公开(公告)号：EP3259249A1

公开(公告)日：2017-12-27

申请号：EP16752034.5

申请日：2016-02-16

申请人： B.G. Negev Technologies & Applications Ltd., at Ben-Gurion University

发明人： PAPPO, Doron ,  PARNES, Regev

IPC分类号： C07C319/18 ,  C07J1/00 ,  C07D317/48 ,  C07B45/06 ,  A61K31/565 ,  A61K31/335

CPC分类号： C07C15/04 ,  A61K31/015 ,  A61K31/10 ,  A61K31/335 ,  A61K31/47 ,  A61K31/565 ,  C07B31/00 ,  C07B37/04 ,  C07B45/06 ,  C07B2200/05 ,  C07C39/14 ,  C07C39/38 ,  C07C43/225 ,  C07C43/23 ,  C07C253/30 ,  C07C317/14 ,  C07C319/18 ,  C07C321/20 ,  C07C323/16 ,  C07C323/56 ,  C07C323/60 ,  C07C327/06 ,  C07D209/10 ,  C07D317/64 ,  C07J1/007 ,  C07J31/006 ,  C07C255/54 ,  A61K2300/00

摘要： Novel selective synthesis route to introduce primary alkyl groups on aromatic compounds is disclosed. The synthesis route is based on electrophilic aromatic substitutions of thionium ion species that are generated in-situ from aldehydes and thiols, affording benzyl sulfide that can be reduced with triethylsilane.

公开(公告)号：EP2755969B1

公开(公告)日：2017-01-18

申请号：EP12750777.0

申请日：2012-08-27

申请人： Syngenta Participations AG

发明人： CASSAYRE, Jérôme Yves ,  EL QACEMI, Myriem

IPC分类号： C07D417/12 ,  C07D275/03 ,  A01N43/26

CPC分类号： A01N43/90 ,  A01N43/00 ,  A01N43/80 ,  A01N51/00 ,  C07C323/22 ,  C07C323/56 ,  C07C327/22 ,  C07C327/32 ,  C07D249/08 ,  C07D275/02 ,  C07D291/04 ,  C07D331/04 ,  C07D417/10 ,  C07D417/12

公开(公告)号：EP2313090B1

公开(公告)日：2016-03-30

申请号：EP09798181.5

申请日：2009-07-13

申请人： Pronova BioPharma Norge AS

发明人： HOLMEIDE, Anne, Kristin ,  HOVLAND, Ragnar ,  BRÆNDVANG, Morten

IPC分类号： C07C323/52 ,  C07C317/44 ,  C07C323/54 ,  C07C323/56 ,  C07C323/61 ,  A23L33/12 ,  A61K31/19 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07C323/54 ,  A23L33/12 ,  C07C317/44 ,  C07C323/52 ,  C07C323/55 ,  C07C323/56 ,  C07C323/61 ,  C07C2601/04

公开(公告)号：EP2816023A4

公开(公告)日：2015-09-09

申请号：EP13749442

申请日：2013-02-12

申请人： TAKEDA PHARMACEUTICAL

发明人： MIWATASHI SEIJI ,  SUZUKI HIDEO ,  OKAWA TOMOHIRO ,  MIYAMOTO YASUFUMI ,  YAMASAKI TAKESHI ,  HITOMI YUKO ,  HIRATA YASUHIRO ,  SHIBUYA AKITO

IPC分类号： C07C59/68 ,  A61K31/192 ,  A61K31/195 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4166 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P43/00 ,  C07C59/70 ,  C07C59/72 ,  C07C229/34 ,  C07C233/47 ,  C07C255/37

CPC分类号： C07C59/135 ,  C07C59/68 ,  C07C59/70 ,  C07C59/72 ,  C07C229/34 ,  C07C233/47 ,  C07C235/34 ,  C07C255/37 ,  C07C255/41 ,  C07C255/46 ,  C07C309/65 ,  C07C309/66 ,  C07C311/21 ,  C07C317/44 ,  C07C323/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/12 ,  C07D213/30 ,  C07D213/55 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D231/12 ,  C07D239/26 ,  C07D239/34 ,  C07D271/10 ,  C07D277/24 ,  C07D285/12 ,  C07D309/06 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

公开(公告)号：EP2268614B1

公开(公告)日：2013-05-15

申请号：EP09719226.4

申请日：2009-03-11

申请人： Showa Denko K.K.

