JP2015520143A - 癌を治療するためのｂｕｂ１阻害薬としての置換されているシクロアルケノピラゾール類 - Google Patents

癌を治療するためのｂｕｂ１阻害薬としての置換されているシクロアルケノピラゾール類 Download PDF

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JP2015520143A
JP2015520143A JP2015510822A JP2015510822A JP2015520143A JP 2015520143 A JP2015520143 A JP 2015520143A JP 2015510822 A JP2015510822 A JP 2015510822A JP 2015510822 A JP2015510822 A JP 2015510822A JP 2015520143 A JP2015520143 A JP 2015520143A
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alkyl
hydrogen
compound
alkoxy
formula
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JP2015520143A5 (US07794700-20100914-C00152.png
Inventor
ヒツチコツク，マリオン
ヒルガー，クリストフ−シユテフアン
メンゲル，アンネ
ブリーム，ハンス
ホルトン，シモン
ピユツター，フエラ
ジーマイスター，ゲルハルト
プレヒトル，シユテフアン
フエルナンデス−モンタルフアン，アマウリ，エルネスト
シユテグマン，クリスティアン
プロイセ，コルネリ
グノート，マルク，ジアン
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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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Publication of JP2015520143A publication Critical patent/JP2015520143A/ja
Publication of JP2015520143A5 publication Critical patent/JP2015520143A5/ja
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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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/695—Silicon compounds
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/188—Preparation; Treatments not provided for in C07F7/20 by reactions involving the formation of Si-O linkages

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Plural Heterocyclic Compounds (AREA)
JP2015510822A 2012-05-11 2013-05-08 癌を治療するためのｂｕｂ１阻害薬としての置換されているシクロアルケノピラゾール類 Ceased JP2015520143A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12167690 2012-05-11
EP12167690.2 2012-05-11
PCT/EP2013/059666 WO2013167698A1 (en) 2012-05-11 2013-05-08 Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer

Publications (2)

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JP2015520143A true JP2015520143A (ja) 2015-07-16
JP2015520143A5 JP2015520143A5 (US07794700-20100914-C00152.png) 2016-07-07

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JP2015510822A Ceased JP2015520143A (ja) 2012-05-11 2013-05-08 癌を治療するためのｂｕｂ１阻害薬としての置換されているシクロアルケノピラゾール類

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US (2) US20150141372A1 (US07794700-20100914-C00152.png)
EP (1) EP2847180B1 (US07794700-20100914-C00152.png)
JP (1) JP2015520143A (US07794700-20100914-C00152.png)
CN (1) CN104411701B (US07794700-20100914-C00152.png)
CA (1) CA2872933A1 (US07794700-20100914-C00152.png)
ES (1) ES2620316T3 (US07794700-20100914-C00152.png)
HK (1) HK1207861A1 (US07794700-20100914-C00152.png)
WO (1) WO2013167698A1 (US07794700-20100914-C00152.png)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016514718A (ja) * 2013-03-21 2016-05-23 バイエル ファーマ アクチエンゲゼルシャフト ３−ヘテロアリール置換インダゾール類
JP2016514717A (ja) * 2013-03-21 2016-05-23 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インダゾール

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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
ES2638144T3 (es) 2011-12-21 2017-10-18 Bayer Intellectual Property Gmbh Bencilpirazoles sustituidos
CN105164116A (zh) * 2013-03-21 2015-12-16 拜耳制药股份公司 杂芳基取代的吲唑
CA2916194A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
CA2916103A1 (en) * 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Diaminoheteroaryl substituted pyrazoles
CA2916116A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
US9682974B2 (en) 2013-10-30 2017-06-20 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
JP6545199B2 (ja) * 2014-06-17 2019-07-17 バイエル ファーマ アクチエンゲゼルシャフト ３−アミノ−１，５，６，７−テトラヒドロ−４ｈ−インドール−４−オン類
CU20170029A7 (es) 2014-09-19 2017-08-08 Bayer Pharma AG Indazoles sustituidos con bencilo en calidad de inhibidores de bub1, útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular, un procedimiento para la preparación de estos compuestos, y compuestos intermediarios
BR112017016193B1 (pt) 2015-01-28 2023-02-23 Bayer Pharma Aktiengesellschaft Derivados de 4h-pirrolo[3,2-c]piridin-4-ona
US10227299B2 (en) 2015-06-17 2019-03-12 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4H-indol-4-ones
WO2017021348A1 (en) * 2015-08-05 2017-02-09 Bayer Pharma Aktiengesellschaft 1h-pyrrol-3-amines
CN108602820A (zh) * 2015-12-16 2018-09-28 拜耳制药股份公司 杂-1,5,6,7-四氢-4h-吲哚-4-酮类化合物
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
AU2021347288A1 (en) 2020-09-23 2023-05-04 Scorpion Therapeutics, Inc. Pyrrolo[3,2-c]pyridin-4-one derivatives useful in the treatment of 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
CA3198202A1 (en) 2020-10-09 2022-04-14 Scorpion Therapeutics, Inc. Methods for treating cancer
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
EP4293019A1 (en) * 2022-06-13 2023-12-20 Netherlands Translational Research Center Holding B.V. 4-substituted (1h-benzo[d]imidazol-2-yl)-1h-pyrazoles as bub1 inhibitors useful for treating cancers

