AU2014272695B2 - Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease - Google Patents

Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease Download PDF

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Publication number
AU2014272695B2
AU2014272695B2 AU2014272695A AU2014272695A AU2014272695B2 AU 2014272695 B2 AU2014272695 B2 AU 2014272695B2 AU 2014272695 A AU2014272695 A AU 2014272695A AU 2014272695 A AU2014272695 A AU 2014272695A AU 2014272695 B2 AU2014272695 B2 AU 2014272695B2
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Prior art keywords
methyl
pyrazol
chlorophenyl
triazolo
cyclopropyl
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AU2014272695A
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AU2014272695A1 (en
Inventor
Jutta Blank
Guido Bold
Simona Cotesta
Vito Guagnano
Heinrich Rueeger
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • A61K31/41—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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/435—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
    • A61K31/4353—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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2014272695A 2013-05-28 2014-05-27 Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease Ceased AU2014272695B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13169441 2013-05-28
EP13169441.6 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
AU2014272695A1 AU2014272695A1 (en) 2015-11-26
AU2014272695B2 true AU2014272695B2 (en) 2016-10-20

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AU2014272695A Ceased AU2014272695B2 (en) 2013-05-28 2014-05-27 Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease

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

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ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
JP2016520118A (ja) 2013-05-28 2016-07-11 ノバルティス アーゲー Ｂｅｔ阻害剤としてのピラゾロ−ピロリジン−４−オン誘導体および疾患の処置におけるその使用
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG10201809353TA (en) 2014-04-23 2018-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
MX2018009870A (es) 2016-02-15 2018-11-29 Cemm Forschungszentrum Fuer Molekulare Medizin Gmbh Inhibidores de taf1 para la terapia del cancer.
TWI830533B (zh) 2016-06-20 2024-01-21 美商英塞特公司 Ｂｅｔ抑制劑之結晶固體形式
AU2017359288A1 (en) 2016-11-14 2019-05-30 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh Combination of a BRD4 inhibitor and an antifolate for the therapy of cancer
IL275478B2 (en) 2017-12-20 2024-06-01 Betta Pharmaceuticals Co Ltd A preparation that functions as a bromodomain protein inhibitor, and the composition
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
AU2020312647A1 (en) * 2019-07-12 2022-02-24 Scenic Immunology B.V. N-substituted-3,4-(fused 5-ring)-5-phenyl-pyrrolidine-2-one compounds as inhibitors of isoQC and/or QC enzyme
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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AU2014272695A1 (en) 2015-11-26
KR20160012195A (ko) 2016-02-02
BR112015029401A8 (pt) 2020-03-17
MX2015016421A (es) 2016-03-03
EA028175B1 (ru) 2017-10-31
BR112015029401A2 (pt) 2017-07-25
WO2014191906A1 (en) 2014-12-04
EP3004108A1 (en) 2016-04-13
CN105263934A (zh) 2016-01-20
EA201592255A1 (ru) 2016-04-29
PT3004108T (pt) 2018-01-24
ES2656471T3 (es) 2018-02-27
JP2016520118A (ja) 2016-07-11
CA2912986A1 (en) 2014-12-04
US9624247B2 (en) 2017-04-18
PL3004108T3 (pl) 2018-03-30
CN105263934B (zh) 2017-09-08
US20160102107A1 (en) 2016-04-14
EP3004108B1 (en) 2017-10-18

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