公开(公告)号：EP2109615B1

公开(公告)日：2011-03-09

申请号：EP08713287.4

申请日：2008-01-25

申请人： Merck Sharp & Dohme Corp.

发明人： DEBENHAM, John, S. ,  HALE, Jeffrey, J. ,  HUO, Pei ,  MADSEN-DUGGAN, Christina, B. ,  WALSH, Thomas, F. ,  YAN, Lin

IPC分类号： C07D491/052 ,  C07D491/16 ,  C07D495/16 ,  A61K31/436 ,  A61P1/00 ,  A61P25/00

CPC分类号： C07D491/052 ,  C07D491/16 ,  C07D495/16

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

公开(公告)号：EP2065388A1

公开(公告)日：2009-06-03

申请号：EP07807337.6

申请日：2007-09-14

申请人： Daiichi Sankyo Company, Limited

发明人： OHSUKI, Satoru ,  TENGEIJI, Atsushi ,  IKEDA, Masahiro ,  SHIBATA, Yoshihiro ,  NAGATA, Chikahiro ,  SHIMADA, Takashi

IPC分类号： C07D495/16 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61P43/00 ,  C07D495/22 ,  C07D498/22 ,  C07D519/00

CPC分类号： C07D495/16 ,  C07D495/20 ,  C07D495/22 ,  C07D498/22

摘要： Problem to be Solved
To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity.
Solution
The present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).

摘要翻译： 要解决的问题为了提供抑制HSP90的作用的新型化合物，特别是抑制作为伴侣蛋白的HSP90的功能的新型化合物并具有抗肿瘤活性。 解决方案本发明提供具有抑制HSP90的ATP酶活性的各种取代基并具有抗肿瘤活性的由式​​（1）表示的吡唑并嘧啶化合物，包含由式（1）表示的化合物的HSP90抑制剂，包含该化合物的药物 （1）表示的化合物的抗癌剂，包含由式（1）表示的化合物的抗癌剂，包含由式（1）表示的化合物的药物组合物和使用由式（1）表示的化合物治疗癌症的方法 ）。

公开(公告)号：EP1497296A1

公开(公告)日：2005-01-19

申请号：EP03741766.4

申请日：2003-04-23

申请人： Wyeth

发明人： GAO, Hong ,  STACK, Gary, Paul ,  SABB, Annmarie, Louise

IPC分类号： C07D487/06 ,  C07D495/16 ,  C07D491/16 ,  A61K31/395 ,  A61P25/18

CPC分类号： C07D487/06

摘要： Compounds of formula (1) are provided: (1) where R1 through R7 are defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.

公开(公告)号：EP1456176A4

公开(公告)日：2004-11-03

申请号：EP02789841

申请日：2002-12-18

申请人： LUMIGEN INC

发明人： AKHAVAN-TAFTI HASHEM ,  DE SILVA RENUKA ,  XIE WENHUA

IPC分类号： G01N21/76 ,  C07D219/02 ,  C07D219/04 ,  C07D219/06 ,  C07D409/04 ,  C07D409/06 ,  C07D411/04 ,  C07D411/06 ,  C07F9/64 ,  C07F9/6558 ,  C12Q1/28 ,  G01N33/58 ,  C07D219/00 ,  C07D221/18 ,  C07D455/03 ,  C07D487/06 ,  C07D495/06 ,  C07D495/16 ,  G01N33/53

CPC分类号： C07D409/06 ,  C07D219/02 ,  C07D411/06 ,  C07F9/64 ,  C07F9/65586 ,  C12Q1/28 ,  G01N33/581 ,  G01N2333/908

摘要： Novel compounds comprising a C-C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.

摘要翻译： 公开了包含在一个碳处被两个含硫原子基团取代的C-C双键的新型化合物。 这些化合物可用于通过与过氧化物酶和过氧化物反应迅速产生化学发光的方法和组合物。 如此产生的化学发光可用作过氧化物酶或产生过氧化物的酶的测定中的可检测信号以及使用酶标记的特异性结合对的测定中的可检测信号。

公开(公告)号：EP1456176A1

公开(公告)日：2004-09-15

申请号：EP02789841.0

申请日：2002-12-18

申请人： LUMIGEN, INC.

发明人： AKHAVAN-TAFTI, Hashem ,  DE SILVA, Renuka ,  XIE, Wenhua

IPC分类号： C07D219/00 ,  C07D219/04 ,  C07D221/18 ,  C07D409/04 ,  C07D411/04 ,  C07D487/06 ,  C07D495/06 ,  C07D495/16 ,  C07D455/03 ,  C12Q1/28 ,  G01N33/53

CPC分类号： C07D409/06 ,  C07D219/02 ,  C07D411/06 ,  C07F9/64 ,  C07F9/65586 ,  C12Q1/28 ,  G01N33/581 ,  G01N2333/908

摘要： Novel compounds comprising a C-C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.

公开(公告)号：EP0527889B1

公开(公告)日：2000-08-02

申请号：EP91909628.9

申请日：1991-05-01

申请人： ABBOTT LABORATORIES

发明人： CHU, Daniel, T. ,  LEE, Cheuk, M. ,  LI, Qun ,  COOPER, Curt, S. ,  PLATTNER, Jacob, J.

IPC分类号： C07D471/04 ,  C07D455/02 ,  C07D491/16 ,  C07D495/16 ,  C07D471/16 ,  C07D519/00 ,  A61K31/435 ,  A61K31/505 ,  A61K31/495 ,  A61K31/54 ,  A61K31/535

CPC分类号： C07D471/04 ,  A61K38/00 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026

摘要： Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R1 is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons, (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) loweralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR7R8; R2 is selected from the group consisting of halogen, loweralkoxy, carbocyclic aryloxy or carbocyclic aryl(loweralkyl)oxy, loweralkyl, loweralkenyl, cycloalkyl of from 3 to 8 carbons, cycloalkenyl of from 4 to 8 carbons, carbocyclic aryl(loweralkyl), cycloalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrogen-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle having formula (II), wherein x is 0 to 3; R9 is selected from (a)-(CH¿2?)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR?10(CH¿2)p-, wherein R10 is selected from S, O and N, n is 1 or 2, and p is 1 or 2; and Y is a non-hydrogen substituent independently selected from loweralkyl, halo(loweralkyl), loweralkoxy, hydroxy-substituted loweralkyl, hydroxy, amino(loweralkyl), halogen and a group having the formula -NR?11R12; R3¿ is hydrogen, halogen or loweralkoxy; R4 is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group; R5 is selected from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR13R14; and A is N or CR6, wherein R6 is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R?1 and R6¿, taken together with the atoms to which they are attached, form a 6-membered saturated ring which may contain an oxygen or a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R5 is hydrogen and A is CH then either (a) R?1 is NR7R8¿, or (b) R2 is a group having formula (III), wherein x is 1-3 and R9 and Y are as defined above.

公开(公告)号：EP0831094A1

公开(公告)日：1998-03-25

申请号：EP96920027.8

申请日：1996-05-31

申请人： Eisai Co., Ltd.

发明人： SUGUMI, Hiroyuki ,  NIIJIMA, Jun ,  KOTAKE, Yoshihiko ,  OKADA, Toshimi ,  KAMATA, Jun-ichi ,  YOSHIMATSU, Kentaro ,  NAGASU, Takeshi ,  NAKAMURA, Katsuji ,  UENAKA, Toshimitsu ,  YAMAGUCHI, Atsumi ,  YOSHINO, Hiroshi ,  KOYANAGI, Nozomu ,  KITO, Kyosuke

IPC分类号： C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  C07D491/16 ,  C07D495/16 ,  C07D498/06 ,  C07D513/06 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54

CPC分类号： C07D471/06 ,  C07D487/06 ,  C07D513/06

摘要： Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same.
A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof:
wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;
   provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded.
Which has an excellent antitumor activity.

摘要翻译： 具有优异抗肿瘤效果的新型稠合多环杂环衍生物及其制备方法。 由以下通式（I）表示的化合物或其药理学上可接受的盐：其中环A表示任选取代的单环芳环或二环稠合环，其中至少一个环为芳环; 环B表示吡咯，4H-1,4-恶嗪，4H-1,4-噻嗪或4（1H） - 吡啶酮; 环C表示任选取代的单环或二环稠合芳环; Y表示由式-ef表示的基团（其中e表示低级亚烷基; f表示任选被羟基化或任选低级烷基化的低级烷基取代的脒基，胍基或氨基）;条件是环A和B 均为任选取代的单环芳环，其具有优异的抗肿瘤活性。