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81. 发明申请

WO2005111010A1 AN IMPROVED PROCESS FOR THE PREPARATION OF 5-CYANOPHTHALIDE 审中-公开
标题翻译：制备5-氰基十八烷酸的改进方法
公开(公告)号：WO2005111010A1
公开(公告)日：2005-11-24
申请号：PCT/IN2004/000132
申请日：2004-05-13
申请人： SUVEN LIFE SCIENCES LTD, , ARAVA VEERA REDDY, Arava , CHINNAPILLAI RAJENDIRAN, Rajendiran , INDRASENA REDDY, Inderasena , VENAKT JASTI, Venkat
发明人： ARAVA VEERA REDDY, Arava , CHINNAPILLAI RAJENDIRAN, Rajendiran , INDRASENA REDDY, Inderasena , VENAKT JASTI, Venkat
IPC分类号： C07D307/87
CPC分类号： C07D307/87 , C07D307/88
摘要： The invention disclosed an improved process for the preparation of 5-cyanophthalide which comprises reacting 5-carboxyphthalide with ammonium carbonate in the presence of ethyl polyphospate with or without a solvent and isolating the 5-cyanophthalide formed by conventional methods .
摘要翻译：本发明公开了一种用于制备5-氰基苯酞的改进方法，其包括在具有或不具有溶剂的多磷酸乙酯存在下使5-羧基邻苯二甲酸酯与碳酸铵反应，并分离通过常规方法形成的5-氰基苯酞。

82. 发明申请

WO2004094399A1 AN IMPROVED PROCESS FOR THE PREPARATION OF CITALOPRAM HYDROBROMIDE 审中-公开
标题翻译：用于制备氢氯化铬的改进方法
公开(公告)号：WO2004094399A1
公开(公告)日：2004-11-04
申请号：PCT/IN2003/000165
申请日：2003-04-21
申请人： NATCO PHARMA LTD , VENKAIAH CHOWDARY, Nannapaneni , KHADGAPATHI, Podile , PULLA REDDY, Muddasani , LINGARAO, Donthineni
发明人： VENKAIAH CHOWDARY, Nannapaneni , KHADGAPATHI, Podile , PULLA REDDY, Muddasani , LINGARAO, Donthineni
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The present invention discloses an improved process for the preparation of citalopram hydrobromide of formula (I) from citalopram base of formula (III) without isolating and crystallizing the latter. The citalopram base of formula (III) is prepared according to earlier known method from the isobenzofuran of formula (II). Accordingly, the organic layer containing citalopram base is directly treated with aqueous hydrobromic acid to get the citalopram hydrobromide.
摘要翻译：本发明公开了一种从式（III）的西酞普兰碱制备式（I）的西酞普兰氢溴酸盐而不使其分离和结晶的改进方法。式（III）的西酞普兰碱基根据先前已知的方法由式（II）的异苯并呋喃制备。因此，含有西酞普兰碱的有机层用氢溴酸水溶液直接处理得到西酞普兰氢溴酸盐。

83. 发明申请

WO03064617A9 PESTALOTIOPSIS MICROSPORIA ISOLATES AND COMPOUNDS DERIVED THEREFROM 审中-公开
标题翻译： PESTALOTIOPSIS MICROSPORIA分离物和化合物衍生自
公开(公告)号：WO03064617A9
公开(公告)日：2004-06-24
申请号：PCT/US0302944
申请日：2003-01-30
申请人： UNIV MONTANA STATE , FORD EUGENE , STROBEL GARY , HARPER JAMES KIMBALL
发明人： FORD EUGENE , STROBEL GARY , HARPER JAMES KIMBALL
IPC分类号： A61K31/343 , C07D307/87 , C07D307/88 , C12P17/04 , A61K9/00 , A61K39/02
CPC分类号： C07D307/87 , A61K31/343 , C07D307/88 , C12P17/04 , C12R1/645
摘要： The present invention relates to the novel isolated 12-30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12-30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12-30, and to uses thereof.
摘要翻译：本发明涉及能够生产新型抗氧化剂和抗真菌剂的新型分离的Pestalotiopsis microspora的12-30菌株。本发明还涉及新型分离的3,5,7三取代异苯并呋喃酮及其衍生物，从培养物微孢子菌属12-30中分离出新的异苯并呋喃酮的方法，以及该化合物作为抗氧化剂和抗真菌剂的新用途。本发明还涉及一种新的1,5,7三取代1,3-二氢异苯并呋喃及其衍生物，其从Pestalotiopsis microspora 12-30的培养物中分离出该新化合物的方法及其应用。

