CO5170416A1 - Derivados de 4,4-biarilpiperidina - Google Patents

Derivados de 4,4-biarilpiperidina

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Publication number
CO5170416A1
CO5170416A1 CO99057228A CO99057228A CO5170416A1 CO 5170416 A1 CO5170416 A1 CO 5170416A1 CO 99057228 A CO99057228 A CO 99057228A CO 99057228 A CO99057228 A CO 99057228A CO 5170416 A1 CO5170416 A1 CO 5170416A1
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Colombia
Prior art keywords
alkyl
heteroaryl
heterocycle
aryl
optionally substituted
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CO99057228A
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English (en)
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Liras Spiros
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Pfizer Prod Inc
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Publication of CO5170416A1 publication Critical patent/CO5170416A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P1/12Antidiarrhoeals
    • 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
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D409/10Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nutrition Science (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Un compuesto de fórmula I<EMI FILE="99057228_1" ID="1" IMF=JPEG >R1 es hidrógeno, (alcoxi C0-C8)-(alquilo C0-C8)-, donde el número total de átomos de carbono es ocho o inferior, aril, aril-(alquilo C1-C8)-, heteroarilo, heteroaril-(alquilo C1-C8)-, heterociclo, heterociclo-(alquilo C1-C8), cicloalquilo C3-C7- o (cicloalquil C3-C7)-(alquilo C1-C8), donde dicho arilo y el resto arilo de dicho aril-(alquilo C1-C8) se seleccionan independientemente, de fenilo y naftilo y donde dicho heteroarilo y el resto heteroarilo de dicho heteroaril-(alquilo C1-C8)- se seleccionan independientemente de pirazinilo, benzofuranilo, quinolilo, isoquinolilo, benzotienilo, isobenzofurilo, pirazolilo, indolilo, isoindolilo, bencimidazolilo, purinilo, carbazolilo, 1,2,5-tiadiazolilo, quinazolinilo, piridazinilo, pirazinilo, cinolinilo, ftalazinilo, quinoxalinilo, xantinilo, hipoxantinilo, pteridinilo, 5-azacitidinilo, 5-azauracililo, triazolopiridinilo, imidazolopiridinilo, pirrolopirimidinilo, pirazolopirimidinilo, oxazolilo, oxadiazolilo, isoxazolilo, tiazolilo, isotiazolilo, furanilo, pirazolilo, pirrolilo, tetrazolilo, triazolilo, tienilo, imidazolilo, piridinilo y pirimidinilo; y donde dicho heterociclo y el resto heterocíclico de dicho heterociclo-(alquilo C1-C8)- se seleccionan de sistemas de anillo monocíclicos o bicíclicos no aromáticos saturados o insaturados, conteniendo dichos sistemas de anillo de cuatro a siete átomos de carbono en el anillo, uno a tres de los cuales puede estar opcionalmente reemplazado por O, N o S, y conteniendo dichos sistemas de anillo bicíclicos de siete a doce átomos de carbono en el anillo, de los cuales de uno a cuatro pueden estar opcionalmente reemplazados por O, N o S; y donde cualquiera de los restos arilo, heteroarilo o heterociclo de R1 puede estar opcionalmente sustituido por uno a tres sustituyentes, preferiblemente con uno o dos sustituyentes, seleccionados independientemente de halo (es decir, cloro, fluoro, bromo o yodo), alquilo C1-C6 opcionalmente sustituido por uno a siete (preferiblemente con cero a cuatro) átomos de flúor, fenilo, bencilo, hidroxi, acetilo, amino, ciano, nitro, alcoxi C1-C6, (alquil C1-C6)amino y [(alquil C1-C6)]2amino, y donde cualquiera de los restos alquilo de R1 (por ejemplo los restos alquilo de grupos alquilo, alcoxi o alquilamino) pueden estar opcionalmente sustituidos por uno a siete (preferiblemente por cero a cuatro) átomos de flúor;R2 es hidrógeno, arilo, heteroarilo, heterociclo, SO2R4, COR4, CONR5R6, COOR4 o C(OH)R5R6, donde cada uno de R4, R5 y R6 se definen, independientemente, como se ha definido antes R1, o R5 y R6, junto con el carbono o - 2 -nitrógeno al que se encuentran unidos, forman un anillo saturado de tres a siete eslabones que contiene de cero a tres heteroátomos seleccionados, independientemente de O, N y S, y donde dicho arilo, heteroarilo y heterociclo se definen como se han definido tales términos en la definición de R1, y donde cualquiera de los restos arilo, heteroarilo y heterociclo de R2 puede estar opcionalmente sustituido con de uno a tres sustituyentes, preferiblemente con uno o dos sustituyentes, seleccionados independientemente de halo (es decir, cloro, fluoro, bromo o yodo), alquilo C1-C6 opcionalmente sustituido por uno a siete (preferiblemente con cero a cuatro) átomos de flúor, fenilo, bencilo, hidroxi, acetilo, amino, ciano, nitro, alcoxi C1-C6, opcionalmente sustituido por uno a siete (preferiblemente cero a cuatro) átomos de flúor, (alquil C1-C6)amino y [(alquil C1-C6)]2amino;R3 es hidroxi, NHSO2R7, C(OH)R7R8, flúor o CONHR7, donde R7 y R8 son iguales o distintos y se seleccionan de hidrógeno, alquilo C1-C4, alcoxi C1-C4 y (alcoxi C1-C4)-(alquilo C1-C4), que tienen un total de 4 o menos átomos de carbono, y donde cualquiera de los restos alquilo de R7 y R8 puede estar opcionalmente sustituido por uno a siete (preferiblemente de cero a cuatro) átomos de flúor; yZ1 y Z2 se seleccionan, independientemente, de hidrógeno, halo y alquilo C1-C5;con la condición de que no existen dos átomos de oxígeno de anillo adyacentes y no hay átomo de oxígeno adyacente a un átomo de nitrógeno de anillo o a un átomo de azufre de anillo en cualquiera de los restos heterociclo o heteroarilo de fórmula I;o una de las sales farmacéuticamente aceptables de dicho compuesto.
CO99057228A 1998-09-09 1999-09-09 Derivados de 4,4-biarilpiperidina CO5170416A1 (es)

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EP (1) EP1112255B1 (es)
JP (1) JP2002524445A (es)
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AP (1) AP2001002088A0 (es)
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AT (1) ATE312819T1 (es)
AU (1) AU749096B2 (es)
BG (1) BG105411A (es)
BR (1) BR9913512A (es)
CA (1) CA2343236C (es)
CO (1) CO5170416A1 (es)
CZ (1) CZ2001850A3 (es)
DE (1) DE69928945T2 (es)
EA (1) EA200100203A1 (es)
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