发明人： AOKI, Hidemasa ,  KUROIWA, Akio ,  SHIBUYA, Akira

IPC分类号： C07C319/04

CPC分类号： C07C319/04 ,  C07C323/56 ,  C07C323/52

公开(公告)号：EP1324970B1

公开(公告)日：2008-11-05

申请号：EP01969762.2

申请日：2001-09-24

申请人： F. Hoffmann-La Roche AG

发明人： LAPIERRE, Jean-Marc ,  ROTSTEIN, David, Mark ,  SJOGREN, Eric, Brian

IPC分类号： C07C65/28 ,  C07C323/56 ,  C07D231/12 ,  C07D207/32 ,  C07D307/38 ,  C07C65/19 ,  C07D295/08 ,  C07D239/38 ,  C07D249/12 ,  A61K31/19 ,  A61K31/33

CPC分类号： C07D207/27 ,  C07C65/19 ,  C07C65/28 ,  C07C229/38 ,  C07C233/83 ,  C07C311/13 ,  C07C317/44 ,  C07C323/56 ,  C07C2602/10 ,  C07D207/327 ,  C07D211/76 ,  C07D231/12 ,  C07D231/14 ,  C07D233/56 ,  C07D233/84 ,  C07D239/26 ,  C07D239/38 ,  C07D249/08 ,  C07D249/12 ,  C07D257/04 ,  C07D277/16 ,  C07D277/30 ,  C07D277/74 ,  C07D285/125 ,  C07D295/155 ,  C07D307/38 ,  C07D333/22 ,  C07D333/24 ,  C07D333/60

摘要： The current invention provides novel retinoid compounds and methods for their synthesis, the use of such compounds for the preparation of medicaments for treating or preventing emphysema, cancer and dermatological disorders, methods for such deseases and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

摘要翻译： 本发明提供新型类视黄醇化合物及其合成方法，治疗或预防肺气肿，癌症和皮肤疾病的方法以及适用于治疗或预防肺气肿，癌症和皮肤疾病的药物组合物。

公开(公告)号：EP1487430A4

公开(公告)日：2007-08-22

申请号：EP03713776

申请日：2003-02-28

申请人： ICAGEN INC

发明人： RIGDON GREGORY COOKSEY ,  STOCKER JONATHAN WALTER ,  MCNAUGHTON-SMITH GRANT A

IPC分类号： C07D333/38 ,  A61K9/00 ,  A61K31/165 ,  A61K31/18 ,  A61K31/381 ,  A61K31/421 ,  A61K31/4245 ,  A61K45/00 ,  A61K45/06 ,  A61K47/02 ,  A61K47/10 ,  A61K47/18 ,  A61K47/32 ,  A61K47/34 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07C311/20 ,  C07C317/44 ,  C07C323/56 ,  C07D263/10 ,  C07D263/14 ,  C07D263/32 ,  C07D271/06 ,  C07D307/52

CPC分类号： C07D271/06 ,  A61K9/0048 ,  A61K31/165 ,  A61K45/06 ,  C07C311/20 ,  C07C317/44 ,  C07C323/56 ,  C07C2601/16 ,  C07D263/32 ,  C07D307/52 ,  A61K2300/00

摘要： This invention relates to the use of compounds able to decrease potassium ion flow through intermediate conductance calcium activated potassium channels for treatment of diseases related to increased intraocular pressure modulated by intermediate conductance calcium activated potassium channels.

公开(公告)号：EP1600438A4

公开(公告)日：2007-05-02

申请号：EP04714501

申请日：2004-02-25

申请人： KANEKA CORP

发明人： YAMAMOTO SHOGO ,  TAKEDA TOSHIHIRO ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

IPC分类号： C07C319/14 ,  C07B53/00 ,  C07B55/00 ,  C07C51/363 ,  C07C51/43 ,  C07C57/58 ,  C07C319/28 ,  C07C323/56

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C51/363 ,  C07C319/14 ,  C07C57/58 ,  C07C323/56

摘要： Optically active compounds having thio groups at the 2-position which are important to the production of drugs and so on can be produced with minimized racemization in high yield and at a low cost by chlorinating an optically active compound having a hydroxyl group at the 2-position with the inversion of configuration at the 2-position to form an optically active compound having a chlorine atom at the 2-position, and reacting the optically active compound having a chlorine atom at the 2-position with a metal thiolate to introduce a thio group to the compound with the invention of configuration at the 2-position. Further, optically active compounds having thio groups at the 2-position can be produced at higher optical purities and in higher yields by conducting the reaction of an optically active compound having a chlorine atom at the 2-position with a metal thiolate in the presence of water. Additionally, optically active carboxylic acids having thio groups at the 2-position can be efficiently rid of coexistent impurities such as optical isomers by crystallization in the presence of an aliphatic hydrocarbon solvent and/or a sulfur-containing solvent, whereby optically active carboxylic acids having thio groups at the 2-position can be obtained as crystalline substances at further enhanced purities.

公开(公告)号：EP1676833A1

公开(公告)日：2006-07-05

申请号：EP06005766.8

申请日：2004-06-17

申请人： AstraZeneca AB

发明人： Lindstedt-Alstermark, Eva-Lotte ,  Li, Lanna ,  Olsson, Christina

IPC分类号： C07C235/20 ,  A61K31/16 ,  A61P3/10

CPC分类号： C07C233/11 ,  C07B2200/07 ,  C07C233/51 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07C255/46 ,  C07C309/66 ,  C07C323/41 ,  C07C323/56 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/14 ,  C07D295/135 ,  C07D295/185

摘要： The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.

摘要翻译： 本发明提供式I化合物制备这些化合物的方法，它们可用于治疗包括脂质紊乱（血脂异常）在内的临床症状，不论是否与胰岛素抵抗有关，其治疗用途的方法和含有它们的药物组合物。

公开(公告)号：EP1583738A1

公开(公告)日：2005-10-12

申请号：EP03785831.3

申请日：2003-12-16

申请人： Merck Patent GmbH

发明人： ADJE, Nathalie ,  BRUNET, Michel ,  ROCHE, Didier ,  ZEILLER, Jean-Jacques ,  YVON, Stéphane ,  GUYARD-DANGREMONT, Valérie ,  CONTARD, Francis ,  GUERRIER, Daniel ,  FERRAND, Gérard ,  BONHOMME, Yves

IPC分类号： C07C309/65 ,  C07C49/755 ,  C07C49/747 ,  C07C59/125 ,  C07C69/708 ,  C07C69/78 ,  C07C65/21 ,  C07C59/60 ,  C07C69/734 ,  C07C229/18 ,  C07C255/40 ,  C07C69/712 ,  C07C323/56 ,  C07C323/52 ,  A61K31/215 ,  A61K31/185 ,  A61P3/10 ,  A61P3/06 ,  C07C323/34 ,  C07C233/76 ,  C07C211/60

CPC分类号： C07C323/56 ,  C07C45/46 ,  C07C45/673 ,  C07C45/68 ,  C07C49/747 ,  C07C49/755 ,  C07C59/72 ,  C07C59/90 ,  C07C65/40 ,  C07C67/30 ,  C07C67/31 ,  C07C69/712 ,  C07C69/736 ,  C07C69/76 ,  C07C205/45 ,  C07C211/60 ,  C07C229/18 ,  C07C233/33 ,  C07C251/44 ,  C07C255/40 ,  C07C309/65 ,  C07C317/44 ,  C07C323/22 ,  C07C323/52 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C47/575

摘要： The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N-OR9, in which R9 represents H or a saturated hydrocarbon-based aliphatic group; CR10R11, in which R10 and R11, which may be identical or different, represent H or a saturated hydrocarbon-based aliphatic group; R1 and R2, which may be identical or different, represent H or a saturated aliphatic hydrocarbon-based chain; or alternatively R1 and R2 together form an optionally substituted saturated aliphatic hydrocarbon-based chain; the radicals R3 and R4, which may be identical or different, take any of the is meanings given above for R1 and R2, or alternatively R1 and the group R4 borne by the carbon alpha to CR1R2 represent nothing and a double bond links the CR1R2 carbon to the alpha CR3R4 carbon; or alternatively one of the radicals R1 and R2 forms with one of the radicals R3 and R4 an optionally substituted saturated or unsaturated aliphatic hydrocarbon-based chain; one of the radicals R5 and R6 represents W, and the other represents Z which is chosen from a saturated or unsaturated aliphatic hydrocarbon-based radical; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic or heterocyclic radical; a radical -alk-Cy, in which alk represents an alkylene chain and Cy represents an optionally substituted saturated, unsaturated and/or aromatic heterocyclic or carbocyclic radical; W represents -XL-CO2R7; -X-L-Tet, in which X and L are as defined below and Tet represents optionally substituted tetrazole; in which L represents a saturated or unsaturated aliphatic hydrocarbon-based chain, which is optionally substituted and/or optionally interrupted by optionally substituted arylene; X represents O; NR8, in which R8 represents H; a saturated aliphatic hydrocarbon-based group; a group -CO-R' or -SO2-R', in which R' takes any of the meanings given below for R7 with the exception of H; or R8 represents an optionally substituted aromatic carbocyclic group; or X represent S(O)m , in which m is chosen from 0, 1 and 2; R7 represents H; a saturated or unsaturated aliphatic hydrocarbon-based group; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic group; an optionally substituted, saturated, unsaturated and/or aromatic heterocyclic group; and the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, and also mixtures thereof in all proportions, which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes.