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1. 发明申请

WO2008080992A2 A PROCESS FOR THE PREPARATION OF 6-[3-(1-ADAMANTYL)-4-METHOXYPHENYL-2-NAPHTOIC ACID 审中-公开
标题翻译：制备6- [3-（1-亚氨基）-4-甲氧基苯基] -2-萘酸的方法
公开(公告)号：WO2008080992A2
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064647
申请日：2007-12-28
申请人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
发明人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
CPC分类号： C07C67/343 , C07C51/09 , C07C2603/74 , C07C65/26 , C07C69/94
摘要： A process for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid from 2-(1-adamantyl)-4-bromanisolee is disclosed, based on transformation of 2-(1-adamantyl)-4-bromanisole into a Grignard's reagent by using metallic magnesium, anhydrous lithium chloride and dibromoethane followed by transmetallation with borates to 3-(adamantyl)-4-methoxyphenylboronic acid, wich is converted into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid esters by Suzuki-Miyaura cross-coupling reaction with alkyl-6-halonaftoates catalyzed by Pd [0] or Pd/phosphine ligands and followed by basic hydrolysis in ethylene glycol or 1,2-propanediol of ester thus obtained into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid.
摘要翻译：从2-（1-金刚烷基）-4-溴胸苷酸制备6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸的方法公开于，基于通过使用金属镁，无水氯化锂和二溴乙烷将2-（1-金刚烷基）-4-溴甲茴香醚转化为格氏试剂，然后用硼酸酯转化为3-（金刚烷基）-4-甲氧基苯基硼酸，将其转化成6- 通过与Pd [0]或Pd /膦配体催化的烷基-6-卤代芴酯通过Suzuki-Miyaura交叉偶联反应形成[3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸酯，然后在乙二醇或1,2-丙二醇酯转化为6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸。

2. 发明申请

WO2008086942A2 A METHOD FOR PREPARATION OF 6-[3-(1-ADAMANTYL)-4-METHOXYPHENYL]-2-NAPHTOIC ACID 审中-公开
标题翻译：制备6- [3-（1-氨基）-4-甲氧基苯基] -2-壬酸的方法
公开(公告)号：WO2008086942A2
公开(公告)日：2008-07-24
申请号：PCT/EP2007/064643
申请日：2007-12-28
申请人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
发明人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
CPC分类号： C07C67/343 , C07C51/09 , C07C2603/74 , C07C65/26 , C07C69/94
摘要： A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on " one pot" synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphtenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.
摘要翻译：基于“一锅”合成方法公开了制备6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸的方法，包括直接合成硼酸衍生物由2-（1-金刚烷基）-4-溴苯甲醚和环丁烷与随后的带有6-卤代萘醌的铃木 - 宫a偶联和乙二醇或1,2-丙二醇中的反应产物的碱性水解。

3. 发明申请

WO2008080993A2 A METHOD FOR PREPARATION OF SUBSTITUTED ADAMANTYLARYLMAGNESIUM HALIDES 审中-公开
标题翻译：一种制备取代的亚氨基甘露聚糖的方法
公开(公告)号：WO2008080993A2
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064648
申请日：2007-12-28
申请人： KALVINSH, Ivars , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir , CHERNOBROVIJS, Aleksandrs
发明人： KALVINSH, Ivars , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir , CHERNOBROVIJS, Aleksandrs
CPC分类号： C07F3/02
摘要： The present invention concerns fine organic synthesis, particularly the method for preparing of substituted adamantylarylmagnesium halides. The known methods for preparing Ghgnard's reagent from substituted adamantylarylhalide give very low yeld of the desired product. Substituted adamantylarylhalides are active intermediates that by interacting with various electrophiles provide for a wide range of biologically active compounds. The aim of current invention was to develop a method for preparing substituted adamantylarylmagnesium halides. The aim was attained adding lithium chloride in the Grignard's reagent synthesis by acting on magnesium metal in dry tetrahydrofuran under argon by substituted adamantylarylhalide. It was demonstrated that adding lithium chloride to adamantylarylhalide within a range from 1:1 to 1:2 provides for stable high yield of the desired end product.
摘要翻译：本发明涉及精细的有机合成，特别是制备取代的金刚烷基芳基卤化镁的方法。从取代的金刚烷基卤化物制备Ghgnard试剂的已知方法给出所需产物的非常低的量。取代的金刚烷基卤化物是通过与各种亲电试剂相互作用提供广泛范围的生物活性化合物的活性中间体。本发明的目的是开发一种制备取代的金刚烷基芳基卤化镁的方法。目的是通过在氩气下通过取代的金刚烷基芳基卤化物在无水四氢呋喃中作用于镁金属，在格氏试剂合成中加入氯化锂。证明在1：1至1：2的范围内将氯化锂加入到金刚烷基卤化物中可提供所需最终产物的稳定高产率。

4. 发明申请

WO2008055843A1 A METHOD FOR PREPARING HIGH PURITY 3-CARBOXY-N,N,N-TRIMETHYL-1-PROPANAMINIUM HYDROXIDE INNER SALT 审中-公开
标题翻译：一种制备高纯度3-羧基-N，N，N-三甲基-1-丙酰胺氢氧化物内盐的方法
公开(公告)号：WO2008055843A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/061795
申请日：2007-11-01
申请人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , VARACHEVA, Larisa , PUGOVICHS, Osvalds
发明人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , VARACHEVA, Larisa , PUGOVICHS, Osvalds
IPC分类号： C07C227/40 , C07C227/18
CPC分类号： C07C227/18 , C07C229/12
摘要： The invention relates to preparation of high purity 3-carboxy-N,N,N-trimethyl-1-propanaminium hydroxide inner salt by saponification of 3-trimethylaminiumbutanoic acid ester salt and following precipitation of inorganic salts with carbon dioxide or sulfur dioxide.
摘要翻译：本发明涉及通过3-三甲基氨基丁酸酯盐皂化制备高纯度3-羧基-N，N，N-三甲基-1-丙铵氢氧化物内盐，随后用二氧化碳或二氧化硫沉淀无机盐。

5. 发明申请

WO2007104781A3 METHOD FOR MANUFACTURING OF R-ENANTIOMER OF N-CARBAMOYLMETHYL-4-PHENYL-2-PYRROLIDONE 审中-公开
公开(公告)号：WO2007104781A3
公开(公告)日：2007-09-20
申请号：PCT/EP2007/052428
申请日：2007-03-15
申请人： VEINBERG, Grigory , VORONA, Maksim , LEBEDEVS, Antons , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars
发明人： VEINBERG, Grigory , VORONA, Maksim , LEBEDEVS, Antons , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars
IPC分类号： C07D207/26
摘要： A process for the preparation of R -enantiomer of N-carbamoylmethyl-4-phenyl-2- pyrrolidone by the N-alkylation of 4( R )-phenyl-2-pyrrolidinone with haloacetic acid ester and the following conversion of intermediate N-alkoxycarbonylmethyl-4( R )- phenyl-2-pyrrolidinone into target product by the treatment with ammonia.

6. 发明申请

WO2007104780A2 METHOD OF PREPARATION AND USE OF PHARMACOLOGICALLY ACTIVE N-CARBAMOYLMETHYL-4(R)-PHENYL-2-PYRROLIDINONE 审中-公开
标题翻译：制备和使用药物活性的N-羰基甲基-4（R） - 苯基-2-吡咯烷酮的方法
公开(公告)号：WO2007104780A2
公开(公告)日：2007-09-20
申请号：PCT/EP2007/052424
申请日：2007-03-15
申请人： VEINBERG, Grigory , VORONA, Maksim , ZVEJNIECE, Liga , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars , KARINA, Ligita , DAMBROVA, Maija
发明人： VEINBERG, Grigory , VORONA, Maksim , ZVEJNIECE, Liga , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars , KARINA, Ligita , DAMBROVA, Maija
CPC分类号： C07D207/27 , A61K31/4015
摘要： The invention relates to the R -enantiomer of N-carbamoylmethyl-4-phenyl-2-pyrrolidinone ( R - Carphedon) of pharmacological value. The method of its preparation includes the N-alkylation of 4( R )-phenyl-2-pyrrolidinone with ethyl bromoacetate in the presence of a strong base and the treatment of intermediate N-ethoxycarbonylmethyl-4( R )-phenyl-2-pyrrolidinone with ammonia.
摘要翻译：本发明涉及N-氨基甲酰基甲基-4-苯基-2-吡咯烷酮（R-卡培芬）的R-对映异构体的药理学价值。其制备方法包括在强碱存在下4（R） - 苯基-2-吡咯烷酮与溴乙酸乙酯的N-烷基化反应，并处理中间体N-乙氧基羰基甲基-4（R） - 苯基-2-吡咯烷酮与氨。

7. 发明申请

WO2007096314A3 ENZYMATIC RESOLUTION OF RACEMIC 3-ARYL-4-AMINOBUTYRIC ACID 审中-公开
公开(公告)号：WO2007096314A3
公开(公告)日：2007-08-30
申请号：PCT/EP2007/051538
申请日：2007-02-18
申请人： VEINBERG, Grigory , VORONA, Maksim , LEBEDEVS, Antons , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars
发明人： VEINBERG, Grigory , VORONA, Maksim , LEBEDEVS, Antons , CHERNOBROVIJS, Aleksandrs , KALVINSH, Ivars
IPC分类号： C12P13/00 , C12P13/02 , C12P41/00
摘要： A process for the enzymatic resolution of racemic 3-aryl-4-aminobutyric acid ester into its R-and S-enantiomers, wherein aryl is represented by phenyl group (Phenybut) or p-chlorophenyl group (Baclofen) and ester group by saturated or unsaturated alkyl containing from 2 to 8 carbon atoms. The disclosed process includes the following steps: (1) selective cyclization of 3(S)-aryl-4-aminobutyric acid ester into 4(S)-aryl-2-pyrrolidinone using racemic 3-aryl-4-aminobutyric acid ester in water solution in the presence of -chymotrypsin; (2) acidification of reaction mixture to pH

8. 发明申请

WO2008015271A1 PYRAZOLOPYRIMIDINES, A PROCESS FOR THEIR PREPARATION AND THE USE AS A MEDICINE 审中-公开
标题翻译：吡唑并嘧啶，其制备方法和用作药物的方法
公开(公告)号：WO2008015271A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/058062
申请日：2007-08-03
申请人： MERZ PHARMA GMBH & CO. KGAA , DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
发明人： DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein R 1 represents chloro or bromo; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 independently represent e. g. hydrogen or C 1-6 -alkyl; R 8 represents a radical R 9 or a radical R 10 , whereby one of the two radicals R 8 denotes R 9 and the other radical R 8 denotes R 10 ; R 9 represents e. g. a phenyl or thiophen group, and R 10 represents e. g. hydrogen or methyl; are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：式（I）的取代的吡唑并嘧啶衍生物其中R 1表示氯或溴; R 2，R 3，R 4，R 5，R 6和R 6，和 R＆lt; 7＆gt;独立地表示e。 G。氢或C 1-6 - 烷基; R 8表示基团R 9或基团R 10，其中两个基团R 8中的一个表示 R 9和另一个基团R 8表示R 10; R 9表示e。 G。苯基或噻吩基，R 10代表e。 G。氢或甲基; 是有效的mGluR5调节剂，可用于预防急性和慢性神经障碍。

9. 发明申请

WO2007021164A1 PHARMACEUTICAL COMPOSITION ON BASIS OF REVERSE TRANSCRIPTASE INHIBITOR AND MELDONIUM 审中-公开
标题翻译：基于逆向转录酶抑制剂和药物的药物组合物
公开(公告)号：WO2007021164A1
公开(公告)日：2007-02-22
申请号：PCT/LV2006/000005
申请日：2006-08-08
申请人： GRINDEKS, joint stock company , KLUSHA, Vija , ISAJEVS, Sergejs , PUPURE, Jolanta , RUMAKS, Juris , GORDJUSHINA, Valentina , TAIVANS, Immanuels , KALVINSH, Ivars
发明人： KLUSHA, Vija , ISAJEVS, Sergejs , PUPURE, Jolanta , RUMAKS, Juris , GORDJUSHINA, Valentina , TAIVANS, Immanuels , KALVINSH, Ivars
IPC分类号： A61K31/15 , A61K31/7072 , A61K31/513 , A61P31/18
CPC分类号： A61K31/513 , A61K31/15 , A61K31/7072 , A61K2300/00
摘要： Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.
摘要翻译：含有临床有效量的逆转录酶抑制剂Zidovudine，拉米夫定或司他夫定之一的新型药物组合物以及药用赋形剂。已经证明，在这些药物组合物中包含Meldonium基本上降低了逆转录酶抑制剂的心脏和神经毒性。

10. 发明申请

WO2006037996A1 NOVEL CYCLIC AND ACYCLIC PROPENONES FOR TREATING CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的新型循环和ACYCLIC PROPENONES
公开(公告)号：WO2006037996A1
公开(公告)日：2006-04-13
申请号：PCT/GB2005/003817
申请日：2005-10-05
申请人： MERZ PHARMA GMBH & CO. KGAA , PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAUSS, Valerjans , TRIFANOVA, Dina , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja
发明人： PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAUSS, Valerjans , TRIFANOVA, Dina , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja
IPC分类号： A61K31/121 , A61K31/122 , A61K31/343 , A61K31/353 , A61K31/404 , A61K31/47 , C07C49/255 , C07C49/553 , C07C49/533 , C07D209/32 , C07D215/14 , C07D307/80 , C07D311/58
CPC分类号： C07D307/80 , C07C45/74 , C07C49/255 , C07C49/553 , C07C49/577 , C07C49/84 , C07D209/12 , C07D209/32 , C07D215/14 , C07D311/58 , C07D319/18 , C07D401/04 , C07D407/06 , C07D413/04 , C07D417/04 , C07D491/04
摘要： The invention relates to novel cyclic and non-cyclic propenone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are useful as medicaments.
摘要翻译：本发明涉及新的环状和非环状丙烯酮衍生物及其药学上可接受的盐。本发明还涉及制备这些化合物的方法。本发明的化合物可用作药物。

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