AR081797A1 - Derivados de pirrolidinona heteroaromaticas fusionadas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar afecciones del sistema inmune y la inflamacion - Google Patents
Derivados de pirrolidinona heteroaromaticas fusionadas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar afecciones del sistema inmune y la inflamacionInfo
- Publication number
- AR081797A1 AR081797A1 ARP100104923A AR081797A1 AR 081797 A1 AR081797 A1 AR 081797A1 AR P100104923 A ARP100104923 A AR P100104923A AR 081797 A1 AR081797 A1 AR 081797A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- alkyl
- inflammation
- heteroaryl
- halo
- Prior art date
Links
- 206010061218 Inflammation Diseases 0.000 title 2
- 230000004054 inflammatory process Effects 0.000 title 2
- 210000000987 immune system Anatomy 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 125000000262 haloalkenyl group Chemical group 0.000 abstract 3
- 125000000232 haloalkynyl group Chemical group 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- -1 C1- alkyl 6 Chemical group 0.000 abstract 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- 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
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- Otolaryngology (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o su sal aceptable para uso farmacéutico, donde: G se selecciona de N y C(R5); L1 y L2 se seleccionan cada uno de ellos independientemente de NH y un enlace; R1 y R2 se seleccionan cada uno de ellos independientemente de hidrógeno, halo, alquilo C1-3, y haloalquilo C1-3, o R1 y R2, junto con el átomo al cual están unidos, forman un cicloalquilo C3-6; R3 se selecciona de alquilo C2-6, cicloalquilo C3-8, heterocicloalquilo C2-5, y heteroarilo C1-9, cada uno opcionalmente sustituido con uno a cinco sustituyentes independientemente seleccionados de halo, oxo, -NO2, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, haloalquenilo C2-6, haloalquinilo C2-6, R6, y R7; R4 se selecciona de cicloalquilo C3-8, heterociclilo C2-5, arilo C6-14 y heteroarilo C1-9, cada uno opcionalmente sustituido con uno a cinco sustituyentes independientemente seleccionados de halo, oxo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, haloalquenilo C2-6, haloalquinilo C2-6, R6, y R7; R5 se selecciona de hidrógeno, halo, OH, CN, alquilo C1-4, heterociclilo C2-5, heteroarilo C1-5, y R6, donde el resto heterociclilo tiene 3 a 6 átomos del anillo y el resto heteroarilo tiene 5 ó 6 átomos del anillo, y los restos heterociclilo y heteroarilo están cada uno de ellos opcionalmente sustituidos con uno a cuatro sustituyentes seleccionados independientemente de halo, NO2, -CN, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, haloalquenilo C2-4, haloalquinilo C2-4, R6, y R7; cada R6 se selecciona independientemente de OR7, -N(R7)R8, -NR7C(O)R8, -C(O)R7, -C(O)OR7, -C(O)N(R7)R8, -C(O)N(R7)OR8, -C(O)N(R7)S(O)2R8, -N(R7)S(O)2R8, -S(O)nR7, y -S(O)2N(R7)R8; cada R7 y R8 se selecciona independientemente de hidrogeno o de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6-(CH2)m-, aril C6-14-(CH2)m-, heterociclilo C2-5-(CH2)m-, y heteroaril C1-9-(CH2)m-, cada uno de ellos opcionalmente sustituido con uno a cinco sustituyentes independientemente seleccionados de halo, oxo, NO2, -CN, alquilo C1-6, haloalquilo C1-6 y R9; cada R9 se selecciona independientemente de OR10, -N(R10)R11, -N(R10)C(O)R11, -C(O)R10, -C(O)OR10, -C(O)N(R10)R11, -C(O)N(R7)OR8, -C(O)N(R10)S(O)2R11, -NR10S(O)2R11, -S(O)nR10, y -S(O)2N(R10)R11; cada R10 y R11 se selecciona independientemente de hidrógeno y alquilo C1-6; cada n se selecciona independientemente de 0, 1 y 2; y cada m se selecciona independientemente de 0, 1, 2, 3, y 4; donde cada uno de los restos heteroarilo antes mencionados tiene uno a cuatro heteroátomos seleccionados independientemente de N, O, y S, y cada uno de los restos heterociclilo antes mencionados está saturado o parcialmente insaturado y tiene uno o dos heteroátomos independientemente seleccionados de N, O y S.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28996909P | 2009-12-23 | 2009-12-23 | |
| US38696410P | 2010-09-27 | 2010-09-27 |
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| Publication Number | Publication Date |
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| AR081797A1 true AR081797A1 (es) | 2012-10-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104923 AR081797A1 (es) | 2009-12-23 | 2010-12-22 | Derivados de pirrolidinona heteroaromaticas fusionadas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar afecciones del sistema inmune y la inflamacion |
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| KR101623997B1 (ko) | 2008-04-16 | 2016-05-24 | 포톨라 파마슈티컬스, 인코포레이티드 | syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드 |
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