JP2016525075A - ヘテロアリール置換ピラゾール類 - Google Patents

ヘテロアリール置換ピラゾール類 Download PDF

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Publication number
JP2016525075A
JP2016525075A JP2016520440A JP2016520440A JP2016525075A JP 2016525075 A JP2016525075 A JP 2016525075A JP 2016520440 A JP2016520440 A JP 2016520440A JP 2016520440 A JP2016520440 A JP 2016520440A JP 2016525075 A JP2016525075 A JP 2016525075A
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JP
Japan
Prior art keywords
alkyl
hydrogen
general formula
methyl
cyano
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Pending
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JP2016520440A
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English (en)
Japanese (ja)
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JP2016525075A5 (enExample
Inventor
メンゲル，アンネ
ヒツチコツク，マーリオン
リヒター，アンニヤ
ベルファツカー，ラルス
ブリーム，ハンス
ジーマイスター，ゲルハルト
ボネ，ヴイルヘルム
フェルナンデス−モンタルバン，アマウリ・エルネスト
シユレーダー，イエンス
ホルトン，サイモン
プロイセ，コーネリア
メンニング，ウルズラ
Original Assignee
バイエル ファーマ アクチエンゲゼルシャフト
バイエル ファーマ アクチエンゲゼルシャフト
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Application filed by バイエル ファーマ アクチエンゲゼルシャフト, バイエル ファーマ アクチエンゲゼルシャフト filed Critical バイエル ファーマ アクチエンゲゼルシャフト
Publication of JP2016525075A publication Critical patent/JP2016525075A/ja
Publication of JP2016525075A5 publication Critical patent/JP2016525075A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016520440A 2013-06-21 2014-06-17 ヘテロアリール置換ピラゾール類 Pending JP2016525075A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13173298.4 2013-06-21
EP13173298 2013-06-21
PCT/EP2014/062689 WO2014202584A1 (en) 2013-06-21 2014-06-17 Heteroaryl substituted pyrazoles

Publications (2)

Publication Number Publication Date
JP2016525075A true JP2016525075A (ja) 2016-08-22
JP2016525075A5 JP2016525075A5 (enExample) 2017-07-20

Family

ID=48651939

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016520440A Pending JP2016525075A (ja) 2013-06-21 2014-06-17 ヘテロアリール置換ピラゾール類

Country Status (8)

Country Link
US (1) US9745285B2 (enExample)
EP (1) EP3010901B1 (enExample)
JP (1) JP2016525075A (enExample)
CN (1) CN105452237A (enExample)
CA (1) CA2916194A1 (enExample)
ES (1) ES2652305T3 (enExample)
HK (1) HK1223098A1 (enExample)
WO (1) WO2014202584A1 (enExample)

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UA111754C2 (uk) 2011-10-06 2016-06-10 Байєр Фарма Акцієнгезелльшафт Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань
CN104125957B (zh) 2011-12-21 2016-05-25 拜耳知识产权有限责任公司 取代的苄基吡唑
US20160046604A1 (en) * 2013-03-21 2016-02-18 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
EP3010911A1 (en) * 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
WO2014202590A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
CN105764893A (zh) 2013-10-30 2016-07-13 拜耳制药股份公司 杂芳基取代的吡唑
TW201613886A (en) 2014-06-17 2016-04-16 Bayer Pharma AG 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
WO2016042084A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 inhibitors
CN107406417B (zh) 2015-01-28 2020-06-09 拜耳制药股份公司 4H-吡咯并[3,2-c]吡啶-4-酮衍生物
CN107922389A (zh) 2015-06-17 2018-04-17 拜耳制药股份公司 3‑氨基‑1,5,6,7‑四氢‑4h‑吲哚‑4‑酮
WO2017148995A1 (en) 2016-03-04 2017-09-08 Bayer Pharma Aktiengesellschaft 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity
WO2017157991A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft 1-alkyl-pyrazoles and -indazoles as bub1 inhibitors for the treatment of hyperproliferative diseases
WO2017157992A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft Annulated pyrazoles as bub1 kinase inhibitors for treating proliferative disorders
WO2018122168A1 (en) 2016-12-29 2018-07-05 Bayer Pharma Aktiengesellschaft Combinations of bub1 kinase and parp inhibitors
WO2018158175A1 (en) 2017-02-28 2018-09-07 Bayer Pharma Aktiengesellschaft Combination of bub1 inhibitors
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
WO2018215282A1 (en) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combination of bub1 and pi3k inhibitors
MX2023003362A (es) 2020-09-23 2023-05-30 Scorpion Therapeutics Inc Derivados de pirrolo[3,2-c]piridin-4-ona utiles en el tratamiento del cancer.
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
BR112023006531A2 (pt) 2020-10-09 2023-10-03 Scorpion Therapeutics Inc Inibidores heterocílicos de egfr e/ou her2, para uso no tratamento de câncer
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
WO2024254298A1 (en) 2023-06-08 2024-12-12 Scorpion Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer
EP4724150A1 (en) 2023-06-08 2026-04-15 Antares Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070179133A1 (en) * 2003-03-14 2007-08-02 David Bebbington Compositions useful as inhibitors of protein kinases
WO2012003405A1 (en) * 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2013050438A1 (en) * 2011-10-06 2013-04-11 Bayer Pharma Aktiengesellschaft Substituted benzylindazoles for use as bub1 kinase inhibitors in the treatment of hyperproliferative diseases.

