AR065934A1 - 5-oxoisoxazoles como inhibidores de lipasas y fosfolipasas - Google Patents
5-oxoisoxazoles como inhibidores de lipasas y fosfolipasasInfo
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- AR065934A1 AR065934A1 ARP080101391A ARP080101391A AR065934A1 AR 065934 A1 AR065934 A1 AR 065934A1 AR P080101391 A ARP080101391 A AR P080101391A AR P080101391 A ARP080101391 A AR P080101391A AR 065934 A1 AR065934 A1 AR 065934A1
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- alkyl
- alkylene
- cycloalkyl
- aryl
- heteroaryl
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Abstract
La presente se refiere a derivados de 5-oxoisoxazol de la formula (1) y el uso de los mismos como sustancias medicinales. Reivindicacion 1: Un compuesto de la formula (1) en la que los significados son: R1 alquilo C5-16), Y-arilo, Y-heteroarilo,donde el arilo o heteroarilo puede estar sustituido una o más veces con F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo (C1-6), O-alcoxi(C1-4)-alquilo (C1-4), S-alquilo (C1-6), alquilo (C1-6), haloalquilo (C2-4), O-haloalquilo (C2-4), alquenilo (C2-6), cicloalquilo (C3-8), O-cicloalquilo (C3-8), alquinilo (C2-6), alquileno (C0-8)-arilo, O-alquileno (C0-8)-arilo, S-arilo, alquileno (C0-8)-heteroarilo, N(R4)(R5), SO2-CH3, SO2-NH2, SF5, COOH, COO-alquilo (C1-6), CON(R6(R7), N(R8)CO(R9),N(R10)SO2(R11), CO(R12), (CR13R14)x-O(R15), O-CO-N(R16)(R17), O-CO-alquileno (C1-6)-CO-O-alquilo (C1-6), O-CO-alquileno (C1-6)-CO-OH, O-CO-alquileno (C1-6)-CO-N(R18)(R19), donde el arilo o heteroarilo puede estar sustituido, a su vez, una o masveces con F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo (C1-6), O-alcoxi (C1-4)-alquilo (C1-4), S-alquilo (C1-6), alquilo (C1-6), haloalquilo (C2-4), alquenilo (C2-6), cicloalquilo (C3-8), O-cicloalquilo (c3-8), alquinilo (C2-6), N(R4a)(R5a), SO2-CH3, SF5, COOH, COO-alquilo (C1-6), CON(R6a)(R7a), N(R8a)CO(R9a), N(R10a)SO2(R11a), CO(R12a), (CR13aR14a)x'-O(R15a), O-CO-N(R16a)(R17a), O-CO-alquileno (C1-6)-CO-O-alquilo (C1-6), O-CO-alquileno (C1-6)-CO-OH, O-CO-alquileno (C1-6)-CO-N(R18a)(R19a);x, x' 0, 1, 2, 3, 4, 5, 6; R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R4a, R5a, R6a, R7a, R9a, R10a, R11a, R12a, R13a, R14a, R15a, R16a, R17a, R18a, R19a independientemente entre sí hidrogeno o alquilo (C1-8); o unradical de la formula (2), con W -C(R26)(R27)-, -C(R26)(R27)-C(R28)(R29)-, -C(R26)(R27)-O-; R20, R21, R22, R23, R24, R25, R26, R27, R28, R29 son iguales o diferentes y son hidrogeno, F, Cl, Br, O, OH, CF3, NO2, CN, OCF3, SF3, O-alquilo (C1-6), O-alcoxi (C1-4)-alquilo (C1-4), S-alquilo (C1-6), alquilo (C1-6), haloalquilo (C2-4), O-haloalquilo (C2-4), alquenilo (C2-6), cicloalquilo (C3-8), O-cicloalquilo (C3-8), cicloalquenilo (C3-8), alquinilo (C2-6), N(R30)(R31), SO2-CH3, COOH, COO-alquilo(C1-6), CON(R32)(R33), N(R34)CO(R35), N(R36)SO2(R37), CO(R38), (CR39R40)x''-O(R41), O-CO-N(R42)(R43), O-CO-alquileno (C1-6)-CO-O-alquilo (C1-6), O-CO-alquileno (C1-6)-CO-OH, O-CO-alquileno (C1-6)-CO-N(R44)(R45); x'' 0, 1, 2, 3, 4, 5, 6; R30, R31,R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, R44, R45 son iguales o diferentes y son hidrogeno o alquilo (C1-6); o R20 y R26 o R21 y R27 junto con los átomos de carbono que tienen forman un sistema de anillos monocíclicos, de 5 o 6miembros, saturados, parcialmente insaturados o aromáticos, cuyos miembros individuales pueden reemplazarse por -CHR46-, -CR46R47-, =(C-R46)-; o R22 y R24 o R23 y R25 junto con los átomos de carbono que tienen forman un