AR048269A1 - Compuestos moduladores de receptores opioides - Google Patents

Compuestos moduladores de receptores opioides

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Publication number
AR048269A1
AR048269A1 ARP050101007A ARP050101007A AR048269A1 AR 048269 A1 AR048269 A1 AR 048269A1 AR P050101007 A ARP050101007 A AR P050101007A AR P050101007 A ARP050101007 A AR P050101007A AR 048269 A1 AR048269 A1 AR 048269A1
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alkyl
aryl
group
heteroaryl
alkoxy
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ARP050101007A
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Janssen Pharmaceutica Nv
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • 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
    • A61P1/10—Laxatives
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
  • Amplitude Modulation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Oscillators With Electromechanical Resonators (AREA)
  • Amplifiers (AREA)
  • Eye Examination Apparatus (AREA)

Abstract

Métodos para preparar dichos compuestos, composiciones farmacéuticas que los contienen, y uso en el tratamiento de trastorno que se pueden aliviar o tratar mediante la modulacion de los receptores opioides. Reivindicacion 1: Un compuesto de formula (1), donde: R1 se selecciona del grupo que consiste en hidrogeno, alquilo C1-6, cicloalquilo, heterociclilo, (donde el cicloalquilo y heterociclilo está opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados de alquilo C1-6, hidroxi(alquilo C1-6), alcoxi C1-6, hidroxi, ciano, amino, alquilamino C1-6, (alquil C1-6)2amino, halogeno, carboxi, aril(alcoxi C1-6)carbonilo, alcoxiC1-6carbonilo, aminocarbonilo, alquilC1-6aminocarbonilo, (alquil C1-6)2aminocarbonilo o aminosulfonilo); y además donde arilo está opcionalmente fusionado a un heterociclo o cicloalquilo; donde alquilo C1-6 de R1 está opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados del grupo que consiste en alcoxiC1-6, arilo, cicloalquilo, heterociclilo, hidroxi, ciano, amino, alquilamino C1-6, (alquil C1-6)2amino, halogeno y carboxi; y donde la porcion arilo y heteroarilo de aril(alquilo C1-6) y heteroaril(alquilo C1-6), respectivamente, están opcionalmente sustituidos con uno a tres sustituyentes independientemente seleccionados de R11, donde R11 es alquilo C1-6, hidroxi(alquilo C1-6), alcoxi C1-6, aril(alquilo C1-6), aril(alcoxi C1-6), arilo, heteroarilo opcionalmente sustituido con alquilo C1-4, cicloalquilo, heterociclilo, ariloxi, heteroariloxi, cicloalquiloxi, heterocicliloxi, amino, alquilamino C1-6, (alquil C1-6)2amino, cicloalquilC1-6aminocarbonilo, hidroxi(alquil C1-6)aminocarbonilo, arilaminocarbonilo, donde arilo está opcionalmente sustituido con carboxi o alcoxiC1-6carbonilo, heterociclilcarbonilo, carboxi, alcoxiC1-6carbonilo, alquilC1-6carbonilo, alquilC1-6carbonilamino, aminocarbonilo, alquilC1-6aminocarbonilo, (alquil C1-6)2aminocarbonilo, ciano, halogeno, trifluorometilo, trifluorometoxi o hidroxi; y donde el arilo en cualquiera de los anteriores sustituyentes de R1 que contienen arilo está opcionalmente fusionado con un heterociclilo o cicloalquilo; R2 es seleccionado del grupo que consiste hidrogeno, alquilo C1-8, hidroxi(alquilo C1-8), aril(alcoxi C1-6)(alquilo C1-6), aril(alquilo C1-8); donde dicho arilo está opcionalmente sustituido con uno a dos sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, alcoxi C1-6, hidroxi, amino, alquilamino C1-6, (alquil C1-6)2amino, aminocarbonilo, alquilC1-6aminocarbonilo, (alquil C1-6)2aminocarbonilo, ciano, fluor, cloro, bromo, trifluorometilo y trifluorometoxi; y donde dichos sustituyentes alquilo y alcoxi de arilo están opcionalmente sustituidos con hidroxi, amino, alquilamino C1-6, (alquil C1-6)2amino o arilo; A se selecciona del grupo que consiste en arilo, el sistema de anillo