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1. 发明专利

DK1824856T3 2,4 (4,6)-PYRIMIDINDERIVATER 未知
公开(公告)号：DK1824856T3
公开(公告)日：2014-01-27
申请号：DK05819148
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , EMBRECHTS WERNER C J , VAN EMELEN KRISTOF , VAN BRANDT SVEN F A , ROMBOUTS FREDERIK J R
IPC分类号： C07D487/08 , A61K31/505 , A61P35/00 , C07D209/00 , C07D221/00 , C07D239/00 , C07D241/00 , C07D259/00 , C07D273/00 , C07D487/22 , C07D498/18

2. 发明专利

AT391129T 未知
公开(公告)号：AT391129T
公开(公告)日：2008-04-15
申请号：AT04804852
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , STORCK PIERRE H , PONCELET V S , VAN EMELEN KRISTOF , BUIJNSTERS P J J A , EMBRECHTS WERNER C J , PERERA TIMOTHY P S
IPC分类号： C07D498/18 , A61K31/519 , A61P35/00 , C07D471/04 , C07D471/18 , C07D487/04

3. 发明专利

DE602004012891T2 未知
公开(公告)号：DE602004012891T2
公开(公告)日：2009-04-09
申请号：DE602004012891
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , STORCK PIERRE H , PONCELET V S , VAN EMELEN KRISTOF , BUIJNSTERS P J J A , EMBRECHTS WERNER C J , PERERA TIMOTHY P S
IPC分类号： C07D498/18 , A61K31/519 , A61P35/00 , C07D471/04 , C07D471/18 , C07D487/04
摘要： The present invention concerns the compounds of formula wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6 alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or substituted C1-4alkyloxy; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents morpholinyl-C1-4alkyl; Het2 represents morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

4. 发明专利

ES2305887T3 DERIVADOS DE PIRIDO Y PIRIMIDOPIRIMIDINAS COMO AGENTES ANTIPROLIFERATIVOS. 未知
公开(公告)号：ES2305887T3
公开(公告)日：2008-11-01
申请号：ES04804852
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , STORCK PIERRE H , PONCELET V S , VAN EMELEN KRISTOF , BUIJNSTERS P J J A
IPC分类号： C07D498/18 , A61K31/519 , A61P35/00 , C07D471/04 , C07D471/18 , C07D487/04
摘要： Un compuesto que tiene la fórmula (Ver fórmula) las formas de N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isómeras de los mismos, en el que: a 1 -a 2 =a 3 -a 4 representa un radical divalente seleccionado de N-CH=CH-CH, N-CH=N-CH o CH-CH=N-CH; Z representa O, NH o S; Y representa -alquil C3 - 9-, -alquenil C3 - 9-, -alquiloxi C1 - 5-alquil C1 - 5-, -alquil C1 - 5-NR 13 -alquil C1 - 5-, -alquil C1 - 5-NR 14 -CO-alquil C1 - 5-, -alquil C1 - 5-CO-NR 15 -alquil C1 - 5-, -alquil C1 - 6-CO-NH-, -alquil C1 - 6-NH-CO-, -CO-NH-alquil C1 - 6-, -NH-CO-alquil C1 - 6-, -CO-alquil C1 - 7-, -alquil C1 - 7-CO-, alquil C1 - 6-CO-alquilo C1 - 6; X 1 representa un enlace directo, O, -O-alquil C1 - 2-, CO, -CO-alquil C1 - 2-, NR 11 , -NR 11 -alquil C1 - 2-, NR 16 -CO-, NR 16 -CO-alquil C1 - 2-, -O-N=CH- o alquilo C1 - 2; X 2 representa un enlace directo, O, -O-alquil C1 - 2-, CO, -CO-alquil C1 - 2-, NR 12 , NR 12 -alquil C1 - 2-, NR 17 -CO-, NR 17 -CO-alquil C1 - 2-, Het 20 -alquil C1 - 2-, -O-N=CH- o alquilo C1 - 2; R 1 representa hidrógeno, ciano, halo, hidroxi, formilo, alcoxi C1 - 6-, alquil C1 - 6-, alcoxi C1 - 6- sustituido con halo, alquilo C1 - 4 sustituido con uno o, cuando sea posible, dos o más sustituyentes seleccionados de hidroxi o halo; R 2 representa hidrógeno, ciano, halo, hidroxi, hidroxicarbonil-, Het 16 -carbonil-, alquiloxi C1 - 4 -carbonil-, alquil C1 - 4-carbonil-, aminocarbonil-, mono o di(alquil C1 - 4)aminocarbonil-, Het 1 , formilo, alquil C1 - 4-, alquinil C2 - 6-, cicloalquil C3 - 6-, cicloalquiloxi C3 - 6-, alcoxi C1 - 6-, Ar 5 , Ar 1 -oxi-, dihidroxiborano, alcoxi C1 - 6- sustituido con halo, alquilo C1 - 4 sustituido con uno o, cuando sea posible, dos o más sustituyentes seleccionados de halo, hidroxi o NR 5 R 6 , alquil C1 - 4-carbonil-, en el que dicho alquilo C1 - 4 está opcionalmente sustituido con uno o, cuando sea posible, dos o más sustituyentes seleccionados de hidroxi o alquiloxi C1 - 4-; R 3 representa hidrógeno, alquilo C1 - 4, ciano o alquilo C1 - 4 sustituido con uno o más sustituyentes seleccionados de halo, alquiloxi C1 - 4-, amino-, mono o di(alquil C1 - 4)amino-, alquil C1 - 4-sulfonil- o fenilo; R 4 representa...

