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21. 发明公开

EP2289887A2 Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them 审中-公开
标题翻译：环氧羧基芥酸酰胺，叠氮和氨基烷醇洗涤剂Verfahren zur Herstellung von Alpha-Ketoamiden damit
公开(公告)号：EP2289887A2
公开(公告)日：2011-03-02
申请号：EP10011260.6
申请日：2001-06-29
申请人： SEIKAGAKU CORPORATION
发明人： Kobayashi, Nubuo , Koji, Tsuneo , Fujita, Takashi , Nishimura, Tomofumi , Hosoda, Akihiko
IPC分类号： C07D303/48 , C07D295/20 , C07D317/66 , C07D207/16 , C07C247/12 , C07C237/22 , C07C271/22 , C07C231/12 , C07C231/16
CPC分类号： C07D295/215 , C07C231/12 , C07C231/16 , C07C237/22 , C07C247/12 , C07C271/22 , C07C2601/14 , C07D207/16 , C07D295/18 , C07D303/46 , C07D303/48 , C07D317/66 , C07D405/12 , C07D407/12 , C07D413/12
摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide azide compounds represented by the following formula:

wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; and processes for preparing α-keto amide compound using the same.
摘要翻译：本发明提供制造中间体，其可以非常经济地和立体选择性地引入具有蛋白酶抑制活性的有用的± - 酮酰胺化合物，并提供由下式表示的叠氮化合物：其中R 1和R 2各自表示烷基，烯基，芳族烃基或杂环基; 以及使用其制备± - 酮酰胺化合物的方法。

22. 发明公开

EP1902014A2 GLUTAMATE AGGRECANASE INHIBITORS 审中-公开
标题翻译： GLUTAMAT，聚集蛋白聚糖酶缝边
公开(公告)号：EP1902014A2
公开(公告)日：2008-03-26
申请号：EP06787028.7
申请日：2006-07-11
申请人： Wyeth
发明人： SUM, Phaik-Eng , HOW, David, Brian , SABATINI, Joshua, James , XIANG, Jason, Shaoyun , IPEK, Manus , FEYFANT, Eric , MANSOUR, Tarek, Suhayl , TAM, Steve , SKOTNICKI, Jerauld, Stanley
IPC分类号： C07C237/22
CPC分类号： C07D213/82 , C07B2200/07 , C07C231/16 , C07C233/83 , C07C235/84 , C07C237/22 , C07C237/42 , C07C259/06 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2603/18 , C07C2603/74 , C07D213/38 , C07D239/26 , C07D239/42 , C07D277/30 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/85 , C07D317/58 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/38 , C07D409/04
摘要： The present invention relates to compounds of the formula (I), which are modulators of metalloproteinase activity. and pharmaceutically acceptable salts thereof, wherein W is -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, Or -C(O)NH-; R1 is phenyl, heteroaryl, biphenyl, bicyciic aryi, tricyclic aryl, bicyclic heteroaryl. or tricyclic heteroaryl, each optionally substituted with one or more of R5 or R6, and when Ri is substituted with more than one of R5 or Re, the substituents can be identical or different; R2 is hydrogen, (C1 -C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, -(CH2)nR11 , -OH, or -0-(C1-C6) alkyl; R3 is -CO2H, -CONH2, -CONHOH, -CONHSO2R7, tetrazole, -SO2NHR7, -SO3H, -PO(OH)NH2, -PO(OH)OR7, -CONHR7, -COOR7, an acid mimetic group, or a 5 or 6-membered heterocycloalkyl or heteroaryl containing 1 to 4 heteroatoms selected from O, N, S; R4 is -CO2H, -CONH2, -(CH2)nOR7, or -CONR9R10;
摘要翻译：本发明涉及金属蛋白酶活性的调节剂。

23. 发明公开

EP1295876A1 EPOXYCARBOXYLIC ACID AMIDES, AZIDES AND AMINO ALCOHOLS AND PROCESSES FOR PREPARATION OF ALPHA-KETO AMIDES BY USING THEM 审中-公开
标题翻译： EPOXYCARBONSÄURE-酰胺，叠氮化物和氨基醇和它们在用于生产α-酮酰胺
公开(公告)号：EP1295876A1
公开(公告)日：2003-03-26
申请号：EP01945730.8
申请日：2001-06-29
申请人： Seikagaku Corporation
发明人： KOBAYASHI, Nobuo , KOJI, Tsuneo , FUJITA, Takashi , NISHIMURA, Tomofumi , HOSODA, Akihiko
IPC分类号： C07D303/48 , C07D295/20 , C07D317/66 , C07D207/16 , C07C247/12 , C07C237/22 , C07C271/22 , C07C231/12 , C07C231/16 , C07M7/00
CPC分类号： C07D295/215 , C07C231/12 , C07C231/16 , C07C237/22 , C07C247/12 , C07C271/22 , C07C2601/14 , C07D207/16 , C07D295/18 , C07D303/46 , C07D303/48 , C07D317/66 , C07D405/12 , C07D407/12 , C07D413/12
摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae:

wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R 6 -O- or R 7 -N(R 8 )-; where R 6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 7 and R 8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R 4 and R 5 represent the same groups as R 7 and R 8 , respectively, and R 4 and R 5 optionally form a ring together; and X represents -O- or -N(R 9 )-, where R 9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R 4 or R 5 ,
and processes for preparing α-keto amide compound using the same.

24. 发明公开

EP1019363A1 PROCESS FOR THE PREPARATION OF AN INORGANIC SALT OF AN OPTICALLY ACTIVE PHENYLGLYCINE DERIVATIVE 失效
标题翻译：工艺生产光学活性的盐无机苯基甘氨酸衍生物
公开(公告)号：EP1019363A1
公开(公告)日：2000-07-19
申请号：EP97940490.2
申请日：1997-09-23
申请人： DSM N.V.
发明人： BOONEN, Jozef, Johannes, Catharina, Jacobus
IPC分类号： C07C231/16
CPC分类号： C07C231/16
摘要： Process for the preparation of an inorganic salt of an optically active phenylglycine derivative, in which a diastereoisomeric salt of the optically active phenylglycine derivative and an optically active acid is treated with a strong inorganic acid, in which at least a portion of the strong inorganic acid is added to a mixture containing an amount of the diastereoisomeric salt as a solid substance. The process according to the invention can be used with particular advantage in the preparation of an optically active phenylglycine derivative via an asymmetric transformation in which the reaction mixture obtained after the asymmetric transformation is treated with a strong inorganic acid without the formed, precipitated diastereoisomeric salt of the optically active phenylglycine derivative and the optically active acid being isolated and dissolved beforehand.

25. 发明公开

EP0757981A1 Verfahren zur Herstellung von racemischen Amino-Derivaten 失效
标题翻译：维他命Zur Herstellung von racmischen Amino-Derivaten
公开(公告)号：EP0757981A1
公开(公告)日：1997-02-12
申请号：EP96112061.5
申请日：1996-07-26
申请人： BAYER AG
发明人： Stelzer, Uwe, Dr. , Jansen, Johannes, Rudolf, Dr.
IPC分类号： C07C233/13 , C07C235/06 , C07B55/00 , C07C211/29 , C07C209/62
CPC分类号： C07C231/16 , C07C209/62 , C07C233/13
摘要： Nach einem neuen Verfahren lassen sich racemische Amino-Derivate der Formel
in welcher

R, R 1 , R 2 und n die in der Beschreibung angegebenen Bedeutungen haben,
herstellen, indem man optisch aktive Amide der Formel
in welcher

R 1 , R 2 , R 3 und n die in der Beschreibung angegebenen Bedeutungen haben,
mit starken Basen, gegebenenfalls in Gegenwart eines organischen Verdünnungsmittels umsetzt und gegebenenfalls die dabei entstehenden racemischen Amide
entweder

a) mit Wasser in Gegenwart einer Base oder einer Säure und gegebenenfalls in Gegenwart eines organischen Verdünnungsmittels umsetzt,
oder

b) sofern es sich bei den Verbindungen der Formel (Ia) um Amide handelt, in denen R 3 für Wasserstoff steht, mit Alkalimetallhydroxid oder Erdalkalimetallhydroxid umsetzt.
摘要翻译：制备方法。的外消旋胺衍生物。式（CH 2）n R 2）-NHR（I）包括处理式C * H（R 1）（（CH 2）n R 2）NH的光学活性酰胺 -C（= O）R 3（II）。与有机溶剂和选择。处理式CH（R 1）（（CH 2）n R 2）NH-C（= O）R 3（Ia）的外消旋酰胺，其中：a）在碱或酸选择。与有机溶剂; 或b）其中R 3 = H与碱金属氢氧化物或碱土金属氢氧化物反应。 n = 0-2; R 1，R 2 = opt。 substd。烷基，环烷基，环烯基，芳基或杂环基; 条件是R 1和R 2）

26. 发明公开

EP0716062A1 A method of preparing D-amino acid-N-(S)-alpha-alkylbenzylamide 失效
标题翻译： Ein Verfahren zur Herstellung von D-Aminosäure-N-（S）-α-烷基苄基酰胺
公开(公告)号：EP0716062A1
公开(公告)日：1996-06-12
申请号：EP95118471.2
申请日：1995-11-23
申请人： Ajinomoto Co., Inc.
发明人： Hijiya, Toyoto, c/o Central Research Laboratories , Mochizuki, Chiaki, c/o Central Research Lab. , Takemoto, Tadashi, c/o Central Research Lab.
IPC分类号： C07B55/00 , C07C231/20 , C07C237/06 , C07C257/06 , C07C251/24
CPC分类号： C07C237/06 , C07C231/16
摘要： The present invention relates to the conversion of L-amino acid amides to the corresponding D-amino acid amides.
An amide formed from an L-amino acid and an optically active (S)-α-alkylbenzylamine is subjected to dehydration condensation with an aryl aldehyde to form a Schiff's base, which is racemized at the amino acid moiety in the presence of a base to yield an N-allylidene-D-amino acid-(S)-amide. Furthermore, this racemization reaction solution is crystallized to obtain a less-soluble diastereomer N-allylidene-D-amino acid-(S)-amide by means of solid/liquid separation. The N-allylidene form is readily hydrolyzed into the amino acid-(S)-amide and the starting aldehyde.
摘要翻译：本发明涉及将L-氨基酸酰胺转化为相应的D-氨基酸酰胺。将由L-氨基酸和光学活性（S）-α-烷基苄基胺形成的酰胺与芳基醛进行脱水缩合以形成希夫碱，其在碱的存在下在氨基酸部分外消旋化，得到N-亚烯丙基-D-氨基酸 - （S） - 酰胺。此外，该外消旋化反应溶液结晶，通过固/液分离获得较不溶解的非对映体N-亚烯丙基-D-氨基酸 - （S） - 酰胺。 N-亚烯丙基形式容易水解成氨基酸 - （S） - 酰胺和起始醛。

27. 发明公开

EP0442585A1 Process for racemization of an optically active amino acid amide 失效
标题翻译： Verfahren zur Racemisierung von einem optisch aktivenAminosäure-Amid。
公开(公告)号：EP0442585A1
公开(公告)日：1991-08-21
申请号：EP91200307.6
申请日：1991-02-14
申请人： DSM N.V.
发明人： Boesten, Wilhelmus Hubertus Joseph
IPC分类号： C07C237/20 , C07C231/20 , C07B55/00
CPC分类号： C07B55/00 , C07C231/16 , C07C319/28
摘要： Process for the racemization of an optically active amino acid amide by reacting the amino acid amide with a carboxylic acid in the presence of a solvent, of water and of 0.5-4 equivalents of an aldehyde, calculated relative to the quantity of amino acid amide. Instead of an amino acid amide, the Schiff base of an amino acid amide and an aldehyde can also be used, in which case no extra aldehyde has to be added and the required quantity of water amounts to at least 1 equivalent relative to the quantity of Schiff base. This process gives fast racemization and a high yield of salt of the racemized amino acid amide and the carboxylic acid.
摘要翻译：通过使氨基酸酰胺与羧酸在溶剂存在下，水和相对于氨基酸酰胺的量计算的0.5-4当量醛的反应使光学活性氨基酸酰胺外消旋化的方法。代替氨基酸酰胺，也可以使用氨基酸酰胺和醛的席夫碱，在这种情况下不需要加入额外的醛，所需量的水相对于席夫基地。该方法快速消旋化，外消旋化氨基酸酰胺和羧酸的盐产率高。

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