专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

51. 发明申请

US20070149586A1 NEW CRYSTALLINE AND STABLE FORM OF ANDOLAST 有权
标题翻译：新的结晶和稳定的形式
公开(公告)号：US20070149586A1
公开(公告)日：2007-06-28
申请号：US11678277
申请日：2007-02-23
申请人： Antonio Giordani , Antonino Santoro , Paolo Senin , Matteo Ghirri , Francesco Makovec , PaoLa Gilotta , Walter Peris , Lucio Claudio Rovati
发明人： Antonio Giordani , Antonino Santoro , Paolo Senin , Matteo Ghirri , Francesco Makovec , PaoLa Gilotta , Walter Peris , Lucio Claudio Rovati
IPC分类号： A61K31/41 , C07D403/02
CPC分类号： C07D257/04
摘要： Described is a new crystalline Form A of Andolast disodium salt, triclinic, displaying a thermal event at 98-112° C. and melting with decomposition at about 400° C. (DSC). Andolast disodium Form A is a not hygroscopic solid, surprisingly stable to several humidity conditions in a temperature range acceptable for ordinary storage conditions. In addition its stability allows both chemical manufacturing and pharmaceutical manufacturing process consistency and reproducibility under conditions more viable and less expensive when compared to those used for highly hygroscopic solids.
摘要翻译：描述了一种新型的Andolast二钠盐晶体A，三斜晶系，在98-112℃显示热事件，并在约400℃下分解熔融（DSC）。 A型固体二钠是一种不吸湿的固体，对于普通储存条件可接受的温度范围，在几种湿度条件下令人惊奇地稳定。此外，与用于高吸湿性固体的那些相比，稳定性允许化学制造和药物制造过程在条件更加可行和更便宜的条件下的一致性和再现性。

52. 发明授权

US07202277B2 Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 有权
标题翻译：具有抗炎和免疫抑制活性的苯甲脒衍生物
公开(公告)号：US07202277B2
公开(公告)日：2007-04-10
申请号：US10467624
申请日：2002-02-06
申请人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
发明人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
IPC分类号： A61K31/17
CPC分类号： C07D213/40 , C07C257/14 , C07C279/18 , C07C279/36 , C07C335/20 , C07C2601/14 , C07C2603/74 , C07D209/14 , C07D209/40 , C07D277/48
摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH—” group.
摘要翻译：可以由通式（I）表示的化合物如下所示：

53. 发明申请

US20060111304A1 Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof 有权
标题翻译：具有抗收缩功能活性的抗蒽醌衍生物（抗cck-1），其制备方法及其药物用途
公开(公告)号：US20060111304A1
公开(公告)日：2006-05-25
申请号：US10523075
申请日：2003-07-23
申请人： Francesco Makovec , Antonio Varnavas , Lucia Lassiani , Lucio Rovati
发明人： Francesco Makovec , Antonio Varnavas , Lucia Lassiani , Lucio Rovati
IPC分类号： A61K38/04 , A61K31/405 , A61K31/381 , A61K31/343 , C07D333/66 , C07D307/87 , C07D209/18
CPC分类号： C07D333/68 , C07D209/42 , C07D307/84
摘要： Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F, Cl, CF3, OCH3, OC2H5, CN; R2 is chosen from H or CH3; R3 is chosen from H, CH3, F, Cl, CF3, OCH3; R4 is chosen from the groups: H, —S—(CH2)m-R5, —SO2—(CH2)m-R5 (n different from 0), a branched alkyl group, a cyclo alkyl, a cyclo alkenyl, the group 1 or 2 adamantile, a phenyl group optionally substituted; R5 is chosen from the groups: H, linear or branched alkyl, cyclo alkyl, the group 1 or 2 adamantile, a suitably substituted phenyl group.
摘要翻译：具有通式（I）的抗CCK活性的蒽醌化合物，其中n是0和7之间的整数; R 1独立地选自基团（II），其中X 1独立地选自S，O，NR 2和X H 2是选自以下的基团：H，C 1 -C 4烷基，F，Cl，CF 3，，OCH 3，OC 2 H 5，CN; R 2选自H或CH 3; R 3选自H，CH 3，F，Cl，CF 3，OCH 3， R 4选自以下基团：H，-S-（CH 2）2，mR 5，-SO 2，（CH 2）m R 5（n不同于0），支链烷基，环烷基，环烯基，1或2族金刚烷基，任选取代的苯基; R 5选自以下基团：H，直链或支链烷基，环烷基，第1或2族金刚烷基，适当取代的苯基。

