UA120065C2 - 4,6-ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]-ПІРАЗИНИ ЯК ІНГІБІТОРИ JAK-КІНАЗИ - Google Patents

4,6-ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]-ПІРАЗИНИ ЯК ІНГІБІТОРИ JAK-КІНАЗИ

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Publication number
UA120065C2
UA120065C2 UAA201707008A UAA201707008A UA120065C2 UA 120065 C2 UA120065 C2 UA 120065C2 UA A201707008 A UAA201707008 A UA A201707008A UA A201707008 A UAA201707008 A UA A201707008A UA 120065 C2 UA120065 C2 UA 120065C2
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UA
Ukraine
Prior art keywords
pyrazines
pyrazolo
substituted
kinase inhibitors
janus kinase
Prior art date
Application number
UAA201707008A
Other languages
English (en)
Ukrainian (uk)
Inventor
Шеллі Ален
Шелли Ален
Марк Лоуренс БОЙЗ
Марк Дж. Чікареллі
Марк Дж. ЧИКАРЕЛЛИ
Джей Бредфорд Фел
Джон П. Фішер
Джон П. Фишер
Джон Ґаудіно
Джон ГАУДИНО
Ерік Джеймс Хікен
Эрик Джэймс Хикен
Рональд Джей Хінклін
Рональд Джэй Хинклин
Крістофер Ф. Крейзер
Кристофер Ф. КРЭЙЗЕР
Елен Лейрд
Элен Лейрд
Джон І. Робінсон
Джон И. Робинсон
Тоні П. Тенґ
Тони П. ТЭНГ
Лоуренс І. Бьорджес
Лоуренс И. Бьорджес
Роберт Ендрю Ріджер
Роберт Эндрю РИДЖЕР
Джед ФЕНЕДЖЕР
Йосітака Сато
Йоситака САТО
Катеріна Лефтеріс
Катерина Лефтерис
Радж К. РАХЕДЖА
Брайдон Л. БЕННЕТ
Original Assignee
Ерей Біофарма Інк.
Эрей Биофарма Инк.
Селджін Корпорейшн
Селджин Корпорейшн
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ерей Біофарма Інк., Эрей Биофарма Инк., Селджін Корпорейшн, Селджин Корпорейшн filed Critical Ерей Біофарма Інк.
Publication of UA120065C2 publication Critical patent/UA120065C2/uk

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
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    • A61P19/00Drugs for skeletal disorders
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • AHUMAN NECESSITIES
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    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00Antineoplastic agents
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    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Transplantation (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
UAA201707008A 2014-12-05 2015-12-04 4,6-ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]-ПІРАЗИНИ ЯК ІНГІБІТОРИ JAK-КІНАЗИ UA120065C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462088068P 2014-12-05 2014-12-05
PCT/US2015/064062 WO2016090285A1 (en) 2014-12-05 2015-12-04 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS

Publications (1)

Publication Number Publication Date
UA120065C2 true UA120065C2 (uk) 2019-09-25

Family

ID=55069089

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UAA201707008A UA120065C2 (uk) 2014-12-05 2015-12-04 4,6-ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]-ПІРАЗИНИ ЯК ІНГІБІТОРИ JAK-КІНАЗИ

Country Status (29)

Country Link
US (3) US10189845B2 (OSRAM)
EP (2) EP3878451A1 (OSRAM)
JP (2) JP6641373B2 (OSRAM)
KR (1) KR20170090476A (OSRAM)
CN (1) CN107278203B (OSRAM)
AU (1) AU2015357585B2 (OSRAM)
BR (1) BR112017011798A2 (OSRAM)
CA (1) CA2969709A1 (OSRAM)
CL (1) CL2017001422A1 (OSRAM)
CO (1) CO2017006674A2 (OSRAM)
CR (1) CR20170309A (OSRAM)
DK (1) DK3227297T3 (OSRAM)
ES (1) ES2865483T3 (OSRAM)
HR (1) HRP20210501T1 (OSRAM)
HU (1) HUE054371T2 (OSRAM)
IL (1) IL252656A0 (OSRAM)
MX (1) MX386316B (OSRAM)
MY (1) MY191016A (OSRAM)
PH (1) PH12017501032A1 (OSRAM)
PL (1) PL3227297T3 (OSRAM)
PT (1) PT3227297T (OSRAM)
RS (1) RS61693B1 (OSRAM)
RU (2) RU2742938C2 (OSRAM)
SG (1) SG11201704542SA (OSRAM)
SI (1) SI3227297T1 (OSRAM)
TW (1) TWI725004B (OSRAM)
UA (1) UA120065C2 (OSRAM)
WO (1) WO2016090285A1 (OSRAM)
ZA (1) ZA201704494B (OSRAM)