sistema de anillosmonocíclicos, de 5 o 6 miembros, saturados, parcialmente insaturados o aromáticos, cuyos miembros individuales pueden reemplazarse por -CHR46-, -CR46R47-, =(C-R46)-; R46, R47 son iguales o diferentes y son F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, SF5,O-alquilo (C1-6), O-alcoxi (C1-4)-alquilo (C1-4), S-alquilo (C1-6), alquilo (C1-6), haloalquilo (C2-4), O-haloalquilo (C2-4), alquenilo (C2-6), cicloalquilo (C3-8), O-cicloalquilo (C3-8), alquinilo (C2-6), N(R48)(R49), SO2-CH3, COOH, COO-alquilo (C1- 6), CON(R50)(R51), N(R52)CO(R53), N(R54)SO2(R55), CO(R56), (CR57R58)x'''-O(R59), O-CO-N(R60)(R61), O-CO-alquileno (C1-6)-CO-O-alquilo (C1-6), O-CO-alquileno (C1-6)-CO-OH, O-CO-alquileno (C1-6)-CO-N(R62)(R63); x''' 0, 1, 2, 3, 4, 5, 6; R48, R49,R50, R51, R52, R53, R54, R55, R56, R57, R58, R59, R60, R61, R62, R63, son iguales o diferentes y son hidrogeno o alquilo (C1-6); Y, Z son iguales o diferentes y son alquileno (C1-2), que puede estar sustituido una vez con F, Cl, CH3 u OH; R2hidrogeno, alquilo (C1-12), Z-arilo, donde el arilo o heteroarilo puede estar opcionalmente sustituido, cicloalquilo (C3-12); R3 alquilo (C1-12), arilo, heteroarilo, donde el arilo o heteroarilo puede estar opcionalmente sustituido, cicloalquilo (C3-12); o R2 y R3 junto con los átomos de carbono que tienen forman un sistema de anillos monocíclicos, saturados o parcialmente insaturados, de 4 a 8 miembros, cuyos miembros individuales pueden reemplazarse por uno a tres átomos o grupos atomicos dela serie -CHR64-, -CR64R65-, =(C-R66)-, -NR67-, -C(=O)-, -O-, con la condicion de que dos unidades de la serie -O- no puedan ser adyacentes; R64, R65, R66, R67 son iguales o diferentes y son hidrogeno, F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, SF5, O-alquilo (C1-6), O-alcoxi (C1-4)-alquilo (C1-4), S-alquilo (C1-6), alquilo (C1-6), haloalquilo (C2-4), O-haloalquilo (c2-4), alquenilo (C2-6), cicloalquilo (C3-8), O-cicloalquilo (C3-8), cicloalquenilo (C3-8), alquinilo (C2-6), N(R68)(R69), SO2-CH3,COOH, COO-alquilo (C1-6), CON(R70)(R71), N(R72)CO(R73), N(R74)SO2(R75), CO(R76), (CR77R78)x''''-O(R79), O-CO-N(R80)(R81), O-CO-alquileno (C1-6)-CO-O-alquilo (C1-6), O-CO-alquileno(C1-6)-CO-OH, O-CO-alquileno (C1-6)-CO-N(R82)(R83); x'''' 0, 1, 2, 3,4, 5, 6; R68, R69, R70, R71, R72, R73, R74, R75, R76, R77, R78, R79, R80, R81, R82, R83 son iguales o diferentes y son hidrogeno o alquilo (C1-6); con la condicion de que se excluya el compuesto con R1 = ciclohexilo, R2 = H y R3 = fenilo; las formastautoméricas de los compuestos y las sales fisiologicamente toleradas de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP07007251 | 2007-04-05 |
Publications (1)
Publication Number | Publication Date |
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AR065934A1 true AR065934A1 (es) | 2009-07-15 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP080101391A AR065934A1 (es) | 2007-04-05 | 2008-04-03 | 5-oxoisoxazoles como inhibidores de lipasas y fosfolipasas |
Country Status (19)
Country | Link |
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US (1) | US9029400B2 (es) |
EP (1) | EP2144891B1 (es) |
JP (1) | JP2010523504A (es) |
KR (1) | KR20090127418A (es) |
CN (1) | CN101657435A (es) |
AR (1) | AR065934A1 (es) |
AU (1) | AU2008235071A1 (es) |
BR (1) | BRPI0810044A2 (es) |
CA (1) | CA2682891A1 (es) |
CL (1) | CL2008000982A1 (es) |
CO (1) | CO6220936A2 (es) |
IL (1) | IL201254A0 (es) |
MA (1) | MA31295B1 (es) |
MX (1) | MX2009010483A (es) |
RU (1) | RU2009140760A (es) |
