公开(公告)号：EP2631235A2

公开(公告)日：2013-08-28

申请号：EP13157997.1

申请日：2011-08-26

Applicant: Meiji Seika Pharma Co., Ltd.

Inventor： Kagabu, Shinzo ,  Mitomi, Masaaki ,  Kitsuda, Shigeki ,  Horikoshi, Ryo ,  Nomura, Masahiro ,  Onozaki, Yasumichi

IPC: C07D401/12 ,  A01N43/40 ,  A01N43/60

CPC classification number: A01N43/40 ,  A01N37/18 ,  A01N43/50 ,  A01N43/54 ,  A01N43/58 ,  A01N43/78 ,  A01N47/02 ,  A01N47/12 ,  A01N47/40 ,  A01N57/32 ,  C07C233/05 ,  C07C233/12 ,  C07C261/04 ,  C07C271/12 ,  C07C311/09 ,  C07D211/98 ,  C07D213/36 ,  C07D213/40 ,  C07D213/42 ,  C07D213/61 ,  C07D213/75 ,  C07D237/08 ,  C07D277/32 ,  C07D333/20 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07F9/582 ,  C07F9/588

Abstract: Specific amine derivatives have been found to possess excellent activities as pest control agents.

Abstract translation: 已发现特定的胺衍生物作为害虫控制剂具有优异的活性。

公开(公告)号：EP2628389A1

公开(公告)日：2013-08-21

申请号：EP11821689.4

申请日：2011-08-26

Applicant: Meiji Seika Pharma Co., Ltd.

Inventor： KAGABU, Shinzo ,  MITOMI, Masaaki ,  KITSUDA, Shigeki ,  HORIKOSHI, Ryo ,  NOMURA, Masahiro ,  ONOZAKI, Yasumichi

IPC: A01N47/40 ,  A01N37/18 ,  A01N43/40 ,  A01N43/54 ,  A01N43/78 ,  A01N47/04 ,  A01N47/12 ,  A01N47/28 ,  A01N51/00 ,  A01N57/32 ,  A01P7/02 ,  A01P7/04 ,  A61K31/341 ,  A61K31/381 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/50

CPC classification number: A01N43/40 ,  A01N37/18 ,  A01N43/50 ,  A01N43/54 ,  A01N43/58 ,  A01N43/78 ,  A01N47/02 ,  A01N47/12 ,  A01N47/40 ,  A01N57/32 ,  C07C233/05 ,  C07C233/12 ,  C07C261/04 ,  C07C271/12 ,  C07C311/09 ,  C07D211/98 ,  C07D213/36 ,  C07D213/40 ,  C07D213/42 ,  C07D213/61 ,  C07D213/75 ,  C07D237/08 ,  C07D277/32 ,  C07D333/20 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07F9/582 ,  C07F9/588

Abstract: Specific amine derivatives have been found to possess excellent activities as pest control agents.

Abstract translation: 已经发现具体的胺衍生物具有优异的作为害虫防治剂的活性。

公开(公告)号：EP1888509B1

公开(公告)日：2013-05-15

申请号：EP06725391.4

申请日：2006-03-29

Applicant: BASF SE

Inventor： WITSCHEL, Matthias ,  ZAGAR, Cyrill ,  HUPE, Eike ,  KÜHN, Toralf ,  MOBERG, William Karl ,  PARRA RAPADO, Liliana ,  STELZER, Frank ,  VESCOVI, Andrea ,  REINHARD, Robert ,  SIEVERNICH, Bernd ,  GROSSMANN, Klaus ,  EHRHARDT, Thomas

IPC: C07C237/22 ,  C07C271/12 ,  C07C321/28 ,  C07C317/48 ,  A01N37/46 ,  C07D335/02 ,  C07D309/06 ,  C07D233/60 ,  C07D233/64 ,  C07D239/60 ,  C07C233/83

CPC classification number: C07C323/60 ,  A01N37/46 ,  C07C233/83 ,  C07C233/85 ,  C07C233/87 ,  C07C237/22 ,  C07C271/12 ,  C07C275/16 ,  C07C311/09 ,  C07C317/50 ,  C07C323/52 ,  C07C323/59 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D233/56 ,  C07D239/60 ,  C07D309/06 ,  C07D317/38 ,  C07D335/02 ,  C07F7/1852

公开(公告)号：EP2580201A2

公开(公告)日：2013-04-17

申请号：EP11736154.3

申请日：2011-06-10

Applicant: Rhodes Technologies

Inventor： GIGUERE, Joshua, R. ,  MCCARTHY, Keith, E. ,  REISCH, Helge, A. ,  SANDOVAL, Sergio ,  STYMIEST, Jake, L.

