公开(公告)号：EP1736467A4

公开(公告)日：2009-07-01

申请号：EP05728832

申请日：2005-04-04

Applicant: DAINIPPON SUMITOMO PHARMA CO

Inventor： BAN HITOSHI ,  ASANO SHIGEHIRO

IPC: A61K31/255 ,  A61K31/44 ,  A61K31/454 ,  A61K31/506 ,  A61K31/55 ,  A61K31/664 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C307/02 ,  C07C307/06 ,  C07C311/05 ,  C07C311/18 ,  C07C311/37 ,  C07C317/32 ,  C07D211/28 ,  C07D211/34 ,  C07D211/58 ,  C07D211/60 ,  C07D211/64 ,  C07D211/70 ,  C07D211/72 ,  C07D213/06 ,  C07D223/06 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D451/02 ,  C07F9/59

CPC classification number: C07D211/60 ,  A61K31/255 ,  A61K31/44 ,  A61K31/454 ,  A61K31/506 ,  A61K31/55 ,  A61K31/664 ,  C07C307/02 ,  C07C307/06 ,  C07C311/18 ,  C07C311/37 ,  C07C2601/14 ,  C07D211/28 ,  C07D211/34 ,  C07D211/58 ,  C07D211/64 ,  C07D211/70 ,  C07D211/72 ,  C07D401/04 ,  C07D417/04 ,  C07D451/02 ,  C07F9/598

Abstract: Disclosed are a compound represented by the formula (1) below, a prodrug thereof, and their pharmaceutically acceptable salts which have an effect of increasing LDL receptor expression and are useful as drugs for treating hyperlipemia, arteriosclerosis and the like. (1) (In the formula, m, n and p independently represent an integer of 0-4 and 3 ≤ m + n ≤ 8; X represents a group expressed as NR4 or the like; R1, R3 and R4 represent a substituted or unsubstituted aryl group or the like; R2 represents a hydrogen atom or the like; a, b, c, d, e and f respectively represent a hydrogen atom, a substituted or unsubstituted alkyl group or the like; Y represents -SO2- or the like; and Z represents an oxygen atom or the like.)

Abstract translation: 公开了由下式（1）表示的化合物，其前药和它们的药学上可接受的盐，其具有增加LDL受体表达的作用并且可用作治疗高脂血症，动脉硬化等的药物。 （1）（式中，m，n和p分别独立地表示0〜4的整数，且3≤m+n≤8; X表示以NR 4等表示的基团; R 1，R 3和R 4表示取代或 未取代的芳基等; R 2表示氢原子等; a，b，c，d，e和f分别表示氢原子，取代或未取代的烷基等; Y表示-SO 2 - 或 类似;并且Z表示氧原子等。）

公开(公告)号：EP1539684B1

公开(公告)日：2009-04-15

申请号：EP03793925.3

申请日：2003-09-08

Applicant: Richter Gedeon Nyrt.

Inventor： GIZUR, Tibor ,  TÖRLEY, Jozsef ,  FOGASSY, Elemér ,  BALINT, Jozsef ,  EGRI, Gabriella ,  DEMETER, Adám

IPC: C07C303/40 ,  C07C311/37 ,  A61K31/18

CPC classification number: C07C311/37 ,  A61K31/18 ,  C07B2200/07 ,  C07C303/40 ,  Y02P20/55

Abstract: New process for industrial preparation of R-(-)-tamsulosine HCl of formula (I). In this process (R,S)-5-[2-(N-benzyl-amino)-propyl]-2-methoxy-benzenesulphonamide of formula (I), acid addition salts and enantiomers thereof and R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III) are new intermediates. R-(-)-tamsulosine HCl of formula (I) is prepared by reacting the secondary benzylamine of formula (II) with an alkylating agent to R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III), the benzyl protecting group is removed and then HCl salt is formed. The optically active compound of formula (II) is prepared by reductive condensation of (4-methoxy-3-sulphamoyl-phenyl)-acetone and benzylamine and the obtained racemic compound is optically resolved by chiral acid.

