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1. 发明申请

US20130324706A1 Branched Linker for Protein Drug Conjugates 审中-公开
标题翻译：蛋白质药物缀合物的分支连接子
公开(公告)号：US20130324706A1
公开(公告)日：2013-12-05
申请号：US14001237
申请日：2012-02-23
申请人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Phillips
发明人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Phillips
IPC分类号： A61K47/48 , C07K5/062
CPC分类号： C07K5/06043 , A61K47/60 , A61K47/64 , A61K47/65 , A61K47/6809 , A61K47/6845
摘要： The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.
摘要翻译：本发明涉及将蛋白质和药物连接到蛋白质药物缀合物的方法，其中药物通过特定的支链接头与蛋白质连接，所述支链接头包含肽链，并衍生自邻羟基对氨基苄基醇，其中肽链通过对氨基与苯环连接，药物通过苄醇部分连接到苯环，并且蛋白质通过邻羟基连接到苯环上; 进一步涉及通过各种中间体制备所述蛋白质 - 药物偶联物的方法，将这种蛋白质药物偶联物的药物用途，例如控制不期望细胞生长的方法用于包含这种蛋白质药物偶联物的药物组合物，以及中间体制备蛋白质药物偶联物。

2. 发明授权

US10294270B2 Branched linker for protein drug conjugates 有权
公开(公告)号：US10294270B2
公开(公告)日：2019-05-21
申请号：US14001237
申请日：2012-02-23
申请人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Allway
发明人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Allway
IPC分类号： A61K47/60 , A61K47/64 , A61K47/65 , A61K47/68 , C07K5/062
摘要： The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.

3. 发明申请

US20110009647A1 Process 054 审中-公开
标题翻译：过程054
公开(公告)号：US20110009647A1
公开(公告)日：2011-01-13
申请号：US12885416
申请日：2010-09-17
申请人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
发明人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
IPC分类号： C07D317/44
CPC分类号： C07D317/44
摘要： The present invention is directed to a process for the preparation of a diastereomerically pure dibenzoyl-L-tartrate salt of a compound of formula (III) and to products of said process.
摘要翻译：本发明涉及一种制备式（III）化合物的非对映体纯的二苯甲酰基-L-酒石酸盐的方法和所述方法的产物。

4. 发明申请

US20090182157A1 New Process 054 有权
标题翻译：新进程054
公开(公告)号：US20090182157A1
公开(公告)日：2009-07-16
申请号：US12270999
申请日：2008-11-14
申请人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
发明人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
IPC分类号： C07D317/44
CPC分类号： C07D317/44
摘要： The present invention is directed to a process for the preparation of a diastereomerically pure dibenzoyl-L-tartrate salt of a compound of formula (III) and to products of said process.
摘要翻译：本发明涉及制备式（III）化合物的非对映体纯的二苯甲酰基-L-酒石酸盐的方法和所述方法的产物。

5. 发明申请

US20100174119A1 PROCESS FOR THE PREPARATION OF ALDEHYDES 审中-公开
标题翻译：制备ALDEHYDES的方法
公开(公告)号：US20100174119A1
公开(公告)日：2010-07-08
申请号：US12666576
申请日：2008-06-30
申请人： Laurent Ducry , Dominique Roberge , Meinrad Mathier , Michael Gottsponer
发明人： Laurent Ducry , Dominique Roberge , Meinrad Mathier , Michael Gottsponer
IPC分类号： C07C45/61
CPC分类号： C07C45/41 , C07B31/00 , C07B41/06 , C07C47/02
摘要： The present invention is related to a method for the production of an aldehyde by reducing an ester of a carboxylic acid with H-DIBAL (diisobutylaluminium hydride).
摘要翻译：本发明涉及通过用H-DIBAL（二异丁基氢化铝）还原羧酸酯来制备醛的方法。

6. 发明授权

US07939698B2 Method for grignard type reactions in microreactors 有权
标题翻译：微反应器中格氏反应的方法
公开(公告)号：US07939698B2
公开(公告)日：2011-05-10
申请号：US12373636
申请日：2007-07-11
申请人： Dominique Roberge , Nikolaus Bieler , Laurent Ducry
发明人： Dominique Roberge , Nikolaus Bieler , Laurent Ducry
IPC分类号： C07C17/38
CPC分类号： C07F3/02 , B01F5/0603 , B01F5/0606 , B01F13/0059 , B01J19/0093 , B01J2219/00867 , B01J2219/00873 , B01J2219/00889 , B01J2219/00984 , C07B49/00
摘要： The present invention relates to a process for Grignard type reactions comprising mixing at least two fluids in a microreactor having at least two injection points.
摘要翻译：本发明涉及格利雅型反应方法，包括在具有至少两个注射点的微反应器中混合至少两种流体。

7. 发明申请

US20100298567A1 NITRATION OF ACTIVATED AROMATICS IN MICROREACTORS 审中-公开
标题翻译：微生物中激活的芳族化合物的硝化
公开(公告)号：US20100298567A1
公开(公告)日：2010-11-25
申请号：US12160804
申请日：2006-01-12
申请人： Dominique Roberge , Laurent Ducry
发明人： Dominique Roberge , Laurent Ducry
IPC分类号： C07D239/02 , C07C205/00 , C07C63/04 , C07D211/72
CPC分类号： C07C201/08 , B01J19/0093 , B01J2219/0086 , B01J2219/00984 , C07C205/23 , C07C205/22 , C07C205/25 , C07C205/37 , C07C205/59 , C07C205/60
摘要： The invention relates to the nitration of aromatic or heteroaromatic compounds, wherein an activated aromatic or heteroaromatic compound and a nitration agent, optionally in the presence of a solvent, are mixed intensely in a microreactor, and wherein the proportion of the nitration agent to the activated aromatic or heteroaromatic compound, the concentration of nitration agent in the reaction mixture, and the temperature are selected at levels such high that the nitration begins autocatalytically, and wherein the nitration product is obtained after leaving the microreactor and, optionally after an after-reaction time outside the microreactor.
摘要翻译：本发明涉及芳族或杂芳族化合物的硝化，其中任选在溶剂存在下的活化芳族或杂芳族化合物和硝化剂在微反应器中强烈混合，并且其中硝化剂与活化的芳族或杂芳族化合物，硝化剂在反应混合物中的浓度和温度选择为使得硝化开始自动催化的水平，并且其中硝化产物在离开微反应器之后获得，并且任选地在反应后时间在微反应器外面。

8. 发明授权

US07816545B2 Process 054 有权
标题翻译：过程054
公开(公告)号：US07816545B2
公开(公告)日：2010-10-19
申请号：US12270999
申请日：2008-11-14
申请人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
发明人： Rhony Aufdenblatten , Martin Hans Bohlin , Laurent Ducry , Ulrika Lindblad , Mattias Magnusson
IPC分类号： C07D317/44
CPC分类号： C07D317/44
摘要： The present invention is directed to a process for the preparation of a diastereomerically pure dibenzoyl-L-tartrate salt of a compound of formula (III) and to products of said process.
摘要翻译：本发明涉及制备式（III）化合物的非对映体纯的二苯甲酰基-L-酒石酸盐的方法和所述方法的产物。

9. 发明申请

US20090270663A1 METHOD FOR GRIGNARD TYPE REACTIONS IN MICROREACTORS 有权
标题翻译：微生物颗粒反应的方法
公开(公告)号：US20090270663A1
公开(公告)日：2009-10-29
申请号：US12373636
申请日：2007-07-11
申请人： Dominique Roberge , Nikolaus Bieler , Laurent Ducry
发明人： Dominique Roberge , Nikolaus Bieler , Laurent Ducry
IPC分类号： C07C17/38
CPC分类号： C07F3/02 , B01F5/0603 , B01F5/0606 , B01F13/0059 , B01J19/0093 , B01J2219/00867 , B01J2219/00873 , B01J2219/00889 , B01J2219/00984 , C07B49/00
摘要： The present invention relates to a process for Grignard type reactions comprising mixing at least two fluids in a microreactor having at least two injection points.
摘要翻译：本发明涉及格利雅型反应方法，包括在具有至少两个注射点的微反应器中混合至少两种流体。

10. 发明申请

US20080119651A1 Process For The Production Of Pyrimidine-5-Carboxylates 审中-公开
标题翻译：制备嘧啶-5-羧酸酯的方法
公开(公告)号：US20080119651A1
公开(公告)日：2008-05-22
申请号：US11666637
申请日：2005-11-04
申请人： Laurent Ducry , Bruno Rittiner
发明人： Laurent Ducry , Bruno Rittiner
IPC分类号： C07D239/36 , C07D239/30 , C07D239/46
CPC分类号： C07D239/30 , C07D239/36
摘要： Pyrimidine-5-carboxylates of formula: wherein R is C1-4 alkyl, R1 is C1-4 alkyl, trifluoromethyl, R2 is hydrogen or C1-4 alkyl and X is hydroxy, chlorine or bromine, are prepared from certain 3-oxoalkanoates of formula (II): with urea and orthoesters of formula (III) R2C(OR). The intermediate 2-acyl-3-ureidoacrylate, without being isolated, is reacted to give a 2-hydroxypyrimidine-5-carboxylate[(I), X═OH] or a hydrate thereof, which is optionally converted into the corresponding chloro or bromo compound (I, X═Cl, Br).
摘要翻译：嘧啶-5-羧酸酯，其结构式如下：其中R是C 1-4烷基，R 1是C 1-4烷基，三氟甲基，R 由式（II）的某些3-氧代链烷酸酯制备：氢或C 1-4烷基，X为羟基，氯或溴，其中脲和原酸酯为式（III）R 2 C（OR）。将不分离的中间体2-酰基-3-脲基丙烯酸酯反应，得到2-羟基嘧啶-5-羧酸酯[（I），X-OH]或其水合物，其任选地转化为相应的氯或溴化合物（I，X-Cl，Br）。

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