IPC: C07D265/30

CPC classification number: C07D489/08 ,  B01J23/42 ,  B01J23/44 ,  B01J31/1855 ,  B01J31/20 ,  B01J31/2295 ,  B01J31/2414 ,  B01J2231/40 ,  B01J2531/64 ,  B01J2531/821 ,  B01J2531/824 ,  B01J2531/828 ,  B01J2531/847 ,  C07C209/00 ,  C07C209/44 ,  C07C269/04 ,  C07D265/30 ,  C07D295/03 ,  C07D295/205 ,  Y02P20/55 ,  C07C211/21 ,  C07C271/12

Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.

Abstract translation: 本公开提供了用于第三cardamines的N-脱烷基化和使用的过渡金属催化剂的制备叔N-烯丙基胺衍生物和它们的仲胺衍生物的方法。 第三cardamines可以是生物碱，更具体地，第三cardamines可以是阿片样物质。 在具体的实施方案中，本公开提供了在使用过程中用于从东罂粟碱纳洛酮和纳曲酮的合成方法。

公开(公告)号：EP2496228A4

公开(公告)日：2013-04-10

申请号：EP10828500

申请日：2010-11-03

Applicant: SK BIOPHARMACEUTICALS CO LTD

Inventor： LEE SUNG JAMES ,  MELNICK SUSAN MARIE

IPC: A61K31/137 ,  A61K31/13 ,  A61P25/00 ,  A61P25/14

CPC classification number: C07C271/12 ,  A61K31/27

Abstract: The invention is directed to a method of treating attention-deficit/hyperactivity disorder (ADHD) in a subject, comprising administering a therapeutically effective amount of a carbamoyl compound, or pharmaceutically acceptable salt thereof.

公开(公告)号：EP2574188A1

公开(公告)日：2013-04-03

申请号：EP11783835.9

申请日：2011-05-19

Applicant: Targacept, Inc. ,  AstraZeneca AB

Inventor： DULL, Gary Maurice ,  GENUS, John ,  RATILAINEN, Tommi ,  RYBERG, Per Olof ,  HELLSTRÖM, Janna ,  WAHLSTRÖM, Niklas ,  WÄNNMAN, Thomas

IPC: C07C29/40 ,  C07C211/21 ,  C07C231/14 ,  C07D213/65

CPC classification number: C07D213/65 ,  C07C29/36 ,  C07C211/21 ,  C07C269/04 ,  C07C33/03 ,  C07C271/12

Abstract: An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.

公开(公告)号：EP2355851A4

公开(公告)日：2012-08-29

申请号：EP09825609

申请日：2009-11-10

Applicant: ALNYLAM PHARMACEUTICALS INC

Inventor： MANOHARAN MUTHIAH ,  JAYARAMAN MUTHUSAMY ,  RAJEEV KALLANTHOTTATHIL G ,  ELTEPU LAXMAN ,  ANSELL STEVEN ,  CHEN JIANXIN

IPC: A61K47/00 ,  A61K31/01

CPC classification number: A61K47/44 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  A61K2039/55555 ,  A61K2039/55561 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R 1 and R 2 are each independently for each occurrence optionally substituted C 10 -C 30 alkyl, optionally substituted C 10 -C 30 alkenyl, optionally substituted C 10 -C 30 alkynyl, optionally substituted C 10 -C 30 acyl, or -linker-ligand; R 3 is H, optionally substituted C 1 -C 10 alkyl, optionally substituted C 2 -C 10 alkenyl, optionally substituted C 2 -C 10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, É-aminoalkyls, É-(substituted)aminoalkyls, É-phosphoalkyls, É-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O=N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, É-aminoalkyl, É-(substituted)aminoalky, É-phosphoalkyl or É-thiophosphoalkyl.