公开(公告)号：EP1631995B1

公开(公告)日：2008-07-16

申请号：EP04732346.4

申请日：2004-05-12

Applicant: Cambridge Enterprise Limited

Inventor： CHUA, Lay-Lay ,  HO, Peter, Kian-Hoon ,  FRIEND, Richard, Henry

IPC: H01L51/30 ,  G03C1/695 ,  C07C311/37 ,  C07C247/00

CPC classification number: G03F7/0046 ,  C07C247/16 ,  C07C311/37 ,  G03C1/695 ,  G03F7/008 ,  G03F7/012 ,  H01L51/0002 ,  H01L51/0003 ,  H01L51/0035 ,  H01L51/0037 ,  H01L51/0038 ,  H01L51/0039 ,  H01L51/0043 ,  H01L51/0059 ,  H01L51/052 ,  Y02E10/549 ,  Y02P70/521

Abstract: A method of forming a polymer device including the steps of: (i) depositing on a substrate a solution comprising a polymer or oligomer and a crosslinking moiety, to form a layer; (ii) curing the layer formed in step (i) under conditions to form an insoluble crosslinked polymer; characterised in that the crosslinking moiety is present in step (i) in an amount in the range of from 0.05 to 5 mol % based on the total number of moles of repeat units of the polymer or oligomer and the crosslinking moiety in the solution.

公开(公告)号：EP1491187A4

公开(公告)日：2008-04-16

申请号：EP03712737

申请日：2003-03-18

Applicant: KISSEI PHARMACEUTICAL

Inventor： KOIZUMI TAKASHI ,  HOYANO YUJI ,  AKAHANE SATOSHI

IPC: A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/216 ,  A61K31/275 ,  A61K31/4245 ,  A61K31/5375 ,  A61K45/06 ,  A61P3/10 ,  A61P13/12 ,  A61P37/02 ,  A61P43/00 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D295/185 ,  A61K45/00 ,  C07D295/18

CPC classification number: C07D271/113 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/216 ,  A61K31/275 ,  A61K31/4245 ,  A61K31/5375 ,  A61K45/06 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14 ,  C07D271/10 ,  C07D277/28 ,  C07D295/185 ,  A61K2300/00

Abstract: A novel medicinal composition which contains as an active ingredient either a compound represented by the general formula [I] (wherein R1 is hydrogen or optionally substituted alkyl; R2 is dialkylamino, alkyl, cycloalkyl, optionally substituted aryl, etc.; T is oxygen, sulfur, etc.; Q is hydrogen or optionally substituted alkyl; and Z is hydrogen, hydroxy, etc.) or a pharmacologically acceptable salt of the compound. The medicinal composition is highly effective in inhibiting mesangial cell proliferation and lowering urinary protein and is useful for the prevention of or treatments for various kidney diseases such as IgA nephropathy, diabetic nephropathy, and nephrotic syndrome.

公开(公告)号：EP1888518A1

公开(公告)日：2008-02-20

申请号：EP06747796.8

申请日：2006-05-22

Applicant: AstraZeneca AB

Inventor： NORDVALL, Gunnar ,  PETERSSON, Carl ,  RAKOS, Laszlo ,  SOHN, Daniel

IPC: C07C311/37 ,  A61K31/18 ,  A61K31/4025 ,  A61K31/435 ,  A61K31/495 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D207/12 ,  C07D213/75 ,  C07D215/38 ,  C07D217/06 ,  C07D239/69 ,  C07D311/04 ,  C07D405/04

CPC classification number: C07C311/44 ,  C07C2602/10 ,  C07D209/08 ,  C07D213/76 ,  C07D215/38 ,  C07D217/08 ,  C07D217/22 ,  C07D235/06 ,  C07D239/69 ,  C07D277/64 ,  C07D295/096 ,  C07D311/58 ,  C07D317/66 ,  C07D405/12 ,  C07D471/04 ,  C07D493/04

Abstract: The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

Abstract translation: 本发明涉及式（I）的新化合物，其中R 1至R 12，P，X，Q和n如式I中所定义，或其盐，溶剂化物或溶剂化盐，其制备方法和新中间体 用于其制备，含有所述化合物的药物制剂以及所述化合物在治疗中的用途。

公开(公告)号：EP1773763A1

公开(公告)日：2007-04-18

申请号：EP04761606.5

申请日：2004-08-02

Applicant: Ambrilia Biopharma Inc.

Inventor： STRANIX, Brent, Richard ,  PERRON, Valérie

IPC: C07C311/37 ,  C07D207/44 ,  C07D213/72 ,  C07D215/38 ,  C07D217/22 ,  C07D241/44 ,  C07D265/30 ,  C07D233/88 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/18 ,  A61K31/44 ,  A61K31/4164 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/47 ,  A61K31/498

CPC classification number: C07C311/41 ,  A61K31/63 ,  A61K31/635 ,  A61K31/662 ,  C07D295/215 ,  C07F9/091 ,  C07F9/6533

Abstract: The present invention provides lysine based compounds of the formula (I); and when the compound of formula (I) comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein Rl may be, for example, (HO)2P(O)-, (NaO)2P(O)-, alkyl­CO- or cycloalkyl-CO-, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein. These lysine based compounds have a physiologically cleavable unit, namely R1 , whereby upon cleavage of the unit, an HIV aspartyl protease inhibitor is released,

Abstract translation: 本发明提供了式（I）的基于赖氨酸的化合物; （O） - ，（NaO）2 P（O） - ，烷基CO-或环烷基时，式（I）化合物包含氨基时，其药学上可接受的铵盐，其中R1可以是例如 -CO-，其中X可以是例如F，Cl和Br，并且其中R2和R3如本文所定义。 这些基于赖氨酸的化合物具有生理学上可裂解的单元，即R1，由此在切割单元时释放HIV天冬氨酰蛋白酶抑制剂，

公开(公告)号：EP1363878A4

公开(公告)日：2005-12-21

申请号：EP02700832

申请日：2002-02-07

Applicant: YONSUNG FINE CHEMICAL CO LTD

Inventor： HAM WON-HUN ,  OH CHANG-YOUNG ,  KIM YONG-HYUN ,  LEE YIU-SUK ,  LEE KEE-YOUNG

IPC: C07C317/22 ,  C07C303/40 ,  C07C311/37

CPC classification number: C07C303/40 ,  C07C311/37

Abstract: The present invention relates to a novel process for preparing sulfamoyl-substituted phenethylamine derivatives, specifically, 5-{2-[2-(2-alkoxy-phenoxy)ethylamino]-propyl}-2-methoxy-benzene sulfonamide of the formula (1).

公开(公告)号：EP1331221A4

公开(公告)日：2005-11-23

申请号：EP01972648

申请日：2001-10-02

Applicant: KISSEI PHARMACEUTICAL

Inventor： OKAZAKI KOSUKE ,  UCHIDA MASAHIKO ,  MUKAIYAMA HARUNOBU ,  KOBAYASHI HIROAKI ,  KAI YUICHIRO ,  TAKEUCHI HIDEKI ,  YOKOYAMA KENJI ,  TERAO YOSHIHIRO ,  HOYANO YUJI ,  SHIOHARA HIROAKI ,  KIKUCHI NORIHIKO

IPC: A61P7/02 ,  A61P9/10 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07D277/28 ,  A61K31/216 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/5375 ,  C07D271/10 ,  C07D295/18

CPC classification number: A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

Abstract: 5-Amidino-2-hydroxybenzenesulfonamide derivatives of the general formula [I] or their pharmacologically acceptable salts, exhibiting potent and selective inhibitory activity against activated blood coagulation factor X and being useful as preventive or therapeutic drugs for diseases whose onset is related to activated blood coagulation factor X; pharmaceutical compositions containing the same; their use in medicines; and intermediates for their preparation: [I] wherein R is hydrogen or optionally substituted lower alkyl; R is di(lower alkyl)amino, lower alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heterocycloalkyl, or an optionally substituted aromatic heterocyclic group; T is oxygen, sulfur, sulfonyl, or the like; Q is hydrogen or optionally substituted lower alkyl; and Z is hydrogen, hydroxyl, or the like.

Abstract translation: 本发明涉及一种由通式表示的5-脒基-2-羟基苯磺酰胺衍生物： worin - [R <1>是一个氢原子或在OPTIONALLY substituiertem低级烷基; [R <2>是二（低级烷基）氨基，低级烷基，环烷基，在OPTIONALLY substituiertem芳基，在任选取代的杂环基团，或在任选被取代的芳香族杂环基。 T为氧原子，硫原子，磺酰基等; Q处于OPTIONALLY substituiertem氢原子或低级烷基; 且Z为氢原子，羟基基团等，或它们的药学上可接受的盐，其施加一个有效的和选择性的活化血液凝固因子X抑制活性，是作为用于疾病的与在相关联的预防或治疗剂是有用 活化血液凝固第X因子，药物组合物包含相同的，它们并涉及其中间体的药物的用途。

公开(公告)号：EP0769498B9

公开(公告)日：2004-11-10

申请号：EP96307048.7

申请日：1996-09-27

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Nakae, Takahiko, c/o Minase Research Institute ,  Kato, Masashi, c/o Minase Research Institute ,  Fujita, Takehito, c/o Minase Research Institute ,  Kawabata, Kazuhito, c/o Minase Research Institute ,  Ohno, Hiroyuki, c/o Minase Research Institute

IPC: C07D403/12 ,  A61K31/635 ,  A61K31/40 ,  C07D207/06 ,  C07C311/37 ,  C07C311/44 ,  C07D403/14 ,  C07D413/12 ,  C07D405/14 ,  C07D417/12 ,  C07D295/32

CPC classification number: C07D295/26 ,  C07C311/29 ,  C07C311/64 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D203/24 ,  C07D207/48 ,  C07D209/42 ,  C07D211/96 ,  C07D231/12 ,  C07D233/56 ,  C07D235/22 ,  C07D249/08 ,  C07D263/38 ,  C07D277/56 ,  C07D307/68 ,  C07D309/10 ,  C07D333/24 ,  C07D491/10 ,  C07H5/10 ,  C07K5/06139 ,  C07K5/06165

公开(公告)号：EP1443041A1

公开(公告)日：2004-08-04

申请号：EP02777984.2

申请日：2002-10-29

Applicant: Kissei Pharmaceutical Co., Ltd.

Inventor： UCHIDA, Masahiko ,  KOBAYASHI, Hiroaki ,  KAI, Yuichiro ,  YOKOYAMA, Kenji ,  TERAO, Yoshihiro ,  MURANAKA, Hideyuki

IPC: C07C311/37 ,  C07C311/29 ,  C07D207/00 ,  C07D211/62 ,  C07D213/00 ,  C07D231/12 ,  C07D233/36 ,  C07D241/04 ,  C07D261/08 ,  C07D263/20 ,  C07D271/00 ,  C07D277/44 ,  C07D295/00 ,  C07D333/00 ,  A61K31/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12

CPC classification number: C07D207/273 ,  A61K31/18 ,  C07C311/29 ,  C07D207/00 ,  C07D207/16 ,  C07D211/42 ,  C07D211/60 ,  C07D213/42 ,  C07D213/82 ,  C07D231/12 ,  C07D233/02 ,  C07D261/08 ,  C07D263/38 ,  C07D271/113 ,  C07D277/28 ,  C07D277/46 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D317/62 ,  C07D333/20

Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula:
wherein R 1 is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.;
Q is a hydrogen atom or an optionally substituted lower alkyl group; and
Z is a hydrogen atom or a hydroxy group etc.,
or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

Abstract translation: 本发明涉及一种5-脒基-2-羟基苯磺酰胺衍生物由如下通式表示： worin - [R <1>是任选substituiertem低级烷基，可任选地substituiertem低级烷氧基，在OPTIONALLY substituiertem低级烯基， 环烷基或低级酰基等; Q处于OPTIONALLY substituiertem氢原子或低级烷基; 和Z是氢原子或羟基基团，等等，或它们的药学上可接受的盐，其施加一个有效的和选择性的活化血液凝固因子X抑制活性，并且作为用于疾病的预防或治疗剂发生在相关联是有用 活化血液凝固第X因子，药物组合物，其包括相同的和在其中间体。 这些化合物用作预防或治疗药用于各种疾病：如脑梗塞，脑血栓，脑栓塞，TIA，脑血管混蛋，阿耳茨海默氏病，心肌梗塞，心脏病发作，心脏衰竭，血栓形成，肺梗死和肺栓塞。