PE20081354A1 - Compuestos de azaindolilo como inhibidores de mek - Google Patents
Compuestos de azaindolilo como inhibidores de mekInfo
- Publication number
- PE20081354A1 PE20081354A1 PE2007001679A PE2007001679A PE20081354A1 PE 20081354 A1 PE20081354 A1 PE 20081354A1 PE 2007001679 A PE2007001679 A PE 2007001679A PE 2007001679 A PE2007001679 A PE 2007001679A PE 20081354 A1 PE20081354 A1 PE 20081354A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- fluoro
- pyridine
- phenylamine
- carboxyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical class CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 abstract 2
- CUMTUBVTKOYYOU-UHFFFAOYSA-N 2-fluoro-4-iodoaniline Chemical compound NC1=CC=C(I)C=C1F CUMTUBVTKOYYOU-UHFFFAOYSA-N 0.000 abstract 1
- GZRMNMGWNKSANY-UHFFFAOYSA-N 4-bromo-2-fluoroaniline Chemical compound NC1=CC=C(Br)C=C1F GZRMNMGWNKSANY-UHFFFAOYSA-N 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical class C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001613 neoplastic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE AZAINDOLILO DE FORMULA (I), DONDE Z1 ES CR1 O N; Z2 ES CR2 O N; Z3 ES CR3 O N; Z4 ES CR4 O N; R1, R2, R3 Y R4 SON H, HALO, CN, CF3, NO2, ENTRE OTROS; W ES X1-NR5- O R11-O-; R5 Y R6 SON H O ALQUILO C1-C12; X1 ES R11, OR11, NR11R12, ENTRE OTROS; X2 ES ARILO, HETEROARILO, ENTRE OTROS; X3 ES H, (CR23R24)pR12, (CR23R24)qNR11R12, ENTRE OTROS; R11 Y R12 SON H, ALQUILO C1-C12, ALQUENILO C2-C8, ARILO, ENTRE OTROS; p ES 1, 2 O 3; q ES 2 O 3; R23 Y R24 SON H O ALQUILO OPCIONALMENTE SUSTITUIDO CON HALO, CIANO, NO2, OH, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ESTER ETILICO DEL ACIDO 3-(4-BROMO-2-FLUORO-FENILAMINO)-1-METIL-1H-PIRROLO[3,2-c]PIRIDINA-2-CARBOXILICO, ESTER ETILICO DEL ACIDO 3-(2-FLUORO-4-YODO-FENILAMINO)-1-METIL-1H-PIRROLO[3,2-c]PIRIDINA-2-CARBOXILICO, ESTER ETILICO DEL ACIDO 1-ETIL-3-(2-FLUORO-4-YODO-FENILAMINO)-1H-PIRROLO[3,2-c]PIRIDINA-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBIDORA DE LA QUINASA MEK Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEOPLASICAS Y/O INFLAMATORIAS
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86805506P | 2006-11-30 | 2006-11-30 | |
| US91762007P | 2007-05-11 | 2007-05-11 | |
| US94474307P | 2007-06-18 | 2007-06-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20081354A1 true PE20081354A1 (es) | 2008-11-14 |
Family
ID=39169665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007001679A PE20081354A1 (es) | 2006-11-30 | 2007-11-29 | Compuestos de azaindolilo como inhibidores de mek |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7855216B2 (es) |
| EP (1) | EP2099796B1 (es) |
| JP (1) | JP5211063B2 (es) |
| AR (1) | AR064031A1 (es) |
| AT (1) | ATE511509T1 (es) |
| AU (1) | AU2007325123B2 (es) |
| CA (1) | CA2672327A1 (es) |
| CL (1) | CL2007003444A1 (es) |
| DK (1) | DK2099796T3 (es) |
| PE (1) | PE20081354A1 (es) |
| PL (1) | PL2099796T3 (es) |
| PT (1) | PT2099796E (es) |
| TW (1) | TW200829586A (es) |
