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1. 发明授权

EP2123661B1 CHIRAL IRIDIUM AQUA COMPLEX AND METHOD FOR PRODUCING OPTICALLY ACTIVE HYDROXY COMPOUND BY USING THE SAME 有权
标题翻译：手性铱水络合物和方法制造光学活性的羟基使用THEREOF
公开(公告)号：EP2123661B1
公开(公告)日：2013-05-22
申请号：EP08710614.2
申请日：2008-01-29
申请人： Sumitomo Chemical Company, Limited , Carreira, Erick M.
发明人： CARREIRA, Erick M.
IPC分类号： C07F17/02 , C07C51/367 , C07C59/48 , C07C201/12 , C07C205/16 , C07C205/32 , C07C253/30 , C07C255/36 , C07F15/00 , C07B53/00 , C07B61/00
CPC分类号： C07F17/02 , C07B53/00 , C07B2200/07 , C07C205/16 , C07C205/26 , C07C205/32 , C07C253/30 , C07C255/36 , C07C255/37

2. 发明公开

EP2213657A4 PROCESS AND APPARATUS FOR PRODUCTION OF CYANOHYDRIN COMPOUND, AND PROCESS FOR PRODUCTION OF ALPHA -HYDROXYESTER COMPOUND 审中-公开
标题翻译：方法和设备用于生产CYANOHYDRINVERBINDUNG及其制造方法的α-羟基酯
公开(公告)号：EP2213657A4
公开(公告)日：2012-01-18
申请号：EP08841132
申请日：2008-10-21
申请人： NIPPOH CHEMICALS
发明人： KINOSHITA YUICHIRO , FUJIWARA NAOKI , NAKAGAWA KAZUYA , MIDORIKAWA KOJI
IPC分类号： C07C67/08 , C07B61/00 , C07C67/22 , C07C69/675 , C07C253/00 , C07C255/16 , C07C255/36
CPC分类号： C07C253/00 , C07C67/22 , C07C69/675 , C07C255/16 , C07C255/36
摘要： A process according to the present invention for producing a cyanohydrin compound flow-reacts a carbonyl compound with hydrogen cyanide in the presence of a catalyst, and can therefore reduce the residence time. This makes it possible to reduce the period of time over which the resulting cyanohydrin compound is exposed to an unreacted portion of the carbonyl compound. As a result, the resulting cyanohydrin compound can be prevented from reacting with the unreacted portion. This makes it possible to produce the cyanohydrin compound in good yield. That is, the process according to the present invention for producing a cyanohydrin compound produces a cyanohydrin compound in good yield from a carbonyl compound and hydrogen cyanide.

3. 发明授权

EP1465863B1 POTASSIUM CHANNEL MODULATORS 有权
标题翻译：钾通道调节剂
公开(公告)号：EP1465863B1
公开(公告)日：2008-07-09
申请号：EP03729413.9
申请日：2003-01-06
申请人： NeuroSearch A/S
发明人： GOULIAEV, Alex, Haahr , SLÖK, Frank, Abildgaard , TEUBER, Lene , DEMNITZ, Joachim
IPC分类号： C07C323/00 , C07C317/00 , C07C271/06 , C07C333/02 , C07C227/22 , C07D213/28 , C07D295/16 , C07F9/02 , A61K31/27 , A61K31/66 , A61K31/426 , A61K31/395 , A61P37/06
CPC分类号： C07D213/30 , C07C233/11 , C07C255/35 , C07C255/36 , C07C255/37 , C07C255/40 , C07C255/41 , C07C271/12 , C07C313/06 , C07C317/10 , C07C317/12 , C07C317/14 , C07C323/52 , C07C333/04 , C07C2601/08 , C07C2601/14 , C07D213/32 , C07D213/70 , C07D213/89 , C07D233/64 , C07D233/84 , C07D263/32 , C07D277/24 , C07D277/26 , C07D277/32 , C07D277/36 , C07D295/108 , C07D295/20 , C07D295/26 , C07D401/12 , C07D417/12 , C07F9/4056 , C07F9/582 , C07F9/6539 , C07F9/65742
摘要： This invention relates to novel compounds characterized by the general Formula (I) any of its enantiomers or any mixture of its enantiomers, or a pharmaceutically acceptable salt thereof, or an N-oxide thereof, useful as potassium channel modulators. More specifically the invention provides chemical compounds useful as modulators of SKCa and/or IKCa channels.

4. 发明公开

EP1902015A1 PROCESS FOR THE PREPARATION OF 1-[CYANO (4-HYDROXYPHENYL)METHYL]CYCLOHEXANOL COMPOUNDS 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON 1- [氰基（4-羟基苯基）甲基]环己烷二醇
公开(公告)号：EP1902015A1
公开(公告)日：2008-03-26
申请号：EP06762178.9
申请日：2006-06-26
申请人： Wyeth
发明人： MITZEL, Frieder , WEBER, Beat, Theodor , MARTI, Hans-Rudolf , HALDIMANN, Richard
IPC分类号： C07C253/30
CPC分类号： C07C253/30 , C07C2601/14 , C07C255/36
摘要： Process for the preparation of 1-[cyano (phenyl) methyl] cyclohexanol compounds of general formula (I) in which R1 is hydrogen, (C1-4) alkyl or (C1-4) alkoxy, wherein a compound of general formula (II) in which R1 is as defined above, is reacted with cyclohexanone, the reaction being carried out in the presence of an organic or inorganic base, and this organic or inorganic base being present in the reaction mixture in at least an equimolar amount, based on the amount of the compound of general formula (II) .
摘要翻译：制备通式（I）的1- [氰基（苯基）甲基]环己醇化合物的方法：其中R 1是氢，（C 1-4）烷基或（C 1-4 1-4）烷氧基，其中通式（II）的化合物（其中R 1定义如上）与环己酮反应，反应在有机或无机碱的存在下进行，并且该有机或无机碱以至少等摩尔量存在于反应混合物中，基于通式（II）的化合物的量。

5. 发明授权

EP0748219B1 COMPOUNDS FOR THE TREATMENT OF DISORDERS RELATED TO VASCULOGENESIS AND/OR ANGIOGENESIS 失效
标题翻译：化合物与血管生成和/或血管相关疾病的治疗。
公开(公告)号：EP0748219B1
公开(公告)日：2005-04-06
申请号：EP95910239.3
申请日：1995-02-09
申请人： Sugen, Inc. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
发明人： GAZIT, Aviv , LEVITZKI, Alexander , APP, Harald , TANG, Cho, Peng , MCMAHON, Gerald, M.
IPC分类号： A61K31/24 , A61K31/42 , A61K31/275 , A61K31/415 , A61K31/495 , C07C211/45 , C07C255/01 , C07D209/18 , C07D231/38 , C07D241/36 , C07C255/41 , C07D239/93
CPC分类号： C07D487/04 , A61K31/235 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/495 , A61K31/502 , A61K31/505 , A61K31/517 , A61K31/535 , A61K38/00 , C07C229/60 , C07C255/36 , C07C255/40 , C07C255/41 , C07C255/66 , C07C317/46 , C07C327/44 , C07D209/18 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/44 , C07K14/71 , C07K16/2863 , C07K2319/32 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/5064 , G01N33/5091 , G01N33/6893 , G01N2333/71 , G01N2500/04
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

6. 发明公开

EP1378570A1 Flk-1 is a receptor for vascular endothelial growth factor 失效
标题翻译：显性阴性膜膜结合蛋白Flk-1 Rezeptor desvaskulärenEndothelzellen-Wachstumsfaktors VEGF
公开(公告)号：EP1378570A1
公开(公告)日：2004-01-07
申请号：EP03009148.2
申请日：1993-11-15
申请人： Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
发明人： Ullrich, Axel, Prof. Dr. , Risau, Werner, Prof. Dr. , Millauer, Birgit, Ph.D.
IPC分类号： C12N15/12 , C12P21/08 , C12N15/86 , C12Q1/68 , G01N33/567 , A61K38/00 , C12N15/62 , C07K14/71
CPC分类号： G01N33/5064 , A61K31/235 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/495 , A61K31/502 , A61K31/505 , A61K31/517 , A61K31/535 , A61K38/00 , C07C229/60 , C07C255/36 , C07C255/40 , C07C255/41 , C07C255/66 , C07C317/46 , C07C327/44 , C07D209/18 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/44 , C07D487/04 , C07K14/71 , C07K16/2863 , C07K2319/32 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/6893 , G01N2333/71 , G01N2500/04
摘要： The present invention relates to the use of ligands for the Flk-1 receptor for the modulation of angiogenesis and vasculogenesis. The invention is based, in part, on the demonstration that Flk-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of Flk-1. These results indicate a major role for Flk-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express Flk-1 and the uses of expressed Flk-1 to evaluate and screen for drugs and analogs of VEGF involved in Flk-1 modulation by either agonist or antagonist activities is described. The invention also relates to the use of Flk-1 ligands, including VEGF agonists and antagonists, in the treatment of disorders, including cancer, by modulating vasculogenesis and angiogenesis.
摘要翻译：本发明涉及用于Flk-1受体的配体用于调节血管生成和血管发生的用途。本发明部分基于Flk-1酪氨酸激酶受体表达与内皮细胞相关的证据，以及作为Flk-1的高亲和力配体的血管内皮生长因子（VEGF）的鉴定。这些结果表明Flk-1在血管发生和血管发生过程中在信号系统中的主要作用。描述表达Flk-1的宿主细胞的工程和表达Flk-1的用途以通过激动剂或拮抗剂活性来评价和筛选参与Flk-1调节的VEGF和类似物。本发明还涉及Flk-1配体，包括VEGF激动剂和拮抗剂在治疗疾病，包括癌症中的用途，通过调节血管发生和血管生成。

7. 发明公开

EP1340754A1 Composés hétérocycliques substitués, procédé pour leur préparation et compositions pharmaceutiques les contenant 失效
标题翻译：取代的杂环化合物，它们的制备方法和含有它们的药物组合物
公开(公告)号：EP1340754A1
公开(公告)日：2003-09-03
申请号：EP03012771.6
申请日：1996-01-30
申请人： SANOFI-SYNTHELABO
发明人： Emonds-Alts, Xavier , Grossriether, Isabelle , Gueule, Patrick , Proietto, Vincenzo , Van Broeck, Didier
IPC分类号： C07D413/06 , C07D401/06 , C07D413/12 , C07D265/10 , C07D265/30 , C07D265/32 , C07D453/02 , C07D309/12 , C07D263/38 , C07D405/12 , C07C219/22 , C07C255/36 , C07C233/18 , C07C255/42 , C07C271/22 , C07C215/30 , A61K31/445 , A61P11/00
CPC分类号： C07D453/02 , C07C215/28 , C07C215/30 , C07C219/22 , C07C233/18 , C07C255/36 , C07C255/42 , C07C255/43 , C07C271/22 , C07D263/38 , C07D265/32 , C07D309/12 , C07D401/06 , C07D413/06 , C07D413/14 , C07D417/14 , Y02P20/55
摘要： L'invention a pour objet des composés de formule :
dans laquelle :

A représente un radical bivalent choisi parmi :

A 1 ) -O-CO-
A 2 ) -CH 2 -O-CO-
A 3 ) -O-CH 2 -CO-
A 4 ) -O-CH 2 -CH 2 -
A 5 ) -N(R 1 )-CO-
A 6 ) -N(R 1 )-CO-CO-
A 7 ) -N(R 1 )-CH 2 -CH 2 -
A 8 ) -O-CH 2 -

dans lesquels:

R 1 représente un hydrogène ou un (C 1 -C 4 )alkyle ;
Am représente un hétérocycle azoté.

APPLICATION : Antagonistes des récepteurs des neurokinines
摘要翻译：式（I）及其酸加成盐的杂环化合物是新的。 A =（A1）-O-CO-; （A2）-CH 2 O - CO; （A3）-O-CH 2 -CO-; （A4）-O-CH2-CH2-; （A5）-N（R 1）-CO-; （A6）-N（R 1）-CO-CO-; （A7）-N（R1）-CH2-CH2-; 或（A8）-O-CH2-; R1 = H或1-4C烷基; M = 2或3; AR1 =苯基选择。 substd。由一个或多个卤素，OH，1-4C烷基，1-4C烷氧基，CF 3或甲基dioxyl的; 噻吩，噻吩基，萘基，咪唑基或吡啶基，所有的选择。 substd。被一个卤素; 吲哚基选择。 N-二substd。通过1-4C烷基或苄基; 或联苯基; T = -CH 2 -Z; -CH（C6H5）2，-C（C 6 H 5）3，或，当A = A4，A7或A8，T可以是另外-CO-B-Z; B =直接键或亚甲基; Z =选择。 substd。单 - ，二 - 或三 - 环芳族或杂芳族GP。上=一组M1-AM4; J1 = AR2-N（R 2）-CH中，Ar 2（CH 2）N-C（R 3）或R14-C（R3）; AR2 =吡啶基; 苯基选择。 substd。由一个或多个卤素，OH，1-4C烷基，1-4C烷氧基，CF 3，NO 2，亚甲二氧基或的; 噻吩，嘧啶或咪唑，所有的选择。 substd。通过1-4C烷基; R2 = H，1-7C烷基，苄基，甲酰基或1-7C烷基羰基; n = 0或1; R3 = H，1-7C烷基，甲酰基，烷基羰基1-7C，CN， - （CH 2）Q-OH， - （CH 2）●O-（1-7C烷基）， - （CH 2）Q-OCHO-， - （ CH 2）q-OCOR17， - （CH 2）q-OCONH-（1-7C烷基），-NR 4 R 5， - （CH 2）qNR6C（= W1）R 7， - （CH 2）qNR6COOR8， - （CH2）qNR6SO2R9， - （CH2 ）qNR6C（= W1）NR 10 R 11，-CH 2 NR 12 R 13，-CH 2 CH 2 NR 12 R 13，-COOH，烷氧基羰基1-7C，-C（= W1）NR 10 R 11，-CH 2 COOH，1-7C烷氧基羰，-CH2-C（= W1） NR 10 R 11，-O-CH2CH2-O-R18，-NR6COCOR19，-CO-NR20-NR 21 R 22，或GP。式（i）或（ii），或双键的; Q = 0，1或2; W1 = O或S; R4，R5 = H或1-7C烷基，或R5可以是另外3-7C环烷基，甲基，苄基或苯基; 或NR4R5 =氮杂环丁烷，吡咯烷，哌啶，吗啉，硫代吗啉，perhydroazepine，哌嗪或4-（1-4C烷基）哌嗪; R6 = H或1-7C烷基; R7 = H，1-7C烷基，乙烯基，苯基，苄基，吡啶基; 3-7C环烷基选择。 substd。由甲基（S），呋喃基，噻吩基，吡咯基或咪唑基; 或R6 + R7 =（CH 2）P; P = 3或4; R8 = 1-7C烷基或苯基; R9 = 1-7C烷基; 个选择。 substd。被1或2 1-7C烷基; 苯基选择。 substd。由一个或多个卤素，烷基1-7C，1-7C烷氧基，CF 3，OH，羧基，烷氧基羰基1-7C，1-7C烷氧基羰氧基，CN，NO 2，或氨基的选择。 substd。被1或2 1-7C烷基; R10，R11 = H或1-7C烷基; 或R11可以是另外3-7C环烷基甲基，3-7C-环环烷基，OH，1-4C烷氧基，苄基或苯基; 或NR 10 R 11 =氮杂环丁烷，吡咯烷，哌啶，吗啉，硫代吗啉，或perhydroazepine; R12，R13 = H或1-7C烷基; 或R13可以是另外3-7C环烷基甲基或苄基; R17 = 1-7C烷基; 或3-7C环烷基选择。 substd。由一个或多个甲基;苯基; 或吡啶基; R18 = H，1-7C烷基，甲酰基，或1-7C烷基羰基; R19 = 1-4C烷氧基; R20-R23 = H或1-7C烷基; 或NR 21 R 22 =吡咯烷，哌啶或吗啉; R24，R25 = H或1-7C烷基; 或R25可以是另外甲酰基或1-7C烷基羰基; R14 = 1-7C烷基，3-7C环烷基，和，当R 3 = H，R 14可以是另外-CONR15R16，和当R 3 = H，CN，COOH，烷氧基羰基1-7C或-C（= W1）NR10R11然后R14 可以是-NR 15 R 16; R15，R16 = 1-7C烷基; 或NR15R16 =氮杂环丁烷，吡咯烷，哌啶，吗啉，硫代吗啉，或perhydroazepine; J2 = Ar3N（R2）-CH或Ar 3相（CH 2）N-CH; AR3 =苯基选择。 substd。由卤素，OH，1-4C烷基，1-4C烷氧基或CF 3; Q = 1-6C烷基或苄基，这是在直立或平伏构型; 且X =阴离子。

8. 发明公开

EP1308435A3 Process for producing optically active amino alcohols 有权
标题翻译：一种制备光学活性的氨基醇处理
公开(公告)号：EP1308435A3
公开(公告)日：2003-06-04
申请号：EP02024517.1
申请日：2002-10-30
申请人： Kanto Kagaku Kabushiki Kaisha
发明人： Watanabe, Masahito , Murata, Kunihiko , Ikariya, Takao
IPC分类号： C07C201/12 , C07C253/30 , C07C213/02
CPC分类号： C07C253/30 , C07B2200/07 , C07C201/12 , C07C213/02 , C07D333/24 , C07C215/30 , C07C255/36 , C07C205/16 , C07C205/26
摘要： A process for producing an optically active amino alcohol is provided that includes a step in which a nitro ketone or a cyano ketone is reacted with a hydrogen-donating organic or inorganic compound in the presence of a transition metal compound catalyst having an optically active nitrogen-containing compound as an asymmetric ligand to give an optically active nitro alcohol or an optically active cyano alcohol, and a step in which the above optically active alcohol is further reduced to efficiently produce an optically active amino alcohol.

9. 发明授权

EP0658159B1 ARYLIDENE AND HETEROARYLIDENE OXINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译： ARYLIDEN-UND HETEROARYLIDEN-OXINDOL DERIVATE ALS TYROSIN KINASE INHIBITOREN
公开(公告)号：EP0658159B1
公开(公告)日：2000-08-23
申请号：EP94918379.2
申请日：1994-05-26
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , LONGO, Antonio , BRASCA, Maria, Gabriella , ORZI, Fabrizio , CRUGNOLA, Angelo , BALLINARI, Dario , MARIANI, Mariangela
IPC分类号： C07D401/06 , A61K31/40 , C07D209/34
CPC分类号： C07D401/06 , C07C255/36 , C07C255/37 , C07C255/41 , C07C327/42 , C07C2602/10 , C07D209/18 , C07D209/34 , C07D215/14
摘要： Arylidene and heteroarylidene oxindole derivatives of formula (I) wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline; R is hydrogen or an oxo (=O) group when Y is tetralin; or R is hydrogen when Y is naphthalene, quinoline or isoquinoline; each of R?1 and R2¿ independently is hydrogen, C¿1?-C6 alkyl or C2-C6 alkanoyl; m is zero, 1 or 2; n is zero, 1, 2 or 3; each of R?3 and R4¿ independently is hydrogen, halogen, cyano, C¿1?-C6 alkyl, carboxy, nitro or -NR?6R7¿ in which each of R?6 and R7¿ independently is hydrogen or C¿1?-C6 alkyl; R?5¿ is hydrogen or C¿1?-C6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.
摘要翻译：羟吲哚，丙烯酰胺，硫代丙烯酰胺和丙烯腈化合物及其药学上可接受的盐，其可用作酪氨酸激酶抑制剂。

10. 发明公开

EP0996614A1 ACRYLONITRILE COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND PESTICIDES CONTAINING THEM 失效
标题翻译：丙烯腈衍生物，用于生产和含农药
公开(公告)号：EP0996614A1
公开(公告)日：2000-05-03
申请号：EP98902207.4
申请日：1998-02-13
申请人： ISHIHARA SANGYO KAISHA, LTD.
发明人： KOYANAGI, Toru,Ishihara Sangyo Kaisha Ltd. , NAKAMURA, Yuji,Ishihara Sangyo Kaisha Ltd. , MORITA, Masayuki,Ishihara Sangyo Kaisha Ltd. , SUGIMOTO, Koji,Ishihara Bioscience K.K. , IKEDA, Tsuyoshi,Ishihara Sangyo Kaisha Ltd. , OGAWA, Munekazu,Ishihara Sangyo Kaisha Ltd.
IPC分类号： C07C255/00 , C07C255/38
CPC分类号： C07D295/26 , A01N37/36 , A01N37/40 , A01N37/44 , A01N37/48 , A01N41/02 , A01N41/04 , A01N43/18 , A01N43/40 , A01N47/02 , A01N47/06 , A01N47/12 , C07C255/36 , C07C255/37 , C07C255/38 , C07C305/18 , C07C307/02 , C07C309/65 , C07C309/66 , C07C309/67 , C07C309/73 , C07C313/04 , C07C313/16 , C07C313/20 , C07C317/46 , C07C323/12 , C07C327/22 , C07C329/04 , C07C329/06 , C07C329/10 , C07C329/16 , C07C329/20 , C07C333/04 , C07C381/00
摘要： Novel compounds useful as active ingredients of pesticides are disclosed. Acrylonitrile compounds of formula (I) or their salts, wherein Q is Qa, Qb, Qc or Qd, Y is =C(R4)- or =N-, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, l is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.

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