CU20160120A7 - Benzimidazol-2-aminas como inhibidores de midh1 - Google Patents
Benzimidazol-2-aminas como inhibidores de midh1Info
- Publication number
- CU20160120A7 CU20160120A7 CUP2016000120A CU20160120A CU20160120A7 CU 20160120 A7 CU20160120 A7 CU 20160120A7 CU P2016000120 A CUP2016000120 A CU P2016000120A CU 20160120 A CU20160120 A CU 20160120A CU 20160120 A7 CU20160120 A7 CU 20160120A7
- Authority
- CU
- Cuba
- Prior art keywords
- benzimidazol
- aminas
- midh1
- formula
- inhibitors
- Prior art date
Links
Classifications
-
- 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)
- 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)
Abstract
La presente invención se refiere a benzimidazol-2-aminas con la fórmula general (I): ESPACIO PARA FÓRMULA que inhiben a la isocitrato deshidrogenasa 1 mutada (mIDH1 R123H), donde R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R11 y R12 son según se los define aquí, métodos para elaborarlos y compuestos intermediarios útiles su elaboración. Los compuestos de fórmula I son útiles en la profilaxis o el tratamiento de diversas enfermedades, particularmente en los neoplasmas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14154680 | 2014-02-11 | ||
| EP14182002 | 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 |
|---|---|
| CU20160120A7 true CU20160120A7 (es) | 2016-12-23 |
| CU24410B1 CU24410B1 (es) | 2019-05-03 |
Family
ID=52462928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU2016000120A CU24410B1 (es) | 2014-02-11 | 2015-02-10 | Benzimidazol-2-aminas como inhibidores de midh1 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US9957235B2 (es) |
| EP (1) | EP3105209B1 (es) |
| JP (1) | JP6534675B2 (es) |
| KR (1) | KR20160115991A (es) |
| CN (1) | CN106573897B (es) |
| AP (1) | AP2016009371A0 (es) |
| AU (1) | AU2015217788B2 (es) |
| BR (1) | BR112016018604A2 (es) |
| CA (1) | CA2939026A1 (es) |
| CL (1) | CL2016002033A1 (es) |
| CR (1) | CR20160361A (es) |
| CU (1) | CU24410B1 (es) |
| DO (1) | DOP2016000208A (es) |
| EA (1) | EA031655B1 (es) |
| IL (1) | IL246785A0 (es) |
| MX (1) | MX2016010474A (es) |
| PE (1) | PE20170143A1 (es) |
| PH (1) | PH12016501581A1 (es) |
| SG (1) | SG11201605810WA (es) |
| SV (1) | SV2016005257A (es) |
| TW (1) | TWI666202B (es) |
| UY (1) | UY35991A (es) |
| WO (1) | WO2015121210A1 (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2939026A1 (en) | 2014-02-11 | 2015-08-20 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| CA2939021C (en) | 2014-02-11 | 2022-07-12 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| ES2953347T3 (es) | 2014-09-19 | 2023-11-10 | Forma Therapeutics Inc | Derivados de piridin-2(1H)-ona quinolinona como inhibidores de isocitrato deshidrogenasa mutante |
| JP6648116B2 (ja) | 2014-09-19 | 2020-02-14 | フォーマ セラピューティクス,インコーポレイテッド | 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのキノリノンピリミジン組成物 |
| 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 |
| CA2988356A1 (en) * | 2015-06-08 | 2016-12-15 | 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 |
| 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 |
| 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 |
| 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 |
| EP3414224B1 (en) * | 2016-02-09 | 2022-03-23 | InventisBio LLC | 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) |
| 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 |
| 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 |
| US11576906B2 (en) | 2018-05-16 | 2023-02-14 | Forma Therapeutics, Inc. | Inhibiting mutant IDH-1 |
| JP7258059B2 (ja) * | 2018-06-26 | 2023-04-14 | 昆薬集団股▲フン▼有限公司 | ベンズイミダゾール誘導体及びそのidh1阻害剤としての応用 |
| 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 |
| AU2021311539A1 (en) | 2020-07-21 | 2023-02-09 | Daiichi Sankyo Company, Limited | Combination drug of temozolomide and inhibitor of mutated IDH1 enzyme |
| 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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| 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 |
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| WO2008153701A1 (en) | 2007-05-24 | 2008-12-18 | Schering Corporation | Compounds for inhibiting ksp kinesin activity |
