CO6220936A2 - 5-oxoisoxazoles como inhibidores de lipasas y fosfolipasas - Google Patents

5-oxoisoxazoles como inhibidores de lipasas y fosfolipasas

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Publication number
CO6220936A2
CO6220936A2 CO09107072A CO09107072A CO6220936A2 CO 6220936 A2 CO6220936 A2 CO 6220936A2 CO 09107072 A CO09107072 A CO 09107072A CO 09107072 A CO09107072 A CO 09107072A CO 6220936 A2 CO6220936 A2 CO 6220936A2
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Prior art keywords
alkyl
alkylene
cycloalkyl
aryl
heteroaryl
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CO09107072A
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English (en)
Inventor
Stefan Petry
Manfred Seidel
Gerhard Zoller
Gunter Muller
Karl-Heinz Baringhaus
Hubert Heuer
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Sanofi Aventis
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Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of CO6220936A2 publication Critical patent/CO6220936A2/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/12Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D413/02Heterocyclic 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
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    • C07D413/02Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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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  • Hematology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
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  • Obesity (AREA)
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  • Dermatology (AREA)
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Abstract

1.- Un compuesto de la fórmula Ien la que los significados son: R1 alquilo (C5-C16), Y-arilo, Y-heteroarilo, donde el arilo o heteroarilo puede estar sustituido una o más veces con F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo (C1-C6), O-alcoxi (C1-C4)-alquilo (C1-C4), S-alquilo (C1-C6), alquilo (C1-C6), haloalquilo (C2-C4), O-haloalquilo (C2-C4), alquenilo (C2-C6), cicloalquilo (C3-C8), O-cicloalquilo (C3-C8), alquinilo (C2-C6)-, alquileno (C0-C8)-arilo, O-alquileno (C0-C8)-arilo, S-arilo, alquileno (C0-C8)-heteroarilo, N(R4)(R5), SO2-CH3, SO2-NH2, SF5, COOH, COO-alquilo (C1-C6), 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-C6)-CO-O-alquilo (C1-C6), O-CO-alquileno (C1-C6)-CO-OH, O-CO-alquileno (C1-C6)-CO-N(R18)(R19), donde el arilo o heteroarilo puede estar sustituido, a su vez, una o más veces con F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo (C1-C6), O-alcoxi (C1-C4)-alquilo (C1-C4), S-alquilo (C1-C6), alquilo (C1-C6), haloalquilo (C2-C4), alquenilo (C2-C6), cicloalquilo (C3-C8), O-cicloalquilo (C3-C8), alquinilo (C2-C6), N(R4a)(R5a), SO2-CH3, SF5, COOH, COO-alquilo (C1-C6), 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-C6)-CO-O-alquilo (C1-C6), O-CO-alquileno (C1-C6)-CO-OH, O-CO-alquileno (C1-C6)-CO-N(R18a)(R19a); x, x' 0, 1, 2, 3, 4, 5, 6; R4, R5, R6, R7, 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 hidrógeno o alquilo (C1-C8); o un radical de la fórmula la con W -C(R26)(R27)-, -C(R26)(R27)-(R28)(R29)-, -C(R26)(R27)-O-R20, R21, R22, R23, R24, R25, R26, R27, R28, R29 son iguales o diferentes y son hidrógeno, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, SF5, O-alquilo (C1-C6), O-alcoxi (C1-C4)-alquilo (C1-C4), S-alquilo (C1-C6), alquilo (C1-C6), haloalquilo (C2-C4), O-haloalquilo (C2-C4), alquenilo (C2-C6), cicloalquilo (C3-C8), O-cicloalquilo (C3-C8), ...
CO09107072A 2007-04-05 2009-09-30 5-oxoisoxazoles como inhibidores de lipasas y fosfolipasas CO6220936A2 (es)

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EP07007251 2007-04-05

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CO6220936A2 true CO6220936A2 (es) 2010-11-19

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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)

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WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 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
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
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
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors

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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
WO2004094394A1 (en) 2003-04-01 2004-11-04 Eli Lilly And Company Benzisothiazol-3-one-carboxylic acid amides as phospholipase inhibitors
US7217727B2 (en) * 2003-04-01 2007-05-15 Eli Lilly And Company 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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CA2682891A1 (en) 2008-10-16
MX2009010483A (es) 2009-10-19
ZA200906212B (en) 2010-05-26
JP2010523504A (ja) 2010-07-15
BRPI0810044A2 (pt) 2014-10-14
EP2144891A1 (de) 2010-01-20
CL2008000982A1 (es) 2008-10-10
CN101657435A (zh) 2010-02-24
AU2008235071A1 (en) 2008-10-16
KR20090127418A (ko) 2009-12-11
US9029400B2 (en) 2015-05-12
US20100152246A1 (en) 2010-06-17
AR065934A1 (es) 2009-07-15
WO2008122357A1 (de) 2008-10-16
EP2144891B1 (de) 2016-06-15
IL201254A0 (en) 2010-05-31
MA31295B1 (fr) 2010-04-01
RU2009140760A (ru) 2011-05-10
UY31000A1 (es) 2008-11-28

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