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1. 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。

2. 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.

3. 发明授权

US06340684B1 Phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
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：US06340684B1
公开(公告)日：2002-01-22
申请号：US09764983
申请日：2001-01-22
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
IPC分类号： A61K31502
CPC分类号： C07D401/06 , C07D237/30 , C07D237/32 , C07D237/34 , C07D405/06
摘要： The present invention provides a compound selected from the group including: N-3-acetyl-1-(3,5-dichloropyridin-4-ylmethyl)-5-cyclopentyloxy-6-methoxy-4H-phthalazine; 6,7-dimethoxy-1-pyridin-4-ylmethyl-4-thiazol-2-yl-phthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)ethanone; 2-methanesulphonyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 2-formyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)-1-imidazol-1-ylmethanone; 1-(3,5-dichloro-pyridin-4-ylmethyl)-3-methansulphonyl-6-difluoromethoxy-5-(tetrahydro-furan-2-yloxy)-4H-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition, which contains a therapeutically effective amount of the above compound in admixture with a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了选自以下的化合物：N-3-乙酰基-1-（3,5-二氯吡啶-4-基甲基）-5-环戊基氧基-6-甲氧基-4H-酞嗪; 6,7-二甲氧基-1-吡啶-4-基甲基-4-噻唑-2-基 - 酞嗪; 1-（6,7-二甲氧基-4-吡啶-4-基甲基-1H-酞嗪-2-基）乙酮; 2-甲磺酰基-6,7-二甲氧基-4-吡啶-4-基甲基-1,2-二氢酞嗪; 2-甲酰基-6,7-二甲氧基-4-吡啶-4-基甲基-1,2-二氢酞嗪; 1-（6,7-二甲氧基-4-吡啶-4-基甲基-1H-酞嗪-2-基）-1-咪唑-1-基甲酮; 1-（3,5-二氯 - 吡啶-4-基甲基）-3-甲磺酰基-6-二氟甲氧基-5-（四氢 - 呋喃-2-基氧基）-4H-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，其含有治疗有效量的上述化合物与药学上可接受的载体的混合物。

4. 发明授权

US06498160B2 Phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
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：US06498160B2
公开(公告)日：2002-12-24
申请号：US09987266
申请日：2001-11-14
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
IPC分类号： A61K31502
CPC分类号： C07D401/06 , C07D237/30 , C07D237/32 , C07D237/34 , C07D405/06
摘要： Phthalazine compounds having formula I wherein , A, B, R, R1, R2 and R3 are as defined herein, useful as phosphodiesterase 4 inhibitors.
摘要翻译： “CUSTOM-CHARACTER FILE =”US06498160-20021224-P00900.TIF“中的具有式I的酞嗪化合物”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/> B，R，R 1，R 2和R 3如本文所定义，可用作磷酸二酯酶4抑制剂。

5. 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。

6. 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。

7. 发明授权

US06589951B1 Phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
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：US06589951B1
公开(公告)日：2003-07-08
申请号：US09581506
申请日：2000-08-10
申请人： Mauro Napoletano , Gabriele Norcini , Daniela Botta , Giancarlo Grancini , Gabriele Morazzoni , Francesco Santangelo , Jorge G. Siro Herrero , José Luis Garcia Navaio , Julio G. Alvarez-Builla
发明人： Mauro Napoletano , Gabriele Norcini , Daniela Botta , Giancarlo Grancini , Gabriele Morazzoni , Francesco Santangelo , Jorge G. Siro Herrero , José Luis Garcia Navaio , Julio G. Alvarez-Builla
IPC分类号： A61K31502
CPC分类号： C07D401/06 , C07D237/30 , C07D237/34 , C07D401/12 , C07D405/12
摘要： Compounds of formula (I) wherein B is alkylene, amino, CONH or a bond; Cy is optionally substituted phenyl or heteroaryl; R is H, phenyl or (C1-4)alkyl optionally substituted; R1 is (C1-6)alkyl or polyfluoro(C1-6)-alkyl; R2 is (C4-7)cycloalkyl optionally containing an oxygen atom and optionally substituted; and the N→O derivatives and pharmaceutically acceptable salt thereof are PDE 4 and TNF&agr; inhibitors.
摘要翻译：其中B为亚烷基，氨基，CONH或键的式（I）化合物; Cy是任选取代的苯基或杂芳基; R为H，苯基或任选取代的（C 1-4）烷基; R1是（C1-6）烷基或多氟（C1-6） - 烷基; R 2是任选地含有氧原子且任选被取代的（C 4-7）环烷基; 并且所述N-> O衍生物及其药学上可接受的盐为PDE4和TNFα抑制剂。

