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1. 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。

2. 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。

3. 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。

4. 发明授权

US5760285A Phosphonyldipeptides useful in the treatment of cardiovascular diseases 失效
标题翻译：可用于治疗心血管疾病的膦酰二肽
公开(公告)号：US5760285A
公开(公告)日：1998-06-02
申请号：US702701
申请日：1996-09-13
申请人： Gabriele Norcini , Gabriele Morazzoni , Francesco Santangelo
发明人： Gabriele Norcini , Gabriele Morazzoni , Francesco Santangelo
IPC分类号： A61K38/00 , C07K5/06 , C07F9/22 , A01N57/36
CPC分类号： C07K5/06191 , A61K38/00
摘要： Compounds of formula (II) ##STR1## wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl or thioalkyl groups having from 1 to 6 carbon atoms in the alkyl moiety, carboxylic groups, nitro groups, amino, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 allyl; R.sub.2 is a straight or branched C.sub.1 -C.sub.6 alkyl or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a naphthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted as above indicated for the R substituent; R.sub.3 is a straight or branched C.sub.1 -C.sub.6 alkyl, optionally containing one or more fluorine atoms, or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety; the carbon atoms marked with an asterisk are asymmetric carbon atoms; and their pharmaceutically acceptable salts, are described. The compounds of formula (II) are useful in the treatment of cardiovascular diseases.
摘要翻译： PCT No.PCT / EP95 / 01322 Sec。 371日期1996年9月13日 102（e）1996年9月13日PCT PCT 1995年4月11日PCT公布。 WO95 / 28417 PCT出版物日期：1995年10月26日化学式（II）其中R是任选被一个或多个选自卤素原子，羟基，烷氧基，烷基或硫代烷基中的一个或多个相同或不同的取代基取代的联苯基在烷基部分具有1至6个碳原子，在烷基部分具有1至6个碳原子的羧基，硝基，氨基，一或二烷基氨基; R1是氢原子或直链或支链C1-C4烯丙基; R2是直链或支链的C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基，其中芳基是苯基，萘基或具有一个或两个选自氮，氧和硫，任选地被如上述R取代基所取代; R3是任选地含有一个或多个氟原子的直链或支链C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基; 标有星号的碳原子是不对称碳原子; 及其药学上可接受的盐。式（II）的化合物可用于治疗心血管疾病。

5. 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.

6. 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。

7. 发明申请

US20080249034A1 Use of Macrolides for Treating Intestinal Inflammation 审中-公开
标题翻译：使用大环内酯类药物治疗肠道炎症
公开(公告)号：US20080249034A1
公开(公告)日：2008-10-09
申请号：US11908550
申请日：2005-03-14
申请人： Mario Del Tacca , Corrado Blandizzi , Gabriele Morazzoni
发明人： Mario Del Tacca , Corrado Blandizzi , Gabriele Morazzoni
IPC分类号： A61K31/7048 , A61P1/00
CPC分类号： A61K31/7048
摘要： The present invention relates to a compound of formula (IA) as defined in the specification or a pharmaceutically acceptable sat thereof, in the preparation of a medicament for both the treatment of inflammatory bowel diseases and the prevention of colon cancer.
摘要翻译：本发明涉及在本说明书中定义的式（IA）化合物或其药学上可接受的盐，在制备用于治疗炎症性肠病和预防结肠癌的药物中的用途。

8. 发明授权

US06297257B1 Benzazine derivatives phosphodiesterase 4 inhibitors 失效
标题翻译：苯并嗪衍生物磷酸二酯酶4抑制剂
公开(公告)号：US06297257B1
公开(公告)日：2001-10-02
申请号：US09581505
申请日：2000-07-13
申请人： Mauro Napoletano , Gabriele Norcini , Daniela Botta , Giancarlo Grancini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Daniela Botta , Giancarlo Grancini , Gabriele Morazzoni
IPC分类号： A01N4342
CPC分类号： C07D401/06
摘要： Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.
摘要翻译：式（I）的化合物，其中A是任选被某些取代基取代且必须被-B-Cy基团取代的正交稠合的杂环，其中变量如说明书中所定义，并且其N-烷基化衍生物及其药学上可接受的盐是磷酸二酯酶 -4抑制剂。

9. 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。

10. 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。

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