del resto de grupo de formulas (2), opcionalmente sustituidos con R3 y R5; donde: A-B se selecciona del grupo que consiste en N-C, C-N, N-N y C-C; D-E se selecciona del grupo que consiste en O-C, S-C, y O-N; R3 es uno a dos sustituyentes independientemente seleccionados del grupo que consiste en hidrogeno, alquil C1-6, arilo, aril(alquilo C1-6), aril(alquenilo C2-6), aril(alquinilo C2-6), heteroarilo, heteroaril(alquilo C1-6), heteroaril(alquenilo C2-6), heteroaril(alquinilo C2-6), amino, alquilamino C1-6, (alquil C1-6)2amino, arilamino, heteroarilamino, ariloxi, heteroariloxi y halogeno; donde la porcion arilo y heteroarilo de R3 está opcionalmente sustituida con uno a cinco sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, hidroxi(alquilo C1-6), alcoxi C1-6, aril(alquilo C1-6), aril(alcoxi C1-6), arilo, ariloxi, heteroaril(alquilo C1-6), heteroaril(alcoxi C1-6), heteroarilo, heteroariloxi, arilamino, heteroarilamino, amino, alquilamino C1-6, (alquil C1-6)2amino, carboxi(alquil C1-6)amino, carboxi, alquilC1-6carbonilo, alcoxiC1-6carbonilo, alquilC1-6carbonilamino, aminocarbonilo, alquilC1-6aminocarbonilo, (alquil C1-6)2aminocarbonilo, carboxi(alquil C1-6)aminocarbonilo, ciano, halogeno, trifluorometilo, trifluorometoxi, hidroxi, alquilC1- 6sulfonilo, alquilC1-6sulfonilamino, -C(O)-NH-CH-(-Rc)-C(O)-NH2 y alquilo C1-6; donde alquilo de R3 está opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste en hidroxi, carboxi, alcoxiC1-4carbonilo, amino, alquilamino C1- 6, (alquil C1-6)2amino, aminocarbonilo, (alquil C1-4)aminocarbonilo, di(alquil C1-4)aminocarbonilo, arilo, heteroarilo, arilamino, heteroarilamino, ariloxi, heteroariloxi, aril(alcoxi C1-4) y heteroaril(alcoxi C1-4); Rc se selecciona del grupo que consiste en hidrogeno, alquilo C1-6, alquilC1-6carbonilo, alcoxiC1-6carbonilo, alquilC1-6carbonilamino, aril(alquilo C1-6), heteroaril(alquilo C1-6), arilo, y heteroarilo; R4 es arilo o heteroarilo; donde R4 está opcionalmente sustituido con uno a cinco sustituyentes independientemente seleccionados del grupo R41; donde R41 es alquilo C1-6, alcoxi C1-6, aril(alcoxi C1-6), aril(alquil C1-6)carboniloxi, heteroaril(alquil C1-6)carboniloxi, heteroarilo, hidroxi, halogeno, aminosulfonilo, formilamino, aminocarbonilo, alquilC1-6aminocarbonilo, (alquil C1-6)2aminocarbonilo, heterociclilcarbonilo, carboxi, o ciano; y donde alquilo C1-6 está opcionalmente sustituido con amino, alquilC1-6amino, o (alquil C1-6)2amino; y donde la porcion arilo de aril(alquil C1-6)carboniloxi está opcionalmente sustituida con uno a cuatro sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, alcoxi C1-6, halogeno, ciano, amino, e hidroxi; R5 es un sustituyente en un átomo de nitrogeno contenido en un anillo ha seleccionado del grupo que consiste en hidrogeno, alquilo C1-4 y arilo; R6 se selecciona del grupo que consiste en hidrogeno y alquilo C1-6; R7 se selecciona del grupo que consiste en hidrogeno y alquilo C1-6; Ra y Rb son sustituyentes independientemente seleccionados del grupo que consiste en hidrogeno y alquilo C16; o Ra y Rb, cuando son distintos de hidrogeno, se toman junto con el nitrogeno al que ambos están unidos para formar un anillo monocíclico de cinco a ocho miembros; L se selecciona del grupo que consiste en O, S y N(Rd); donde Rd es hidrogeno, alquilo C1-6 o arilo; y enantiomeros, diastereomeros, racematos aceptables para uso farmacéutico, y sales de los mismos.
ARP050101007A 2004-03-15 2005-03-15 Compuestos moduladores de receptores opioides AR048269A1 (es)

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ARP050101007A AR048269A1 (es) 2004-03-15 2005-03-15 Compuestos moduladores de receptores opioides
ARP140101566A AR095848A2 (es) 2004-03-15 2014-04-11 Derivados imidazolicos de propionamida moduladores de receptores opioides

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