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BRPI0417534A - pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents - Google Patents

pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents

Info

Publication number
BRPI0417534A
BRPI0417534A BRPI0417534-4A BRPI0417534A BRPI0417534A BR PI0417534 A BRPI0417534 A BR PI0417534A BR PI0417534 A BRPI0417534 A BR PI0417534A BR PI0417534 A BRPI0417534 A BR PI0417534A
Authority
BR
Brazil
Prior art keywords
alkyl
het
alkyloxy
morpholinyl
hydrogen
Prior art date
Application number
BRPI0417534-4A
Other languages
Portuguese (pt)
Inventor
Eddy Jean Edgard Freyne
Marc Willems
Pierre Henri Storck
Virginie Sophie Poncelet
Kristof Van Emelen
Peter Jacobus Johan Buijnsters
Werner Constant Joha Embrechts
Timothy Pietro Suren Perera
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Priority claimed from PCT/EP2004/053501 external-priority patent/WO2005058913A1/en
Publication of BRPI0417534A publication Critical patent/BRPI0417534A/en
Publication of BRPI0417534B1 publication Critical patent/BRPI0417534B1/en
Publication of BRPI0417534B8 publication Critical patent/BRPI0417534B8/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"DERIVADOS DE PIRIDO- E PIRIMIDOPIRIMIDINA COMO AGENTES ANTIPROLIFERATIVOS". A presente invenção refere-se aos compostos da fórmula às formas de N-óxido, aos sais de adição e às formas estereoquimicamente isoméricas farmaceuticamente aceitáveis dos mesmos, em que a¬ 1¬-a¬ 2¬=a¬ 3¬-a¬ 4¬ representa um radical divalente selecionado de N-CH=CH-CH, N-CH=N-CH ou CH-CH=N-CH; Z representa NH; Y representa -C~ 3-9~ alquil-, -C~ 1-5~ alquil-NR¬ 13¬ -C~ 1-5~ alquil-, -C~ 1-6~ alquil-NH-CO- ou -CO-NH -C~ 1-6~ alquil-; X¬ 1¬ representa -0- ou -NR¬ 11¬-; X¬ 2¬ representa -C~ 1-2 alquil-, -0-C~ 1-2~ alquila, -O- ou -0-CH~ 2~-; R¬ 1¬ representa hidrogênio ou halo; R¬ 2¬ representa hidrogênio, ciano, halo, hidroxicarbonil-, C~ 1-4~ alquiloxicarbonil-, Het¬ 16¬ -carbonil- ou Ar¬ 5¬; R¬ 3¬ representa hidrogênio; R¬ 4¬ representa hidróxi, C~ 1-4~ alquilóxi-, Ar¬ 4¬-C~ 1-4~ alquilóxi ou R¬ 4¬ representa C~ 1-4~ alquilóxi substituído por um ou quando possível dois ou mais substituintes selecionados de C~ 1-4~ alquilóxi- ou Het¬ 2¬-; R¬ 11¬ representa hidrogênio; R¬ 12¬ representa hidrogênio, C~ 1-4~ alquil- ou C~ 1-4~ alquil-óxi-carbonil-; R¬ 13¬ representa Het¬ 14¬-C~ 1-4~ alquila, em particular morfolinil-C~ 1-4~ alquila; Het¬ 2¬ representa um heterociclo selecionado de morfolinila ou piperidinila opcionalmente substituída por C~ 1-4~ alquiL-, preferencialmente metila; Het¬ 14¬ representa morfolinila; Het¬ 16¬ representa um heterocicLo selecionado de morfolinila ou pirrolidinila; Ar¬ 4¬ representa fenila; Ar¬ 5¬ representa fenila opcionalmente substituída por ciano."PYRIDUM AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS" The present invention relates to compounds of the formula to N-oxide forms, addition salts and to pharmaceutically acceptable stereochemically isomeric forms thereof, wherein a¬ 1¬-a¬ 2¬ = a¬ 3¬-a¬ 4¬ represents a divalent radical selected from N-CH = CH-CH, N-CH = N-CH or CH-CH = N-CH; Z represents NH; Y represents -C- 3-9-alkyl-, -C- 1-5-alkyl-NR¬ 13¬ -C-1-5-alkyl-, -C- 1-6-alkyl-NH-CO- or - CO-NH-C 1-6 alkyl-; X¬ 1¬ represents -0- or -NR¬ 11¬-; X 2 represents C 1-2 alkyl-, -O-C 1-2 alkyl, -O- or -O-CH 2 2-; R¬ 1¬ represents hydrogen or halo; R¬ 2¬ represents hydrogen, cyano, halo, hydroxycarbonyl-, C 1-4 -alkyloxycarbonyl-, Het¬ 16¬ -carbonyl- or Ar¬ 5¬; R¬ 3¬ represents hydrogen; R¬4¬ represents hydroxy, C1-4-alkyloxy-, Ar¬4¬-C1-4-alkyloxy or R¬4¬ represents C1-4-alkyloxy substituted by one or when possible two or more substituents selected from C 1-4-alkyloxy or Het¬ 2¬-; R¬ 11¬ represents hydrogen; R 12 represents hydrogen, C 1-4 alkyl or C 1-4 alkyloxycarbonyl; R 13 13 represents Het 14 14 -C 1-4 alkyl, in particular morpholinyl C 1-4 alkyl; Het¬ 2¬ represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C 1-4 alkyl, preferably methyl; Het¬ 14¬ represents morpholinyl; Het 16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar¬ 4¬ represents phenyl; Ar¬ 5¬ represents phenyl optionally substituted by cyano.

BRPI0417534A 2003-12-18 2004-12-15 pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents, intermediates, their preparation process and pharmaceutical composition comprising them and use BRPI0417534B8 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EPPCT/EP03/51062 2003-12-18
EP0351062 2003-12-18
EPPCT/EP03/51058 2003-12-18
EP0351058 2003-12-18
PCT/EP2004/053501 WO2005058913A1 (en) 2003-12-18 2004-12-15 Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents

Publications (3)

Publication Number Publication Date
BRPI0417534A true BRPI0417534A (en) 2007-03-27
BRPI0417534B1 BRPI0417534B1 (en) 2018-12-18
BRPI0417534B8 BRPI0417534B8 (en) 2021-05-25

Family

ID=34957036

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0417534A BRPI0417534B8 (en) 2003-12-18 2004-12-15 pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents, intermediates, their preparation process and pharmaceutical composition comprising them and use

Country Status (1)

Country Link
BR (1) BRPI0417534B8 (en)

Also Published As

Publication number Publication date
BRPI0417534B8 (en) 2021-05-25
BRPI0417534B1 (en) 2018-12-18

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 18/12/2018, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 15/12/2004 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 21A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2859 DE 21-10-2025 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.