MX2018001204A - 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 sustituido.Info
- Publication number
- MX2018001204A MX2018001204A MX2018001204A MX2018001204A MX2018001204A MX 2018001204 A MX2018001204 A MX 2018001204A MX 2018001204 A MX2018001204 A MX 2018001204A MX 2018001204 A MX2018001204 A MX 2018001204A MX 2018001204 A MX2018001204 A MX 2018001204A
- Authority
- MX
- Mexico
- Prior art keywords
- cyclohexyl
- propanoic acid
- anilino
- acid derivatives
- hydrogen atom
- Prior art date
Links
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical class COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical class 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- WYDYPIFUWLGBTD-UHFFFAOYSA-N 3-(2-anilino-1-cyclohexylbenzimidazol-5-yl)propanoic acid Chemical class N(C1=CC=CC=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)CCC(=O)O WYDYPIFUWLGBTD-UHFFFAOYSA-N 0.000 abstract 2
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- RNMAUIMMNAHKQR-QFBILLFUSA-N 3-[2-[4-(trifluoromethoxy)anilino]-1-[(1R,5R)-3,3,5-trimethylcyclohexyl]benzimidazol-5-yl]propanoic acid Chemical compound FC(OC1=CC=C(C=C1)NC1=NC2=C(N1[C@H]1CC(C[C@H](C1)C)(C)C)C=CC(=C2)CCC(=O)O)(F)F RNMAUIMMNAHKQR-QFBILLFUSA-N 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se relaciona con un método para preparar derivados de ácido 3-(2-anilino-1-ciclohexil-1H-bencimidazol-5-il) propanoico sustituido de la fórmula general (I) (ver Fórmula) en la cual R1 representa un átomo de hidrógeno o R1 representa un grupo que se selecciona de la serie de alquil C1-C3-, alcoxi C1-C3-, haloalquil C1-C3- y haloalcoxi C1-C3-, R2 representa un átomo de hidrógeno o un grupo alquilo C1-C3, R3 representa un átomo de hidrógeno o un grupo alquilo C1-C3, R4 representa un grupo ciclohexilo, el cual está sustituido opcionalmente de manera simple o múltiple por un grupo alquilo C1-C3, y R5 representa un átomo de hidrógeno o un grupo alquilo C1-C6; y también intermediarios que pueden usarse para preparar derivados del ácido 3-(2-anilino-1-ciclohexil-1H-bencimidazol-5-il)propanoic o sustituido. La presente invención también se relaciona con una forma cristalina del ácido 3-(2-{[4-(trifluorometoxi)fenil]amino}- 1-[(1R,5R)-3,3,5-trimetilciclohexil]-1H-bencimidazol-5-il)propano ico, composiciones farmacéuticas que comprenden esta forma cristalina, y también el uso de esta forma cristalina para preparar un medicamento para el tratamiento de una enfermedad.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15178413 | 2015-07-27 | ||
| PCT/EP2016/067614 WO2017017046A1 (en) | 2015-07-27 | 2016-07-25 | Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1h-benzimidazol-5-yl)propanoic acid derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2018001204A true MX2018001204A (es) | 2018-04-24 |
Family
ID=53758091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018001204A MX2018001204A (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 |
|---|---|---|---|---|
| SG11201605810WA (en) | 2014-02-11 | 2016-08-30 | Bayer Pharma AG | Benzimidazol-2-amines as midh1 inhibitors |
| US9951027B2 (en) | 2014-02-11 | 2018-04-24 | 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 |
| JP6830909B2 (ja) | 2015-06-08 | 2021-02-17 | 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Ｎ−メンチルベンズイミダゾール |
| ES2877424T3 (es) | 2015-07-07 | 2021-11-16 | Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts | 2-Aril- y 2-arilalquil-bencimidazoles como inhibidores de MIDH1 |
| 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 |
| US20210113598A1 (en) | 2017-08-01 | 2021-04-22 | Deutsches Krebsforschungszentrum (DKFZ) Stiftung des öffentlichen Rechts | Combination of MIDH1 Inhibitors and DNA Hypomethylating Agents (HMA) |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104219954B (zh) | 2009-06-23 | 2017-03-22 | 翻译基因组学研究院 | 苯甲酰胺衍生物 |
| SG11201605810WA (en) | 2014-02-11 | 2016-08-30 | Bayer Pharma AG | Benzimidazol-2-amines as midh1 inhibitors |
| US9951027B2 (en) | 2014-02-11 | 2018-04-24 | 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 |
| JP6830909B2 (ja) * | 2015-06-08 | 2021-02-17 | 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Ｎ−メンチルベンズイミダゾール |
| ES2877424T3 (es) | 2015-07-07 | 2021-11-16 | Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts | 2-Aril- y 2-arilalquil-bencimidazoles como inhibidores de MIDH1 |
| 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 |
-
2016
- 2016-07-14 TW TW105122263A patent/TW201718513A/zh unknown
- 2016-07-25 CN CN201680043928.5A patent/CN107848985B/zh not_active Expired - Fee Related
- 2016-07-25 AU AU2016299329A patent/AU2016299329B2/en not_active Ceased
- 2016-07-25 MX MX2018001204A patent/MX2018001204A/es unknown
- 2016-07-25 PE PE2018000132A patent/PE20181039A1/es unknown
- 2016-07-25 KR KR1020187005191A patent/KR20180030906A/ko not_active Withdrawn
- 2016-07-25 HK HK18112179.8A patent/HK1252848A1/zh unknown
- 2016-07-25 JP JP2018504195A patent/JP6787998B2/ja not_active Expired - Fee Related
- 2016-07-25 EP EP16741641.1A patent/EP3328838A1/en not_active Withdrawn
- 2016-07-25 US US15/748,027 patent/US10703727B2/en not_active Expired - Fee Related
- 2016-07-25 CA CA2993480A patent/CA2993480A1/en not_active Abandoned
- 2016-07-25 WO PCT/EP2016/067614 patent/WO2017017046A1/en not_active Ceased
- 2016-07-25 BR BR112018001535A patent/BR112018001535A2/pt not_active Application Discontinuation
- 2016-07-25 RU RU2018106948A patent/RU2018106948A/ru 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 CO CONC2018/0000795A patent/CO2018000795A2/es unknown
- 2018-01-26 CL CL2018000241A patent/CL2018000241A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20180222871A1 (en) | 2018-08-09 |
| PE20181039A1 (es) | 2018-07-03 |
| AR105494A1 (es) | 2017-10-11 |
| WO2017017046A1 (en) | 2017-02-02 |
| AU2016299329A1 (en) | 2018-02-01 |
| JP2018527328A (ja) | 2018-09-20 |
| RU2018106948A (ru) | 2019-08-27 |
| EP3328838A1 (en) | 2018-06-06 |
| CL2018000241A1 (es) | 2018-07-13 |
| CA2993480A1 (en) | 2017-02-02 |
| US10703727B2 (en) | 2020-07-07 |
| IL256926A (en) | 2018-03-29 |
| CN107848985B (zh) | 2021-09-03 |
| AU2016299329B2 (en) | 2020-08-13 |
| CO2018000795A2 (es) | 2018-05-10 |
| BR112018001535A2 (pt) | 2018-09-18 |
| HK1252848A1 (zh) | 2019-06-06 |
| JP6787998B2 (ja) | 2020-11-18 |
| TW201718513A (zh) | 2017-06-01 |
| CN107848985A (zh) | 2018-03-27 |
| KR20180030906A (ko) | 2018-03-26 |
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