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公开(公告)号：US20090182008A1
公开(公告)日：2009-07-16
申请号：US12331086
申请日：2008-12-09
IPC分类号： A61K31/47 , C07D215/02
CPC分类号： C07D215/14 , C07B2200/13
摘要： The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous form.
摘要翻译： 本发明涉及匹伐他汀半钙盐的新结晶形式，下文称为多晶型A，B，C，D，E和F，以及无定形形式。 此外，本发明涉及制备这些结晶形式的方法和包含这些结晶形式或无定形形式的无定形形式和药物组合物。
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公开(公告)号：US20090281162A1
公开(公告)日：2009-11-12
申请号：US12386413
申请日：2009-04-17
IPC分类号： A61K31/40 , C07D207/34
CPC分类号： C07D207/34
摘要： The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C, D and E. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.
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公开(公告)号：US20060142582A1
公开(公告)日：2006-06-29
申请号：US10544752
申请日：2004-02-02
IPC分类号： C07D215/16
CPC分类号： C07D215/14 , C07B2200/13
摘要： The present invention is directed to new crystalline forms of Pitavastatin hernicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous form.
摘要翻译： 本发明涉及匹伐他汀鞣酸盐的新结晶形式，以下称为多晶型A，B，C，D，E和F，以及无定形形式。 此外，本发明涉及制备这些结晶形式的方法和包含这些结晶形式或无定形形式的无定型形式和药物组合物。
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公开(公告)号：US20060205805A1
公开(公告)日：2006-09-14
申请号：US11431184
申请日：2006-05-09
IPC分类号： A61K31/401 , C07D207/337
CPC分类号： C07D207/34
摘要： The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C, D and E. The present invention also is directed to crystalline Form A of Atorvastatin calcium (2:1) that is stable against the formation of the AED impurity. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.
摘要翻译： 本发明涉及阿托伐他汀钙（2:1）的新结晶形式，以下称为多晶型X，A，B1，B2，C，D和E.本发明还涉及阿托伐他汀的晶型A 对于形成AED杂质是稳定的钙（2:1）。 此外，本发明涉及制备这些结晶形式的方法和包含结晶形式的药物组合物。
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5.发明申请公开(公告)号：US20060110807A1
公开(公告)日：2006-05-25
申请号：US10529802
申请日：2003-10-02
IPC分类号： C12P7/62
CPC分类号： C12P7/62 , C12P7/6436 , C12P11/00 , C12P13/02 , C12P17/10
摘要： The present invention relates to an improved process for the preparation of phenolic carboxylic acid derivatives catalysed by biocatalytic esterification, transesterification or amidation of a corresponding lower alkyl ester. Biocatalysis is performed in the presence of suitable enzymes, e.g. hydrolases, especially esterases, amidases, lipases and proteases.
摘要翻译： 本发明涉及通过相应的低级烷基酯的生物催化酯化，酯交换或酰胺化催化的酚羧酸衍生物的制备方法。 在合适的酶存在下进行生物催化，例如 水解酶，特别是酯酶，酰胺酶，脂肪酶和蛋白酶。
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公开(公告)号：US09556326B2
公开(公告)日：2017-01-31
申请号：US13879107
申请日：2011-10-17
申请人： Edoardo Menozzi , Kai-Uwe Schoning
发明人： Edoardo Menozzi , Kai-Uwe Schoning
IPC分类号： C08K5/3415 , C07D207/46 , C08F8/30 , C08F8/32 , C08F222/40 , C08K5/00 , C08L39/04 , C08L23/02 , C08F222/06
CPC分类号： C08K5/3415 , C07D207/46 , C08F8/30 , C08F8/32 , C08F222/06 , C08F222/40 , C08K5/005 , C08L23/02 , C08L39/04 , C08L2203/12 , C08L2203/16 , Y10T428/139 , Y10T428/1397 , C08F210/14 , C08L23/24
摘要： A compound of the formula (I) wherein m and n are independently of one another a number from 1 to 50; the ratio of m/n is 1:10 to 10:1, the recurring units X can have the same definition or different definitions, the recurring units Y can have the same definition or different definitions and the recurring units X and Y can have a random, alternating or block distribution; the recurring unit X is a group of the formula (I-a) and the recurring unit Y is a group of the formula (I-b) the radicals R1 independently of one another are C1-C12alkyl or C3-C12cycloalkyl; the radicals R2 and R4 are independently of one another C12-C30alkyl; the radicals R3 are independently of one another hydrogen, C1-C12alkyl or C3-C12cycloalkyl.
