公开(公告)号：EP2444079B1

公开(公告)日：2016-11-30

申请号：EP11181066.9

申请日：2006-05-17

Applicant: SARcode Bioscience Inc.

Inventor： Gadek, Thomas ,  Burnier, John

IPC: A61K31/166 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4725 ,  A61P27/02

CPC classification number: A61K31/4725 ,  A61B3/101 ,  A61B3/145 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0051 ,  A61K9/0053 ,  A61K31/197 ,  A61K31/198 ,  A61K31/275 ,  A61K31/341 ,  A61K31/352 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K33/00 ,  A61K33/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  A61K45/06 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/00 ,  C07D217/02 ,  C07D217/06 ,  C07D217/20 ,  C07D217/26 ,  C07D307/52 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/5047 ,  G01N33/566 ,  G01N33/6872 ,  G01N2333/705 ,  G01N2333/70525 ,  G01N2333/70546 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20 ,  G01N2800/16 ,  Y10S514/912 ,  Y10S514/914

公开(公告)号：EP2687507A1

公开(公告)日：2014-01-22

申请号：EP12757861.5

申请日：2012-03-14

Applicant: Taisho Pharmaceutical Co., Ltd.

Inventor： BUSUJIMA, Tsuyoshi ,  OI, Takahiro ,  TANAKA, Hiroaki ,  SHIRASAKI, Yoshihisa ,  IWAKIRI, Kanako ,  SATO, Nagaaki ,  TOKITA, Shigeru

IPC: C07D209/44 ,  A61K31/4035 ,  A61K31/454 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K31/538 ,  A61K31/55 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D217/04 ,  C07D217/06 ,  C07D217/22 ,  C07D223/16

CPC classification number: C07D217/18 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07D209/44 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  C07D217/20 ,  C07D217/22 ,  C07D217/26 ,  C07D223/16 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04

Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action:

wherein
Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, R B represents a C 4-18 alkyl group, a C 3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II):

wherein
V represents the formula -CR 11 R 12 -, -CO-, -CO-O-, or -CO-NH-,
W represents a single bond or a C 1-3 alkylene group, and
Ring B represents a C 3-8 cycloalkyl group, a C 3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group,
Y represents a nitrogen atom or the formula N + (R F ),
R F represents a C 1-4 alkyl group, and
m and n, which may be the same or different, each represent an integer of 0 or 1.

Abstract translation: 提供了具有优异的单酰基甘油酰基转移酶2抑制作用的由以下通式（I）表示的化合物或其药学上可接受的盐：其中环A表示部分饱和的杂芳基，芳基或杂芳基，RB表示 C 4-18烷基，C 3-8环烷基，部分饱和芳基，芳基或下式（II）：其中V表示式-CR 11 R 12 - ， - CO-， -CO-O-或-CO-NH-，W表示单键或C 1-3亚烷基，环B表示C 3-8环烷基，C 3-8环烯基，部分饱和 杂芳基，饱和杂环基，芳基或杂芳基，Y表示氮原子或式N +（RF），RF表示C 1-4烷基，m和n可以是 相同或不同，每个表示0或1的整数。

公开(公告)号：EP2628728A1

公开(公告)日：2013-08-21

申请号：EP12159520.1

申请日：2012-03-14

Applicant: Divi's Laboratories Limited

Inventor： Divi, Murali. Krishna, Prasad ,  Rao, Pendyala, Srinivas ,  Ramana, Lavu, Venkata

IPC: C07D217/20 ,  C07B57/00

CPC classification number: C07D217/20 ,  C07B57/00 ,  C07B2200/07

Abstract: The resolution of racemic 1-(4-methoxybenzyl)-octahydro-isoquinoline, a key intermediate in the synthesis of the antitussive agent dextromethorphan, is reported using (R)-2-(6-methoxy-2-naphthyl) propionic acid in good yields. The resolving agent and the undesired isomer of the octahydro-isoquinoline have been recovered in good yield.

