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91. 发明公开

EP2208726A1 Cyclic amide derivatives, and their production and use as antithrombotic agents 有权
标题翻译： Cyclische Amidderivate und deren Herstellung und Verwendung als Antithrombosemittel
公开(公告)号：EP2208726A1
公开(公告)日：2010-07-21
申请号：EP10161428.7
申请日：2005-05-20
申请人： Takeda Pharmaceutical Company Limited
发明人： KUBO, Keiji , IMAEDA, Yasuhiro
IPC分类号： C07D211/76 , C07D401/04 , C07D413/04 , C07D403/04 , C07D417/04 , A61K31/506 , A61K31/5377 , A61K31/45 , A61P7/02
CPC分类号： C07D211/76 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I):

wherein R 1 represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent chain hydrocarbon group, a represents 0, 1, or 2, X 1 represents an optionally substituted lower alkylene or an optionally substituted lower alkenylene, Y 1 represents - C(O)-, -S(O)- or -S(O) 2 -, A represents a piperazine ring which may be further substituted or a piperidine ring which may be further substituted, X 2 represents a bond or an optionally substituted lower alkylene, Y 2 represents -C(O)-, -S(O)-, -S(O) 2 - or -C(=NR 7 )-, X 3 represents an optionally substituted C 1-4 alkylene or an optionally substituted C 2-4 alkenylene, Z 3 represents -N(R 4 )-, -O- or a bond, Z 1 represents -C(R 2 )(R 2' )-, -N(R 2 )-, etc., and Z 2 represents - C(R 3 )(R 3' )-, -N(R 3 )-, etc., or a salt thereof.
摘要翻译：本发明提供用作治疗血栓形成的药物的环状酰胺衍生物，其由式（I）表示：其中R 1表示任选取代的环状烃基或任选取代的杂环基，W表示键或任选地取代的二价链烃基，a表示0,1或2，X 1表示任选取代的低级亚烷基或任选取代的低级亚烯基，Y 1表示-C（O） - ， - S（O） - 或-S（ O）2 - ，A表示可以被进一步取代的哌嗪环或可进一步被取代的哌啶环，X 2表示键或任选取代的低级亚烷基，Y 2表示-C（O） - ， - S（ O） - ， - （O）2 - 或-C（= NR 7） - ，X 3表示任选取代的C 1-4亚烷基或任选取代的C 2-4亚烯基，Z 3表示-N ） - ，-O-或键，Z 1表示-C（R 2）（R 2'） - ， - N（R 2） - 等，Z 2表示-C（R 3）（R 3 '） - ， - N（R 3 ） - 等，或其盐。

92. 发明公开

EP2116529A1 PROCESS FOR PRODUCTION OF AMIDE OR LACTAM 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES AMIDS ODER LACTAMS
公开(公告)号：EP2116529A1
公开(公告)日：2009-11-11
申请号：EP07859896.8
申请日：2007-12-20
申请人： Daicel Chemical Industries, Ltd.
发明人： ISHII, Yasutaka , IWAHAMA, Takahiro , NAKANO, Tatsuya
IPC分类号： C07D201/04 , C07C231/10 , C07D211/76 , C07D223/10 , C07D225/02 , C07D227/087
CPC分类号： C07C231/10 , C07D201/04 , C07D211/76 , C07D223/10 , C07D225/02 , C07D227/087
摘要： Disclosed is a process for producing an amide or lactam in a high yield in a simple manner by allowing a rearrangement reaction of an oxime compound to proceed without causing large amounts of by-products such as ammonium sulfate.
Specifically, disclosed is a process for producing an amide or lactam in which a corresponding amide or lactam is produced by rearranging an oxime compound in the presence of a compound containing a structure represented by following Formula (1):

-Z-X (1)

wherein Z represents P, N, S, B, or Si atom; and X represents a leaving group, where Z is bonded to one or more atoms or groups besides X. In the process, X may be a halogen atom.
摘要翻译：公开了通过使肟化合物的重排反应进行而不产生大量的副产物如硫酸铵，以简单的方式生产酰胺或内酰胺的方法。具体地，公开了一种制备酰胺或内酰胺的方法，其中通过在含有下式（1）表示的结构的化合物的存在下重排肟化合物来制备相应的酰胺或内酰胺：€ƒ€ƒ€ ƒ€ƒ€ƒ€ƒ-ZX€ƒ€ƒ€ƒ€ƒ（1）其中Z表示P，N，S，B或Si原子; 并且X表示离去基团，其中Z键合到除X以外的一个或多个原子或基团。在该过程中，X可以是卤素原子。

93. 发明公开

EP2076491A1 NEW BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS 有权
标题翻译： NEW苯甲酰胺衍生物作为缓激肽拮抗剂的
公开(公告)号：EP2076491A1
公开(公告)日：2009-07-08
申请号：EP07824994.3
申请日：2007-10-27
申请人： Richter Gedeon Nyrt.
发明人： VÁGÓ, István , BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VASTAG, Mónika
IPC分类号： C07D207/08 , A61K31/18 , A61P29/00 , C07D207/26 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/58 , C07D211/62 , C07D211/68 , C07D211/76 , C07D219/06
CPC分类号： C07D295/185 , C07D207/08 , C07D207/26 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/58 , C07D211/62 , C07D211/68 , C07D211/76 , C07D219/06 , C07D223/10 , C07D239/42 , C07D241/06 , C07D241/20 , C07D243/08 , C07D279/12 , C07D295/20 , C07D295/26 , C07D307/14 , C07D307/24 , C07D307/68 , C07D401/06 , C07D487/08
摘要： The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I), wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

94. 发明公开

EP2032527A1 VERFAHREN ZUR ALKENYLIERUNG VON CARBONSÄUREAMIDEN 审中-公开
标题翻译：甲酰胺的方法烯基
公开(公告)号：EP2032527A1
公开(公告)日：2009-03-11
申请号：EP07729832.1
申请日：2007-06-04
申请人： BASF SE
发明人： STAFFEL, Wolfgang , KESSINGER, Roland , HENKELMANN, Jochem , KÄSHAMMER, Stefan
IPC分类号： C07C231/12 , C07C233/03 , C07D207/26 , C07D209/48 , C07D211/76
CPC分类号： C07C231/12 , C07D207/267 , C07D209/48 , C07D223/10 , C07C233/03
摘要： The present invention relates to a process for preparing N-(1-alkenyl)carboxamides of the formula I, wherein a carboxamide of the formula II is reacted with an alkyne of the formula III in the presence of a catalyst which is selected from carbonyl complexes, the halides or oxides of rhenium, of manganese, of tungsten, of molybdenum, of chromium and of iron.

95. 发明公开

EP1978012A1 Alternative synthesis of renin inhibitors and intermediates thereof 审中-公开
标题翻译：替代合成铼仁诺n和Zwischenprodukte daraus
公开(公告)号：EP1978012A1
公开(公告)日：2008-10-08
申请号：EP08158568.9
申请日：2005-08-30
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： Sedelmeier, Gottfried , Mickel, Stuart, John , Rueeger, Heinrich
IPC分类号： C07C53/128 , C07D413/04 , C07D207/38 , C07C271/10 , C07D307/32 , C07D211/76
CPC分类号： C07D207/26 , C07C271/16 , C07C271/22 , C07D211/76 , C07D307/33
摘要： The present invention relates to synthetic routes to prepare a compound of the formula

wherein R 1 is halogen, C 1-6 halogenalkyl, C 1-6 alkoxy-C 1-6 alkyloxy or C 1-6 alkoxy-C 1-6 alkyl; R 2 is halogen, C 1-4 alkyl or C 1-4 alkoxy; R 3 and R 4 are independently branched C 3-6 alkyl; and R 5 is cycloalkyl, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkanoyloxy-C 1-6 alkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, C 1-6 dialkylamino-C 1-6 alkyl, C 1-6 alkanoylamino-C 1-6 alkyl, HO(O)C-C 1-6 alkyl, C 1-6 alkyl-O-(O)C-C 1-6 alkyl, H 2 N-C(O)-C 1-6 alkyl, C 1-6 alkyl-HN-C(O)-C 1-6 alkyl or (C 1-6 alkyl) 2 N-C(O)-C 1-6 alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
摘要翻译：本发明涉及制备下式化合物的合成路线：其中R 1为卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R 2是卤素，C 1-4烷基或C 1-4烷氧基; R 3和R 4独立地为支链C 3-6烷基; R 5为环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1 -6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1-6烷酰基氨基-C 1-6烷基，HO（O）C 1-6烷基，C 1-6烷基 - O（O）C 1-6烷基，H 2 NC（O）-C 1-6烷基，C 1-6烷基-NH-C（O）-C 1-6烷基或（C 1-6烷基） 2 NC（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

96. 发明公开

EP1957448A1 SUBSTITUTED AZACYCLOALKANES USEFUL FOR TREATING CNS CONDITIONS 审中-公开
标题翻译：中枢神经系统莱顿SUITABLE SUBSITUIERTE氮杂环烷烃的治疗
公开(公告)号：EP1957448A1
公开(公告)日：2008-08-20
申请号：EP06809245.1
申请日：2006-11-10
申请人： Pfizer Products Inc.
发明人： BOYD, James Gorham , BUTLER, Todd William , O'NEILL, Brian Thomas
IPC分类号： C07D205/04 , C07D207/14 , C07D207/48 , C07D211/58 , C07D211/64 , C07D211/76 , A61K31/4439 , A61K31/4468 , A61K31/45 , A61P25/00 , C07D213/38 , C07D239/42 , C07D277/42 , C07D263/58 , A61K31/506
CPC分类号： C07D211/58 , C07D205/04 , C07D207/14 , C07D211/76 , C07D239/42 , C07D263/58 , C07D401/04 , C07D417/04
摘要： The invention relates to substituted azacycloalkaπe compounds useful in treating conditions of the Central Nervous System (CNS); a pharmaceutical composition comprising same; a method of treating such conditions and of treating conditions in which inhibition of beta-secretase is indicated.

97. 发明公开

EP1950211A1 PROCESS FOR PRODUCTION OF CINNAMAMIDE DERIVATIVE 审中-公开
标题翻译：生产肉桂酰胺衍生物的方法
公开(公告)号：EP1950211A1
公开(公告)日：2008-07-30
申请号：EP06832861.6
申请日：2006-11-17
申请人： Eisai R&D Management Co., Ltd.
发明人： SHIMOMURA, Naoyuki , SATO, Nobuaki , KANEKO, Toshihiko , TAKAISHI, Mamoru , WAKASUGI, Kazunori , YOSHIKAWA, Seiji , NISHIKAWA, Yoshihiro , NAKAMURA, Taiju , FUKUYAMA, Tohru
IPC分类号： C07D401/10 , A61K31/4439 , A61P25/28 , A61P43/00 , C07D211/76 , C07D211/78 , C07D233/61
CPC分类号： C07D401/10
摘要： A compound (8) represented by the formula: (8)

wherein R 1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3)

wherein R 1 and n are as defined above; and Q represents a single bond or -CH(Y)- where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.
摘要翻译：由式（8）表示的化合物（8）其中R1表示可以具有取代基的6至14元芳族烃环基团; （3）表示的化合物（3）（其中R1和n如上所定义）反应，可以高效地制备n为0至2的化合物。和Q代表单键或-CH（Y） - ，其中Y代表氢原子或C1-6烷基]与3-甲氧基-4-（4-甲基-1H-咪唑-1-基）苯甲醛在基地的存在。

98. 发明授权

EP1830840B1 CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权
标题翻译：作为11-β-羟基类固醇脱氢酶1抑制剂的环烷基内酰胺衍生物
公开(公告)号：EP1830840B1
公开(公告)日：2008-07-16
申请号：EP05854586.4
申请日：2005-12-16
申请人： ELI LILLY AND COMPANY
发明人： AICHER, Thomas, Daniel , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan
IPC分类号： A61K31/4015 , C07D207/27 , C07D211/76 , C07D401/06 , C07D403/06 , C07D495/04 , A61K31/4025 , A61K31/4412 , A61P3/04
CPC分类号： C07D207/26 , C07D405/06 , C07D409/06 , C07D409/14 , C07D495/04
摘要： The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from -(C1-C4) alkylene-, -S-, -CH(OH)-, or -O-; A is methylene, -S-, -O-, or -NH-; and the other substituents are as defined in the claims.
摘要翻译：本发明提供了用作11-β羟基类固醇脱氢酶1的有效和选择性抑制剂的式I化合物。本发明还提供了药物组合物，其包含式I化合物或其药用盐和药学上可接受的载体，稀释剂或赋形剂。另外，本发明提供了用于治疗代谢综合征，糖尿病，高血糖症，肥胖症，高血压，高脂血症，与高血糖症相关的其他症状和相关病症的式I化合物的组合物。式（I）其中，R 0是（II）或（III）G 1是亚甲基或亚乙基; L是选自 - （C 1 -C 4）亚烷基 - ， - S - ， - CH（OH） - 或-O-的二价连接基团; A是亚甲基，-S - ， - O-或-NH-; 而其他取代基如权利要求中所定义。

99. 发明公开

EP1640373A4 PROCESS FOR PRODUCING 3-ACYLAMINOBENZOFURAN-2-CARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：用于生产3- ACYLAMINOBENZOFURAN -2-羧酸衍生物
公开(公告)号：EP1640373A4
公开(公告)日：2008-07-02
申请号：EP04746957
申请日：2004-06-29
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： SEKI MASAHIKO , YOSHIDA SHIN-ICHI , YAGI NOBUHIRO , HATSUDA MASANORI , KIMURA MAYUMI , KONDO KAZUHIKO
IPC分类号： C07D405/14 , C07C209/04 , C07C211/45 , C07C227/16 , C07C229/48 , C07C253/14 , C07C255/49 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/81 , C07D213/85 , C07D265/32 , C07D307/85 , C07D333/62 , C07D333/68 , C07D405/12 , C07D413/14
CPC分类号： C07D405/14 , C07C253/14 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/85 , C07D265/32 , C07D295/192 , C07D333/62 , C07D333/68 , C07D405/12 , C07C255/50 , C07C255/51 , C07C255/53 , C07C255/54 , C07C255/56 , C07C255/57
摘要： An excellent process for efficiently producing a benzofuran derivative or pyridofuran derivative or a pharmacologically acceptable salt of either, the derivatives being represented by the general formula [I]: [I] (wherein X represents -N= or -CH=; R1 represents hydrogen, halogeno, lower alkyl, lower alkoxy, cyano, or amino optionally substituted by lower alkyl; ring A represents a nitrogenous heterocyclic group; ring B represents an optionally substituted benzene ring or pyridine ring; and R3 represents hydrogen or lower alkyl). The derivatives are useful as an inhibitor against an activated blood coagulation factor X.

100. 发明公开

EP1558606A4 LACTAM-CONTAINING DIAMINOALKYL, BETA-AMINOACIDS, ALPHA-AMINOACIDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 审中-公开
标题翻译： LACTAMHALTIGE DIAMINOALKYLVERBINDUNGEN，BETA-AMINOSUUREN，ALPHA-氨基糖苷衍生物DAVON ALSFAKTOR-XA-INHIBITOREN
公开(公告)号：EP1558606A4
公开(公告)日：2008-05-07
申请号：EP03773077
申请日：2003-10-01
申请人： SQUIBB BRISTOL MYERS CO
发明人： QIAO JENNIFER X , HAN WEI
IPC分类号： C07D409/02 , A61K31/44 , A61K31/445 , A61P7/02 , C07D211/76 , C07D211/80 , C07D213/64 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12
CPC分类号： C07D213/64 , C07D211/76 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present application describes lactam-containing diaminoalkyl, b-aminoacids, a-aminoacids and derivatives thereof of Formula ( I): P-M-M1 or pharmaceutically acceptable salt forms thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式（I）的含内酰胺的二氨基烷基，β-氨基酸，α-氨基酸及其衍生物：P-M-M1或其药学上可接受的盐形式，其中M为直链核心。本发明化合物可用作胰蛋白酶样丝氨酸蛋白酶，特别是Xa因子的抑制剂。

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