摘要翻译： 式（I）的化合物，其中m和n彼此独立地为1至50的数; m / n的比例为1:10至10:1，重复单元X可以具有相同的定义或不同的定义，重复单元Y可以具有相同的定义或不同的定义，并且重复单元X和Y可以具有 随机，交替或块分布; 重复单元X是式（I-a）的基团，重复单元Y是式（I-b）的基团，基团R 1彼此独立地是C 1 -C 12烷基或C 3 -C 12环烷基; 基团R 2和R 4彼此独立地为C 12 -C 30烷基; 基团R 3彼此独立地为氢，C 1 -C 12烷基或C 3 -C 12环烷基。
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7.发明授权公开(公告)号：US09550941B2
公开(公告)日：2017-01-24
申请号：US13879114
申请日：2011-10-17
申请人： Edoardo Menozzi , Kai-Uwe Schoning
发明人： Edoardo Menozzi , Kai-Uwe Schoning
IPC分类号： C09K15/30 , C07D401/14 , C08K5/3492 , C08K3/00
CPC分类号： C08K5/34926 , C07D401/14 , C08K3/013 , C09K15/30
摘要： A compound of the formula (I), wherein one or two radicals of the radicals R1 are independently of one another C1-C20alkyloxy or C3-C12cycloalkyloxy and the remaining radicals R1 are independently of one another hydrogen, C1-C20alkyl or C3-C12cycloalkyl; the radicals R0 and R2 are independently of one another hydrogen, C1-C20alkyl, C3-C12cycloalkyl or a group of the formula (II-a) with R3 being hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C1-C20alkyloxy or C3-C12cycloalkyloxy; Y is C2-C12alkylene; m is 0 or 1; n is 1, 2 or 3; when n is 1, X is hydrogen, C1-C20alkyl, C3-C12cycloalkyl or a group of the formula (II-a); when n is 2, X is C2-C12alkylene; when n is 3, X is a group N(Z—)3 with Z being C2-C12alkyl.
摘要翻译： 式（I）的化合物，其中基团R 1的一个或两个基团彼此独立地为C 1 -C 20烷氧基或C 3 -C 12环烷氧基，其余基团R 1彼此独立地为氢，C 1 -C 20烷基或C 3 -C 12环烷基; 基团R 0和R 2彼此独立地为氢，C 1 -C 20烷基，C 3 -C 12环烷基或式（II-a）基团，其中R 3为氢，C 1 -C 20烷基，C 3 -C 12环烷基，C 1 -C 20烷氧基或C 3 -C 12环烷氧基 ; Y是C 2 -C 12亚烷基; m为0或1; n为1,2或3; 当n为1时，X为氢，C 1 -C 20烷基，C 3 -C 12环烷基或式（II-a）基团; 当n为2时，X为C 2 -C 12亚烷基; 当n为3时，X为N（Z-）3，Z为C 2 -C 12烷基
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公开(公告)号：US09458380B2
公开(公告)日：2016-10-04
申请号：US14114538
申请日：2012-04-25
申请人： Walter Fischer , Abdel-Ilah Basbas , Kai-Uwe Schoning , Cinzia Tartarini , Werner Holzl , Bruno Rotzinger
发明人： Walter Fischer , Abdel-Ilah Basbas , Kai-Uwe Schoning , Cinzia Tartarini , Werner Holzl , Bruno Rotzinger
IPC分类号： C09K15/06 , C08K5/1535 , C08K5/52 , C07D307/58 , C07D307/64 , C07D405/12
CPC分类号： C08K5/1535 , C07D307/58 , C07D307/64 , C07D307/68 , C07D405/12 , C08K5/13 , C08K5/1345 , C08K5/3435 , C08K5/357 , C08K5/52 , C08K5/526 , C09K15/06 , C09K15/12 , C09K15/20 , C09K15/22 , C09K15/30
摘要： A composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation; and b) a compound of formula I (Formula I) (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently from each other H, C1-C8-alkyl, C4-C8-cycloalkyl, phenyl, C1-C4-alkoxy or halogen; n is 1, 2, 3, or 4; and when n is 1 A is —C(=0)-OR′1, —C(=0)-N(R′2)(R′3), —CN, phenyl, which is unsubstituted or substituted by one or more C1-C8-alkyl, C4-C8-alkoxy, C5-C7-cycloalkyl or halogen, —H or —S02-phenyl; when n is 2 A is —C(=0)-O—Z1—O—C(=0)-, —C(=0)-N(R″1)—Z2—N(R″2)—C(=0)- or piperazine-N,N′-biscarbonyl.