公开(公告)号：EP2435402A2

公开(公告)日：2012-04-04

申请号：EP10726924.3

申请日：2010-05-26

Applicant: Novartis AG

Inventor： COPPOLA, Gary, Mark ,  IWAKI, Yuki ,  KARKI, Rajeshri, Ganesh ,  KAWANAMI, Toshio ,  KSANDER, Gary, Michael ,  MOGI, Muneto ,  SUN, Robert

IPC: C07C233/45 ,  C07C233/57 ,  C07C233/64 ,  A61K31/166 ,  A61K31/165

CPC classification number: A61K31/194 ,  A61K45/06 ,  C07C233/47 ,  C07C233/63 ,  C07C233/87 ,  C07C235/52 ,  C07C235/74 ,  C07C235/82 ,  C07C251/12 ,  C07C257/06 ,  C07C271/12 ,  C07C275/16 ,  C07C311/19 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D207/34 ,  C07D209/18 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D239/28 ,  C07D261/18 ,  C07D271/10 ,  C07D277/64 ,  C07D285/12 ,  C07D303/48 ,  C07D307/68 ,  C07D309/40 ,  C07D333/24 ,  C07D333/40

Abstract: The present invention provides a compound of formula I′; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式I'化合物; 或其药学上可接受的盐，其中R 1，R 2，R 3，X和n如本文所定义。 本发明还涉及制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：EP2224912A4

公开(公告)日：2012-01-04

申请号：EP08866209

申请日：2008-12-31

Applicant: TEKMIRA PHARMACEUTICALS CORP ,  UNIV BRITISH COLUMBIA ,  ALNYLAM PHARMACEUTICALS

Inventor： HOPE MICHAEL J ,  SEMPLE SEAN C ,  CHEN JIANXIN ,  MADDEN THOMAS D ,  MUI BARBARA ,  CULLIS PIETER R ,  CIUFOLINI MARCO A ,  WONG KIM F ,  MANOHARAN MUTHIAH ,  RAJEEV KALLANTHOTTATHIL G ,  SRINIVASULU MASUNU

IPC: A61K9/127 ,  A61K31/7088 ,  C07C229/30 ,  C07D317/28

CPC classification number: A61K31/7088 ,  A61K9/127 ,  A61K9/1275 ,  C07C215/10 ,  C07C217/08 ,  C07C217/28 ,  C07C219/08 ,  C07C229/12 ,  C07C271/12 ,  C07C323/25 ,  C07D317/28

公开(公告)号：EP2367571A1

公开(公告)日：2011-09-28

申请号：EP09825613.4

申请日：2009-11-10

Applicant: Alnylam Pharmaceuticals Inc.

Inventor： MANOHARAN, Muthiah ,  RAJEEV, Kallanthottathil, G. ,  JAYARAMAN, Muthusamy ,  BUTLER, David ,  NARAYANANNAIR, Jayaprakash, K. ,  MAIER, Martin ,  ELTEPU, Laxman

IPC: A61K47/00 ,  A61K31/01

CPC classification number: A61K47/44 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  A61K2039/55555 ,  A61K2039/55561 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32 ,  Y02A50/464

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R 1 and R 2 are each independently for each occurrence optionally substituted C 10 -C 30 alkyl, optionally substituted C 10 -C 30 alkenyl, optionally substituted C 10 -C 30 alkynyl, optionally substituted C 10 -C 30 acyl, or -linker-ligand; R 3 is H, optionally substituted C 1 -C 10 alkyl, optionally substituted C 2 -C 10 alkenyl, optionally substituted C 2 -C 10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, É-aminoalkyls, É-(substituted)aminoalkyls, É-phosphoalkyls, É-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O=N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, É-aminoalkyl, É-(substituted)aminoalky, É-phosphoalkyl or É-thiophosphoalkyl.

Abstract translation: 本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。 特别地，本发明提供具有以下结构的脂质：（式（I）或（XXXV））。