54. 发明授权

US06605722B2 Tyrosine derivatives with anti-leukotrienen activity 失效
标题翻译：具有抗白三烯活性的酪氨酸衍生物
公开(公告)号：US06605722B2
公开(公告)日：2003-08-12
申请号：US10203424
申请日：2002-08-08
申请人： Francesco Makovec , Walter Peris , Lucio Claudio Rovati
发明人： Francesco Makovec , Walter Peris , Lucio Claudio Rovati
IPC分类号： C07D21538
CPC分类号： C07D401/12 , C07D215/14 , C07D215/18
摘要： Compounds which can be represented by general formula (I) indicated below and in which: R1 and R2 are selected, independently, from hydrogen, an alkyl group having from 1 to 4 carbon atoms, a halogen group such as a fluoro, chloro or bromo group, the methoxy group, the cyano group, or the trifluoromethyl group, and R3 is selected, independently, from a phenyl or a 2 (or 3 or 4)-pyridyl group, unsubstituted or mono- or di-substituted with an alkyl or alkoxy group having from 1 to 4 carbon atoms, with a halogen group such as a fluoro or chloro group, with the trifluoromethyl group, with the cyano group, with the nitro group, with the amino group, or with the phenyl group, a 1 (or 2)-naphthyl group, a 2 (or 3)-indolyl group as such or N-alkylated with an alkyl group having from 1 to 3 carbon atoms, a 2 (or 3, 4, 5, 6, 7 or 8)-quinolinyl or a 1 (or 3, 4, 5, 6, 7 or 8)-isoquinolinyl group, unsubstituted or mono- or di-substituted with a group selected, independently, from the methyl, ethyl, propyl, isopropyl, methoxy, fluoro, chloro, trifluoromethyl, cyano, amino, or nitro groups, a 2 (or 5 or 6)-quinoxalyl group, a (or 4, 5, 6, 7 or 8) cinnolyl group, or a 2 (or 4, 5, 6 or 7)-benzimidazolyl group, and in which the configuration of the chiral centre marked with an asterisk (*) in the general formula (I) may be, independently, L, D or DL (racemic).
摘要翻译：可以由下述通式（I）表示的化合物，其中：R 1和R 2独立地选自氢，具有1至4个碳原子的烷基，卤素基团如氟，氯或溴基团，甲氧基，氰基或三氟甲基，R 3独立地选自苯基或2（或3或4） - 吡啶基，未取代或被烷基或烷氧基单取代或二取代具有1至4个碳原子的基团，具有卤素基团如氟或氯基团，具有三氟甲基，氰基，硝基与氨基或苯基具有1（或2） - 萘基，2（或3） - 吲哚基，或具有1至3个碳原子的烷基进行N-烷基化，2（或3，4，5，6，7或8） - 喹啉基或1个（或3个，4个，5个，6个，7个或8个）异喹啉基，未取代或单 - 或二 - 取代基，独立地选自甲基，乙基， 2-（或5或6） - 喹喔啉基，（或4,5,6,7或8）噌啉基，或 2（或4,5,6或7） - 苯并咪唑基，其中通式（I）中带有星号（*）的手性中心的构型可独立地为L，D或DL（外消旋）。

