EA202092671A1 - Оптимизированная комбинированная терапия и ее применение для лечения злокачественной опухоли и аутоиммунного заболевания - Google Patents

Оптимизированная комбинированная терапия и ее применение для лечения злокачественной опухоли и аутоиммунного заболевания

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EA202092671A1
EA202092671A1 EA202092671A EA202092671A EA202092671A1 EA 202092671 A1 EA202092671 A1 EA 202092671A1 EA 202092671 A EA202092671 A EA 202092671A EA 202092671 A EA202092671 A EA 202092671A EA 202092671 A1 EA202092671 A1 EA 202092671A1
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compounds
drug
combination therapy
autoimmune disease
disorder
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EA202092671A
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English (en)
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Вэй ХЭ
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Чжэцзян Дтрм Байофарма Ко., Лтд.
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Publication of EA202092671A1 publication Critical patent/EA202092671A1/ru

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    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • 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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    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Представлены серии новых мультизамещенных фтором пиразолопиримидиновых соединений или солей. Соединения представляют собой ингибиторы тирозинкиназы Брутона (ВТК). Соединения обладают лучшими избирательностью ингибирования киназы и фармакокинетическими свойствами. Представлен также способ получения соединений. Представлена также комбинированная терапия, включающая в себя соединения в комбинации с композицией другого направленного лекарственного средства или с другим лекарственным средством. Оптимизированная комбинированная терапия оказывает кооперативный эффект, подавляя существующую опухоль лучше, чем однонаправленное лекарственное средство, и вызывает полное исчезновение определенных опухолей. Оптимизированная комбинированная терапия излечивает устойчивость опухоли к лекарственному средству и рецидив злокачественной опухоли лучше, чем однонаправленное лекарственное средство, и цикл лечения является более коротким. Настоящее изобретение также относится к комбинированному соединению и фармацевтическому препарату, где указанное комбинированное соединение действует в качестве активного ингредиента, где указанный фармацевтический препарат является более безопасным в более низких дозах и обладает эффективностью кооперативного эффекта. Представлен также способ применения соединений и их получения для лечения и подавления аутоиммунного заболевания или нарушения, гетерогенного аутоиммунного заболевания или нарушения, воспалительного заболевания, злокачественной опухоли или нарушения.
EA202092671A 2015-03-19 2016-03-18 Оптимизированная комбинированная терапия и ее применение для лечения злокачественной опухоли и аутоиммунного заболевания EA202092671A1 (ru)

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CN201510119944.5A CN106146508A (zh) 2015-03-19 2015-03-19 优化的联合用药及其治疗癌症和自身免疫疾病的用途

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EA202092671A EA202092671A1 (ru) 2015-03-19 2016-03-18 Оптимизированная комбинированная терапия и ее применение для лечения злокачественной опухоли и аутоиммунного заболевания

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EP (1) EP3272752A4 (ru)
JP (2) JP7012534B2 (ru)
KR (2) KR102428387B1 (ru)
CN (4) CN106146508A (ru)
AU (2) AU2016232923B2 (ru)
BR (1) BR112017019790B1 (ru)
CA (2) CA2980016C (ru)
EA (2) EA037058B1 (ru)
IL (1) IL254435B1 (ru)
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