AR063311A1 - Compuestos organicos - Google Patents

Compuestos organicos

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Publication number
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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    • C07DHETEROCYCLIC COMPOUNDS
    • 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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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • 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
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators 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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    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals 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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    • C07D405/12Heterocyclic 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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    • C07D417/02Heterocyclic 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
    • 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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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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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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)
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PE (1) PE20080888A1 (es)
RU (1) RU2009118489A (es)
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WO (1) WO2008048991A2 (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006064189A1 (en) 2004-12-14 2006-06-22 Astrazeneca Ab Oxadiazole derivatives as dgat inhibitors
WO2007071966A1 (en) 2005-12-22 2007-06-28 Astrazeneca Ab Pyrimido- [4, 5-b] -oxazines for use as dgat inhibitors
MX2008015228A (es) 2006-05-30 2008-12-12 Astrazeneca Ab Acido 5-fenilamino-1,3,4-oxadiazol-2-ilcarbonilamino-4-fenoxi-cicl ohexanocarboxilico sustituido como inhibidor de diacilglicerol aciltransferasa de acetil coenzima a.
AU2007266890B2 (en) 2006-05-30 2011-02-17 Astrazeneca Ab 1, 3, 4 -oxadiazole derivatives as DGAT1 inhibitors
BRPI0821274A2 (pt) 2007-12-20 2017-06-13 Astrazeneca Ab composto ou um sal, ou pró-droga farmaceuticamente aceitável do mesmo, uso do mesmo, método para tratar uma doença em um animal de sangue quente, e, composição farmacêutica
WO2009112445A1 (en) * 2008-03-10 2009-09-17 Novartis Ag Method of increasing cellular phosphatidyl choline by dgat1 inhibition
US20110301192A1 (en) * 2008-10-01 2011-12-08 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
AU2010226826A1 (en) * 2009-03-18 2011-10-13 Merck Sharp & Dohme Corp. Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
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