84. 发明申请

WO2004026855A1 METHOD FOR MANUFACTURE OF DIHYDROISOBENZOFURAN DERIVATIVES 审中-公开
标题翻译：二氢苯并呋喃衍生物的制备方法
公开(公告)号：WO2004026855A1
公开(公告)日：2004-04-01
申请号：PCT/DK2003/000599
申请日：2003-09-17
申请人： H. LUNDBECK A/S , SOMMER, Michael, Bech , NIELSEN, Ole
发明人： SOMMER, Michael, Bech , NIELSEN, Ole
IPC分类号： C07D307/87
CPC分类号： C07D491/10
摘要： The present invention relates to a method for the manufacture of dihydroisobenzofurans of formula I; comprising generation a dianion of formula II, reaction of the dianion with a carbonyl compound of formula III and acidification of the reaction mixture to generate a diol of formula IV; followed by ring closure of the diol of formula IV to obtain the dihydroisobenzofuran of formula I.
摘要翻译：本发明涉及制备式I的二氢异苯并呋喃的方法; 包括产生式II的二价阴离子，二价阴离子与式III的羰基化合物反应，并酸化反应混合物以产生式IV的二醇; 然后闭合式IV的二醇，得到式I的二氢异苯并呋喃。

85. 发明申请

WO2004016602A1 PROCESS FOR THE PREPARATION OF HIGH PURITY CITALOPRAM AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译：制备高纯度CITALOPRAM及其药学上可接受的盐的方法
公开(公告)号：WO2004016602A1
公开(公告)日：2004-02-26
申请号：PCT/IN2002/000167
申请日：2002-08-14
申请人： NATCO PHARMA LIMITED
发明人： MUDDASANI, Pulla, Reddy , NANNAPANENI, Wenkaiah, Chowoary
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： This invention discloses an improved process for the preparation of high purity citalopram base and its hydrobromide salt of formulae (I) and (Ia): which comprises: i. Isolation of crude citalopram base after water work up of the reaction into a non polar aromatic or dialkyl ether solvent. ii. Extraction of the citalopram base into aqueous organic acid. iii. Neutralization of acid layer with organic base to a controlled pH (7.0-8.0) iv. Extraction of the pure base into a non-polar aromatic or dialkyl ether solvent and crytallization form the same solvent after concentrating to certain volume under reduced pressure. v. Preparation of high purity citalopram hydrobromide in a non-polar aromatic or dialkyl ether solvent using 40-50 % HBr in acetic acid as HBr source and crystallizing out form the same solvent. Alternatively preparation of HBr salt in aqueous medium using aqueous HBr and crystallizing out from the same medium at 0 10 °C. vi. Recrystallization of high purity citalopram hydrobromide salt of pharmaceutically acceptable grade form a mixture of alcoholic solvent.
摘要翻译：本发明公开了制备高纯度西酞普兰碱及其式（I）和（Ia）的氢溴酸盐的改进方法：其包括：在将反应水加工成非极性芳族或二烷基醚溶剂后，分离粗制西酞普兰碱。 II。将西酞普兰碱提取成含水有机酸。 III。将酸性有机碱中和至受控pH（7.0-8.0）iv。将纯碱萃取到非极性芳族或二烷基醚溶剂中，并在减压下浓缩至一定体积后形成相同的溶剂。 v。在非极性芳族或二烷基醚溶剂中使用40-50％HBr在乙酸中作为HBr源制备高纯度西酞普兰氢溴酸盐，并从相同的溶剂中结晶出来。或者使用HBr水溶液在水性介质中制备HBr盐，并在0°C从相同的介质中析出。六。可药用级别的高纯度西酞普兰氢溴酸盐的重结晶形成醇溶剂的混合物。

86. 发明申请

WO03064617A2 PESTALOTIOPSIS MICROSPORIA ISOLATES AND COMPOUNDS DERIVED THEREFROM 审中-公开
标题翻译： PESTALOTIOPSIS MICROSPORIA分离物和化合物衍生自
公开(公告)号：WO03064617A2
公开(公告)日：2003-08-07
申请号：PCT/US0302944
申请日：2003-01-30
申请人： UNIV MONTANA STATE , FORD EUGENE , STROBEL GARY , HARPER JAMES KIMBALL
发明人： FORD EUGENE , STROBEL GARY , HARPER JAMES KIMBALL
IPC分类号： A61K31/343 , C07D307/87 , C07D307/88 , C12P17/04 , C12N
CPC分类号： C07D307/87 , A61K31/343 , C07D307/88 , C12P17/04 , C12R1/645
摘要： The present invention relates to the novel isolated 12-30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12-30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12-30, and to uses thereof.
摘要翻译：本发明涉及能够生产新型抗氧化剂和抗真菌剂的新型分离的Pestalotiopsis microspora的12-30菌株。本发明还涉及新型分离的3,5,7三取代异苯并呋喃酮及其衍生物，从培养物微孢子菌属12-30中分离出新的异苯并呋喃酮的方法，以及该化合物作为抗氧化剂和抗真菌剂的新用途。本发明还涉及一种新的1,5,7三取代1,3-二氢异苯并呋喃及其衍生物，其从Pestalotiopsis microspora 12-30的培养物中分离出该新化合物的方法及其应用。

87. 发明申请

WO02024619A1 AMINE COMPOUNDS 审中-公开
标题翻译：胺化合物
公开(公告)号：WO02024619A1
公开(公告)日：2002-03-28
申请号：PCT/GB2001/004264
申请日：2001-09-25
IPC分类号： C07C217/16 , C07C217/20 , C07C317/28 , C07D307/79 , C07D333/54 , C07C43/20 , A61K31/34 , A61K31/38 , C07C43/23 , C07D307/87
CPC分类号： C07D307/79 , C07C217/16 , C07C217/20 , C07C317/28 , C07C2601/02 , C07D333/54
摘要： Ar is a bicyclic or tricyclic aromatic group including at least one benzene ring, the oxygen group of the side chain being attached to the benzene ring of Ar; A is a straight or branched alkylene group of 6 to 16 carbon atoms which may be interrupted by -O-, -S-, -SO-, -SO2-, -NR -, -CH(OH)- or -CO-, wherein R is hydrogen or a straight or branched alkyl group of 1 to 4 carbon atoms; and R and R are each independently hydrogen or a straight or branched alkyl or alkenyl group of 1 to 4 carbon atoms, optionally substituted by phenyl or a cycloalkyl group of 3 to 7 carbon atoms; are useful for the treatment of fungal infection.
摘要翻译： Ar是包含至少一个苯环的双环或三环芳基，侧链的氧基连接到Ar的苯环上; A可以被-O - ， - S - ， - SO - ， - SO 2 - ， - NR 4 - ， - CH（OH） - 或 - CO-，其中R 4是氢或1至4个碳原子的直链或支链烷基; R 1和R 2各自独立地为氢或1-4个碳原子的直链或支链烷基或链烯基，任选被苯基或3-7个碳原子的环烷基取代; 可用于治疗真菌感染。

88. 发明申请

WO0180619A3 PHARMACEUTICAL COMPOSITION CONTAINING CITALOPRAM 审中-公开
标题翻译：包含CITALOPRAM的药物组合物
公开(公告)号：WO0180619A3
公开(公告)日：2002-02-21
申请号：PCT/DK0100520
申请日：2001-07-30
申请人： LUNDBECK & CO AS H , LILJEGREN KEN , HOLM PER , NIELSEN OLE , WAGNER SVEN
发明人： LILJEGREN KEN , HOLM PER , NIELSEN OLE , WAGNER SVEN
IPC分类号： A61K20060101 , A61K9/20 , A61K9/48 , A61K31/343 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/36 , A61K47/38 , A61P25/14 , A61P25/24 , C07D307/87 , A61K9/14
CPC分类号： C07D307/87 , A61K9/2054 , A61K9/4866 , A61K31/343
摘要： A solid unit dosage form comprising citalopram, which is prepared by direct compression of a mixture of citalopram base or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients, or by filling of said mixture in a hard gelatine capsule. Large crystals of a pharmaceutical acceptable salt of citalopram and method for the manufacture of said large crystals.
摘要翻译：包含西酞普兰的固体单位剂型，其通过直接压制西酞普兰碱或其药学上可接受的盐和药学上可接受的赋形剂的混合物或通过将所述混合物填充在硬明胶胶囊中来制备。西酞普兰药物可接受盐的大晶体和用于制造所述大晶体的方法。

89. 发明申请

WO01080619A2 PHARMACEUTICAL COMPOSITION CONTAINING CITALOPRAM 审中-公开
标题翻译：包含CITALOPRAM的药物组合物
公开(公告)号：WO01080619A2
公开(公告)日：2001-11-01
申请号：PCT/DK2001/000520
申请日：2001-07-30
IPC分类号： A61K20060101 , A61K9/20 , A61K9/48 , A61K31/343 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/36 , A61K47/38 , A61P25/14 , A61P25/24 , C07D307/87
CPC分类号： C07D307/87 , A61K9/2054 , A61K9/4866 , A61K31/343
摘要： A solid unit dosage form comprising citalopram, which is prepared by direct compression of a mixture of citalopram base or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients, or by filling of said mixture in a hard gelatine capsule. Large crystals of a pharmaceutical acceptable salt of citalopram and method for the manufacture of said large crystals.
摘要翻译：包含西酞普兰的固体单位剂型，其通过直接压制西酞普兰碱或其药学上可接受的盐和药学上可接受的赋形剂的混合物或通过将所述混合物填充在硬明胶胶囊中来制备。西酞普兰药物可接受盐的大晶体和用于制造所述大晶体的方法。

90. 发明申请

WO01068632A1 METHOD FOR THE PREPARATION OF 5-CYANO-1-(4-FLUOROPHENYL)-1,3-DIHYDROISOBENZOFURANS 审中-公开
标题翻译： 5-氰基-1-（4-氟代戊基）-1,3-二氢苯并呋喃的制备方法
公开(公告)号：WO01068632A1
公开(公告)日：2001-09-20
申请号：PCT/DK2001/000186
申请日：2001-03-16
IPC分类号： A61K31/343 , A61P25/24 , C07D307/87
CPC分类号： C07D307/87
摘要： A method for the preparation of 5-cyano-1-(4-fluorophenyl)-1,3-dihydroisobenzo-furan comprising conversion of a 5-substituted 1-(4-fluorophenyl)-1,3-dihydro-isobenzofuran derivative.
摘要翻译：制备5-氰基-1-（4-氟苯基）-1,3-二氢异苯并呋喃的方法，包括5-取代的1-（4-氟苯基）-1,3-二氢异苯并呋喃衍生物的转化。

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