55. 发明授权

US5985885A Quinazoline-4-amino-2-(piperidine-1-yl-4-substituted) derivatives having antihypertensive activity, a method for their preparation and their pharmaceutical use 有权
标题翻译：具有抗高血压活性的喹唑啉-4-氨基-2-（哌啶-1-基-4-取代）衍生物，其制备方法及其药物用途
公开(公告)号：US5985885A
公开(公告)日：1999-11-16
申请号：US155993
申请日：1998-10-09
申请人： Francesco Makovec , Walter Peris , Lucio Claudio Rovati , Luigi Angelo Rovati
发明人： Francesco Makovec , Walter Peris , Lucio Claudio Rovati , Luigi Angelo Rovati
IPC分类号： C07D401/04 , A61K31/00 , A61K31/505 , A61K31/517 , A61K31/529 , A61P9/00 , A61P9/12 , A61P13/00 , A61P43/00 , C07D239/95 , C07D401/14 , C07D405/14
CPC分类号： C07D239/95
摘要： New quinazolines are described of general formula (I), in which Ar is an unsubstituted phenyl group or a phenyl group mono-substituted with a methoxy, ethoxy or methyl group; an unsubstituted pyridyl group (2-, 3- or 4-yl) or a pyridyl group mono-substituted with a methoxy or methyl group; an unsubstituted furyl group (2- or 3-yl) or a furyl group substituted with a methoxy or methyl group; a benzofuryl group (2- or 3-yl); an indolyl group (2- or 3-yl); a thiophenyl group (2- or 3-yl); a naphthyl group (1- or 2-yl) and their salts obtained from pharmaceutically acceptable inorganic or organic acids. These new quinazolines are useful in the treatment of hypertension, congestive heart failure, prostate hypertrophy, various urinary tract disorders and pathological symptoms caused by hyperactivity or disfunctioning of the noradrenergic neural system. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 03370 Sec。 371日期：1998年10月9日 102（e）1998年10月9日PCT PCT 1996年7月31日PCT公布。出版物WO97 / 37979 日期：1997年10月16日新的喹唑啉描述为通式（I），其中Ar是未取代的苯基或被甲氧基，乙氧基或甲基单取代的苯基; 未取代的吡啶基（2-，3-或4-基）或被甲氧基或甲基单取代的吡啶基; 未取代的呋喃基（2-或3-基）或被甲氧基或甲基取代的呋喃基; 苯并呋喃基（2-或3-基）; 吲哚基（2-或3-基）; 噻吩基（2-或3-基）; 萘基（1-或2-基）及其由药学上可接受的无机酸或有机酸获得的盐。这些新的喹唑啉可用于治疗高血压，充血性心力衰竭，前列腺肥大，各种尿路疾病以及由去甲肾上腺素能神经系统的多动症或功能障碍引起的病理学症状。

56. 发明授权

US5976576A Pharmaceutical composition for inhalation containing CR 2039 (Andolast) 有权
标题翻译：含有CR 2039（Andolast）的吸入药物组合物
公开(公告)号：US5976576A
公开(公告)日：1999-11-02
申请号：US129794
申请日：1998-08-06
申请人： Francesco Makovec , Paolo Senin , Lucio Claudio Rovati
发明人： Francesco Makovec , Paolo Senin , Lucio Claudio Rovati
IPC分类号： A61K9/72 , A61K9/00 , A61K9/14 , A61K31/41 , A61K47/26 , A61K47/36 , A61K47/44 , A61P11/00 , A61P11/06 , A61P37/08
CPC分类号： A61K9/0075
摘要： A pharmaceutical composition comprising, as active ingredient, N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt (CR 2039, Andolast) or another pharmaceutically-acceptable salt thereof and a flavoring, and optionally including a pharmaceutically-acceptable inert carrier and/or a pharmaceutically-acceptable sweetener, the composition being suitable for administration by oral inhalation.
摘要翻译：一种药物组合物，其包含作为活性成分的N-4-（1H-四唑-5-基）苯基-4-（1H-四唑-5-基）苯甲酰胺二钠盐（CR 2039，Andolast）或其它药学上可接受的盐并且任选地包括药学上可接受的惰性载体和/或药学上可接受的甜味剂，所述组合物适于通过口服吸入给药。

