AU2015217788B2 - Benzimidazol-2-amines as mIDH1 inhibitors - Google Patents

Benzimidazol-2-amines as mIDH1 inhibitors Download PDF

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Publication number
AU2015217788B2
AU2015217788B2 AU2015217788A AU2015217788A AU2015217788B2 AU 2015217788 B2 AU2015217788 B2 AU 2015217788B2 AU 2015217788 A AU2015217788 A AU 2015217788A AU 2015217788 A AU2015217788 A AU 2015217788A AU 2015217788 B2 AU2015217788 B2 AU 2015217788B2
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AU
Australia
Prior art keywords
amino
phenyl
trimethylcyclohexyl
alkyl
propanoic acid
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Ceased
Application number
AU2015217788A
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AU2015217788A1 (en
Inventor
Sonja Anlauf
Marcus Bauser
Paul Matthew Blaney
Stefan KAULFUSS
Roland Neuhaus
Duy Nguyen
Olaf Panknin
Hartmut Rehwinkel
Sven Ring
Wolfgang Schwede
Holger Siebeneicher
Katja Zimmermann
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German Cancer Research Center
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German Cancer Research Center
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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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
AU2015217788A 2014-02-11 2015-02-10 Benzimidazol-2-amines as mIDH1 inhibitors Ceased AU2015217788B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2015217788A1 AU2015217788A1 (en) 2016-08-04
AU2015217788B2 true AU2015217788B2 (en) 2019-06-27

Family

ID=52462928

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015217788A Ceased AU2015217788B2 (en) 2014-02-11 2015-02-10 Benzimidazol-2-amines as mIDH1 inhibitors

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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WO2016044781A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
US10138226B2 (en) * 2014-10-23 2018-11-27 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as MIDH1 inhibitors
JP6672288B2 (ja) 2014-10-23 2020-03-25 バイエル・ファルマ・アクティエンゲゼルシャフト 腫瘍の治療のためのmidh1阻害剤としての1−シクロヘキシル−2−フェニルアミノベンゾイミダゾール
EP3303302B1 (en) * 2015-06-08 2019-03-20 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
WO2017005674A1 (en) * 2015-07-07 2017-01-12 Bayer Pharma Aktiengesellschaft 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors
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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JP2020535112A (ja) * 2017-08-01 2020-12-03 ドイッチェス・クレープスフォルシュングスツェントルムDeutsches Krebsforschungszentrum Midh1阻害剤とdna低メチル化剤(hma)との組合せ
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
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WO2019222551A1 (en) 2018-05-16 2019-11-21 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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AU2019296173B2 (en) * 2018-06-26 2022-01-06 Kpc Pharmaceuticals, Inc. Benzimidazole derivatives and use thereof as IDH1 inhibitors
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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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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JP6672288B2 (ja) 2014-10-23 2020-03-25 バイエル・ファルマ・アクティエンゲゼルシャフト 腫瘍の治療のためのmidh1阻害剤としての1−シクロヘキシル−2−フェニルアミノベンゾイミダゾール
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WO2017005674A1 (en) 2015-07-07 2017-01-12 Bayer Pharma Aktiengesellschaft 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors
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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Also Published As

Publication number Publication date
CN106573897B (zh) 2019-09-24
AP2016009371A0 (en) 2016-08-31
MX2016010474A (es) 2016-10-31
UY35991A (es) 2015-09-30
SV2016005257A (es) 2018-10-02
PE20170143A1 (es) 2017-03-19
US20170197921A1 (en) 2017-07-13
CL2016002033A1 (es) 2017-03-31
KR20160115991A (ko) 2016-10-06
IL246785A0 (en) 2016-08-31
CU20160120A7 (es) 2016-12-23
CN106573897A (zh) 2017-04-19
JP2017505790A (ja) 2017-02-23
PH12016501581A1 (en) 2017-02-06
BR112016018604A2 (pt) 2017-08-08
EA201691590A1 (ru) 2017-02-28
JP6534675B2 (ja) 2019-06-26
AU2015217788A1 (en) 2016-08-04
US10442772B2 (en) 2019-10-15
US9957235B2 (en) 2018-05-01
EP3105209B1 (en) 2019-08-21
US20190062285A1 (en) 2019-02-28
CR20160361A (es) 2016-10-03
CU24410B1 (es) 2019-05-03
TW201613874A (en) 2016-04-16
SG11201605810WA (en) 2016-08-30
EP3105209A1 (en) 2016-12-21
WO2015121210A1 (en) 2015-08-20
CA2939026A1 (en) 2015-08-20
EA031655B1 (ru) 2019-02-28
TWI666202B (zh) 2019-07-21
DOP2016000208A (es) 2016-09-15

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Owner name: DEUTSCHES KREBSFORSCHUNGSZENTRUM, STIFTUNG DES OEFFENTLICHEN RECHTS

Free format text: FORMER OWNER(S): BAYER PHARMA AKTIENGESELLSCHAFT

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