AR095311A1 - 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante - Google Patents
3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutanteInfo
- Publication number
- AR095311A1 AR095311A1 ARP140101012A ARP140101012A AR095311A1 AR 095311 A1 AR095311 A1 AR 095311A1 AR P140101012 A ARP140101012 A AR P140101012A AR P140101012 A ARP140101012 A AR P140101012A AR 095311 A1 AR095311 A1 AR 095311A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- haloalkyl
- cycloalkyl
- group
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
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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
- A61K31/535—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
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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
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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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuesto de la fórmula (1) en el tratamiento de enfermedades o trastornos asociados con tales proteínas IDH mutantes incluyendo pero sin limitar a, trastornos de proliferación celular como el cáncer. Reivindicación 1: Un compuesto de acuerdo a la fórmula (1) en donde R¹ es hidrógeno, metilo o etilo; R²ᵃ es hidrógeno, metilo o haloalquilo C₁₋₃; R²ᵇ es OH, halógeno, alcoxilo C₁₋₆, haloalquilo C₁₋₃, NH₂, NH(CH₃) o N(CH₃)₂; R³ y R⁴ son cada uno independientemente hidrógeno, metilo o etilo o R³ y R⁴ se unen formando ciclopropilo, ciclobutilo u oxetanilo; R⁵ y R⁶ son cada uno independientemente hidrógeno, deuterio, halógeno, -C(O)OCH₃, alquilo C₁₋₃ o haloalquilo C₁₋₃; R⁷ es un compuesto del grupo de fórmulas (2) en donde: el anillo A es un anillo de heteroarilo de 6 miembros que tiene de uno a tres átomos de nitrógeno; el anillo B es un anillo de heteroarilo de 5 miembros que tiene de uno a cuatro heteroátomos cada uno independientemente seleccionado del grupo que consiste en N, O y S; X es N o CH; cada R⁸ es independientemente hidrógeno, halógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, alcoxilo C₁₋₃ o haloalcoxilo C₁₋₃; n es 1 ó 2; R⁹ es hidrógeno, halógeno, haloalquilo C₁₋₃, alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heterocíclico de 5 ó 6 miembros opcionalmente sustituido, heteroarilo opcionalmente sustituido, -OR⁹ᵃ, -SO₂R⁹ᵃ, C(O)NHR⁹ᵃ, CH₂R⁹ᵇ o CHCH₃R⁹ᵇ, siempre y cuando X sea N, R⁹ sea hidrógeno, haloalquilo C₁₋₃, alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -SO₂R⁹ᵃ o C(O)NHR⁹ᵃ, en donde: dicho alquilo C₁₋₆ es opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en OH, fenilo y fenoxilo, y dicho cicloalquilo C₃₋₆, heterocíclico de 5 ó 6 miembros, arilo y heteroarilo son cada uno opcionalmente sustituidos por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en: halógeno, hidroxilo, ciano, -NRR, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxilo C₁₋₃, y haloalcoxilo C₁₋₃; R⁹ᵃ es un alquilo C₁₋₆ opcionalmente sustituido, haloalquilo C₁₋₆, cicloalquilo C₁₋₆ opcionalmente sustituido, fenilo opcionalmente sustituido, o heterocíclico opcionalmente sustituido, en donde: dicho alquilo C₁₋₆ se sustituye opcionalmente por un cicloalquilo C₃₋₆, dicho cicloalquilo C₃₋₆ y heterocíclico son cada uno opcionalmente sustituidos por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en: hidroxilo, CH₂OH, -NRR, ciano, alquilo C₁₋₃, haloalquilo C₁₋₃, y alcoxilo C₁₋₃, y dicho fenilo se sustituye opcionalmente por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en: halógeno, hidroxilo, ciano, -NRR, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxilo C₁₋₃, y haloalcoxilo C₁₋₃; R⁹ᵇ es cicloalquilo C₁₋₆ opcionalmente sustituido, fenilo opcionalmente sustituido o heterocíclico opcionalmente sustituido, dicho cicloalquilo C₃₋₆ y heterocíclico son cada uno opcionalmente sustituidos por uno a cuatro sustituyentes independientemente seleccionados del grupo que consiste en hidroxilo, CH₂OH, -NRR, -NRC(O)CH₃, heterocíclico de 4 a 6 miembros, ciano, halógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, y alcoxilo C₁₋₃, y dicho fenilo se sustituye opcionalmente por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en: halógeno, hidroxilo, ciano, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxilo C₁₋₃, y haloalcoxilo C₁₋₃; y cada R es independientemente seleccionado del grupo que consiste en H, alquilo C₁₋₃ y cicloalquilo C₃₋₆; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361783210P | 2013-03-14 | 2013-03-14 | |
| US201361892131P | 2013-10-17 | 2013-10-17 | |
| PCT/IB2014/059695 WO2014141104A1 (en) | 2013-03-14 | 2014-03-12 | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095311A1 true AR095311A1 (es) | 2015-10-07 |
Family
ID=50382516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101012A AR095311A1 (es) | 2013-03-14 | 2014-03-14 | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante |
Country Status (29)
| Country | Link |
|---|---|
| US (4) | US9434719B2 (es) |
| EP (1) | EP2970240B1 (es) |
| JP (1) | JP6387360B2 (es) |
| KR (1) | KR20150131224A (es) |
| CN (1) | CN105263929B (es) |
| AP (1) | AP2015008707A0 (es) |
| AR (1) | AR095311A1 (es) |
| AU (1) | AU2014229313B2 (es) |
| BR (1) | BR112015023412A8 (es) |
| CA (1) | CA2903979A1 (es) |
| CL (1) | CL2015002472A1 (es) |
| CR (1) | CR20150491A (es) |
| CU (1) | CU20150119A7 (es) |
| DO (1) | DOP2015000240A (es) |
| EA (1) | EA028033B1 (es) |
| ES (1) | ES2665619T3 (es) |
| GE (1) | GEP201706699B (es) |
| HK (1) | HK1213251A1 (es) |
| IL (1) | IL240972A0 (es) |
| MX (1) | MX355945B (es) |
| NI (1) | NI201500128A (es) |
| PE (1) | PE20151939A1 (es) |
| PH (1) | PH12015502018A1 (es) |
| SG (1) | SG11201507063YA (es) |
| TN (1) | TN2015000392A1 (es) |
| TW (1) | TW201444831A (es) |
| UY (1) | UY35470A (es) |
| WO (1) | WO2014141104A1 (es) |
| ZA (1) | ZA201506452B (es) |
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| WO2014141104A1 (en) | 2013-03-14 | 2014-09-18 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
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