AR108682A1 - Derivados de pirazol-3-iloxi ligandos del receptor sigma - Google Patents
Derivados de pirazol-3-iloxi ligandos del receptor sigmaInfo
- Publication number
- AR108682A1 AR108682A1 ARP170101529A ARP170101529A AR108682A1 AR 108682 A1 AR108682 A1 AR 108682A1 AR P170101529 A ARP170101529 A AR P170101529A AR P170101529 A ARP170101529 A AR P170101529A AR 108682 A1 AR108682 A1 AR 108682A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- aromatic
- nr8r9
- heterocyclyl
- Prior art date
Links
- 125000003118 aryl group Chemical group 0.000 abstract 11
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 150000002431 hydrogen 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
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 230000035755 proliferation Effects 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 229940044683 chemotherapy drug Drugs 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 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
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Para uso en reducir la proliferación de las células cancerosas y mejorar la eficacia de un fármaco quimioterápico. Reivindicación 1: Un compuesto para su uso en la reducción de la proliferación de células cancerosas, caracterizado porque el compuesto tiene la fórmula general (1), donde R¹ se selecciona a partir del grupo constituido por hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo no aromático sustituido o no sustituido, heterociclilo aromático sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹ y halógeno; R² se selecciona a partir del grupo constituido por hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo aromático o no aromático sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹ y halógeno; R³ y R⁴ se seleccionan independientemente a partir del grupo constituido por hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo aromático o no aromático, sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹, y halógeno, o juntos forman un sistema anular condensado sustituido opcionalmente; R⁵ y R⁶ se seleccionan independientemente a partir del grupo constituido por hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo aromático o no aromático, sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹, y halógeno, o juntos forman, con el átomo de nitrógeno al cual se encuentran unidos, un grupo heterociclilo aromático o no aromático, sustituido o no sustituido; n se selecciona entre 1, 2, 3, 4, 5, 6, 7 u 8; t es 1, 2 ó 3; R⁸ y R⁹ se seleccionan cada uno independientemente entre hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, heterociclilo aromático o no aromático, sustituido o no sustituido, alcoxi sustituido o no sustituido, ariloxi sustituido o no sustituido y halógeno; o una de sus sales, isómeros, profármacos o solvatos farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16382258 | 2016-06-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR108682A1 true AR108682A1 (es) | 2018-09-12 |
Family
ID=56134287
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170101529A AR108682A1 (es) | 2016-06-06 | 2017-06-05 | Derivados de pirazol-3-iloxi ligandos del receptor sigma |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20190142840A1 (es) |
| EP (1) | EP3463339B1 (es) |
| JP (1) | JP7094231B2 (es) |
| CN (1) | CN109310672B (es) |
| AR (1) | AR108682A1 (es) |
| ES (1) | ES2969815T3 (es) |
| TW (1) | TW201808300A (es) |
| WO (1) | WO2017211763A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7696199B2 (en) * | 2004-08-27 | 2010-04-13 | Laboratorios Del Dr. Esteve, S.A. | Sigma receptor inhibitors |
| GB0907973D0 (en) * | 2009-05-08 | 2009-06-24 | Modern Biosciences Plc | Combination therapy |
| EP2292236A1 (en) * | 2009-08-14 | 2011-03-09 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention or treatment of pain induced by chemotherapy |
| PH12012501027A1 (en) | 2009-11-25 | 2022-04-01 | Esteve Labor Dr | 4-[2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine salts |
| HUE029738T2 (en) | 2010-02-04 | 2017-04-28 | Esteve Labor Dr | 4- [2 - [[5-Methyl-1- (2-naphthalenyl) -1H-pyrazol-3-yl] oxy] ethyl] morpholine hydrochloride polymorphs and solvates |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
-
2017
- 2017-06-05 US US16/306,946 patent/US20190142840A1/en not_active Abandoned
- 2017-06-05 TW TW106118544A patent/TW201808300A/zh unknown
- 2017-06-05 EP EP17726968.5A patent/EP3463339B1/en active Active
- 2017-06-05 ES ES17726968T patent/ES2969815T3/es active Active
- 2017-06-05 WO PCT/EP2017/063614 patent/WO2017211763A1/en not_active Ceased
- 2017-06-05 JP JP2018564983A patent/JP7094231B2/ja active Active
- 2017-06-05 CN CN201780034885.9A patent/CN109310672B/zh active Active
- 2017-06-05 AR ARP170101529A patent/AR108682A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3463339C0 (en) | 2023-12-06 |
| TW201808300A (zh) | 2018-03-16 |
| CN109310672B (zh) | 2022-05-03 |
| WO2017211763A1 (en) | 2017-12-14 |
| CN109310672A (zh) | 2019-02-05 |
| EP3463339B1 (en) | 2023-12-06 |
| JP7094231B2 (ja) | 2022-07-01 |
| JP2019517572A (ja) | 2019-06-24 |
| US20190142840A1 (en) | 2019-05-16 |
| EP3463339A1 (en) | 2019-04-10 |
| ES2969815T3 (es) | 2024-05-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |