公开(公告)号：EP2268606A1

公开(公告)日：2011-01-05

申请号：EP09738022.4

申请日：2009-04-20

Applicant: F. Hoffmann-La Roche AG

Inventor： ANDJELKOVIC, Mirjana ,  CECCARELLI, Simona M. ,  CHOMIENNE, Odile ,  KAPLAN, Gerald Lewis ,  MATTEI, Patrizio ,  TILLEY, Jefferson Wright

IPC: C07C233/51 ,  C07C235/12 ,  C07C235/20 ,  C07C237/12 ,  C07C275/16 ,  C07D213/55 ,  C07D277/30 ,  C07D333/24 ,  A61K31/197 ,  A61K31/426 ,  A61K31/381 ,  A61K31/4406 ,  A61P9/12 ,  A61P3/06 ,  A61P3/08

CPC classification number: C07D213/56 ,  C07C237/12 ,  C07C275/16 ,  C07C317/44 ,  C07D277/30 ,  C07D333/24

Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula (I) wherein A
1 , A
2 , R
1 , m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新的4-二甲氨基丁酸衍生物及其药学上可接受的盐，其中A 1，A 2，R 1，m和n如说明书和权利要求中所定义。 这些化合物抑制肉碱棕榈酰转移酶（CPT）活性，特别是CPT2活性，并可用作药物。

公开(公告)号：EP1216980A4

公开(公告)日：2010-12-08

申请号：EP00962993

申请日：2000-09-29

Applicant: EISAI R&D MAN CO LTD

Inventor： SHINODA MASANOBU ,  EMORI EITA ,  MATSUURA FUMIYOSHI ,  KANEKO TOSHIHIKO ,  OHI NORIHITO ,  KASAI SHUNJI ,  YOSHITOMI HIDEKI ,  YAMAZAKI KAZUTO ,  MIYASHITA SADAKAZU ,  HIBARA TARO ,  SEIKI TAKASHI ,  CLARK RICHARD ,  HARADA HITOSHI

IPC: C07C59/66 ,  C07C59/68 ,  C07C233/51 ,  C07C233/55 ,  C07C233/87 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C235/60 ,  C07C235/78 ,  C07C235/84 ,  C07C255/57 ,  C07D209/14 ,  C07D209/42 ,  C07D213/30 ,  C07D213/55 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D215/04 ,  C07D217/26 ,  C07D231/14 ,  C07D233/90 ,  C07D239/52 ,  C07D241/24 ,  C07D261/18 ,  C07D263/26 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D277/34 ,  C07D277/56 ,  C07D307/54 ,  C07D307/79 ,  C07D333/24 ,  C07D401/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D213/30 ,  C07C59/66 ,  C07C59/68 ,  C07C233/51 ,  C07C233/55 ,  C07C233/87 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C235/60 ,  C07C235/78 ,  C07C235/84 ,  C07C255/57 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/14 ,  C07D209/42 ,  C07D213/55 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D215/04 ,  C07D217/26 ,  C07D231/14 ,  C07D233/90 ,  C07D239/52 ,  C07D241/24 ,  C07D261/18 ,  C07D263/26 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D277/34 ,  C07D277/56 ,  C07D307/54 ,  C07D307/79 ,  C07D333/24 ,  C07D401/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

公开(公告)号：EP2208721A1

公开(公告)日：2010-07-21

申请号：EP08854528.0

申请日：2008-10-27

Applicant: Zhejiang Hisun Pharmaceutical Co. Ltd. ,  Central South University

Inventor： YU, Niefang ,  LIU, Xiaoyu ,  HU, Xiaodong

IPC: C07C259/06 ,  C07C233/51 ,  A61K31/16 ,  A61P35/00

CPC classification number: C07C323/63 ,  C07C259/06 ,  C07C275/42 ,  C07C311/07 ,  C07C335/22 ,  C07D213/53 ,  C07D333/20

Abstract: The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.

