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1. 发明申请

US20060166996A1 Phthalazine derivatives as phosphodiesterase 4 inhibitors 审中-公开
标题翻译：酞嗪衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：US20060166996A1
公开(公告)日：2006-07-27
申请号：US10540273
申请日：2003-12-22
申请人： Mauro Napoletano , Franco Pellacini , Gabriele Morazzoni , Jean-Dominique Moriggi , Carlo Riva , Thomas Haack , Leopoldo Allievi , Marco Pauselli
发明人： Mauro Napoletano , Franco Pellacini , Gabriele Morazzoni , Jean-Dominique Moriggi , Carlo Riva , Thomas Haack , Leopoldo Allievi , Marco Pauselli
IPC分类号： C07D237/30 , A61K31/502
CPC分类号： C07D401/06 , C07D401/14 , C07D417/14
摘要： Compounds of formula I wherein R and R1 are as defined in the description. The compounds of formula I are PDE 4 inhibitors.
摘要翻译：式I化合物，其中R和R 1如说明书中所定义。式I的化合物是PDE 4抑制剂。

2. 发明授权

US07488811B2 Macrolide compounds endowed with antiinflammatory activity 失效
标题翻译：具有抗炎活性的大环内酯类化合物
公开(公告)号：US07488811B2
公开(公告)日：2009-02-10
申请号：US10522671
申请日：2003-07-29
申请人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
发明人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
IPC分类号： A61K31/70
CPC分类号： C07H17/08
摘要： Macrolide compounds lacking cladinose in position 3 having antiinflammatory activity and substantially free of antibiotic properties, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them as active ingredient.
摘要翻译： 3位具有抗炎活性且基本上不含抗生素特性的大分子胶体化合物，其药学上可接受的盐和含有它们作为活性成分的药物组合物。

3. 发明申请

US20060058246A1 Macrolide compounds endowed with antiinflammatory activity 失效
标题翻译：具有抗炎活性的大环内酯类化合物
公开(公告)号：US20060058246A1
公开(公告)日：2006-03-16
申请号：US10522671
申请日：2003-07-29
申请人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
发明人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： 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.
摘要翻译：对具有抗炎活性的大环内酯类化合物进行了描述，更具体地说，具有抗炎活性的位置3中缺乏切蛋白的大环内酯衍生物，其药学上可接受的盐和含有它们作为活性成分的药物组合物。

4. 发明授权

US07704960B2 Macrolide compounds endowed with antiinflammatory activity 失效
标题翻译：具有抗炎活性的大环内酯类化合物
公开(公告)号：US07704960B2
公开(公告)日：2010-04-27
申请号：US12259335
申请日：2008-10-28
申请人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
发明人： Mauro Napoletano , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： 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.
摘要翻译：对具有抗炎活性的大环内酯类化合物进行了描述，更具体地说，具有抗炎活性的位置3中缺乏切蛋白的大环内酯衍生物，其药学上可接受的盐和含有它们作为活性成分的药物组合物。

5. 发明申请

US20090054357A1 MACROLIDE COMPOUNDS ENDOWED WITH ANTIINFLAMMATORY ACTIVITY 失效
标题翻译：具有抗炎活性的MACROLIDE化合物
公开(公告)号：US20090054357A1
公开(公告)日：2009-02-26
申请号：US12259335
申请日：2008-10-28
申请人： Mauro NAPOLETANO , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
发明人： Mauro NAPOLETANO , Ermanno Moriggi , Andrea Mereu , Fernando Ornaghi , Gabriele Morazzoni , Roberto Longoni , Carlo Riva , Luciano Pacchetti , Franco Pellacini
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： 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.
摘要翻译：对具有抗炎活性的大环内酯类化合物进行了描述，更具体地说，具有抗炎活性的位置3中缺乏切蛋白的大环内酯衍生物，其药学上可接受的盐和含有它们作为活性成分的药物组合物。

