EA201791179A1 - Дейтерированный триазолопиридазин в качестве модулятора киназы - Google Patents

Дейтерированный триазолопиридазин в качестве модулятора киназы

Info

Publication number
EA201791179A1
EA201791179A1 EA201791179A EA201791179A EA201791179A1 EA 201791179 A1 EA201791179 A1 EA 201791179A1 EA 201791179 A EA201791179 A EA 201791179A EA 201791179 A EA201791179 A EA 201791179A EA 201791179 A1 EA201791179 A1 EA 201791179A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
met
cell
subject
present
Prior art date
Application number
EA201791179A
Other languages
English (en)
Other versions
EA033193B1 (ru
Inventor
Патрик Блазиус Фюрер
Рональд Арнодус Хендрика Джосеф Гилиссен
Йоаннис Николас Хупис
Ливен Меерпоэль
Тимоти Пьетро Сюрен Перера
Филипп Джеймс Пай
Original Assignee
Янссен Фармасьютика Нв
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 Янссен Фармасьютика Нв filed Critical Янссен Фармасьютика Нв
Publication of EA201791179A1 publication Critical patent/EA201791179A1/ru
Publication of EA033193B1 publication Critical patent/EA033193B1/ru

Links

Classifications

    • 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
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к триазолопиридазиновому соединению формулы (I)его N-оксидам, фармацевтически приемлемым солям и сольватам, где D представляет собой дейтерий, применению таких соединений в качестве модуляторов протеинтирозинкиназы, в частности ингибиторов c-Met, применению таких соединений для уменьшения или ингибирования киназной активности c-Met в клетке или субъекте и модулирования экспрессии c-Met в клетке или субъекте и применению таких соединений для предупреждения или лечения у субъекта нарушения, связанного с пролиферацией клеток, и/или нарушений, связанных с c-Met. Настоящее изобретение дополнительно относится к фармацевтическим композициям, содержащим соединения по настоящему изобретению, и к способам лечения состояний, таких как формы рака, и других нарушений, связанных с пролиферацией клеток.
EA201791179A 2014-12-04 2015-12-03 Дейтерированный триазолопиридазин в качестве модулятора киназы EA033193B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14196387 2014-12-04
EP14196585 2014-12-05
PCT/EP2015/078525 WO2016087586A1 (en) 2014-12-04 2015-12-03 A deuterated triazolopyridazine as a kinase modulator

Publications (2)

Publication Number Publication Date
EA201791179A1 true EA201791179A1 (ru) 2017-09-29
EA033193B1 EA033193B1 (ru) 2019-09-30

Family

ID=54771127

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791179A EA033193B1 (ru) 2014-12-04 2015-12-03 Дейтерированный триазолопиридазин в качестве модулятора киназы

Country Status (22)

Country Link
US (2) US10138246B2 (ru)
EP (1) EP3227296B1 (ru)
JP (1) JP6795502B2 (ru)
KR (1) KR102643179B1 (ru)
CN (1) CN107108632B (ru)
AU (1) AU2015357085B2 (ru)
BR (1) BR112017010849B1 (ru)
CA (1) CA2968294C (ru)
DK (1) DK3227296T3 (ru)
EA (1) EA033193B1 (ru)
ES (1) ES2795666T3 (ru)
HU (1) HUE050285T2 (ru)
IL (1) IL252356B (ru)
MX (1) MX2017007114A (ru)
MY (1) MY183207A (ru)
PL (1) PL3227296T3 (ru)
PT (1) PT3227296T (ru)
SG (1) SG11201704078XA (ru)
SI (1) SI3227296T1 (ru)
TW (1) TWI695837B (ru)
WO (1) WO2016087586A1 (ru)
ZA (1) ZA201703386B (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI695837B (zh) * 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒
CN106279176B (zh) * 2015-06-11 2020-09-08 中国科学院上海药物研究所 氘代的3-[(6-喹啉基)二氟甲基]-6-[(1-甲基)-4-吡唑基][1,2,4]三唑并[4,3-b]哒嗪及其应用
WO2019161320A1 (en) * 2018-02-17 2019-08-22 Apollomics Inc. Cancer treatment using combination of neutrophil modulator with modulator of immune checkpoint
WO2022140528A1 (en) * 2020-12-23 2022-06-30 Genzyme Corporation Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors
EP4267573A1 (en) 2020-12-23 2023-11-01 Genzyme Corporation Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1306095A3 (en) 1992-03-05 2003-06-25 Board Of Regents, The University Of Texas System Methods and compositions for targeting the vasculature of solid tumors
US5474765A (en) 1992-03-23 1995-12-12 Ut Sw Medical Ctr At Dallas Preparation and use of steroid-polyanionic polymer-based conjugates targeted to vascular endothelial cells
EP0822788B1 (en) 1995-04-19 2002-09-04 Schneider (Usa) Inc. Drug release coated stent
CA2372053C (en) 1999-04-28 2008-09-02 Board Of Regents, The University Of Texas System Compositions and methods for cancer treatment by selectively inhibiting vegf
US6776796B2 (en) 2000-05-12 2004-08-17 Cordis Corportation Antiinflammatory drug and delivery device
AP3433A (en) * 2005-12-21 2015-10-31 Janssen Pharmaceutica Nv Triazolopyridazines as tyrosine kinase modultors
JP5548123B2 (ja) * 2007-06-21 2014-07-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 6−{ジフルオロ[6−(1−メチル−1H−ピラゾル−4−イル)[1,2,4]トリアゾロ[4,3−b]ピリダジン−3−イル]メチル}キノリンの多形および水和物の形態、塩、ならびに製造方法
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
PA8792501A1 (es) 2007-08-09 2009-04-23 Sanofi Aventis Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met.
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
TWI695837B (zh) * 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒

Also Published As

Publication number Publication date
BR112017010849A2 (pt) 2018-01-09
BR112017010849B1 (pt) 2023-12-12
CA2968294A1 (en) 2016-06-09
JP6795502B2 (ja) 2020-12-02
AU2015357085A1 (en) 2017-07-27
JP2017537112A (ja) 2017-12-14
SI3227296T1 (sl) 2020-09-30
TW201636350A (zh) 2016-10-16
US20190031670A1 (en) 2019-01-31
US10138246B2 (en) 2018-11-27
HUE050285T2 (hu) 2020-11-30
ZA201703386B (en) 2021-07-28
NZ733447A (en) 2023-09-29
CN107108632A (zh) 2017-08-29
SG11201704078XA (en) 2017-06-29
CN107108632B (zh) 2022-04-19
IL252356A0 (en) 2017-07-31
US20170267684A1 (en) 2017-09-21
KR20170123606A (ko) 2017-11-08
ES2795666T3 (es) 2020-11-24
PT3227296T (pt) 2020-06-17
MX2017007114A (es) 2018-05-02
KR102643179B1 (ko) 2024-03-04
MY183207A (en) 2021-02-18
EA033193B1 (ru) 2019-09-30
WO2016087586A1 (en) 2016-06-09
AU2015357085B2 (en) 2020-01-30
EP3227296A1 (en) 2017-10-11
EP3227296B1 (en) 2020-03-04
US10464939B2 (en) 2019-11-05
TWI695837B (zh) 2020-06-11
PL3227296T3 (pl) 2020-09-21
IL252356B (en) 2020-03-31
DK3227296T3 (da) 2020-06-08
CA2968294C (en) 2023-09-19

Similar Documents

Publication Publication Date Title
PH12019501321B1 (en) Use of pyrazolopyrimidine derivatives for the treatment of pi3k-delta related disorders
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EA201990665A1 (ru) Регуляторы hpk1 на основе производных пиразолопиридина и их применение для лечения рака
EA201790317A1 (ru) Ингибиторы smyd
EA201791018A1 (ru) Производные 6-амино-7-бицикло-7-деазапурина в качестве ингибиторов протеинкиназы
EA201592068A1 (ru) Ингибиторы энхансера zeste гомолога 2
EA201690752A1 (ru) Ингибиторы g12c kras
EA201692079A1 (ru) Ингибиторы лизин-специфической деметилазы-1
EA201790599A1 (ru) Соединения и композиции в качестве ингибиторов киназ
EA201290103A1 (ru) Гетероциклические соединения и их использование
EA201591753A1 (ru) 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh
EA201490891A1 (ru) Пиридопиразины, обладающие противораковой активностью через ингибирование fgfr киназ
MY159523A (en) Triazolopyridazines as tyrosine kinase modulators
EA201791179A1 (ru) Дейтерированный триазолопиридазин в качестве модулятора киназы
PH12020500343A1 (en) Pyruvate kinase activators for use in treating blood disorders
EA201491747A1 (ru) Замещенные пиридопиримидиновые соединения и их применение в качестве flt3 ингибиторов
MX2017002986A (es) Compuestos de piperidina sustituidos.
PH12016502353A1 (en) Pharmaceutical composition
EA201790908A1 (ru) Новые производные тиенопиримидина в качестве ингибиторов nik
EA201992137A1 (ru) ПИРИМИДОПИРИМИДИНОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ Wee-1
TW201613577A (en) Pharmaceutical combinations
JOP20220107A1 (ar) مثبطات egfr تفارغية وطرق استخدامها
MX2020003126A (es) Derivados de iminopirimidina ciclicos como inhibidores de cinasa.
PH12016500735A1 (en) Substituted pyrimidine compounds and their use as syk inhibitors
MX2018007517A (es) Compuestos triciclicos y composiciones como inhibidores de quinasa.