Abstract translation: 本发明涉及由式（I）表示的化合物或包含至少一种这样的化合物的组合物，其是组蛋白脱乙酰酶的抑制剂。 这些化合物的详细描述在说明书中公开。 这些化合物和包含其的组合物可用作治疗增殖性疾病的药物以及涉及与组蛋白脱乙酰酶（HDAC）活性的酶有关或与之相关的其它疾病。

公开(公告)号：EP1280770B1

公开(公告)日：2010-06-23

申请号：EP01917102.4

申请日：2001-03-21

Applicant: Bayer Aktiengesellschaft

Inventor： RUTHER, Michael ,  HAGEMANN, Hermann ,  SCHNEIDER, Udo ,  DOLLINGER, Markus ,  DAHMEN, Peter ,  WACHENDORFF-NEUMANN, Ulrike ,  FISCHER, Reiner ,  GRAFF, Alan ,  BRETSCHNEIDER, Thomas ,  ERDELEN, Christoph ,  DREWES, Mark, Wilhelm ,  FEUCHT, Dieter ,  LIEB, Folker

IPC: C07D207/38 ,  C07D209/54 ,  C07D491/10 ,  A01N43/36 ,  A01N43/38 ,  A01N43/90 ,  C07C233/51 ,  C07D309/14 ,  C07C233/52 ,  A01N43/12 ,  C07D307/94 ,  C07C69/757 ,  C07D309/38 ,  A01N43/16 ,  C07C49/733 ,  A01N35/06

CPC classification number: C07D491/10 ,  A01N43/06 ,  A01N43/12 ,  A01N43/16 ,  A01N43/36 ,  A01N43/38 ,  A01N43/90 ,  A01N47/06 ,  C07C45/46 ,  C07C49/657 ,  C07C49/747 ,  C07C69/013 ,  C07C69/612 ,  C07C69/738 ,  C07C69/757 ,  C07C233/51 ,  C07D207/38 ,  C07D209/54 ,  C07D307/94 ,  C07D309/14 ,  C07D309/38 ,  C07F7/0818

Abstract: The invention relates to novel C2 phenyl-substituted cyclic keto-enols of formula (I), in which W, X, Y, Z and CKE have the meanings as cited in the description. The invention also relates to methods for producing said C2 phenyl-substituted cyclic keto-enols and to their use as pesticides and herbicides.

公开(公告)号：EP1471881B1

公开(公告)日：2008-10-15

申请号：EP03715039.8

申请日：2003-01-22

Applicant: SOCIETE D'EXPLOITATION DE PRODUITS POUR LES INDUSTRIES CHIMIQUES, S.E.P.P.I.C.

Inventor： STOLTZ, Corinne ,  GARCIA, Christine

IPC: A61K8/44 ,  A61K31/41 ,  A61K31/55 ,  A61Q17/04 ,  A61Q19/02 ,  C07C233/49 ,  C07C233/51

CPC classification number: C07C233/51 ,  A61K8/44 ,  A61K31/00 ,  A61K31/41 ,  A61K31/55 ,  A61K2800/782 ,  A61Q17/04 ,  A61Q19/02 ,  C07C233/49

Abstract: Use of a compound inactivating the kinase A protein in a composition containing a cosmetically acceptable medium in order to lighten the skin, particularly a compound of formula (I) or the salts thereof, where R1 represents the characterizing chain of a fatty acid, comprising 3-30 carbon atoms; R2 represents the characterizing chain of an amino acid and m ranges from 1-50; or a mixture of said compounds or the salts thereof. A method for non-therapeutic treatment of the skin in order to lighten the skin by administering a composition containing a cosmetically acceptable medium and an effective amount of at least one compound inactivating the kinase A protein. A pharmaceutical composition for carrying out therapeutic treatment of the skin in order to lighten the skin, containing a cosmetically acceptable medium and an effective amount of at least one compound inactivating the kinase A protein. A compound of formula (Ia).

