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1. 发明授权

US08546428B2 Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol 有权
标题翻译：（α，βR）-6-溴-α-[2-（二甲基氨基）乙基] -2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐
公开(公告)号：US08546428B2
公开(公告)日：2013-10-01
申请号：US12515986
申请日：2007-12-03
申请人： Jean François Alexandre Lucas Hegyi , Wim Albert Alex Aelterman , Yolande Lydia Lang , Sigrid Carl Maria Stokbroekx , Carina Leys , Peter Jozef Maria Van Remoortere , Anne Faure
发明人： Jean François Alexandre Lucas Hegyi , Wim Albert Alex Aelterman , Yolande Lydia Lang , Sigrid Carl Maria Stokbroekx , Carina Leys , Peter Jozef Maria Van Remoortere , Anne Faure
IPC分类号： A61K31/04
CPC分类号： C07D215/227
摘要： The present invention relates to the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.
摘要翻译：本发明涉及（α，βR）-6-溴-α-[2-（二甲基氨基）乙基] -2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐，包含作为活性成分的所述盐的药物组合物及其制备方法。

2. 发明申请

US20100028428A1 FUMARATE SALT OF (ALPHA S, BETA R)-6-BROMO-ALPHA-[2-(DIMETHYLAMINO)ETHYL]-2-METHOXY-ALPHA-1-NAPHTHALENYL-BETA-PHENYL-3-QUINOLINEETHANOL 有权
标题翻译：（ALPHA S，BETA R）-6-溴-α-丙氨酸 - [2-（二甲基氨基）乙基] -2-甲氧基-1-萘基] - 苯基-3-喹啉乙醇的盐酸盐
公开(公告)号：US20100028428A1
公开(公告)日：2010-02-04
申请号：US12515986
申请日：2007-12-03
申请人： Jean Francois Alexandre Lucas Hegyi , Wim Albert Alex Aelterman , Yolande Lydia Lang , Sigrid Carl Maria Stokbroekx , Carina Leys , Peter Josef Maria Van Remoortere , Anne Faure
发明人： Jean Francois Alexandre Lucas Hegyi , Wim Albert Alex Aelterman , Yolande Lydia Lang , Sigrid Carl Maria Stokbroekx , Carina Leys , Peter Josef Maria Van Remoortere , Anne Faure
IPC分类号： A61K9/28 , C07D215/02 , A61K31/47
CPC分类号： C07D215/227
摘要： The present invention relates to the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1 -naphthalenyl-beta-phenyl-3-quinolineethanol, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.
摘要翻译：本发明涉及（α，βR）-6-溴-α-[2-（二甲基氨基）乙基] -2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐，包含作为活性成分的所述盐的药物组合物及其制备方法。

3. 发明申请

US20100130523A1 MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE 审中-公开
标题翻译：甲基脱乙酰壳多糖抑制剂的单盐酸盐
公开(公告)号：US20100130523A1
公开(公告)日：2010-05-27
申请号：US12598743
申请日：2008-05-13
申请人： Julius W.J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
发明人： Julius W.J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
IPC分类号： A61K31/506 , C07D211/28 , C07D401/14 , A61P35/00 , A61P35/02
CPC分类号： C07D211/26 , C07D401/14
摘要： This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.
摘要翻译：本发明提供了单盐酸盐和组蛋白脱乙酰酶抑制剂JNJ-26481585的单盐酸盐水合物的新型结晶形式。本发明还涉及这些形式的制备方法，这些方法中使用的中间体，包含这些形式的药物组合物，以及这些形式在医学治疗中的用途，例如作为抑制增殖性疾病的药物，例如癌症和白血病。

4. 发明申请

US20120289527A1 MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE 有权
标题翻译：甲基脱乙酰壳多糖抑制剂的单盐酸盐
公开(公告)号：US20120289527A1
公开(公告)日：2012-11-15
申请号：US13483678
申请日：2012-05-30
申请人： Julius W.J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
发明人： Julius W.J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00 , C07D211/28
CPC分类号： C07D211/26 , C07D401/14
摘要： This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.
摘要翻译：本发明提供了单盐酸盐和组蛋白脱乙酰酶抑制剂JNJ-26481585的单盐酸盐水合物的新型结晶形式。本发明还涉及这些形式的制备方法，这些方法中使用的中间体，包含这些形式的药物组合物，以及这些形式在医学治疗中的用途，例如作为抑制增殖性疾病的药物，例如癌症和白血病。

