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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Publication number
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 (enExample
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)
  • 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)
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 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
JP2016520118A true JP2016520118A (ja) 2016-07-11
JP2016520118A5 JP2016520118A5 (enExample) 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)

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)

Cited By (1)

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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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BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
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.
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
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
NZ725930A (en) 2014-04-23 2023-04-28 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
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
CN109153647A (zh) 2016-02-15 2019-01-04 分子医学研究中心责任有限公司 用于治疗癌症的taf1抑制剂
EP3472157B1 (en) 2016-06-20 2023-04-12 Incyte Corporation Crystalline solid forms of a bet inhibitor
KR20190103154A (ko) 2016-11-14 2019-09-04 체엠엠 - 포르슝스첸트룸 퓨어 몰레쿨라레 메디친 게엠베하 암의 치료법을 위한 brd4 억제제 및 항폴레이트의 조합
WO2019120234A2 (zh) 2017-12-20 2019-06-27 贝达药业股份有限公司 作为溴结构域蛋白质抑制剂的化合物和组合物
CA3092907A1 (en) * 2018-03-05 2019-09-12 Klinikum Rechts Der Isar Der Technischen Universitat Munchen Treatment of tumors by a combination of an oncolytic adenovirus and a cdk4/6 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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

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