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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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52462928&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI666202(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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

Landscapes

  • 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)
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

Family

ID=52462928

Family Applications (1)

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA031655B1 (ru) 2014-02-11 2019-02-28 Байер Фарма Акциенгезельшафт Бензимидазол-2-амины в качестве ингибиторов midhi
JP6688735B2 (ja) 2014-02-11 2020-04-28 バイエル・ファルマ・アクティエンゲゼルシャフト ｍＩＤＨ１阻害剤としてのベンズイミダゾール−２−アミン
AU2015317321B2 (en) 2014-09-19 2020-03-12 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
PL3447050T3 (pl) 2014-09-19 2020-07-27 Forma Therapeutics, Inc. Chinolinonowe pochodne pirydyn-2(1H)-onu jako inhibitory zmutowanej dehydrogenazy izocytrynianowej
CA2965213A1 (en) 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors
ES2822654T3 (es) * 2014-10-23 2021-05-04 Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts Benzimidazol-2-aminas como inhibidores de mIDH1
US10370339B2 (en) 2015-06-08 2019-08-06 Bayer Pharma Aktiengesellschaft N-Methylbenzimidazoles as mIDH1 inhibitors
CN107949557B (zh) * 2015-07-07 2021-11-02 德国癌症研究公共权益基金会 作为mIDH1抑制剂的2-芳基-和2-芳烷基-苯并咪唑类
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
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
TW201708193A (zh) 2015-07-27 2017-03-01 拜耳製藥公司 突變之異檸檬酸脫氫酶ｉｄｈ１ ｒ１３２ｈ之抑制劑
AU2017217536A1 (en) * 2016-02-09 2018-08-09 Inventisbio Inc. Inhibitor of indoleamine-2,3-dioxygenase (IDO)
WO2019015672A1 (zh) * 2017-07-21 2019-01-24 南京明德新药研发股份有限公司 吡啶并咪唑类化合物及其应用
WO2019025256A1 (en) 2017-08-01 2019-02-07 Bayer Aktiengesellschaft COMBINATION OF MIDH1 INHIBITORS AND DNA HYPOMETHYLATION (AHM) AGENTS
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
PT3720442T (pt) 2018-05-16 2023-03-13 Forma Therapeutics Inc Inibição de idh-1 mutante
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
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
WO2020001474A1 (zh) * 2018-06-26 2020-01-02 南京明德新药研发有限公司 苯并咪唑衍生物及其作为idh1抑制剂的应用
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
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
KR20230042065A (ko) * 2020-07-21 2023-03-27 다이이찌 산쿄 가부시키가이샤 테모졸로마이드와 돌연변이 idh1 효소 억제제의 조합 의약
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010151441A1 (en) * 2009-06-23 2010-12-29 Translational Genomics Research Institute Benzamide derivatives

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
CN1161340C (zh) 1998-11-30 2004-08-11 先灵公司 为玻连蛋白受体拮抗剂的苯并咪唑化合物
US6340681B1 (en) 1999-07-16 2002-01-22 Pfizer Inc 2-benzimidazolylamine compounds as ORL-1-receptor agonists
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
EP1411928A1 (en) 2001-07-20 2004-04-28 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
CA2477505A1 (en) 2002-03-01 2003-09-12 Smithkline Beecham Corporation Diamino-pyrimidines and their use as angiogenesis inhibitors
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
EP1677791A4 (en) 2003-10-31 2007-08-15 Takeda Pharmaceutical NITROGENIC CONDENSED HETEROCYCLIC COMPOUNDS
WO2005121132A1 (ja) 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗ｈｃｖ作用を有する縮合ヘテロ環化合物
EP1810677A1 (en) 2004-10-08 2007-07-25 Takeda Pharmaceutical Company Limited Receptor function regulating agent
BRPI0608581A2 (pt) 2005-03-14 2010-01-19 Transtech Pharma Inc derivados de benzazol, composiÇÕes e mÉtodos de uso como inibidores de b-secretase
WO2008153701A1 (en) * 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
WO2009059214A1 (en) 2007-11-02 2009-05-07 The Regents Of The University Of California Abeta-binding small molecules
WO2009116074A2 (en) 2008-02-13 2009-09-24 Cadila Healthcare Limited Substituted benzimidazoles as cannabinoid modulator
UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones
WO2011072174A1 (en) 2009-12-09 2011-06-16 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
WO2012172043A1 (en) * 2011-06-15 2012-12-20 Laboratoire Biodim Purine derivatives and their use as pharmaceuticals for prevention or treatment of bacterial infections
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN103435554A (zh) * 2013-09-06 2013-12-11 中国药科大学 2-苯氨基苯并咪唑类化合物及其用途
EA031655B1 (ru) 2014-02-11 2019-02-28 Байер Фарма Акциенгезельшафт Бензимидазол-2-амины в качестве ингибиторов midhi
JP6688735B2 (ja) 2014-02-11 2020-04-28 バイエル・ファルマ・アクティエンゲゼルシャフト ｍＩＤＨ１阻害剤としてのベンズイミダゾール−２−アミン
ES2822654T3 (es) 2014-10-23 2021-05-04 Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts Benzimidazol-2-aminas como inhibidores de mIDH1
CA2965213A1 (en) 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors
US10392402B2 (en) 2015-05-18 2019-08-27 Translational Drug Development, Llc Heterocyclic compounds as kinase inhibitors
CN114907271B (zh) 2015-05-22 2024-05-07 转化药物开发有限责任公司 苯甲酰胺和活性化合物的组合物及其使用方法
US10370339B2 (en) 2015-06-08 2019-08-06 Bayer Pharma Aktiengesellschaft N-Methylbenzimidazoles as mIDH1 inhibitors
CN107949557B (zh) 2015-07-07 2021-11-02 德国癌症研究公共权益基金会 作为mIDH1抑制剂的2-芳基-和2-芳烷基-苯并咪唑类
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
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
TW201708193A (zh) 2015-07-27 2017-03-01 拜耳製藥公司 突變之異檸檬酸脫氫酶ｉｄｈ１ ｒ１３２ｈ之抑制劑
EP3423439A4 (en) 2016-03-02 2019-08-14 Translational Drug Development Llc aminobenzimidazole derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010151441A1 (en) * 2009-06-23 2010-12-29 Translational Genomics Research Institute Benzamide derivatives

Also Published As

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

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