5. 发明授权

US08759519B2 Mono-hydrochloric salts of an inhibitor of histone deacetylase 有权
标题翻译：组蛋白脱乙酰酶抑制剂的单盐酸盐
公开(公告)号：US08759519B2
公开(公告)日：2014-06-24
申请号：US13483678
申请日：2012-05-30
申请人： Julius W. J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
发明人： Julius W. J. Dickens , Ioannes Nicolaos Houpis , Yolande Lydia Lang , Carina Leys , Sigrid Carl Maria Stokbroekx , Johan Erwin Edmond Weerts
IPC分类号： C07D405/14 , C07D211/26
CPC分类号： C07D211/26 , C07D401/14
摘要： This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.
摘要翻译：本发明提供了单盐酸盐和组蛋白脱乙酰酶抑制剂JNJ-26481585的单盐酸盐水合物的新型结晶形式。本发明还涉及这些形式的制备方法，这些方法中使用的中间体，包含这些形式的药物组合物，以及这些形式在医学治疗中的用途，例如作为抑制增殖性疾病的药物，例如癌症和白血病。

6. 发明申请

US20100016623A1 PROCESS FOR REGIOSELECTIVE MONO-TOSYLATION OF DIOLS 有权
标题翻译：二异氰酸酯单取代的方法
公开(公告)号：US20100016623A1
公开(公告)日：2010-01-21
申请号：US12515407
申请日：2007-11-09
申请人： Michel Joseph Maurice Guillaume , Yolande Lydia Lang
发明人： Michel Joseph Maurice Guillaume , Yolande Lydia Lang
IPC分类号： C07C303/02
CPC分类号： C07C303/28 , C07C309/73
摘要： The present invention concerns the use of dibutyl tin oxide for regioselective catalytic diol mono-tosylation at a concentration lower than 2 mol %. The present invention also concerns the use of a generic acetal compound of Formula (Ic) in a catalytic process for regioselective diol mono-tosylat ion, wherein Y is selected from the group of C1-6alkyl, phenyl and benzyl. The concentration of the generic acetal compound of Formula (Ic) is less than about 2 mol %, preferably ranges between about 2 mol % and about 0.0005 mol %, preferably ranges between about 0.1 mol % and about 0.005 mol %.
摘要翻译：本发明涉及二氧化锡二氧化锡在浓度低于2mol％的区域选择性催化二醇单甲苯磺酰化中的用途。本发明还涉及式（Ic）的通式缩醛化合物在区域选择性二醇单甲苯磺酰离子的催化方法中的用途，其中Y选自C 1-6烷基，苯基和苄基。式（Ic）的通式缩醛化合物的浓度小于约2mol％，优选在约2mol％至约0.0005mol％之间，优选在约0.1mol％至约0.005mol％之间。

7. 发明申请

US20150141652A1 PROCESS FOR PREPARING 2-[(2E)-2-FLUORO-2-(3-PIPERIDINYLIDENE)ETHYL]-1H-ISOINDOLE-1,3(2H)-DIONE 审中-公开
标题翻译：制备2 - [（2E）-2-氟-2-（3-哌啶子基）乙基] -1H-ISOINDLELE-1,3（2H） - 酮的方法
公开(公告)号：US20150141652A1
公开(公告)日：2015-05-21
申请号：US14348319
申请日：2012-09-28
申请人： Yolande Lydia Lang , Dominique Paul, Michel Depre
发明人： Yolande Lydia Lang , Dominique Paul, Michel Depre
IPC分类号： C07D401/06 , C07D211/22 , C07D211/34
CPC分类号： C07D401/06 , C07D211/22 , C07D211/34 , C07D211/70 , C07D401/04 , C07F9/4006 , C07F9/5407
摘要： The present invention relates to an improved process for preparing 2-[(2E)-2-fluoro-2-(3-piperidinylidene)ethyl]-1H-isoindole-1,3(2H)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3E)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo 3-quinolinecarboxylic acid.
摘要翻译：本发明涉及一种制备2 - [（2E）-2-氟-2-（3-亚哌啶基）乙基] -1H-异吲哚-1,3（2H） - 二酮或其盐的改进方法，其中是抗菌化合物7 - [（3E）-3-（2-氨基-1-氟亚乙基）-1-哌啶基] -1-环丙基-6-氟-1,4-二氢-8 - 甲氧基-4-氧代-3-喹啉羧酸。

8. 发明授权

US08143432B2 Process for regioselective mono-tosylation of diols 有权
标题翻译：二醇区域选择性单甲苯磺酰化方法
公开(公告)号：US08143432B2
公开(公告)日：2012-03-27
申请号：US12515407
申请日：2007-11-09
申请人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang
发明人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang
IPC分类号： C07C303/04
CPC分类号： C07C303/28 , C07C309/73
摘要： The present invention concerns the use of dibutyl tin oxide for regioselective catalytic diol mono-tosylation at a concentration lower than 2 mol %. The present invention also concerns the use of a generic acetal compound of Formula (Ic) in a catalytic process for regioselective diol mono-tosylation, wherein Y is selected from the group of C1-6alkyl, phenyl and benzyl. The concentration of the generic acetal compound of Formula (Ic) is less than about 2 mol %, preferably ranges between about 2 mol % and about 0.0005 mol %, preferably ranges between about 0.1 mol % and about 0.005 mol %.
摘要翻译：本发明涉及二氧化锡二氧化锡在浓度低于2mol％的区域选择性催化二醇单甲苯磺酰化中的用途。本发明还涉及式（Ic）的通式缩醛化合物在区域选择性二醇单甲苯磺酰化的催化方法中的用途，其中Y选自C 1-6烷基，苯基和苄基。式（Ic）的通式缩醛化合物的浓度小于约2mol％，优选在约2mol％至约0.0005mol％之间，优选在约0.1mol％至约0.005mol％之间。

9. 发明授权

US07470809B2 Process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid 有权
标题翻译：制备[2-（4-氟 - 苄基） - 苯基] - 乙酸的方法
公开(公告)号：US07470809B2
公开(公告)日：2008-12-30
申请号：US11574300
申请日：2005-08-26
申请人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang , Armin Roessler , Lars Ulmer , Stefan Marcel Herman Leurs , Dirk De Smaele
发明人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang , Armin Roessler , Lars Ulmer , Stefan Marcel Herman Leurs , Dirk De Smaele
IPC分类号： C07C51/00 , C07C55/28
CPC分类号： C07C57/58 , C07C51/08 , C07C51/373 , C07C51/377 , C07C65/34 , C07C63/72
摘要： The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): a) reacting phthalic anhydride with fluorobenzene or a derivative thereof in appropriate reaction conditions; b) over reducing the product obtained in step a) at the ketone moiety; c) reducing the product obtained in step b) with sodium dihydro-bis(2-methoxyethoxy)aluminate (Red-Al) to the corresponding alcohol; d) chlorinating the alcohol obtained in step c); e) inserting CO into the product obtained in step d) through an appropriate Pd-containing catalytic system. In an alternative embodiment, the step e) is replaced by the steps f1) and f2): f1) reacting the product obtained in step d) with sodium cyanide; f2) hydrolysing the product obtained in step f1). The present invention provides a process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity >95%.
摘要翻译：本发明涉及生产由邻苯二甲酸酐获得的化合物的[2-（4-氟 - 苄基） - 苯基] - 乙酸的新方法。该方法包括随后的步骤a）至e）：a）在合适的反应条件下使邻苯二甲酸酐与氟苯或其衍生物反应; b）在酮部分上还原在步骤a）中获得的产物; c）将步骤b）中得到的产物用二氢 - 双（2-甲氧基乙氧基）铝酸钠（Red-Al）还原成相应的醇; d）氯化步骤c）中得到的醇; e）通过合适的含Pd催化体系将CO插入到步骤d）中获得的产物中。在替代实施方案中，步骤e）被步骤f1）和f2）代替：f1）使步骤d）中获得的产物与氰化钠反应; f2）水解步骤f1）中获得的产物。本发明提供了适用于工业规模的反应器（例如更清洁和更有效）的[2-（4-氟 - 苄基） - 苯基] - 乙酸的生产方法。此外，得到纯度> 95％的结晶物质的2-（4-氟 - 苄基） - 苯基] - 乙酸。

10. 发明授权

US06998494B2 Preparation of trans-fused 3,3a,8,12b-tetrahydro-2h-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan derivatives 失效
标题翻译：反式熔融的3,3a，8,12b-四氢-2h-二苯并[3,4：6,7]环庚并[1,2-b]呋喃衍生物的制备
公开(公告)号：US06998494B2
公开(公告)日：2006-02-14
申请号：US10496279
申请日：2002-12-02
申请人： Yolande Lydia Lang , Bart Petrus Anna Maria Jozef Medaer , Georges Joseph Cornelius Hoornaert , Thierry Brossette , Frans Josef Cornelius Compernolle , Michel Joseph Maurice André Guillaume , Hua Mao , Tomasz Kozlecki
发明人： Yolande Lydia Lang , Bart Petrus Anna Maria Jozef Medaer , Georges Joseph Cornelius Hoornaert , Thierry Brossette , Frans Josef Cornelius Compernolle , Michel Joseph Maurice André Guillaume , Hua Mao , Tomasz Kozlecki
IPC分类号： C07D307/93
CPC分类号： C07D307/93
摘要： The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I) in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.
摘要翻译：本发明涉及制备式（I）的四种非对映异构体中的每一种的方法，化学式id =“CHEM-US-00001”num =“000

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