公开(公告)号：EP2139487A2

公开(公告)日：2010-01-06

申请号：EP08744513.6

申请日：2008-03-27

申请人： Pharmacyclics, Inc.

发明人： HONIGBERG, Lee ,  VERNER, Erik ,  BUGGY, Joseph, J. ,  LOURY, David ,  CHEN, Wei

IPC分类号： A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61K31/519 ,  C07D253/06 ,  C07D487/04 ,  C07D473/34

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

摘要翻译： 本文描述的是不可逆的激酶抑制剂化合物，合成这种不可逆抑制剂的方法，以及使用这种不可逆抑制剂治疗疾病的方法。 本文进一步描述了用于确定蛋白质（包括激酶）的适当不可逆抑制剂的方法，测定和系统。

公开(公告)号：EP1523475B1

公开(公告)日：2009-12-23

申请号：EP03763692.5

申请日：2003-07-03

申请人： Sanofi-Aventis Deutschland GmbH

发明人： SCHOENAFINGER, Karl ,  DEFOSSA, Elisabeth ,  KADEREIT, Dieter ,  VON ROEDERN, Erich ,  KLABUNDE, Thomas ,  BURGER, Hans-Joerg ,  HERLING, Andreas ,  WENDT, Karl-Ulrich

IPC分类号： C07D211/62 ,  C07D249/08 ,  C07D257/04 ,  C07D271/10 ,  C07D253/06 ,  C07D231/26 ,  C07D307/68 ,  C07D235/18 ,  A61K31/17 ,  A61P3/10

CPC分类号： C07D211/60 ,  C07D211/62 ,  C07D231/12 ,  C07D231/26 ,  C07D233/56 ,  C07D235/18 ,  C07D249/08 ,  C07D249/12 ,  C07D253/07 ,  C07D257/04 ,  C07D271/10 ,  C07D271/113 ,  C07D307/68

摘要： The invention relates to heterocyclically substituted benzoylureas, in addition to their physiologically compatible salts and physiologically functional derivatives. The invention relates in particular to compounds of formula (I), in which the groups are defined as cited in the description, in addition to their physiologically compatible salts and to a method for producing said compounds. The compounds are suitable e.g. for treating type 2 diabetes.

公开(公告)号：EP1597242B1

公开(公告)日：2008-07-23

申请号：EP04708367.0

申请日：2004-02-05

申请人： Janssen Pharmaceutica NV

发明人： LEWI, Paulus Joannes ,  JANSSEN, Paul Adriaan, Jan ,  DE JONGE, Marc René ,  KOYMANS, Lucien Maria Henricus ,  VINKERS, Hendrik Maarten ,  DAEYAERT, Frederik Frans Desiré ,  HEERES, Jan ,  LEENDERS, Ruben Gerardus George ,  HOORNAERT, Georges Joseph Cornelius ,  KILONDA, Amuri ,  LUDOVICI, Donald W., Janssen Pharmaceutica Inc.

IPC分类号： C07D253/06 ,  A61K31/53

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D253/075

摘要： The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

公开(公告)号：EP1458692B1

公开(公告)日：2008-06-18

申请号：EP02807048.0

申请日：2002-12-18

申请人： Apotex Pharmachem Inc.

发明人： GUNTOORI, Bhaskar, Reddy ,  CHE, Daqing ,  MURTHY, Keshava, K., S.

IPC分类号： C07D253/06 ,  C07C277/08 ,  C07C281/18

CPC分类号： C07D253/075

摘要： A process for the manufacture of 3,5-diamino-kgg6-substituted-1,2,4-triazines is disclosed which comprises the steps of: (a) reacting a compound of formula (II): with aminoguanidine salts, (b) dehydrating the compound obtained to form a compound of formula (IV), and (c) cyclization of the compound of formula (IV) into a 3,5-diamino-6-substituted-1,2,4-triazine compound of formula (I) or into a hydrated form thereof.

公开(公告)号：EP1054875B1

公开(公告)日：2008-04-23

申请号：EP99902412.8

申请日：1999-01-22

申请人： Chemtura Corporation ,  Crompton Co./Cie

发明人： PARK, Sheldon, Bernard ,  MISHRA, Anupama ,  DEKEYSER, Mark, Achiel ,  MCDONALD, Paul, Thomas

IPC分类号： C07D273/04 ,  C07D285/16 ,  C07D253/06 ,  C07D413/04 ,  C07D498/04 ,  C07F9/6533 ,  A01N47/38 ,  A01N57/24

CPC分类号： C07D253/06 ,  A01N47/38 ,  A01N57/24 ,  C07D273/04 ,  C07D285/16 ,  C07D413/04 ,  C07F9/6533

摘要： Insecticidal dihydro-oxadiazine compounds having formula (I): wherein X is O, N or S; R is a substituted or unsubstituted phenyl or C4-C5 heterocyclic group; R?2, R3, R4, and R5¿ are one of the following: a) R?2, R3, and R4¿ are independently, hydrogen, alkyl, alkoxy, or furanyl; and R5 is nitro, cyano, alkyl, dialkylamino, alkylthio, alkoxy, haloalkoxy, phenoxy, phenylthio, or alkoxycarbonyl, wherein R?3 and R5¿ together can form a ring; or b) R?3, R4, and R5¿ are hydrogen; and R2 is alkylthio, alkylsulfinyl, alkylsulfonyl, nitroalkoxy, hydroxy, dialkoxyphosphinyl, cyano, acyloxy, alkoxy, haloalkoxy, cycloalkyl, or alkenyl; or R2 is a substituted or unsubstituted phenyl, phenylthio, phenylsulfinyl, phenylsulfonyl, pyrazolyl, furanyl, thienyl, phenylalkoxy, or benzoyloxy; and R6 is hydrogen alkyl, alkylthio, alkoxyalkyl, acyl, benzyl, or alkoxycarbonyl.

公开(公告)号：EP1881966A2

公开(公告)日：2008-01-30

申请号：EP06752194.8

申请日：2006-05-03

申请人： Dow AgroSciences LLC

发明人： SHABER, Steven Howard ,  MEYER, Kevin Gerald ,  NIYAZ, Noormohamed Mohamed ,  RIEDER, Brent Jeffrey ,  SULLENBERGER, Michael Thomas ,  SMITH, Frisby Davis ,  ERICKSON, William Randal ,  YAP, Maurice Chee Hoong

IPC分类号： C07D253/06 ,  C07D405/12 ,  C07D401/06 ,  C07D401/12 ,  C07D409/10 ,  C07D417/12 ,  C07D403/12 ,  C07D409/04 ,  C07D409/14 ,  C07F7/08 ,  A01N43/707 ,  A01N43/78

CPC分类号： C07D253/06 ,  A01N43/707 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D417/12 ,  C07F7/0812

摘要： This invention relates to substituted dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides.

公开(公告)号：EP1524974A4

公开(公告)日：2007-12-05

申请号：EP02807554

申请日：2002-05-06

申请人： PARATEK PHARM INNC

发明人： LEVY STUART B ,  ALEKSHUN MICHEAL N ,  PODLOGAR BRENT ,  OHEMENG KWASI ,  VERMA ATUL ,  WARCHOL TADEUSZ ,  BHATIA BEENA

IPC分类号： G01N33/50 ,  A61K31/341 ,  A61K31/352 ,  A61K31/40 ,  A61K31/407 ,  A61K31/409 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/429 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/551 ,  A61K31/553 ,  A61K31/555 ,  A61K31/7088 ,  A61K45/00 ,  A61K47/18 ,  A61K47/20 ,  A61K47/22 ,  A61K47/34 ,  A61K48/00 ,  A61P1/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/08 ,  A61P17/00 ,  A61P19/00 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  C07D235/08 ,  C07D235/22 ,  C07D243/10 ,  C07D253/06 ,  C07D261/20 ,  C07D307/60 ,  C07D311/30 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D491/052 ,  C07D498/04 ,  C07D498/14 ,  C07D513/04 ,  C12N15/09 ,  C12Q1/02 ,  G01N33/15 ,  A61K31/33 ,  A61K31/34 ,  A61K31/35 ,  A61K31/38 ,  A61K31/41 ,  A61K31/54

CPC分类号： A61K31/47 ,  A61K31/40 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/555

摘要： Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker under the control of a transcription factor responsive element and 2) a transcription factor, with a compound under conditions which allow interaction of the compound with the microbial cell; and measuring the ability of the compound to affect the growth or survival of the microbial cell as an indication of whether the test compound modulates the activity of a transcription factor.

公开(公告)号：EP1337150A4

公开(公告)日：2007-09-26

申请号：EP01273864

申请日：2001-10-26

申请人： DOW AGROSCIENCES LLC

发明人： KELLY MARTHA JEAN ,  EVANS KAREN ANDERSON ,  GALLAGHER JAMES JOSEPH ,  MULVIHILL MARK JOSEPH

IPC分类号： A01N43/707 ,  C07D253/06 ,  A01N43/64 ,  A01N43/90 ,  A01N47/06 ,  C07D253/07 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/06 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D253/06 ,  A01N43/64 ,  A01N43/707 ,  A01N43/90 ,  A01N47/06 ,  C07D253/07 ,  C07D487/04

摘要： This invention relates to dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides and insecticides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides and insecticides.

公开(公告)号：EP1581232A1

公开(公告)日：2005-10-05

申请号：EP03778700.9

申请日：2003-12-19

申请人： Pfizer Products Inc.

发明人： DOMBROSKI, Mark Anthony,c/o Pfizer Global R&D ,  DUPLANTIER, Allen Jacob,c/o Pfizer Global R&D

IPC分类号： A61K31/53 ,  C07D253/06 ,  C07D405/06 ,  C07D401/06

CPC分类号： C07D253/075 ,  C07D401/06 ,  C07D405/06

摘要： The present invention provides benzamide inhibitors of the P2X7 receptor of the formula (I), wherein R1 and R2 are as defined in claim 1. R3 is a nitrogen linked (C1-C10) heterocyclyl of formula (II), wherein R4 and R7 are as defined in claim 1. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

公开(公告)号：EP1559709A1

公开(公告)日：2005-08-03

申请号：EP05001823.3

申请日：1996-06-27

申请人： Eisai Co., Ltd.

发明人： Kikuchi, Kouichi c/o Eisai Co,Ltd Tsukuba Res Labs ,  Tagama, Katsuya ,  Yoshimura, Hiroyuki ,  Hibi, Shigeki c/o Eisai Co,Ltd Tsukuba Res Labs ,  Nagai, Mitsuo c/o Eisai Co,Ltd Tsukuba Res Labs ,  Abe, Shinya ,  Okita, Makoto ,  Hida, Takayuki c/o Eisai Co,Ltd Tsukuba Res Labs ,  Higashi, Seiko ,  Tokuhara, Naoki c/o Eisai Co,Ltd Tsukuba Res Labs ,  Kobayashi, Seiichi

IPC分类号： C07D209/08 ,  C07D213/80 ,  C07D231/14 ,  C07D241/42 ,  C07D241/44 ,  C07D253/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D403/04 ,  C07D409/04

CPC分类号： C07D401/04 ,  C07D209/14 ,  C07D231/12 ,  C07D241/24 ,  C07D241/44 ,  C07D249/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

摘要： Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I):
wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a -CONH- group or a group represented by the formula -CR 6 =CR 7 - in which R 6 and R 7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.

摘要翻译： 描述了由下式（I）表示的含杂环羧酸衍生物：其中A表示例如含有至少一个氮原子并可以具有取代基的杂芳基，B表示例如， 亚芳基，-CONH-基或由式-CR 6 = CR 7表示的基团，其中R 6和R 7表示H，低级烷基等，D 表示亚芳基，亚杂芳基等，n1表示0或1，M表示例如羟基或低级烷氧基; 或其生理上可接受的盐。 作为视黄酸相关化合物代替视黄酸，它允许为各种疾病提供预防和/或治疗。