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1. 发明申请

WO2009047314A2 METHOD OF PRODUCING NUCLEOSIDES 审中-公开
标题翻译：生产核蛋白的方法
公开(公告)号：WO2009047314A2
公开(公告)日：2009-04-16
申请号：PCT/EP2008063582
申请日：2008-10-10
申请人： CILAG AG , JUNGMANN OLIVER , KRAUT NORBERT
发明人： JUNGMANN OLIVER , KRAUT NORBERT
IPC分类号： C07H19/00 , C07H19/06 , C07H19/12 , C07H19/16
CPC分类号： C07H19/00 , C07H19/06 , C07H19/12 , C07H19/16 , Y02P20/55
摘要： Method of producing a free nucleoside compound, the compound 2'- deoxy-5-azacytidine (Decitabine) being excluded, by reacting a glycoside donor preferably a 1-halogen derivative, or 1-0-acyl, 1-0-alkyl, or an imidate preferably a trichloromethyl derivative, or a thio-alkyl derivative of a blocked monosaccharide or oligosaccharide preferably ribose and 2-desoxyribose derivatives with a protected nucleoside base, in a suitable anhydrous solvent and in the presence of a catalyst, and removing the protecting groups from said blocked nucleoside compound, wherein said catalyst is selected from the group comprising salts of an aliphatic sulphonic acid and/or salts a strong inorganic acid containing a non-nucleophilic anion.
摘要翻译：通过使糖苷供体优选为1-卤素衍生物，或1-0-酰基，1-0-烷基，或其盐或其盐，通过使衍生自由核苷化合物的方法，除去化合物2'-脱氧-5-氮杂胞苷（地西他滨）酰亚胺化物优选三氯甲基衍生物，或封闭单糖或寡糖的硫代烷基衍生物，优选核糖和2-脱氧核糖衍生物与被保护的核苷碱基，在合适的无水溶剂中，在催化剂存在下，并除去保护基从所述封闭的核苷化合物中，其中所述催化剂选自脂肪族磺酸盐和/或含有非亲核阴离子的强无机酸的盐。

2. 发明申请

WO2005063696A3 NEUE KRISTALLINE FORMEN VON ENTACAPONE UND DEREN HERSTELLUNG 审中-公开
公开(公告)号：WO2005063696A3
公开(公告)日：2005-07-14
申请号：PCT/CH2004/000754
申请日：2004-12-27
申请人： CILAG AG , BADER, Thomas , FUREGATI, Markus , JUNGMANN, Oliver
发明人： BADER, Thomas , FUREGATI, Markus , JUNGMANN, Oliver
IPC分类号： C07C255/41
摘要： Beschrieben werden drei neue kristalline Formen von Entacapone. Diese sind periphere und selektive COMT-Inhibitoren, welche - in Kombination mit Levodopa und einem Decarboxylasehemmer - zur Behandlung des Parkinson-Syndroms verwendet werden können. Diese neuen Formen entstehen durch Kristallisation von Entacapone unter jeweils bestimmten Bedingungen. In gewissen Fällen kann dabei das Entacapone als Rohprodukt eingesetzt werden, in einem speziellen Fall sogar in stitu als Produkt einer Knoevenagel-Kondensation von 3,4-Dihydroxy-5-nitro-benzaldehyd und N,N-Diethyl-2-cyano-acetamid. Beschrieben werden weiterhin Verbesserungen dieser Kondensation bezüglich des Katalysators und der Herstellung ihrer beiden Komponenten.

3. 发明申请

WO2005063696A2 NOVEL CRYSTALLINE FORMS OF ENTACAPONE AND PRODUCTION THEREOF 审中-公开
标题翻译：恩他卡朋及其生产的新型结晶形态
公开(公告)号：WO2005063696A2
公开(公告)日：2005-07-14
申请号：PCT/CH2004000754
申请日：2004-12-27
申请人： CILAG AG , BADER THOMAS , FUREGATI MARKUS , JUNGMANN OLIVER
发明人： BADER THOMAS , FUREGATI MARKUS , JUNGMANN OLIVER
IPC分类号： C07C253/30 , C07C255/41 , A61K31/277 , A61P25/16
CPC分类号： C07C255/41 , C07B2200/13
摘要： The invention relates to three novel forms of entacapone. These are peripheral and selective COMT inhibitors which in combination with levodopa and decarboxylase inhibitors can be used to treating Parkinson's syndrome. Said novel forms arise by crystallization of entacapone in respectively determined conditions. In certain cases, entacapone can be used as a raw product, in a special case it can be used in situ as the product of Knoevenagel condensation of 3,4-dihydroxy-5-nitro-benzaldehyde and N,N-diethyl-2-cyano-acetamide. Also disclosed are improvements of said condensation in relation to the catalyst and the production of the two components thereof.
摘要翻译：描述恩他卡朋的三个新的结晶形式。这些是外周和选择性的COMT抑制剂，其 - 可用于帕金森氏病的治疗 - 结合左旋多巴和脱羧酶抑制剂。分别在特定条件下引起的恩他卡朋的结晶这些新的形式，。在某些情况下，恩他卡朋可以甚至在štítu产物3,4-二羟基-5-硝基 - 苯甲醛和N，N-二乙基-2-氰基乙酰胺的Knoevenagel缩合用作粗而，在特殊情况下。相对于该催化剂和生产它的两个部件的描述对这些缩合进一步的改进。

