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1.发明申请PROCESS FOR PREPARING ORGANIC COMPOUNDS BY A TRANSITION METAL-CATALYSED CROSS-COUPLING REACTION OF AN ARYL-X, HETEROARYL-X, CYCLOALKENYL-X OR ALKENYL-X COMPOUND WITH AN ALKYL, ALKENYL, CYCLOALKYL OR CYCLOALKENYL HALIDE 审中-公开通过亚苄基，亚苄基，环烷基或环烷基卤化物的ARYL-X，HETEROARYL-X，CYCLOALKENYL-X或ALKENYL-X化合物的过渡金属催化交联偶联反应制备有机化合物的方法公开(公告)号：US20120046471A1
公开(公告)日：2012-02-23
申请号：US13232028
申请日：2011-09-14
Applicant: Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldermar Maximilian Czaplik
Inventor： Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldermar Maximilian Czaplik
IPC: C07D213/16 , C07C1/26 , C07C209/68 , C07C67/343 , C07C41/30
CPC classification number: C07C1/326 , C07B37/04 , C07C2523/745 , C07C2523/75
Abstract: This invention relates to a process for preparing functionalized aryl, heteroaryl, cycloalkenyl, or alkenyl compounds, by a transition-metal-catalyzed cross-coupling reaction of a substituted or unsubstituted aryl-X, heteroaryl-X, cycloalkenyl-X or alkenyl-X compound with an alkyl, alkenyl, cycloalkyl or cycloalkenyl halide, where X is a halide, diazonium, tosylate (p-toluenesulphonate), mesylate (methanesulphonate) or triflate (trifluoromethanesulphonate) leaving group.
Abstract translation: 本发明涉及通过取代或未取代的芳基-X，杂芳基-X，环烯基-X或链烯基-X的过渡金属催化交叉偶联反应制备官能化芳基，杂芳基，环烯基或烯基化合物的方法 与烷基，烯基，环烷基或环烯基卤化物的化合物，其中X是卤化物，重氮，甲苯磺酸酯（对甲苯磺酸酯），甲磺酸酯（甲磺酸酯）或三氟甲磺酸酯（三氟甲磺酸酯）离去基团。
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公开(公告)号：US07589081B2
公开(公告)日：2009-09-15
申请号：US10554603
申请日：2004-05-03
Applicant: Alexander Zapf , Mark Sundermeier , Ralf Jackstell , Matthias Beller , Thomas Riermeier , Axel Monsees , Uwe Dingerdissen
Inventor： Alexander Zapf , Mark Sundermeier , Ralf Jackstell , Matthias Beller , Thomas Riermeier , Axel Monsees , Uwe Dingerdissen
IPC: A61K31/675 , C07F9/28
CPC classification number: C07D295/023 , B01J31/2447 , B01J2231/40 , B01J2531/824 , B01J2531/828 , C07C209/10 , C07C213/08 , C07D295/155 , C07F9/572 , C07F9/5728 , C07F9/6506 , C07C211/48 , C07C211/54 , C07C211/55 , C07C211/56 , C07C217/92
Abstract: The present invention relates to novel nitrogen-containing monodentate phosphane ligands of formula (I) and to their use in catalytic reactions, especially in the improvement of haloaromatic compounds.
Abstract translation: 本发明涉及式（I）的新型含氮单齿膦配体和它们在催化反应中的用途，特别是在改进卤代芳族化合物中。
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Patent Agency Ranking
3.发明申请Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof 有权盐酸奥洛他定的多形态形式及其制备奥洛他定及其盐的方法公开(公告)号：US20070232814A1
公开(公告)日：2007-10-04
申请号：US11392098
申请日：2006-03-28
Applicant: Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
Inventor： Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
IPC: C07D313/10
CPC classification number: C07F9/5325 , C07D313/12 , C07F9/5352 , C07F9/5442
Abstract: The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.
Abstract translation: 本发明提供盐酸奥洛他定（[（Z）-3-（二甲基氨基）亚丙基] -6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸盐酸盐），选择性组胺H1受体 拮抗剂，用于治疗季节性过敏性结膜炎的眼部症状。 本发明还提供了大规模生产奥洛他定的新方法，并且以成本有效的方式提供低水平的杂质，并且不需要使用现有技术中使用的昂贵且危险的碱，丁基锂 奥洛他定的反应。 本发明进一步提供了用于生产奥洛他定的3-二甲基氨基丙基三苯基溴化鏻及其相应的氢溴酸盐的大规模生产的新方法和奥洛他定的药学上可接受的盐。
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4.发明授权Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof 有权盐酸奥洛他定的多形态形式及其制备奥洛他定及其盐的方法公开(公告)号：US07687646B2
公开(公告)日：2010-03-30
申请号：US11392098
申请日：2006-03-28
Applicant: Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
Inventor： Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
IPC: C07D313/10
CPC classification number: C07F9/5325 , C07D313/12 , C07F9/5352 , C07F9/5442
Abstract: The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.
Abstract translation: 本发明提供盐酸奥洛他定（[（Z）-3-（二甲基氨基）亚丙基] -6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸盐酸盐），选择性组胺H1受体 拮抗剂，用于治疗季节性过敏性结膜炎的眼部症状。 本发明还提供了大规模生产奥洛他定的新方法，并且以成本有效的方式提供低水平的杂质，并且不需要使用现有技术中使用的昂贵且危险的碱，丁基锂 奥洛他定的反应。 本发明进一步提供了用于生产奥洛他定的3-二甲基氨基丙基三苯基溴化鏻及其相应的氢溴酸盐的大规模生产的新方法和奥洛他定的药学上可接受的盐。
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公开(公告)号：US20070123707A1
公开(公告)日：2007-05-31
申请号：US10554603
申请日：2004-05-03
Applicant: Alexander Zapf , Mark Sundermeier , Ralf Jackstell , Matthias Belller , Thomas Riermeier , Axel Monsees , Uwe Dingerdissen
Inventor： Alexander Zapf , Mark Sundermeier , Ralf Jackstell , Matthias Belller , Thomas Riermeier , Axel Monsees , Uwe Dingerdissen
IPC: C07F15/00 , C07F9/6506
CPC classification number: C07D295/023 , B01J31/2447 , B01J2231/40 , B01J2531/824 , B01J2531/828 , C07C209/10 , C07C213/08 , C07D295/155 , C07F9/572 , C07F9/5728 , C07F9/6506 , C07C211/48 , C07C211/54 , C07C211/55 , C07C211/56 , C07C217/92
Abstract: The present invention relates to novel nitrogen—containing monodentate phosphane ligands of formula (I) and to their use in catalytic reactions, especially in the improvement of haloaromatic compounds.
Abstract translation: 本发明涉及式（I）的新型含氮单齿膦配体和它们在催化反应中的用途，特别是在改进卤代芳族化合物中。
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6.发明授权Process for preparing organic compounds by a transition metal-catalysed cross-coupling reaction of an aryl-X, heteroaryl-X, cycloalkenyl-X or alkenyl-X compound with an alkyl, alkenyl, cycloalkyl or cycloalkenyl halide 失效通过芳基-X，杂芳基-X，环烯基-X或烯基-X化合物与烷基，烯基，环烷基或环烯基卤化物的过渡金属催化交叉偶联反应制备有机化合物的方法公开(公告)号：US08030520B2
公开(公告)日：2011-10-04
申请号：US12407947
申请日：2009-03-20
Applicant: Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldemar Maximilian Czaplik
Inventor： Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldemar Maximilian Czaplik
IPC: C07C211/00
CPC classification number: C07C1/326 , C07B37/04 , C07C2523/745 , C07C2523/75
Abstract: This invention relates to a process for preparing functionalized aryl, heteroaryl, cycloalkenyl, or alkenyl compounds, by a transition-metal-catalyzed cross-coupling reaction of a substituted or unsubstituted aryl-X, heteroaryl-X, cycloalkenyl-X or alkenyl-X compound with an alkyl, alkenyl, cycloalkyl or cycloalkenyl halide, where X is a halide, diazonium, tosylate (p-toluenesulphonate), mesylate (methanesulphonate) or triflate (trifluoromethanesulphonate) leaving group.
Abstract translation: 本发明涉及通过取代或未取代的芳基-X，杂芳基-X，环烯基-X或链烯基-X的过渡金属催化交叉偶联反应制备官能化芳基，杂芳基，环烯基或烯基化合物的方法 与烷基，烯基，环烷基或环烯基卤化物的化合物，其中X是卤化物，重氮，甲苯磺酸酯（对甲苯磺酸酯），甲磺酸酯（甲磺酸酯）或三氟甲磺酸酯（三氟甲磺酸酯）离去基团。
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公开(公告)号：US20090247764A1
公开(公告)日：2009-10-01
申请号：US12407947
申请日：2009-03-20
Applicant: Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldermar Maximilian Czaplik
Inventor： Mark Sundermeier , Matthias Gotta , Axel Jacobi von Wangelin , Waldermar Maximilian Czaplik
IPC: C07D213/127 , C07C2/58
CPC classification number: C07C1/326 , C07B37/04 , C07C2523/745 , C07C2523/75
Abstract: A process for preparing organic compounds of the general formula (I) R—R′ (I), where R is a substituted or unsubstituted aromatic, heteroaromatic, cycloalkenylic or alkenylic radical and R′ is a substituted or unsubstituted alkylic, alkenylic, cycloalkylic or cycloalkenylic radical, by reacting a corresponding compound of the general formula (II) R—X (II), where X is chlorine, bromine, iodine, diazonium, mesylate (methanesulphonate), tosylate (p-toluenesulphonate) or triflate (trifluorosutphonate) and R is as defined for formula (I), with a corresponding compound of the general formula (III) R′—Y (III), where Y is chlorine, bromine or iodine and R′ is as defined for formula (I), wherein the reaction is carried out in the presence of a) stoichiometric amounts of elemental magnesium, based on the compound of the general formula (II), and b) catalytic amounts of a transition metal compound, based on the compound of the general formula (II), and, if appropriate, c) in the presence of a nitrogen-, oxygen- and/or phosphorus-containing additive in a catalytic or stoichiometric amount, based on the compound of the general formula (II), is described. It is particularly advantageous that the process of the invention is carried out as a one-pot reaction and the organomagnesium compound (Grignard compound) formed in situ as intermediate is not isolated.
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