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2. 发明公开

EP2289887A3 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：环氧羧酸酰胺，叠氮化物和氨基醇以及通过使用它们制备α-酮酰胺的方法
公开(公告)号：EP2289887A3
公开(公告)日：2011-07-06
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：本发明的目的在于提供能够非常经济且立体地选择性地得到具有蛋白酶抑制活性的有用的α-酮酰胺化合物的制造中间体，并且提供下式所示的叠氮化合物：其中R1和R2各自表示烷基，烯基，芳族烃基或杂环基团; 以及使用其制备α-酮酰胺化合物的方法。

3. 发明公开

EP0873290A1 VERFAHREN ZUR RACEMISIERUNG VON N-ACETYL-D(L)-$g(a)-AMINOCARBONSÄUREN 失效
标题翻译：过程对于N-乙酰基-D-（L）的外消旋 - G（A）氨基羧酸
公开(公告)号：EP0873290A1
公开(公告)日：1998-10-28
申请号：EP96942357.0
申请日：1996-12-05
申请人： Degussa Aktiengesellschaft
发明人： DRAUZ, Karlheinz , BOMMARIUS, Andreas , KARRENBAUER, Michael , KNAUP, Günter
IPC分类号： C07B55 , C07C231 , C07C233 , C07C319 , C07C323 , C12P13 , C12P41
CPC分类号： C12P41/007 , C07C231/16 , C07C323/59 , C12P13/12
摘要： With known methods of racemizing N-acetyl-D(L)-α-aminocarboxylic acids in the non-aqueous state by heating them to temperatures above room temperature, significant quantities of by-products are formed, especially acetyl dipeptides. By converting at least a proportion of the N-acetyl-D(L)-α-aminocarboxylic acids to corresponding N-acetyl-D(L)-α-aminocarboxylic acid salts before or during the heating, it is possible to increase the sojourn time of the educt which is to be racemized at higher temperatures without any evident increase in the quantity of by-product formed (in particular acetylated dipeptides). Also disclosed is the production of optically active amino acids by enzymatic splitting of racemic compounds.

4. 发明公开

EP2825525A1 NEW POLYMORPHIC FORM OF A LONG-ACTING BETA-2 ADRENOCEPTOR AGONIST 有权转让
标题翻译： NEUE POLYMORPHE FORM EINES BETA-2-ADRENOREZEPTOR-AGONISTEN MIT LANGER WIRKUNGSDAUER
公开(公告)号：EP2825525A1
公开(公告)日：2015-01-21
申请号：EP13711936.8
申请日：2013-03-12
申请人： Laboratorios Lesvi S.L.
发明人： BENET-BUCHHOLZ, Jordi , CERÓN BERTRAN, Jordi , FREIXAS PASCUAL, Gloria , DALMASES BARJOAN, Pere , NAVARRO MUÑOZ, Isabel
IPC分类号： C07C231/24 , C07C233/43 , A61K31/16 , A61P11/08
CPC分类号： C07C233/43 , C07B2200/13 , C07C231/16 , C07C231/24
摘要： New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterized by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.
摘要翻译：长效β-2肾上腺素受体激动剂的新多晶型形式提供了称为D型的新型多形态的酒石酸阿米美他醇，其特征在于以下至少之一：（i）粉末X射线衍射图在约6.8,13.3,13.6,3.8,14.1,18.2,18.7,20.0±0.2度2θ处具有峰; 或（ii）DSC热分析图，显示起始于约19-120℃的吸热峰，最大值为约129-131℃，随后为约137-138℃，最大值为放热峰。其中形式D的DSC热分析图具有在约168-170℃下起始的另外的吸热峰。还提供了制备新的多晶型物的方法及其用途及其制备中间体。

5. 发明公开

EP2289888A3 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：EP2289888A3
公开(公告)日：2011-07-13
申请号：EP10011261.4
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 amino alcohol compounds represented by the following formula:

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 9 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.
摘要翻译：本发明提供制造中间体，其可以被极端经济和立体选择性地引入具有蛋白酶抑制活性的有用的α-酮酰胺化合物，并提供由下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物： CHEM> 其中R 1和R 2各自表示烷基，烯基，芳族烃基或杂环基; R 3表示烷基，烯基，芳族烃基，杂环基，R 6 -O-或R 7 -N（R 8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，链烯基，芳香族烃基或杂环基，R 4和R 5表示与R 7和R 7相同的基团， 8>，R 4和R 5任选地形成环; 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，并且用相同的方法制备α-酮酰胺化合物。

6. 发明公开

EP1136466A3 Verfahren zur Racemisierung von N-Acylaminosäuren mittels Übergangsmetallkatalysatoren 审中-公开
标题翻译：由过渡金属催化剂的装置，用于N-酰基氨基酸外消旋化的方法
公开(公告)号：EP1136466A3
公开(公告)日：2003-06-04
申请号：EP01102629.1
申请日：2001-02-07
申请人： Aventis Research & Technologies GmbH & Co KG
发明人： Riermeier, Thomas, Dr. , Beller, Matthias, Prof. Dr. , Schichl, Daniel , Hateley, Martin, Dr.
IPC分类号： C07B55/00 , C07C231/16 , C07C233/47
CPC分类号： C07C231/16 , C07C233/47
摘要： Gegenstand der vorliegenden Erfindung ist ein Verfahren zur Racemisierung von N-Acy laminosäuren der allgemeinen Formel (I),R-CH(NR 1 COR 2 )CO 2 H bei dem in einem Lösungsmittel ein enantiomerenangereichertes Gemisch oder eine enantiomerenreine Verbindung der Formel (I), in Gegenwart eines Übergangsmetallsalzes, Übergangsmetallkomplexes oder Übergangsmetallkomplexsalzes oder eines Gemisches davon, enthaltend mindestens ein Element aus der Gruppe Fe, Ru, Os, Co, Rh, Ir, Ni, Pd, Pt, bevorzugt bei einer Temperatur von 10 - 150 °C umgesetzt wird.

7. 发明公开

EP2289888A2 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：EP2289888A2
公开(公告)日：2011-03-02
申请号：EP10011261.4
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 amino alcohol compounds represented by the following formula:

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 9 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.
摘要翻译：本发明提供制造中间体，其可以被极端经济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氨基醇化合物：其中R 1和R 2各自表示烷基，烯基，芳族烃基或杂环基; R 3表示烷基，烯基，芳香族烃基，杂环基，R 6 -O-或R 7 -N（R 8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，烯基，芳香族烃基或杂环基，R 4和R 5分别表示与R 7和R 8相同的基团，R 9和R 5任选地一起形成一个戒指并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，以及使用相同。

8. 发明公开

EP1366018A1 OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS 有权
标题翻译：作者（R）-2-芳基丙酸AS多形AND MONONUCLEATEN细胞的趋化性的抑制剂OMEGA氨基烷基
公开(公告)号：EP1366018A1
公开(公告)日：2003-12-03
申请号：EP02744900.8
申请日：2002-02-25
申请人： Dompé S.P.A.
发明人： ALLEGRETTI, Marcello , BERTINI, Riccardo , BERDINI, Valerio , BIZZARRI, Cinzia , CESTA, Maria, Candida , DI CIOCCIO, Vito , CASELLI, Gianfranco , COLOTTA, Francesco , GANDOLFI, Carmelo
IPC分类号： C07C233/40 , C07C233/51 , C07C233/44 , C07C235/34 , C07C235/70 , C07C237/22 , C07C279/12 , C07C281/16 , C07C231/02 , C07C231/16 , C07D211/06 , C07D211/58 , C07D233/48 , C07D239/14 , C07D295/13 , C07D471/08 , A61K31/16 , A61K31/395
CPC分类号： C07C233/51 , A61K31/165 , A61K31/198 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07B2200/07 , C07C231/02 , C07C231/16 , C07C233/40 , C07C233/44 , C07C235/34 , C07C235/70 , C07C235/78 , C07C237/20 , C07C237/22 , C07C279/12 , C07C281/16 , C07D211/04 , C07D211/58 , C07D233/24 , C07D233/46 , C07D295/13 , C07D451/04
摘要： (R) -2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (Leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of he chemataxis of neutrophils and monocites induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of nutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, rheumatoid arthritis and in the prevention and the treatment of injury caused by ischemia and reperfusion.

9. 发明公开

EP1136466A2 Verfahren zur Racemisierung von N-Acylaminosäuren mittels Übergangsmetallkatalysatoren 审中-公开
标题翻译： Verfahren zur Racemisierung von N-AcylaminosäurenmittelsÜbergangsmetallkatalysatoren
公开(公告)号：EP1136466A2
公开(公告)日：2001-09-26
申请号：EP01102629.1
申请日：2001-02-07
申请人： Aventis Research & Technologies GmbH & Co KG
发明人： Riermeier, Thomas, Dr. , Beller, Matthias, Prof. Dr. , Schichl, Daniel , Hateley, Martin, Dr.
IPC分类号： C07B55/00 , C07C231/16 , C07C233/47
CPC分类号： C07C231/16 , C07C233/47
摘要： Gegenstand der vorliegenden Erfindung ist ein Verfahren zur Racemisierung von N -Acylaminosäuren der allgemeinen Formel (I),
bei dem in einem Lösungsmittel ein enantiomerenangereichertes Gemisch oder eine enantiomerenreine Verbindung der Formel (I), in Gegenwart eines Übergangsmetallsalzes, Übergangsmetallkomplexes oder Übergangsmetallkomplexsalzes oder eines Gemisches davon, enthaltend mindestens ein Element aus der Gruppe Fe, Ru, Os, Co, Rh, Ir, Ni, Pd, Pt, bevorzugt bei einer Temperatur von 10 - 150 °C umgesetzt wird.
摘要翻译： N-酰基氨基酸的催化外消旋化是通过将溶剂中的对映体纯酸或富含对映异构体的混合物与金属为Fe，Ru的过渡金属盐，复合或复合盐进行处理来实现的， Os，Co，Rh，Ir，Ni，Pd和/或Pt。式（I）的N-酰基氨基酸的催化外消旋化是通过将溶剂中的对映体纯（I）或富含对映体的混合物（I）在过渡金属盐，复合或复合盐中进行的，其中金属是Fe，Ru，Os，Co，Rh，Ir，Ni，Pd和/或Pt。 R 1，R 2和R 2 = H，1-8C任选环烷基，2-18C烯基或炔基，4-14C芳基或杂芳基，其中（i）芳基含有5-，6-或7 含有0-3个杂原子如O，N或S的任选的芳环; 烷基，O-烷基，OCO-烷基，O-芳基，芳基，F，Cl，Br，I，OH，CF 3，NO 2中的至多6个其它取代基取代烷基和芳基，NO，Si（烷基）3，CN，COOH，CHO，SO 3 H，NH 2，NH-烷基，N-（烷基）2，PO（烷基）2，SO 2 - 烷基，SO-烷基，CF 3（sic） - 烷基，CONH 2，CO-烷基，COO-烷基，NHCOH，NHCOO-烷基，CO-芳基，COO-芳基，PO（芳基）2，PO 3 H 2，PO（O-烷基）2或SO 3 - 烷基，芳基分别为1-8℃和4-14℃。独立权利要求也包括用于（I）使上述方法的组合的N-酰基氨基酸的动态动力学外消旋物拆分与（a）用手性外消旋体拆分试剂进行对映选择性结晶或（b）用酰基转移酶的对映选择性去酰化。

10. 发明授权

EP0757981B1 Verfahren zur Herstellung von racemischen Amino-Derivaten 失效
标题翻译：一种用于制备外消旋氨基衍生物的方法
公开(公告)号：EP0757981B1
公开(公告)日：2000-02-16
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

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