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1. 发明申请

US20060002851A1 Methods for carbon isotope labeling synthesis by transition metal-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide 失效
标题翻译：通过使用叠氮化物和碳同位素一氧化碳通过异氰酸酯过渡金属促进羰基化的碳同位素标记合成方法
公开(公告)号：US20060002851A1
公开(公告)日：2006-01-05
申请号：US11086632
申请日：2005-03-22
申请人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
发明人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
IPC分类号： A61K51/00 , C07D25/08
CPC分类号： C07C333/04 , A61K51/04 , A61K51/0453 , A61K51/0455 , C07B59/00 , C07B2200/05 , C07C231/10 , C07C269/02 , C07C273/1827 , C07C333/08 , C07D205/08 , C07D207/263 , C07D207/267 , C07D213/64 , C07C233/07 , C07C271/28 , C07C275/28 , C07C275/64
摘要： Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
摘要翻译：提供了使用碳同位素标记的一氧化碳通过异氰酸酯过渡金属促进羰基化的方法和试剂。所得碳同位素标记的化合物可用作放射性药物，特别用于正电子发射断层扫描（PET）。还提供了用于PET研究的相关工具包。

2. 发明申请

US20030114664A1 Method for producing cyclic lactams 有权
标题翻译：环状内酰胺的制备方法
公开(公告)号：US20030114664A1
公开(公告)日：2003-06-19
申请号：US10257877
申请日：2002-10-17
发明人： Frank Ohlbach , Andreas Ansmann , Peter Bassler , Rolf-Hartmuth Fischer , Hermann Luyken , Stefan Maixner , Johann-Peter Melder
IPC分类号： C07D21/08 , C07D25/08 , C07D211/40 , C07D27/26
CPC分类号： C07D201/08 , C07D201/16
摘要： The invention relates to a method for producing cyclic lactams of formula (II) by reacting a compound (I) of formula (I) with water in the presence of an organic, liquid dilution agent in the liquid phase. In formula (II), n and m respectively can have the values 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of nnullm is at least 3, preferably at least 4 and R1 and R2 represent C1-C6 alkyl, C5-C7 cycloalkyl or C6-C12 aryl groups. In formula (I), R1, R2, m and n are defined as above and R represents nitrile, carboxylic acid amide and carboxylic acid groups. The inventive method is characterized in that a) compound (I) is reacted with water in the liquid phase in the presence of an organic, liquid dilution agent (III) to form a mixture (IV) containing a lactam (II) and said mixture (IV) is subjected to an aqueous treatment to obtain a two-phase system.
摘要翻译：本发明涉及在液相中有机液体稀释剂存在下使式（I）化合物（I）与水反应制备式（II）的环状内酰胺的方法。在式（II）中，n和m分别具有0,1,2,3,4,5,6,7,8和9的值，并且n + m的和至少为3，优选至少为4，并且 R1和R2表示C1-C6烷基，C5-C7环烷基或C6-C12芳基。在式（I）中，R 1，R 2，m和n如上定义，R代表腈，羧酸酰胺和羧酸基团。本发明的方法的特征在于：a）化合物（I）在液相中在有机液体稀释剂（III）的存在下与水反应，形成含有内酰胺（II）的混合物（IV），所述混合物（IV）进行水处理以获得两相体系。

3. 发明申请

US20020128253A1 Diphenylazetidinone derivatives, process for their preparation, medicaments comprising these compounds and their use 有权
公开(公告)号：US20020128253A1
公开(公告)日：2002-09-12
申请号：US10021044
申请日：2001-12-19
发明人： Heiner Glombik , Werner Kramer , Stefanie Flohr , Wendelin Frick , Hubert Heuer , Gerhard Jaehne , Andreas Lindenschmidt , Hans-Ludwig Schaefer
IPC分类号： A61K031/397 , C07D25/08
CPC分类号： C07D401/14 , C07D205/08 , C07D409/12
摘要： Compounds of the formula I, 1 in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

4. 发明申请

US20040010139A1 Process for the manufacture of optically active 3-substituted lactams by asymmetric hydrogenation of 3-alkylidenelactams 失效
标题翻译：通过3-亚烷基内酰胺的不对称氢化制备光学活性3-取代的内酰胺的方法
公开(公告)号：US20040010139A1
公开(公告)日：2004-01-15
申请号：US10391170
申请日：2003-03-18
发明人： William A. Nugent , Tai Yue
IPC分类号： C07D417/02 , C07D413/02 , C07D43/02 , C07D25/08 , C07D27/12 , C07D211/40
CPC分类号： C07D207/263 , C07D207/26 , C07D207/267 , C07D211/76 , C07D223/10 , C07D405/06
摘要： The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) 1 process, comprising: contacting a compound of formula (II): 2 with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrLnullXnull wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected from 3
摘要翻译：本发明一般涉及有效制备式（I）方法的光学活性3-取代内酰胺的方法，其包括：使式（II）化合物与氢在合适的压力下在铱络合物式（R 2）IrL + X其中L是螯合二烯，X是非配位阴离子，R 2选自

5. 发明申请

US20020128252A1 Diphenylazetidinone derivatives, process for their preparation, medicaments comprising these compounds and their use 有权
标题翻译：二苯基氮杂环丁酮衍生物，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US20020128252A1
公开(公告)日：2002-09-12
申请号：US10021028
申请日：2001-12-19
发明人： Heiner Glombik , Werner Kramer , Stefanie Flohr , Wendelin Frick , Hubert Heuer , Gerhard Jaehne , Andreas Lindenschmidt , Hans-Ludwig Schafer
IPC分类号： A61K031/397 , C07D25/08
CPC分类号： C07D401/14 , C07D205/08 , C07D409/12
摘要： Compounds of the formula I, 1 in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.
摘要翻译：其中R1，R2，R3，R4，R5和R6具有说明书中给出的含义的式I化合物及其生理上可接受的盐。该化合物适合用作例如降血脂药。

6. 发明授权

US06982251B2 Substituted 2-azetidinones useful as hypocholesterolemic agents 失效
公开(公告)号：US06982251B2
公开(公告)日：2006-01-03
申请号：US10166942
申请日：2002-06-11
申请人： Anima Ghosal , Shmuel Zbaida , Swapan K. Chowdhury , Robert M. Iannucci , Wenqing Feng , Kevin B. Alton , James E. Patrick , Harry R. Davis
发明人： Anima Ghosal , Shmuel Zbaida , Swapan K. Chowdhury , Robert M. Iannucci , Wenqing Feng , Kevin B. Alton , James E. Patrick , Harry R. Davis
IPC分类号： A61K31/7056 , A61K31/397 , A61K31/675 , C07H17/02 , C07D25/08
CPC分类号： A61K31/70 , A61K45/06 , C07H15/26
摘要： Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

7. 发明申请

US20030125544A1 Method for producing cyclic lactams 有权
标题翻译：环状内酰胺的制备方法
公开(公告)号：US20030125544A1
公开(公告)日：2003-07-03
申请号：US10258943
申请日：2002-10-29
发明人： Frank Ohlbach , Andreas Ansmann , Peter Bassler , Rolf-Hartmuth Fischer , Hermann Luyken , Stefan Maixner , Johann-Peter Melder
IPC分类号： C07D21/08 , C07D25/08 , C07D27/26 , C07D211/40
CPC分类号： C07D201/08
摘要： A process is provided for the preparation of cyclic lactams of formula (II): 1 in which n and m can each have the values 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of nnullm is at least 3, preferably at least 4, and R1 and R2 are C1-C6-alkyl, C5-C7-cycloalkyl or C6-C12-aryl groups, by reacting a compound (I) of the formula 2 in which R1, R2, m and n are as defined above and R are nullsicnull nitrile, carboxamide and carboxylic acid groups, with steam in the gas phase, wherein a) the compound (I) is reacted with steam in the gas phase with the addition, before or after the reaction, of an organic diluent (III) which exhibits a miscibility gap with water under specific quantity, pressure and temperature conditions, to give a mixture (IV) containing a lactam (II), b) the mixture (IV) is converted, before or after the separation of ammonia, under quantity, pressure and temperature conditions such that the diluent (III) and water are liquid and exhibit a miscibility gap, to give a two-phase system consisting of a phase (V) containing a higher proportion of diluent (III) than water, and a phase (VI) containing a higher proportion of water than diluent (III), c) the phase (V) is separated from the phase (VI), and d) the diluent (III) and optionally by-products selected from the group consisting of low-boiling component nullsicnull, high-boiling component nullsicnull and unreacted compound (I) are separated from the phase (V) to give a lactam (II).
摘要翻译：提供了制备式（II）的环状内酰胺的方法：其中n和m各自可以具有0,1,2,3,4,5,6,7,8和9以及n + m为至少3，优选至少4，并且R 1和R 2为C 1 -C 6 - 烷基，C 5 -C 7 - 环烷基或C 6 -C 12 - 芳基，其中R 1， R2，m和n如上所定义，R是具有气相中蒸汽的[sic]腈，甲酰胺和羧酸基团，其中a）化合物（I）与气相中的蒸汽反应，在反应之前或之后，在特定量，压力和温度条件下与水显示出混溶性间隙的有机稀释剂（III），得到含有内酰胺（II）的混合物（IV），b）混合物（IV）在数量，压力和温度条件下，在氨分离之前或之后转化，使得稀释剂（III）和水是液体并且表现出混溶性间隙，以产生两相系统的缺点含有比水更高比例的稀释剂（III）的相（V）的沉淀，以及含有比稀释剂（III）更高比例的水的相（VI），c）将相（V）从相（ VI）和d）稀释剂（III）和任选的选自低沸点组分[sic]，高沸点组分[sic]和未反应化合物（I）的副产物与相（V ），得到内酰胺（II）。

8. 发明申请

US20040002599A1 Substituted benzoycyclohexenones 失效
标题翻译：取代的苯并环己烯酮
公开(公告)号：US20040002599A1
公开(公告)日：2004-01-01
申请号：US10220711
申请日：2002-10-21
发明人： Klaus-Helmut Muller , Hans-Georg Schwarz , Stefan Herrmann , Dorothee Hoischen , Stefan Lehr , Otto Schallner , Mark Wilhelm Drewes , Peter Dahmen , Dieter Feucht , Rolf Pontzen , Akihiko Yanagi , Shinichi Narabu , Toshio Goto , Seishi Ito , Chieko Ueno
IPC分类号： C07D207/273 , C07D25/08 , C07D249/12 , C07D251/30 , C07D241/18
CPC分类号： C07D239/10 , A01N43/50 , A01N43/54 , A01N43/653 , A01N43/713 , C07D233/32 , C07D233/36 , C07D249/12 , C07D257/04
摘要： The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1 in which n, A, R1, R2, R3, R4, Y and Z are each as defined in the description, and also to processes for their preparation and to their use as herbicides.
摘要翻译：本发明涉及式（I）的新型取代的苯甲酰基环己酮，其中n，A，R 1，R 2，R 3，R 4，Y和Z各自如说明书中所定义，还涉及其制备方法和作为除草剂的用途。

9. 发明申请

US20030105028A1 Substituted 2-azetidinones useful as hypocholesterolemic agents 失效
标题翻译：用作降胆固醇药的取代的2-氮杂环丁酮
公开(公告)号：US20030105028A1
公开(公告)日：2003-06-05
申请号：US10166942
申请日：2002-06-11
申请人： Schering Corporation
发明人： Anima Ghosal , Shmuel Zbaida , Swapan K. Chowdhury , Robert M. Iannucci , Wenqing Feng , Kevin B. Alton , James E. Patrick , Harry R. Davis
IPC分类号： A61K031/7056 , A61K031/397 , A61K031/675 , C07H017/02 , C07D25/08
CPC分类号： A61K31/70 , A61K45/06 , C07H15/26
摘要： Hypocholesterolemic substituted 2-azetidinone compounds of the formula: 1 are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.
摘要翻译：公开了低胆固醇血症的取代的2-氮杂环丁酮化合物，以及通过施用所述化合物，含有它们的药物组合物以及取代的2-氮杂环丁酮降胆固醇和胆固醇生物合成抑制剂的组合来降低胆固醇的方法治疗和预防动脉粥样硬化。

10. 发明申请

US20020042508A1 Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same 失效
标题翻译：高度对映体纯的内酰胺取代的丙酸衍生物及其制备和使用方法
公开(公告)号：US20020042508A1
公开(公告)日：2002-04-11
申请号：US09957182
申请日：2001-09-20
发明人： Neil Warren Boaz , Sheryl Davis Debenham
IPC分类号： C07F009/576 , C07F009/572 , C07F009/568 , C07D25/08 , C07D27/26 , C07D211/40
CPC分类号： C07D203/04 , C07B2200/07 , C07C231/18 , C07C253/30 , C07C269/06 , C07C2601/02 , C07D205/08 , C07D207/27 , C07D211/76 , C07D223/10 , C07D225/02 , C07F9/5532 , C07F9/564 , C07F9/568 , C07F9/572 , C07F9/59 , Y02P20/52 , C07C233/47 , C07C233/83 , C07C233/84 , C07C255/60 , C07C271/22
摘要： The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
摘要翻译：本发明涉及高度对映体纯的内酰胺取代的丙酸衍生物及其制备和使用方法。本发明涉及多步合成来制备内酰胺化合物。在反应顺序的一个步骤中，进行内酰胺 - 酰胺的不对称氢化以产生最终可以转化成一系列药物化合物的中间体。本发明还考虑了多步合成中间体的原位合成，其为内酰胺化合物的总体合成提供经济优势。

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