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1. 发明申请

WO2005065046A2 AN EFFICIENT INDUSTRIAL PROCESS FOR 3-HYDROXY-3-(3’-SULFAMYL-4’-CHLOROPHENYL)PHTALIMIDINE 审中-公开
标题翻译： 3-羟基-3-（3'-磺酰基-4'-氯苯基）苯并咪唑的有效工业方法
公开(公告)号：WO2005065046A2
公开(公告)日：2005-07-21
申请号：PCT/IN2004/000370
申请日：2004-11-30
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra
发明人： KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra
CPC分类号： C07D209/48
摘要： The oximination/cyclization of 2-(4-chlorobenzoyl)benzoic acid with hydroxylamine hydrochloride in presence of molar quantities of inorganic base in water or in alcoholic solvents to form 4-(4’-chlorophenyl)-5,6-bent-oxazine-l-one Formula (8) in high yield and purity; reduction of latter with zinc metal and acetic acid to the corresponding phtalimidine of Formula (9); followed by conversion into 2-(3’-chlorosulphonyl-4’-chlorophenyl)phtalimidine Formula (10) by reaction with chlorosulphonic acid and thionyl chloride in the absence of solvent. Amidation of compound of formula (10) was carried out with ammonia gas/solution in non.-aqueous solvent like ketones and polar aprotic solvents like dimethylformamide, to yield compound of formula (11). Oxidation of Formula (11) with hydrogen peroxide in presence of alkali results in high yield of chlorihalidone.
摘要翻译：在水或醇溶剂中存在无机碱的摩尔量存在下，将2-（4-氯苯甲酰基）苯甲酸与羟胺盐酸盐进行肟化/环化，形成4-（4'-氯苯基）-5,6-弯 - 恶嗪 - （8）高产纯度; 用锌金属和乙酸将后者还原成相应的式（9）的对甲苯胺; 然后在不存在溶剂的情况下通过与氯磺酸和亚硫酰氯反应转化为2-（3'-氯磺酰基-4'-氯苯基）苯并咪唑配方（10）。式（10）化合物的酰胺化用氨水/溶液在非水溶剂如酮和极性非质子溶剂如二甲基甲酰胺中进行，得到式（11）的化合物。在碱存在下用过氧化氢氧化式（11）导致氯代吡喃酮的高产率。

2. 发明申请

WO2010074532A3 RADIOACTIVE CELL MARKER 审中-公开
公开(公告)号：WO2010074532A3
公开(公告)日：2010-09-10
申请号：PCT/KR2009007780
申请日：2009-12-24
申请人： KYUNGPOOK NAT UNIV IND ACAD , YOO JEONG SOO , JEON HAK RIM , PANDYA DARPAN NAVINCHANDRA , LEE HWA YOUNG , OH JI EUN
发明人： YOO JEONG SOO , JEON HAK RIM , PANDYA DARPAN NAVINCHANDRA , LEE HWA YOUNG , OH JI EUN
IPC分类号： C07F13/00
CPC分类号： C07F7/2212
摘要： The present invention relates to the radioactive marker compound of chemical formula 1 or 2, a composition containing the radioactive marker compound, and a method for preparing the radioactive marker compound. The marker compound of the invention enables cells to be marked with high efficiency and the movements of a marked cell to be monitored over a long period.

