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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Expired - Fee Related
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CN201580019265.9A
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Chinese (zh)
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • 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
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • 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)
  • 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 2014-02-11
EP14154680.4 2014-02-11
EP14182002.7 2014-08-22
EP14182002 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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Country Link
US (2) US9957235B2 (https=)
EP (1) EP3105209B1 (https=)
JP (1) JP6534675B2 (https=)
KR (1) KR20160115991A (https=)
CN (1) CN106573897B (https=)
AP (1) AP2016009371A0 (https=)
AU (1) AU2015217788B2 (https=)
BR (1) BR112016018604A2 (https=)
CA (1) CA2939026A1 (https=)
CL (1) CL2016002033A1 (https=)
CR (1) CR20160361A (https=)
CU (1) CU24410B1 (https=)
DO (1) DOP2016000208A (https=)
EA (1) EA031655B1 (https=)
IL (1) IL246785A0 (https=)
MX (1) MX2016010474A (https=)
PE (1) PE20170143A1 (https=)
PH (1) PH12016501581A1 (https=)
SG (1) SG11201605810WA (https=)
SV (1) SV2016005257A (https=)
TW (1) TWI666202B (https=)
UY (1) UY35991A (https=)
WO (1) WO2015121210A1 (https=)

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WO2016062677A1 (en) * 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
EP3303302B1 (en) 2015-06-08 2019-03-20 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
EP3319945B1 (en) * 2015-07-07 2021-04-28 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors
JP6824954B2 (ja) * 2015-07-16 2021-02-03 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５−ヒドロキシアルキルベンズイミダゾール
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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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AU2015217788B2 (en) 2019-06-27
EA031655B1 (ru) 2019-02-28
MX2016010474A (es) 2016-10-31
PH12016501581A1 (en) 2017-02-06
DOP2016000208A (es) 2016-09-15
SG11201605810WA (en) 2016-08-30
US20170197921A1 (en) 2017-07-13
PE20170143A1 (es) 2017-03-19
JP2017505790A (ja) 2017-02-23
EP3105209A1 (en) 2016-12-21
CU20160120A7 (es) 2016-12-23
US10442772B2 (en) 2019-10-15
AU2015217788A1 (en) 2016-08-04
CA2939026A1 (en) 2015-08-20
CN106573897A (zh) 2017-04-19
AP2016009371A0 (en) 2016-08-31
KR20160115991A (ko) 2016-10-06
JP6534675B2 (ja) 2019-06-26
EA201691590A1 (ru) 2017-02-28
CU24410B1 (es) 2019-05-03
CR20160361A (es) 2016-10-03
EP3105209B1 (en) 2019-08-21
TW201613874A (en) 2016-04-16
SV2016005257A (es) 2018-10-02
UY35991A (es) 2015-09-30
US20190062285A1 (en) 2019-02-28
US9957235B2 (en) 2018-05-01
TWI666202B (zh) 2019-07-21
BR112016018604A2 (pt) 2017-08-08
CL2016002033A1 (es) 2017-03-31
WO2015121210A1 (en) 2015-08-20
IL246785A0 (en) 2016-08-31

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