CO5611145A2 - Derivados de bencimidazol n3 alquilado como inhibidores mek - Google Patents
Derivados de bencimidazol n3 alquilado como inhibidores mekInfo
- Publication number
- CO5611145A2 CO5611145A2 CO04090140A CO04090140A CO5611145A2 CO 5611145 A2 CO5611145 A2 CO 5611145A2 CO 04090140 A CO04090140 A CO 04090140A CO 04090140 A CO04090140 A CO 04090140A CO 5611145 A2 CO5611145 A2 CO 5611145A2
- Authority
- CO
- Colombia
- Prior art keywords
- heteroaryl
- nr3r4
- heterocyclyl
- aryl
- cr4r5
- Prior art date
Links
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 3
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000005865 C2-C10alkynyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate 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
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
-
- 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
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- 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
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
1.- Un compuesto de la fórmula y sales farmacéuticamente aceptables, prodrogas y solvates de él, en donde:R1, R2, R9 y R10 se seleccionan independientemente de hidrógeno, halógeno, ciano, nitro, trifluorometilo, difluorometoxi, trifluorometoxi, azido, -OR3, -C(O)R3, -C(O)OR3, NR4C(O)OR6, -OC(O)R3, -NR4SO2R6, -SO2NR3R4, -NR4C(O)R3, -C(O)NR3R4, -NR5C(O)NR3R4, -NR5C (NCN) NR3R4, -NR3R4, yalquilo de C1-C10, alquenilo de C2-C10, alquinilo de C2-C10, cicloalquilo de C3-C10, ciclalquilalquilo de C3-C10, -S(O)j(alquilo de C1-C6), -S(O)j(CR4R5)m-arilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, -O(CR4R5)m-arilo, -NR4(CR4R5)m-arilo, -O(CR4R5)m-heteroarilo, -NR4(CR4R5)m-heteroarilo, -O(CR4R5)m-heterociclilo y -NR4(CR4R5)m-heterociclilo, donde cada porción de alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo y heterociclilo se sustituye optativamente con oxo, halógeno, ciano, nitro, trifluorometilo, difluorometoxi, trifluorometoxi, azido, -NR4SO2R6, -SO2NR3R4, -C(O)R3, -C(O)OR3, -OC(O)R3, -NR4C(O)OR6, -NR4C(O)R3, -C(O)NR3R4, -NR3R4, -NR5C(O) NR3R4, -NR5C(NCN) NR3R4, -OR3, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo;R3 se selecciona de hidrógeno, trifluorometilo, yalquilo de C1-C10, alquenilo de C2-C10, alquinilo de C2-C10, cicloalquilo de C3-C10, cicloalquilalquilo de C3-C10, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, yheterociclilalquilo, donde cada porción de alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo y heterociclilo se sustituye optativamente con uno a cinco grupos que se seleccionan independientemente de oxo, halógeno, ciano, nitro, trifluorometilo, difluorometoxi, trifluorometoxi, azido, -NR´SO2R´´´´, -SO2NRR´´, -C(O)R´, -C(O)OR´, -OC(O)R´, -NR´C(O)OR´´´´, -NRAND#39C(O)R´´, -C(O)NR´R´´, -SR´´´´, -S(O)R´´´´, -SO2R´, -NR´R´´, -NR´C(O)NR´´R´´´´, -NR´C(NCN)NR´´R´´´, -OR´, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo, y heterociclilquilo; ...