| WO (1) | WO2008067481A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2297070A2 (en) * | 2008-07-03 | 2011-03-23 | Bayer Schering Pharma Aktiengesellschaft | Compounds and processes for production of radiopharmaceuticals |
| JP5651125B2 (ja) | 2008-12-10 | 2015-01-07 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｍｅｋ阻害剤に対する耐性を付与するｍｅｋ突然変異 |
| MX360932B (es) | 2010-02-25 | 2018-11-21 | Dana Farber Cancer Inst Inc | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
| MX343368B (es) | 2010-03-09 | 2016-11-01 | The Broad Inst Inc * | Metodo de diagnostico y tratamiento de cancer en pacientes que tienen o desarrollan resistencia a una primera terapia de cancer. |
| SG10201505951VA (en) * | 2010-07-30 | 2015-08-28 | Oncotherapy Science Inc | Quinoline derivatives and melk inhibitors containing the same |
| WO2013169858A1 (en) | 2012-05-08 | 2013-11-14 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| UY34893A (es) | 2012-07-10 | 2014-02-28 | Takeda Pharmaceutical | Derivados de azaindol |
| AU2013337702A1 (en) | 2012-11-02 | 2015-05-21 | Merck Patent Gmbh | Method of reducing adverse effects in a cancer patient undergoing treatment with a MEK inhibitor |
| UA111925C2 (uk) | 2012-12-11 | 2016-06-24 | Федора Фармасьютікалз Інк. | БІЦИКЛІЧНІ СПОЛУКИ ТА ЇХ ВИКОРИСТАННЯ ЯК АНТИБАКТЕРІАЛЬНИХ АГЕНТІВ ТА ІНГІБІТОРІВ β-ЛАКТАМАЗИ |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| US20170114323A1 (en) | 2014-06-19 | 2017-04-27 | Whitehead Institute For Biomedical Research | Uses of kinase inhibitors for inducing and maintaining pluripotency |
| KR20180134347A (ko) | 2016-04-15 | 2018-12-18 | 제넨테크, 인크. | 암의 진단 및 치료 방법 |
| CN111065393B (zh) | 2017-05-19 | 2023-08-18 | 恩福莱克逊治疗有限公司 | 用于治疗皮肤疾病的吡咯并吡啶-苯胺类化合物 |
| CA3063535A1 (en) | 2017-05-19 | 2018-11-22 | Nflection Therapeutics, Inc. | Fused heteroaromatic-aniline compounds for treatment of dermal disorders |
| JP7530829B2 (ja) | 2017-09-08 | 2024-08-08 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | がんの診断及び治療方法 |
| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| CA3120352A1 (en) | 2018-11-20 | 2020-05-28 | Nflection Therapeutics, Inc. | Thienyl-aniline compounds for treatment of dermal disorders |
| CN113473978B (zh) | 2018-11-20 | 2025-03-28 | 恩福莱克逊治疗有限公司 | 用于治疗皮肤疾病氰基芳烃-苯胺化合物 |
| JP7393808B2 (ja) | 2018-11-20 | 2023-12-07 | エヌフレクション セラピューティクス インコーポレイテッド | 皮膚障害の処置のためのナフチリジノン－アニリン化合物 |
| US12371667B2 (en) | 2021-05-13 | 2025-07-29 | Washington University | Enhanced methods for inducing and maintaining naive human pluripotent stem cells |
| CN118591373A (zh) | 2021-11-23 | 2024-09-03 | 恩福莱克逊治疗有限公司 | 吡咯并吡啶-苯胺化合物的制剂 |
| CA3247162A1 (en) * | 2022-01-28 | 2023-08-03 | Insilico Medicine Ip Limited | Ectunocleotide pyrophosphatase-phosphodiesterase 1 (ENPP1) inhibitors and their uses |
| US20250171451A1 (en) * | 2022-03-04 | 2025-05-29 | Samjin Pharmaceutical Co., Ltd. | Novel heterocyclic compound and pharmaceutical composition comprising same |
| WO2024033381A1 (en) | 2022-08-10 | 2024-02-15 | Vib Vzw | Inhibition of tcf4/itf2 in the treatment of cancer |
