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PE20070848A1 - Derivados de pirimidina como ligandos del receptor de histamina h4 - Google Patents

Derivados de pirimidina como ligandos del receptor de histamina h4

Info

Publication number
PE20070848A1
PE20070848A1 PE2006001621A PE2006001621A PE20070848A1 PE 20070848 A1 PE20070848 A1 PE 20070848A1 PE 2006001621 A PE2006001621 A PE 2006001621A PE 2006001621 A PE2006001621 A PE 2006001621A PE 20070848 A1 PE20070848 A1 PE 20070848A1
Authority
PE
Peru
Prior art keywords
alkyl
dimethylbutyl
pyrimidin
cycloalkyl
histamine
Prior art date
Application number
PE2006001621A
Other languages
English (en)
Inventor
Andrew Simon Bell
Charlotte Alice Louise Lane
Matthew Duncan Selby
Nigel Alan Swain
David Howard Williams
Charles Eric Mowbray
Original Assignee
Pfizer Ltd
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 Pfizer Ltd filed Critical Pfizer Ltd
Publication of PE20070848A1 publication Critical patent/PE20070848A1/es

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    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
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    • 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
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • 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]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
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    • 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
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    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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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    • 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
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    • 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
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    • C07D497/08Bridged systems

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
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  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C8), CICLOALQUIL(C3-C7)-ALQUILO(C0-C6) OPCIONALMENTE SUSTITUIDO CON METILO, ALCOXIALQUILO(C3-C8), CF3-ALQUILO(C1-C6), ENTRE OTROS; R2 ES NH(CH2)2NH2, NH(CH2)2NHCH3, NH(CH2)2NH(CH3)2, ENTRE OTROS; R3 ES H, ALQUILO(C1-C8), (CH2)p-CICLOALQUILO(C3-C7), ALCOXIALQUILO(C3-C8), ENTRE OTROS; R4 ES H O R1 Y R4 JUNTO CON EL ATOMO DE N AL QUE ESTAN UNIDOS FORMAN UN GRUPO HETEROCICLICO NO AROMATICO DE 4 A 8 MIEMBROS QUE CONTIENE UNO O MAS HETEROATOMOS SELECCIONADOS DE N, O, S, S(O) O S(O)2, ENTRE OTROS; R5 ES H O NR11R12, DONDE R11 Y R12 SON CADA UNO H, ALQUILO(C1-C6), (CH2)l-CICLOALQUILO(C3-C7), ENTRE OTROS; l Y p SON DE 0 A 3; R8 ES H O ALQUILO(C1-C3). SON COMPUESTOS PREFERIDOS: N-(3,3-DIMETILBUTIL)-6-(4-METILPIPERAZIN-1-IL)PIRIMIDIN-4-AMINA, N-(3,3-DIMETILBUTIL)-N'-[(3S)-PIRROLIDIN-3-IL]PIRIMIDIN-4,6-DIAMINA, N-(3,3-DIMETILBUTIL)-N'-[(3R)-PIRROLIDIN-3-IL]PIRIMIDIN-4,6-DIAMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON LIGANDOS DEL RECEPTOR DE HISTAMINA H4 SIENDO UTILES EN EL TRATAMIENTO DE ASMA, RINITIS ALERGICA, TRASTORNO PULMONAR OBSTRUCTIVO CRONICO
PE2006001621A 2005-12-20 2006-12-18 Derivados de pirimidina como ligandos del receptor de histamina h4 PE20070848A1 (es)

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US75261205P 2005-12-20 2005-12-20

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PE20070848A1 true PE20070848A1 (es) 2007-09-10

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PE2006001621A PE20070848A1 (es) 2005-12-20 2006-12-18 Derivados de pirimidina como ligandos del receptor de histamina h4

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US (1) US7943628B2 (es)
EP (1) EP1966162B1 (es)
JP (1) JP5166280B2 (es)
KR (2) KR20120025010A (es)
CN (1) CN101341134B (es)
AP (1) AP2008004486A0 (es)
AR (1) AR058557A1 (es)
AU (1) AU2006327876B2 (es)
BR (1) BRPI0620201A2 (es)
CA (1) CA2634018C (es)
CR (1) CR10061A (es)
CY (1) CY1118987T1 (es)
DK (1) DK1966162T3 (es)
DO (1) DOP2006000288A (es)
EA (1) EA200801381A1 (es)
EC (1) ECSP088559A (es)
ES (1) ES2628482T3 (es)
GT (1) GT200600518A (es)
HR (1) HRP20170896T1 (es)
HU (1) HUE034650T2 (es)
IL (1) IL191432A (es)
LT (1) LT1966162T (es)
MA (1) MA30082B1 (es)
ME (1) ME00004B (es)
NL (1) NL2000323C2 (es)
NO (1) NO341075B1 (es)
PE (1) PE20070848A1 (es)
PL (1) PL1966162T3 (es)
PT (1) PT1966162T (es)
RS (2) RS56102B1 (es)
SI (1) SI1966162T1 (es)
TN (1) TNSN08269A1 (es)
TW (1) TW200732306A (es)
UY (1) UY30045A1 (es)
WO (1) WO2007072163A2 (es)
ZA (1) ZA200805294B (es)

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