公开(公告)号：EP1592665A4

公开(公告)日：2007-07-18

申请号：EP04709299

申请日：2004-02-09

Applicant: SHENZHEN CHIPSCREEN BIOSCIENCE

Inventor： LU XIAN-PING ,  LI ZHIBIN ,  XIE AIHUA ,  LI BOYU ,  NING ZHIQIANG ,  SHAN SONG ,  DENG TUO ,  HU WEIMING

IPC: A61K20060101 ,  A61K31/165 ,  A61K31/277 ,  A61K31/44 ,  A61K31/4406 ,  A61P17/06 ,  A61P35/00 ,  C07C233/51 ,  C07C237/40 ,  C07C237/42 ,  C07D213/56

CPC classification number: C07D213/56 ,  C07C233/51 ,  C07C237/42

Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis.

公开(公告)号：EP1664048A2

公开(公告)日：2006-06-07

申请号：EP04768367.7

申请日：2004-09-06

Applicant: Alizyme Therapeutics Limited

Inventor： PALMER, Richard, Michael, John Alizyme ,  MEYERS, Nicholas, Leslie Alizyme Therapeutics ,  KNIGHT, John

IPC: C07D471/08 ,  C07C233/51 ,  A61K31/439 ,  A61P1/00

CPC classification number: C07D471/08 ,  C07C231/12 ,  C07C233/54

Abstract: The present invention relates to an improved process for the production of [(±)-endo]-4-amino-5-chloro-2-methoxy-N-(I-azabicyclo[3.3. 1]non-4-yl)benzamide hydrochloride, and intermediates thereof.

公开(公告)号：EP1285908A4

公开(公告)日：2005-09-21

申请号：EP01932262

申请日：2001-05-25

Applicant: KYORIN SEIYAKU KK

Inventor： MIYACHI HIROYUKI ,  NOMURA MASAHIRO ,  TAKAHASHI YUKIE ,  TANASE TAKAHIRO ,  MURAKAMI KOUJI ,  SUZUKI MASAHIRO

IPC: A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C59/68 ,  C07C69/734 ,  C07C69/738 ,  C07C229/34 ,  C07C233/51 ,  C07C233/55 ,  C07C233/87 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C251/48 ,  C07C323/56 ,  A61K31/192 ,  C07C233/81 ,  C07C235/44 ,  C07C235/78

CPC classification number: C07C59/68 ,  C07C69/734 ,  C07C69/738 ,  C07C229/34 ,  C07C233/51 ,  C07C233/55 ,  C07C233/87 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C251/48 ,  C07C323/56

Abstract: Novel substituted phenylpropionic acid derivatives of the general formula (1), which bind to human peroxisome proliferator activated receptor alpha (PPAR alpha ) as ligand to activate the receptor and thereby exhibit a potent lipid-decreasing effect; and use thereof as drugs: (1) wherein R is lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, optionally substituted phenyl, optionally substituted phenoxy, or optionally substituted benzyloxy; R is hydrogen, lower alkyl, or lower alkoxy; R is lower alkoxy; and A is -CH2CONH-, -NHCOCH2-, -CH2CH2CO-, CH2CH2CH2-, -CH2CH2O-, -CONHCH2-, -CH2NHCH2-, -COCH2O-, -OCH2CO-, -COCH2NH-, or NHCH2CO-.