3. 发明申请

WO2005065046A3 AN EFFICIENT INDUSTRIAL PROCESS FOR 3-HYDROXY-3-(3'-SULFAMYL-4'-CHLOROPHENYL)PHTALIMIDINE 审中-公开
标题翻译： 3-羟基-3-（3'-磺酰基-4'-氯苯基）苯并咪唑的有效工业方法
公开(公告)号：WO2005065046A3
公开(公告)日：2006-08-17
申请号：PCT/IN2004000370
申请日：2004-11-30
申请人： IPCA LAB LTD , KUMAR ASHOK , SINGH DHARMENDRA , JADHAV ATUL , PANDYA DARPAN NAVINCHANDRA
发明人： KUMAR ASHOK , SINGH DHARMENDRA , JADHAV ATUL , PANDYA DARPAN NAVINCHANDRA
IPC分类号： C07D209/44
CPC分类号： C07D209/48
摘要： The oximination/cyclization of 2-(4-chlorobenzoyl)benzoic acid with hydroxylamine hydrochloride in presence of molar quantities of inorganic base in water or in alcoholic solvents to form 4-(4'-chlorophenyl)-5,6-bent-oxazine-l-one Formula (8) in high yield and purity; reduction of latter with zinc metal and acetic acid to the corresponding phtalimidine of Formula (9); followed by conversion into 2-(3'-chlorosulphonyl-4'-chlorophenyl)phtalimidine Formula (10) by reaction with chlorosulphonic acid and thionyl chloride in the absence of solvent. Amidation of compound of formula (10) was carried out with ammonia gas/solution in non.-aqueous solvent like ketones and polar aprotic solvents like dimethylformamide, to yield compound of formula (11). Oxidation of Formula (11) with hydrogen peroxide in presence of alkali results in high yield of chlorihalidone.
摘要翻译：在水或醇溶剂中存在无机碱的摩尔量存在下，将2-（4-氯苯甲酰基）苯甲酸与羟胺盐酸盐进行肟化/环化，形成4-（4'-氯苯基）-5,6-弯 - 恶嗪 - （8）高产纯度; 用锌金属和乙酸将后者还原成相应的式（9）的对甲苯胺; 然后在不存在溶剂的情况下通过与氯磺酸和亚硫酰氯反应转化为2-（3'-氯磺酰基-4'-氯苯基）苯并咪唑配方（10）。式（10）化合物的酰胺化用氨水/溶液在非水溶剂如酮和极性非质子溶剂如二甲基甲酰胺中进行，得到式（11）的化合物。在碱存在下用过氧化氢氧化式（11）导致氯代吡喃酮的高产率。

4. 发明申请

WO2006046253A1 A ONE-POT PROCESS FOR THE PREPARATION OF ANTIEMETIC AGENT, 1,2,3,9-TETRAHYDRO-9-METHYL-3[(2-METHYL)-1H-IMIDAZOLE-1-YL)METHYL]-4H-CARBAZOL-4-O 审中-公开
标题翻译： 1,9-四氢-9-甲基-3 [（2-甲基）-1H-咪唑-1-基）甲基] -4H-卡巴唑-4的制备方法1制备方法 -O
公开(公告)号：WO2006046253A1
公开(公告)日：2006-05-04
申请号：PCT/IN2004/000336
申请日：2004-10-26
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra , PANMAND, Deepak, Shankar , THAKUR, Gajendrasingh, Ramsingh
发明人： KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra , PANMAND, Deepak, Shankar , THAKUR, Gajendrasingh, Ramsingh
IPC分类号： C07D233/56
CPC分类号： C07D403/06
摘要： A one-pot industrial process for preparing 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazole-1-yl)methyl]-4H-carbazol-4-one of Formula-(I) from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one of Formula-(IV) involves reaction of Formula (IV) with HNR 1 R 2 salt and paraformaldehyde, where R 1 ,R 2 are independently alkyl groups or together forms a cyclic alkyl group, in a solvent system of acetic acid and hydrocarbon solvent to form a crude mixture of intermediate compounds of Formula (III) and (VIII), which is converted to ondansetron (Formula (I)) without isolation by reaction with 2methyimidazole in a suitable solvent system in the same pot.
摘要翻译：制备式为1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮的一锅工业方法 - （I）由式（Ⅳ）的1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮包括式（Ⅳ）与HNR 1 R 其中R 1，R 2，R 2独立地为烷基或一起形成环烷基，在乙酸的溶剂体系中酸和烃溶剂形成式（III）和（VIII）的中间体化合物的粗制混合物，其在相同的罐中在合适的溶剂体系中与2-甲基咪唑反应而不分离而转化成昂丹司琼（式（I））。

