AR063311A1 - Compuestos organicos - Google Patents

Compuestos organicos

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AR063311A1
AR063311A1 ARP070104573A ARP070104573A AR063311A1 AR 063311 A1 AR063311 A1 AR 063311A1 AR P070104573 A ARP070104573 A AR P070104573A AR P070104573 A ARP070104573 A AR P070104573A AR 063311 A1 AR063311 A1 AR 063311A1
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Argentina
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substituted
unsubstituted
lower alkyl
hydrogen
formula
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ARP070104573A
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Novartis Ag
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    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/12Antihypertensives
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
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    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57Aryl or substituted aryl radicals
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07ORGANIC CHEMISTRY
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    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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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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    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)

Abstract

La presente proporciona compuestos de la siguiente estructura: A-L1-B-C-D que son utiles para el tratamiento o la prevencion de las condiciones o los trastornos asociados con la actividad de DGAT1 en animales, en particular en seres humanos. Reivindicacion 1: Un compuesto que tiene la siguiente estructura: A-L1-B-C-D y sales farmacéuticamente aceptables y pro-fármacos del mismo, en donde: A se selecciona a partir de un alquilo sustituido o insustituido, alcoxilo sustituido o insustituido, cicloalquilo sustituido o insustituido, arilo sustituido o insustituido, y un heterociclilo sustituido o insustituido, en donde A está enlazado con L1 por medio de un miembro de carbono del anillo, cuando A es un anillo, L1 se selecciona a partir del grupo que consiste en: un grupo amina de la formula -(CH2)n-(CR4R4')p-(CH2)m-N(R3)-, un grupo tiocarbamoílo de la formula -(CH2)n-(CR4R4')p(CH2)m-N(R3)-C(S), un grupo amida de la formula -C(O)-N(R3)-(CH2)n-(CR4R4')p-(CH2)m-, un grupo amidina de la formula -C(NH)-N(R3)-(CH2)n-(CR4R4')p(CH2)m-, un grupo amida de la formula -(CH2)n-(CR4R4')p-(CH2)m-C(O)-N(R3)-, un grupo sulfonamida de la formula -(CH2)n-(CR4R4')p-(CH2)mS(O2)-N(R3)-, un grupo carbamato de la formula -(CH2)n- (CR4R4')p-(CH2)m-(O)-C(O)-N(R3)-, o un grupo urea de la formula -(CH2)n--(CR4R4')p-(CH2)m-N(R3)-C (O)-N(R3A)-, en donde: R3 y R3A son, independientemente uno del otro, hidrogeno o alquilo inferior, m, n, y p son, independientemente unos de otros, un entero de 0 a 2, R4 y R4' son, independientemente uno del otro, hidrogeno, halogeno, hidroxilo, alcoxilo inferior, alcoxilo inferior-carbonilo, carboxilo, o alquilo inferior, o R4 y R4' se unen juntos para formar un residuo espiro de la formula (2) en donde: X es NR3', O, S, o CR3-R4-, r y s son, independientemente uno del otro, cero o un entero de 1 a 3, R3' es hidrogeno o alquilo inferior, R3ö es hidrogeno, halogeno, hidroxilo, alcoxilo, o alquilo inferior, R4ö es hidrogeno o alquilo inferior, B es un grupo heteroarilo divalente sustituido o insustituido seleccionado a partir de uno de los siguientes grupos de formulas (3) en donde X1 y X2' se seleccionan independientemente a partir de O, NH, NR9 o S, en donde R9 se selecciona a partir de alquilo inferior, alquilo inferior-amino, alcoxilo inferior-alquilo, hidroxi-alquilo inferior, X1', X2, X3, y X4 se seleccionan independientemente a partir de N o CH, C es como en formula (4) en donde R1 se selecciona a partir de H, ciano, alquilo inferior-sulfonil-amino, alcanoil-amino, halogeno, alquilo inferior, trifluoro-metilo, alcoxilo inferior, alquilo inferior-amino, dialquilo inferior-amino, y NO2, R'1, R2, y R'2 se seleccionan independientemente a partir de hidrogeno, halogeno, trifluoro-metilo, ariloxilo, alquilo inferior, alcoxilo inferior, alquilo inferior-amino, dialquilo inferior-amino, y NO2, o C también puede ser un grupo arilo o heteroarilo bicíclico sustituido o insustituido, D se selecciona a partir de hidrogeno, halogeno, hidroxilo, ciano, alcanoil-amino, carboxilo, carbamoílo, -O-L2-E, -S-L2-E', -C(O)-O-L2-E, -L2-Eö, y -NR6-L2-E', L2 es -(CH2)n'-(CR5R5')p'-(CH2)m'-, E es: alquilo, acilo, alcoxi-carbonilo, ácido fosfonico, fosfonato, cicloalcoxi- carbonilo, ariloxi-carbonilo, heterocicliloxi-carbonilo, carboxilo, carbamoílo, sulfonilo, -SO2-OH, sulfamoílo, sulfonil carbamoilo, sulfoniloxilo, sulfonamido, -C(O)-O-R-PRO, arilo sustituido o insustituido, heterociclilo sustituido o insustituido, o heteroarilo sustituido o insustituido, y, cuando n' + m' + p' es igual a cero, E no es sulfoniloxilo o sulfonamido, E' es: alquilo, arilo, alcoxi-carbonilo, cicloalcoxi-carbonilo, ariloxi carbonilo heterocicliloxi-carbonilo, carboxilo, carbamoílo, sulfonil carbamoilo, sulfonilo, -SO2-OH, sulfamoílo, sulfonamido, ácido fosfonico, fosfonato, sulfoniloxilo, -C(O)-O-R-PRO, arilo sustituido o insustituido, heterociclilo sustituido o insustituido, o heteroarilo sustituido o insustituido, y, cuando n' + m' + p' es igual a cero, E' no es sulfamoílo, sulfonamido, ácido fosfonico, fosfonato, o sulfoniloxilo, Eö es: alquilo, acilo, alcoxi-carbonilo, ácido fosfonico, fosfonato, cicloalcoxi-carbonilo, ariloxi-carbonilo, heterocicliloxi-carbonilo, carboxilo, carbamoílo, sulfonilo, sulfamoílo, sulfoniloxilo, sulfonamido, -SO2-OH, sulfonil-carbamoilo, -C(O)-O-R-PRO, arilo sustituido o insustituido, heterociclilo sustituido o insustituido, o heteroarilo sustituido o insustituido, m', n', y p' son, independientemente unos de otros, un entero de 0 a 4, m' + n' + p' es entre 0 y 12, de preferencia 0, 1, 2, 3, o 4, R5 y R5' son, independientemente uno del otro, hidrogeno, halogeno, hidroxilo, alcoxilo inferior, o alquilo inferior, o R5 y R5' se unen juntos para formar un residuo espiro de la formula (5) en donde X' es NRx, O, S, o CRx'Rxö, r' y s' son, independientemente uno del otro, cero o un entero de 1 a 3, Rx es hidrogeno o alquilo inferior, Rx' es hidrogeno, halogeno, hidroxilo, alcoxilo, o alquilo inferior, Rxö es hidrogeno o alquilo interior; o un estereoisomero, enantiomero, o tautomero del mismo, una sal farmacéuticamente aceptable del mismo, o un pro-fármaco del mismo.
ARP070104573A 2006-10-18 2007-10-16 Compuestos organicos AR063311A1 (es)

