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1. 发明申请

WO2004056769B1 SYNTHESIS OF AMINES AND INTERMEDIATES FOR THE SYNTHESIS THEREOF 审中-公开
标题翻译：合成氨基和合成的中间体
公开(公告)号：WO2004056769B1
公开(公告)日：2004-11-04
申请号：PCT/EP0350992
申请日：2003-12-12
申请人： CIBA SC HOLDING AG , BERENS ULRICH , DOSENBACH OLIVER , SPRENGER DANIEL
发明人： BERENS ULRICH , DOSENBACH OLIVER , SPRENGER DANIEL
IPC分类号： C07D209/16 , C07D209/18 , C07D209/38 , C07D409/04
CPC分类号： C07D409/04 , C07D209/16 , C07D209/18 , C07D209/38
摘要： The invention relates in a first embodiment to a method for the manufacture of esters of the formula (I), or especially of amides of the formula (II), wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

2. 发明申请

WO2004031109A3 CHIRAL DIOLS, THEIR MANUFACTURE AND LIGANDS AND CATALYSTS DERIVED THEREFROM 审中-公开
标题翻译： CHIRAL DIOLS，它们的制造和配体及其衍生的催化剂
公开(公告)号：WO2004031109A3
公开(公告)日：2004-12-23
申请号：PCT/EP0310568
申请日：2003-09-23
申请人： CIBA SC HOLDING AG , BERENS ULRICH
发明人： BERENS ULRICH
IPC分类号： B01J31/24 , C07C29/36 , C07C29/38 , C07C29/40 , C07C29/70 , C07D307/88 , C07D333/16 , C07F9/28 , C07F9/46 , C07F9/6568 , C07F9/6571 , C07F17/02
CPC分类号： B01J31/2466 , B01J31/1865 , B01J31/1875 , B01J31/2476 , B01J2231/643 , B01J2231/645 , B01J2531/80 , B01J2531/821 , B01J2531/822 , C07B2200/07 , C07C29/36 , C07C29/40 , C07D307/88 , C07D333/16 , C07F9/46 , C07F9/65683 , C07F9/65719 , C07F17/02 , C07C33/26
摘要： The present invention relates to a method for the preparation of C2-symmetric 1,4-diols of the formula IVA or IVB, wherein ring A, R1 and R2 have the meanings given in the specification, that makes use of the metallation of pure enantiomers of alpha-(aryl or heteroaryl)-alpha-substituted alkanol compounds or the use of said alkanol compounds in the preparation of said mmetric 1,4-diols; novel C2-symmetric 1,4-diols in enantiomerically pure form; and methods of use or their use in the synthesis of chiral ligands which find use to produce catalysts for a variety of asymmetric transformations such as hydrogenations.
摘要翻译：本发明涉及制备式IVA或IVB的C2对称1,4-二醇的方法，其中环A，R 1和R 2具有本说明书中给出的含义，其使用纯对映异构体的金属化的α-（芳基或杂芳基）-α-取代的链烷醇化合物或所述链烷醇化合物在制备所述mm的1,4-二醇中的用途; 对映体纯形式的新型C2对称1,4-二醇; 以及其用于合成手性配体的方法或其用于制备各种不对称转化如氢化的催化剂。

3. 发明申请

WO2004056769A3 SYNTHESIS OF AMINES AND INTERMEDIATES FOR THE SYNTHESIS THEREOF 审中-公开
标题翻译：合成氨基和合成的中间体
公开(公告)号：WO2004056769A3
公开(公告)日：2004-09-16
申请号：PCT/EP0350992
申请日：2003-12-12
申请人： CIBA SC HOLDING AG , BERENS ULRICH , DOSENBACH OLIVER , SPRENGER DANIEL
发明人： BERENS ULRICH , DOSENBACH OLIVER , SPRENGER DANIEL
IPC分类号： C07D209/16 , C07D209/18 , C07D209/38 , C07D409/04
CPC分类号： C07D409/04 , C07D209/16 , C07D209/18 , C07D209/38
摘要： The invention relates in a first embodiment to a method for the manufacture of esters of the formula (I), or especially of amides of the formula (II), wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
摘要翻译：本发明在第一个实施方案中涉及用于制备式（I）酯或特别是式（II）的酰胺的酯的方法，其中符号具有说明书中给出的含义以及其它中间体和可用于合成标准物中提及的色胺和其他物质的化合物。合成方法和中间体在药物的合成中是有用的。

