PE20121471A1 - Derivados de sulfonamida heterociclicos utiles como inhibidores de mek - Google Patents
Derivados de sulfonamida heterociclicos utiles como inhibidores de mekInfo
- Publication number
- PE20121471A1 PE20121471A1 PE2012000608A PE2012000608A PE20121471A1 PE 20121471 A1 PE20121471 A1 PE 20121471A1 PE 2012000608 A PE2012000608 A PE 2012000608A PE 2012000608 A PE2012000608 A PE 2012000608A PE 20121471 A1 PE20121471 A1 PE 20121471A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halogen
- helpful
- heterocyclic sulfonamide
- mek inhibitors
- Prior art date
Links
- 229940124530 sulfonamide Drugs 0.000 title abstract 2
- 150000003456 sulfonamides Chemical class 0.000 title abstract 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- -1 CYANE Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- DTEYYLFSKSOIBO-UHFFFAOYSA-N 1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonic acid Chemical compound OCC(O)CC1(S(O)(=O)=O)CC1 DTEYYLFSKSOIBO-UHFFFAOYSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
Classifications
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- 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
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DERIVADO DE SULFONAMIDA HETEROCICLICO DE FORMULA (I) DONDE: R1a Y R1b SON HIDROXILO, CIANO, NITRO, ALQUILO C1-6, ALQUENILO C2-6, ENTRE OTROS; R2a ES H O ALQUILO C1-6; R2b ES ALQUILO C1-6, ALQUENILO C2-6, CICLOALQUILO, ARILO, ENTRE OTROS; R3 Y R4 SON H, ALQUILO C1-6, ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO POR HALOGENO, HIDROXIALQUILO C1-6 O ALCOXILO C1-6, R5 ES H, HALOGENO, ALQUILO C1-3 O ALQUILO C1-3 SUSTITUIDO POR HALOGENO; X ES -N(R6)-; R6 ES H O ALQUILO C1-6; W ES NR22, O O S. R22 ES H, ALQUILO C1-6, ALQUENILO C2-6, CICLOALQUILO, ARILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [7-(4-BROMO-2-FLUORO-FENIL-AMINO)-6-METIL-5-OXO-1,2,3,5-TETRAHIDRO-IMIDAZO-[1,2-a]-PIRIDIN-8-IL]-AMIDA DEL ACIDO CICLOPROPAN-SULFONICO; [7-(2-FLUORO-4-YODO-FENIL-AMINO)-6-METIL-5-OXO-1,2,3,5-TETRAHIDRO-IMIDAZO-[1,2-a]-PIRIDIN-8-IL]-AMIDA DEL ACIDO 1-(2,3-DIHIDROXI-PROPIL)-CICLOPROPAN-SULFONICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES INHIBIDOR DE LA PROTEINA CINASA DE MEK SIENDO UTIL EN EL TRATAMIENTO DE ENFERMEDADES HIPERPROLIFERATIVAS COMO CANCER E INFLAMACION
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2678CH2009 | 2009-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121471A1 true PE20121471A1 (es) | 2012-11-01 |
Family
ID=43416908
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000608A PE20121471A1 (es) | 2009-11-04 | 2010-11-02 | Derivados de sulfonamida heterociclicos utiles como inhibidores de mek |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US8466289B2 (es) |
| EP (1) | EP2496575B1 (es) |
| JP (1) | JP5466767B2 (es) |
| KR (1) | KR101398772B1 (es) |
| CN (1) | CN102596951B (es) |
| AR (1) | AR078900A1 (es) |
| AU (1) | AU2010317167B2 (es) |
| BR (1) | BR112012010519A2 (es) |
| CA (1) | CA2779935A1 (es) |
| CL (1) | CL2012001027A1 (es) |
| CO (1) | CO6541547A2 (es) |
| CR (1) | CR20120234A (es) |
| DO (1) | DOP2012000127A (es) |
| EA (1) | EA201200651A1 (es) |
| EC (1) | ECSP12011878A (es) |
| ES (1) | ES2487628T3 (es) |
| GT (1) | GT201200138A (es) |
| IL (1) | IL219113A0 (es) |
| MA (1) | MA33721B1 (es) |
| MX (1) | MX2012005293A (es) |
| MY (1) | MY156209A (es) |
| NI (1) | NI201200084A (es) |
| NZ (1) | NZ599565A (es) |
| PE (1) | PE20121471A1 (es) |
| PH (1) | PH12012500823A1 (es) |
| TN (1) | TN2012000153A1 (es) |
| TW (1) | TW201139449A (es) |
| UY (1) | UY33000A (es) |
| WO (1) | WO2011054828A1 (es) |
| ZA (1) | ZA201202530B (es) |
Families Citing this family (19)
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|---|---|---|---|---|
| EA201391820A1 (ru) * | 2011-06-09 | 2014-12-30 | Новартис Аг | Гетероциклические сульфонамидные производные |
| WO2014142660A1 (en) | 2013-03-12 | 2014-09-18 | Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis | Combinations of inhibitors of mek, egfr and erbb2 in the treatment of kras-mutant lung cancer and kras-mutant colon cancer |
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| US9629851B2 (en) | 2013-09-20 | 2017-04-25 | Stitching Het Nederlands Kanker Institut—Antoni Van Leeuwenhoek Ziekenhuis | ROCK in combination with MAPK pathway |
| WO2015041534A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | P90rsk in combination with raf/erk/mek |
| WO2015156674A2 (en) | 2014-04-10 | 2015-10-15 | Stichting Het Nederlands Kanker Instituut | Method for treating cancer |
| WO2015178770A1 (en) | 2014-05-19 | 2015-11-26 | Stichting Het Nederlands Kanker Instituut | Compositions for cancer treatment |
| EP3018131A1 (en) | 2014-11-07 | 2016-05-11 | Bayer Pharma Aktiengesellschaft | Synthesis of copanlisib and its dihydrochloride salt |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| CN106518885B (zh) * | 2016-10-26 | 2018-10-16 | 云南大学 | 1,3-二氮杂环并吡啶季铵盐类化合物及其中间体化合物、制备方法和应用 |
| KR20200110452A (ko) * | 2018-02-12 | 2020-09-23 | 어레이 바이오파마 인크. | 담도암을 치료하기 위한 방법 및 조합 요법 |
| WO2019197605A2 (en) | 2018-04-12 | 2019-10-17 | Umc Utrecht Holding B.V. | Drug combinations for use in the treatment of ras-mutant cancer |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN111548344B (zh) * | 2020-06-10 | 2025-01-28 | 北京深度制耀科技有限公司 | Stat3小分子抑制剂及其应用 |
| EP4375273A4 (en) * | 2021-07-21 | 2025-05-21 | Chugai Seiyaku Kabushiki Kaisha | Method for producing arylamide derivative |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
| CN119528775A (zh) * | 2024-08-05 | 2025-02-28 | 瑞博(苏州)制药有限公司 | 一种含环丁基的丙酸甲酯及丙二醇衍生物的合成方法 |
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2010
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