6. 发明授权

US06492360B1 Phthalazine derivatives phosphodiesterase 4 inhibitors 失效
公开(公告)号：US06492360B1
公开(公告)日：2002-12-10
申请号：US09976436
申请日：2001-10-15
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gian Marco Leali , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gian Marco Leali , Gabriele Morazzoni
IPC分类号： A61K31502
CPC分类号： C07D401/06 , C07D237/30 , C07D237/32 , C07D237/34 , C07D401/14 , C07D405/06 , 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 or a COR4 group wherein R4 is hydroxy, (C1-C6)-alkoxy, amino optionally substituted; 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; (c) —COR6 wherein R6 is hydrogen, aryl, aryl-(C1-C6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, formula (1), 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; aryloxy, heterocyclyloxy, aryl-(C1-C4)alkoxy, heterocyclyloxy-(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, and optionally interrupted; the N→O derivatives of the compounds of formula (I) and the pharmaceutically acceptable salts thereof are PDE 4 inhibitors.

7. 发明授权

US06358973B1 Benzazine derivatives as phosphodiesterase 4 inhibitors 失效
标题翻译：苯并嗪衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：US06358973B1
公开(公告)日：2002-03-19
申请号：US09806496
申请日：2001-04-13
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni , Lorenzo Pradella
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni , Lorenzo Pradella
IPC分类号： C07D4006
CPC分类号： C07D401/06
摘要： Compounds of formula I: wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen, cyano, (C1-4)alkoxycarbonyl, carbamoyl; optionally substituted (C4-7)-cycloalkyl, aryl or heterocycle; (C1-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl optionally branched and/or substituted by (C4-7) cycloalkyl, aryl or heterocycle; aryloxy, heterocyclyloxy, aryl(C1-4)alkoxy, heterocyclyl(C1-4)alkoxy, amino substituted by one or two (C1-4)alkyl group(s), aryl-amino, heterocyclyl-amino, aryl(C1-4)alkyl-amino, or heterocyclyl(C1-4)alkylamino; Y is methylene or ethylene; W is an optionally substituted aryl or heterocycle; R1 is hydrogen, (C4-7)cycloalkyl or a (C2-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl group optionally substituted by hydroxy, oxo, (C4-7)cycloalkyl, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); R2 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; the N→O derivatives of the compounds of formula I and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are PDE 4 inhibitors and may be used in compositions and methods involving PDE 4 inhibition.
摘要翻译：式I化合物：其中A是含有氮原子，任选饱和或不饱和并任选进一步被氧代基（= O）取代的杂环; R为：氢，氰基，（C 1-4）烷氧基羰基，氨基甲酰基; 任选取代的（C 4-7） - 环烷基，芳基或杂环; （C 1-8）烷基，（C 2-8）烯基或任选被（C 4-7）环烷基，芳基或杂环支链和/或取代的（C 2-8）炔基; 芳氧基，杂环氧基，芳基（C 1-4）烷氧基，杂环基（C 1-4）烷氧基，被一个或两个（C 1-4）烷基取代的氨基，芳基 - 氨基，杂环基 - 氨基，芳基）烷基 - 氨基或杂环基（C 1-4）烷基氨基; Y是亚甲基或亚乙基; W是任选取代的芳基或杂环; R1是氢，（C4-7）环烷基或（C2-8）烷基，（C2-8）烯基或（C2-8）炔基，任选被羟基，氧代，（C 4-7）环烷基，芳基或杂环并且任选被一个或多个杂原子或杂团中断; R2是（C1-6）烷基或多氟（C1-6）烷基; 式I化合物的N-> O衍生物及其药学上可接受的盐。式（I）化合物是PDE 4抑制剂，可用于涉及PDE4抑制的组合物和方法。

