EA028175B1 - Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания - Google Patents

Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания Download PDF

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Publication number
EA028175B1
EA028175B1 EA201592255A EA201592255A EA028175B1 EA 028175 B1 EA028175 B1 EA 028175B1 EA 201592255 A EA201592255 A EA 201592255A EA 201592255 A EA201592255 A EA 201592255A EA 028175 B1 EA028175 B1 EA 028175B1
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EA
Eurasian Patent Office
Prior art keywords
methyl
chlorophenyl
triazolo
cyclopropyl
dihydropyrrolo
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EA201592255A
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English (en)
Russian (ru)
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EA201592255A1 (ru
Inventor
Ютта Бланк
Гвидо Больд
Симона Котеста
Вито Гуаньяно
Хайнрих Рюэгер
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201592255A1 publication Critical patent/EA201592255A1/ru
Publication of EA028175B1 publication Critical patent/EA028175B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
EA201592255A 2013-05-28 2014-05-27 Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания EA028175B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13169441 2013-05-28
PCT/IB2014/061736 WO2014191906A1 (en) 2013-05-28 2014-05-27 Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease

Publications (2)

Publication Number Publication Date
EA201592255A1 EA201592255A1 (ru) 2016-04-29
EA028175B1 true EA028175B1 (ru) 2017-10-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201592255A EA028175B1 (ru) 2013-05-28 2014-05-27 Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания

Country Status (14)

Country Link
US (1) US9624247B2 (https=)
EP (1) EP3004108B1 (https=)
JP (1) JP2016520118A (https=)
KR (1) KR20160012195A (https=)
CN (1) CN105263934B (https=)
AU (1) AU2014272695B2 (https=)
BR (1) BR112015029401A8 (https=)
CA (1) CA2912986A1 (https=)
EA (1) EA028175B1 (https=)
ES (1) ES2656471T3 (https=)
MX (1) MX2015016421A (https=)
PL (1) PL3004108T3 (https=)
PT (1) PT3004108T (https=)
WO (1) WO2014191906A1 (https=)

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US11466034B2 (en) 2017-12-20 2022-10-11 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition

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SG11201506924YA (en) 2013-03-15 2015-09-29 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
MX2015016421A (es) 2013-05-28 2016-03-03 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
PL3134403T3 (pl) 2014-04-23 2020-07-13 Incyte Corporation 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
KR20180134860A (ko) 2016-02-15 2018-12-19 체엠엠 - 포르슝스첸트룸 퓨어 몰레쿨라레 메디친 게엠베하 암의 치료를 위한 taf1 억제제
CA3028689A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Crystalline solid forms of a bet inhibitor
US20190262355A1 (en) 2016-11-14 2019-08-29 Cemm-Forschungszentrum Für Molekulare Medizin Gmbh Combination of a brd4 inhibitor and an antifolate for the therapy of cancer
KR20210031852A (ko) * 2018-03-05 2021-03-23 클리니쿰 레히츠 데어 이자르 데어 테크니쉔 우니베르지테트 뮌헨 종양 세포 붕괴성 아데노바이러스와 cdk4/6 억제제의 조합물에 의한 종양의 치료
MX2022000521A (es) * 2019-07-12 2022-06-14 Scenic Immunology B V Compuestos n-sustituidos-3,4-(5-anillo fusionado)-5-fenil-pirrolid in-2-ona como inhibidores de la enzima isoqc y/o qc.
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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US11466034B2 (en) 2017-12-20 2022-10-11 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition
US11845762B2 (en) 2017-12-20 2023-12-19 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition

Also Published As

Publication number Publication date
WO2014191906A1 (en) 2014-12-04
BR112015029401A2 (pt) 2017-07-25
KR20160012195A (ko) 2016-02-02
EP3004108A1 (en) 2016-04-13
CN105263934B (zh) 2017-09-08
JP2016520118A (ja) 2016-07-11
AU2014272695A1 (en) 2015-11-26
US20160102107A1 (en) 2016-04-14
MX2015016421A (es) 2016-03-03
EA201592255A1 (ru) 2016-04-29
EP3004108B1 (en) 2017-10-18
AU2014272695B2 (en) 2016-10-20
PL3004108T3 (pl) 2018-03-30
PT3004108T (pt) 2018-01-24
US9624247B2 (en) 2017-04-18
CN105263934A (zh) 2016-01-20
CA2912986A1 (en) 2014-12-04
BR112015029401A8 (pt) 2020-03-17
ES2656471T3 (es) 2018-02-27

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