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1. 发明申请

WO2008125578A2 A METHOD FOR THE PREPARATION OF AN ENANTIOMER OF A TETRACYCLIC BENZAZEPINE 审中-公开
标题翻译：一种制备四羧酸苯并噻唑类化合物的方法
公开(公告)号：WO2008125578A2
公开(公告)日：2008-10-23
申请号：PCT/EP2008/054316
申请日：2008-04-10
申请人： N.V. ORGANON , KEMPERMAN, Gerardus Johannes
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： The present invention relates to a method for the preparation of mirtazapine and tetracyclic analogous compounds having substantial enantiomeric excess of the R or S form. The invention further relates to a novel intermediate and its use for the preparation of mirtazapine having a substantial enantiomeric excess of the R or S form. The method comprising the steps of a: providing a carboxylic acid compound according to Formula (I) having a substantial enantiomeric excess of the R or S form, b: converting the carboxylic acid group of compound I into a ketone group, producing a ketone compound of Formula (II), c: optionally reducing ketone compound II with a mild reduction agent to form the intermediate hydroxy compound of Formula (III) and d: forming the mirtazapine of Formula (IV) by reduction of the ketone compound II or of the hydroxy compound III using a strong reduction agent.
摘要翻译：本发明涉及制备具有R或S形式的显着对映体过量的米氮平和四环类似物的方法。本发明还涉及一种新的中间体及其用于制备具有R或S形式的基本对映体过量的米氮平的用途。该方法包括以下步骤：a）提供具有R或S形式的基本对映异构体过量的式（I）的羧酸化合物，b：将化合物I的羧酸基团转化为酮基，产生酮化合物式（II）的化合物，c：任选地用温和的还原剂还原酮化合物II以形成式（III）的中间体羟基化合物，和d：通过还原酮化合物II或式羟基化合物III使用强还原剂。

2. 发明申请

WO2010149727A2 INJECTABLE FORMULATIONS CONTAINING ASENAPINE AND METHOD OF TREATMENT USING SAME 审中-公开
标题翻译：含有ASENAPINE的注射剂及其使用方法
公开(公告)号：WO2010149727A2
公开(公告)日：2010-12-29
申请号：PCT/EP2010/058960
申请日：2010-06-24
申请人： N.V. ORGANON , FAASSEN, Werenfridus Adrianus , KEMPERMAN, Gerardus Johannes , VAN LAARHOVEN, Johannes, Antonius, Hendrikus
发明人： FAASSEN, Werenfridus Adrianus , KEMPERMAN, Gerardus Johannes , VAN LAARHOVEN, Johannes, Antonius, Hendrikus
IPC分类号： A61K9/00
CPC分类号： A61K9/19 , A61K9/0019 , A61K9/10 , A61K31/40 , A61K31/407 , A61K47/10 , C07D491/044
摘要： The present invention provides a formulation comprising asenapine hemipamoate suspended particles, which formulation can be administered via a Depot provided by an IM injection of the formulation, and which depot does not display a particle-size dependent release rate. The present invention provides also methods of treatment using the same.
摘要翻译：本发明提供了一种含有阿替平半胱氨酸盐悬浮颗粒的制剂，该制剂可以通过经IM注射制剂提供的贮库来施用，并且该贮库不显示粒度依赖性释放速率。本发明还提供了使用其的治疗方法。

3. 发明申请

WO2008125577A1 A METHOD FOR THE PREPARATION OF AN ENANTIOMERICALLY PURE BENZAZEPINE 审中-公开
标题翻译：一种制备纯粹的苯甲腈的方法
公开(公告)号：WO2008125577A1
公开(公告)日：2008-10-23
申请号：PCT/EP2008/054315
申请日：2008-04-10
申请人： N.V. ORGANON , SEERDEN, Johannes Paulus Gerardus , KEMPERMAN, Gerardus Johannes
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D471/04 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： The invention relates to a method for the preparation of a cyclic compound according to formula (III) comprising reacting a compound according to Formula (I) and a compound according to formula (II), wherein in Formula (I), R 1 , R 2 , R 3 and R 4 may be hydrogen or substituent groups comprising one or more carbon atoms and/or hetero-atoms, wherein R 1 , R 2 , R 3 and R 4 can be combined in aromatic or aliphatic ring structures, -Y is a ring element comprising 1-3 substituted or unsubstituted carbon atoms and/or heteroatoms in the ring and -R 5 is hydrogen or a hydrocarbon substituent group comprising one or more carbon atoms and optionally one or more hetero atoms, and wherein in Formula (II), Z 1 and Z 2 are, leaving groups, X is a reactive functional hydrocarbon group for subsequent ring closure, comprising one or more carbon atoms and a reactive functional group and having a chain of between 1 to 6 atoms between the carbon atom attached to the central carbon atom of formula (II) and the reactive functional group and R 8 is hydrogen or a hydrocarbon substituent different from X making the central carbon atom of formula II a chiral centre in Formula (III) and wherein reactive functional group X can be or can be extended to be compound of formula (IV) which can be ring closed to produce the polycyclic component of formula (V). More in particular, the invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.
摘要翻译：本发明涉及制备根据式（III）的环状化合物的方法，包括使根据式（I）的化合物与式（II）化合物反应，其中在式（I）中R 1， R 1，R 2，R 3和R 4可以是氢或包含一个或多个碳原子的取代基和/或杂原子，其中R 1，R 2，R 3和R 4可以在芳族或脂族环结构-Y是在环中包含1-3个取代或未取代的碳原子和/或杂原子的环元素，-R 5是氢或包含一个或多个碳原子的烃取代基和任选的一个或多个杂原子，并且其中在式（II）中，Z 1和Z 2是离去基团，X是用于后续环的反应性官能烃基封闭，包含一个或多个碳原子和反应性官能团并具有一个CH 在连接到式（II）的中心碳原子的碳原子和反应性官能团和R 8之间的1至6个原子之间的ain是氢或与X不同的烃取代基，使得中心碳式II的原子是式（III）中的手性中心，并且其中反应性官能团X可以或可以扩展为可以闭环以产生式（V）的多环组分的式（IV）化合物。更具体地，本发明涉及米氮平前体和米氮平的制备，其优选具有显着的对映体过量。

4. 发明申请

WO2009087058A1 PROCESS FOR THE PREPARATION OF ASENAPINE AND INTERMEDIATE PRODUCTS USED IN SAID PROCESS 审中-公开
标题翻译：在制剂过程中使用的ASENAPINE和中间产品的制备方法
公开(公告)号：WO2009087058A1
公开(公告)日：2009-07-16
申请号：PCT/EP2008/068187
申请日：2008-12-22
申请人： N.V. ORGANON , KEMPERMAN, Gerardus Johannes
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D491/044 , C07D207/08 , A61K31/407 , A61P25/24
CPC分类号： C07D491/044 , C07D207/08
摘要： The invention relates to a novel process for the preparation of asenapine, i.e. trans -5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.
摘要翻译：本发明涉及一种制备阿替平的新方法，即反式-5-氯-2-甲基-2,3,3a，12b-四氢-1H-二苯并[2,3：6,7]氧杂环庚烯并[4， 5-c]吡咯，以及用于所述方法的新型中间产物。

5. 发明申请

WO2007144409A1 STEREOSELECTIVE SYNTHESIS OF (S)-1-METHYL-3-PHENYLPIPERAZINE 审中-公开
标题翻译：（S）-1-甲基-3-苯基哌嗪的立体选择性合成
公开(公告)号：WO2007144409A1
公开(公告)日：2007-12-21
申请号：PCT/EP2007/055914
申请日：2007-06-14
申请人： N.V. ORGANON , VAN VLIET, Michiel, Christian, Alexander , KEMPERMAN, Gerardus Johannes , SCHREUDER GOEDHEIJT, Marcel
发明人： VAN VLIET, Michiel, Christian, Alexander , KEMPERMAN, Gerardus Johannes , SCHREUDER GOEDHEIJT, Marcel
IPC分类号： C07D241/04
CPC分类号： C07D241/04 , C07D471/14 , C12P17/12
摘要： This invention provides for a compound according to Formula (1), wherein R 1 is methyl, ethyl, n-propyl, isopropyl, benzyl or 2-haloethyl and the use thereof in a method to prepare (S)-1-methyl-3-phenylpiperazine by enzymatic hydrolysis of the compound, followed by separation and cleavage of the oxalamic groups, whereby the protease of Streptomyces griseus is used as enzyme for the enzymatic hydrolysis.
摘要翻译：本发明提供式（1）化合物，其中R 1是甲基，乙基，正丙基，异丙基，苄基或2-卤代乙基，以及其在制备（S ）-1-甲基-3-苯基哌嗪通过酶水解化合物，然后分离和切割草酰胺基团，由此将灰链霉菌的蛋白酶用作酶水解的酶。

6. 发明公开

EP2240492A1 PROCESS FOR THE PREPARATION OF ASENAPINE AND INTERMEDIATE PRODUCTS USED IN SAID PROCESS 有权转让
标题翻译：过程阿塞那平，在这种方法中使用的中间产品
公开(公告)号：EP2240492A1
公开(公告)日：2010-10-20
申请号：EP08870123.0
申请日：2008-12-22
申请人： N.V. Organon
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D491/044 , C07D207/08 , A61K31/407 , A61P25/24
CPC分类号： C07D491/044 , C07D207/08
摘要： The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