5. 发明专利

BG106367A INTERLEUKIN-5-INHIBITING 6-AZAURACIL DERIVATIVES 未知
公开(公告)号：BG106367A
公开(公告)日：2002-09-30
申请号：BG10636702
申请日：2002-01-30
申请人： JANSSEN PHARMACEUTICA NV
发明人： LACRAMPE JEAN FERNAND A , FREYNE EDDY JEAN E , DEROOSE FREDERIK D , FORTIN JEROME MICHEL C , COESEMANS ERWIN
IPC分类号： C07D413/10 , A61K31/53 , A61K31/5377 , A61K51/04 , A61P1/02 , A61P1/04 , A61P11/06 , A61P11/08 , A61P15/02 , A61P17/06 , A61P27/02 , A61P27/16 , A61P37/08 , A61P43/00 , C07D417/10 , C07D417/14
摘要： The present invention relates to IL-5 inhibiting 6-azauracil derivatives of formula useful for treating eosinophil-dependant inflammatory diseases, to processes and intermediates for their preparation as well as to pharmaceutical compositions comprising the said derivatives. It further relates to the use of such derivatives as a medicine, and to processes for making a receptor or imaging an organ using the said derivatives. 21 claims

6. 发明专利

ES2442458T3 Derivados de 2,4 (4,6)-pirimidina 未知
公开(公告)号：ES2442458T3
公开(公告)日：2014-02-11
申请号：ES05819148
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , EMBRECHTS WERNER C J , VAN EMELEN KRISTOF , VAN BRANDT SVEN F A , ROMBOUTS FREDERIK J R
IPC分类号： C07D487/08 , A61K31/505 , A61P35/00 , C07D209/00 , C07D221/00 , C07D239/00 , C07D241/00 , C07D259/00 , C07D273/00 , C07D487/22 , C07D498/18
摘要： Un compuesto que tiene la fórmula (I).**Fórmula** las formas N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamenteisoméricas del mismo, en la que: Z1 y Z2 representan cada uno independientemente NR22 ; Y representa -alquilo C3-9-, -alquenilo C3-9-, -alquinilo C3-9-, -alquil C3-7-CO-NH- opcionalmente sustituido con amino,mono- o di(alquil C1-4)amino, aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, o alquil C1-4-oxicarbonilamino-, -alquenil C3-7-CO-NH- opcionalmente sustituido con amino, mono- odi(alquil C1-4)amino, aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, oalquil C1-4-oxicarbonilamino-, -alquinil C3-7-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C1-4)amino,aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, o alquil C1-4-oxicarbonilamino-, -alquil C1-5-oxi-alquilo C1-5-, -alquil C1-5-NR6-alquilo C1-5-, -alquil C1-5-NR7-CO-alquilo C1-5-, -alquilC1-6-CO-NH-, -alquil C1-6-NH-CO-, -alquil C1-3-NH-CS-Het9-, -alquil C1-3-NH-CO-Het3-, -alquil C1-2-CO-Het10-CO-, -Het4-alquil C1-3-CO-NH-alquilo C1-3-, -alquil C1-7-CO-, -alquil C1-6-CO-alquilo C1-6-, -alquil C1-2-NH-CO-L1 -NH-, -NHCO-L2-NH-, -alquil C1-2-CO-NH-L3-CO-, -alquil C1-2-NH-CO-L1-NH-CO-alquilo C1-3-, -alquil C1-2-NH-CO-L1-NH-CO-, -CO-NH-L2-CO-, -alquil C1-2-CO-NH-L3-CO-NH-alquilo C1-3-, -alquil C1-2-CO-NH-L3-CO-NH-, -alquil C1-2-CO-NR10-alquil C1-3-CO-, -alquil C1-2-NR11-CH2-CO-NH-alquilo C1-3-, -NR12-CO-alquil C1-3-NH-, Het5-CO-alquilo C1-2-, -alquil C1-5-CO-NH-alquil C1-3-CO-NH-, -alquil C1-5-NR13-CO-alquil C1-3-NH-, -Het6-CO-Het7-, -Het8-NH-alquil C1-3-CO-NH-, -alquil C1-3-NH-CO-Het32-CO-, o-alquil C1-3-CO-Het33 -CO-NH-.