Family Cites Families (20)

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Publication number Priority date Publication date Assignee Title
CN102666537A (zh) 2009-10-20 2012-09-12 艾格尔生物制药股份有限公司 治疗黄病毒科病毒感染的氮杂吲唑
US20130178475A1 (en) 2010-03-17 2013-07-11 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
CN104125957B (zh) 2011-12-21 2016-05-25 拜耳知识产权有限责任公司 取代的苄基吡唑
CA2861804C (en) 2011-12-27 2021-10-26 Ironwood Pharmaceuticals, Inc. 2-benzyl,3(pyrimidin-2-yl)substituted pyrazoles useful as sgc stimulators
EP2847180B1 (en) 2012-05-11 2017-01-04 Bayer Pharma Aktiengesellschaft Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer
WO2014047111A1 (en) 2012-09-18 2014-03-27 Ironwood Pharmaceuticals, Inc. Sgc stimulators
EP2897953B8 (en) 2012-09-19 2019-06-26 Cyclerion Therapeutics, Inc. Sgc stimulators
CA2907730A1 (en) 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Diaminoheteroaryl substituted indazoles
US20160046604A1 (en) 2013-03-21 2016-02-18 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
EP2976336A1 (en) 2013-03-21 2016-01-27 Bayer Pharma Aktiengesellschaft 3-heteroaryl substituted indazoles
JP2016522231A (ja) 2013-06-21 2016-07-28 バイエル ファーマ アクチエンゲゼルシャフト ジアミノヘテロアリール置換ピラゾール類
WO2014202583A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
WO2014202590A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
EP3010911A1 (en) 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
CN105764893A (zh) 2013-10-30 2016-07-13 拜耳制药股份公司 杂芳基取代的吡唑
CA2961578A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 kinase inhibitors
WO2016042081A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 kinase inhibitors
CA2961570A1 (en) 2014-09-19 2016-03-24 Lars Barfacker Benzyl substituted indazoles
WO2016042084A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070179133A1 (en) * 2003-03-14 2007-08-02 David Bebbington Compositions useful as inhibitors of protein kinases
WO2012003405A1 (en) * 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2013050438A1 (en) * 2011-10-06 2013-04-11 Bayer Pharma Aktiengesellschaft Substituted benzylindazoles for use as bub1 kinase inhibitors in the treatment of hyperproliferative diseases.

Also Published As

Publication number Publication date
ES2652305T3 (es) 2018-02-01
CA2916194A1 (en) 2014-12-24
US9745285B2 (en) 2017-08-29
US20160145238A1 (en) 2016-05-26
EP3010901A1 (en) 2016-04-27
CN105452237A (zh) 2016-03-30
EP3010901B1 (en) 2017-09-13
WO2014202584A1 (en) 2014-12-24
HK1223098A1 (zh) 2017-07-21

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