AR080496A1 - Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad - Google Patents

Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad

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Publication number
AR080496A1
AR080496A1 ARP110100765A ARP110100765A AR080496A1 AR 080496 A1 AR080496 A1 AR 080496A1 AR P110100765 A ARP110100765 A AR P110100765A AR P110100765 A ARP110100765 A AR P110100765A AR 080496 A1 AR080496 A1 AR 080496A1
Authority
AR
Argentina
Prior art keywords
heterocycloalkyl
aminoalkyl
cycloalkyl
aryl
optionally substituted
Prior art date
Application number
ARP110100765A
Other languages
English (en)
Original Assignee
Kalypsys Inc
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 Kalypsys Inc filed Critical Kalypsys Inc
Publication of AR080496A1 publication Critical patent/AR080496A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Abstract

Compuestos y métodos que pueden ser utiles como inhibidores de la H4R para el tratamiento y la prevencion de enfermedades inflamatorias, autoinmunes, alérgicas y oculares. Reivindicacion 1: El compuesto caracterizado porque tiene la formula estructural (1), o una sal del mismo, donde el anillo que comprende X1-5 es aromático; X1 y X5 se seleccionan independientemente de C, CH y N; X2 se selecciona de [C(R6)(R7)], NR8, O y S; X3 se selecciona de [C(R9)(R10)], NR11, O, y S; X4 se selecciono de [C(R12)(R13)], NR14, O y S; X6 se selecciona de CR18 y N; X7 se selecciona de CR19 y N; Y1 se selecciona de un enlace, alquilo inferior, alcoxi inferior, OR15, NR16R17, y aminoalquilo inferior; Y2 se selecciona de un enlace, alquilo inferior, alcoxi inferior, OR20, NR21R22, S, C(O)NH2, C(O)NHR23, C(O)NR23R24 y aminoalquilo inferior; R1 se selecciono del grupo que consiste en: arilo, heterocicloalquilo, cicloalquilo, y heteroarilo, donde cualquiera puede estar opcionalmente sustituido, cuando Y1 es un enlace; y ninguno, cuando Y1 se selecciona de OR15, NR16R17, alquilo inferior, alcoxi inferior, o aminoalquilo inferior; R2, se selecciona de alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterocicloalquilo y heteroarilodonde cualquiera puede estar opcionalmente sustituido; R6, R7, R9, R10, R12, R13, R18 y R19 se seleccionan independientemente de ninguno, hidrogeno, alquilo, alquenilo, alquinilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcíonalmente sustituido; R8, R11, y R14 se seleccionan independientemente de ninguno, hidrogeno, alquilo, heteroalquilo, alcoxi, haloalquilo, perhaloalquilo, aminoalquilo, C-amido, carboxilo, acilo, hidroxi, arilo, arilalquilo, cicloalquilo, cicloaIquiIaIquiIo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; R15, R16, R20 y R21 se seleccionan independientemente de aminoalquilo, alquilaminoalquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilaminoheterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; R17 y R22 se selecciona independientemente de hidrogeno, aminoalquilo, alquilaminoalquil arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilaminoheterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; y R23 y R24 se seleccionan independientemente de hidrogeno, alquilo, alquenilo, alquinilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, perhaloalcoxi, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido.
ARP110100765A 2010-03-10 2011-03-11 Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad AR080496A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US31261510P 2010-03-10 2010-03-10

Publications (1)

Publication Number Publication Date
AR080496A1 true AR080496A1 (es) 2012-04-11

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Country Status (17)

Country Link
US (1) US8569300B2 (es)
EP (1) EP2545058B1 (es)
JP (1) JP5888654B2 (es)
KR (1) KR20130016253A (es)
CN (1) CN102869666B (es)
AR (1) AR080496A1 (es)
AU (1) AU2011224316B2 (es)
BR (1) BR112012022211A2 (es)
CA (1) CA2791417A1 (es)
ES (1) ES2607125T3 (es)
IL (1) IL221829A (es)
MX (1) MX2012010404A (es)
NZ (1) NZ602041A (es)
RU (1) RU2012137180A (es)
TW (1) TW201200518A (es)
UY (1) UY33271A (es)
WO (1) WO2011112766A2 (es)

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Also Published As

Publication number Publication date
AU2011224316A1 (en) 2012-09-13
EP2545058B1 (en) 2016-08-24
JP5888654B2 (ja) 2016-03-22
AU2011224316B2 (en) 2016-09-15
BR112012022211A2 (pt) 2017-07-18
MX2012010404A (es) 2013-05-20
US8569300B2 (en) 2013-10-29
KR20130016253A (ko) 2013-02-14
CN102869666A (zh) 2013-01-09
WO2011112766A3 (en) 2012-01-19
RU2012137180A (ru) 2014-04-20
CA2791417A1 (en) 2011-09-15
EP2545058A4 (en) 2013-07-24
WO2011112766A2 (en) 2011-09-15
ES2607125T3 (es) 2017-03-29
JP2013522222A (ja) 2013-06-13
IL221829A (en) 2014-11-30
EP2545058A2 (en) 2013-01-16
UY33271A (es) 2011-10-31
US20110237565A1 (en) 2011-09-29
TW201200518A (en) 2012-01-01
CN102869666B (zh) 2015-09-09
NZ602041A (en) 2014-08-29

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