JP2016520118A - 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 - Google Patents

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 Download PDF

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JP2016520118A
JP2016520118A JP2016516280A JP2016516280A JP2016520118A JP 2016520118 A JP2016520118 A JP 2016520118A JP 2016516280 A JP2016516280 A JP 2016516280A JP 2016516280 A JP2016516280 A JP 2016516280A JP 2016520118 A JP2016520118 A JP 2016520118A
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methyl
chlorophenyl
pyrazol
triazolo
cyclopropyl
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Japanese (ja)
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JP2016520118A5 (esLanguage
Inventor
ブランク，ジュッタ
ボールド，グィド
コテスタ，シモナ
グァニャノ，ヴィット
ルエゲル，ヘインリッヒ
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ノバルティス アーゲー
ノバルティス アーゲー
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Publication of JP2016520118A publication Critical patent/JP2016520118A/ja
Publication of JP2016520118A5 publication Critical patent/JP2016520118A5/ja
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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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
JP2016516280A 2013-05-28 2014-05-27 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 Pending JP2016520118A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13169441.6 2013-05-28
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
JP2016520118A true JP2016520118A (ja) 2016-07-11
JP2016520118A5 JP2016520118A5 (esLanguage) 2017-06-29

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JP2016516280A Pending JP2016520118A (ja) 2013-05-28 2014-05-27 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

Country Status (14)

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

Cited By (1)

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Publication number Priority date Publication date Assignee Title
JP2022542540A (ja) * 2019-07-12 2022-10-05 シーニック・イミュノロジー・ヴェンノーツハップ ｉｓｏＱＣ及び／又はＱＣ酵素の阻害剤としてのＮ－置換－３，４－（縮合５－環）－５－フェニル－ピロリジン－２－オン化合物

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EP2970282B1 (en) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CN105263934B (zh) 2013-05-28 2017-09-08 诺华股份有限公司 作为bet抑制剂的吡唑并‑吡咯烷‑4‑酮衍生物及其在治疗疾病中的用途
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic 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
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
PL3674302T3 (pl) 2014-04-23 2023-07-24 Incyte Holdings Corporation 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
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
WO2017140728A1 (en) 2016-02-15 2017-08-24 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh Taf1 inhibitors for the therapy of cancer
HRP20230466T1 (hr) 2016-06-20 2023-07-21 Incyte Corporation Kristalni čvrsti oblici bet inhibitora
MX2019005443A (es) 2016-11-14 2019-11-21 Cemm Forschungszentrum Fuer Molekulare Medizin Gmbh Combinacion de un inhibidor de brd4 y un antifolato para la terapia del cancer.
TWI713952B (zh) 2017-12-20 2020-12-21 大陸商貝達藥業股份有限公司 作為溴結構域蛋白質抑制劑的化合物和組合物
FI3762004T3 (fi) * 2018-03-05 2023-12-11 Klinikum Rechts Der Isar Der Technischen Univ Muenchen Kasvainten hoitaminen onkolyyttisen adenoviruksen ja CDK4/6-inhibiittorin yhdistelmällä
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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PT3004108T (pt) 2018-01-24
CA2912986A1 (en) 2014-12-04
EP3004108A1 (en) 2016-04-13
EA201592255A1 (ru) 2016-04-29
CN105263934A (zh) 2016-01-20
AU2014272695A1 (en) 2015-11-26
BR112015029401A2 (pt) 2017-07-25
BR112015029401A8 (pt) 2020-03-17
US9624247B2 (en) 2017-04-18
EA028175B1 (ru) 2017-10-31
WO2014191906A1 (en) 2014-12-04
MX2015016421A (es) 2016-03-03
US20160102107A1 (en) 2016-04-14
PL3004108T3 (pl) 2018-03-30
EP3004108B1 (en) 2017-10-18
CN105263934B (zh) 2017-09-08
AU2014272695B2 (en) 2016-10-20
KR20160012195A (ko) 2016-02-02
ES2656471T3 (es) 2018-02-27

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