AR078900A1 - Derivados de sulfonamida heterociclicos y composiciones farmaceuticas que los comprenden - Google Patents
Derivados de sulfonamida heterociclicos y composiciones farmaceuticas que los comprendenInfo
- Publication number
- AR078900A1 AR078900A1 ARP100104067A ARP100104067A AR078900A1 AR 078900 A1 AR078900 A1 AR 078900A1 AR P100104067 A ARP100104067 A AR P100104067A AR P100104067 A ARP100104067 A AR P100104067A AR 078900 A1 AR078900 A1 AR 078900A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- alkoxy
- amino
- alkynyl
- Prior art date
Links
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
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- 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
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- 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
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- 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 ha demostrado que los compuestos actuan como inhibidores de MEK, lo cual puede ser util en el tratamiento de enfermedades hiperproliferativas, como cáncer e inflamacion. Reivindicacion 1: Un compuesto de la formula (1) en donde X es -N(R6)-, en donde R6 es H o alquilo C1-6; R1a y R1b se seleccionan cada uno independientemente a partir de hidroxilo, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxilo C1-6, alqueniloxilo C2-6, alquiniloxilo C2-6, halogeno, alquilo C1-6-C(O)-, -C(O)OH, -C(O)-O-alquilo C1-6, amino, alquilo C1-6-NH-, di-alquilo C1-6-N-, alquilo C1-6-NH-C(O)-, di-alquilo C1-6-N-C(O)-, alquilo C1-6-C(O)-NH-, alquilo C1-6-C(O)-N-alquilo C1-6-, alquilo C1-6-SO2-NH-, alquilo C1-6-SO2-N-alquilo C1-6-, alquilo C1-6-S-, alquilo C1-6-S(O)-, alquilo C1-6-SO2-, NH2-SO2-, alquilo C1-6-NH-SO2- y di-alquilo C1-6-N-SO2-, en donde cada una de dichas fracciones de alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 está opcionalmente sustituida por uno o más sustituyentes, cada uno independientemente seleccionado a partir de halogeno, hidroxilo, alcoxilo C1-6, amino, alquilo C1-6-NH-, di-alquilo C1-6-N- o ciano; R2a es H o alquilo C1-6; R2b es una fraccion química seleccionada a partir de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, NR10R12, cicloalquilo, arilo, hetero-cicloalquilo, o heteroarilo, en donde esta fraccion química está opcionalmente sustituida por uno a tres sustituyentes, cada uno independientemente seleccionado a partir de halogeno, ciano, hidroxilo, alcoxilo C1-6, alqueniloxilo C2-6, alquiniloxilo C2-6, alquilo C1-6-S-, alquilo C1-6 sustituido por halogeno, amino, alquilo C1-6-NH-, di-alquilo C1-6-N-, HC(O)NH-, alquilo C1-6-C(O)NH-, HC(O)N-alquilo C1-6-, alquilo C1-6-C(O)-N-alquilo C1-6-, cicloalquilo monocíclico o hetero-cicloalquilo monocíclico, en donde este cicloalquilo y este hetero-cicloalquilo están opcionalmente sustituidos por uno o dos sustituyentes, cada uno independientemente seleccionado a partir de halogeno, ciano, hidroxilo, alcoxilo C1-6, alqueniloxilo C2-6, alquiniloxilo C2-6, alquilo C1-6-S-, halo-alquilo C1-6, amino, alquilo C1-6-NH-, di-alquilo C1-6-N-, HC(O)-NH-, alquilo C1-6-C(O)-NH-, HC(O)-N-alquilo C1-6-, o alquilo C1-6-C(O)-N-alquilo C1-6-; W es NR22, O, o S; R3 y R4 son cada uno independientemente H, alquilo C1-6, alquilo C1-6 sustituido por halogeno, hidroxi-alquilo C1-6, o alcoxilo C1-6; R5 es H, halogeno, alquilo C1-3, o alquilo C1-3 sustituido por halogeno; R10 y R12 son cada uno independientemente H, o una fraccion química seleccionada a partir de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C1-6-C(O)-, alcoxilo C1-6, cicloalquilo C3-14, arilo C6-14, cicloheteroalquilo de 4 a 14 miembros, o heteroarilo de 5 a 14 miembros, en donde cada una de estas fracciones químicas está opcionalmente sustituida por uno o más sustituyentes, cada uno independientemente seleccionado a partir de halogeno, hidroxilo, alcoxilo C1-6, amino, alquilo C1-6-amino, di-alquilo C1-6-amino, o ciano; y R22 es H, o una fraccion química seleccionada a partir de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo, arilo, hetero-cicloalquilo, aril-alquilo C1-6-, alquilo C1-6-aril-, o diaril-alquilo C1-6-, en donde cada una de estas fracciones químicas está opcionalmente sustituida por uno o más sustituyentes, cada uno independientemente seleccionado a partir de hidroxilo, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxilo C1-6, alqueniloxilo C2-6, alquiniloxilo C2-6, halogeno, alquilo C1-6-C(O)-, -C(O)OH, -C(O)-O-alquilo C1-6, amino, alquilo C1-6-NH-, di-alquilo C1-6-N-, alquilo C1-6-NH-C(O)-, di-alquilo C1-6-N-C(O)-, alquilo C1-6-C(O)-NH-, alquilo C1-6-C(O)-N-alquilo C1-6-, alquilo C1-6-SO2-NH-, alquilo C1-6-SO2-N-alquilo C1-6-alquilo C1-6-S-, alquilo C1-6-S(O)-, alquilo C1-6-SO2-, NH2-SO2-, alquilo C1-6-NH-SO2- y di-alquilo C1-6-N-SO2-, en donde cada una de dichas fracciones de alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 está opcionalmente sustituida por uno o más sustituyentes, cada uno independientemente seleccionado a partir de halogeno, hidroxilo, alcoxilo C1-6, amino, alquilo C1-6-NH-, di-alquilo C1-6-N-, o ciano; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2678CH2009 | 2009-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078900A1 true AR078900A1 (es) | 2011-12-14 |
Family
ID=43416908
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104067A AR078900A1 (es) | 2009-11-04 | 2010-11-03 | Derivados de sulfonamida heterociclicos y composiciones farmaceuticas que los comprenden |
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 (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2014DN00123A (es) * | 2011-06-09 | 2015-05-22 | Novartis Ag | |
| EP2968564B1 (en) | 2013-03-12 | 2019-05-08 | 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 |
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| EP3046557A1 (en) | 2013-09-20 | 2016-07-27 | Stichting Het Nederlands Kanker Instituut | 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 |
| US20170027940A1 (en) | 2014-04-10 | 2017-02-02 | 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 |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| 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 |
| 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 |
| 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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