公开(公告)号：EP0968182B1

公开(公告)日：2004-05-06

申请号：EP97935666.4

申请日：1997-08-07

申请人： Darwin Discovery Limited

发明人： OWEN, David, Alan, Darwin Discovery Limited ,  MONTANA, John, Gary, Darwin Discovery Limited ,  KEILY, John, Fraser, Darwin Discovery Limited ,  WATSON, Robert, John, Darwin Discovery Limited ,  BAXTER, Andrew, Douglas, Darwin Discovery Limited

IPC分类号： C07C317/44 ,  C07D209/48 ,  C07D277/36 ,  C07D307/38 ,  C07D213/70 ,  C07D233/84 ,  C07D207/40 ,  C07D233/74 ,  C07D237/32 ,  A61K31/19 ,  A61K31/215

CPC分类号： C07C317/44 ,  C07C2601/08 ,  C07D207/48

公开(公告)号：EP1154992A4

公开(公告)日：2003-05-28

申请号：EP00919316

申请日：2000-02-18

申请人： FIBROGEN INC

发明人： HO WEN-BIN

IPC分类号： C07C311/06 ,  C07C311/19 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07C317/14 ,  C07D213/42 ,  C07D233/84 ,  C07D257/04 ,  C07D285/14 ,  C07D317/46 ,  C07D317/58 ,  C07D319/20 ,  C07D333/20 ,  C07D333/28 ,  C07D333/34 ,  C07D333/38 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/04 ,  C07C311/21 ,  A61K31/18 ,  A61P19/02

CPC分类号： C07D213/42 ,  C07C311/06 ,  C07C311/19 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07C317/14 ,  C07C2601/16 ,  C07C2603/74 ,  C07D233/84 ,  C07D257/04 ,  C07D285/14 ,  C07D317/46 ,  C07D317/58 ,  C07D319/20 ,  C07D333/20 ,  C07D333/28 ,  C07D333/34 ,  C07D333/38 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/04

公开(公告)号：EP1255737A4

公开(公告)日：2003-04-16

申请号：EP00959012

申请日：2000-09-06

申请人： LG CHEM INVESTMENT LTD

发明人： SHIN HYUN-IK ,  CHANG JAY-HYOK ,  LEE KYOO-WOONG ,  LEE HYUN-IL ,  KIM SUNG-KEE ,  NAM DO-HYUN

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D405/06

CPC分类号： C07D233/64

摘要： The present invention relates to a process for preparing a 1-substituted 5-hydroxymethylimidazole of formula (1). According to the present invention, the desired compound can be prepared more safely, more rapidly and more purely in higher yield than prior art process.

摘要翻译： 本发明涉及制备式（1）的1-取代的5-羟甲基咪唑的方法。 根据本发明，所需化合物可以比现有技术方法更安全，更快速和更纯粹地以更高产率制备。

公开(公告)号：EP0873123B1

公开(公告)日：2003-04-09

申请号：EP96938647.3

申请日：1996-11-05

申请人： UNIVERSITY OF PITTSBURGH

发明人： SEBTI, Said, M. ,  HAMILTON, Andrew, D. ,  ROSENBERG, Saul, H. ,  AUGERI, David, J. ,  BARR, Kenneth, J. ,  DONNER, Bernard, G. ,  FAKHHOURY, Stephen, A. ,  JANOWICK, David, A. ,  KALVIN, Douglas, M. ,  LARSEN, John, J. ,  LIU, Gang ,  O'CONNOR, Stephen, J. ,  SHEN, Wang ,  SWENSON, Rolf, E. ,  SORENSON, Bryan, K. ,  SULLIVAN, Gerard, M. ,  SZCZEPANKIEWICZ, Bruce ,  TASKER, Andrew, S. ,  WASICAK, James, T. ,  WINN, Martin

IPC分类号： A61K31/415 ,  A61K31/44 ,  C07D213/34 ,  C07D213/30 ,  C07D213/62 ,  C07D213/72 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D213/82 ,  C07D213/56 ,  C07D233/54 ,  C07D233/90 ,  C07D405/12 ,  C07D405/04 ,  C07D417/12 ,  C07D401/12

CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/34 ,  C07D213/36 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D249/08 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is selected from: (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halogen, (g) haloalkyl, (h) aryl-L2 - and (i) heterocyclic - L3; R2 is selected from the group consisting of: (a) formula (II), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (III), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is pyridyl, substituted pyridyl, imidazolyl, or substituted imidazolyl; R4 is selected from hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, and (heterocyclic)alkyl; and L1 is absent or is selected from (a) -L4-N(R4)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R7)-L5-, (f) -L4-N(R7)-C(W)-L7-L5-, (g) -L4-N(R7)-S(O)p-L7-L5-, (h) C2-C4-alkylene optionally substituted with 1 or 2 hydroxy groups, (i) C2-to-C4-alkenylene, and (j) C2-to-C4-alkynylene, are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.