8. 发明授权

US06329370B1 Phthalazine derivatives phosphodiesterase 4 inhibitors 失效
标题翻译：酞嗪衍生物磷酸二酯酶4抑制剂
公开(公告)号：US06329370B1
公开(公告)日：2001-12-11
申请号：US09743813
申请日：2001-01-22
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gian Marco Leali , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gian Marco Leali , Gabriele Morazzoni
IPC分类号： A61K315377
CPC分类号： C07D401/06 , C07D237/30 , C07D237/32 , C07D237/34 , C07D401/14 , C07D405/06 , C07D417/04 , C07D417/14
摘要： The present invention provides a compound selected from the group including: 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-phenyl-phthalazine; 4-(3,5-dichloro-pyridin-4-ylmethyl)-7-methoxy-1H-phthalazin-2-carboxylic acid methyl ester; benzyl-{3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-ynyl}-methyl-amine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(5-morpholin-4-yl-pent-1-ynyl)-phthalazine dihydrochloride; 3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-yn-1-ol; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-morpholin-4-yl-phthalazine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-(1,2,4)triazol-1-yl-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition which includes a therapeutically effective amount of the above compound in admixture with a suitable carrier.
摘要翻译：本发明提供了选自以下的化合物：1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-苯基 - 酞嗪; 4-（3,5-二氯 - 吡啶-4-基甲基）-7-甲氧基-1H-酞嗪-2-甲酸甲酯; 苄基 - {3- {1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基 - 二氮杂萘-5-基} - 丙-2-炔基} - 甲基 - 胺; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-5-（5-吗啉-4-基 - 戊-1-炔基） - 酞嗪二盐酸盐; 3- {1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基 - 二氮杂萘-5-基} - 丙-2-炔-1-醇; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-吗啉-4-基 - 酞嗪; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-（1,2,4）三唑-1-基 - 酞嗪; 其N-> O衍生物; 及其药学上可接受的盐。本发明还提供一种药物组合物，其包含治疗有效量的上述化合物与合适的载体的混合物。

9. 发明授权

US07956042B2 Crystalline forms of macrolide compounds endowed with antiinflammatory activity 失效
标题翻译：具有抗炎活性的大环内酯化合物的结晶形式
公开(公告)号：US07956042B2
公开(公告)日：2011-06-07
申请号：US11994784
申请日：2006-07-05
申请人： Paolo Maragni , Dario Braga , Roberto Brescello , Livius Cotarca , Alessandro Di Maria , Franco Massaccesi , Elisa Melotto , Ivan Michieletto , Gabriele Morazzoni , Mauro Napoletano , Franco Pellacini , Angelo Restelli , Massimo Verzini
发明人： Paolo Maragni , Dario Braga , Roberto Brescello , Livius Cotarca , Alessandro Di Maria , Franco Massaccesi , Elisa Melotto , Ivan Michieletto , Gabriele Morazzoni , Mauro Napoletano , Franco Pellacini , Angelo Restelli , Massimo Verzini
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.
摘要翻译：本发明涉及具有抗炎活性的大环内酯类化合物，更具体地涉及具有抗炎活性的大环内酯衍生物的新稳定结晶形式，制备这种形式的方法，含有它们作为活性成分的药物组合物以及使用所述结晶形式用于治疗炎性疾病。

10. 发明申请

US20090018089A1 CRYSTALLINE FORMS OF MACROLIDE COMPOUNDS ENDOWED WITH ANTIINFLAMMATORY ACTIVITY 失效
标题翻译：具有抗炎活性的大环化合物的结晶形式
公开(公告)号：US20090018089A1
公开(公告)日：2009-01-15
申请号：US11994784
申请日：2006-07-05
申请人： Paolo Maragni , Dario Braga , Roberto Brescello , Livius Cotarca , Alessandro Di Maria , Franco Massaccesi , Elisa Melotto , Ivan Michieletto , Gabriele Morazzoni , Mauro Napoletano , Franco Pellacini , Angelo Restelli , Massimo Verzini
发明人： Paolo Maragni , Dario Braga , Roberto Brescello , Livius Cotarca , Alessandro Di Maria , Franco Massaccesi , Elisa Melotto , Ivan Michieletto , Gabriele Morazzoni , Mauro Napoletano , Franco Pellacini , Angelo Restelli , Massimo Verzini
IPC分类号： A61K31/7048 , C07D313/00 , A61P29/00
CPC分类号： C07H17/08
摘要： the present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.
摘要翻译：本发明涉及具有抗炎活性的大环内酯化合物，更具体地说涉及具有抗炎活性的大环内酯衍生物的新稳定结晶形式，制备这种形式的方法，含有它们作为活性成分的药物组合物以及使用所述结晶形式用于治疗炎性疾病。

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