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61. 发明专利

AT319729T 未知
公开(公告)号：AT319729T
公开(公告)日：2006-03-15
申请号：AT03809747
申请日：2003-10-28
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , MEREU ANDREA , MORIGGI ERMANNO , ORNAGHI FERNANDO , MORAZZONI GABRIELE , PELLACINI FRANCO
IPC分类号： A61P29/00 , C07H17/00 , A61K31/70
摘要： Macrolides with anti-inflammatory activity are described. Particularly described are 9a-azalides and their anti-inflammatory activity without cladinose in position 3, the pharmaceutically acceptable salts thereof and the pharmaceutical composition that contain them as active principle.

62. 发明专利

BR0313162A 未知
公开(公告)号：BR0313162A
公开(公告)日：2005-07-05
申请号：BR0313162
申请日：2003-07-29
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , MORIGGI ERMANNO , MEREU ANDREA , ORNAGHI FERNANDO , MORAZZONI GABRIELE , LONGONI ROBERTO , RIVA CARLO , PACCHETTI LUCIANO , PELLACINI FRANCO
IPC分类号： A61K31/351 , A61K31/381 , A61K31/427 , A61K31/7048 , A61P11/00 , A61P29/00 , C07D407/12 , C07D417/14 , C07H17/08
摘要： Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.

63. 发明专利

ITMI20031451A1 DERIVATI DIIDRO-FTALAZINICI INIBITORI DELLA FOSFODIESTERASI 4 未知
公开(公告)号：ITMI20031451A1
公开(公告)日：2005-01-17
申请号：ITMI20031451
申请日：2003-07-16
申请人： ZAMBON SPA
发明人： ALLIEVI LEOPOLDO , HAACK THOMAS , MORAZZONI GABRIELE , MORIGGI ERMANNO , MORIGGI JEAN DOMINIQUE , NAPOLETANO MAURO , PELLACINI FRANCO , PIPPO LARA
IPC分类号： A61K31/502 , A61P11/06 , C07C20060101 , C07C311/49 , C07D237/30 , C07D237/34 , C07D401/06 , C07D401/14 , C07D407/14 , C07D413/14

64. 发明专利

CA2511182A1 PHTHALAZINE DERIVATIVES AS PHOSPHODIESTERASE 4 INHIBITORS 未知
公开(公告)号：CA2511182A1
公开(公告)日：2004-07-08
申请号：CA2511182
申请日：2003-12-22
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , RIVA CARLO , PELLACINI FRANCO , MORAZZONI GABRIELE , MORIGGI JEAN-DOMINIQUE , PAUSELLI MARCO , ALLIEVI LEOPOLDO , HAACK THOMAS
IPC分类号： A61P29/00 , C07D401/06 , C07D401/14 , C07D417/14 , A61K31/502 , C07D409/14 , C07D413/14
摘要： Compounds of formula I wherein R and R1 are as defined in the description.Th e compounds of formula I are PDE 4 inhibitors.

65. 发明专利

DK1042300T3 未知
公开(公告)号：DK1042300T3
公开(公告)日：2004-06-28
申请号：DK98966900
申请日：1998-12-17
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , NORCINI GABRIELE , BOTTA DANIELA , GRANCINI GIANCARLO , MORAZZONI GABRIELE , SANTANGELO FRANCESCO , SIRO HERRERO JORGE G , GARCIA NAVIO JOSE LUIS , ALVAREZ-BUILLA JULIO G
IPC分类号： A61K31/502 , A61P11/00 , A61P11/06 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D237/30 , C07D237/34 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14
摘要： A process for preparing a compound of formula I: wherein G is methylene, ethylene, CONH, amino or a bond; R is H, phenyl or a (C1-4)alkyl group optionally substituted by phenyl; Cy is phenyl or a 5- or 6-membered heterocycle of the group consisting of pyrrole, imidazole, pyrazole, pyrrolidine, pyrroline, imidazoline, imidazolidine, pyrazolidine, pyrazoline, pyridine, pyrazine, pyrimidine, pyridazine, piperazine, piperidine, and triazine, the Cy residue being optionally substituted by one or more substituent(s) selected from the group consisting of keto, nitro, carboxy, fluorine, chlorine, bromine, or iodine; R1 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; and R2 is aryl, aryl-(C1-10)-alkyl, (C4-7)cycloalkyl or (C4-7)heterocycle wherein the heteroatom is an oxygen atom.