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36416402P | 2002-03-13 | 2002-03-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5611145A2 true CO5611145A2 (es) | 2006-02-28 |
Family
ID=28041882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO04090140A CO5611145A2 (es) | 2002-03-13 | 2004-09-10 | Derivados de bencimidazol n3 alquilado como inhibidores mek |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20030216460A1 (es) |
| EP (1) | EP1482944A4 (es) |
| JP (1) | JP2005526076A (es) |
| KR (1) | KR20040098013A (es) |
| CN (1) | CN1652792A (es) |
| AR (1) | AR038972A1 (es) |
| AU (1) | AU2003220202A1 (es) |
| CA (1) | CA2478534A1 (es) |
| CO (1) | CO5611145A2 (es) |
| DO (1) | DOP2003000614A (es) |
| IL (1) | IL163996A0 (es) |
| MX (1) | MXPA04008894A (es) |
| PA (1) | PA8569201A1 (es) |
| PL (1) | PL378635A1 (es) |
| RU (1) | RU2300528C2 (es) |
| TW (1) | TW200406203A (es) |
| UA (1) | UA76837C2 (es) |
| WO (1) | WO2003077855A2 (es) |
Families Citing this family (74)
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| US7235537B2 (en) * | 2002-03-13 | 2007-06-26 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
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| US7781595B2 (en) | 2003-09-22 | 2010-08-24 | S*Bio Pte Ltd. | Benzimidazole derivatives: preparation and pharmaceutical applications |
| US7732616B2 (en) * | 2003-11-19 | 2010-06-08 | Array Biopharma Inc. | Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof |
| ATE495155T1 (de) * | 2003-11-19 | 2011-01-15 | Array Biopharma Inc | Heterocyclische inhibitoren von mek |
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| NZ547327A (en) * | 2003-11-21 | 2009-08-28 | Array Biopharma Inc | AKT protein kinase inhibitors |
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| US20090030058A1 (en) * | 2005-12-21 | 2009-01-29 | Mohammed Pervez | Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer |
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| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
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| US6469009B1 (en) * | 1996-04-08 | 2002-10-22 | Ucb, S.A. | Pharmaceutical compositions for the treatment of rhinitis |
| US6506798B1 (en) * | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
| US6821963B2 (en) * | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| YU49401A (sh) * | 1999-01-13 | 2004-07-15 | Warner-Lambert Company | Benzoheterocikli i njihova upotreba kao inhibitori mek |
| ATE309205T1 (de) * | 1999-01-13 | 2005-11-15 | Warner Lambert Co | Benzenesulfonamid-derivative und ihre verwendung als mek-inhibitoren |
| IL147150A0 (en) * | 1999-07-16 | 2002-08-14 | Warner Lambert Co | Method for treating chronic pain using mek inhibitors |
-
2003
- 2003-03-13 JP JP2003575909A patent/JP2005526076A/ja active Pending
- 2003-03-13 KR KR10-2004-7014206A patent/KR20040098013A/ko not_active Withdrawn
- 2003-03-13 UA UA20040907721A patent/UA76837C2/uk unknown
- 2003-03-13 AR ARP030100888A patent/AR038972A1/es not_active Application Discontinuation
- 2003-03-13 TW TW092105719A patent/TW200406203A/zh unknown
- 2003-03-13 EP EP03716498A patent/EP1482944A4/en not_active Withdrawn
- 2003-03-13 MX MXPA04008894A patent/MXPA04008894A/es not_active Application Discontinuation
- 2003-03-13 PL PL378635A patent/PL378635A1/pl unknown
- 2003-03-13 CN CNA038107678A patent/CN1652792A/zh active Pending
- 2003-03-13 IL IL16399603A patent/IL163996A0/xx unknown
- 2003-03-13 US US10/387,682 patent/US20030216460A1/en not_active Abandoned
- 2003-03-13 PA PA20038569201A patent/PA8569201A1/es unknown
- 2003-03-13 WO PCT/US2003/007565 patent/WO2003077855A2/en not_active Ceased
- 2003-03-13 DO DO2003000614A patent/DOP2003000614A/es unknown
- 2003-03-13 AU AU2003220202A patent/AU2003220202A1/en not_active Abandoned
- 2003-03-13 RU RU2004127925/04A patent/RU2300528C2/ru not_active IP Right Cessation
- 2003-03-13 CA CA002478534A patent/CA2478534A1/en not_active Abandoned
-
2004
- 2004-09-10 CO CO04090140A patent/CO5611145A2/es not_active Application Discontinuation
-
2005
- 2005-10-25 US US11/258,398 patent/US20060106225A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| UA76837C2 (uk) | 2006-09-15 |
| KR20040098013A (ko) | 2004-11-18 |
| US20030216460A1 (en) | 2003-11-20 |
| EP1482944A4 (en) | 2006-04-19 |
| AU2003220202A1 (en) | 2003-09-29 |
| WO2003077855A3 (en) | 2004-03-04 |
| RU2004127925A (ru) | 2005-05-27 |
| TW200406203A (en) | 2004-05-01 |
| US20060106225A1 (en) | 2006-05-18 |
| RU2300528C2 (ru) | 2007-06-10 |
| MXPA04008894A (es) | 2005-06-20 |
| AR038972A1 (es) | 2005-02-02 |
| CN1652792A (zh) | 2005-08-10 |
| IL163996A0 (en) | 2005-12-18 |
| CA2478534A1 (en) | 2003-09-25 |
| PA8569201A1 (es) | 2004-05-21 |
| WO2003077855A2 (en) | 2003-09-25 |
| PL378635A1 (pl) | 2006-05-15 |
| DOP2003000614A (es) | 2009-09-30 |
| EP1482944A2 (en) | 2004-12-08 |
| JP2005526076A (ja) | 2005-09-02 |
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