RU2016112266A - Ингибитор PI3K для лечения респираторного заболевания - Google Patents

Ингибитор PI3K для лечения респираторного заболевания Download PDF

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Publication number
RU2016112266A
RU2016112266A RU2016112266A RU2016112266A RU2016112266A RU 2016112266 A RU2016112266 A RU 2016112266A RU 2016112266 A RU2016112266 A RU 2016112266A RU 2016112266 A RU2016112266 A RU 2016112266A RU 2016112266 A RU2016112266 A RU 2016112266A
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compound
use according
infection
respiratory
patient
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RU2016112266A
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Аугустин АМУР
Джули Николь Хэмблин
Эдит ХЭССЕЛ
Дэвид МИЧАЛОВИЧ
Сривидия СРИСКАНТХАРАДЖАХ
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Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
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Priority claimed from GB201318415A external-priority patent/GB201318415D0/en
Priority claimed from GB201319828A external-priority patent/GB201319828D0/en
Priority claimed from GB201409018A external-priority patent/GB201409018D0/en
Application filed by Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед filed Critical Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
Publication of RU2016112266A publication Critical patent/RU2016112266A/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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Communicable Diseases (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (27)

1. Соединение формулы (I)
Figure 00000001
где
R1 представляет собой
Figure 00000002
, и
R2 представляет собой
Figure 00000003
; или
R1 представляет собой
Figure 00000004
, и
R2 представляет собой
Figure 00000005
или его фармацевтически приемлемая соль для применения в лечении или предупреждении респираторной инфекции, лечении поражения дыхательных путей и/или предупреждении повреждения дыхательных путей у пациента.
2. Соединение для применения по п. 1, представляющее собой
6-(1Н-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1H-индазол, или его фармацевтически приемлемая соль.
3. Соединение для применения по п. 1, представляющее собой
N-[5-[4-(5-{[(2R,6S)-2,6-диметил-4-морфолинил]метил}-1,3-оксазол-2-ил)-1Н-индазол-6-ил]-2-(метилокси)-3-пиридинил]метансульфонамид,
или его фармацевтически приемлемая соль.
4. Соединение для применения по п. 1 или 2, представляющее собой гемисукцинат 6-(1Н-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1Н-индазола.
5. Соединение для применения по п. 1 или 3, представляющее собой N-[5-[4-(5-{[(2R,6S)-2,6-диметил-4-морфолинил]метил}-1,3-оксазол-2-ил)-1Н-индазол-6-ил]-2-(метилокси)-3-пиридинил]метансульфонамид.
6. Соединение для применения по п. 1, где применение представляет собой лечение или предупреждение респираторной инфекции.
7. Соединение для применения по п. 6, где респираторная инфекция представляет собой бактериальную инфекцию.
8. Соединение для применения по п. 7, где бактериальная инфекция представляет собой инфекцию S. pneumoniae, Н. influenzae и/или М. catarrhalis.
9. Соединение для применения по п. 7 или 8, где бактериальная инфекция представляет собой ринит, синусит, ларингит, бронхит, бронхиолит, тонзиллит, пневмонию и/или туберкулез.
10. Соединение для применения по п. 1, где пациент имеет первичное расстройство.
11. Соединение для применения по п. 10, где первичное расстройство представляет собой хроническую обструктивную болезнь легких (COPD).
12. Применение соединения по любому из пп. 1-5 или его фармацевтически приемлемой соли для изготовления лекарственного средства для использования в лечении или предупреждении респираторной инфекции, лечении поражения дыхательных путей и/или предупреждении повреждения дыхательных путей у пациента.
13. Способ лечения или предупреждения респираторной инфекции, лечения поражения дыхательных путей и/или предупреждения повреждения дыхательных путей у пациента, включающий введение безопасного и эффективного количества соединения по любому из пп. 1-5 или его фармацевтически приемлемой соли пациенту, нуждающемуся в этом.
RU2016112266A 2013-10-17 2014-10-15 Ингибитор PI3K для лечения респираторного заболевания RU2016112266A (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB201318415A GB201318415D0 (en) 2013-10-17 2013-10-17 Novel use
GB1318415.5 2013-10-17
GB201319828A GB201319828D0 (en) 2013-11-11 2013-11-11 Novel use
GB1319828.8 2013-11-11
GB201409018A GB201409018D0 (en) 2014-05-21 2014-05-21 Novel use
GB1409018.7 2014-05-21
PCT/EP2014/072074 WO2015055691A1 (en) 2013-10-17 2014-10-15 Pi3k inhibitor for treatment of respiratory disease

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Publication Number Publication Date
RU2016112266A true RU2016112266A (ru) 2017-11-20

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US (1) US20160263109A1 (ru)
EP (1) EP3057588A1 (ru)
JP (1) JP6475707B2 (ru)
KR (1) KR20160062178A (ru)
CN (1) CN105611929A (ru)
AU (2) AU2014336251A1 (ru)
CA (1) CA2925064A1 (ru)
RU (1) RU2016112266A (ru)
WO (1) WO2015055691A1 (ru)

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KR102672515B1 (ko) 2022-04-07 2024-06-04 한양대학교 에리카산학협력단 레일 로봇 및 레일 로봇 시스템

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EP3057588A1 (en) 2016-08-24
US20160263109A1 (en) 2016-09-15
AU2014336251A1 (en) 2016-04-14
KR20160062178A (ko) 2016-06-01
CN105611929A (zh) 2016-05-25
CA2925064A1 (en) 2015-04-23
JP2016533367A (ja) 2016-10-27
AU2017225139A1 (en) 2017-10-05
WO2015055691A1 (en) 2015-04-23
JP6475707B2 (ja) 2019-02-27

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