| WO2025026383A1 (en) * | 2023-08-02 | 2025-02-06 | Insilico Medicine Ip Limited | Crytsalline forms of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp1) inhibitors and uses thereof |
| KR20250067072A (ko) * | 2023-11-07 | 2025-05-14 | 보로노이 주식회사 | 헤테로아릴 유도체 화합물 및 이의 용도 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7235537B2 (en) * | 2002-03-13 | 2007-06-26 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
| CA2483162C (en) * | 2002-04-23 | 2011-08-23 | Aventis Pharmaceuticals Inc. | Use of 3-substituted amino-1h-indole-2-carboxylic acid and 3-substituted amino benzo[b]thiophene-2-carboxylic acid derivatives as il-4 inhibitors |
| US6929411B2 (en) * | 2003-09-03 | 2005-08-16 | Hewlett-Packard Development Company, L.P. | Selectable control of raster image processor |
| GB0412914D0 (en) * | 2004-06-10 | 2004-07-14 | Oxagen Ltd | Compounds |
| US7598259B2 (en) * | 2004-06-15 | 2009-10-06 | Schering Corporation | mGluR1 antagonists as therapeutic agents |
| AR049300A1 (es) * | 2004-06-15 | 2006-07-12 | Schering Corp | Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos |
| DE102005013621A1 (de) * | 2005-03-24 | 2006-09-28 | Curacyte Discovery Gmbh | Substituierte 2-Aryl(Hetaryl)-5-aminothieno[2,3-d]pyrimidin-6-carbonsäureamide, Verfahren zu ihrer Herstellung und Verwendung als Pharmazeutika |
| AR070127A1 (es) * | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
-
2007
- 2007-11-29 PT PT07854844T patent/PT2099796E/pt unknown
- 2007-11-29 PL PL07854844T patent/PL2099796T3/pl unknown
- 2007-11-29 AT AT07854844T patent/ATE511509T1/de active
- 2007-11-29 US US11/947,656 patent/US7855216B2/en not_active Expired - Fee Related
- 2007-11-29 TW TW096145474A patent/TW200829586A/zh unknown
- 2007-11-29 CA CA002672327A patent/CA2672327A1/en not_active Abandoned
- 2007-11-29 CL CL200703444A patent/CL2007003444A1/es unknown
- 2007-11-29 AR ARP070105307A patent/AR064031A1/es unknown
- 2007-11-29 AU AU2007325123A patent/AU2007325123B2/en not_active Ceased
- 2007-11-29 EP EP07854844A patent/EP2099796B1/en active Active
- 2007-11-29 DK DK07854844.3T patent/DK2099796T3/da active
- 2007-11-29 JP JP2009539490A patent/JP5211063B2/ja not_active Expired - Fee Related
- 2007-11-29 PE PE2007001679A patent/PE20081354A1/es not_active Application Discontinuation
- 2007-11-29 WO PCT/US2007/085962 patent/WO2008067481A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP5211063B2 (ja) | 2013-06-12 |
| ATE511509T1 (de) | 2011-06-15 |
| AU2007325123B2 (en) | 2012-12-13 |
| EP2099796A1 (en) | 2009-09-16 |
| WO2008067481A1 (en) | 2008-06-05 |
| PT2099796E (pt) | 2011-09-06 |
| AR064031A1 (es) | 2009-03-04 |
| CL2007003444A1 (es) | 2008-06-27 |
| TW200829586A (en) | 2008-07-16 |
| US7855216B2 (en) | 2010-12-21 |
| EP2099796B1 (en) | 2011-06-01 |
| PL2099796T3 (pl) | 2011-10-31 |
| JP2010511626A (ja) | 2010-04-15 |
| US20080242655A1 (en) | 2008-10-02 |
| CA2672327A1 (en) | 2008-06-05 |
| HK1135099A1 (en) | 2010-05-28 |
| AU2007325123A1 (en) | 2008-06-05 |
| DK2099796T3 (da) | 2011-09-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |