公开(公告)号：EP1553089A1

公开(公告)日：2005-07-13

申请号：EP03771407.8

申请日：2003-07-29

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： MORIYA, Minoru c/o BANYU PHARMACEUTICAL CO, LTD. ,  KANATANI, Akio; c/o BANYU PHARMACEUTICAL CO., LTD. ,  IWAASA, Hisashi; c/o BANYU PHARMACEUTICAL CO., LTD ,  ISHIHARA, Akane; c/o BANYU PHARMACEUTICAL CO., LTD ,  FUKAMI, Takehiro; c/o BANYU PHARMACEUTICAL CO, LTD

IPC分类号： C07D235/30

CPC分类号： C07D403/12 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  C07D235/30 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

摘要： This invention relates to a benzimidazole derivative of the general formula [I]
[wherein B 1 , B 2 , and B 3 represent hydrogen atom or lower alkyl; R 1 and R 2 are same or different and represent lower alkyl, etc.; R 3 and R 4 represent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.

摘要翻译： 本发明涉及通式为苯并咪唑衍生物，其中B 1，B 2和B 3表示氢原子或低级烷基; R 1和R 2相同或不同，代表低级烷基等; R 3和R 4代表氢原子等; W代表3至8元芳族或烯类杂环等; 并且Ar表示取代或未取代的芳族杂环等。该化合物用作黑色素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病和代谢性疾病的药物。

公开(公告)号：EP1473292A1

公开(公告)日：2004-11-03

申请号：EP04008840.3

申请日：1998-10-29

申请人： Boehringer Ingelheim Pharmaceuticals, Inc.

发明人： Regan, John, R. ,  Cirillo, Pier, F. ,  Hickey, Eugene, R. ,  Moss, Neil ,  Cywin, Charles, L. ,  Pargellis, Christopher ,  Gilmore, Thomas A.

IPC分类号： C07D333/36 ,  C07D231/40 ,  C07D235/30 ,  A61K31/38 ,  A61K31/415

CPC分类号： C07D235/30 ,  C07D231/40 ,  C07D333/36

摘要： Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

摘要翻译： 新型芳香族杂环化合物抑制参与免疫调节和炎症的细胞因子生成，如白介素-1和肿瘤坏死因子的产生。 因此，该化合物可用于治疗涉及炎症的疾病或病理状况的药物组合物，例如慢性炎性疾病。

公开(公告)号：EP1448199A1

公开(公告)日：2004-08-25

申请号：EP02789445.0

申请日：2002-11-05

申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS INC.

发明人： CYWIN, C.,Boehringer Ingelheim Pharma., Inc. ,  LEE, J.,Boehringer Ingelheim Pharma., Inc. ,  ROTH, G. P.,Boehringer Ingelheim Pharma., Inc. ,  SARKO, C. R.,Boehringer Ingelheim Pharma., Inc. ,  SNOW, R. J.,Boehringer Ingelheim Pharma., Inc. ,  WILSON, N. S.,Boehringer Ingelheim Pharma., Inc. ,  PULLEN, S. S.,Boehringer Ingelheim Pharma., Inc.

IPC分类号： A61K31/4439 ,  A61K31/422 ,  A61K31/4184 ,  C07D409/12 ,  C07D401/12 ,  C07D413/12 ,  C07D407/12 ,  C07D235/30

CPC分类号： C07D401/12 ,  C07D235/30 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

摘要： Disclosed are substituted benzimidazole compounds of formula (I) wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention are useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.

公开(公告)号：EP0980359B1

公开(公告)日：2004-06-23

申请号：EP98917745.6

申请日：1998-04-30

申请人： Nissan Chemical Industries, Ltd.

发明人： TANIKAWA, Keizo Nissan Chemical Industries, Ltd. ,  KAMIKAWAJI, Yoshimasa Nissan Chemical Industries, ,  HIROTSUKA, Mitsuaki Nissan Chemical Industries, ,  IWAMA, Takehisa Nissan Chemical Industries, Ltd. ,  YAMAMOTO, Akiko Nissan Chemical Industries, Ltd. ,  FUJITA, Yoichiro Nissan Chemical Industries, Ltd.