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WO2002047690A1 (en) * 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
JP2002544271A (ja) * 1999-05-12 2002-12-24 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー 抗腫瘍薬としての４，５，６，７−テトラヒドロインダゾール誘導体
WO2006030124A1 (fr) * 2004-09-13 2006-03-23 Sanofi-Aventis Derives de pyrazole condense, leur preparation et leur application en therapeutique.
JP2006321799A (ja) * 2005-05-18 2006-11-30 Carlsbad Technology Inc 癌治療
JP2009543768A (ja) * 2006-07-14 2009-12-10 アステックス・セラピューティクス・リミテッド 医薬組み合わせ
WO2011115804A1 (en) * 2010-03-17 2011-09-22 Ironwood Pharmaceuticals, Inc. Sgc stimulators
EP2594270A2 (en) * 2011-11-18 2013-05-22 BIP Patents The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc)
JP2014531465A (ja) * 2011-10-06 2014-11-27 バイエル・ファルマ・アクチェンゲゼルシャフトＢａｙｅｒ Ｐｈａｒｍａ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 過増殖性疾患の処置におけるｂｕｂ１キナーゼ阻害剤として使用するための置換ベンジルインダゾール類

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Patent Citations (8)

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JP2002544271A (ja) * 1999-05-12 2002-12-24 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー 抗腫瘍薬としての４，５，６，７−テトラヒドロインダゾール誘導体
WO2002047690A1 (en) * 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
WO2006030124A1 (fr) * 2004-09-13 2006-03-23 Sanofi-Aventis Derives de pyrazole condense, leur preparation et leur application en therapeutique.
JP2006321799A (ja) * 2005-05-18 2006-11-30 Carlsbad Technology Inc 癌治療
JP2009543768A (ja) * 2006-07-14 2009-12-10 アステックス・セラピューティクス・リミテッド 医薬組み合わせ
WO2011115804A1 (en) * 2010-03-17 2011-09-22 Ironwood Pharmaceuticals, Inc. Sgc stimulators
JP2014531465A (ja) * 2011-10-06 2014-11-27 バイエル・ファルマ・アクチェンゲゼルシャフトＢａｙｅｒ Ｐｈａｒｍａ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 過増殖性疾患の処置におけるｂｕｂ１キナーゼ阻害剤として使用するための置換ベンジルインダゾール類
EP2594270A2 (en) * 2011-11-18 2013-05-22 BIP Patents The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016514718A (ja) * 2013-03-21 2016-05-23 バイエル ファーマ アクチエンゲゼルシャフト ３−ヘテロアリール置換インダゾール類
JP2016514717A (ja) * 2013-03-21 2016-05-23 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インダゾール

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Publication number Publication date
CA2872933A1 (en) 2013-11-14
ES2620316T3 (es) 2017-06-28
CN104411701A (zh) 2015-03-11
US20170275267A1 (en) 2017-09-28
EP2847180B1 (en) 2017-01-04
CN104411701B (zh) 2017-01-18
HK1207861A1 (en) 2016-02-12
EP2847180A1 (en) 2015-03-18
WO2013167698A1 (en) 2013-11-14
US20150141372A1 (en) 2015-05-21

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