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US82998006P 2006-10-18 2006-10-18
US95234107P 2007-07-27 2007-07-27

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EP (1) EP2074089B1 (es)
JP (1) JP5298022B2 (es)
KR (1) KR20090071642A (es)
AR (1) AR063311A1 (es)
AU (1) AU2007311087B2 (es)
BR (1) BRPI0718478A2 (es)
CA (1) CA2666880A1 (es)
CL (1) CL2007002974A1 (es)
ES (1) ES2440253T3 (es)
MX (1) MX2009004047A (es)
PE (1) PE20080888A1 (es)
RU (1) RU2009118489A (es)
TW (1) TW200829563A (es)
WO (1) WO2008048991A2 (es)

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AU2005315430B2 (en) 2004-12-14 2010-05-27 Astrazeneca Ab Oxadiazole derivatives as DGAT inhibitors
AR058562A1 (es) 2005-12-22 2008-02-13 Astrazeneca Ab Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1
CN101472905B (zh) 2006-05-30 2011-12-14 阿斯利康(瑞典)有限公司 作为酰基辅酶甘油二酯酰基转移酶的抑制剂的取代的5-苯基氨基-1,3,4-噁二唑-2-基羰基氨基-4-苯氧基-环己烷甲酸
EP2041099A1 (en) 2006-05-30 2009-04-01 AstraZeneca AB 1, 3, 4 -oxadiazole derivatives as dgat1 inhibitors
WO2009081195A1 (en) 2007-12-20 2009-07-02 Astrazeneca Ab Carbamoyl compounds as dgat1 inhibitors 190
WO2009112445A1 (en) * 2008-03-10 2009-09-17 Novartis Ag Method of increasing cellular phosphatidyl choline by dgat1 inhibition
WO2010039668A2 (en) * 2008-10-01 2010-04-08 The Regents Of The University Of California Inhibitors of cyclin kinase inhibitor p21
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
AR075858A1 (es) * 2009-03-18 2011-05-04 Schering Corp Compuestos biciclicos como inhibidores de diacilglicerol aciltransferasa
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