5. 发明申请

WO2011102626A2 POLYAZAMACROCYCLIC COMPOUND, AND A PRODUCTION METHOD AND A BIOMEDICAL USE THEREFOR 审中-公开
标题翻译：聚山梨醇化合物及其制备方法及其生物医学用途
公开(公告)号：WO2011102626A2
公开(公告)日：2011-08-25
申请号：PCT/KR2011000977
申请日：2011-02-14
申请人： KYUNGPOOK NAT UNIV IND ACAD , YOO JEONGSOO , PANDYA DARPAN NAVINCHANDRA
发明人： YOO JEONGSOO , PANDYA DARPAN NAVINCHANDRA
IPC分类号： C07D257/02 , A61K49/06 , A61K49/10 , A61P35/00
CPC分类号： C07D257/02 , A61K51/082 , A61K51/088 , A61K51/1051 , A61K51/1093
摘要： According to the present invention, a novel polyazamacrocyclic compound which is used as a bifunctional chelating agent (BFC) can be synthesised selectively and in high yield. The novel polyazamacrocyclic compound synthesised in this way chelates with metals and so can be conjugated with bioactive molecules such as peptides, and can be used in the diagnosis and treatment of medical conditions.
摘要翻译：根据本发明，可以选择性且高收率地合成用作双功能螯合剂（BFC）的新型多氮杂环化合物。以这种方式合成的新型多氮杂环化合物与金属螯合，因此可以与肽等生物活性分子缀合，可用于医疗条件的诊断和治疗。

6. 发明申请

WO2010074532A2 RADIOACTIVE CELL MARKER 审中-公开
标题翻译：放射性细胞标记
公开(公告)号：WO2010074532A2
公开(公告)日：2010-07-01
申请号：PCT/KR2009007780
申请日：2009-12-24
申请人： KYUNGPOOK NAT UNIV IND ACAD , YOO JEONG SOO , JEON HAK RIM , PANDYA DARPAN NAVINCHANDRA , LEE HWA YOUNG , OH JI EUN
发明人： YOO JEONG SOO , JEON HAK RIM , PANDYA DARPAN NAVINCHANDRA , LEE HWA YOUNG , OH JI EUN
IPC分类号： C07F13/00
CPC分类号： C07F7/2212
摘要： The present invention relates to the radioactive marker compound of chemical formula 1 or 2, a composition containing the radioactive marker compound, and a method for preparing the radioactive marker compound. The marker compound of the invention enables cells to be marked with high efficiency and the movements of a marked cell to be monitored over a long period.
摘要翻译：本发明涉及化学式1或2的放射性标记化合物，含有放射性标记化合物的组合物以及制备放射性标记化合物的方法。本发明的标记化合物能够高效地标记细胞，并且长时间监测标记细胞的移动。

7. 发明申请

WO2006109318A1 NOVEL POLYMORPH OF 3-HYDROXY-3-(3’-SULFAMYL-4’-CHLOROPHENYL)PHTHALIMIDINE 审中-公开
标题翻译： 3-羟基-3-（3'-磺酰基-4'-氯苯基）对苯二胺的新型聚
公开(公告)号：WO2006109318A1
公开(公告)日：2006-10-19
申请号：PCT/IN2005/000109
申请日：2005-04-11
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , SAXENA, Ashvini , SINGH, Dharmendra , DHURANDHARE, Vijay , PANDYA, Darpan, Navinchandra
发明人： KUMAR, Ashok , SAXENA, Ashvini , SINGH, Dharmendra , DHURANDHARE, Vijay , PANDYA, Darpan, Navinchandra
IPC分类号： C07D209/34 , A61K31/404
CPC分类号： C07D209/34
摘要： Disclosed herein is a novel crystalline form of Chlorthalidone designated as Form II, its solvates thereof; the processes for their preparation; isolation of this new form; and its use in pharmaceutical preparations. The present invention further discloses the novel processes for preparation of Form I and its characterization.
摘要翻译：本文公开了一种命名为形式II的氯噻酮的新结晶形式，其溶剂合物; 其准备过程; 隔离这种新形式; 及其在药物制剂中的应用。本发明还公开了制备形式I及其表征的新方法。

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