AR089807A1 - Compuestos de imidazopirrolidinona - Google Patents
Compuestos de imidazopirrolidinonaInfo
- Publication number
- AR089807A1 AR089807A1 ARP130100227A ARP130100227A AR089807A1 AR 089807 A1 AR089807 A1 AR 089807A1 AR P130100227 A ARP130100227 A AR P130100227A AR P130100227 A ARP130100227 A AR P130100227A AR 089807 A1 AR089807 A1 AR 089807A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- nr9r10
- optionally substituted
- independently selected
- halo
- Prior art date
Links
Classifications
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- 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
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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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
- A61K31/395—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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Compuestos en el tratamiento de un trastorno o una enfermedad mediada por la actividad de MDM2 y/o MDM4, y composiciones que comprenden tales compuestos. Los compuestos de la presente se utilizan como agentes antineoplasicos. Reivindicación 1: Un compuesto de la fórmula (1) o una sal del mismo, en donde A se selecciona a partir del grupo de formulas (2); B se selecciona a partir del grupo de formulas (3); cada R¹ se selecciona independientemente a partir de halo y metilo; R² se selecciona a partir de cloro, fluoro, trifluorometilo, metilo y ciano; R³ se selecciona a partir de isopropilo, ciclopropilo, isobutilo, ciclobutilo y ciclopentilo, o R³ es un resto de formula (4), en donde R²² se selecciona a partir de OH, OCH₃, NH₂, NHMe, NMe₂, NHCOMe y NHCOH; R⁴ se selecciona a partir del grupo de formulas (5), en donde R¹⁵ se selecciona independientemente a partir de OCH₃, CH₂CH₃, OH, OCF₃ y H; R¹⁶ se selecciona a partir de H, -O-alquilo C₁₋₄, halo, OCF₃, CN, -C(O)NR⁹R¹⁰, -C(O)-morfolinil-4-ilo, hidroxi-azetidin-1-il-carbonilo, -CH₂NR⁹R¹⁰, -CH₂NR⁹-C(O)R¹⁰, CH₂CN, metil-imidazolil-, -CH₂C(O)NR⁹R¹⁰, -CH₂C(O)OH, -C(O)OH, -CH₂C(O)O-alquilo C₁₋₄, -N(R⁹)-C(O)-alquilo C₁₋₄, -NR⁹R¹⁰ y alquilo C₁₋₄ opcionalmente sustituido por 1 ó 2 OH; R¹⁷ se selecciona a partir de H, -O-alquilo C₁₋₄, -CH₂C(O)NR⁹R¹⁰, -CH₂C(O)O-alquilo C₁₋₄, -CH₂C(O)OH, -NR⁹R¹⁰, -C(O)NR⁹R¹⁰, -CH₂NR⁹R¹⁰, -C(O)OCH₃ y -CH₂CN; R¹⁸ se selecciona a partir de H, -O-alquilo C₁₋₄, OH, CH₂NR⁹R¹⁰, -NR⁹R¹⁰ y azetidin-1-ilo, dicho azetidin-1-ilo es sustituido por OH o ambos CH₃ y OH; R¹⁹ se selecciona a partir de H, -O-alquilo C₁₋₄, alquilo C₁₋₄, -NR⁹R¹⁰, -N(R⁹)-C(O)alquilo C₁₋₄ y -C(O)NR⁹R¹⁰; R²⁰ se selecciona a partir de H, CH₃ y -CH₂CH₃; R²¹ se selecciona a partir de -NR⁹R¹⁰, -CH₂NR⁹R¹⁰, C(O)NR⁹R¹⁰ y CN; R⁵ se selecciona a partir de: H, heterociclilo¹-C(O)-(CH₂)ₙ-, alquilo C₁₋₄-, dicho alquilo C₁₋₄ opcionalmente sustituido por 1 ó 2 sustituyentes independientemente seleccionados a partir de OH, =O, heterociclilo¹-alquilo C₁₋₄-, en donde dicho alquilo de heterociclilo¹-alquilo C₁₋₄- es opcionalmente