公开(公告)号：EP2139852A1

公开(公告)日：2010-01-06

申请号：EP07849595.9

申请日：2007-12-19

申请人： Pharmos Corporation

发明人： YACOVAN, Avihai ,  ALROY, Iris ,  AIZIKOVICH, Alexander ,  MIRILASHVILI, Sima ,  GRYNSZPAN, Flavio

IPC分类号： C07C311/39 ,  A61K31/18 ,  A61P29/00 ,  C07C311/40 ,  C07C311/48 ,  C07C311/51 ,  C07D207/48 ,  C07D209/08 ,  C07D213/42 ,  C07D213/74 ,  C07D217/02 ,  C07D231/38 ,  C07D239/52 ,  C07D295/12 ,  C07D307/14 ,  C07D307/52 ,  C07D309/04 ,  C07D317/58 ,  C07D319/18 ,  C07D405/12 ,  C07D471/08

CPC分类号： C07C311/39 ,  C07C311/40 ,  C07C311/48 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07C2603/74 ,  C07D209/08 ,  C07D209/48 ,  C07D213/38 ,  C07D213/42 ,  C07D217/04 ,  C07D231/38 ,  C07D295/12 ,  C07D295/13 ,  C07D295/22 ,  C07D307/14 ,  C07D307/52 ,  C07D317/58 ,  C07D319/18 ,  C07D405/12 ,  C07D471/08

摘要： The present invention relates to sulfonamide derivatives of formula (I) (wherein R1, R2, R3, R3', R4and R5are as defined in the claims), to pharmaceutical compositions comprising the same, and to uses thereof. Compounds of the invention have a common wide range of beneficial therapeutic indications. In particular, compounds of the invention are useful analgesic and anti-inflammatory agents.

摘要翻译： 本发明提供了本文定义的式（I）的磺酰胺化合物，含有其的药物组合物和使用这些化合物和药物组合物的治疗方法。 这些化合物具有普遍广泛的有益治疗适应症，特别是作为止痛剂和抗炎剂。

公开(公告)号：EP1644324B1

公开(公告)日：2009-09-30

申请号：EP04739792.2

申请日：2004-06-11

申请人： Bayer CropScience AG

发明人： PAZENOK, Sergiy ,  FORD, Mark, James ,  SCHLEGEL, Günter

IPC分类号： C07C303/40 ,  C07C311/51

CPC分类号： C07C303/40 ,  C07C311/51

摘要： The invention relates to a process for the preparation of a compound of formula (1) which comprises reaction of a compound of formula (II) with a compound of the formula (III) in the presence of a chlorinating agent, followed by reaction of the resultant compound of the formula (IV) with a compound of formula (V) in the presence of a base wherein the various symbols are as defined in claim 1.

公开(公告)号：EP1615629B1

公开(公告)日：2009-03-18

申请号：EP03719773.8

申请日：2003-04-16

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： CHRISTENSEN, Siegfried, B., IV ,  CUMMINGS, Maxwell, D. ,  LEE, Jinhwa ,  XIANG, Jia-ning

IPC分类号： C07C311/51 ,  C07D213/71 ,  A61K31/18 ,  A61K31/24 ,  A61K31/235 ,  A61K31/44 ,  A61P31/04

CPC分类号： C07C311/51 ,  C07D213/70

摘要： Novel PDF inhibitors and novel methods for their use are provided.

公开(公告)号：EP1888519A2

公开(公告)日：2008-02-20

申请号：EP06840910.1

申请日：2006-05-19

申请人： F.HOFFMANN-LA ROCHE AG

发明人： BOYD, Edward ,  BROOKFIELD, Frederick ,  GRIDLEY, Jonathan ,  KOERNER, Matthias ,  KUBBIES, Manfred ,  LAU, Raymond ,  REIFF, Ulrike ,  TIEFENTHALER, Georg ,  VON DER SAAL, Wolfgang ,  WOODCOCK, Timothy

IPC分类号： C07C311/51 ,  C07C303/40 ,  A61K31/18

CPC分类号： C07C311/51

摘要： Objects of the present invention are the compounds of formula (I) Their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.

公开(公告)号：EP1726580A4

公开(公告)日：2008-02-13

申请号：EP05721059

申请日：2005-03-14

申请人： TAKEDA PHARMACEUTICAL

发明人： YASUMA TSUNEO ,  NEGORO NOBUYUKI ,  SASAKI SHINOBU

IPC分类号： C07C229/42 ,  A61K31/16 ,  A61K31/195 ,  A61K31/222 ,  A61K31/337 ,  A61K31/343 ,  A61K31/382 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/4152 ,  A61K31/42 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/5375 ,  A61P3/10 ,  A61P43/00 ,  C07C233/18 ,  C07C233/53 ,  C07C235/06 ,  C07C259/06 ,  C07C309/66 ,  C07C311/21 ,  C07C311/51 ,  C07C317/18 ,  C07C317/32 ,  C07C323/12 ,  C07D207/27 ,  C07D207/404 ,  C07D209/08 ,  C07D209/14 ,  C07D211/46 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D213/76 ,  C07D215/06 ,  C07D215/12 ,  C07D231/12 ,  C07D231/22 ,  C07D231/24 ,  C07D261/08 ,  C07D277/28 ,  C07D295/18 ,  C07D305/06 ,  C07D307/79 ,  C07D335/02 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/18 ,  C07F9/40

CPC分类号： C07C311/21 ,  C07C229/42 ,  C07C309/66 ,  C07C311/51 ,  C07C317/18 ,  C07C317/32 ,  C07C323/12 ,  C07C2601/02 ,  C07C2602/08 ,  C07D213/74 ,  C07D215/06 ,  C07D231/24 ,  C07D277/28 ,  C07D307/79 ,  C07D409/12 ,  C07D417/12 ,  C07F9/4006

摘要： A compound represented by the formula (1) (wherein the symbols are the same as defined in the description), a salt thereof, and a prodrug thereof. They unexpectedly have excellent GPR40 receptor agonistic activity and are excellent in properties required of medicines, such as stability. They can be a medicine which is safe and useful as a preventive/therapeutic agent for pathological states or diseases in which a GPR40 receptor participates, such as diabetes.

摘要翻译： 由式（1）（其中符号与说明书中定义的相同）代表的化合物，其盐及其前药。 它们意外地具有优异的GPR40受体激动剂活性，并且在稳定性等药物所需的性能方面优异。 它们可以是安全有用的药物，作为GPR40受体参与的病理状态或疾病（例如糖尿病）的预防/治疗剂。

公开(公告)号：EP1127869A4

公开(公告)日：2007-05-02

申请号：EP99954398

申请日：1999-11-05

申请人： TOYAMA CHEMICAL CO LTD

发明人： CHAKI HISAAKI ,  TAKAKURA TADAKAZU ,  TSUCHIDA KEIICHI ,  YOKOTANI JUNICHI ,  KOTSUBO HIRONORI ,  AIKAWA YUKIHIKO ,  HIRONO SHUICHI ,  SHIOZAWA SHUNICHI

IPC分类号： C07D277/60 ,  A01N63/00 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/495 ,  A61K38/00 ,  A61K45/00 ,  A61P19/02 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07C59/64 ,  C07C59/84 ,  C07C59/90 ,  C07C65/24 ,  C07C65/34 ,  C07C65/36 ,  C07C65/38 ,  C07C65/40 ,  C07C69/618 ,  C07C69/738 ,  C07C69/767 ,  C07C69/78 ,  C07C69/94 ,  C07C229/34 ,  C07C233/01 ,  C07C233/47 ,  C07C235/16 ,  C07C235/20 ,  C07C235/84 ,  C07C251/32 ,  C07C251/40 ,  C07C251/48 ,  C07C251/60 ,  C07C255/49 ,  C07C275/24 ,  C07C311/06 ,  C07C311/51 ,  C07D207/04 ,  C07D207/08 ,  C07D207/32 ,  C07D207/333 ,  C07D209/18 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D213/50 ,  C07D235/26 ,  C07D241/08 ,  C07D401/10 ,  C07D401/14 ,  C07K7/06 ,  C07K7/64 ,  C07C69/73 ,  C07C205/49

CPC分类号： C07D207/333 ,  A61K38/00 ,  C07C59/64 ,  C07C59/84 ,  C07C65/24 ,  C07C65/34 ,  C07C65/36 ,  C07C65/38 ,  C07C65/40 ,  C07C69/738 ,  C07C69/94 ,  C07C229/34 ,  C07C233/01 ,  C07C233/47 ,  C07C235/20 ,  C07C235/84 ,  C07C251/32 ,  C07C251/48 ,  C07C251/60 ,  C07C255/49 ,  C07C275/24 ,  C07C311/06 ,  C07C311/51 ,  C07D207/08 ,  C07D209/42 ,  C07D235/26 ,  C07D277/60 ,  C07K7/06 ,  C07K7/64 ,  Y02P20/55

摘要： Compounds represented by formula (I) wherein N1 represents an atom to which a donor hydrogen atom in a hydrogen bond donor group is bonded or a hydrogen bond acceptor atom in a hydrogen bond acceptor group; N3 represents a hydrogen bond acceptor atom in a hydrogen bond acceptor group; and N2, N4 and N5 represent each an arbitrary carbon atom constituting a hydrophobic group; having an atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 among the five atoms constituting a pharmacophore specified by the interatomic distances among N1, N2, N3, N4 and N5; and, in the optimized stereochemical structure thereof, the interatomic distances between the atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 fall within the scope of the pharmacophore interatomic distance, or salts thereof. Because of having an effect of inhibiting the activity of a transcription factor AP-1, these compounds are useful as preventives/remedies for diseases in which the excessive expression of AP-1 participates and as AP-1 inhibitors.

公开(公告)号：EP1334966A4

公开(公告)日：2007-04-18

申请号：EP01976719

申请日：2001-10-17

申请人： TAKEDA PHARMACEUTICAL

发明人： IKEMOTO TOMOMI ,  NISHIGUCHI ATSUKO ,  TOMIMATSU KIMINORI

IPC分类号： C07C303/40 ,  C07C311/51 ,  C07B57/00 ,  C07C303/44 ,  C07C311/14 ,  C07C311/28

CPC分类号： C07C311/51 ,  C07B2200/07 ,  C07C303/40 ,  C07C303/44 ,  C07C311/14 ,  C07C2601/16

摘要： A process for preparing a diastereomer of a compound represented by the general formula (I) wherein the asymmetric carbon atom of R1 or R2 takes R- or S-configuration, or a salt thereof, characterized by resolving a mixture of diastereomers of the compound or salts of them: (I) wherein R?1 and R2¿ are each independently optionally substituted hydrocarbyl or an optionally substituted heterocyclic group, with the proviso that only one of R?1 and R2¿ contains one asymmetric carbon atom; and Ra is an optically active hydrocarbon group which may be substituted or an optically active heterocyclic group which may be substituted.

公开(公告)号：EP1615629A4

公开(公告)日：2007-02-28

申请号：EP03719773

申请日：2003-04-16

申请人： CHRISTENSEN SIEGFRIED B IV ,  CUMMINGS MAXWELL D ,  LEE JINHWA ,  XIANG JIA NING ,  SMITHKLINE BEECHAM CORP

发明人： CHRISTENSEN SIEGFRIED B IV ,  CUMMINGS MAXWELL D ,  LEE JINHWA ,  XIANG JIA-NING

IPC分类号： C07C311/51 ,  A61K31/18 ,  A61K31/235 ,  A61K31/24 ,  A61K31/44 ,  A61P31/04 ,  C07D213/70 ,  C07D213/71

CPC分类号： C07C311/51 ,  C07D213/70

摘要： Novel PDF inhibitors and novel methods for their use are provided.

公开(公告)号：EP1708700A1

公开(公告)日：2006-10-11

申请号：EP04806386.1

申请日：2004-12-13

申请人： Pharmacia Corporation

发明人： WADHWA, Manpreet Vick S.

IPC分类号： A61K31/42 ,  C07D261/08 ,  C07C311/51 ,  A61P25/04

CPC分类号： A61K31/42 ,  C07D261/08

摘要： Compounds having the structure MgX1X2, wherein X1 is parecoxib anion and X2 is as selected from the group consisting of parecoxib anion, chloride, bromide, sulfate, phosphate, nitrate, acetate, propionate, succinate, glycolate, stearate, lactate, malate, tartrate, citrate, ascorbate, glutamate, benzoate, salicylate, methanesulfonate, and toluenesulfonate are disclosed; also disclosed are compounds having the strucure MX1(X2)n wherein M is a metal cation selected from the group consisting of Ca2+, Zn2+, and K+; X1 is parecoxid anion; X2 is selected from the group consisting of parecoxid anion and another pharmaceutically acceptable anion; and n is 0 when M is K+ and n is 1 when M is Ca2+ or Zn2+; Compositions of the invention are useful treatment and prevention of a very wide range of disorders mediated by COX-2, including inflammation, pain and/or fever.

公开(公告)号：EP1565438A1

公开(公告)日：2005-08-24

申请号：EP03783127.8

申请日：2003-11-13

申请人： ELI LILLY AND COMPANY

发明人： MADER, Mary, Margaret ,  MARTIN-CABREJAS, Luisa, Maria,Lilly, S. A. ,  RICHETT, Michael, Enrico

IPC分类号： C07D209/08 ,  C07D307/79 ,  C07D333/54 ,  C07D317/62 ,  C07D319/18 ,  C07C311/51 ,  A61K31/18 ,  A61P35/00 ,  C07D277/64

CPC分类号： C07D307/79 ,  C07C311/51 ,  C07C2602/06 ,  C07C2602/08 ,  C07D209/08 ,  C07D209/30 ,  C07D277/64 ,  C07D317/44 ,  C07D317/62 ,  C07D319/18 ,  C07D333/54 ,  C07D495/04

摘要： The present invention provides antitumor compounds of the formula (I); and antitumor methods.

摘要翻译： 本发明提供式（I）的抗肿瘤化合物; 和抗肿瘤方法。