| US8168800B2 (en) | 2007-11-02 | 2012-05-01 | The Regents Of The University Of California | Aβ-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 |
| EP2445345B1 (en) * | 2009-06-23 | 2014-08-27 | The Translational Genomics Research Institute | Benzamide derivatives |
| 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 |
| CA2939026A1 (en) | 2014-02-11 | 2015-08-20 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| CA2939021C (en) | 2014-02-11 | 2022-07-12 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| 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 |
| US10392402B2 (en) | 2015-05-18 | 2019-08-27 | Translational Drug Development, Llc | Heterocyclic compounds as kinase inhibitors |
| EP3297674B1 (en) | 2015-05-22 | 2023-01-04 | Translational Drug Development Llc | Benzamide and active compound compositions and methods of use |
| CA2988356A1 (en) | 2015-06-08 | 2016-12-15 | 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 |
| 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 |
| 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 |
| JP6768078B2 (ja) | 2016-03-02 | 2020-10-14 | トランスレイショナル・ドラッグ・ディベロップメント・エルエルシー | アミノベンゾイミダゾール誘導体 |
-
2015
- 2015-02-10 CA CA2939026A patent/CA2939026A1/en not_active Abandoned
- 2015-02-10 WO PCT/EP2015/052676 patent/WO2015121210A1/en not_active Ceased
- 2015-02-10 SG SG11201605810WA patent/SG11201605810WA/en unknown
- 2015-02-10 JP JP2016551221A patent/JP6534675B2/ja not_active Expired - Fee Related
- 2015-02-10 AP AP2016009371A patent/AP2016009371A0/en unknown
- 2015-02-10 MX MX2016010474A patent/MX2016010474A/es unknown
- 2015-02-10 CN CN201580019265.9A patent/CN106573897B/zh not_active Expired - Fee Related
- 2015-02-10 US US15/118,154 patent/US9957235B2/en active Active
- 2015-02-10 EP EP15703288.9A patent/EP3105209B1/en active Active
- 2015-02-10 KR KR1020167024825A patent/KR20160115991A/ko not_active Withdrawn
- 2015-02-10 EA EA201691590A patent/EA031655B1/ru not_active IP Right Cessation
- 2015-02-10 CU CU2016000120A patent/CU24410B1/es unknown
- 2015-02-10 CR CR20160361A patent/CR20160361A/es unknown
- 2015-02-10 PE PE2016001465A patent/PE20170143A1/es unknown
- 2015-02-10 AU AU2015217788A patent/AU2015217788B2/en not_active Ceased
- 2015-02-10 BR BR112016018604A patent/BR112016018604A2/pt not_active Application Discontinuation
- 2015-02-11 TW TW104104623A patent/TWI666202B/zh not_active IP Right Cessation
- 2015-02-11 UY UY0001035991A patent/UY35991A/es not_active Application Discontinuation
-
2016
- 2016-07-14 IL IL246785A patent/IL246785A0/en unknown
- 2016-08-10 PH PH12016501581A patent/PH12016501581A1/en unknown
- 2016-08-11 DO DO2016000208A patent/DOP2016000208A/es unknown
- 2016-08-11 SV SV2016005257A patent/SV2016005257A/es unknown
- 2016-08-11 CL CL2016002033A patent/CL2016002033A1/es unknown
-
2018
- 2018-03-16 US US15/923,895 patent/US10442772B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP3105209A1 (en) | 2016-12-21 |
| TW201613874A (en) | 2016-04-16 |
| KR20160115991A (ko) | 2016-10-06 |
| IL246785A0 (en) | 2016-08-31 |
| PH12016501581A1 (en) | 2017-02-06 |
| SG11201605810WA (en) | 2016-08-30 |
| PE20170143A1 (es) | 2017-03-19 |
| MX2016010474A (es) | 2016-10-31 |
| US20190062285A1 (en) | 2019-02-28 |
| UY35991A (es) | 2015-09-30 |
| EP3105209B1 (en) | 2019-08-21 |
| TWI666202B (zh) | 2019-07-21 |
| AU2015217788B2 (en) | 2019-06-27 |
| CA2939026A1 (en) | 2015-08-20 |
| US20170197921A1 (en) | 2017-07-13 |
| CR20160361A (es) | 2016-10-03 |
| CN106573897A (zh) | 2017-04-19 |
| US10442772B2 (en) | 2019-10-15 |
| DOP2016000208A (es) | 2016-09-15 |
| US9957235B2 (en) | 2018-05-01 |
| SV2016005257A (es) | 2018-10-02 |
| JP6534675B2 (ja) | 2019-06-26 |
| JP2017505790A (ja) | 2017-02-23 |
| EA031655B1 (ru) | 2019-02-28 |
| BR112016018604A2 (pt) | 2017-08-08 |
| CU24410B1 (es) | 2019-05-03 |
| AP2016009371A0 (en) | 2016-08-31 |
| WO2015121210A1 (en) | 2015-08-20 |
| AU2015217788A1 (en) | 2016-08-04 |
| CL2016002033A1 (es) | 2017-03-31 |
| CN106573897B (zh) | 2019-09-24 |
| EA201691590A1 (ru) | 2017-02-28 |
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