7. 发明专利

DE602004012891D1 未知
公开(公告)号：DE602004012891D1
公开(公告)日：2008-05-15
申请号：DE602004012891
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE , VAN EMELEN KRISTOF , BUIJNSTERS P J J A , EMBRECHTS WERNER C J , PERERA TIMOTHY P S
IPC分类号： C07D498/18 , A61K31/519 , A61P35/00 , C07D471/04 , C07D471/18 , C07D487/04
摘要： The present invention concerns the compounds of formula wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6 alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or substituted C1-4alkyloxy; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents morpholinyl-C1-4alkyl; Het2 represents morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

8. 发明专利

SK34499A3 PDE IV INHIBITING 2-CYANOIMINOIMIDAZOLE DERIVATIVES 未知
公开(公告)号：SK34499A3
公开(公告)日：2000-04-10
申请号：SK34499
申请日：1997-09-24
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , FERNANDEZ-GADEA FRANCISCO J , ANDRES-GIL JOSE I
IPC分类号： C07D233/44 , A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/00 , A61P37/08 , C07D233/48 , C07D233/88 , C07D405/12
摘要： PCT No. PCT/EP97/05322 Sec. 371 Date Mar. 19, 1999 Sec. 102(e) Date Mar. 19, 1999 PCT Filed Sep. 24, 1997 PCT Pub. No. WO98/14432 PCT Pub. Date Apr. 9, 1998The present invention concerns 2-cyanoiminoimidazole derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy; R4 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R4 is -O-R7 or -NH-R8; R5 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R6 is a hydrogen or C1-4alkyl; or R4 and R6, or R4 and R5 taken together may form a bivalent radical; -A-B- is -CR10=CR11- or -CHR10-CHR11-; L is hydrogen; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidinyl; substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.

9. 发明专利

SG118994G (1H-imidazol-1-ylmethyl) substituted benzimidazole derivatives 未知
公开(公告)号：SG118994G
公开(公告)日：1995-04-28
申请号：SG118994
申请日：1994-08-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： RAEYMAEKERS ALFONS HERMAN M , FREYNE EDDY JEAN E , SANZ GERARD CHARLES
IPC分类号： A61K31/415 , C07D235/06 , C07D235/18 , C07D235/24 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14

10. 发明专利

CY1803A Novel (1H-imidazol-1-ylmethyl) substituted benzimidazole derivatives 未知
公开(公告)号：CY1803A
公开(公告)日：1987-09-09
申请号：CY180387
申请日：1987-09-09
申请人： JANSSEN PHARMACEUTICA NV
发明人： RAEYMAEKERS ALFONS HERMAN M , FREYNE EDDY JEAN E , SANZ GERARD CHARLES
IPC分类号： A61K31/425 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P5/00 , A61P5/24 , A61P17/00 , A61P19/06 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D521/00 , C07D235/06 , C07D235/18 , C07D235/24
摘要： Novel (1H-imidazol-1-ylmethyl) substituted benzimidazole derivatives of formula wherein A is a bivalent radical having the formula the pharmaceutically acceptable salts and possible stereochemically isomeric forms thereof, which compounds possess androgen formation inhibiting properties; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.

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