4. 发明申请

WO2011113476A2 METHOD FOR PRODUCING 2'-DEOXYADENOSINE COMPOUNDS 审中-公开
标题翻译：生产2'-脱氧腺苷化合物的方法
公开(公告)号：WO2011113476A2
公开(公告)日：2011-09-22
申请号：PCT/EP2010053352
申请日：2010-03-16
申请人： CILAG AG , JUNGMANN OLIVER , THALER ADRIAN , HAENSELER ROLF
发明人： JUNGMANN OLIVER , THALER ADRIAN , HAENSELER ROLF
CPC分类号： C07H19/173
摘要： (A) reacting the alkali metal salt of 2, 6-dichlorpurine with a 2-desoxy-3, 5 -di-O-p-toluoyl-alpha-D-erythro-pentofuranose or a derivative thereof, in a suitable organic solvent, said reaction optionally being carried out in the presence of a Lewis-acid, whereby a mixture comprising the intermediate N (9) -beta-compound, the N (7) -beta-regio- isomer, and the N (9) -alpha-stereoisomer is formed; (B) isolating from said reaction mixture formed the crude reaction product comprising the intermediate N (9) -beta- compound by a purification method, preferably by precipitation or crystallization, using a suitable organic solvent or a mixture of such organic solvents or a mixture of one or more of such organic solvents with water, without using a chromatographic purification method, and (C) subjecting the isolated intermediate N (9 ) -beta-compound to ammonolysis, where upon the 2 '-deoxyadenosine compound is formed, and (D) precipitating or crystallizing the 2 '-deoxyadenosine compound as formed in step (C) from a suitable organic solvent.
摘要翻译：（A）使2,6-二氯嘌呤的碱金属盐与2-脱氧-3,5-二-O-对甲苯酰-α-D-赤型呋喃糖或其衍生物在合适的有机溶剂中反应，所述反应任选地在路易斯酸存在下进行，由此得到包含中间体N（9） - β-化合物，N（7） - 对 - 位异构体和N（9）-α-立体异构体的混合物形成了; （B）通过纯化方法，优选通过沉淀或结晶，使用合适的有机溶剂或这种有机溶剂或混合物的混合物形成包含中间体N（9） - 乙酸酯化合物的粗制反应产物的一种或多种这样的有机溶剂与水反应，而不使用色谱纯化方法，和（C）使分离的中间体N（9） - β-化合物进行氨解，其中在形成2'-脱氧腺苷化合物时，和（ D）从合适的有机溶剂中使步骤（C）中形成的2'-脱氧腺苷化合物沉淀或结晶。

5. 发明申请

WO2011113476A3 METHOD FOR PRODUCING 2'-DEOXYADENOSINE COMPOUNDS 审中-公开
公开(公告)号：WO2011113476A3
公开(公告)日：2011-09-22
申请号：PCT/EP2010/053352
申请日：2010-03-16
申请人： CILAG AG , JUNGMANN, Oliver , THALER, Adrian , HÄNSELER, Rolf
发明人： JUNGMANN, Oliver , THALER, Adrian , HÄNSELER, Rolf
IPC分类号： C07H19/173
摘要： (A) reacting the alkali metal salt of 2, 6-dichlorpurine with a 2-desoxy-3, 5 -di-O-p-toluoyl-alpha-D-erythro-pentofuranose or a derivative thereof, in a suitable organic solvent, said reaction optionally being carried out in the presence of a Lewis-acid, whereby a mixture comprising the intermediate N (9) -beta-compound, the N (7) -beta-regio- isomer, and the N (9) -alpha-stereoisomer is formed; (B) isolating from said reaction mixture formed the crude reaction product comprising the intermediate N (9) -beta- compound by a purification method, preferably by precipitation or crystallization, using a suitable organic solvent or a mixture of such organic solvents or a mixture of one or more of such organic solvents with water, without using a chromatographic purification method, and (C) subjecting the isolated intermediate N (9 ) -beta-compound to ammonolysis, where upon the 2 '-deoxyadenosine compound is formed, and (D) precipitating or crystallizing the 2 '-deoxyadenosine compound as formed in step (C) from a suitable organic solvent.