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WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
WO2016090285A1 (en) 2014-12-05 2016-06-09 Array Biopharma Inc. 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
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AU2017286653B2 (en) 2016-06-16 2021-11-04 Denali Therapeutics Inc. Pyrimidin-2-ylamino-1H-pyrazols as LRRK2 inhibitors for use in the treatment of neurodegenerative disorders
GB201617758D0 (en) * 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
US20200157081A1 (en) * 2017-05-24 2020-05-21 Denali Therapeutics Inc. Compounds, compositions and methods
EP3668858A1 (en) 2017-08-14 2020-06-24 Pfizer Inc Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
CN113924301B (zh) * 2019-04-12 2024-08-16 北京普祺医药科技股份有限公司 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途
KR20230031981A (ko) 2019-05-14 2023-03-07 프로벤션 바이오, 인코포레이티드 제1형 당뇨병을 예방하기 위한 방법 및 조성물
CN113150012B (zh) * 2020-01-22 2023-03-24 浙江海正药业股份有限公司 吡唑并[1,5-a]吡嗪类衍生物及其制备方法和用途
IL297050A (en) 2020-04-04 2022-12-01 Pfizer Methods of treating the 2019 corona virus disease
KR20230092863A (ko) 2020-06-11 2023-06-26 프로벤션 바이오, 인코포레이티드 제1형 당뇨병을 예방하기 위한 방법 및 조성물
WO2023083200A1 (zh) * 2021-11-12 2023-05-19 南京明德新药研发有限公司 吡唑并环化合物及其应用
WO2024235167A1 (zh) * 2023-05-12 2024-11-21 海南康哲美丽科技有限公司 一种吡唑并吡嗪类化合物及其晶型的制备方法

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PH12012502046A1 (en) * 2010-04-14 2017-07-26 Array Biopharma Inc 5,7-substituted~imidazo[1,2-c]pyrimidines as inhibitors of jak kinases
BR112014008865A2 (pt) * 2011-10-12 2017-04-25 Array Biopharma Inc imidazo[1,2-c]pirimidinas 5,7-substituídas
SI2831077T1 (sl) * 2012-03-28 2016-09-30 Merck Patent Gmbh Biciklični pirazinonski derivati
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AU2015357585A1 (en) 2017-07-13
CA2969709A1 (en) 2016-06-09
IL252656A0 (en) 2017-07-31
JP2018507167A (ja) 2018-03-15
TW201632523A (zh) 2016-09-16
US20170362240A1 (en) 2017-12-21
CL2017001422A1 (es) 2018-01-05
DK3227297T3 (da) 2021-04-06
SI3227297T1 (sl) 2021-04-30
CR20170309A (es) 2018-02-02
HUE054371T2 (hu) 2021-09-28
EP3227297A1 (en) 2017-10-11
US20200291039A1 (en) 2020-09-17
RU2021102805A (ru) 2021-02-12
PT3227297T (pt) 2021-04-09
CN107278203B (zh) 2020-05-19
US20190177328A1 (en) 2019-06-13
BR112017011798A2 (pt) 2017-12-26
RU2017123387A (ru) 2019-01-11
JP2020055859A (ja) 2020-04-09
US10189845B2 (en) 2019-01-29
JP6641373B2 (ja) 2020-02-05
EP3227297B1 (en) 2021-01-20
MX386316B (es) 2025-03-18
CN107278203A (zh) 2017-10-20
RU2742938C2 (ru) 2021-02-11
TWI725004B (zh) 2021-04-21
ES2865483T3 (es) 2021-10-15
US11028093B2 (en) 2021-06-08
PH12017501032A1 (en) 2017-11-27
WO2016090285A1 (en) 2016-06-09
RS61693B1 (sr) 2021-05-31
KR20170090476A (ko) 2017-08-07
CO2017006674A2 (es) 2017-10-20
HRP20210501T1 (hr) 2021-05-14
AU2015357585B2 (en) 2020-07-02
PL3227297T3 (pl) 2021-10-25
MX2017007284A (es) 2017-08-25
ZA201704494B (en) 2022-03-30
EP3878451A1 (en) 2021-09-15
MY191016A (en) 2022-05-28
SG11201704542SA (en) 2017-07-28
US10730880B2 (en) 2020-08-04
RU2017123387A3 (OSRAM) 2019-06-03

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