公开(公告)号：EP1165472A4

公开(公告)日：2002-11-20

申请号：EP00916019

申请日：2000-03-02

申请人： SQUIBB BRISTOL MYERS CO

发明人： SINGH AMBARISH ,  CHEN CHIEN-KUANG ,  GROSSO JOHN A ,  DELANEY EDWARD J ,  WANG XUEBAO ,  POLNIASZEK RICHARD P ,  THOTTATHIL JOHN K

IPC分类号： A61K31/421 ,  A61K31/422 ,  A61P9/04 ,  A61P9/12 ,  A61P15/10 ,  C07C303/22 ,  C07C309/32 ,  C07D231/12 ,  C07D233/54 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D233/66 ,  C07D233/78 ,  C07D233/80 ,  C07D233/84 ,  C07D233/86 ,  C07D233/91 ,  C07D261/16 ,  C07D263/32 ,  C07D263/50 ,  C07D277/22 ,  C07D277/24 ,  C07D277/26 ,  C07D277/28 ,  C07D413/12 ,  C07F5/02

CPC分类号： C07D413/12 ,  C07C303/22 ,  C07D261/16 ,  C07D263/32 ,  C07D263/50 ,  C07C309/32

摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension, congestive heart failure and male erectile dysfunction.

公开(公告)号：EP1211245A1

公开(公告)日：2002-06-05

申请号：EP00953518.8

申请日：2000-08-18

申请人： ISHIHARA SANGYO KAISHA, LTD.

发明人： MORINO, Kyuya, Ishihara Sangyo Kaisha, Ltd. ,  YOTSUYA, Shuichi, Ishihara Sangyo Kaisha, Ltd. ,  OGAWA, Munekazu, Ishihara Sangyo Kaisha, Ltd.

IPC分类号： C07D233/84 ,  C07D417/04 ,  A61K31/4164 ,  A61K31/426 ,  A61P33/02

CPC分类号： C07D233/84 ,  A61K31/4164 ,  Y02A50/411

摘要： The present invention provides an agent for controlling animal diseases caused by parasites, which contains, as an active ingredient, an imidazole compound represented by the formula (I):
wherein R 1 is a cyano group, R 2 is an alkyl group which may be substituted, or a phenyl group which may be substituted, R 3 is a chlorine atom, and R 4 is a dimethylamino group.

摘要翻译： 本发明提供一种用于控制由寄生虫引起的动物疾病的药剂，其含有式（I）表示的咪唑化合物作为活性成分：其中R 1为氰基的R CH 2，R 2， 可以被取代的烷基或可被取代的苯基，R 3是氯原子，R 4是二甲基氨基。

公开(公告)号：EP1072588A4

公开(公告)日：2001-07-18

申请号：EP99913673

申请日：1999-04-15

申请人： SHIONOGI & CO

发明人： AOKI TSUTOMU ,  KONOIKE TOSHIRO

IPC分类号： C07C313/08 ,  C07C319/14 ,  C07C323/09 ,  C07D233/84 ,  C07D401/06 ,  B01J31/02 ,  C07C321/28 ,  C07C323/62

CPC分类号： C07D401/06 ,  C07C313/08 ,  C07C319/14 ,  C07C323/09 ,  C07D233/84

摘要： A process for producing a compound represented by formula (I) which comprises reacting a compound represented by formula (V) with a compound represented by formula (VI) in the presence of a base; a process for producing a compound represented by formula (II) which comprises causing a halogenating agent to act on the compound represented by formula (I); a process for producing a compound represented by formula (IV) which comprises reacting the compound represented by formula (II) with a compound represented by formula (III); and the compound represented by formula (I), wherein Alk represents branched alkyl; Hal1 and Hal2 each represents halogeno; R?1 and R2¿ each independently represents halogeno, alkyl, alkoxy, nitro, and cyano; R?3 and R5¿ each represents hydrogen or an organic residue; and R4 represents an organic residue.

摘要翻译： （I）表示的化合物的制备方法，其包括在碱的存在下使式（V）所示的化合物与式（VI）所示的化合物反应; （II）表示的化合物的制备方法，其包括使卤化剂作用于式（I）表示的化合物; （IV）所示化合物的制备方法，其包括使式（II）所示化合物与式（III）所示化合物反应; 和由式（I）表示的化合物，其中Alk表示支链烷基; Hal1和Hal2各自代表卤代; R 1和R 2各自独立地表示卤代，烷基，烷氧基，硝基和氰基; R 3和R 5各自代表氢或有机残基; 和R4代表有机残基。

公开(公告)号：EP0721944B1

公开(公告)日：2001-01-17

申请号：EP95926500.0

申请日：1995-07-26

申请人： SUNTORY LIMITED

发明人： FUKAMI, Harukazu ,  SUMIDA, Motoo ,  NIWATA, Shinjiro ,  KAKUTANI, Saki ,  SAITOH, Masayuki ,  SHIBATA, Hiroshi ,  KISO, Yoshinobu

IPC分类号： C07D233/80 ,  C07D233/86 ,  A61K31/415 ,  A61K31/495 ,  C07D233/84 ,  C07D405/12 ,  C07D403/12 ,  C07D403/04 ,  C07D401/04

CPC分类号： C07D401/04 ,  C07D233/80 ,  C07D233/86 ,  C07D403/04 ,  C07D405/12

摘要： An imidazolidine derivative represented by general formula (1) and medicines containing the derivative as the active ingredient, representative examples of which include a chymase inhibitor and a preventive or remedy for cardiac and circulatory diseases caused by abnormal palpitation induced by angiotensin II, wherein A and B represent each an aromatic hydrocarbon group which may be substituted by one to three substituents selected from among halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylenedioxy, phenoxy, nitro, cyano, phenyl, C2-C5 alkanoylamino, carboxyl which may be esterified with C1-C4 alkyl or alkenyl, carboxyalkyl which may be esterified with C1-C4 alkyl or alkenyl, carboxyalkyloxy which may be esterified with C1-C4 alkyl or alkenyl, N-alkylpiperazinylcarbonyl, N-alkylpiperazinylcarbonylalkyl, N-alkyl-piperazinylcarbonylalkyloxy and morpholinocarbonyl; X represents sulfonyl or carbonyl; and Y represents oxygen or sulfur.

公开(公告)号：EP0968182A1

公开(公告)日：2000-01-05

申请号：EP97935666.4

申请日：1997-08-07

申请人： Darwin Discovery Limited

发明人： OWEN, David, Alan,Darwin Discovery Limited ,  MONTANA, John, Gary,Darwin Discovery Limited ,  KEILY, John, Fraser,Darwin Discovery Limited ,  WATSON, Robert, John,Darwin Discovery Limited ,  BAXTER, Andrew, Douglas,Darwin Discovery Limited

IPC分类号： C07C317/44 ,  C07D209/48 ,  C07D277/36 ,  C07D307/38 ,  C07D213/70 ,  C07D233/84 ,  C07D207/40 ,  C07D233/74 ,  C07D237/32 ,  A61K31/19 ,  A61K31/215

CPC分类号： C07C317/44 ,  C07C2601/08 ,  C07D207/48

摘要： The invention concerns hydroxamic acid and carboxylic acid derivatives of formulae (I): B-X-(CH2)n-CHR1-(CH2)m-CONHOH and (Ia): B-S(O)1-2-(CH2)n-CHR1-(CH2)m-COOR2, in which X is O, NR¿3? or S(O)0-2, and the other variables have the definitions given in the claims, having MMP and TNF inhibitory activity.

公开(公告)号：EP0949249A1

公开(公告)日：1999-10-13

申请号：EP97949167.7

申请日：1997-12-19

申请人： SHIONOGI & CO., LTD.

发明人： HAJIMA, Makoto ,  HOZUMI, Yasuyuki ,  KABAKI, Mikio

IPC分类号： C07D233/84 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D233/84

摘要： The present invention provides a process for producing a compound of the formula (III):
wherein R 1 and R 3 are independently hydrogen or an organic group: R 2 is an organic group; and R 4 is an optionally substituted aryl,
by reacting the compound of formula (I):
wherein R 1 , R 2 , and R 3 are as defined above, with the compound of formula (II):

        R 4 -S-Hal     (II)

wherein R 4 is as defined above and Hal is halogen, in the presence of base.

摘要翻译： 本发明提供了制备式（III）化合物的方法：其中R 1和R 3独立地是氢或有机基团：R 2是有机基团; 和R 4是任选取代的芳基，通过使式（I）的化合物：其中R 1，R 2和R 3如上所定义的与式 （II）：R 4 -S-Hal其中R 4如上所定义，Hal为卤素，在碱的存在下。