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PE20060620A1 - Analogos de biaril piperazinil-piridina sustituidos como moduladores del receptor de capsaicina vr1 - Google Patents

Analogos de biaril piperazinil-piridina sustituidos como moduladores del receptor de capsaicina vr1

Info

Publication number
PE20060620A1
PE20060620A1 PE2005000929A PE2005000929A PE20060620A1 PE 20060620 A1 PE20060620 A1 PE 20060620A1 PE 2005000929 A PE2005000929 A PE 2005000929A PE 2005000929 A PE2005000929 A PE 2005000929A PE 20060620 A1 PE20060620 A1 PE 20060620A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
phenyl
modulators
substituted
Prior art date
Application number
PE2005000929A
Other languages
English (en)
Inventor
Charles A Blum
Harry Brielmann
Xiaozhang Zheng
Bertrand L Chenard
Original Assignee
Neurogen Corp
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 Neurogen Corp filed Critical Neurogen Corp
Publication of PE20060620A1 publication Critical patent/PE20060620A1/es

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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
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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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Child & Adolescent Psychology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE BIARIL PIPERAZINIL-PIRIDINA DE FORMULA II, DONDE Ar2 ES FENILO O HETEROCICLO DE SEIS MIEMBROS, CADA UNO DE LOS CUALES ESTA SUSTITUIDO CON 0 A 4 SUSTITUYENTES ELEGIDOS DE R2; X, Y Y Z SON CRx O N, DE TAL MODO QUE POR LO MENOS UNO DE X, Y Y Z ES N; D, K, J Y F SON N, CH O CARBONO SUSTITUIDO CON UN SUSTITUYENTE REPRESENTADO POR R1 O R10; Rx ES H, HALOGENO, ALQUILO C1-C4, ENTRE OTROS; R1 ES HALOGENO, CIANO, NITRO, ENTRE OTROS; R10 ES UN GRUPO DE FORMULA -Q-M-Ry Y GRUPOS QUE SE FORMAN CON R1 PARA FORMAR UN ANILLO HETEROCICLO O CARBOCICLO DE 5 A 7 MIEMBROS, ENTRE OTROS; Q ES ALQUILENO C0-C4; M ES O, C(=O), OC(=O), ENTRE OTROS; Ry ES H, HALOALQUILO C1-C8, ALQUILO C1-C8, ENTRE OTROS; R2 ES OH, AMINO, CIANO, ENTRE OTROS; R3 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R4 ES ALQUILO C1-C3, HALOALQUILO C1-C3 U OXO. SON COMPUESTOS PREFERIDOS: 2-{4-[6-(3-CLORO-4-FLUOR-FENIL)-2-MORFOLIN-4-IL-PIRIMIDIN-4-IL]-PIPERAZIN-1-IL}-NICOTINAMIDA, ACIDO 2-{4-[6-(3-CLORO-4-FLUOR-FENIL)-2-MORFOLIN-4-IL-PIRIMIDIN-4-IL]-PIPERAZIN-1-IL}-NICOTINICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE CAPSAICINA VR1 Y SON UTILES EN EL TRATAMIENTO DEL DOLOR CRONICO Y AGUDO, INCLUYENDO DOLOR NEUROPATICO
PE2005000929A 2004-08-13 2005-08-11 Analogos de biaril piperazinil-piridina sustituidos como moduladores del receptor de capsaicina vr1 PE20060620A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US60172104P 2004-08-13 2004-08-13
US64179605P 2005-01-05 2005-01-05

Publications (1)

Publication Number Publication Date
PE20060620A1 true PE20060620A1 (es) 2006-08-11

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PE2005000929A PE20060620A1 (es) 2004-08-13 2005-08-11 Analogos de biaril piperazinil-piridina sustituidos como moduladores del receptor de capsaicina vr1

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US (2) US7662830B2 (es)
EP (1) EP1786800B1 (es)
JP (1) JP4955554B2 (es)
KR (1) KR20070046924A (es)
CN (1) CN101014587B (es)
AR (1) AR050194A1 (es)
BR (1) BRPI0514319A (es)
CA (1) CA2577301C (es)
CR (1) CR8992A (es)
EC (1) ECSP077318A (es)
HN (1) HN2007006799A (es)
IL (1) IL181040A0 (es)
MA (1) MA28857B1 (es)
MX (1) MX2007001696A (es)
MY (1) MY145822A (es)
NI (1) NI200700040A (es)
NO (1) NO20071243L (es)
NZ (1) NZ553388A (es)
PE (1) PE20060620A1 (es)
RU (1) RU2413726C2 (es)
SG (1) SG157399A1 (es)
TW (1) TW200605889A (es)
WO (1) WO2006026135A2 (es)
ZA (1) ZA200701530B (es)

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Also Published As

Publication number Publication date
US20110003813A1 (en) 2011-01-06
MA28857B1 (fr) 2007-09-03
WO2006026135A2 (en) 2006-03-09
JP4955554B2 (ja) 2012-06-20
ZA200701530B (en) 2008-11-26
AR050194A1 (es) 2006-10-04
RU2007106042A (ru) 2008-09-20
NI200700040A (es) 2008-04-01
NO20071243L (no) 2007-04-27
CN101014587A (zh) 2007-08-08
JP2008509932A (ja) 2008-04-03
TW200605889A (en) 2006-02-16
IL181040A0 (en) 2007-07-04
AU2005280366A1 (en) 2006-03-09
CR8992A (es) 2007-08-14
CA2577301C (en) 2014-05-27
RU2413726C2 (ru) 2011-03-10
KR20070046924A (ko) 2007-05-03
MY145822A (en) 2012-04-30
MX2007001696A (es) 2007-04-23
EP1786800A2 (en) 2007-05-23
US7662830B2 (en) 2010-02-16
HN2007006799A (es) 2010-11-03
EP1786800A4 (en) 2009-05-06
SG157399A1 (en) 2009-12-29
EP1786800B1 (en) 2017-01-04
WO2006026135A3 (en) 2006-06-15
BRPI0514319A (pt) 2008-06-10
CN101014587B (zh) 2013-12-18
US8334382B2 (en) 2012-12-18
US20060122394A1 (en) 2006-06-08
CA2577301A1 (en) 2006-03-09
NZ553388A (en) 2011-01-28
ECSP077318A (es) 2007-04-26

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