AR128267A1 - Derivados de azaindol y su uso como inhibidores de la erk-quinasa - Google Patents
Derivados de azaindol y su uso como inhibidores de la erk-quinasaInfo
- Publication number
- AR128267A1 AR128267A1 ARP230100088A ARP230100088A AR128267A1 AR 128267 A1 AR128267 A1 AR 128267A1 AR P230100088 A ARP230100088 A AR P230100088A AR P230100088 A ARP230100088 A AR P230100088A AR 128267 A1 AR128267 A1 AR 128267A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- compound
- erk
- alkyl group
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 101000876610 Dictyostelium discoideum Extracellular signal-regulated kinase 2 Proteins 0.000 abstract 1
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 abstract 1
- 101001052493 Homo sapiens Mitogen-activated protein kinase 1 Proteins 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
- C07D213/643—2-Phenoxypyridines; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/027—Organoboranes and organoborohydrides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicación 1: Compuesto de la fórmula (1) en donde: R¹ representa un grupo alquilo (C₁-C₆); R² representa un grupo alquilo (C₁-C₆), un grupo cicloalquilo (C₃-C₆), o un grupo alquilo (C₁-C₆) sustituido por uno o más radicales seleccionados de átomos de halógeno, grupo ciano, grupo alcoxi (C₁-C₆) y grupo cicloalquilo (C₃-C₆); o R¹ y R² forman junto con el átomo de nitrógeno un grupo heterocíclico de 3 a 6 miembros; R³, R⁴, R⁵, R⁶, R⁷, R⁸ y R⁹ representan, independientemente entre sí, un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo (C₁-C₆), un grupo trifluorometilo o un grupo ciano, en donde dicho grupo alquilo (C₁-C₆) está opcionalmente sustituido con un grupo alcoxi (C₁-C₆); o una de sus sales farmacéuticamente aceptables. Reivindicación 16: Compuesto de acuerdo con cualquiera de las reivindicaciones anteriores, para uso en la prevención y/o inhibición y/o tratamiento de una enfermedad o condición mediada por actividad de quinasas ERK, en particular por actividad de quinasas ERK2. Reivindicación 17: Compuesto para uso de acuerdo con la reivindicación 16, en donde la enfermedad o el estado se selecciona de cánceres y metástasis.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP22305031.1A EP4212531A1 (en) | 2022-01-14 | 2022-01-14 | Azaindole derivatives and their use as erk kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR128267A1 true AR128267A1 (es) | 2024-04-10 |
Family
ID=80445694
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP230100088A AR128267A1 (es) | 2022-01-14 | 2023-01-13 | Derivados de azaindol y su uso como inhibidores de la erk-quinasa |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11827637B2 (es) |
| EP (2) | EP4212531A1 (es) |
| JP (1) | JP2025502377A (es) |
| KR (1) | KR20240134887A (es) |
| CN (1) | CN118541370A (es) |
| AR (1) | AR128267A1 (es) |
| AU (1) | AU2023207276A1 (es) |
| CL (1) | CL2024002070A1 (es) |
| CO (1) | CO2024008809A2 (es) |
| IL (1) | IL314199A (es) |
| MX (1) | MX2024008629A (es) |
| TW (1) | TW202334147A (es) |
| WO (1) | WO2023135233A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4212531A1 (en) * | 2022-01-14 | 2023-07-19 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
| WO2025012389A1 (en) * | 2023-07-12 | 2025-01-16 | Agv Discovery | Salts of (s)-1-(1-(3-chlorophenyl)-2-(dimethylamino)ethyl)-4-(5- morpholino-1h-pyrrolo[2,3-b]pyridin-3-yl)pyridin-2(1h)-one, their preparation and their use as erk kinase inhibitors |
| WO2025012386A1 (en) * | 2023-07-12 | 2025-01-16 | Agv Discovery | Crystalline form of (s)-1-(1-(3-chlorophenyl)-2- (dimethylamino)ethyl)-4-(5-morpholino-1h-pyrrolo[2,3- b]pyridin-3-yl)pyridin-2(1h)-one, its preparation and its use as erk kinase inhibitor |
