AR108388A2 - Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas - Google Patents
Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasasInfo
- Publication number
- AR108388A2 AR108388A2 ARP170101175A ARP170101175A AR108388A2 AR 108388 A2 AR108388 A2 AR 108388A2 AR P170101175 A ARP170101175 A AR P170101175A AR P170101175 A ARP170101175 A AR P170101175A AR 108388 A2 AR108388 A2 AR 108388A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- independently selected
- inhibitors
- halo
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical group C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical class C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 102000020233 phosphotransferase Human genes 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- -1 -OR6 Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- 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
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- 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
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Abstract
Los compuestos son inhibidores de la actividad quinasa, en particular de la actividad de la Pl3-quinasa. Reivindicación 1: Un compuesto de fórmula (1), en la que: R¹ es un heteroarilo bicíclico de 9 ó 10 miembros, en el que el heteroarilo bicíclico de 9 ó 10 miembros contiene de uno a tres heteroátomos seleccionados de forma independiente de entre oxígeno y nitrógeno, y está sustituido opcionalmente con alquilo C₁₋₆, cicloalquilo C₃₋₆, halo, -CN o -NHSO₂R⁵, o piridinilo opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de entre alquilo C₁₋₆, -OR⁶, halo y -NHSO₂R⁷; R² y R³, junto con el átomo de nitrógeno al que están fijados, están unidos para formar un heterociclilo de 6 ó 7 miembros en el que el heterociclilo de 6 ó 7 miembros contiene, opcionalmente, un átomo de oxígeno u otro átomo de nitrógeno y está opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de alquilo C₁₋₆; R⁴ es hidrógeno o metilo; R⁶ es hidrógeno o alquilo C₁₋₄; y R⁵ y R⁷ son, cada uno de forma independiente, alquilo C₁₋₆ o fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de halo; o una sal de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17403309P | 2009-04-30 | 2009-04-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR108388A2 true AR108388A2 (es) | 2018-08-15 |
Family
ID=42225106
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101429A AR076435A1 (es) | 2009-04-30 | 2010-04-28 | Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos |
| ARP170101175A AR108388A2 (es) | 2009-04-30 | 2017-05-05 | Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101429A AR076435A1 (es) | 2009-04-30 | 2010-04-28 | Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos |
Country Status (40)
| Country | Link |
|---|---|
| US (14) | US20120046286A1 (es) |
| EP (3) | EP3260453B1 (es) |
| JP (1) | JP5570589B2 (es) |
| KR (2) | KR101679642B1 (es) |
| CN (1) | CN102459253B (es) |
| AR (2) | AR076435A1 (es) |
| AU (1) | AU2010243613B2 (es) |
| BR (1) | BRPI1016219B8 (es) |
| CA (1) | CA2759476C (es) |
| CL (1) | CL2011002706A1 (es) |
| CO (1) | CO6390057A2 (es) |
| CR (1) | CR20110603A (es) |
| CY (1) | CY1119515T1 (es) |
| DK (2) | DK2424864T3 (es) |
| DO (1) | DOP2011000328A (es) |
| EA (1) | EA021056B1 (es) |
| ES (3) | ES2531274T3 (es) |
| HK (2) | HK1165801A1 (es) |
| HR (2) | HRP20150173T1 (es) |
| HU (1) | HUE034724T2 (es) |
| IL (1) | IL215803A (es) |
| JO (1) | JO3025B1 (es) |
| LT (1) | LT2899191T (es) |
| MA (1) | MA33304B1 (es) |
| ME (2) | ME02053B (es) |
| MX (1) | MX2011011534A (es) |
| MY (1) | MY160454A (es) |
| NZ (1) | NZ596071A (es) |
| PE (1) | PE20120321A1 (es) |
| PL (2) | PL2424864T3 (es) |
| PT (2) | PT2899191T (es) |
| RS (2) | RS53830B1 (es) |
| SG (2) | SG175782A1 (es) |
| SI (2) | SI2424864T1 (es) |
| SM (2) | SMT201700481T1 (es) |
| TW (3) | TWI516487B (es) |
| UA (1) | UA101098C2 (es) |
| UY (1) | UY32585A (es) |
| WO (1) | WO2010125082A1 (es) |
| ZA (1) | ZA201107878B (es) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2280705B1 (en) | 2008-06-05 | 2014-10-08 | Glaxo Group Limited | Novel compounds |
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