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1. 发明专利

CA2352275C IL-5 INHIBITING 6-AZAURACIL DERIVATIVES 未知
公开(公告)号：CA2352275C
公开(公告)日：2008-11-18
申请号：CA2352275
申请日：1999-11-22
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , LACRAMPE JEAN FERNAND ARMAND , PETIT DAVY PETRUS FRANCISCUS M
IPC分类号： C07D253/06 , C07D253/075 , A61K31/53 , A61P1/04 , A61P11/02 , A61P11/06 , A61P17/04 , A61P17/06 , A61P27/14 , A61P29/00 , C07D413/10 , C07D417/10
摘要： The present invention is concerned with the compounds of formula (I), the N- oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 5; -A-B- is -(CH2)r-, -(CH2)t-O-, -(CH2)t-S(-O)u- or -(CH2)t-NR3-; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

2. 发明专利

AT365723T 未知
公开(公告)号：AT365723T
公开(公告)日：2007-07-15
申请号：AT99965509
申请日：1999-12-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , LACRAMPE JEAN FERNAND ARMAND , EMBRECHTS WERNER CONSTANT JOHA , FORTIN JEROME MICHEL CLAUDE
IPC分类号： C07D253/06 , A61K31/53 , A61K51/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR or a direct bond; or -X-R is CN; R is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R is aryl, Het , optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R is H or C1-4alkyl; R and R are -C(=O)-Z-R , C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(=O)O, aryl, cyano, nitro, Het , R , NR R or C1-4alkyl substituted with -C(=O)-Z-R , Het , R or NR R ; Z is O, S, NH, -CH2O or -CH2-S-; R is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het , phenyl; or R is an oxygen containing radical; aryl is optionally substituted phenyl; Het , Het , Het and Het are optionally substituted heterocycles; Het is a monocyclic heterocycle; provided however that R is other than NH

3. 发明专利

NZ512748A IL-5 inhibiting 6-azauracil derivatives 未知
公开(公告)号：NZ512748A
公开(公告)日：2004-05-28
申请号：NZ51274899
申请日：1999-12-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , LACRAMPE JEAN FERNAND ARMAND , EMBRECHTS WERNER CONSTANTJOHAN , FORTIN JEROME MICHEL CLAUDE
IPC分类号： A61K31/53 , A61K51/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/06 , C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： A compound of formula (I) where: - p represents an integer being 0, 1 or 2; - q represents an integer being 1; - X represents S; - R1 represents hydrogen; - R2 represents pyridinyl substituted with -C(=O)-Z-R14, or C1-6alkyl substituted with one or two substituents selected from NR7R8 and Het3; - Each R4 independently represents halo; - Each R5 independently represents halo; - Each R7 and each R8 are independently selected from hydrogen, C1-4alkyl, -C(=O)-Z-R14, and Het3; - Each Z independently represents O or S; - Each R14 independently represents hydrogen and C1-20alkyl, or R14 represents a radical of formulae (a) or (p); - Het3 represents a monocyclic heterocycle selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl and tetrahydropyranyl. A process for the production of a compound of formula (I) is also disclosed. A compound of formula (I) may be also used to treat eosiniphil-dependent inflammatory diseases. Also, a process for imaging an organ, using a radio-labelled compound of formula (I).

4. 发明专利

AU763460B2 4,5-dihydro-isoxazole derivatives and their pharmaceutical use 未知
公开(公告)号：AU763460B2
公开(公告)日：2003-07-24
申请号：AU1039300
申请日：1999-10-07
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , GIL JOSE IGNACIO ANDRES , DEROOSE FREDERIK DIRK , PETIT DAVY PETRUS FRANCISCUS M , MATESANZ-BALLESTEROS MARIA ENC , ESCOBAR ROSA MARIA ALVAREZ
IPC分类号： C07D487/04 , A61K31/42 , A61K31/4427 , A61K31/4725 , A61K31/4738 , A61K31/496 , A61K31/506 , A61P3/12 , A61P9/10 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P37/06 , C07D261/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D498/04
摘要： The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A 1 =A 2 -A 3 =A 4 - is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, -N-, -O-, -CR 5 R 6 -, amide, ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R 1 represents hydrogen, halo, hydroxy, C (2-6) alkenyl, C (2-6) alkynyl, C (3-6) cycloalkyl, C (3-6) cycloalkenyl, cyano, guanidine, nitro, NR 17 R 18 , an optionally substituted C (1-6) alkyl or C (1-6) alkyloxy; R 2 and R 3 each independently represent hydrogen, halo, C (1-6) alkyloxy or an optionally substituted C (1-6) alkyl; R 5 and R 6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C (1-6) alkyl, C (2-6) alkenyl, C (2-6) alkynyl, C (3-6) cycloalkyl, C (3-6) cycloalkenyl, C (1-6) alkyloxy, cyano, (C-O)R 25 , (C-O)OR 16 , (SO 2 )R 16 , aminocarbonyloxy, aminoC (1-6) alkyl, NR 17 R 18 , N 3 , Ar or Het; or R 5 and R 6 together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C (6-14) aryl; Het represents an optionally substituted C (1-14) heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

5. 发明专利

BR0013014A 未知
公开(公告)号：BR0013014A
公开(公告)日：2002-04-16
申请号：BR0013014
申请日：2000-07-31
申请人： JANSSEN PHARMACEUTICA NV
发明人： LACRAMPE JEAN FERNAND ARMAND , FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , FORTIN JEROME MICHEL CLAUDE , 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 useful for treating eosinophil-dependent 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 marking a receptor or imaging an organ using the said derivatives.

