BRPI0518424A2 - derivados de 2,4 (4,6) pirimidina - Google Patents

derivados de 2,4 (4,6) pirimidina

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Publication number
BRPI0518424A2
BRPI0518424A2 BRPI0518424-0A BRPI0518424A BRPI0518424A2 BR PI0518424 A2 BRPI0518424 A2 BR PI0518424A2 BR PI0518424 A BRPI0518424 A BR PI0518424A BR PI0518424 A2 BRPI0518424 A2 BR PI0518424A2
Authority
BR
Brazil
Prior art keywords
alkyl
het
piperazinyl
hydrogen
pyrrolidinyl
Prior art date
Application number
BRPI0518424-0A
Other languages
English (en)
Inventor
Eddy Jean Adgard Freyne
Marc Willems
Werner Constant Johan Embrechts
Emelen Kristof Van
Brandt Sven Franciscus Anna Van
Frederik Jan Rita Rombouts
Original Assignee
Jassen Pharaceutica N V
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.)
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Publication date
Application filed by Jassen Pharaceutica N V filed Critical Jassen Pharaceutica N V
Publication of BRPI0518424A2 publication Critical patent/BRPI0518424A2/pt
Publication of BRPI0518424B1 publication Critical patent/BRPI0518424B1/pt
Publication of BRPI0518424B8 publication Critical patent/BRPI0518424B8/pt

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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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/18Bridged systems
    • 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
    • C07D487/08Bridged 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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
    • AHUMAN NECESSITIES
    • 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
    • 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
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • 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
    • C07D498/08Bridged 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
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/18Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)

Abstract

DERIVADOS DE 2,4 (4,6) PIRIMIDINA. A presente invenção refere-se a compostos da fórmula. As formas de N-óxido, os sais de adição farmaceuticamente aceitáveis e as formas estereoquimicamente isoméricas dos mesmos, em que: Z¹ e Z² representa NH; Y representa -C~ 3-9~ alquila-, -C~ 3-9~ alquenila-, -C~ 1-5~ alquil-NR^ 6^-C~ 1-5~ alquila-, -C~ 1-5~ alquil-NR^ 7^-CO-C~ 1-5~ alquila-, -C~ 1-6~ alquil-CO-NH-, -C~ 1-6~ alquil- NH-CO-, -C~ 1-2~ alquil-CO-Het^ 10^-CO-, -C~ 1-3~ alquil-NH-CO-Hetü-, -Het^ 4^-C.~ 1-3~ alquil-CO-NH-C~ 1-3~ alquila-, -C~ 1-2~ alquil-NH-CO-L¹-NH-, -NH-CO-L²-NH-, -C~ 1-2~ alquil-CO-NH-Lü-CO-, -C~ 1-2~ alquil-NH-CO-L¹-NH-CO-C~ 1-3~ alquila-, -C~ 1-2~ alquil- CO-NH-Lü-CO-NH-C~ 1-3~ alquila-, -C~ 1-2~ alquil-NR¹¹-CH~ 2~-CO-NH-C~ 1-3~ alquila-, Het^ 5^-CO-C~ 1-2~ alquila, -C~ 1-5~ aIquiI-CO-NH-C~ 1-3~ alquil-CO-NH-, -C~ 1-5~ alquil- NR¹ü-CO-C~ 1-3~ alquil-NH-, -C13 alquil-NH-CO-Het^ 27^-CO- ou -C~ 1-3~ alquil-CO- Het^ 28^-CO-NH-; X¹ representa uma ligação direta, O, -O-C~ 1-2~ alquila-, -CO-C~ 1-2~ alquila-, -NR^ 16^-C~ 1-2~ alquila-, -CO-NR^ 17^-, Het^ 23^-C~ 1-2~ alquila- ou C~ 1-2~ alquila; X² representa uma ligação direta, O, -O-C~ 1-2~ alquila-, -CO-C~ 1-2~ alquila-, -NR^ 18^-C~ 1-2~ alquila-, -CO-NR^ 19^-, Het^ 24^-C~ 1-2~ alquila- ou C~ 1-2~ alquila; R¹ e R^ 5^ representam, cada um independentemente, hidrogênio, halo, C~ 1-6~ alquilóxi- ou C~ 1-6~ alquilóxi- substituído por Het¹ ou C~ 1-4~ alquilóxi-; R² e R^ 4^ representam, cada um independentemente, hidrogênio ou halo; Rü representa hidrogênio ou ciano; R^ 6^, R^ 7^, R^ 13^, R^ 17^ e R^ 19^ representam hidrogênio; R¹¹ representa hidrogênio ou C~ 1-4~ alquila; R^ 16^e R^ 18^ representa hidrogênio, C~ 1-4~ alquila ou Het^ 17^-C~ 1-4~ alquila-; L¹, L¹ e Lü representam, cada um independentemente, C~ 1-8~ alquila opcionalmente substituida por um ou, onde possível, dois ou mais substituintes selecionados de fenita, metil-sulfeto, ciano, C~ 1-4~ polihaloalquil- fenila-, C~ 1-4~ alquilóxi, piridinila, mono- ou di(C~ 1-4~ alquil)-amino- ou C~ 3-6~ ciclo alquila; Het¹, Het², Het^ 17^ representam, cada um independentemente, morfolinila, oxazolila, isoxazolila ou piperazinila; Hetü, Het^ 4^, Het^ 5^ representam, cada um independentemente, mor- folinila, piperazinila, piperidinila ou pirrolidinila; Het^ 10^ representa piperazinila, piperidinila, pirrolidinila ou azetidinila; Het²² representa morfolinila, oxazolila, isoxazolila ou piperazinila em que o referido Het²² é opcionalmente substituido por C~ 1-4~ alquila; Het²ü e Het^ 24^ representam, cada um independentemente, um heterociclo selecionado de pirrolidinila, piperazinila ou piperidinila em que os referidos Het²ü ou Het^ 24^ são opcionalmente substituidos por Het²²-carbonila; Het^ 27^ e Het^ 28^ representam, cada um independentemente, um heterociclo selecionado de morfolinila, piperazinila, piperidinila ou pirrolidinila.
BRPI0518424A 2004-12-08 2005-12-08 derivados de 2,4 (4,6) pirimidina, composição farmacêutica que os compreende, intermediários e uso dos mesmos BRPI0518424B8 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US63429104P 2004-12-08 2004-12-08
EP04106384.3 2004-12-08
EP04106384 2004-12-08
US60/634,291 2004-12-08
PCT/EP2005/056606 WO2006061415A1 (en) 2004-12-08 2005-12-08 2,4 (4,6) pyrimidine derivatives