TW (1) | TW200911765A (es) |
UY (1) | UY31000A1 (es) |
WO (1) | WO2008122357A1 (es) |
ZA (1) | ZA200906212B (es) |
Families Citing this family (8)
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WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2011157827A1 (de) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
Family Cites Families (6)
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DE19960917A1 (de) | 1999-12-17 | 2001-06-21 | Bayer Ag | Neue 3-Oxo-2,1-benzisoxazol-1(3H)-carboxamide zur Behandlung von ZNS-Erkrankungen |
WO2004093872A1 (en) | 2003-03-31 | 2004-11-04 | Eli Lilly And Company | 3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors |
EP1613608A1 (en) * | 2003-04-01 | 2006-01-11 | Eli Lilly And Company | Phospholipase inhibitors |
EP1615900A1 (en) | 2003-04-01 | 2006-01-18 | Eli Lilly And Company | Benzisothiazol-3-one-carboxylic acid amides as phospholipase inhibitors |
DE102004005172A1 (de) * | 2004-02-02 | 2005-08-18 | Aventis Pharma Deutschland Gmbh | Indazolderivate als Inhibitoren der Hormon Sensitiven Lipase |
DE102005018389A1 (de) | 2005-04-20 | 2006-10-26 | Sanofi-Aventis Deutschland Gmbh | Azolderivate als Inhibitoren von Lipasen und Phospholipasen |
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2008
- 2008-03-22 EP EP08716677.3A patent/EP2144891B1/de active Active
- 2008-03-22 MX MX2009010483A patent/MX2009010483A/es unknown
- 2008-03-22 JP JP2010501403A patent/JP2010523504A/ja not_active Withdrawn
- 2008-03-22 CN CN200880010963A patent/CN101657435A/zh active Pending
- 2008-03-22 WO PCT/EP2008/002314 patent/WO2008122357A1/de active Application Filing
- 2008-03-22 KR KR1020097020724A patent/KR20090127418A/ko not_active Application Discontinuation
- 2008-03-22 CA CA002682891A patent/CA2682891A1/en not_active Abandoned
- 2008-03-22 AU AU2008235071A patent/AU2008235071A1/en not_active Abandoned
- 2008-03-22 RU RU2009140760/04A patent/RU2009140760A/ru not_active Application Discontinuation
- 2008-03-22 BR BRPI0810044-6A2A patent/BRPI0810044A2/pt not_active Application Discontinuation
- 2008-04-02 TW TW097111928A patent/TW200911765A/zh unknown
- 2008-04-03 UY UY31000A patent/UY31000A1/es not_active Application Discontinuation
- 2008-04-03 AR ARP080101391A patent/AR065934A1/es unknown
- 2008-04-04 CL CL200800982A patent/CL2008000982A1/es unknown
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2009
- 2009-09-08 ZA ZA200906212A patent/ZA200906212B/xx unknown
- 2009-09-30 IL IL201254A patent/IL201254A0/en unknown
- 2009-09-30 CO CO09107072A patent/CO6220936A2/es not_active Application Discontinuation
- 2009-10-02 MA MA32250A patent/MA31295B1/fr unknown
- 2009-10-05 US US12/573,335 patent/US9029400B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
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KR20090127418A (ko) | 2009-12-11 |
CA2682891A1 (en) | 2008-10-16 |
US9029400B2 (en) | 2015-05-12 |
JP2010523504A (ja) | 2010-07-15 |
EP2144891B1 (de) | 2016-06-15 |
WO2008122357A1 (de) | 2008-10-16 |
EP2144891A1 (de) | 2010-01-20 |
TW200911765A (en) | 2009-03-16 |
RU2009140760A (ru) | 2011-05-10 |
US20100152246A1 (en) | 2010-06-17 |
UY31000A1 (es) | 2008-11-28 |
MX2009010483A (es) | 2009-10-19 |
AU2008235071A1 (en) | 2008-10-16 |
CO6220936A2 (es) | 2010-11-19 |
BRPI0810044A2 (pt) | 2014-10-14 |
CN101657435A (zh) | 2010-02-24 |
ZA200906212B (en) | 2010-05-26 |
MA31295B1 (fr) | 2010-04-01 |
IL201254A0 (en) | 2010-05-31 |
CL2008000982A1 (es) | 2008-10-10 |
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