PE20181039A1 - Metodo para preparar derivados de acido 3-(2-anilino-1-ciclohexil-1h-bencimidazol-5-il)propanoico sustituido - Google Patents
Metodo para preparar derivados de acido 3-(2-anilino-1-ciclohexil-1h-bencimidazol-5-il)propanoico sustituidoInfo
- Publication number
- PE20181039A1 PE20181039A1 PE2018000132A PE2018000132A PE20181039A1 PE 20181039 A1 PE20181039 A1 PE 20181039A1 PE 2018000132 A PE2018000132 A PE 2018000132A PE 2018000132 A PE2018000132 A PE 2018000132A PE 20181039 A1 PE20181039 A1 PE 20181039A1
- Authority
- PE
- Peru
- Prior art keywords
- formula
- hydrogen atom
- alkyl group
- anilino
- acid derivatives
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
LLa presente invencion se refiere a un metodo para preparar derivados de acido 3-(2-anilino-1-ciclohexil-1H-bencimidazol-5-il)propanoico sustituido de la formula general (I) donde R1 representa un atomo de hidrogeno o R1 representa un grupo que se selecciona de alquil C1-C3, alcoxi C1-C3, haloalquil C1-C3- y haloalcoxi C1-C3-; R2 representa un atomo de hidrogeno o un grupo alquilo C1- C3; R3 representa un atomo de hidrogeno o un grupo alquilo C1-C3; R4 representa un grupo C1-C3 ohexilo, el cual esta sustituido opcionalmente de manera simple o multiple por un grupo alquilo C1-C3; R5 representa un atomo de hidrogeno o un grupo alquilo C1-C6; R6 es alquilo C1-C6. Dicho metodo comprende hacer reaccionar un compuesto de formula (II) con un compuesto de formula (III) para formar un compuesto de formula (IV). Tambien se refiere a intermediarios para preparar los compuestos de formula (I). La presente invencion tambien se relaciona con una forma cristalina del acido 3-(2-{[4-(trifluorometoxi)fenil]amino}-1-[(1R,5R)-3,3,5-trimetilciclohexil]-1H-bencimidazol-5-il)propanoico y composiciones farmaceuticas que comprenden esta forma cristalina
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15178413 | 2015-07-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181039A1 true PE20181039A1 (es) | 2018-07-03 |
Family
ID=53758091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018000132A PE20181039A1 (es) | 2015-07-27 | 2016-07-25 | Metodo para preparar derivados de acido 3-(2-anilino-1-ciclohexil-1h-bencimidazol-5-il)propanoico sustituido |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US10703727B2 (es) |
| EP (1) | EP3328838A1 (es) |
| JP (1) | JP6787998B2 (es) |
| KR (1) | KR20180030906A (es) |
| CN (1) | CN107848985B (es) |
| AR (1) | AR105494A1 (es) |
| AU (1) | AU2016299329B2 (es) |
| BR (1) | BR112018001535A2 (es) |
| CA (1) | CA2993480A1 (es) |
| CL (1) | CL2018000241A1 (es) |
| CO (1) | CO2018000795A2 (es) |
| HK (1) | HK1252848A1 (es) |
| IL (1) | IL256926A (es) |
| MX (1) | MX2018001204A (es) |
| PE (1) | PE20181039A1 (es) |
| RU (1) | RU2018106948A (es) |
| TW (1) | TW201718513A (es) |
| WO (1) | WO2017017046A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9951027B2 (en) | 2014-02-11 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as MIDH1 inhibitors |
| PE20170143A1 (es) | 2014-02-11 | 2017-03-19 | Bayer Pharma AG | Benzimidazol-2-aminas como inhibidores de midh1 |
| EP3209660B1 (en) | 2014-10-23 | 2020-06-17 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors |
| US10370339B2 (en) | 2015-06-08 | 2019-08-06 | Bayer Pharma Aktiengesellschaft | N-Methylbenzimidazoles as mIDH1 inhibitors |
| WO2017005674A1 (en) | 2015-07-07 | 2017-01-12 | Bayer Pharma Aktiengesellschaft | 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 |
| 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 |
| 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 |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010151441A1 (en) | 2009-06-23 | 2010-12-29 | Translational Genomics Research Institute | Benzamide derivatives |
| US9951027B2 (en) | 2014-02-11 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as MIDH1 inhibitors |
| PE20170143A1 (es) | 2014-02-11 | 2017-03-19 | Bayer Pharma AG | Benzimidazol-2-aminas como inhibidores de midh1 |
| EP3209660B1 (en) | 2014-10-23 | 2020-06-17 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors |
| JP6783756B2 (ja) | 2014-10-23 | 2020-11-11 | 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阻害剤としてのベンゾイミダゾール−２−アミン |
| US10370339B2 (en) | 2015-06-08 | 2019-08-06 | Bayer Pharma Aktiengesellschaft | N-Methylbenzimidazoles as mIDH1 inhibitors |
| WO2017005674A1 (en) | 2015-07-07 | 2017-01-12 | Bayer Pharma Aktiengesellschaft | 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 |
| 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 |
-
2016
- 2016-07-14 TW TW105122263A patent/TW201718513A/zh unknown
- 2016-07-25 US US15/748,027 patent/US10703727B2/en active Active
- 2016-07-25 AU AU2016299329A patent/AU2016299329B2/en not_active Ceased
- 2016-07-25 JP JP2018504195A patent/JP6787998B2/ja active Active
- 2016-07-25 WO PCT/EP2016/067614 patent/WO2017017046A1/en active Application Filing
- 2016-07-25 RU RU2018106948A patent/RU2018106948A/ru not_active Application Discontinuation
- 2016-07-25 EP EP16741641.1A patent/EP3328838A1/en not_active Withdrawn
- 2016-07-25 KR KR1020187005191A patent/KR20180030906A/ko unknown
- 2016-07-25 MX MX2018001204A patent/MX2018001204A/es unknown
- 2016-07-25 PE PE2018000132A patent/PE20181039A1/es unknown
- 2016-07-25 CN CN201680043928.5A patent/CN107848985B/zh active Active
- 2016-07-25 CA CA2993480A patent/CA2993480A1/en not_active Abandoned
- 2016-07-25 BR BR112018001535A patent/BR112018001535A2/pt not_active Application Discontinuation
- 2016-07-27 AR ARP160102275A patent/AR105494A1/es unknown
-
2018
- 2018-01-15 IL IL256926A patent/IL256926A/en unknown
- 2018-01-26 CL CL2018000241A patent/CL2018000241A1/es unknown
- 2018-01-26 CO CONC2018/0000795A patent/CO2018000795A2/es unknown
- 2018-09-21 HK HK18112179.8A patent/HK1252848A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3328838A1 (en) | 2018-06-06 |
| AR105494A1 (es) | 2017-10-11 |
| HK1252848A1 (zh) | 2019-06-06 |
| KR20180030906A (ko) | 2018-03-26 |
| CN107848985A (zh) | 2018-03-27 |
| AU2016299329A1 (en) | 2018-02-01 |
| CO2018000795A2 (es) | 2018-05-10 |
| TW201718513A (zh) | 2017-06-01 |
| RU2018106948A (ru) | 2019-08-27 |
| MX2018001204A (es) | 2018-04-24 |
| IL256926A (en) | 2018-03-29 |
| JP2018527328A (ja) | 2018-09-20 |
| US10703727B2 (en) | 2020-07-07 |
| CL2018000241A1 (es) | 2018-07-13 |
| US20180222871A1 (en) | 2018-08-09 |
| CN107848985B (zh) | 2021-09-03 |
| JP6787998B2 (ja) | 2020-11-18 |
| AU2016299329B2 (en) | 2020-08-13 |
| BR112018001535A2 (pt) | 2018-09-18 |
| WO2017017046A1 (en) | 2017-02-02 |
| CA2993480A1 (en) | 2017-02-02 |
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