CO5200852A1 - Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides - Google Patents

Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides

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Publication number
CO5200852A1
CO5200852A1 CO00069653A CO00069653A CO5200852A1 CO 5200852 A1 CO5200852 A1 CO 5200852A1 CO 00069653 A CO00069653 A CO 00069653A CO 00069653 A CO00069653 A CO 00069653A CO 5200852 A1 CO5200852 A1 CO 5200852A1
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Colombia
Prior art keywords
optionally substituted
alkyl
hydrogen
alkenyl
independently
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CO00069653A
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English (en)
Inventor
Robert J Ardecky
Marcus F Boehm
Amy L Faulkner
Lawrence G Hamann
Todd K Jones
Christopher M Mapes
Pierre Yves Michellys
John S Tyhonas
Anthony W Thompson
Chen Jyun-Hung
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Lilly Co Eli
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Publication of CO5200852A1 publication Critical patent/CO5200852A1/es

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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—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
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
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    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—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
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    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—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

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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

Un compuesto modulador RXR que tiene la estructura:<EMI FILE="00069653_1" ID="1" IMF=JPEG >en dondeR1 es hidrógeno, F, CI, Br, ó I;R2 hasta R4 cada uno independientemente se seleccionan del grupo conformado por hidrógeno, alquil y heteroalquil C1-C5 opcionalmente sustituidos, haloalquil C1-C5, cicloalquil C3-C7 opcionalmente sustituido, alquenil, heteroalquenil y alquinil C2-C5 opcionalmente sustituidos, haloalquenil y haloalquinil C2-C5, aril, heteroaril, alcoxi, ariloxi; ó R2 y R4 cada uno independientemente es NR10R11; ó R2 y R3 ó R3 y R4 tomados en conjunto forman un sistema anular carbocíclico ó heterocíclico de cinco a siete miembros opcionalmente sustituido; R5 y R6 cada uno independientemente son hidrógeno, F, CI, Br, I, CN, NH2, OH, SH, alquil ó heteroalquil C1-C3 opcionalmente sustituidos, alquenil ó heteroalquenil C2-C3 opcionalmente sustituidos; ó R5 y R6 tomados en conjunto forman un sistema anular carbocíclico ó heterocíclico de tres a ocho miembros; R7 es alquil C1-C5 opcionalmente sustituido, alquenil C2-C5 opcionalmente sustituido, ó haloalquil C2-C5; R8 es hidrógeno, F, CI, Br, I, CN, alquil ó heteroalquil C1-C3 opcionalmente sustituidos, haloalquil C1-C3, alquenil C2-C3 opcionalmente sustituido, ó haloalquenil ó alquinil C2-C3; R9 es hidrógeno ó halógeno; R10 y R11 cada uno independientemente es H ó alquil ó tomados en conjunto forman un anillo cicloalquílico de 5 ó 6 miembros; R12 es hidrógeno ó alquil; y Y es NR12; compuesto que cuando es administrado a un individuo, disminuye los niveles de glucosa sanguínea, pero no eleva los triglicéridos.
CO00069653A 1999-09-14 2000-09-14 Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides CO5200852A1 (es)

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US15389099P 1999-09-14 1999-09-14

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CO5200852A1 true CO5200852A1 (es) 2002-09-27

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CO00069653A CO5200852A1 (es) 1999-09-14 2000-09-14 Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides

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US (2) US6593493B1 (es)
EP (1) EP1216221A2 (es)
JP (1) JP2003529545A (es)
AU (1) AU7586600A (es)
CA (1) CA2383565A1 (es)
CO (1) CO5200852A1 (es)
PE (1) PE20010647A1 (es)
WO (1) WO2001019770A2 (es)

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US6593493B1 (en) 2003-07-15
US20040049072A1 (en) 2004-03-11
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WO2001019770A2 (en) 2001-03-22

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