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9.发明申请公开(公告)号：US20130207043A1
公开(公告)日：2013-08-15
申请号：US13879114
申请日：2011-10-17
申请人： Edoardo Menozzi , Kai-Uwe Schoning
发明人： Edoardo Menozzi , Kai-Uwe Schoning
IPC分类号： C09K15/30 , C07D401/14
CPC分类号： C08K5/34926 , C07D401/14 , C08K3/013 , C09K15/30
摘要： A compound of the formula (I), wherein one or two radicals of the radicals R1 are independently of one another C1-C20alkyloxy or C3-C12cycloalkyloxy and the remaining radicals R1 are independently of one another hydrogen, C1-C20alkyl or C3-C12cycloalkyl; the radicals R0 and R2 are independently of one another hydrogen, C1-C20alkyl, C3-C12cycloalkyl or a group of the formula (II-a) with R3 being hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C1-C20alkyloxy or C3-C12cycloalkyloxy; Y is C2-C12alkylene; m is 0 or 1; n is 1, 2 or 3; when n is 1, X is hydrogen, C1-C20alkyl, C3-C12cycloalkyl or a group of the formula (II-a); when n is 2, X is C2-C12alkylene; when n is 3, X is a group N(Z—)3 with Z being C2-C12alkyl
摘要翻译： 式（I）的化合物，其中基团R 1的一个或两个基团彼此独立地为C 1 -C 20烷氧基或C 3 -C 12环烷氧基，其余基团R 1彼此独立地为氢，C 1 -C 20烷基或C 3 -C 12环烷基; 基团R 0和R 2彼此独立地为氢，C 1 -C 20烷基，C 3 -C 12环烷基或式（II-a）基团，其中R 3为氢，C 1 -C 20烷基，C 3 -C 12环烷基，C 1 -C 20烷氧基或C 3 -C 12环烷氧基 ; Y是C 2 -C 12亚烷基; m为0或1; n为1,2或3; 当n为1时，X为氢，C 1 -C 20烷基，C 3 -C 12环烷基或式（II-a）基团; 当n为2时，X为C 2 -C 12亚烷基; 当n为3时，X为N（Z-）3，Z为C 2 -C 12烷基
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公开(公告)号：US20090061494A1
公开(公告)日：2009-03-05
申请号：US11887982
申请日：2006-04-03
申请人： Kai-Uwe Schoning
发明人： Kai-Uwe Schoning
摘要： Diols of the formula I: or corresponding polymers wherein R1 has been integrated into a polymeric backbone, wherein n ranges from (1) to (4); X is a divalent linking group selected from the group consisting of ether, ester, amino and amido groups; R1 is an n-valent hydrocarbon residue containing at least one reactive group selected from the group consisting of carbon-carbon double or triple bonds and silyl groups; R2, R3 and R4 independently are hydrogen or C1-C4alkyl; are conveniently prepared by treatment of an epoxide of the formula II wherein all residues and the index n are as defined for formula I, or a corresponding polymer, with an epoxide hydrolase, e.g. from lyophilized cells of Aspergillus niger.
摘要翻译： 式I的二醇或其中R 1已经整合到聚合物主链中的相应聚合物，其中n为（1）至（4）; X是选自醚，酯，氨基和酰胺基的二价连接基团; R1是含有至少一个选自碳 - 碳双键或三键和甲硅烷基的反应性基团的n价烃基; R2，R3和R4独立地是氢或C1-C4烷基; 方便地通过处理式II的环氧化物制备，其中所有残基和指数n如式I所定义，或相应的聚合物与环氧化物水解酶如 来自黑曲霉的冻干细胞。
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