8. 发明授权

US06525055B1 Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
标题翻译：三环酞嗪衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：US06525055B1
公开(公告)日：2003-02-25
申请号：US09830679
申请日：2001-04-30
申请人： Mauro Napoletano , Gabriele Norcini , Franco Pellacini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Franco Pellacini , Gabriele Morazzoni
IPC分类号： A61K315025
CPC分类号： 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.
摘要翻译：式（I）的三环酞嗪化合物，其中A是含有1至4个氮原子的5-7元杂环，任选地部分或完全不饱和，并且任选地被（C 1-4）烷基取代， Z是NH，亚甲基，任选支链和/或不饱和的和/或被C5-7环烷基残基中断的C2-6亚烷基链; Cy是任选被一个或多个取代基取代的苯基或杂环，或其中R4是羟基，烷氧基，任选被一个或两个（C 1-6）烷基或羟基取代的氨基的COR 4基团; R为（C 1-6）烷基或多氟（C 1-6）烷基; R1是氢; 任选被羟基，氧代，芳基或杂环取代的（C 1-8） - 烷基，（C 2-8） - 烯基或（C 2-8） - 炔基，并且任选被一个或多个杂原子或杂团中断; 芳氧基芳基 - （C 1-10） - 烷氧基，（C 1-4）烷氧基或任选含有氧原子且任选被环状部分中的极性取代基取代的（C 4-7）环烷氧基; 描述了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。

9. 发明授权

US6166051A Thiol derivatives with metallopeptidase (ACE/NEP) inhibitory activity 失效
标题翻译：具有金属肽酶（ACE / NEP）抑制活性的硫醇衍生物
公开(公告)号：US6166051A
公开(公告)日：2000-12-26
申请号：US91415
申请日：1998-06-23
申请人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
发明人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
IPC分类号： C07D213/55 , C07D277/30 , C07D333/24 , A61K31/44 , A61K31/426 , C07D213/04
CPC分类号： C07D333/24 , C07D213/55 , C07D277/30
摘要： Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 05496 Sec。 371日期1998年6月23日第 102（e）1998年6月23日PCT 1996年12月9日PCT PCT。公开号WO97 / 24341 日期1997年7月10日描述了其中R，R 1，R 2，R 3具有本说明书中报道的含义，其制备方法和含有它们作为活性成分的药物组合物的式（I）化合物。式（I）化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

10. 发明授权

US5760241A Thiol derivatives with metallopeptidase inhibitory activity 失效
标题翻译：具有金属肽酶抑制活性的硫醇衍生物
公开(公告)号：US5760241A
公开(公告)日：1998-06-02
申请号：US774298
申请日：1996-12-24
申请人： Francesco Santangelo , Mario Fantucci , Claudio Semeraro , Franco Pellacini , Stefano Romagnano , Gabriele Norcini
发明人： Francesco Santangelo , Mario Fantucci , Claudio Semeraro , Franco Pellacini , Stefano Romagnano , Gabriele Norcini
IPC分类号： A61P9/00 , C07C323/60 , C07C327/32 , C07D213/55 , C07D213/56 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/24 , C07D277/26 , C07D277/30 , C07D307/54 , C07D333/24 , C07D417/12
CPC分类号： C07C323/60 , C07C327/32 , C07D213/55 , C07D213/56 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/30 , C07D307/54 , C07D333/24 , C07D417/12
摘要： Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：其中R，R 1，R 2，R 3，R 4，m和n具有本说明书中报道的含义，其制备方法和含有它们作为活性成分的药物组合物的式（I）化合物。式I化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

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