CN105051030A - 二氨基杂芳基取代的吲唑 - Google Patents

二氨基杂芳基取代的吲唑 Download PDF

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Publication number
CN105051030A
CN105051030A CN201480017090.3A CN201480017090A CN105051030A CN 105051030 A CN105051030 A CN 105051030A CN 201480017090 A CN201480017090 A CN 201480017090A CN 105051030 A CN105051030 A CN 105051030A
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CN
China
Prior art keywords
alkyl
group
hydrogen
pyrimidine
base
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Pending
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CN201480017090.3A
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English (en)
Chinese (zh)
Inventor
C-S.希尔格
M.希奇科克
H.布里姆
G.西迈斯特
A.E.弗南德斯-蒙塔尔班
J.施勒德
S.霍尔顿
C.普罗伊泽
K.登纳
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Bayer Pharma AG
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Bayer Pharma AG
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Publication of CN105051030A publication Critical patent/CN105051030A/zh
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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/33—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480017090.3A 2013-03-21 2014-03-19 二氨基杂芳基取代的吲唑 Pending CN105051030A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13160350.8 2013-03-21
EP13160350 2013-03-21
PCT/EP2014/055540 WO2014147144A1 (en) 2013-03-21 2014-03-19 Diaminoheteroaryl substituted indazoles

Publications (1)

Publication Number Publication Date
CN105051030A true CN105051030A (zh) 2015-11-11

Family

ID=47900948

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480017090.3A Pending CN105051030A (zh) 2013-03-21 2014-03-19 二氨基杂芳基取代的吲唑

Country Status (10)

Country Link
US (2) US20160052912A1 (https=)
EP (1) EP2976334A1 (https=)
JP (1) JP2016514717A (https=)
CN (1) CN105051030A (https=)
AR (1) AR095708A1 (https=)
CA (1) CA2907730A1 (https=)
HK (1) HK1217324A1 (https=)
TW (1) TW201514167A (https=)
UY (1) UY35499A (https=)
WO (1) WO2014147144A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2014147204A1 (en) * 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
HK1218750A1 (zh) * 2013-03-21 2017-03-10 Bayer Pharma Aktiengesellschaft 3-杂芳基取代的吲唑
ES2652305T3 (es) 2013-06-21 2018-02-01 Bayer Pharma Aktiengesellschaft Pirazoles heteroaril sustituidos
US9765058B2 (en) 2013-06-21 2017-09-19 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
CA2928998A1 (en) 2013-10-30 2015-05-07 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
EP3157914B1 (en) 2014-06-17 2018-09-26 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
AU2015316796A1 (en) 2014-09-19 2017-03-30 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as Bub1 inhibitors
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
ES2924359T3 (es) 2017-04-11 2022-10-06 Sunshine Lake Pharma Co Ltd Compuestos de indazol sustituidos con flúor y usos de los mismos
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999066051A2 (en) * 1998-06-16 1999-12-23 Sugen, Inc. Nek-related and bub1-related protein kinases
JP2010111624A (ja) * 2008-11-06 2010-05-20 Shionogi & Co Ltd Ｔｔｋ阻害作用を有するインダゾール誘導体
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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7378532B2 (en) * 2004-03-26 2008-05-27 Yung Shin Pharmaceutical Ind. Co., Ltd. Fused pyrazolyl compound
TW201038567A (en) * 2009-03-27 2010-11-01 Pathway Therapeutics Ltd Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
ES2638144T3 (es) * 2011-12-21 2017-10-18 Bayer Intellectual Property Gmbh Bencilpirazoles sustituidos
ES2620316T3 (es) * 2012-05-11 2017-06-28 Bayer Pharma Aktiengesellschaft Cicloalquenopirazoles sustituidos como inhibidores de BUB1 para el tratamiento del cáncer
WO2014147204A1 (en) * 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
HK1218750A1 (zh) * 2013-03-21 2017-03-10 Bayer Pharma Aktiengesellschaft 3-杂芳基取代的吲唑

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999066051A2 (en) * 1998-06-16 1999-12-23 Sugen, Inc. Nek-related and bub1-related protein kinases
JP2010111624A (ja) * 2008-11-06 2010-05-20 Shionogi & Co Ltd Ｔｔｋ阻害作用を有するインダゾール誘導体
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.

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JUNGSEOG KANG ET AL.: "Structure and Substrate Recruitment of the Human Spindle Checkpoint Kinase Bub1", 《MOLECULAR CELL》 *

Also Published As

Publication number Publication date
CA2907730A1 (en) 2014-09-25
EP2976334A1 (en) 2016-01-27
JP2016514717A (ja) 2016-05-23
HK1217324A1 (zh) 2017-01-06
TW201514167A (zh) 2015-04-16
AR095708A1 (es) 2015-11-04
US20160052912A1 (en) 2016-02-25
US20170283396A1 (en) 2017-10-05
UY35499A (es) 2014-10-31
WO2014147144A1 (en) 2014-09-25

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