| WO2025012357A1 (en) * | 2023-07-12 | 2025-01-16 | Ipsen Pharma | Fluorinated azaindole derivatives and their use as erk kinase inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI339206B (en) | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| RU2376299C2 (ru) | 2004-05-14 | 2009-12-20 | Вертекс Фармасьютикалз, Инкорпорейтед | Пиррольные соединения в качестве ингибиторов erk протеинкиназ, их синтез и промежуточные соединения |
| US7361764B2 (en) | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| CN100396678C (zh) | 2004-11-16 | 2008-06-25 | 财团法人工业技术研究院 | 1-苯甲基-3-(5’-羟甲基-2’-呋喃基)吲唑的吲哚类似物的合成及用途 |
| ES2431466T3 (es) | 2006-06-30 | 2013-11-26 | Sunesis Pharmaceuticals, Inc. | Inhibidores de piridinonil pdk1 |
| CN101790527A (zh) | 2006-07-20 | 2010-07-28 | 凯利普西斯公司 | Rho激酶的苯并噻吩抑制剂 |
| CN101605779B (zh) | 2006-12-15 | 2013-11-20 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物 |
| WO2012094313A1 (en) | 2011-01-04 | 2012-07-12 | Kinentia Biosciences Llc | Pyrazole derivatives as erk inhibitors |
| EP2739143B1 (en) | 2011-08-05 | 2018-07-11 | Gary A. Flynn | Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors |
| JO3215B1 (ar) | 2012-08-09 | 2018-03-08 | Phenex Pharmaceuticals Ag | حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy |
| WO2014060395A1 (en) | 2012-10-16 | 2014-04-24 | F. Hoffmann-La Roche Ag | Serine/threonine kinase inhibitors |
| GB2515785A (en) | 2013-07-03 | 2015-01-07 | Redx Pharma Ltd | Compounds |
| JP2018502853A (ja) | 2015-01-23 | 2018-02-01 | コンフルエンス・ライフ・サイエンシズ，インコーポレーテッド | 炎症およびがんを処置するための複素環式ｉｔｋ阻害剤 |
| EP3170822A1 (en) | 2015-11-18 | 2017-05-24 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
| MX2021005171A (es) * | 2018-11-16 | 2021-10-01 | California Inst Of Techn | Inhibidores de cinasas reguladas por señal extracelular (erk) y usos de los mismos. |
| EP4212531A1 (en) * | 2022-01-14 | 2023-07-19 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
-
2022
- 2022-01-14 EP EP22305031.1A patent/EP4212531A1/en not_active Withdrawn
- 2022-12-30 TW TW111150950A patent/TW202334147A/zh unknown
-
2023
- 2023-01-13 CN CN202380016949.8A patent/CN118541370A/zh active Pending
- 2023-01-13 JP JP2024542357A patent/JP2025502377A/ja active Pending
- 2023-01-13 EP EP23700812.3A patent/EP4463453A1/en active Pending
- 2023-01-13 IL IL314199A patent/IL314199A/en unknown
- 2023-01-13 KR KR1020247023085A patent/KR20240134887A/ko active Pending
- 2023-01-13 WO PCT/EP2023/050692 patent/WO2023135233A1/en active Application Filing
- 2023-01-13 US US18/096,996 patent/US11827637B2/en active Active
- 2023-01-13 AU AU2023207276A patent/AU2023207276A1/en active Pending
- 2023-01-13 AR ARP230100088A patent/AR128267A1/es unknown
- 2023-01-13 MX MX2024008629A patent/MX2024008629A/es unknown
- 2023-10-06 US US18/377,633 patent/US20240308997A1/en active Pending
-
2024
- 2024-07-03 CO CONC2024/0008809A patent/CO2024008809A2/es unknown
- 2024-07-09 CL CL2024002070A patent/CL2024002070A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20230227451A1 (en) | 2023-07-20 |
| US20240308997A1 (en) | 2024-09-19 |
| CN118541370A (zh) | 2024-08-23 |
| JP2025502377A (ja) | 2025-01-24 |
| EP4463453A1 (en) | 2024-11-20 |
| TW202334147A (zh) | 2023-09-01 |
| MX2024008629A (es) | 2024-08-19 |
| CO2024008809A2 (es) | 2024-08-08 |
| US11827637B2 (en) | 2023-11-28 |
| KR20240134887A (ko) | 2024-09-10 |
| AU2023207276A1 (en) | 2024-08-01 |
| IL314199A (en) | 2024-09-01 |
| EP4212531A1 (en) | 2023-07-19 |
| WO2023135233A1 (en) | 2023-07-20 |
| CL2024002070A1 (es) | 2024-11-29 |
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