Publications (3)

Publication Number Publication Date
BRPI0518424A2 true BRPI0518424A2 (pt) 2008-11-25
BRPI0518424B1 BRPI0518424B1 (pt) 2020-10-13
BRPI0518424B8 BRPI0518424B8 (pt) 2021-05-25

Family

ID=34930016

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0518424A BRPI0518424B8 (pt) 2004-12-08 2005-12-08 derivados de 2,4 (4,6) pirimidina, composição farmacêutica que os compreende, intermediários e uso dos mesmos

Country Status (22)

Country Link
US (2) US8148388B2 (pt)
EP (1) EP1824856B1 (pt)
JP (1) JP5022909B2 (pt)
KR (1) KR101428506B1 (pt)
CN (1) CN101072779B (pt)
AR (1) AR051788A1 (pt)
AU (1) AU2005313348B2 (pt)
BR (1) BRPI0518424B8 (pt)
CA (1) CA2588761C (pt)
CR (1) CR9234A (pt)
DK (1) DK1824856T3 (pt)
EA (1) EA013368B1 (pt)
ES (1) ES2442458T3 (pt)
IL (1) IL183706A0 (pt)
MX (1) MX2007006821A (pt)
MY (1) MY169441A (pt)
NO (1) NO340130B1 (pt)
NZ (1) NZ554820A (pt)
TW (1) TWI374140B (pt)
UA (1) UA90693C2 (pt)
WO (1) WO2006061415A1 (pt)
ZA (1) ZA200705040B (pt)

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Also Published As

Publication number Publication date
CA2588761A1 (en) 2006-06-15
ZA200705040B (en) 2008-09-25
EA013368B1 (ru) 2010-04-30
BRPI0518424B1 (pt) 2020-10-13
AR051788A1 (es) 2007-02-07
CR9234A (es) 2008-09-09
UA90693C2 (en) 2010-05-25
CN101072779A (zh) 2007-11-14
EA200701245A1 (ru) 2007-12-28
KR101428506B1 (ko) 2014-08-12
US20120065395A1 (en) 2012-03-15
CA2588761C (en) 2015-04-21
NO340130B1 (no) 2017-03-13
ES2442458T3 (es) 2014-02-11
IL183706A0 (en) 2007-09-20
HK1112455A1 (en) 2008-09-05
TWI374140B (en) 2012-10-11
AU2005313348A1 (en) 2006-06-15
MX2007006821A (es) 2007-07-24
CN101072779B (zh) 2010-12-22
KR20070085438A (ko) 2007-08-27
NO20073492L (no) 2007-07-09
JP5022909B2 (ja) 2012-09-12
BRPI0518424B8 (pt) 2021-05-25
WO2006061415A1 (en) 2006-06-15
NZ554820A (en) 2010-10-29
MY169441A (en) 2019-04-11
EP1824856A1 (en) 2007-08-29
US8394955B2 (en) 2013-03-12
JP2008523033A (ja) 2008-07-03
DK1824856T3 (da) 2014-01-27
TW200635931A (en) 2006-10-16
EP1824856B1 (en) 2013-10-23
US8148388B2 (en) 2012-04-03
AU2005313348B2 (en) 2011-10-06
US20100160310A1 (en) 2010-06-24

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