CO6210771A2 - Moduladores 2-aminopirimidina del receptor de histamina h4 - Google Patents

Moduladores 2-aminopirimidina del receptor de histamina h4

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Publication number
CO6210771A2
CO6210771A2 CO09089676A CO09089676A CO6210771A2 CO 6210771 A2 CO6210771 A2 CO 6210771A2 CO 09089676 A CO09089676 A CO 09089676A CO 09089676 A CO09089676 A CO 09089676A CO 6210771 A2 CO6210771 A2 CO 6210771A2
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Colombia
Prior art keywords
compounds
formula
alkyl
methyl
pharmaceutically acceptable
Prior art date
Application number
CO09089676A
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English (en)
Inventor
Hui Cai
Frank Chavez
James P Edwards
Jing Liu
Neelakandha Mani
Michele C Rizzolio
Brad M Savall
Deborah Smith
Jennifer D Venable
Jianmei Wei
Danielle K Wiener
Ronald L Wolin
Original Assignee
Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of CO6210771A2 publication Critical patent/CO6210771A2/es

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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
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    • 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]
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D239/24—Heterocyclic 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
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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • C07D401/04—Heterocyclic 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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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/04—Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D471/00—Heterocyclic 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
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Abstract

Se describen compuestos de 2-aminopirimidina, que son útiles como moduladores del receptor de H4; dichos compuestos se pueden usar en composiciones farmacéuticas y métodos para el tratamiento de estados de enfermedad, trastornos y condiciones mediadas por la actividad del receptor de H4 tales como alergia, asma, enfermedades autoinmunes y prurito. 1.- Una entidad química seleccionada de compuestos de la fórmula (I):en donde R1 es: a) un grupo alquilo de C1-6, opcionalmente sustituido con -OH, -Oalquilo de C1-4, -CF3, o -O-(cicloalquilo monocíclico); b) un grupo bencilo, -CH2-(heteroarilo monocíclico) o fenetilo, cada uno opcionalmente sustituido con halógeno; c) un grupo cicloalquilo monocíclico, -(CH2)0-1-tetrahidrofuranilo, o -(CH2)0-1-tetrahidropiranilo, cada uno opcionalmente fusionado a un anillo de fenilo, y cada uno opcionalmente sustituido con alquilo de C1-4 o fenilo; o d) un grupo adamantilo; R2 es H, F, metilo o metoxi; o R1 y R2 tomados juntos forman -(CH2)3-5- o -(CH2)2OCH2-; y -N(R3)R4 es uno de los siguientes sistemas acíclico, monocíclico, espirocíclico, en puente o de anillo fusionado:en donde q es 0 o 1; R3 y R4 se toman juntos como se define por la estructura de cada una de dichas porciones; Ra es H o OH; Rb y Rc son cada uno independientemente H o alquilo de C1-3; y cada sustituyente Rd es metilo o dos sustituyentes Rd tomados juntos forman un puente de metileno o etileno; siempre que cuando R1 es metilo, entonces -N(R3)R4 se selecciona de dichos sistemas espirocíclico, en puente y de anillo fusionado; y sales farmacéuticamente aceptables de compuestos de la fórmula (I), profármacos farmacéuticamente aceptables de compuestos de la fórmula (I), y metabolitos farmacéuticamente aceptables de la fórmula (I).
CO09089676A 2007-02-14 2009-08-26 Moduladores 2-aminopirimidina del receptor de histamina h4 CO6210771A2 (es)

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US (6) US7923451B2 (es)
EP (2) EP2124560A4 (es)
JP (1) JP5281586B2 (es)
KR (1) KR20090110877A (es)
CN (1) CN101668423B (es)
AR (1) AR065354A1 (es)
AU (1) AU2008216727B2 (es)
BR (1) BRPI0807815A2 (es)
CA (1) CA2678077A1 (es)
CL (1) CL2008000467A1 (es)
CO (1) CO6210771A2 (es)
CR (1) CR11027A (es)
EA (1) EA016133B1 (es)
EC (1) ECSP099582A (es)
GT (1) GT200900231A (es)
IL (1) IL200335A0 (es)
MX (1) MX2009008787A (es)
NI (1) NI200900159A (es)
NZ (1) NZ578977A (es)
PE (1) PE20081776A1 (es)
TW (1) TW200904437A (es)
UY (1) UY30917A1 (es)
WO (1) WO2008100565A1 (es)

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JP6635949B2 (ja) 2014-06-04 2020-01-29 トーマス・ヘレデイズ・スティフテルス・フォー・メディシンスク・フォルスクニング 炎症性および自己免疫性の病気の処置のためのｍｔｈ１阻害剤
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