6. 发明专利

NO20020565D0 未知
公开(公告)号：NO20020565D0
公开(公告)日：2002-02-05
申请号：NO20020565
申请日：2002-02-05
申请人： JANSSEN PHARMACEUTICA NV
发明人： LACRAMPE JEAN FERNAND ARMAND , FORTIN JEROME MICHEL CLAUDE , FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , COESEMANS ERWIN
IPC分类号： A61K31/53 , C07D413/10 , 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 , C07D
摘要： The present invention relates to IL-5 inhibiting 6-azauracil derivatives useful for treating eosinophil-dependent 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 marking a receptor or imaging an organ using the said derivatives.

7. 发明专利

BR9916366A 未知
公开(公告)号：BR9916366A
公开(公告)日：2001-09-18
申请号：BR9916366
申请日：1999-12-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , LACRAMPE JEAN FERNAND ARMAND , EMBRECHTS WERNER CONSTANT JOHA , FORTIN JEROME MICHEL CLAUDE
IPC分类号： A61K31/53 , A61K51/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/06 , C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR or a direct bond; or -X-R is CN; R is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R is aryl, Het , optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R is H or C1-4alkyl; R and R are -C(=O)-Z-R , C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(=O)O, aryl, cyano, nitro, Het , R , NR R or C1-4alkyl substituted with -C(=O)-Z-R , Het , R or NR R ; Z is O, S, NH, -CH2O or -CH2-S-; R is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het , phenyl; or R is an oxygen containing radical; aryl is optionally substituted phenyl; Het , Het , Het and Het are optionally substituted heterocycles; Het is a monocyclic heterocycle; provided however that R is other than NH

8. 发明专利

AU2100100A Il-5 inhibiting 6-azauracil derivatives 未知
公开(公告)号：AU2100100A
公开(公告)日：2000-07-12
申请号：AU2100100
申请日：1999-12-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK , LACRAMPE JEAN FERNAND ARMAND , EMBRECHTS WERNER CONSTANT JOHA , FORTIN JEROME MICHEL CLAUDE
IPC分类号： A61K31/53 , A61K51/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/06 , C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR or a direct bond; or -X-R is CN; R is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R is aryl, Het , optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R is H or C1-4alkyl; R and R are -C(=O)-Z-R , C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(=O)O, aryl, cyano, nitro, Het , R , NR R or C1-4alkyl substituted with -C(=O)-Z-R , Het , R or NR R ; Z is O, S, NH, -CH2O or -CH2-S-; R is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het , phenyl; or R is an oxygen containing radical; aryl is optionally substituted phenyl; Het , Het , Het and Het are optionally substituted heterocycles; Het is a monocyclic heterocycle; provided however that R is other than NH

9. 发明专利

CA2354511A1 IL-5 INHIBITING 6-AZAURACIL DERIVATIVES 未知
公开(公告)号：CA2354511A1
公开(公告)日：2000-06-29
申请号：CA2354511
申请日：1999-12-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , LACRAMPE JEAN FERNAND ARMAND , EMBRECHTS WERNER CONSTANT JOHA , FORTIN JEROME MICHEL CLAUDE , DEROOSE FREDERIK DIRK
IPC分类号： A61K31/53 , A61K51/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/06 , C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is concerned with the compounds of formula (I), a N- oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or -X-R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl , NH2C1-4alkyl, mono- or di(C1-4alkyl)NH2C1-4alkyl or mono- or di(C1- 4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3- 7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are -C(=O)-Z-R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1- 6alkylO, C1-6alkylthio, C1-6alkylC(=O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with -C(=O)-Z-R14, Het3, R6 or NR7R8; Z is O, S, NH , - CH2-O- or -CH2-S-; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC 1- 20alkyl, Het5, phenyl; or R14 is an oxygen containing radical; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het5 are optionally substituted heterocycles; Het4 is a monocyclic heterocycle; provided however that R2 is other than NH2C(=O), C1-6alkylOC(=O)C1-6alkyl; and R11 is other than COOH, C1-4alkylOC(=O), NH2C(=O),C1-4alkylNH2C(=O), OHC1-4alkylNH2C(=O), C1-4alkylC(=O)NH2C(=O), C3-7cycloalkylNH2C(=O); and R7, R8, R9, R10, R12, R1 3, R15 and R16 are other than C1-4alkylC(=O)OC1-4alkylC(=O), OHC1-4alkylC(=O); and Het3 is other than a monocyclic heterocycle susbstituted with COOH or C1 - 4alkylOC(=O); and the compounds of formula (I) contain at least one -C(=O)-Z - R14 moiety; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

10. 发明专利

AU1967700A Il-5 inhibiting 6-azauracil derivatives 未知
公开(公告)号：AU1967700A
公开(公告)日：2000-06-13
申请号：AU1967700
申请日：1999-11-22
申请人： JANSSEN PHARMACEUTICA NV
发明人： LACRAMPE JEAN FERNAND ARMAND , LIGNY YANNICK , FREYNE EDDY JEAN EDGARD , DEROOSE FREDERIK DIRK
IPC分类号： C07D253/06 , A61K31/53 , A61P11/06 , A61P27/14 , A61P29/00 , A61P37/08 , A61P43/00 , C07D253/075 , C07D403/10 , C07D405/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; -A-B- represents -(CH2)r-, -(CH2)t-O-, -(CH2)t-S(=O)u- or -(CH2)t-NR3-; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, -C(=Q)-X2-R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(=O)-NH-NH or NH-NH-C(=O), R15 may be replaced by R11; Q is O, S or NR3; X2 is O, S, NR5, C(=O)-NH-NH, NH-NH-C(=O) or a direct bond; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, -Y-C1-4alkanediyl-C(=O)-O-R14, Het3

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