Abstract translation: 报道了使用（R）-2-（6-甲氧基-2-萘基）丙酸合成消旋剂右美沙芬的外消旋1-（4-甲氧基苄基） - 八氢异喹啉的一种关键中间体 产量。 已经以良好的收率回收了八氢异喹啉的拆分剂和不需要的异构体。

公开(公告)号：EP2586772A1

公开(公告)日：2013-05-01

申请号：EP11798156.3

申请日：2011-06-22

Applicant: Taisho Pharmaceutical Co., Ltd.

Inventor： TAKAYAMA Tetsuo ,  KAWAMURA Madoka ,  WAKASUGI Daisuke ,  NISHIKAWA Rie ,  SEKIGUCHI Yoshinori

IPC: C07D217/18 ,  A61K31/472 ,  A61P11/02 ,  A61P11/06 ,  A61P17/04 ,  A61P37/08 ,  A61P43/00 ,  C07D217/20

CPC classification number: C07D217/18 ,  C07D217/20

Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a pharmaceutical.

Abstract translation: 由式（I）表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用，因此可用作药物。

公开(公告)号：EP1861373A2

公开(公告)日：2007-12-05

申请号：EP06735796.2

申请日：2006-02-23

Applicant: MALLINCKRODT, INC.

Inventor： BAO, Jian ,  CANTRELL, Gary, L. ,  MOSER, Frank, W. ,  WANG, Peter, Xianqi

IPC: C07D221/28 ,  C07D489/02 ,  C07D217/20 ,  C07D491/10

CPC classification number: C07D491/10 ,  C07D217/20 ,  C07D221/28 ,  C07D489/02

Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ß,Ϝ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ß,Ϝ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting a,ß-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ß,Ϝ-bicyclic ketone compounds, wherein the ß,Ϝ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.

公开(公告)号：EP1774968A4

公开(公告)日：2007-11-07

申请号：EP05767135

申请日：2005-07-29

Applicant: EDUCATION CT OF TRADITIONAL CH ,  NAKAJIMA HIROSHI

Inventor： NAKAJIMA HIROSHI ,  TANAHASHI TAKAO ,  YAMADA JUN ,  SUN SHU-JIAN ,  SUGIMOTO YUMI

IPC: A61K31/472 ,  A23L1/30 ,  A23L2/52 ,  A61K31/4725 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  C07D217/20

CPC classification number: C07D217/20 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725

Abstract: This invention provides a psychotropic agent, an analgesic, and/or an antiphlogistic, and a heath food that can safely take over a long period of time and is characterized by comprising, as an effective ingredient, a benzylisoquinoline derivative represented by general formula (I) or a bisbenzylisoquinoline derivative represented by general formula (II) or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP1278758A4

公开(公告)日：2005-10-19

申请号：EP01928978

申请日：2001-04-27

Applicant: UNIV ARIZONA STATE

Inventor： PETTIT GEORGE R ,  LIPPERT JOHN W III

IPC: A61K47/48 ,  C07C255/43 ,  C07D213/82 ,  C07D217/20 ,  C07D295/02 ,  C07D295/027 ,  C07D453/04 ,  C07F9/12 ,  C07F9/02 ,  A01N57/00 ,  A01N57/26 ,  A61K31/66 ,  A61K31/685 ,  C07F9/22 ,  C07F9/28

CPC classification number: C07D213/82 ,  A61K47/55 ,  C07C255/43 ,  C07D217/20 ,  C07D295/027 ,  C07D453/04 ,  C07F9/12

公开(公告)号：EP1485357A1

公开(公告)日：2004-12-15

申请号：EP03744359.5

申请日：2003-03-13

Applicant: DSM IP Assets B.V.