57. 发明授权

US5922875A Aromatic acid diamides with antigastrin activity, a method for their preparation and their pharmaceutical use 失效
标题翻译：具有抗胃酸活性的芳香酸二酰胺，其制备方法及其药物用途
公开(公告)号：US5922875A
公开(公告)日：1999-07-13
申请号：US981804
申请日：1997-12-29
申请人： Francesco Makovec , Walter Peris , Lucio C. Rovati , Luigi A. Rovati
发明人： Francesco Makovec , Walter Peris , Lucio C. Rovati , Luigi A. Rovati
IPC分类号： C07D221/10 , A61K31/40 , A61K31/445 , A61K31/55 , A61P1/00 , A61P1/04 , A61P5/00 , A61P25/00 , A61P25/24 , A61P25/26 , A61P27/02 , B01J23/44 , C07B61/00 , C07D221/20 , C07D223/14 , C07D223/32 , C07D491/10 , C07D491/113 , C07D211/00 , C07D215/00 , C07D401/00
CPC分类号： C07D221/20 , C07D491/10
摘要： A compound represented by the general formula (I) shown below ##STR1## or a pharmaceutically acceptable salt thereof can be used as the active ingredient in a pharmaceutical preparation. The pharmaceutical preparation is desirable for its anti-ulcer activity, for therapeutic use against tumors sustained by gastrin and other bioactive polypeptides correlated therewith, for therapeutic use in treating disorders of the gastrointestinal tract, for the treatment of pathological conditions of the central nervous system linked to imbalances in the neural physiological levels of gastrin or other bioactive polypeptides correlated therewith, for use in the treatment and prevention of pathological eye conditions caused by surgical treatment of cataracts or chronic ocular inflammation, and for the prevention of diseases of other sensory organs.
摘要翻译： PCT No.PCT / EP96 / 02829 371日期1997年12月29日第 102（e）1997年12月29日PCT PCT 1996年6月28日PCT公布。出版物WO97 / 02248 日期1997年1月23日由下述通式（I）表示的化合物或其药学上可接受的盐可用作药物制剂中的活性成分。药物制剂对于其抗溃疡活性是理想的，用于治疗胃泌素和与其相关的其它生物活性多肽所持续的肿瘤的治疗用途，用于治疗胃肠道疾病的治疗用途，用于治疗中枢神经系统的病理状况与胃泌素或与其相关的其他生物活性多肽的神经生理学水平的不平衡，用于治疗和预防由手术治疗白内障或慢性眼部炎症引起的病理性眼病以及预防其它感觉器官疾病。

58. 发明授权

US4642340A Stable compounds of glucosamine sulphate 失效
标题翻译：硫酸氨基葡萄糖稳定化合物
公开(公告)号：US4642340A
公开(公告)日：1987-02-10
申请号：US373542
申请日：1982-04-30
申请人： Paolo Senin , Francesco Makovec , Luigi Rovati
发明人： Paolo Senin , Francesco Makovec , Luigi Rovati
IPC分类号： A61K31/70 , A61K31/7008 , A61P29/00 , C07H5/06
CPC分类号： C07H5/06
摘要： The compound consists of a mixed salt of glucosamine sulphate and sodium chloride corresponding to the formula: ##STR1## and is in the form of a crystalline powder with a melting point above 300.degree. C. The salt is stable at ambient temperatures and humidities and has pharmacological properties practically identical to those of glucosamine sulphate.
摘要翻译：该化合物由硫酸氨基葡萄糖和氯化钠的混合盐组成，相应于下式：，为熔点高于300℃的结晶性粉末形式。该盐在环境温度和湿度下是稳定的并具有药理学性质实际上与硫酸葡糖胺相同。

59. 发明授权

US08372866B2 2-aryl and 2-heteroaryl 4H-1-benzopyran-4-one-6-amidino derivatives, new pharmacological agents for the treatment of arthritis, cancer and related pain 失效
标题翻译： 2-芳基和2-杂芳基4H-1-苯并吡喃-4-酮-6-脒基衍生物，用于治疗关节炎，癌症和相关疼痛的新药物
公开(公告)号：US08372866B2
公开(公告)日：2013-02-12
申请号：US12919141
申请日：2008-03-06
申请人： Antonio Giordani , Sabrina Pucci , Roberto Artusi , Gianfranco Caselli , Marco Lanza , Laura Mennuni , Francesco Makovec , Lucio Claudio Rovati , Stefania Mazza
发明人： Antonio Giordani , Ilario Verpilio , Sabrina Pucci , Roberto Artusi , Gianfranco Caselli , Marco Lanza , Laura Mennuni , Francesco Makovec , Lucio Claudio Rovati
IPC分类号： A61K31/4433 , C07D405/04
CPC分类号： C07D311/30 , C07D401/04 , C07D405/10 , C07D407/04
摘要： 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
摘要翻译：可用作治疗关节炎，癌症和相关疼痛的药物的2-芳基和2-杂芳基4h-1-苯并吡喃-4-酮-6-脒基衍生物式（I）。

60. 发明申请

US20110118289A1 6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS 有权
标题翻译： 6-1H-咪唑 - 喹唑啉和喹啉衍生物，新的MAO抑制剂和咪唑啉受体配体
公开(公告)号：US20110118289A1
公开(公告)日：2011-05-19
申请号：US12999862
申请日：2008-06-20
申请人： Antonio Giordani , Marco Lanza , Gianfranco Caselli , Stefano Mandelli , Simona Zanzola , Francesco Makovec , Lucio Claudio Rovati
发明人： Antonio Giordani , Marco Lanza , Gianfranco Caselli , Stefano Mandelli , Simona Zanzola , Francesco Makovec , Lucio Claudio Rovati
IPC分类号： A61K31/517 , C07D401/10 , A61K31/4709 , C07D405/14 , C07D403/10 , A61P25/36
CPC分类号： A61K31/517 , A61K31/4178 , A61K31/485 , C07D401/04 , C07D403/04 , C07D405/14 , A61K2300/00
摘要： The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3).Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related disorders, Parkinson disease, drug abuse, and morphine tolerance and dependence.
摘要翻译：本发明涉及6-（1H-咪唑-1-基）-2-芳基和2-杂芳基喹唑啉和喹啉衍生物，式（I）化合物，其药学上可接受的盐和溶剂化物以及相应的药物组合物，其作用作为单胺氧化酶（MAO）抑制剂和咪唑啉受体配体：其中：X独立地选自-CH基或氮原子（-N），W独立地选自芳基，杂芳基或苯并稠合的杂芳基，例如作为1,3-苯并间二氧杂环戊烯，苯并呋喃，2,3-二氢苯并呋喃，苯并噻吩，2,3-二氢苯并噻吩，吲哚，2,3-二氢吲哚，苯并咪唑，苯并恶唑，苯并噻唑，2H-3,4-二氢苯并吡喃，[1,4] 苯并二恶英，2,3-二氢 - [1,4] - 苯并二恶英（1,4-苯并二恶烷）。 R 1独立地选自氢（-H），C 1 -C 4烷基，羟甲基（-CH 2 OH），氨基甲基（-CH 2 NH 2），烷基氨基甲基[CH 2 NH（R 2）]或二烷基氨基甲基[ -CF 3）。式（I）化合物引发适于临床治疗抑郁症和相关疾病，帕金森病，药物滥用和吗啡耐受性和依赖性的药理学特征。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式