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

derivados de 2,4 (4,6) pirimidina

Info

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.)
Filing date
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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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/18—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (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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CN101360751B (zh) 2005-11-16 2011-09-14 S*Bio私人有限公司 氧连接的嘧啶衍生物
CA2654583C (en) 2006-07-13 2015-11-24 Janssen Pharmaceutica N.V. Mtki quinazoline derivatives
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US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
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JP7335362B2 (ja) 2019-06-12 2023-08-29 ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ 過酸化ジアシルを生成するためのプロセス
JP7281563B2 (ja) 2019-06-12 2023-05-25 ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ ペルオキシエステルを生成するためのプロセス
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Also Published As

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

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