AR055619A1 - Diaminopirimidinas como moduladores p2x2/3 - Google Patents

Diaminopirimidinas como moduladores p2x2/3

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Publication number
AR055619A1
AR055619A1 ARP060103785A ARP060103785A AR055619A1 AR 055619 A1 AR055619 A1 AR 055619A1 AR P060103785 A ARP060103785 A AR P060103785A AR P060103785 A ARP060103785 A AR P060103785A AR 055619 A1 AR055619 A1 AR 055619A1
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AR
Argentina
Prior art keywords
alkyl
hydroxyalkyl
alkoxy
aryl
amino
Prior art date
Application number
ARP060103785A
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English (en)
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Hoffmann La Roche
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Publication date
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Publication of AR055619A1 publication Critical patent/AR055619A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links

Abstract

Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, en el que X es -CH2-; -O-; -S(O)n-; o -NRc; en el que n va de 0 a 2 y Rc es H o alquilo; D es un O opcional; R1 es alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, halo, haloalquilo, o hidroxialquilo; R2, R3, R4 y R5 cada uno es independientemente H; alquilo, aminosulfonilo, alquenilo, halo, amido, haloalquilo, alcoxi, hidroxi, haloalcoxi, nitro, amino, hidroxialquilo, alcoxialquilo, hidroxialcoxi, alquinilalcoxi, alquilsulfonilo, arilsulfonilo, ciano, arilo, heteroarilo, heterociclilo, heterociclilalcoxi, ariloxi, heteroariloxi, aralquiloxi, heteroaralquiloxi, fenoxi opcionalmente sustituido, ; -C:::C-Ra-; - (CH2)m-(Z)n-(CO)-Rb; -(CH2)m-(Z)n-SO2-(NRc)n-Rb; en el que m y n cada uno es independientemente 0 o 1, Z es O o NRc; Ra es H, alquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, hidroxialquilo, alcoxialquilo, alquilsulfonilalquilo, aminoalquilo, cianoalquilo, alquilsililo, cicloalquilo, cicloalquilalquilo, heterociclo; y heterocicliloalquilo; Rb es H, alquilo, hidroxi, alcoxi, amino, hidroxialquilo o alcoxialquilo, y cada Rc es independientemente H o alquilo; o R3 y R4 junto con los átomos a los que están unidos pueden formar un anillo de 5 o 6 miembros que opcionalmente incluye uno o dos heteroátomos seleccionados de entre O, S y N; o R2 y R3 junto a los átomos a los que están unidos pueden formar un anillo de 5 o 6 miembros que opcionalmente incluye uno o dos heteroátomos seleccionados de entre O, S y N; R6 es H, alquilo, halo, haloalquilo, amino, o alcoxi; y uno de R7 y R8 es H y el otro es R9, o ambos R7 y R8 son R9; cada R9 es independientemente -(C=O)-Rd; - (O=)P(ORg)2; -S(=O)2ORg; o un mono-, di- o tri-péptido, donde Rd es alquilo, alcoxi, alcoxialquilo, alcoxialcoxialquilo, alquilcarboniloxialquilo, amino, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroariloalquilo, heterociclilo, cicloalquiloxi, cicloalquilalquiloxi, ariloxi, arilalquiloxi, heteroariloxi, heteroariloalquiloxi, heterocicliloxi, hidroxialquilo, -(CH2)p-C(=O)-Re, -(CH=CH)-C(=O)-Re, o -CH(NH2)-Rf; en el que Re es H, hidroxi, alquilo, alcoxi, amino, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroariloalquilo, heterociclilo, cicloalquiloxi, cicloalquilalquiloxi, ariloxi, arilalquiloxi, heteroariloxi, heteroariloalquiloxi, o heterocicliloxi; p es 2 o 3; Rf es H, alquilo, hidroxialquilo, aminoalquilo, fenilo opcionalmente sustituido, bencilo, guanidinilalquilo, carboxialquilo, amidoalquilo, tioalquilo o imidazolalquilo; y Rg es H, alquilo, un ion metálico alcalino o un ion metálico alcalino-térreo; siempre y cuando R1 sea isopropilo, R2, R5 y R6 sean H, R3 sea metoxi y R4 sea metilo o metoxi, entonces Rd no sea metilo.
ARP060103785A 2005-09-01 2006-08-30 Diaminopirimidinas como moduladores p2x2/3 AR055619A1 (es)

Applications Claiming Priority (1)

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US71339805P 2005-09-01 2005-09-01

Publications (1)

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AR055619A1 true AR055619A1 (es) 2007-08-29

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ID=37116194

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US (1) US7799796B2 (es)
EP (1) EP1924566B1 (es)
JP (1) JP4850913B2 (es)
CN (1) CN101300235B (es)
AR (1) AR055619A1 (es)
CA (1) CA2620129C (es)
ES (1) ES2562056T3 (es)
TW (1) TW200745056A (es)
WO (1) WO2007025901A1 (es)

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JP2009506999A (ja) 2009-02-19
CA2620129C (en) 2014-12-23
US7799796B2 (en) 2010-09-21
TW200745056A (en) 2007-12-16
CN101300235B (zh) 2011-12-07
CN101300235A (zh) 2008-11-05
ES2562056T3 (es) 2016-03-02
US20070049534A1 (en) 2007-03-01
CA2620129A1 (en) 2007-03-08

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