66. 发明专利

AU2003269861A1 MACROLIDE COMPOUNDS ENDOWED WITH ANTIINFLAMMATORY ACTIVITY 未知
公开(公告)号：AU2003269861A1
公开(公告)日：2004-02-23
申请号：AU2003269861
申请日：2003-07-29
申请人： ZAMBON SPA
发明人： ORNAGHI FERNANDO , MORAZZONI GABRIELE , LONGONI ROBERTO , RIVA CARLO , PACCHETTI LUCIANO , PELLACINI FRANCO , NAPOLETANO MAURO , MORIGGI ERMANNO , MEREU ANDREA
IPC分类号： A61K31/351 , A61K31/381 , A61K31/427 , A61K31/7048 , A61P11/00 , A61P29/00 , C07D407/12 , C07D417/14 , C07H17/08
摘要： Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.

67. 发明专利

ITMI20021726A1 MACROLIDI AD ATTIVITA' ANTIINFIAMMATORIA. 未知
公开(公告)号：ITMI20021726A1
公开(公告)日：2004-02-02
申请号：ITMI20021726
申请日：2002-08-01
申请人： ZAMBON SPA
发明人： LONGONI ROBERTO , MORAZZONI GABRIELE , MORIGGI ERMANNO , NAPOLETANO MAURO , ORNAGHI FERNANDO , PACCHETTI LUCIANO , PELLACINI FRANCO , RIVA CARLO
IPC分类号： A61K31/00 , A61K31/351 , A61K31/381 , A61K31/427 , A61K31/7048 , A61P11/00 , A61P29/00 , C07D407/12 , C07D417/14 , C07H17/08

68. 发明专利

AU766129B2 Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors 未知
公开(公告)号：AU766129B2
公开(公告)日：2003-10-09
申请号：AU6332499
申请日：1999-10-01
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , NORCINI GABRIELE , PELLACINI FRANCO , MORAZZONI GABRIELE
IPC分类号： A61K31/5025 , A61P11/00 , A61P11/06 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D487/04
摘要： Tricyclic phthalazine compounds of formula (I)wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally substituted by a (C1-4)alkyl group in turn optionally substituted; Z is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; Cy is phenyl or heterocycle optionally substituted by one or more substituents, or a COR4 group wherein R4 is hydroxy, alkoxy, amino optionally substituted by one or two (C1-6)alkyl groups or by hydroxy; R is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R1 is hydrogen; a (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatoms or heterogroups; a (C1-4)alkoxy group or a (C4-7)cycloalkoxy group optionally containing an oxygen atom and optionally substituted by a polar substituent in the cyclic moiety, aryloxy aryl-(C1-10)-alkoxy; the N-O derivatives and the pharmaceutically acceptable salts thereof are described. The compounds of formula (I) are PDE 4 inhibitors.

