AR044399A1 - Compuestos heterociclicos y su uso como activadores de receptores de ppar. composiciones farmaceuticas que los contienen - Google Patents

Compuestos heterociclicos y su uso como activadores de receptores de ppar. composiciones farmaceuticas que los contienen

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Publication number
AR044399A1
AR044399A1 ARP040101732A ARP040101732A AR044399A1 AR 044399 A1 AR044399 A1 AR 044399A1 AR P040101732 A ARP040101732 A AR P040101732A AR P040101732 A ARP040101732 A AR P040101732A AR 044399 A1 AR044399 A1 AR 044399A1
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AR
Argentina
Prior art keywords
hydrogen
aralkyl
bond
optionally substituted
carbon atoms
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ARP040101732A
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English (en)
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Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33476920&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044399(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR044399A1 publication Critical patent/AR044399A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • 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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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
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  • Hospice & Palliative Care (AREA)
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  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)

Abstract

La presente proporciona agentes farmacológicos que se unen a receptores activados por el proliferador de peroxisoma (PPARs). Por consiguiente, los compuestos de la presente son útiles para el tratamiento de condiciones mediadas por la actividad del receptor de PPAR en mamíferos. Dichas condiciones incluyen dislipidemia, hiperlipidemia, hipercolesteremia, aterosclerosis, hipertrigliceridemia, falla cardiaca, infarto al miocardio, enfermedades vasculares, enfermedades cardiovasculares, hipertensión, obesidad, inflamación, artritis, cáncer, enfermedad de Alzheimer, trastornos de la piel, enfermedades respiratorias, trastornos oftálmicos, enfermedades inflamatorias del intestino, colitis ulcerativa, enfermedad de Crohn, y condiciones en donde están implicadas la tolerancia dañada a glucosa, hiperglicemia y resistencia a insulina, tal como diabetes de tipo 1 y de tipo 2, y síndrome X. Reivindicación 1: Un compuesto de la fórmula (1), en donde L es un radical seleccionado del grupo que consiste en las fórmula (2) y (3), en donde: R1 es hidrógeno, alquilo opcionalmente sustituido, arilo, heteroarilo, aralquilo o cicloalquilo; R2 es hidrógeno, hidroxi, oxo, alquilo opcionalmente sustituido, arilo, aralquilo, alcoxi, ariloxi, aralcoxi, alquiltio, ariltio o aralquiltio; R3 es hidrógeno; o R2 y R3 combinados son alquileno que en conjunto con los átomos de carbono a los cuales están unidos forman un anillo de 5 a 7 miembros fusionados; o R2 y R3 combinados son un enlace entre los átomos de carbono a los cuales están unidos; n es 0 o un entero de 1 ó 2; Ya es hidrógeno; o Ya y R2 combinados son un enlace entre los átomos de carbono a los cuales están unidos; R4a es hidrógeno; o R4a e Ya combinados son un enlace entre los átomos de carbono a los cuales están unidos; R'' es hidrógeno, alquilo opcionalmente sustituido, alcoxi o halógeno; m es un entero de 1 ó 2; Yb es hidrógeno; R4b es hidrógeno; o R4b y Yb combinados son un enlace entre los átomos de carbono a los cuales están unidos; R y R' son independientemente hidrógeno, halógeno, alquilo opcionalmente sustituido, alcoxi, aralquilo o heteroaralquilo; o R y R' combinados junto con los átomos de carbono a los cuales están unidos forman un anillo aromático o heteroaromático de 5 ó 6 miembros fusionado, opcionalmente sustituido, siempre que R y R' estén unidos a los átomos de carbono adyacentes entre sí; o R-C y R'-C independientemente pueden ser reemplazados por nitrógeno; X1 es -Z-(CH2)p-Q-W, en donde; Z es un enlace, O, S, S(O) o S(O)2; o Z es -C(O)NR5-, en donde R5 es hidrógeno, alquilo o aralquilo; p es un entero de 1 a 8; Q es un enlace; o Q es O(CH2)r- o -S(CH2)r-, en donde r es 0 o un entero de 1 a 8; o Q es -C(OH2)1-8O-, -S(CH2)1-8O-, -S(CH2)1-8S- o -C(O)-, o Q es -C(O)NR6-, en donde R6 es hidrógeno, alquilo opcionalmente sustituido, cicloalquilo, arilo, heteroarilo, aralquilo o heteroaralquilo; o Q es -NR7, -NR7C(O)-, -NR7C(O)NR8- o - NR7C(O)O-, en donde R7 es hidrógeno, alquilo opcionalmente sustituido, cicloalquilo, arilo, heteroarilo, aralquilo o heteroaralquilo; R8 es hidrógeno, alquilo o aralquilo; W es cicloalquilo, arilo, heterociclilo, aralquilo o heteroaralquilo; o W y R6 tomados con el átomo de nitrógeno al cual están unidos forman un anillo bicíclico de 8 a 12 miembros, el cual puede estar opcionalmente sustituido o puede contener otro átomo heterogéneo seleccionado de oxígeno, nitrógeno y azufre; X2 es C(R9)2-, O, S o -NR10-, en donde R9 es hidrógeno o alquilo inferior; R10 es hidrógeno, alquilo o aralquilo; siempre que W no sea 2-metilquinolin-4-ilo cuando Z es O, p es 1, Q es un enlace, X2 es -C(R9)2-, en donde R9 es hidrógeno, y X1 está localizado en la posición 4; o W no es 2-butil-4-cloro-5-hidroximetilimidazol-1-ilo cuando Z es un enlace, p es 1, Q es un enlace, X2 es -NR10- en donde R10 es hidrógeno, y X1 está ubicado en la posición 4; o un isómero óptico del mismo; o una mezcla de isómeros ópticos de los mismos o una sal farmacéuticamente aceptable del mismo.
ARP040101732A 2003-05-20 2004-05-19 Compuestos heterociclicos y su uso como activadores de receptores de ppar. composiciones farmaceuticas que los contienen AR044399A1 (es)

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US47206703P 2003-05-20 2003-05-20

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AR044399A1 true AR044399A1 (es) 2005-09-14

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Country Link
US (1) US7652061B2 (es)
EP (1) EP1638963B1 (es)
JP (1) JP4637843B2 (es)
KR (2) KR100849747B1 (es)
CN (1) CN1795193B (es)
AR (1) AR044399A1 (es)
AT (1) ATE442365T1 (es)
AU (1) AU2004240754B9 (es)
BR (1) BRPI0410779A (es)
CA (1) CA2525764C (es)
CL (1) CL2004001169A1 (es)
CO (1) CO5650248A2 (es)
DE (1) DE602004023080D1 (es)
EC (1) ECSP056175A (es)
ES (1) ES2331131T3 (es)
IS (1) IS8160A (es)
MA (1) MA27777A1 (es)
MX (1) MXPA05012465A (es)
NO (1) NO20056056L (es)
PE (1) PE20050157A1 (es)
PT (1) PT1638963E (es)
RU (1) RU2374241C2 (es)
TN (1) TNSN05295A1 (es)
TW (1) TW200524918A (es)
WO (1) WO2004103995A1 (es)
ZA (1) ZA200508905B (es)

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