TWI666202B - 作為ｍＩＤＨ１抑制劑之苯并咪唑－２－胺 - Google Patents

作為ｍＩＤＨ１抑制劑之苯并咪唑－２－胺 Download PDF

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Publication number
TWI666202B
TWI666202B TW104104623A TW104104623A TWI666202B TW I666202 B TWI666202 B TW I666202B TW 104104623 A TW104104623 A TW 104104623A TW 104104623 A TW104104623 A TW 104104623A TW I666202 B TWI666202 B TW I666202B
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TW
Taiwan
Prior art keywords
amino
phenyl
trimethylcyclohexyl
alkyl
benzimidazol
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TW104104623A
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English (en)
Chinese (zh)
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TW201613874A (en
Inventor
哈木特 瑞溫凱
歐拉夫 潘克寧
史文 林
索賈 安拉芙
賀爾格 席比尼奇
都伊 恩古彥
沃夫根 先威德
馬庫斯 巴瑟
卡佳 茲莫曼
史塔芬 卡福斯
羅蘭 紐郝斯
保羅 馬修 布蘭利
Original Assignee
德商拜耳製藥公司
德國癌症研究中心
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Application filed by 德商拜耳製藥公司, 德國癌症研究中心 filed Critical 德商拜耳製藥公司
Publication of TW201613874A publication Critical patent/TW201613874A/zh
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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)
TW104104623A 2014-02-11 2015-02-11 作為ｍＩＤＨ１抑制劑之苯并咪唑－２－胺 TWI666202B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
??14154680.4 2014-02-11
EP14154680 2014-02-11
EP14182002 2014-08-22
??14182002.7 2014-08-22

Publications (2)

Publication Number Publication Date
TW201613874A TW201613874A (en) 2016-04-16
TWI666202B true TWI666202B (zh) 2019-07-21

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TW104104623A TWI666202B (zh) 2014-02-11 2015-02-11 作為ｍＩＤＨ１抑制劑之苯并咪唑－２－胺

Country Status (23)

Country Link
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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HUE062424T2 (hu) 2014-09-19 2023-11-28 Forma Therapeutics Inc Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok
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
US10138226B2 (en) * 2014-10-23 2018-11-27 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as MIDH1 inhibitors
CA2988356A1 (en) * 2015-06-08 2016-12-15 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
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CA2992364A1 (en) 2015-07-16 2017-01-19 Bayer Pharma Aktiengesellschaft 5-hydroxyalkylbenzimidazoles as midh1 inhibitors
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
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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US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US10532047B2 (en) 2018-05-16 2020-01-14 Forma Therapeutics, Inc. Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
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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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TW202216139A (zh) 2020-07-21 2022-05-01 日商第一三共股份有限公司 帝盟多與變異型ｉｄｈ１酵素阻礙劑之組合藥
CN112062687B (zh) * 2020-09-02 2023-11-21 上海信谊万象药业股份有限公司 一种盐酸阿扎司琼中间体3-氨基-5-氯-2-羟基苯甲酸甲酯的合成方法

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Also Published As

Publication number Publication date
CU24410B1 (es) 2019-05-03
US20190062285A1 (en) 2019-02-28
JP6534675B2 (ja) 2019-06-26
JP2017505790A (ja) 2017-02-23
PH12016501581A1 (en) 2017-02-06
DOP2016000208A (es) 2016-09-15
KR20160115991A (ko) 2016-10-06
IL246785A0 (en) 2016-08-31
UY35991A (es) 2015-09-30
EP3105209B1 (en) 2019-08-21
SG11201605810WA (en) 2016-08-30
AP2016009371A0 (en) 2016-08-31
TW201613874A (en) 2016-04-16
CA2939026A1 (en) 2015-08-20
CR20160361A (es) 2016-10-03
EA031655B1 (ru) 2019-02-28
EA201691590A1 (ru) 2017-02-28
AU2015217788B2 (en) 2019-06-27
WO2015121210A1 (en) 2015-08-20
CU20160120A7 (es) 2016-12-23
BR112016018604A2 (pt) 2017-08-08
PE20170143A1 (es) 2017-03-19
US9957235B2 (en) 2018-05-01
US10442772B2 (en) 2019-10-15
CN106573897A (zh) 2017-04-19
CN106573897B (zh) 2019-09-24
US20170197921A1 (en) 2017-07-13
MX2016010474A (es) 2016-10-31
CL2016002033A1 (es) 2017-03-31
SV2016005257A (es) 2018-10-02
EP3105209A1 (en) 2016-12-21
AU2015217788A1 (en) 2016-08-04

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