公开(公告)号：EP3194364B1

公开(公告)日：2020-11-04

申请号：EP15766217.2

申请日：2015-09-11

Applicant: Johnson Matthey Public Limited Company

Inventor： NEDDEN, Hans, Guenter ,  JURCIK, Vaclav ,  WILLS, Martin ,  HODGKINSON, Roy

IPC: C07C303/40 ,  C07C311/18 ,  C07C303/34 ,  C07F15/00 ,  C07C311/37 ,  C07C311/46

公开(公告)号：EP2888229A4

公开(公告)日：2016-03-30

申请号：EP13825992

申请日：2013-08-01

Applicant: MERCK SHARP & DOHME

Inventor： HARVEY ANDREW ,  AVERY THOMAS ,  PAUL DHARAM ,  RIPPER JUSTIN ,  HUFF BELINDA ,  SINGH RAJINDER ,  SCHAEFFER LAURENT ,  JOSEPH CHRISTOPHE ,  MORICE CHRISTOPHE ,  GIETHLEN BRUNO

IPC: C07C311/37 ,  A61K31/18 ,  A61K31/415 ,  C07C311/08 ,  C07C311/48 ,  C07C311/49 ,  C07D213/74 ,  C07D231/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/47 ,  C07D241/20 ,  C07D261/14 ,  C07D277/42

CPC classification number: C07C311/37 ,  C07C211/53 ,  C07C217/82 ,  C07C303/36 ,  C07C307/10 ,  C07C311/08 ,  C07C311/30 ,  C07C311/39 ,  C07C311/48 ,  C07C311/49 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/50 ,  C07D213/74 ,  C07D231/38 ,  C07D233/72 ,  C07D237/20 ,  C07D239/42 ,  C07D239/47 ,  C07D241/20 ,  C07D261/14 ,  C07D277/42 ,  C07D295/135 ,  C07D305/08 ,  C07F9/588

Abstract: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.

公开(公告)号：EP2890688A1

公开(公告)日：2015-07-08

申请号：EP13756110.6

申请日：2013-08-28

Applicant: Janssen Sciences Ireland UC

Inventor： VANDICK, Koen ,  LAST, Stefaan Julien ,  ROMBOUTS, Geert ,  VERSCHUEREN, Wim Gaston ,  RABOISSON, Pierre Jean-Marie Bernard

IPC: C07D309/14 ,  C07D231/14 ,  C07D333/46 ,  C07C311/37 ,  C07D295/26 ,  A61K31/18 ,  A61K31/277 ,  A61K31/351 ,  A61K31/4453 ,  A61K31/381 ,  A61P31/20 ,  A61P1/18 ,  A61K31/337 ,  A61K31/341 ,  A61K31/4164

CPC classification number: C07C311/37 ,  A61K31/18 ,  A61K31/337 ,  A61K31/34 ,  A61K31/341 ,  A61K31/351 ,  A61K31/397 ,  A61K31/401 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07C311/14 ,  C07C311/16 ,  C07C311/20 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/14 ,  C07D207/273 ,  C07D207/36 ,  C07D211/28 ,  C07D211/56 ,  C07D211/76 ,  C07D211/96 ,  C07D213/42 ,  C07D213/81 ,  C07D213/82 ,  C07D223/06 ,  C07D233/84 ,  C07D233/90 ,  C07D277/56 ,  C07D295/13 ,  C07D295/26 ,  C07D305/08 ,  C07D307/22 ,  C07D307/60 ,  C07D307/68 ,  C07D309/14 ,  C07D333/38 ,  C07D333/48 ,  C07D491/107 ,  C07D493/08

Abstract: Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R
1 , R
2 and R
4 have the meaning as defined herein. The present invention also relates to pharmaceutical compositions containing these inhibitors and to their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Abstract translation: 包括立体化学异构体形式的式（I）的HBV复制抑制剂及其盐，水合物，溶剂合物，其中B，R 1，R 2和R 4具有如本文所定义的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HBV治疗中单独使用或与其它HBV抑制剂组合的用途。

公开(公告)号：EP2888229A1

公开(公告)日：2015-07-01

申请号：EP13825992.4

申请日：2013-08-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： HARVEY, Andrew ,  AVERY, Thomas ,  PAUL, Dharam ,  RIPPER, Justin ,  HUFF, Belinda ,  SINGH, Rajinder ,  SCHAEFFER, Laurent ,  JOSEPH, Christophe ,  MORICE, Christophe ,  GIETHLEN, Bruno

IPC: C07C311/37 ,  C07D239/42 ,  C07D239/47 ,  C07D231/38 ,  C07D277/42 ,  C07D213/74 ,  C07D241/20 ,  C07D261/14 ,  C07C311/08 ,  C07D237/20 ,  C07C311/48 ,  C07C311/49 ,  A61K31/18 ,  A61K31/415

CPC classification number: C07C311/37 ,  C07C211/53 ,  C07C217/82 ,  C07C303/36 ,  C07C307/10 ,  C07C311/08 ,  C07C311/30 ,  C07C311/39 ,  C07C311/48 ,  C07C311/49 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/50 ,  C07D213/74 ,  C07D231/38 ,  C07D233/72 ,  C07D237/20 ,  C07D239/42 ,  C07D239/47 ,  C07D241/20 ,  C07D261/14 ,  C07D277/42 ,  C07D295/135 ,  C07D305/08 ,  C07F9/58

Abstract: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.

Abstract translation: 本发明涉及式（I）化合物，其具有说明书中所述的取代基，其用于α7烟碱乙酰胆碱受体（α7nAChR）的阳性调节。 本发明还涉及这些化合物在治疗或预防α7nAChR的阳性调节有利的广泛范围的疾病中的用途，包括神经变性和神经精神疾病以及神经性疼痛和炎性疾病。

公开(公告)号：EP2344451A4

公开(公告)日：2014-08-13

申请号：EP09812186

申请日：2009-09-02

Applicant: ACUCELA INC

Inventor： SCOTT IAN L ,  KUKSA VLADIMIR ALEKSANDROVICH ,  KUBOTA RYO ,  HONG FENG

IPC: C07C323/32 ,  A61K31/10 ,  A61K31/18 ,  A61P27/02 ,  C07C311/37 ,  C07C317/22 ,  C07C317/32 ,  C07C323/20 ,  C07C323/41 ,  C07C323/62

CPC classification number: C07C323/32 ,  C07B2200/05 ,  C07C311/37 ,  C07C317/22 ,  C07C317/32 ,  C07C323/20 ,  C07C323/41 ,  C07C323/62 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18

公开(公告)号：EP1997495B1

公开(公告)日：2013-01-02

申请号：EP08010543.0

申请日：2004-03-11

Applicant: Axikin Pharmaceuticals, Inc.

Inventor： Li, Yingfu ,  Bacon, Kevin ,  Sugimoto, Hiromi ,  Fukushima, Keiko ,  Hashimoto, Kentaro ,  Marumo, Makiko ,  Moriwaki, Toshiya ,  Nunami, Noriko ,  Tsuno, Naoki ,  Urbahns, Klaus ,  Yoshida, Nagahiro

IPC: A61K31/4965 ,  A61K31/439 ,  A61K31/4015 ,  A61K31/405 ,  A61K31/497 ,  C07C311/37 ,  C07D241/04 ,  C07D453/02 ,  C07D207/40 ,  C07D403/06 ,  C07D487/04 ,  C07D401/04 ,  C07D243/08 ,  C07D403/04 ,  C07D207/34

CPC classification number: C07D487/04 ,  A61K31/439 ,  C07C311/29 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/40 ,  C07D207/404 ,  C07D207/48 ,  C07D211/54 ,  C07D223/12 ,  C07D241/04 ,  C07D243/08 ,  C07D257/04 ,  C07D295/13 ,  C07D295/22 ,  C07D295/26 ,  C07D303/06 ,  C07D303/36 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D453/02 ,  C07D487/02 ,  C07D487/08

公开(公告)号：EP1828110B1

公开(公告)日：2009-04-08

申请号：EP05701921.8

申请日：2005-01-18

Applicant: Hovione Inter AG

Inventor： Mendes, Zita ,  Baptista, Joana ,  Martin, Dionisio ,  Heggie, William

IPC: C07C303/38 ,  C07C311/37 ,  C07C309/46 ,  A61K31/18

CPC classification number: C07C303/38 ,  C07B2200/07 ,  C07C303/08 ,  C07C303/22 ,  C07C309/49 ,  C07C311/37 ,  C07C309/88

Abstract: A process for producing tamsulosin of formula (I) and pharmaceutically acceptable addition salts, thereof comprises the steps of : a) Reacting compound R,R-[2-(4-methoxy-phenyl)-1-methyl-ethyl]-(1-phenyl-ethyl)-amine of formula (II) or a salt thereof (II) with chlorosulfonic acid with or without an organic solvent, to obtain compound R,R-2methoxy-5-[2-(1-phenyl-ethylamino)-propyl]-benzenesulfonic acid of formula (III) b) Hydrogenolysis of compound R,R-2-methoxy-5-[2-(1-phenyl-ethylamino)-propyl]- benzenesulfonic acid of formula III or a salt thereof carried out in an alcohol in the presence of a palladium catalyst using hydrogen or a source of hydrogen, to obtain compound R-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula (IV) c)Reacting primary amine R-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula (IV), or a salt thereof, with a compound of formula (V) wherein X represents an halogen atom selected from the group consisting of C1;Br and I, to obtain 5- [(2R)-2-[2-(2-ethoxy-phenoxy)-ethylamino]-propyl]-2-methoxy-benzenesulfonic acid compound of formula (VI) d) Reacting compound of formula (VI) with an halogenating agent, to obtain the corresponding sulfonylchloride of formula (VII). e)Reacting compound VII with ammonia to obtain compound I.

公开(公告)号：EP1692100A4

公开(公告)日：2007-11-21

申请号：EP04808357

申请日：2004-12-09

Applicant: CJ CORP

Inventor： CHO SEONG-HWAN ,  LIM DONG-KWON ,  LEE KWANG-HYEG ,  YOUN YONG-SIK ,  PARK CHOONG-SIL

IPC: C07C303/40 ,  C07C311/37 ,  C07C311/46

CPC classification number: C07C303/40 ,  C07B2200/07 ,  C07C311/46

Abstract: Provided is a method of preparing an optically pure compound having formula 1 or its salts. The method includes: reacting ®-2-(4-methoxy-3-aminosulfonyl-phenyl)-1-methylethylamine or its salts with a compound selected form the group consisting of chloroacetic acid, bromoacetic acid, fluoroacetic acid, iodoacetic acid, α-halogenoacetic acid anhydride, and α-halogenoacetyl halide in the presence of a base or an acylating agent.

公开(公告)号：EP1836162A2

公开(公告)日：2007-09-26

申请号：EP05858615.7

申请日：2005-08-23

Applicant: IDEXX Laboratories Inc

Inventor： MURTHY, Yerramilli, V., S., N.

IPC: C07C311/37 ,  C07C255/49

CPC classification number: C07C317/32 ,  C07B2200/07 ,  C07C233/18 ,  C07C235/08 ,  C07C311/37 ,  C07C311/46

Abstract: D-(threo)-1-aryl-2-disubstitutedacylamido-3-fluoro-1-propanol compounds compounds and analogues thereof (“Fenicol Compounds”), compositions comprising an effective amount of a Fenicol Compound, and methods for treating or preventing a bacterial infection in an animal comprising administering to an animal in need thereof an effective amount of a Fenicol Compound are disclosed.

公开(公告)号：EP1805138A1

公开(公告)日：2007-07-11

申请号：EP05796943.8

申请日：2005-10-18

Applicant: Pharmeste S.r.l.

Inventor： BARALDI, Pier Giovanni ,  BOREA, Pier Andrea ,  GEPPETTI, Pierangelo

IPC: C07C335/12 ,  C07C335/16 ,  C07C311/21 ,  C07C311/37 ,  A61K31/17 ,  A61K31/18

CPC classification number: C07C335/18 ,  C07C311/47 ,  C07C335/12 ,  C07C335/16

Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the 10 vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.