7. 发明授权

EP2038260B1 STEREOSELECTIVE SYNTHESIS OF (S)-1-METHYL-3-PHENYLPIPERAZINE 有权转让
标题翻译：作者（S）-1-甲基-3-苯基哌嗪立体选择性合成
公开(公告)号：EP2038260B1
公开(公告)日：2010-09-01
申请号：EP07730171.1
申请日：2007-06-14
申请人： N.V. Organon
发明人： VAN VLIET, Michiel, Christian, Alexander , KEMPERMAN, Gerardus Johannes , SCHREUDER GOEDHEIJT, Marcel
IPC分类号： C07D241/04
CPC分类号： C07D241/04 , C07D471/14 , C12P17/12
摘要： This invention provides for a compound according to Formula (1), wherein R1 is methyl, ethyl, n-propyl, isopropyl, benzyl or 2-haloethyl and the use thereof in a method to prepare (S)-1-methyl-3-phenylpiperazine by enzymatic hydrolysis of the compound, followed by separation and cleavage of the oxalamic groups, whereby the protease of Streptomyces griseus is used as enzyme for the enzymatic hydrolysis.

8. 发明公开

EP2146993A2 A METHOD FOR THE PREPARATION OF MIRTAZAPINE 有权转让
标题翻译：用于生产米氮平
公开(公告)号：EP2146993A2
公开(公告)日：2010-01-27
申请号：EP08736038.4
申请日：2008-04-10
申请人： N.V. Organon
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： The present invention relates to a method for the preparation of mirtazapine and tetracyclic analogous compounds having substantial enantiomeric excess of the R or S form. The invention further relates to a novel intermediate and its use for the preparation of mirtazapine having a substantial enantiomeric excess of the R or S form. The method comprising the steps of a: providing a carboxylic acid compound according to Formula (I) having a substantial enantiomeric excess of the R or S form, b: converting the carboxylic acid group of compound I into a ketone group, producing a ketone compound of Formula (II), c: optionally reducing ketone compound II with a mild reduction agent to form the intermediate hydroxy compound of Formula (III) and d: forming the mirtazapine of Formula (IV) by reduction of the ketone compound II or of the hydroxy compound III using a strong reduction agent.

9. 发明公开

EP2102203A1 A METHOD FOR THE PREPARATION OF AN ENANTIOMERICALLY PURE BENZAZEPINE 无效转让
标题翻译：用于生产对映纯苯并氮杂
公开(公告)号：EP2102203A1
公开(公告)日：2009-09-23
申请号：EP08736037.6
申请日：2008-04-10
申请人： N.V. Organon , Seerden, Johannes Paulus Gerardus
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D471/04 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： The invention relates to a method for the preparation of a cyclic compound according to formula (III) comprising reacting a compound according to Formula (I) and a compound according to formula (II), wherein in Formula (I), R1, R2, R3 and R4 may be hydrogen or substituent groups comprising one or more carbon atoms and/or hetero-atoms, wherein R1, R2, R3 and R4 can be combined in aromatic or aliphatic ring structures, -Y is a ring element comprising 1-3 substituted or unsubstituted carbon atoms and/or heteroatoms in the ring and -R5 is hydrogen or a hydrocarbon substituent group comprising one or more carbon atoms and optionally one or more hetero atoms, and wherein in Formula (II), Z1 and Z2 are, leaving groups, X is a reactive functional hydrocarbon group for subsequent ring closure, comprising one or more carbon atoms and a reactive functional group and having a chain of between 1 to 6 atoms between the carbon atom attached to the central carbon atom of formula (II) and the reactive functional group and R8 is hydrogen or a hydrocarbon substituent different from X making the central carbon atom of formula II a chiral centre in Formula (III) and wherein reactive functional group X can be or can be extended to be compound of formula (IV) which can be ring closed to produce the polycyclic component of formula (V). More in particular, the invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.

10. 发明授权

EP2240492B1 PROCESS FOR THE PREPARATION OF ASENAPINE AND INTERMEDIATE PRODUCTS USED IN SAID PROCESS 有权转让
标题翻译：过程阿塞那平，在这种方法中使用的中间产品
公开(公告)号：EP2240492B1
公开(公告)日：2011-10-05
申请号：EP08870123.0
申请日：2008-12-22
申请人： N.V. Organon
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D491/044 , C07D207/08 , A61K31/407 , A61P25/24
CPC分类号： C07D491/044 , C07D207/08
摘要： The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

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