4. 发明申请

WO2005075467A2 CRYSTALLINE FORMS OF ZOLMITRIPTAN 审中-公开
标题翻译： ZOLMITRIPTAN的晶体形式
公开(公告)号：WO2005075467A2
公开(公告)日：2005-08-18
申请号：PCT/EP2005050362
申请日：2005-01-28
申请人： CIBA SC HOLDING AG , VAN DER SCHAAF PAUL ADRIAAN , BLATTER FRITZ , SZELAGIEWICZ MARTIN , BERENS ULRICH , DE PAUL SUSAN
发明人： VAN DER SCHAAF PAUL ADRIAAN , BLATTER FRITZ , SZELAGIEWICZ MARTIN , BERENS ULRICH , DE PAUL SUSAN
IPC分类号： A61K31/422 , C07D413/06 , C07D413/00
CPC分类号： C07D413/06
摘要： The present invention is directed to a novel crystalline form of Zolmitriptan, herein designated as Form A, and several novel solvates of Zolmitriptan, herein designated as Form B, C, D, E, F, and G, processes for the preparation thereof and pharmaceutical compositions comprising these crystalline forms.
摘要翻译：本发明涉及Zolmitriptan的新型结晶形式，本文命名为A型，以及佐米曲坦的几种新型溶剂合物，本文命名为B型，C，D，E，F和G型，其制备方法和药物包含这些结晶形式的组合物。

5. 发明申请

WO2006067060A3 ENANTIOSELECTIVE SYNTHESIS OF A STERICALLY HINDERED AMINE 审中-公开
标题翻译：一种不规则的胺类化合物的选择性合成
公开(公告)号：WO2006067060A3
公开(公告)日：2006-08-24
申请号：PCT/EP2005056678
申请日：2005-12-12
申请人： CIBA SC HOLDING AG , BERENS ULRICH , MALAN CHRISTOPHE , KIRNER HANS JUERG
发明人： BERENS ULRICH , MALAN CHRISTOPHE , KIRNER HANS JUERG
IPC分类号： C07C209/70 , C07C209/68 , C07C211/26
CPC分类号： C07C231/18 , C07C209/50 , C07C233/13 , C07C2601/04 , C07C211/29
摘要： Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C 1 -C 4 alkyl or CF 3 ; R 1 is H or methyl or ethyl; R 2 is H or methyl or acyl; R 3 is H or methyl; R' 4 is -CH 3 or =CH 2 ; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R 3 are as in formula (I); A is acyl; and R 4 is -CH 3 or =CH 2 ; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R 1 as methyl or ethyl and/or R 2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.
摘要翻译：其中R是苯基的式（I）化合物或被Cl，Br，C 1 -C 4烷基或CF 3取代的苯基， ; R 1是H或甲基或乙基; R 2是H或甲基或酰基; R 3是H或甲基; R“4是-CH 3或= CH 2; 可以通过氢化其中R和R 3如式（I）中的式（II）化合物的高对映体纯度获得; A是酰基; 和R 4是-CH 3或= CH 2 H 2。在手性铑或钌催化剂存在下。可以随后引入作为甲基或乙基的残基R 1，和/或作为H或甲基的R 2 2，通过脱酰基和任选的烷基化引入外消旋。

6. 发明申请

WO2006021528A3 PROCESS FOR PREPARING FLAKE-FORM PIGMENTS BASED ON ALUMINIUM AND ON SIOZ (Z=0 . 7-2.0) 审中-公开
标题翻译：基于铝和硫化物制备FLAKE-FORM颜料的方法（Z = 0.7-2.0）
公开(公告)号：WO2006021528A3
公开(公告)日：2006-05-04
申请号：PCT/EP2005053994
申请日：2005-08-15
申请人： CIBA SC HOLDING AG , BUJARD PATRICE , BERENS ULRICH
发明人： BUJARD PATRICE , BERENS ULRICH
IPC分类号： C09C1/00
CPC分类号： C09D5/36 , B42D25/387 , B82Y30/00 , C01P2004/62 , C01P2004/64 , C01P2006/60 , C09C1/0015 , C09C1/0018 , C09C1/0021 , C09C1/0078 , C09C1/642 , C09C2200/1008 , C09C2200/1037 , C09C2200/1041 , C09C2200/1054 , C09C2200/301 , C09C2200/302 , C09C2200/303 , C09C2200/304 , C09C2200/308 , C09C2220/20 , C09D11/322 , Y10T428/2995
摘要： The present invention relates to process for the production of plane-parallel platelets, comprising the steps of: a) vapour-deposition of a separating agent onto a carrier to produce a separating agent 5 layer, b) vapour-deposition of at least one product layer onto the separating agent layer, and c) dissolution of the separating agent layer in a solvent and production of a suspension in which the at least one product layer is present in the form of plane-parallel platelets, wherein the separating agent is selected from the group consisting of anthracene, anthraquinone, acetamidophenol, acetylsalicylic acid, camphoric anhydride, benzimidazole, benzene-1,2,4-tricarboxylic acid, biphenyl-2,2-dicarboxylic acid, bis(4-hydroxyphenyl)sulfone, dihydroxyanthraquinone, hydantoin, 3-hydroxybenzoic acid, 8-hydroxyquinoline-5-sulfonic acid monohydrate, 4-hydroxycoumarin, 7-hydroxycoumarin, 3-hydroxynaphthalene-2-carboxylic acid, isophthalic acid, 4,4-methylene-bis-3-hydroxynaphthalene-2-carboxylic acid, naphthalene-1,8-dicarboxylic anhydride, phthalimide and its potassium salt, phenolphthalein, phenothiazine, saccharin and its salts, tetraphenylmethane, triphenylene, triphenylmethanol, and also mixtures of at least two of those substances, especially pentaerythritol (C(CH 2 OH) 4 ), trimesic acid (= 1,3,5 bezene tricarboxylic acid), DL-alanine, DL-valine, 2,6- 20 diaminopurine, ascorbic acid, 1,3,5-benzenetricarboxylic acid, o-acetylsalicyclic acid, diphenic acid, terephthalic acid, pyrogallol, cyanuric acid, hexamethyltetramine (urotropin), fumaric acid, and 4-acetylbenzoic acid and also mixtures of at least two of those substances.
摘要翻译：本发明涉及生产平面平行血小板的方法，包括以下步骤：a）将分离剂气相沉积到载体上以产生分离剂5层，b）至少一种产物的气相沉积层，并且c）将分离剂层溶解在溶剂中并产生悬浮液，其中至少一个产物层以平面平行血小板的形式存在，其中分离剂选自由蒽，蒽醌，乙酰氨基苯酚，乙酰水杨酸，樟脑酸酐，苯并咪唑，苯-1,2,4-三羧酸，联苯-2,2-二羧酸，双（4-羟基苯基）砜，二羟基蒽醌，乙内酰脲， 3-羟基苯甲酸，8-羟基喹啉-5-磺酸一水合物，4-羟基香豆素，7-羟基香豆素，3-羟基萘-2-羧酸，间苯二甲酸，4,4-亚甲基 - 双-3-羟基萘-2-羧酸酸，萘-1,8-二羧酸酐，邻苯二甲酰亚胺及其钾盐，酚酞，吩噻嗪，糖精及其盐，四苯基甲烷，三亚苯基，三苯基甲醇，以及这些物质中的至少两种，特别是季戊四醇（C（CH < （2,3,5,5-三嗪），DL-丙氨酸，DL-缬氨酸，2,6-二氨基嘌呤，抗坏血酸，1,3,5-苯三甲酸，邻乙酰基水杨酸，二苯酸，对苯二甲酸，连苯三酚，氰尿酸，六甲基四胺（促尿蛋白原），富马酸和4-乙酰基苯甲酸，以及这些物质中的至少两种的混合物。

7. 发明申请

WO2005068453A2 CRYSTALLINE FORMS OF RIZATRIPTAN BENZOATE 审中-公开
标题翻译：结晶形式的利塞平苯甲酸盐
公开(公告)号：WO2005068453A2
公开(公告)日：2005-07-28
申请号：PCT/EP2005000034
申请日：2005-01-05
申请人： RATIOPHARM GMBH , VAN DER SCHAAF PAUL ADRIAAN , BERGHAUSEN JOERG , BLATTER FRITZ , SZELAGIEWICZ MARTIN , BERENS ULRICH
发明人： VAN DER SCHAAF PAUL ADRIAAN , BERGHAUSEN JOERG , BLATTER FRITZ , SZELAGIEWICZ MARTIN , BERENS ULRICH
IPC分类号： C07D403/06 , C07D403/00
CPC分类号： C07D403/06
摘要： The present invention is directed to the novel polymorphic Form A and Form B of Rizatriptan benzoate, processes for the preparation thereof and pharmaceutical compositions comprising these crystalline forms.
摘要翻译：本发明涉及苯甲酸利扎曲普坦的新型多晶型A和型B，其制备方法和包含这些晶型的药物组合物。

8. 发明申请

WO03031456A3 LIGANDS FOR ASYMMETRIC REACTIONS 审中-公开
标题翻译：非对称反应的配体
公开(公告)号：WO03031456A3
公开(公告)日：2003-07-24
申请号：PCT/EP0211039
申请日：2002-10-02
申请人： SOLVIAS AG , BERENS ULRICH
发明人： BERENS ULRICH
IPC分类号： C07C67/303 , B01J31/18 , B01J31/22 , B01J31/24 , C07B53/00 , C07B61/00 , C07C45/50 , C07C69/34 , C07C231/12 , C07C233/47 , C07F9/6506 , C07F9/655 , C07F9/6553 , C07F9/6568 , C07F9/6571 , C07F9/6574 , C07F9/70 , C07F9/80 , C07F15/00 , C07F19/00
CPC分类号： C07F15/008 , B01J31/1845 , B01J31/1865 , B01J31/187 , B01J31/226 , B01J31/2471 , B01J2231/321 , B01J2231/323 , B01J2231/52 , B01J2231/643 , B01J2531/80 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/845 , B01J2531/847 , C07B53/00 , C07C45/505 , C07F9/65066 , C07F9/65517 , C07F9/655354 , C07F9/65683 , C07F9/65719 , C07F15/00 , C07F15/0073
摘要： The invention relates to a process for the manufacture of ligands capable of forming metal complexes and such complexes; novel ligands with new backbones, complexes thereof with transition metals, the use of complexes of said ligands with transition metals as catalysts, as well as novel intermediates for the manufacture of said ligands. The ligand complexes are useful in stereoselective synthesis, especially hydrogenation, of various organic molecules. Especially, the process according to the invention is directed to the synthesis of compounds of the formulae IA and IIA, wherein the substituents have the meanings given in the description, and to novel compounds of these formulae as ligands.
摘要翻译：本发明涉及制备能够形成金属络合物和这种络合物的配体的方法; 具有新骨架的新配体，与过渡金属的配合物，所述配体与过渡金属的配合物作为催化剂的用途，以及用于制备所述配体的新型中间体。配体络合物可用于各种有机分子的立体选择性合成，尤其是氢化。特别地，根据本发明的方法涉及合成式IA和IIA的化合物，其中取代基具有说明书中给出的含义，并且涉及这些式的新化合物作为配体。

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