4887-95-0Relevant articles and documents
Benzimidazole derivatives, their preparation and their application in medicine and pharmacology (by machine translation)
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, (2019/07/16)
The invention relates to a new control or inhibit indocyanine 2, 3 - dioxygenase (IDO) activity of the benzimidazole derivatives, their preparation and their application in medicine and pharmacology. Specifically, the invention relates to a compound of general formula (I) compound of formula and its pharmaceutically acceptable salt, containing the compound or its pharmaceutically acceptable salt of the pharmaceutical composition, the use of the compound or its pharmaceutically acceptable salts for treating and/or preventing the relevance of the IDO-mediated disease, especially a tumor of the method and the compound or its pharmaceutically acceptable salts thereof. The invention also relates to the compound or its pharmaceutically acceptable salt or containing the compound or its pharmaceutically acceptable salts for the preparation of a pharmaceutical composition for treating and/or preventing the relevance of the IDO-mediated disease, in particular of the use of the drug in the tumor. Wherein the general formula (I) of each substituent is as defined in the specification. (by machine translation)
Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs
Nakao, Syuhei,Mabuchi, Miyuki,Shimizu, Tadashi,Itoh, Yoshihiro,Takeuchi, Yuko,Ueda, Masahiro,Mizuno, Hiroaki,Shigi, Naoko,Ohshio, Ikumi,Jinguji, Kentaro,Ueda, Yuko,Yamamoto, Masatatsu,Furukawa, Tatsuhiko,Aoki, Shunji,Tsujikawa, Kazutake,Tanaka, Akito
, p. 1071 - 1074 (2014/03/21)
A series of 1-aryl-3,4-substituted-1H-pyrazol-5-ol derivatives was synthesized and evaluated as prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors to obtain a novel anti-prostate cancer drug. After modifying 1-(1H-benzimidazol-2-yl)-3,4-dimethyl-1H-pyrazol-5-ol (1), a hit compound found during random screening using a recombinant PCA-1/ALKBH3, 1-(1H-5- methylbenzimidazol-2-yl)-4-benzyl-3-methyl-1H-pyrazol-5-ol (35, HUHS015), was obtained as a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of 35 was 7.2% in rats after oral administration. As expected, continuously administering 35 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.
Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives
Ogino, Yoshio,Ohtake, Norikazu,Nagae, Yoshikazu,Matsuda, Kenji,Moriya, Minoru,Suga, Takuya,Ishikawa, Makoto,Kanesaka, Maki,Mitobe, Yuko,Ito, Junko,Kanno, Tetsuya,Ishihara, Akane,Iwaasa, Hisashi,Ohe, Tomoyuki,Kanatani, Akio,Fukami, Takehiro
scheme or table, p. 5010 - 5014 (2009/05/07)
Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, orally available, and brain-penetrable Y5 selective antagonist (5k). Crown Copyright