CN106573897B - 作为mIDH1抑制剂的苯并咪唑-2-胺 - Google Patents

作为mIDH1抑制剂的苯并咪唑-2-胺 Download PDF

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Publication number
CN106573897B
CN106573897B CN201580019265.9A CN201580019265A CN106573897B CN 106573897 B CN106573897 B CN 106573897B CN 201580019265 A CN201580019265 A CN 201580019265A CN 106573897 B CN106573897 B CN 106573897B
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amino
phenyl
trimethylcyclohexyl
alkyl
propionic acid
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CN106573897A (zh
Inventor
H.雷文克尔
O.潘克宁
S.林格
S.安劳夫
H.西贝奈歇尔
D.阮
W.施维德
M.鲍泽
K.齐默曼
S.考尔富斯
R.诺伊豪斯
P.M.布拉尼
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Deutsches Krebsforschungszentrum DKFZ
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Bayer Pharma AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580019265.9A 2014-02-11 2015-02-10 作为mIDH1抑制剂的苯并咪唑-2-胺 Expired - Fee Related CN106573897B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP14154680.4 2014-02-11
EP14154680 2014-02-11
EP14182002 2014-08-22
EP14182002.7 2014-08-22
PCT/EP2015/052676 WO2015121210A1 (en) 2014-02-11 2015-02-10 Benzimidazol-2-amines as midh1 inhibitors

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CN106573897A CN106573897A (zh) 2017-04-19
CN106573897B true CN106573897B (zh) 2019-09-24

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US (2) US9957235B2 (enExample)
EP (1) EP3105209B1 (enExample)
JP (1) JP6534675B2 (enExample)
KR (1) KR20160115991A (enExample)
CN (1) CN106573897B (enExample)
AP (1) AP2016009371A0 (enExample)
AU (1) AU2015217788B2 (enExample)
BR (1) BR112016018604A2 (enExample)
CA (1) CA2939026A1 (enExample)
CL (1) CL2016002033A1 (enExample)
CR (1) CR20160361A (enExample)
CU (1) CU24410B1 (enExample)
DO (1) DOP2016000208A (enExample)
EA (1) EA031655B1 (enExample)
IL (1) IL246785A0 (enExample)
MX (1) MX2016010474A (enExample)
PE (1) PE20170143A1 (enExample)
PH (1) PH12016501581A1 (enExample)
SG (1) SG11201605810WA (enExample)
SV (1) SV2016005257A (enExample)
TW (1) TWI666202B (enExample)
UY (1) UY35991A (enExample)
WO (1) WO2015121210A1 (enExample)

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CA2965201A1 (en) * 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
CN107108554B (zh) * 2014-10-23 2020-11-06 德国癌症研究中心 作为midh1抑制剂用于治疗肿瘤的1-环己基-2-苯基氨基苯并咪唑
JP6830909B2 (ja) * 2015-06-08 2021-02-17 ドイチェス クレープスフォルシュングスツェントルム シュティフトゥング デス エッフェントリッヒェン レヒツ mIDH1阻害剤としてのN−メンチルベンズイミダゾール
ES2877424T3 (es) 2015-07-07 2021-11-16 Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts 2-Aril- y 2-arilalquil-bencimidazoles como inhibidores de MIDH1
CN108026052B (zh) * 2015-07-16 2021-10-08 德国癌症研究公共权益基金会 作为mIDH1抑制剂的5-羟烷基苯并咪唑类
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
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TW201718513A (zh) * 2015-07-27 2017-06-01 拜耳製藥公司 製備經取代之3-(2-苯胺-1-環己基-1h-苯并咪唑-5-基)丙酸衍生物之方法
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US20210113598A1 (en) * 2017-08-01 2021-04-22 Deutsches Krebsforschungszentrum (DKFZ) Stiftung des öffentlichen Rechts Combination of MIDH1 Inhibitors and DNA Hypomethylating Agents (HMA)
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TWI760017B (zh) * 2019-12-23 2022-04-01 大陸商昆藥集團股份有限公司 一種idh1突變體抑制劑的鹽型、晶型及其製備方法
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CL2016002033A1 (es) 2017-03-31
JP6534675B2 (ja) 2019-06-26
SV2016005257A (es) 2018-10-02
US20190062285A1 (en) 2019-02-28
AP2016009371A0 (en) 2016-08-31
EA201691590A1 (ru) 2017-02-28
CU24410B1 (es) 2019-05-03
UY35991A (es) 2015-09-30
PH12016501581A1 (en) 2017-02-06
CR20160361A (es) 2016-10-03
TWI666202B (zh) 2019-07-21
CN106573897A (zh) 2017-04-19
JP2017505790A (ja) 2017-02-23
CU20160120A7 (es) 2016-12-23
EP3105209A1 (en) 2016-12-21
WO2015121210A1 (en) 2015-08-20
IL246785A0 (en) 2016-08-31
DOP2016000208A (es) 2016-09-15
MX2016010474A (es) 2016-10-31
TW201613874A (en) 2016-04-16
CA2939026A1 (en) 2015-08-20
US9957235B2 (en) 2018-05-01
KR20160115991A (ko) 2016-10-06
BR112016018604A2 (pt) 2017-08-08
SG11201605810WA (en) 2016-08-30
EP3105209B1 (en) 2019-08-21
AU2015217788A1 (en) 2016-08-04
PE20170143A1 (es) 2017-03-19
US10442772B2 (en) 2019-10-15
EA031655B1 (ru) 2019-02-28
AU2015217788B2 (en) 2019-06-27
US20170197921A1 (en) 2017-07-13

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