69. 发明专利

BR9911175A 未知
公开(公告)号：BR9911175A
公开(公告)日：2001-03-20
申请号：BR9911175
申请日：1999-07-13
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , PELLACINI FRANCO , LEALI GIAN MARCO , NORCINI GABRIELE , GRANCINI GIANCARLO , MORAZZONI GABRIELE
IPC分类号： A61K31/502 , A61K31/5377 , A61P11/00 , A61P29/00 , A61P37/08 , C07D237/30 , C07D237/32 , C07D237/34 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of formula wherein ----- is a single or double bond; Z is NH, methylene, a (C2-C6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (C5-C7)cycloalkyl residue; A is phenyl or heterocycle optionally substituted by one or more substituent(s) selected among oxo, nitro, carboxy groups and halogen atoms, or a COR4 group wherein R4 is hydroxy, (C1-C6)-alkoxy, amino optionally substituted by one or two (C1-C6)alkyl group(s) or by hydroxy; R is a (C1-C6)alkyl or polyfluoro(C1-C6)alkyl group; R1 is absent when ----- is a double bond or, when ----- is a single bond, is (a) hydrogen; (b) (C1-C6)alkyl optionally substituted by aryl, by heterocycle or by a COR5 group wherein R5 is hydroxy, (C1-C4)alkoxy or hydroxamino; (c)-COR6 wherein R6 is hydrogen, aryl, aryl-(C1-C6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, or (C1-C4)alkyl optionally substituted by heterocycle; (d) (C1-C4)-alkylsulfonyl; R2 represents two hydrogen atoms or a group =O when ----- is a single bond, or, when ----- is a double bond, R2 is hydrogen, cyano, (C1-C4)alkoxycarbonyl, amido, optionally substituted aryl or heterocycle, (C1-C8)alkyl, (C2-C8)alkenyl or (C2-C8)alkynyl optionally branched and/or substituted by aryl or heterocycle; aryloxy, heterocyclyloxy, aryl-(C1-C4)alkoxy, heterocyclyl-(C1-C4)alkoxy, amino substituted by one or two (C1-C4)-alkyl group(s), arylamino, heterocyclylamino, aryl-(C1-C4)alkylamino, heterocyclyl-(C1-C4)-alkylamino; R3 is hydrogen, or a (C1-C8)alkyl, (C2-C8)alkenyl or (C2-C8)alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); the N->O derivatives of the compounds of formula I and the pharmaceutically acceptable salts thereof are PDE 4 inhibitors.

70. 发明专利

AP2000001993A0 Phthalazine derivatives phosphodiesterase 4 inhibitors. 未知
公开(公告)号：AP2000001993A0
公开(公告)日：2000-12-31
申请号：AP2000001993
申请日：1999-07-13
申请人： ZAMBON SPA
发明人： NAPOLETANO MAURO , NORCINI GABRIELE , GRANCINI GIANCARLO , PELLACINI FRANCO , LEALI GIAN MARCO , MORAZZONI GABRIELE
IPC分类号： A61K31/502 , A61K31/5377 , A61P11/00 , A61P29/00 , A61P37/08 , C07D237/30 , C07D237/32 , C07D237/34 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of formula (i), wherein is a single or double bond; z is nh, methylene, a (c2-c6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (c5-c7)cycloalkyl residue; a is phenyl or heterocycle optionally substituted by one or more substituent(s)selected among oxo, intro, carboxy groups and halogen atoms, or a cor4 group wherein r4 is hydroxy, (c1-c6)-alkoxy, amino optionally substituted by one or two (c1-c6)alkyl group(s)or by hydroxy; r is a (c1-c6)alkyl or polyfluoro(c1-c6)alkyl group; r1 is absent when is a double bond or, when is a single bond, is (a)hydrogen; (b)(c1-c6)alkyl optionally substituted by aryl, by heterocycle or by a cor5 group wherein r5 is hydroxy, (c1-c4)alkoxy or hydroxamino; (c)-cor6 wherein r6 is hydrogen, aryl, aryl-(c1c6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (c1-c4)alkoxy, carboxy, (c1-c4)alkoxycarbonyl, formula (i), or (c1-c4)alkyl optionally substituted by heterocycle; (d)(c1-c4)-alkylsulfonyl; r2 represents two hydrogen atoms or a group =0 when is a single bond or when is a double bond, r2 is hydrogen, cyano, (c1-c4)alkoxycarbonyl, amido, optionally substituted aryl or heterocycle, (c1-c8)alkyl, (c2-c8)alkenyl or (c2-c8)alkynyl optionally branched and/or substituted by aryl or heterocycle; aryloxy, heterocyclyloxy, aryl-(c1-c4)alkoxy, heterocyclyl-(c1-c4)alkoxy, amino substituted by one or two (c1-c4)-alkyl group(s), arylamino, heterocyclylamino, aryl(c1-c4)alkylamino, heterocyclyl-(c1-c4)-alkylamino; r3 is hydrogen, or a (c1-c8)alkyl, (c2-c8)alkenyl or (c2-c8)alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s)or heterogroup(s); the n o derivatives of the compounew of formula (i)and the pharmaceutically acceptable salts thereof are pde 4 inhibitors.

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