Inventor： PUENTENER, Kurt ,  SCALONE, Michelangelo ,  WANG, Shaoning

IPC: C07D217/20

CPC classification number: C07D217/20

Abstract: The asymmetrical hydrogenation of 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolinium salts to yield (S) or (R)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinolinium salts can be effected with superior optical yield by the use of an iridium or rhodium complex catalyst comprising a chiral dipohsphine ligand of the general formula (I) or (II), (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinoline and salts thereof are intermediate products in the manufacture of dextromethorphan, a known antitussive agent.

公开(公告)号：EP0929527B1

公开(公告)日：2004-10-27

申请号：EP97936381.9

申请日：1997-08-04

Applicant: Aventis Pharmaceuticals Inc.

Inventor： WATSON, Timothy, James-Norman

IPC: C07D217/06 ,  C07D221/20

CPC classification number: C07D217/20 ,  C07D217/06

Abstract: A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.

公开(公告)号：EP1383760A1

公开(公告)日：2004-01-28

申请号：EP02714555.6

申请日：2002-04-09

Applicant: FUJISAWA PHARMACEUTICAL CO., LTD. ,  DAISO CO., LTD.

Inventor： TAKASUGI, Hisashi,Fujisawa Pharmaceutical Co. Ltd ,  TERASAWA, Takeshi,Fujisawa Pharmaceutical Co. Ltd ,  INOUE, Yoshikazu,Fujisawa Pharmaceutical Co. Ltd ,  NAKAMURA, Hideko,Fujisawa Pharmaceutical Co. Ltd ,  NAGAYOSHI, Akira,Fujisawa Pharmaceutical Co. Ltd ,  FURUKAWA, Yoshiro,Daiso Co. Ltd ,  MIKAMI, Masafumi,Daiso Co. Ltd ,  HINOUE, Kazumasa,Daiso Co. Ltd ,  OHTSUBO, Makoto,Daiso Co. Ltd

IPC: C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  A61K31/395 ,  A61P3/06

CPC classification number: C07D207/335 ,  C07C271/24 ,  C07C2601/10 ,  C07C2602/08 ,  C07D209/44 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/50 ,  C07D213/56 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D217/04 ,  C07D217/18 ,  C07D217/20 ,  C07D233/64 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D277/24 ,  C07D277/28 ,  C07D277/40 ,  C07D277/46 ,  C07D277/48 ,  C07D295/033 ,  C07D295/135 ,  C07D295/15 ,  C07D295/155 ,  C07D295/192 ,  C07D295/205 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds of the formula (I) wherein X1 is wherein R?1, R2 and R10¿ are independently hydrogen or a suitable substituent; R?11 and R12¿ are independently hydrogen or a suitable substituent; R is unsaturated 5 to 6-membered heteromonocyclic group; A is direct bond or -NH-; X2 is monocyclic arylene, unsaturated 5 to 6-membered heteromonocyclic group or cycloalkenylene; Y is bivalent group selected from ethylene, trimethylene and vinylene, wherein CH2 is optionally replaced by NH or O, and CH is optionally replaced by N; and Z is -(CH¿2?)n-, -CO-(CH2)m-, -CH=CH- or -CO-NH-, wherein n is 1, 2 or 3 and m is 1 or 2, or a salt thereof. The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.

Abstract translation: 本发明涉及式（I）化合物，其中X 1是其中R 1，R 2和R 10独立地是氢或合适的取代基; R 11和R 12独立地是氢或合适的取代基; R是不饱和的5至6元杂单环基团; A是直接键或-NH-; X 2是单环亚芳基，不饱和5至6元杂单环基或环亚烯基; Y是选自乙烯，三亚甲基和亚乙烯基的二价基团，其中CH 2任选地被NH或O取代，CH任选地被N替代; Z为 - （CH 2）n - ， - CO - （CH 2）m - ， - CH = CH-或-CO-NH-，其中n为1,2或3，m为1或2， 。 本发明的化合物抑制载脂蛋白B（Apo B）分泌，并且可用作预防和治疗由ApoB升高的循环水平引起的疾病或病症的药物。