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AR063219A1 - Derivados de azetidinona, una composicion que los comprende y su uso en el tratamiento del dolor y de trastornos del metabolismo lipidico. - Google Patents

Derivados de azetidinona, una composicion que los comprende y su uso en el tratamiento del dolor y de trastornos del metabolismo lipidico.

Info

Publication number
AR063219A1
AR063219A1 ARP070104078A ARP070104078A AR063219A1 AR 063219 A1 AR063219 A1 AR 063219A1 AR P070104078 A ARP070104078 A AR P070104078A AR P070104078 A ARP070104078 A AR P070104078A AR 063219 A1 AR063219 A1 AR 063219A1
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AR
Argentina
Prior art keywords
alkyl
alkylene
aryl
group
optionally
Prior art date
Application number
ARP070104078A
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English (en)
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Schering Corp
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Publication of AR063219A1 publication Critical patent/AR063219A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D471/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Derivados de azetidinona, a composiciones que comprenden un derivado de azetidinona y a su uso para tratar o prevenir un trastorno del metabolismo lipídico, dolor, diabetes, una afeccion vascular, desmielinizacion o enfermedad hepática grasa no alcoholica. Reivindicacion 1: Un compuesto que tiene la formula (1) o su sal, solvato, éster, profármaco o estereoisomero aceptable para uso farmacéutico, donde: R1 es H, alquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, difenilmetilo, cicloalquilalquilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo o -alquilen-C(O)N(alquilo)2, donde un grupo alquilo, arilo o heteroarilo puede estar opcional e independientemente sustituido con uno o más de los siguientes grupos: -(C=NO-alquil)CH3, -NC(O)NH2, -NC(O)NH(alquilo), -NC(O)N(alquilo)2, -SO2NH2, -SO2NH(alquilo), -SO2N(alquilo)2, -CF3, -OH, -halo, -CN, -alcoxi, -C(O)O-alquilo, -S(O)alquilo, -SO2-alquilo o -P(O)(O-alquilo)2, y un grupo arilo además puede estar opcional e independientemente sustituido con uno o más grupos alquilo; R2 es H, alquilo, cicloalquilo, arilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, R6-A-, alquil-O-C(O)-, (alquil)2N-alquilen-C(O)-, (alquil)2-N-C(O)-alquilen-C(O)-, CN-alquilen-C(O)-, alquil-Oalquilen-C(O)-, alquil-C(O)-alquilen-C(O)-, alquil-C(O)-NH-alquilen-C(O)-, alquil-NH-C(O)-, aril-NH-C(O)-, alquil-O-C(O)-alquilen-C(O)-, alquil-O-C(O)-cicloalquilen-alquilen-, NH2-C(O)-NH- alquilen-C(O)-, NH2-C(O)-alquilen-C(O)-, alquil-C(O)-NH-alquilen-S-alquilen-C(O)-, alquil-O-C(O)-alquilen-C(O)-, alquil-S-alquilen-C(O)-, alquil-C(O)-cicloalquilen-alquilen-C(O)-, alquil-S-alquileno-, (-NHC(O)alquil)C(O)-, alquil(-C(O)Oalquil)-NH- C(O)- o -C(O)-alquilen-N(R6)2-; o alquil-S-alquilen(-NHC(O)alquil-C(O)-, donde un grupo alquilo o arilo puede estar opcional e independientemente sustituido con uno o más de los siguientes grupos; -(C=N-O-alquil)CH3, -NH-C(O)NH-alquilo, -C(O)NH2, - CN, -C(O)NH-alquilo, -C(O)O-alquilo, -C(O)H, -C(O)OH, -NC(O)NH2, -NC(O)NH(alquilo), -NC(O)N(alquil)2, -SO2NH2, -SO2NH(alquilo), -SO2N(alquilo)2, -CF3, -OH, -halo, haloalquilo, -CN, -alcoxi, -C(O)O-alquilo, -S(O)alquilo, -SO2-alquilo o -P(O)(O- alquilo)2, y un grupo arilo además puede estar opcional e independientemente sustituido con uno o más grupos alquilo; R3 es H, alquilo, arilo, arilalquilo, arilalquenilo, arilalquinilo, NH-arilalquilo, arilalcoxi, ariltio, arilalquiltio, arilcarbonilo, ariloxi, cicloalquilo, arilsulfonilo, heteroarilo, heteroarilalquilo, heteroarilalquenilo, heteroarilalquinilo, heteroarilalcoxi, heteroariloxi o heteroarilsulfonilo, donde un grupo alquilo o arilo puede estar opcional e independientemente sustituido con uno o más de los siguientes grupos; -(C=N-O-alquil)CH3, -NC(O)NH2, -NC(O)NH(alquilo), -NC(O)N(alquilo)2, -SO2NH2, -SO2NH(alquilo), -SO2N(alquilo)2, -CF3, -OH, -halo, -CN, -alcoxi, -C(O)O-alquilo, -S(O)alquilo, -SO2- alquilo o -P(O)(O-alquilo)2, un grupo arilo puede estar opcional e independientemente sustituido con uno o más grupos alquilo, y un grupo heteroarilo puede estar opcional e independientemente sustituido con uno o más grupos arilo o heteroarilo. cada aparicion de R4 y R5 es independientemente -C(R7)2-, donde el átomo de carbono en el anillo de un grupo y el átomo de carbono en el anillo de un grupo puede estar opcionalmente unido por un grupo -CH2-CH2-; cada aparicion de R6 es independientemente alquilo. alquenilo, arilo, heteroarilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, cicloalquenilo, heterocicloalquenilo, cicloalquilo benzofusionado, heterocicloalquilo benzofusionado, o heterocicloalquenilo benzofusionado; cada aparicion de R7 es independientemente -H, -alquilo, -CN u -OH; A es -C(O)-, -OC(O)-, -alquilen-C(O)-, -O-alquilen-C(O)-, -C(O)-alquilen-C(O)-, -C(O)-NHCH2-C(O)-, -C(O)-N(alquil)-CH2-C(O)-, -alquilen-, -alquenileno, -alquenilen-C(O)-, grupo de formula (2), -O- C(O)-alquilen-C(O)-, -cicloalquilen-NH-C(O)-, -NHC(O)-, -alquilen-NHC(O)-, -alquilen-C(O)NH-alquilen-C(O)-, -alquilen-C(O)NH-alquilen-C(O)-, -C(O)-NH-alquilen-C(O)-, -alquilen-O-alquilen-C(O)-, -alquilen(alcoxi)-C(O)- o -S-alquilen-C(O)-, donde un grupo A está unido al átomo de nitrogeno al cual está unido mediante un grupo C(O) terminal; u es un entero que varia de 0 hasta 3; y v es un entero que varía de 0 hasta 3; de modo que la suma de u y v es de 3 a 5, de modo que el compuesto de formula (1) no es un compuesto de formula (1A), (1B), (1C) o (1D) como se expone en la memoria descriptiva anterior.
ARP070104078A 2006-09-15 2007-09-14 Derivados de azetidinona, una composicion que los comprende y su uso en el tratamiento del dolor y de trastornos del metabolismo lipidico. AR063219A1 (es)

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EP (1) EP2061792A2 (es)
JP (1) JP2010503677A (es)
CN (1) CN101583612A (es)
AR (1) AR063219A1 (es)
CA (1) CA2663502A1 (es)
MX (1) MX2009002921A (es)
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WO2008033464A2 (en) 2008-03-20
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