CN104411701B - 作为Bub1抑制剂的用于治疗癌症的取代的环烯并吡唑 - Google Patents

作为Bub1抑制剂的用于治疗癌症的取代的环烯并吡唑 Download PDF

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Publication number
CN104411701B
CN104411701B CN201380036066.XA CN201380036066A CN104411701B CN 104411701 B CN104411701 B CN 104411701B CN 201380036066 A CN201380036066 A CN 201380036066A CN 104411701 B CN104411701 B CN 104411701B
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alkyl
hydrogen
compound
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formula
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CN104411701A (zh
Inventor
M·希契科克
C-S·希尔格
A·门格尔
H·布里姆
S·霍尔顿
V·皮特
G·西迈斯特
S·普雷希特尔
A·E·费尔南德斯-蒙塔尔万
C·斯特格曼
C·普罗伊塞
M·J·格诺特
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Bayer Pharma AG
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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)
  • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380036066.XA 2012-05-11 2013-05-08 作为Bub1抑制剂的用于治疗癌症的取代的环烯并吡唑 Expired - Fee Related CN104411701B (zh)

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)

Publication Number Publication Date
CN104411701A CN104411701A (zh) 2015-03-11
CN104411701B true CN104411701B (zh) 2017-01-18

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CN201380036066.XA Expired - Fee Related CN104411701B (zh) 2012-05-11 2013-05-08 作为Bub1抑制剂的用于治疗癌症的取代的环烯并吡唑

Country Status (8)

Country Link
US (2) US20150141372A1 (OSRAM)
EP (1) EP2847180B1 (OSRAM)
JP (1) JP2015520143A (OSRAM)
CN (1) CN104411701B (OSRAM)
CA (1) CA2872933A1 (OSRAM)
ES (1) ES2620316T3 (OSRAM)
HK (1) HK1207861A1 (OSRAM)
WO (1) WO2013167698A1 (OSRAM)

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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
EP2794596B1 (en) 2011-12-21 2017-05-31 Bayer Intellectual Property GmbH Substituted benzylpyrazoles
EP2976334A1 (en) * 2013-03-21 2016-01-27 Bayer Pharma Aktiengesellschaft Diaminoheteroaryl substituted indazoles
CA2907594A1 (en) * 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
WO2014147203A1 (en) 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft 3-heteroaryl substituted indazoles
HK1222852A1 (zh) * 2013-06-21 2017-07-14 Bayer Pharma Aktiengesellschaft 二氨基杂芳基取代的吡唑
EP3010904A1 (en) 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
US9745285B2 (en) 2013-06-21 2017-08-29 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
CA2928998A1 (en) 2013-10-30 2015-05-07 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
TW201613886A (en) * 2014-06-17 2016-04-16 Bayer Pharma AG 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
PE20170697A1 (es) 2014-09-19 2017-06-24 Bayer Pharma AG Indazoles sustituidos con benzilo como inhibidores de bub1
SG11201705908VA (en) 2015-01-28 2017-08-30 Bayer Pharma AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
EP3310775B1 (en) * 2015-06-17 2020-04-01 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
EP3331611B1 (en) 2015-08-05 2021-06-02 Bayer Pharma Aktiengesellschaft 1h-pyrrol-3-amines
JP2019504826A (ja) * 2015-12-16 2019-02-21 バイエル ファーマ アクチエンゲゼルシャフト ヘテロ−１，５，６，７−テトラヒドロ−４ｈ−インドール−４−オン類
WO2017148995A1 (en) 2016-03-04 2017-09-08 Bayer Pharma Aktiengesellschaft 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity
WO2017157992A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft Annulated pyrazoles as bub1 kinase inhibitors for treating proliferative disorders
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
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
WO2022076831A2 (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
CN116036121B (zh) * 2022-12-16 2024-10-18 福州载基生物科技有限公司 人bub1基因在制备抗肿瘤药物中的用途
WO2024254266A1 (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
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Also Published As

Publication number Publication date
EP2847180A1 (en) 2015-03-18
HK1207861A1 (en) 2016-02-12
US20150141372A1 (en) 2015-05-21
CA2872933A1 (en) 2013-11-14
ES2620316T3 (es) 2017-06-28
JP2015520143A (ja) 2015-07-16
EP2847180B1 (en) 2017-01-04
CN104411701A (zh) 2015-03-11
US20170275267A1 (en) 2017-09-28
WO2013167698A1 (en) 2013-11-14

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