IPC分类号： C07D235/30 ,  C07D235/14 ,  A61K31/415

CPC分类号： C07D235/14 ,  C07D235/30

公开(公告)号：EP1394152A1

公开(公告)日：2004-03-03

申请号：EP02720536.8

申请日：2002-04-19

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Shuichi ,  KOTAKE, Makoto ,  MIYAMOTO, Mitsuaki ,  KAWAHARA, Tetsuya ,  KAJIWARA, Akiharu ,  HISHINUMA, Ieharu ,  OKANO, Kazuo ,  MIYAZAWA, Syuhei ,  CLARK, Richard ,  OZAKI, Fumihiro ,  SATO, Nobuaki ,  SHINODA, Masanobu ,  KAMADA, Atsushi ,  TSUKADA, Itaru ,  MATSUURA, Fumiyoshi ,  NAOE, Yoshimitsu ,  TERAUCHI, Taro ,  OOHASHI, Yoshiaki ,  ITO, Osamu ,  TANAKA, Hiroshi ,  MUSYA, Takashi ,  KOGUSHI, Motoji ,  KAWADA, Tsutomu ,  MATSUOKA, Toshiyuki ,  KOBAYASHI, Hiroko ,  CHIBA, Ken-ichi ,  KIMURA, Akifumi ,  ONO, Naoto

IPC分类号： C07D235/30 ,  A61K31/4184 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06

CPC分类号： C07D209/44

摘要： A 2-iminoimidazole derivative represented by the formula:
{wherein ring C represents a benzene ring, a pyridine ring, etc.; R 1 represents optionally substituted C 1-6 alkyl, etc.; R 201 represents hydrogen, halogen, acyl, etc. ; R 6 represents hydrogen, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, etc.; Y 1 represents a single bond,-CH 2 -, etc.; Y 2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula:
[wherein R 10 -R 14 represent hydrogen, C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, etc., and R 11 and R 12 or R 12 and R 13 may bond together to form a 5- to 8-membered heterocycle], etc.} or a salt thereof.

摘要翻译： 由下式表示的2-亚氨基咪唑衍生物：其中环C表示苯环，吡啶环等; R1代表任选取代的C1-6烷基等; R201代表氢，卤素，酰基等; R6代表氢，C1-6烷基，C1-6烷氧基羰基等; Y1表示单键，-CH2-等; Y2表示单键，-CO-等; 并且Ar代表氢，由下式表示的基团：[其中R10-R14表示氢，C1-6烷基，羟基，C1-6烷氧基等，并且R11和R12或R12和R13可以键合在一起形成5 - 至8-元杂环]等等或其盐。

公开(公告)号：EP1133477B1

公开(公告)日：2004-02-18

申请号：EP99964497.4

申请日：1999-11-23

申请人： Abbott GmbH & Co. KG

发明人： LUBISCH, Wilfried ,  KOCK, Michael ,  HÖGER, Thomas ,  SCHULT, Sabine ,  GRANDEL, Roland ,  MÜLLER, Reinhold

IPC分类号： C07D235/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61P25/00 ,  A61P9/00

CPC分类号： C07D401/04 ,  C07D235/30 ,  C07D401/14 ,  C07D403/04

摘要： The invention relates to compounds of general formula (1a) or (1b) wherein R?1 and R4¿ are hydrogen or defined substituents, A is a saturated or monoethenoid heterocyclic ring with 4 to 8 members which contains one or two nitrogen atoms, wherein additionally one oxygen or sulfur atom can be present. Said ring can be further substituted. The invention also relates to their tautomer forms, possible enantiomer and diastereomer forms, their prodrugs, as well as possible physiologically acceptable salts. The invention also relates to the use of said compounds for treating diseases related to a pathologically increased activity of PARP.

公开(公告)号：EP1366766A1

公开(公告)日：2003-12-03

申请号：EP03014599.9

申请日：1998-03-13

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Saunders, Jeffrey O. ,  Armistead, David M. ,  Badia, Michael C. ,  Bethiel, Randy S. ,  Frank, Catharine A. ,  Naegele, Doug ,  Novak, Perry M. ,  Pearlman, David A. ,  Ronkin, Steven M.

IPC分类号： A61K31/422 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4168 ,  C07D413/12 ,  C07D417/12 ,  C07D235/30

CPC分类号： C07D263/58 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  C07D235/30 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula (I) which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes.
   (I)
A is a saturated, unsaturated or partially saturated monocyclic ring system optionally comprising up to 4 heteroatoms selected from N,O, and S wherein each A optionally comprises up to 4 substituents selected from R 1 , R 4 and R 5 ;
X and Y are independently selected from CH 2 , CHR 3 , CHR 4 , O, S, NH, NR 3 , NR 4 , CH, CR 3 , CR 4 and N.

摘要翻译： 本发明涉及作为IMPDH抑制剂的式（I）化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 （I） A是饱和的，不饱和的或部分饱和的单环体系，任选地包含多达4个选自N，O和S的杂原子，其中每个A任选地包含至多4个选自R 1， 4>和R 5; X和Y独立地选自CH 2，CHR 3，CHR 4，O，S，NH，NR 3，NR 4，CH，CR 3，CR 4和N.

公开(公告)号：EP1097127B1

公开(公告)日：2003-03-12

申请号：EP99934576.2

申请日：1999-07-06

申请人： MERCK PATENT GmbH

发明人： HÖLZEMANN, Günter ,  GOODMAN, Simon ,  KESSLER, Horst ,  GIBSON, Christoph ,  SCHMITT, Jörg, Simon

IPC分类号： C07C243/38 ,  C07D235/30 ,  A61K31/15 ,  A61K31/415

CPC分类号： C07D271/113 ,  C07C281/06 ,  C07D235/30

摘要： The invention relates to compounds of formula (I), wherein X, Y, Z, R?1 and R2¿ have the meanings cited in claim 1, and to the salts and solvates thereof. Said compounds can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, thrombosis, cardiac infarctions, coronary heart diseases, arteriosclerosis, in pathological processes that are maintained or propagated by angiogenesis and in tumor therapy.

公开(公告)号：EP1244639A4

公开(公告)日：2003-02-05

申请号：EP00975498

申请日：2000-10-26

申请人： MERCK & CO INC

发明人： THOMPSON WAYNE ,  CLAREMON DAVID A ,  MUNSON PETER M ,  MCCAULEY JOHN A

IPC分类号： A61K31/4184 ,  A61K31/433 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/30 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/415 ,  A61P25/00

CPC分类号： C07D403/12 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/30 ,  C07D405/12 ,  C07D417/12

公开(公告)号：EP1243580A1

公开(公告)日：2002-09-25

申请号：EP00985987.7

申请日：2000-12-28

申请人： Nissan Chemical Industries, Ltd.

发明人： NIKI, Toshio, Nissan Chem. Ind. Ltd. Ctr. Res. In ,  MIZUKOSHI, Takashi ,  TAKAHASHI, Hiroaki ,  SATOW, Jun ,  OGURA, Tomoyuki, Nissan Chemical Industries Ltd. ,  YAMAGISHI, Kazuhiro, Nissan Chem. Ind. Ltd. ,  SUZUKI, Hiroyuki, Nissan Chemical Industries Ltd. ,  HAYASAKA, Fumio, Nissan Chemical Industries Ltd.

IPC分类号： C07D213/74 ,  C07D277/18 ,  C07D277/42 ,  C07D277/60 ,  C07D277/82 ,  C07D263/48 ,  C07D263/58 ,  C07D233/50 ,  C07D233/88 ,  C07D271/10 ,  C07D285/12 ,  C07D327/04 ,  C07D339/06 ,  C07D279/06 ,  C07D279/12 ,  C07D239/46 ,  C07D235/30 ,  C07D487/04 ,  C07D417/04 ,  C07D285/10

CPC分类号： C07D263/62 ,  A01N43/10 ,  A01N43/28 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/74 ,  A01N43/78 ,  A01N43/80 ,  A01N43/84 ,  A01N43/86 ,  A01N43/88 ,  A01N47/20 ,  C07C335/32 ,  C07D239/84 ,  C07D265/18 ,  C07D277/42 ,  C07D277/82 ,  C07D279/08 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F7/0818

摘要： A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient:
wherein G is
or the like, A is a 3- to 13-membered, mono-, di- or tri-cyclic ring which contains at least one hetero atom selected from among oxygen atoms, sulfur atoms and nitrogen atoms, which is composed of from 3 to 13 atoms arbitrarily selected from among carbon atoms, oxygen atoms, sulfur atoms and nitrogen atoms and which may be substituted by from 1 to 13 Ys, provided that when A is a quinolone ring, the nitrogen atom in the quinolone ring is present at the α-position to the imino bond,
   Z is -OR 1 or the like,
   B is -CH 2 - or the like,
   Y is Y'-D-(CH 2 ) p - or the like,
   D is a single bond or the like,
   X is halogen or the like, and
   R 1 is a hydrogen atom, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl or the like.

摘要翻译： 下式的杂环亚氨基化合物（1）和到其农业化学上可接受的盐; 和农用化学，杀真菌剂和杀虫剂含有至少一个构件从测试作为活性成分的化合物的族群中的： worin G是或类似物中，A是3-至13-元单 ，它由3〜13族原子任意选自碳原子，氧原子，硫原子和氮中选出的二价或三环状环，其包含选自氧原子，硫原子和氮原子中选择的至少一个杂原子，所有 原子且可被1至13个伊苏提供确实当A为喹诺酮环substituiertem，在喹诺酮环中的氮原子存在于α位的亚氨基键，Z是-OR <1>或 像，B是-CH 2 - 或类似物，Y是Y“D-（CH2）p-或类似物，D是单键或类似物，X是卤素或类似物，且R <1>是一个 氢原子，C1-C6烷基，C1-C6卤代烷基等。