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AR063800A1 - Derivados de acido nicotinico, composiciones farmaceuticas que las contienen y metodos de uso de los mismos - Google Patents

Derivados de acido nicotinico, composiciones farmaceuticas que las contienen y metodos de uso de los mismos

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Publication number
AR063800A1
AR063800A1 ARP070105047A ARP070105047A AR063800A1 AR 063800 A1 AR063800 A1 AR 063800A1 AR P070105047 A ARP070105047 A AR P070105047A AR P070105047 A ARP070105047 A AR P070105047A AR 063800 A1 AR063800 A1 AR 063800A1
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AR
Argentina
Prior art keywords
substituted
alkyl
aryl
alkylene
groups
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ARP070105047A
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English (en)
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Schering Corp
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Filing date
Publication date
Priority claimed from US11/600,216 external-priority patent/US7750015B2/en
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR063800A1 publication Critical patent/AR063800A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/16—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Composiciones farmacéuticas que comprenden uno o más compuestos y métodos para utilizarlos. Reivindicación 1: Un compuesto que presenta la fórmula (1), o una sal, solvato, éster o tautómero del mismo aceptable para uso farmacéutico, donde: Q se selecciona del grupo que consta de: fórmulas (2), L se selecciona del grupo que consta de fórmulas (f) a (g), y (i); R1 se selecciona del grupo que consta de H, alquilo, arilalquilo, -alquilen-S-alquilo, alquenilo, alquinilo, haloalquilo, donde un grupo alquilo puede estar sustituido opcionalmente con uno o más de los siguientes grupos, que pueden ser iguales o diferentes: -OH, cicloalquilo, -C(O)-alquilo, -alquilen-C(O)-O-alquilo, -O-R10, -alquilen-O-alquilo, arilo, -alquilen-arilo, heteroarilo, -alquilen-heteroarilo, halógeno, -(CH2)n-N(R7)2, -alquilen-cicloalquilo, o -alquilen-cicloalquenilo, donde el cicloalquilo o la porción cicloalquilo de dicho -alquilen-cicloalquilo de R1 no está sustituida o está sustituida con uno o más grupos X, dicho arilo o la porción arilo de dicho -alquilen-arilo de R1 no está sustituido o está sustituido con uno o más grupos Y, y dicho heteroarilo o la porción heteroarilo de dicho -alquilen-heteroarilo de R1 no está sustituido o está sustituido con uno o más grupos Y; R2 se selecciona del grupo que consta de H, halógeno, alquilo, haloalquilo, alquilo sustituido con uno o más -OH, -C(O)-alquilo, -C(O)-O-alquilo, -C(O)-OH, -O-R10, -alquilen-O-alquilo, arilo no sustituido, arilo sustituido con uno o más grupos Y, heteroarilo no sustituido, heteroarilo sustituido con uno o más grupos Y, y halógeno; o R1 y R2 junto con los átomos de carbono anulares a los que están unidos según se muestra, forman un anillo cicloalquenilo de 5 o 6 miembros o un anillo heterocíclico de 5 o 6 miembros que presenta 1 o 2 heteroátomos; R3 se selecciona del grupo que consta de H, alquilo, alquilo sustituido con uno o más grupos hidroxilo, -alquilen-O-alquilo, cicloalquilo, -alquilen- cicloalquilo, -alquilen-C(O)-O-alquilo, -alquilen-O-C(O)-alquilo, alquenilo, arilo, y heteroarilo, donde el cicloalquilo o la porción cicloalquilo de dicho -alquilen-cicloalquilo de R3 no está sustituido o está sustituido con uno o más grupos X, dicho arilo de R3 no está sustituido o está sustituido con uno o más grupos Y, y dicho heteroarilo de R3 no está sustituido o está sustituido con uno o más grupos Y; R4 se selecciona del grupo que consta de H, halógeno, alquilo, haloalquilo, -O- cicloalquilo, -O-alquinilo, -O-R10, -C(O)-O-alquilo, -S(O)m-R9, -N(R7)2, -N(R7)-NH-C(O)-alquilo, -N(R7)-NH-C(O)-O-alquilo, -O-N=C(R12)2, -N(R7)-N=C(R12)2, -C(O)-alquilo, heterociclilo no sustituido, heterociclilo sustituido con uno o más grupos X, - O-N(R7)-C(O)-O-alquilo, -C(O)-N(R7)2, -CN, -N3, y -O-C(O)-alquilo; R5 se selecciona del grupo que consta de H, alquilo, -OH, haloalquilo, arilalquilo, -O-alquilo, -O-arilo, cicloalquilo, heterociclilo, -O-cicloalquilo, -O-heterociclilo, -O- arilalquilo o -alquilen-O-alquilo-alquilen-C(O)-R8, -alquilen-C(O)-N(R11)2, -alquilen-C(=N-O-alquil)-arilo, cicloalquilo, -alquilen-cicloalquilo, -alquilen-C(O)-O-alquilo, -alquilen-O-C(O)-alquilo, -alquilen-C(O)-heterociclilo y alquenilo, donde el cicloalquilo o la porción cicloalquilo de dicho -alquilen-cicloalquilo de R5 no está sustituido o está sustituido con uno o más grupos X, y la porción arilo de dicho -alquilen-C(=N-O-alquil)-arilo de R5 no está sustituida o está sustituida con uno o más grupos Y; R6 se selecciona del grupo que consta de H, alquilo, alquenilo, alquilo sustituido con uno o más grupos hidroxilo, -alquilen-O-alquilo, -OR10, halógeno, arilo, heteroarilo y -N(R7)2, donde el arilo de R6 no está sustituido o está sustituido con uno o más grupos Y, y dicho heteroarilo de R6 no está sustituido o está sustituido con uno o más grupos Z; cada R7 se selecciona de manera independiente del grupo que consta de H, alquilo, cicloalquilo, arilo, -C(O)-alquilo, y -C(O)- arilo, donde el cicloalquilo de R7 no está sustituido o está sustituido con uno o más grupos X, y la porción arilo de dicho -C(O)-arilo o dicho arilo de R7 no está sustituido o está sustituido con uno o más grupos Y; dos grupos R7 junto con el átomo de N al que están unidos forman un heterociclilo; R8 se selecciona del grupo que consta de arilo, -OH y heterociclilo, donde el heterociclilo de R8 no está sustituido o está sustituido con uno o más grupos X, y dicho arilo de R8 no está sustituido o está sustituido con uno o más grupos Y; R9 se selecciona del grupo que consta de alquilo, -alquilen-cicloalquilo, alquenilo, -N(R11)2 y -alquilen-arilo, donde la porción cicloalquilo de dicho -alquilen-cicloalquilo de R9 no está sustituida o está sustituida con uno o más grupos X, y la porción arilo de dicho -alquilen-arilo de R9 no está sustituida o está sustituida con uno o más grupos Y, y con la salvedad que cuando R9 es -N(R11)2, m es 1 o 2; R10 se selecciona del grupo que consta de H, alquilo, cicloalquilo, arilalquilo, haloalquilo, -alquilen-O-alquilo, -alquilen-arilo, -alquenilen-arilo, -alquilen-heteroarilo, alquenilo, -C(O)-alquilo, alquinilo y -alquilen-cicloalquilo, donde la porción alquinilo de un grupo -O-alquinilo puede estar sustituida de manera opcional con -OH o alcoxi; la porción cicloalquilo de un grupo -O-cicloalquilo puede estar sustituida de manera opcional con un grupo -alquilen-O-alquilen-arilo; la porción cicloalquilo de dicho -alquilen-cicloalquilo de R10 no está sustituida o está sustituida con uno o más grupos X; la porción arilo de dicho -alquilen-arilo o -alquenilen-arilo de R10 no está sustituida o está sustituida con uno o más grupos Y; y la porción heteroarilo de dicho -alquilen- heteroarilo de R10 no está sustituida o está sustituida con uno o más grupos Z; R11 se selecciona del grupo que consta de H, alquilo y arilo, donde el arilo de R11 no está sustituido o está sustituido con uno o más grupos Y; o dos grupos R11 junto con el átomo de N al que están unidos, forman un heterociclilo; cada R12 se selecciona de manera independiente del grupo que consta de alquilo, arilo y heteroarilo, donde el arilo de R12 no está sustituido o está sustituido con uno o más grupos Y, y dicho heteroarilo de R12 no está sustituido o está sustituido con uno o más grupos Z; o donde ambos grupos R12, junto con el átomo de carbono al que están unidos, se combinan para formar un grupo heterociclilo; Ra y Rb se seleccionan cada uno de manera independiente del grupo que consta de H, alquilo, arilo y heteroarilo, donde el arilo de Ra y Rb no está sustituido o está sustituido con uno o más grupos Y, y dicho heteroarilo de Ra y Rb no está sustituido o está sustituido con uno o más grupos Z; Rc se selecciona del grupo que consta de H, alquilo, alquilen-arilo, y -C(O)-alquilo, donde la porción arilo de dicho alquilen-arilo de Rc no está sustituida o está sustituida con uno o más grupos Y; Rd se selecciona del grupo que consta de H, alquilo y alquilen-arilo, donde la porción arilo de dicho alquilen-arilo de Rd no está sustituida o está sustituida con uno o más grupos Y; cada X se selecciona de manera independiente del grupo que consta halógeno, alquilo, haloalquilo, -O- alquilo, -O-haloalquilo y -OH; cada Y se selecciona de manera independiente del grupo que consta de halógeno, alquilo, haloalquilo, -O-alquilo, -O-haloalquilo, -CN, -NO2, -OH, -S(O2)-alquilo, -S(O2)-arilo, -S(O2)-NH2, -S(O2)-NH-alquilo, -S(O2)-NH- arilo, -S(O2)-N(alquilo)2, -S(O2)-N(arilo)2, -S(O2)-N(alquil)(arilo) y arilo; cada Z se selecciona de manera independiente del grupo que consta de alquilo, haloalquilo, halógeno, -O-alquilo, -O-haloalquilo, -CN, -OH, arilo y N-óxido; n es 0, 1, 2 o 3; m es 0, 1 o 2; y con la salvedad que cuando L es (f), y R2, R3 y R5 son cada uno H, entonces R1 no es -CH3.
ARP070105047A 2006-11-15 2007-11-13 Derivados de acido nicotinico, composiciones farmaceuticas que las contienen y metodos de uso de los mismos AR063800A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11/600,216 US7750015B2 (en) 2005-05-17 2006-11-15 Nitrogen-containing heterocyclic compounds and methods of use thereof
US11/771,538 US7737155B2 (en) 2005-05-17 2007-06-29 Nitrogen-containing heterocyclic compounds and methods of use thereof

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Publication Number Publication Date
AR063800A1 true AR063800A1 (es) 2009-02-18

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US (3) US7737155B2 (es)
EP (1) EP2059519B1 (es)
JP (1) JP5020331B2 (es)
KR (1) KR20090083461A (es)
CN (1) CN101589041A (es)
AR (1) AR063800A1 (es)
AU (1) AU2007319940A1 (es)
CA (1) CA2669670A1 (es)
CL (1) CL2007003265A1 (es)
CO (1) CO6220970A2 (es)
EC (1) ECSP099335A (es)
MX (1) MX2009005217A (es)
NO (1) NO20092286L (es)
PE (1) PE20081345A1 (es)
RU (1) RU2009122245A (es)
TW (1) TW200825090A (es)
WO (1) WO2008060476A2 (es)

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CO6220970A2 (es) 2010-11-19
WO2008060476A2 (en) 2008-05-22
US7737155B2 (en) 2010-06-15
US20080019978A1 (en) 2008-01-24
US20110152259A1 (en) 2011-06-23
NO20092286L (no) 2009-08-13
TW200825090A (en) 2008-06-16
AU2007319940A1 (en) 2008-05-22
JP5020331B2 (ja) 2012-09-05
WO2008060476A3 (en) 2008-12-24
CA2669670A1 (en) 2008-05-22
EP2059519A2 (en) 2009-05-20
MX2009005217A (es) 2009-07-31
RU2009122245A (ru) 2010-12-20
US20100227873A1 (en) 2010-09-09
PE20081345A1 (es) 2008-10-24
EP2059519B1 (en) 2013-12-18
CL2007003265A1 (es) 2008-06-06
ECSP099335A (es) 2009-06-30
CN101589041A (zh) 2009-11-25
JP2010509397A (ja) 2010-03-25

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