CO6150182A2 - Modulares de benzofuro y benzotienopirimidina del receptor h4 de histamina - Google Patents

Modulares de benzofuro y benzotienopirimidina del receptor h4 de histamina

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Publication number
CO6150182A2
CO6150182A2 CO09005353A CO09005353A CO6150182A2 CO 6150182 A2 CO6150182 A2 CO 6150182A2 CO 09005353 A CO09005353 A CO 09005353A CO 09005353 A CO09005353 A CO 09005353A CO 6150182 A2 CO6150182 A2 CO 6150182A2
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Colombia
Prior art keywords
chemical entity
further characterized
accordance
formula
methoxy
Prior art date
Application number
CO09005353A
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English (en)
Inventor
Frank Chavez
Michael P Curtis
James P Edwards
Laurent Gomez
Cheryl A Grice
Aaron M Kearney
Brad M Savall
Anne E Fitzgerald
Jing Liu
Neelakandha Mani
Original Assignee
Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of CO6150182A2 publication Critical patent/CO6150182A2/es

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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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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
    • C07D471/02—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 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
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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
    • C07D239/28—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 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
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  • Cardiology (AREA)
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  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
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Abstract

1.- Una entidad química seleccionada de compuestos de la fórmula (I):en donde R1 y R2 son cada uno independientemente H, CI, F, Br, metilo, etilo, metoxi, NO2, o CF3; R5 es H, metoxi, CI, F, Br, o CF3; A es N o CRa; donde Ra es H o CI; con la condición de que al menos dos de R1, R2, R5, y Ra sean H; X es O o S; -N(R3)R4 es uno de los radicales: donde q es 0 o 1; R3 y R4 se toman en conjunto o separadamente como se define por la estructura de cada uno de dichos radicales; Rb, Rc, y Rd son cada uno independientemente H o alquilo de C1-3, y cada sustituyente Re es metilo o dos sustituyentes Re tomados juntos forman un puente metileno o etileno; R6 es H o metilo; R7 es H; alquilo de C1-4 no sustituido o sustituido con -OH, -SCH3, o -NH2; alilo; o ciclopropilo; y sales farmacéuticamente aceptables de compuestos de fórmula (I), profármacos farmacéuticamente aceptables de compuestos de fórmula (I), y metabolitos farmacéuticamente activos de fórmula (I). 2.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque R1 es H, metoxi, CI, Br, F, o CF3. 3.- La entidad química de conformidad con a reivindicación 1, caracterizada además porque R2 es H. 4.- La entidad química de conformidad con la reivindicación 2, caracterizada además porque R2 es H. 5.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque R5 es H o CF3. 6.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque A es N. 7.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque A es CRa.
CO09005353A 2006-07-11 2009-01-22 Modulares de benzofuro y benzotienopirimidina del receptor h4 de histamina CO6150182A2 (es)

Applications Claiming Priority (1)

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US83019206P 2006-07-11 2006-07-11

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CO6150182A2 true CO6150182A2 (es) 2010-04-20

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US (2) US7576092B2 (es)
EP (1) EP2040549B1 (es)
JP (1) JP5352458B2 (es)
KR (1) KR20090028819A (es)
CN (1) CN101511190A (es)
AR (1) AR061891A1 (es)
AU (1) AU2007272956B2 (es)
BR (1) BRPI0715452A2 (es)
CA (1) CA2657908A1 (es)
CL (1) CL2007002007A1 (es)
CO (1) CO6150182A2 (es)
CR (1) CR10609A (es)
EA (1) EA015344B1 (es)
EC (1) ECSP099061A (es)
ES (1) ES2441958T3 (es)
IL (1) IL196448A0 (es)
MX (1) MX2009000457A (es)
MY (1) MY145349A (es)
NO (1) NO20090268L (es)
PE (1) PE20080520A1 (es)
TW (1) TW200821315A (es)
UY (1) UY30479A1 (es)
WO (1) WO2008008359A2 (es)
ZA (1) ZA200900959B (es)

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CL2008000467A1 (es) 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
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MY156663A (en) 2008-06-12 2016-03-15 Janssen Pharmaceutica Nv Use of a histamine h4 antagonist for the treatment of post-operative adhesions
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WO2010064705A1 (ja) * 2008-12-05 2010-06-10 大日本住友製薬株式会社 Ｈ４受容体アンタゴニスト作用を有する新規７位置換ジヒドロピラノピリミジン誘導体
WO2010075270A1 (en) 2008-12-22 2010-07-01 Incyte Corporation 4, 6-disubstituted 2-amino-pyrimidines as histamine h4 receptor modulators
EP2201982A1 (en) 2008-12-24 2010-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Histamine H4 receptor antagonists for the treatment of vestibular disorders
IT1393337B1 (it) 2009-03-06 2012-04-20 Italiana Sint Spa Sintesi di (4as, 7as)-ottaidro-1h-pirrolo[3,4-b]piridina
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
EP2671883A1 (en) 2012-06-05 2013-12-11 Bioprojet New 6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands
ES2683380T3 (es) 2012-06-08 2018-09-26 Sensorion Inhibidores del receptor H4 para tratar el tinnitus
CN102875558A (zh) * 2012-11-05 2013-01-16 贵州大学 2-氯-4-取代-8-硝基苯并呋喃[3,2-d]嘧啶类化合物及其制备方法和用途
SG11201507117XA (en) 2013-03-06 2015-10-29 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor
JPWO2017131171A1 (ja) * 2016-01-29 2018-11-22 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 新規化合物及びその薬理学的に許容される塩
JP7507161B2 (ja) 2019-01-04 2024-06-27 ベルブルック ラボズ，エルエルシー 治療薬としてのｃＧＡＳ活性の阻害剤
CN116997339A (zh) * 2021-02-11 2023-11-03 贝尔布鲁克实验室有限责任公司 作为治疗剂的cGAS活性抑制剂
CN116589472B (zh) * 2023-05-22 2024-09-13 郑州大学 一种苯并呋喃[3,2-d]并嘧啶-2-胺类化合物及其制备方法和应用

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