sustituido por 1 ó 2 OH, y dicho heterociclilo¹ puede ser opcionalmente sustituido por metilo o etilo, alquilo C₁₋₄-OC(O)(CH₂)ₘ-, y ciano; R⁶ se selecciona a partir de: H, alquilo C₁₋₄-, opcionalmente sustituido por alcoxilo C₁₋₄, alcoxilo C₁₋₄, opcionalmente sustituido por alcoxilo C₁₋₄, alcoxi C₁₋₄alcoxi C₁₋₄alquilo C₁₋₄-, halo, R⁹(R¹⁰)N-C(O)-(CH₂)ₘ-, ciano, R⁹(R¹⁰)N-(CH₂)ₘ-, R⁹(R¹⁰)N-(CH₂)ₙ-O-(CH₂)ₘ-, alquilo C₁₋₄-C(O)-(R¹⁰)N-(CH₂)ₘ-, -O-(CH₂)ₚ-heteroarilo²; R⁷ se selecciona a partir de: H, halo, y alquilo C₁₋₄-, opcionalmente sustituido por alcoxilo C₁₋₄; cada R⁸ se selecciona independientemente a partir de H, metilo, etilo, hidroxietilo y metoxietilo-, en donde dicho metilo o etilo es opcionalmente sustituido por 1, 2 ó 3 sustituyentes fluoro; cada R⁹ se selecciona independientemente a partir de H, metilo o etilo; cada R¹⁰ se selecciona independientemente a partir de H y alquilo C₁₋₄ en donde dicho alquilo C₁₋₄ es opcionalmente sustituido por 1 ó 2 sustituyentes independientemente seleccionados a partir de metoxilo, etoxilo, hidroxilo y halo; o R⁹ y R¹⁰, junto con el átomo N al cual están unidos, pueden formar un anillo heterocíclico saturado de 5 ó 6 miembros que comprende además átomos de carbono cíclicos y opcionalmente un heteroátomo cíclico independientemente seleccionado a partir de N, O y S, y en donde, cuando el anillo contiene un átomo S, dicho S es opcionalmente sustituido por uno o dos sustituyentes oxo; R¹¹ es H, alquilo C₁₋₄, alcoxilo C₁₋₄ o halo; R¹² es H o halo; R¹³ se selecciona a partir de NH₂, -C(O)OH, -NH(C(O)-CH₃) y -C(O)-NH(CH₃); R¹⁴ se selecciona a partir de -C(O)-NR⁹(R¹⁰), alquilo C₁₋₄, -C(O)-alquilo C₁₋₄, -C(O)O-alquilo C₁₋₄; cada R²³ se selecciona independientemente a partir de H, halo, ciclopropilo y alquilo C₁₋₄; n es 1, 2 ó 3; d es 0, 1, 2, ó 3; heterociclilo¹ es un grupo monocíclico completamente saturado o parcialmente saturado de 3, 4, 5 ó 6 miembros que comprende átomos de carbono cíclicos y 1 ó 2 heteroátomos cíclicos independientemente seleccionado a partir de N, O y S; heteroarilo² es un grupo monocíclico completamente insaturado de 5 ó 6 miembros que comprende átomos de carbono cíclicos y 1, 2, 3 ó 4 heteroátomos cíclicos independientemente seleccionados a partir de N, O y S, en donde el número total de átomos de S cíclicos no excede 1, y el número total de átomos de O cíclicos no excede 1; y m es 0, 1 ó 2; * indica el punto de fijación al resto de la molécula.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261591001P | 2012-01-26 | 2012-01-26 | |
| US201261669902P | 2012-07-10 | 2012-07-10 | |
| CNPCT/CN2012/086703 | 2012-12-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089807A1 true AR089807A1 (es) | 2014-09-17 |
Family
ID=47997596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100227A AR089807A1 (es) | 2012-01-26 | 2013-01-25 | Compuestos de imidazopirrolidinona |
Country Status (45)
Families Citing this family (84)
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