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RU2003127391A - Лечение рака - Google Patents

Лечение рака Download PDF

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Publication number
RU2003127391A
RU2003127391A RU2003127391/15A RU2003127391A RU2003127391A RU 2003127391 A RU2003127391 A RU 2003127391A RU 2003127391/15 A RU2003127391/15 A RU 2003127391/15A RU 2003127391 A RU2003127391 A RU 2003127391A RU 2003127391 A RU2003127391 A RU 2003127391A
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RU
Russia
Prior art keywords
inhibitor
pharmaceutical composition
rapamycin
compound
formula
Prior art date
Application number
RU2003127391/15A
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English (en)
Other versions
RU2322981C2 (ru
Inventor
Хейди ЛАНЕ (CH)
Хейди ЛАНЕ
Теренс О`РЕЙЛЛИ (CH)
Теренс О`РЕЙЛЛИ
Джинетта Марджори ВУД (CH)
Джинетта Марджори ВУД
Original Assignee
Новартис АГ (CH)
Новартис Аг
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26245731&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2003127391(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0104072A external-priority patent/GB0104072D0/en
Priority claimed from GB0124957A external-priority patent/GB0124957D0/en
Application filed by Новартис АГ (CH), Новартис Аг filed Critical Новартис АГ (CH)
Publication of RU2003127391A publication Critical patent/RU2003127391A/ru
Application granted granted Critical
Publication of RU2322981C2 publication Critical patent/RU2322981C2/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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Claims (10)

1. Применение соединения формулы I
Figure 00000001
где r1 обозначает СН3 или С3-С6алкинил,
R2 обозначает Н или –СН2-СН2-ОН, и
Х обозначает =О, (Н, Н) или (Н, ОН)
при условии, что R2 не обозначает Н, если Х обозначает=0 и r1 обозначает СН3, для приготовления фармацевтической композиции, предназначенной для лечения плотных опухолей.
2. Применение соединения формулы I по п.1 для приготовления фармацевтической композиции, предназначенной для лечения инвазии плотных опухолей или симптомов, связанных с ростом такой опухоли.
3. Применение рапамицина или производного рапамицина для приготовления фармацевтической композиции, предназначенной для ингибирования или контроля нарушенной регуляции ангиогенеза.
4. Фармацевтическая композиция, предназначенная для лечения плотных опухолей, содержащая соединение формулы I по п.1 в сочетании с одним или несколькими фармацевтически приемлемыми разбавителями или носителями.
5. Фармацевтическая композиция, предназначенная для ингибирования или контроля нарушенной регуляции ангиогенеза, содержащая рапамицин или производное рапамицина в сочетании с одним или несколькими фармацевтически приемлемыми разбавителями или носителями.
6. Фармацевтическая композиция, содержащая а) соединение формулы I по п.1 и б) коагент, представляющий собой химиотерапевтический агент.
7. Фармацевтическая композиция по п.6, где коагент выбирают из группы, включающей
I. ингибитор ароматазы,
II. антиэстроген, антиандроген или агонист гонадорелина,
III. ингибитор топоизомеразы I или ингибитор топоизомеразы II,
IV. агент, обладающий активностью в отношении микротрубочек, алкилирующий агент, антинеопластический антиметаболит или содержащее платину соединение,
V. соединение, обладающее способностью воздействовать на/понижать активность протеин- или липидкиназы, или протеин- или липидфосфатазы, другое антиангиогенное соединение или соединение, индуцирующее процессы дифференцировки клеток,
VI. антагонист рецептора брадикинина 1 или ангиотензина II,
VII. ингибитор циклооксигеназы, бисфосфонат, ингибитор гистон-деацетилазы, ингибитор гепараназы, модификатор биологической реакции, ингибитор убиквитина, или ингибитор, блокирующий антиапоптозные пути,
VIII. ингибитор онкогенных изоформ Ras,
IX. ингибитор теломеразы и
X. ингибитор протеазы, ингибитор матриксной металлопротеазы, ингибитор метионинаминопептидазы или ингибитор протеосомы.
8. Фармацевтическая композиция, содержащая а) рапамицин или производное рапамицина и б) коагент, представляющий собой химиотерапевтический агент, выбранный из агентов, перечисленных в разделах (I.) и (V)-(X.) по п.7.
9. Способ лечения плотных опухолей у пациента, нуждающегося в таком лечении, заключающийся в том, что пациенту вводят терапевтически эффективное количество соединения формулы I по п.1 необязательно одновременно или последовательно в сочетании с химиотерапевтическим агентом.
10. Способ ингибирования или контроля нарушенной регуляции ангиогенеза у пациента, нуждающегося в таком лечении, заключающийся в том, что пациенту вводят терапевтически эффективное количество рапамицина или производного рапамицина необязательно одновременно или последовательно с введением химиотерапевтического агента.
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