансплантированного органа или ткани у реципиента. 2. The use of the compounds of formula I according to claim 1 in the manufacture of a pharmaceutical composition intended to prevent or reduce the symptoms of chronic rejection of a transplanted organ or tissue in a recipient. 3. Применение соединения формулы I по п. 1 при изготовлении фармацевтической композиции, предназначенной для предупреждения или лечения рестеноза и/или окклюзий сосуда, являющихся результатом повреждения сосуда. 3. The use of the compound of the formula I according to claim 1 in the manufacture of a pharmaceutical composition for preventing or treating restenosis and / or occlusions of a vessel resulting from damage to the vessel. 4. Применение соединения формулы I по п. 1 при изготовлении фармацевтической композиции, предназначенной для предупреждения или уменьшения острого или хронического отторжения у реципиента трансплантата органа или ткани, представляющего собой ксенотрансплантат. 4. The use of the compound of formula I according to claim 1 in the manufacture of a pharmaceutical composition intended to prevent or reduce acute or chronic rejection in a recipient of an organ or tissue transplant, which is a xenograft. 5. Применение соединения формулы I по п. 1 для предупреждения или лечения пролиферации и утолщения новой внутренней оболочки, рестеноза и/или окклюзий сосуда, являющихся результатом повреждения сосуда, или для предупреждения или уменьшения симптомов хронического отторжения трансплантированного органа или ткани у реципиента, острого или хронического отторжения у реципиента трансплантата органа или ткани, представляющего собой ксенотрансплантат. 5. The use of a compound of formula I in accordance with claim 1 for preventing or treating proliferation and thickening of the inner lining, restenosis and / or occlusions of a vessel resulting from damage to the vessel, or to prevent or reduce symptoms of chronic rejection of a transplanted organ or tissue in a recipient, acute or chronic rejection in the recipient of an organ or tissue transplant that is a xenograft. 6. Фармацевтическая композиция, предназначенная для предупреждения или лечения пролиферации и утолщения новой внутренней оболочки, рестеноза и/или окклюзий сосудов, являющихся результатом повреждения сосуда, или для предупреждения или уменьшения симптомов хронического отторжения трансплантированного органа или ткани у реципиента, острого или хронического отторжения у реципиента трансплантата органа или ткани, представляющего собой ксенотрансплантат, включающая соединение формулы I по п. 1 вместе с одним или с несколькими фармацевтически приемлемыми растворителями или носителями. 6. Pharmaceutical composition intended to prevent or treat the proliferation and thickening of the new inner lining, restenosis and / or occlusions of vessels resulting from vessel damage, or to prevent or reduce the symptoms of chronic rejection of a transplanted organ or tissue in a recipient, acute or chronic rejection in a recipient a graft of an organ or tissue representing a xenograft comprising a compound of formula I in accordance with claim 1, together with one or more pharmaceutics Eski acceptable diluents or carriers. 7. Способ предупреждения или лечения пролиферации и утолщения новой внутренней оболочки, рестеноза и/или окклюзий сосуда, являющихся результатом повреждения сосуда, включающий стадию введения реципиенту терапевтически эффективного количества соединения формулы I по п. 1. 7. A method of preventing or treating proliferation and thickening of the new inner lining, restenosis and / or occlusions of the vessel resulting from damage to the vessel, including the stage of administering to the recipient a therapeutically effective amount of the compound of formula I in claim 1. 8. Способ предупреждения или уменьшения симптомов хронического отторжения трансплантированного органа или ткани у реципиента, острого или хронического отторжения у реципиента трансплантата органа или ткани, представляющего собой ксенотрансплантат, включающий стадию введения реципиенту терапевтически эффективного количества соединения формулы I по п. 1. 8. A method of preventing or reducing the symptoms of chronic rejection of a transplanted organ or tissue in a recipient, acute or chronic rejection in a recipient of an organ or tissue transplant, which is a xenograft, comprising the step of administering to the recipient a therapeutically effective amount of the compound of formula I in claim 1. 9. Применение по любому из пп. 1-5, где соединение формулы I представляет собой 40-O-(2-гидрокси)этилрапамицин. 9. The use according to any one of paragraphs. 1-5, where the compound of formula I is a 40-O- (2-hydroxy) ethyl rapamycin. 10. Фармацевтическая композиция по п. 6, где соединение формулы I представляет собой 40-O-(2-гидрокси)этилрапамицин. 10. The pharmaceutical composition of claim 6, wherein the compound of formula I is 40-O- (2-hydroxy) ethyl rapamycin.
RU98119312/14A 1996-03-27 1997-03-26 Application of rapamycin derivatives in vasopathy and xenotransplantation RU2214247C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9606452.2A GB9606452D0 (en) 1996-03-27 1996-03-27 Organic compounds
GB9606452.2 1996-03-27

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JP (2) JP2000507226A (en)
KR (2) KR20070083654A (en)
CN (1) CN1124135C (en)
AT (1) ATE224194T1 (en)
AU (1) AU716514B2 (en)
BR (1) BR9708358A (en)
CA (1) CA2247275C (en)
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CZ (1) CZ292483B6 (en)
DE (1) DE69715611T2 (en)
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ES (2) ES2184078T3 (en)
GB (1) GB9606452D0 (en)
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HU (1) HU226422B1 (en)
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TR (1) TR199801919T2 (en)
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