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PE20121613A1 - Derivados de quinolina amida como moduladores alostericos positivos de receptores m1 - Google Patents

Derivados de quinolina amida como moduladores alostericos positivos de receptores m1

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Publication number
PE20121613A1
PE20121613A1 PE2012000830A PE2012000830A PE20121613A1 PE 20121613 A1 PE20121613 A1 PE 20121613A1 PE 2012000830 A PE2012000830 A PE 2012000830A PE 2012000830 A PE2012000830 A PE 2012000830A PE 20121613 A1 PE20121613 A1 PE 20121613A1
Authority
PE
Peru
Prior art keywords
quinoline
alkyl
receptors
halogen
derivatives
Prior art date
Application number
PE2012000830A
Other languages
English (en)
Inventor
Scott D Kududk
Kelly-Ann Schlegel
Zhi-Qiang Yang
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20121613A1 publication Critical patent/PE20121613A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60N-oxides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/47042-Quinolinones, e.g. carbostyril
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • 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]
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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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
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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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
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    • 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
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    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE QUINOLINA DE FORMULA (I), DONDE X1 ES N O N-O; X2-X3 ES -CH2-CH2-, -O-CH2, -CH2-O- O CH2; X4, X5, X6 Y X7 SON N, N-O, CH, O; R1 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R2A Y R2B SON H, OH, HALOGENO, JUNTOS FORMAN =O; R3 ES HALOGENO, O-ALQUILO C1-C6, S-ALQUILO C1-C6, ENTRE OTROS; R4 ES OH, HALOGENO, ALQUILO C1-C6, O-ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-[(6-CLOROPIRIDIN-3-IL)METIL]-N-[(1S,2S)-2-HIDROXICICLOHEXIL]QUINOLINA-2-CARBOXAMIDA, N-[(1S,2S)-2-HIDROXICICLOHEXIL]-4-[(6-METILPIRIDIN-3-IL)METIL]QUINOLINA-2-CARBOXAMIDA, N-[(1S,2S)-2-HIDROXICICLOHEXIL]-4-(PIRIDIN-3-ILMETIL)QUINOLINA-2-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS DE LOS RECEPTORES M1 Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS TALES COMO LA ENFERMEDAD DE ALZHEIMER, ESQUIZOFRENIA, TRASTORNOS DEL DOLOR O DEL SUENO
PE2012000830A 2009-12-17 2010-12-13 Derivados de quinolina amida como moduladores alostericos positivos de receptores m1 PE20121613A1 (es)

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US28753509P 2009-12-17 2009-12-17

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US (2) US9199939B2 (es)
EP (1) EP2512243B1 (es)
JP (1) JP5651708B2 (es)
KR (1) KR101494059B1 (es)
CN (1) CN102651970B (es)
AR (1) AR079510A1 (es)
AU (1) AU2010340142B2 (es)
BR (1) BR112012014180A2 (es)
CA (1) CA2782347C (es)
CL (1) CL2012001605A1 (es)
CO (1) CO6551729A2 (es)
CR (1) CR20120327A (es)
CY (1) CY1117726T1 (es)
DK (1) DK2512243T3 (es)
DO (1) DOP2012000167A (es)
EA (1) EA022494B1 (es)
EC (1) ECSP12011983A (es)
ES (1) ES2575154T3 (es)
GE (1) GEP201606506B (es)
GT (1) GT201200201A (es)
HN (1) HN2012001265A (es)
HR (1) HRP20160574T1 (es)
HU (1) HUE029734T2 (es)
IL (1) IL220130A0 (es)
MA (1) MA33920B1 (es)
ME (1) ME02421B (es)
MX (1) MX336774B (es)
NI (1) NI201200107A (es)
NZ (1) NZ600674A (es)
PE (1) PE20121613A1 (es)
PH (1) PH12012501222A1 (es)
PL (1) PL2512243T3 (es)
PT (1) PT2512243E (es)
RS (1) RS54798B1 (es)
SG (1) SG181719A1 (es)
SI (1) SI2512243T1 (es)
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UA (1) UA106406C2 (es)
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