公开(公告)号：EP2141143A3

公开(公告)日：2010-05-05

申请号：EP09013103.8

申请日：2003-03-27

Applicant: Schering Corporation

Inventor： Wu, Wenxue ,  Liao, Hongbiao ,  Tsai, David, J. ,  Andrews, David, R. ,  Gala, Dinesh ,  Lee, Gary, M ,  Schwartz, Martin, Lawrence ,  McAllister, Timothy, L. ,  Fu, Xiaoyong ,  Maloney, Donal ,  Thiruvengadam, T., K. ,  Tann, Chou-Hang

IPC: C07C49/245 ,  C07C69/54 ,  C07C69/76

CPC classification number: C07D295/185 ,  C07B2200/07 ,  C07C45/512 ,  C07C67/343 ,  C07C309/73 ,  C07D295/088 ,  C07D295/092 ,  C07D295/192 ,  C07D295/205 ,  C07C49/255 ,  C07C69/734 ,  C07C49/84

Abstract: The invention relates to a process for preparing 4-trifluoromethyl methoxyacetophenone comprising:
(a) reacting the compound of Formula XIII with the compound of formula XIX to form the product of formula XX: and
(b) hydrolyzing the compound of formula XX to 4-trifluoromethyl methoxyacetophenone:

公开(公告)号：EP2155659A1

公开(公告)日：2010-02-24

申请号：EP08749469.6

申请日：2008-05-09

Applicant: Bayer Schering Pharma Aktiengesellschaft

Inventor： RUDOLPH, Joachim ,  DUMAS, Jaques ,  LI, Yingfu ,  AUCLAIR, Daniel ,  LOBELL, Mario ,  HITCHCOCK, Marion ,  HARTUNG, Ingo ,  KOPPITZ, Marcus ,  BRITTAIN, Dominic ,  PUEHLER, Florian ,  PETERSEN, Kirstin ,  GUENTHER, Judith ,  BADER, Benjamin

IPC: C07C217/92 ,  C07C233/65 ,  C07C255/59 ,  C07C271/16 ,  C07C307/10 ,  C07D211/22 ,  C07D317/22 ,  C07D497/04 ,  C07D295/088 ,  A61K31/136 ,  A61K31/4465 ,  A61K31/277 ,  A61K31/167 ,  A61K31/357 ,  A61K31/495

CPC classification number: C07D233/60 ,  C07C217/92 ,  C07C237/30 ,  C07C237/44 ,  C07C243/38 ,  C07C255/58 ,  C07C255/59 ,  C07C271/16 ,  C07C271/28 ,  C07C271/44 ,  C07C275/28 ,  C07C275/36 ,  C07C307/02 ,  C07C307/10 ,  C07C309/66 ,  C07C311/08 ,  C07C311/09 ,  C07C311/17 ,  C07C311/48 ,  C07C2601/08 ,  C07C2601/10 ,  C07D205/04 ,  C07D207/08 ,  C07D207/27 ,  C07D207/48 ,  C07D209/08 ,  C07D211/22 ,  C07D211/46 ,  C07D211/96 ,  C07D213/30 ,  C07D213/34 ,  C07D213/68 ,  C07D231/18 ,  C07D233/84 ,  C07D265/30 ,  C07D277/22 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  C07D317/22 ,  C07D317/64 ,  C07D327/04 ,  C07D403/12

Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper- proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract translation: 本发明涉及新的substituiertem苯氨基苯化合物，药物组合物含有受试化合物和用于治疗过度增殖和/或血管生成病症，作为唯一的药物或与其它活性成分组合使用这些化合物或组合物。

公开(公告)号：EP2142506A1

公开(公告)日：2010-01-13

申请号：EP08738388.1

申请日：2008-03-26

Applicant: Council of Scientific & Industrial Research

Inventor： KAMAL, Ahmed ,  PRASAD, Bandari, Rajendra

IPC: C07D213/74 ,  C07D239/42 ,  C07D239/94 ,  C07D311/74 ,  C07D471/04 ,  C07D295/088 ,  C07D295/15 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D295/15 ,  C07D213/74 ,  C07D239/42 ,  C07D239/94 ,  C07D295/088 ,  C07D311/74 ,  C07D471/04

Abstract: The present invention provides novel benzophenone hybrids as potential anticancer agents. More particularly, the present invention relates to N1-[4-chloro- 2-(2-chlorøbenzoyl)phenyl]-2-[4-(aryl) piperazinojacetamide with aliphatic chain length variations of formula (A).

公开(公告)号：EP2139850A1

公开(公告)日：2010-01-06

申请号：EP08748100.8

申请日：2008-04-09

Applicant: Methylgene, Inc.

Inventor： TESSIER, Pierre ,  LEIT, Silvana ,  SMIL, David ,  DÉZIEL, Robert ,  AJAMIAN, Alain ,  CHANTIGNY, Yves, Andre ,  DOMINGUEZ, Celia

IPC: C07C259/06 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33 ,  C07C311/19 ,  C07C323/50 ,  C07D521/00

CPC classification number: C07D307/79 ,  C07C259/06 ,  C07C275/42 ,  C07C311/08 ,  C07C311/21 ,  C07C323/52 ,  C07D205/04 ,  C07D207/263 ,  C07D207/337 ,  C07D209/08 ,  C07D209/44 ,  C07D211/34 ,  C07D211/46 ,  C07D211/52 ,  C07D211/64 ,  C07D211/76 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/74 ,  C07D215/26 ,  C07D219/04 ,  C07D231/14 ,  C07D233/84 ,  C07D235/16 ,  C07D235/28 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D249/06 ,  C07D267/20 ,  C07D277/36 ,  C07D277/74 ,  C07D285/12 ,  C07D295/088 ,  C07D295/155 ,  C07D295/192 ,  C07D295/205 ,  C07D295/26 ,  C07D311/84 ,  C07D317/50 ,  C07D333/24 ,  C07D401/04 ,  C07D401/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D491/10 ,  C07D513/04

Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.

Abstract translation: 本发明涉及用于抑制组蛋白脱乙酰酶的化合物。 更特别地，本发明提供式（I）的式化合物和其N-氧化物，水合物，溶剂合物，药学上可接受的盐，前药和复合物以及其外消旋和局部混合物，非对映异构体和对映异构体，其中基团L， M，X和Y如本文所定义。

公开(公告)号：EP1490346B1

公开(公告)日：2009-12-02

申请号：EP03733842.3

申请日：2003-03-27

Applicant: Schering Corporation

Inventor： WU, Wenxue ,  LIAO, Hongbiao ,  TSAI, David, J. ,  ANDREWS, David, R. ,  GALA, Dinesh ,  LEE, Gary, M. ,  SCHWARTZ, Martin, Lawrence ,  MCALLISTER, Timothy, L. ,  FU, Xiaoyong ,  MALONEY, Donal ,  THIRUVENGADAM, T., K. ,  TANN, Chou-Hang

IPC: C07D295/18 ,  C07D295/08 ,  C07B37/04

CPC classification number: C07D295/185 ,  C07B2200/07 ,  C07C45/512 ,  C07C67/343 ,  C07C309/73 ,  C07D295/088 ,  C07D295/092 ,  C07D295/192 ,  C07D295/205 ,  C07C49/255 ,  C07C69/734 ,  C07C49/84

Abstract: The present invention describes the synthesis of the following compounds in high stereochemical purity by a novel stereoselective alkylation of 2-methyl-4-protected piperazines using an inorganic base. (I)

公开(公告)号：EP2114869A1

公开(公告)日：2009-11-11

申请号：EP08727346.2

申请日：2008-01-02

Applicant: Boehringer Ingelheim International GmbH ,  Boehringer Ingelheim Pharma GmbH & Co. KG

Inventor： DAHMANN, Georg ,  HICKEY, Eugene, Richard ,  LI, Xiang ,  MAO, Wang ,  MARSHALL, Daniel, Richard ,  MORWICK, Tina, Marie ,  SIBLEY, Robert ,  SNOW, Roger, John ,  SORCEK, Ronald, John ,  WU, Frank ,  YOUNG, Erick, Richard, Roush

IPC: C07C237/42 ,  C07C275/42 ,  C07D217/22 ,  A61K31/167 ,  A61K31/277 ,  A61K31/472 ,  A61P9/10

CPC classification number: C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/42 ,  C07C323/62 ,  C07C2602/08 ,  C07D209/44 ,  C07D211/26 ,  C07D211/34 ,  C07D217/02 ,  C07D217/04 ,  C07D223/16 ,  C07D231/12 ,  C07D249/08 ,  C07D277/46 ,  C07D277/60 ,  C07D285/135 ,  C07D295/088 ,  C07D295/135 ,  C07D307/68 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

Abstract: Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.

Abstract translation: 描述了用作Rho激酶抑制剂的取代的酰胺和脲衍生物，所述抑制剂可用于治疗各种病症如心血管疾病，癌症，神经疾病，肾病，支气管哮喘，勃起功能障碍和青光眼。

公开(公告)号：EP1461038B9

公开(公告)日：2009-09-23

申请号：EP02772265.1

申请日：2002-09-04

Applicant: Actimis Pharmaceuticals, Inc.,

Inventor： LI, Yingfu ,  WATANABE, Akihiko ,  LOWINGER, Timothy, B. ,  BACON, Kevin ,  KAWAMURA, Norihiro ,  SHINTANI, Takuya ,  KIKUCHI, Tetsuo ,  MORIWAKI, Toshiya ,  URBAHNS, Klaus ,  FUKUSHIMA, Keiko ,  NUNAMI, Noriko ,  YOSHINO, Takashi ,  MURATA, Toshiki ,  YAMAUCHI, Megumi ,  YOSHINO, Hiroko

IPC: A61K31/445 ,  A61K31/496 ,  A61P11/06 ,  A61P37/00 ,  A61P29/00 ,  C07D295/22 ,  C07D471/04 ,  C07D211/58 ,  C07D243/06 ,  C07D211/28 ,  C07C311/18 ,  C07D211/96 ,  C07D307/14 ,  C07D207/14 ,  C07D213/71

CPC classification number: C07D213/70 ,  C07C311/29 ,  C07C323/67 ,  C07D207/14 ,  C07D207/48 ,  C07D209/08 ,  C07D211/28 ,  C07D211/58 ,  C07D211/96 ,  C07D213/65 ,  C07D213/71 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D241/04 ,  C07D241/06 ,  C07D243/08 ,  C07D257/04 ,  C07D295/088 ,  C07D295/13 ,  C07D295/194 ,  C07D295/26 ,  C07D307/14 ,  C07D333/38 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.

公开(公告)号：EP2090565A3

公开(公告)日：2009-09-09

申请号：EP09006377.7

申请日：2002-03-25

Applicant: Nisshinbo Industries, Inc.

Inventor： Sato, Takaya ,  Masuda, Gen ,  Nozu, Ryutaro ,  Maruo, Tatsuya

IPC: C07C217/08 ,  C07D295/08 ,  C07F9/54 ,  H01G9/038

CPC classification number: H01M6/166 ,  C07C217/08 ,  C07D295/088 ,  C07F9/5407 ,  H01G11/62 ,  H01G11/64 ,  H01M6/162 ,  H01M10/052 ,  H01M10/0566 ,  H01M10/0568 ,  H01M2300/0025 ,  Y02E60/13

Abstract: An ionic liquid of general formula (1) below, e.g. for use as an electrolyte salt or a liquid electrolyte for electrical storage devices.

In formula (1), R 1 to R 4 are each independently an alkyl group of 1 to 5 carbons or an alkoxyalkyl group of the formula R' -O- (CH 2 ) n -, with the proviso that at least one group from among R 1 to R 4 is the above alkoxyalkyl group, and two of the other groups form a ring. Y is a monovalent anion.

公开(公告)号：EP1819693B1

公开(公告)日：2009-08-26

申请号：EP05851697.2

申请日：2005-11-15

Applicant: ELI LILLY AND COMPANY

Inventor： FRANCISKOVICH, Jeffry, Bernard ,  HERRON, David, Kent ,  KLIMKOWSKI, Valentine, Joseph ,  MARQUART, Angela, Lynn ,  MASTERS, John, Joseph ,  MENDEL, David ,  RATZ, Andrew, Michael ,  SMITH, Gerald, Floyd ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC: C07D401/00 ,  C07D409/00 ,  C07D401/12 ,  C07D409/12 ,  C07D213/75 ,  C07D409/14 ,  C07C271/16 ,  C07C235/64 ,  A61K31/4465 ,  A61K31/4436 ,  A61P7/02

CPC classification number: C07D213/75 ,  C07C235/64 ,  C07C237/06 ,  C07C271/16 ,  C07C275/10 ,  C07C275/16 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07D211/22 ,  C07D211/46 ,  C07D295/088 ,  C07D295/192 ,  C07D295/205 ,  C07D295/215 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.

公开(公告)号：EP1795524A4

公开(公告)日：2009-08-05

申请号：EP05785275

申请日：2005-09-20

Applicant: ASTELLAS PHARMA INC

Inventor： HAYASHIBE SATOSHI ,  KANAYAMA TAKATOSHI ,  OHMORI JUNYA ,  TOBE TAKAHIKO ,  MAENO KYOICHI ,  SHITAKA YOSHITSUGU ,  SUZUKI JOTAROU ,  KAWABATA SHIGEKI ,  SHIRAISHI NOBUYUKI ,  YAMASAKI SHINGO ,  SUZUKI DAISUKE ,  HOSHII HIROAKI

IPC: C07C217/54 ,  A61K31/445 ,  A61P25/28 ,  C07D211/22

CPC classification number: C07C217/74 ,  C07C215/42 ,  C07C2601/08 ,  C07D211/22 ,  C07D295/088 ,  C07D307/94 ,  C07D319/14 ,  C07D401/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D413/04 ,  C07D453/02

Abstract: A compound useful as an NMDA antagonist having a wide safety region which is a therapeutic agent for Alzheimer's disease, vascular dementia (vascular agnosia), Parkinson's disease, ischemic apoplexy, and pains or a preventive agent for these. The compound is an amine derivative or salt thereof characterized by comprising an amine-containing structure (A) and a di- or tricyclic fused ring (indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[a]naphthalene, etc.) bonded to the structure (A) through X1 (a bond, lower alkylene, etc.). The NMDA antagonist contains the derivative or salt as an active ingredient.

Abstract translation: 本发明提供作为具有广泛安全性的NMDA拮抗剂的化合物，可用作治疗剂或阿尔茨海默氏病，脑血管性痴呆，帕金森病，缺血性中风，疼痛等的预防剂。具体地提供了胺衍生物或其盐 其特征在于其中含胺结构A与2-或3-环稠合环结合（例如，茚满，四氢萘酮，4,5,6,7-四氢苯并噻吩，4,5,6,7-四氢苯并呋喃， 8-二氢-6H-茚并[4,5-b]呋喃，2,3-二氢-1H-环戊二烯并[1]萘）通过X 1（键或低级亚烷基）; 和含有它作为其活性成分的NMDA拮抗剂。