6. 发明申请

WO2009047313A2 METHOD OF PRODUCING 2' -DEOXY-5-AZACYTIDINE (DECITABINE) 审中-公开
标题翻译： 2'-氧代-5-氮杂环丁烷的生产方法（DECATABINE）
公开(公告)号：WO2009047313A2
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063581
申请日：2008-10-10
申请人： Cilag AG , JUNGMANN, Oliver , KRAUT, Norbert
发明人： JUNGMANN, Oliver , KRAUT, Norbert
IPC分类号： C07H19/12
CPC分类号： C07H19/12 , Y02P20/55
摘要： Method of producing 2'-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I), wherein R is a removable substituent known per se; and R 1 is a removable substituent; further providing a silylated base of formula (II), wherein R 2 is a protecting group, preferably a trimethylsilyl TMS ) -residue; reacting the compound of formula (I) and the compound of formula (II) together in a suitable anhydrous solvent and in the presence of a suitable catalyst; and removing the substituents R from the compound obtained in order to obtain the compound 2'-deoxy-5-azacytidine (Decitabine), characterized in that said catalyst is selected from the group comprising a salt of an aliphatic sulphonic acid or a salt of a strong inorganic acid.
摘要翻译：通过提供式（I）化合物制备2'-脱氧-5-氮杂胞苷（地西他滨）的方法，其中R是本身已知的可除去的取代基; R1是可取代的取代基; 进一步提供式（II）的甲硅烷基化碱，其中R 2是保护基，优选三甲基甲硅烷基TMS） - 残基; 使式（I）化合物和式（II）化合物在合适的无水溶剂中和在合适的催化剂存在下反应; 并从得到的化合物中除去取代基R，得到化合物2'-脱氧-5-氮杂胞苷（地西他滨），其特征在于所述催化剂选自脂肪族磺酸盐或其盐强无机酸。

7. 发明申请

WO2009047313A3 METHOD OF PRODUCING 2' -DEOXY-5-AZACYTIDINE (DECITABINE) 审中-公开
标题翻译：制备2'-氧代-5-氮杂（方法）的方法
公开(公告)号：WO2009047313A3
公开(公告)日：2012-03-01
申请号：PCT/EP2008063581
申请日：2008-10-10
申请人： CILAG AG , JUNGMANN OLIVER , KRAUT NORBERT
发明人： JUNGMANN OLIVER , KRAUT NORBERT
IPC分类号： C07H19/12
CPC分类号： C07H19/12 , Y02P20/55
摘要： Method of producing 2'-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I), wherein R is a removable substituent known per se; and R1 is a removable substituent; further providing a silylated base of formula (II), wherein R2 is a protecting group, preferably a trimethylsilyl TMS ) -residue; reacting the compound of formula (I) and the compound of formula (II) together in a suitable anhydrous solvent and in the presence of a suitable catalyst; and removing the substituents R from the compound obtained in order to obtain the compound 2'-deoxy-5-azacytidine (Decitabine), characterized in that said catalyst is selected from the group comprising a salt of an aliphatic sulphonic acid or a salt of a strong inorganic acid.
摘要翻译：通过提供式（I）化合物制备2'-脱氧-5-氮杂胞苷（地西他滨）的方法，其中R是本身已知的可除去的取代基; 并且R 1是可除去的取代基; 进一步提供式（II）的甲硅烷基化碱，其中R 2是保护基，优选三甲基甲硅烷基TMS） - 残基; 使式（I）化合物和式（II）化合物在合适的无水溶剂中和在合适的催化剂存在下反应; 并从得到的化合物中除去取代基R，得到化合物2'-脱氧-5-氮杂胞苷（地西他滨），其特征在于，所述催化剂选自脂肪族磺酸盐或其盐强无机酸。

8. 发明申请

WO2009047314A3 METHOD OF PRODUCING NUCLEOSIDES 审中-公开
公开(公告)号：WO2009047314A3
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063582
申请日：2008-10-10
申请人： Cilag AG , JUNGMANN, Oliver , KRAUT, Norbert
发明人： JUNGMANN, Oliver , KRAUT, Norbert
IPC分类号： C07H19/00 , C07H19/06 , C07H19/12 , C07H19/16
摘要： Method of producing a free nucleoside compound, the compound 2'- deoxy-5-azacytidine (Decitabine) being excluded, by reacting a glycoside donor preferably a 1-halogen derivative, or 1-0-acyl, 1-0-alkyl, or an imidate preferably a trichloromethyl derivative, or a thio-alkyl derivative of a blocked monosaccharide or oligosaccharide preferably ribose and 2-desoxyribose derivatives with a protected nucleoside base, in a suitable anhydrous solvent and in the presence of a catalyst, and removing the protecting groups from said blocked nucleoside compound, wherein said catalyst is selected from the group comprising salts of an aliphatic sulphonic acid and/or salts a strong inorganic acid containing a non-nucleophilic anion.

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