公开(公告)号：EP1309575B1

公开(公告)日：2005-06-08

申请号：EP01965314.6

申请日：2001-08-03

Applicant: Galderma Research & Development

Inventor： BERNARDON, Jean-Michel ,  CLARY, Laurence

IPC: C07D277/34 ,  C07C235/52 ,  A61K31/195 ,  C07D207/40 ,  C07C237/22 ,  A61K31/21 ,  C07D417/12 ,  A61K31/426 ,  A61K31/16 ,  C07C233/87 ,  A61K31/427 ,  A61P17/00 ,  C07C233/51 ,  A61K31/4015

CPC classification number: A61K8/49 ,  A61K8/42 ,  A61K8/44 ,  A61K2800/70 ,  A61Q19/00 ,  C07C233/47 ,  C07C233/51 ,  C07C233/87 ,  C07C237/22 ,  C07C259/06 ,  C07D207/40 ,  C07D237/22 ,  C07D277/20 ,  C07D277/34 ,  C07D417/12

公开(公告)号：EP0817643A4

公开(公告)日：2004-10-06

申请号：EP96913778

申请日：1996-04-01

Applicant: EMISPHERE TECH INC

Inventor： LEONE-BAY ANDREA ,  HO KOC-KAN ,  SARUBBI DONALD J ,  MILSTEIN SAM J ,  PRESS JEFFERY BRUCE

IPC: C07D295/20 ,  A61K9/00 ,  A61K9/08 ,  A61K9/16 ,  A61K9/20 ,  A61K9/48 ,  A61K31/197 ,  A61K31/198 ,  A61K31/40 ,  A61K31/44 ,  A61K38/00 ,  A61K38/04 ,  A61K38/11 ,  A61K38/21 ,  A61K38/22 ,  A61K38/23 ,  A61K38/27 ,  A61K38/28 ,  A61K38/29 ,  A61K39/00 ,  A61K39/395 ,  A61K45/00 ,  A61K47/12 ,  A61K47/16 ,  A61K47/18 ,  A61K47/20 ,  A61K47/22 ,  A61K47/48 ,  C07C53/126 ,  C07C53/134 ,  C07C229/08 ,  C07C229/10 ,  C07C229/42 ,  C07C231/12 ,  C07C233/34 ,  C07C233/47 ,  C07C233/48 ,  C07C233/51 ,  C07C233/52 ,  C07C233/54 ,  C07C233/55 ,  C07C233/63 ,  C07C233/81 ,  C07C233/83 ,  C07C233/84 ,  C07C233/87 ,  C07C235/24 ,  C07C235/34 ,  C07C235/38 ,  C07C235/40 ,  C07C235/52 ,  C07C235/56 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C235/78 ,  C07C235/82 ,  C07C235/84 ,  C07C237/22 ,  C07C237/40 ,  C07C237/42 ,  C07C239/06 ,  C07C239/08 ,  C07C259/06 ,  C07C271/22 ,  C07C303/22 ,  C07C303/40 ,  C07C309/59 ,  C07C311/19 ,  C07D207/34 ,  C07D207/416 ,  C07D213/75 ,  C07D213/81 ,  C07D295/215 ,  C07D317/68 ,  C07D333/38 ,  C07C57/26 ,  C07C57/30 ,  C07C59/205 ,  C07C59/76

CPC classification number: C07D213/81 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0056 ,  A61K9/1617 ,  A61K9/4858 ,  A61K38/212 ,  A61K38/23 ,  A61K38/27 ,  A61K38/29 ,  A61K47/18 ,  A61K47/183 ,  A61K47/20 ,  A61K47/22 ,  A61K47/541 ,  C07C233/34 ,  C07C233/47 ,  C07C233/48 ,  C07C233/51 ,  C07C233/52 ,  C07C233/54 ,  C07C233/55 ,  C07C233/63 ,  C07C233/81 ,  C07C233/83 ,  C07C233/84 ,  C07C233/87 ,  C07C235/24 ,  C07C235/34 ,  C07C235/38 ,  C07C235/40 ,  C07C235/52 ,  C07C235/60 ,  C07C235/64 ,  C07C235/82 ,  C07C237/22 ,  C07C237/40 ,  C07C237/42 ,  C07C259/06 ,  C07C271/22 ,  C07C309/59 ,  C07C311/19 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D207/34 ,  C07D295/215 ,  C07D317/68 ,  C07D333/38