236418-11-4Relevant academic research and scientific papers
Benzimidazole derivative and pharmaceutical purposes thereof
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Paragraph 0372-0374; 0375-0376, (2019/10/29)
The invention discloses a benzimidazole derivative and pharmaceutical purposes thereof, and particularly discloses a benzimidazole derivative shown in a formula I and purposes of the benzimidazole derivative to preparation of drugs for treating and/or pre
Discovery of new orally active prostaglandin D2 receptor antagonists
Iwahashi, Maki,Naganawa, Atsushi,Kinoshita, Atsushi,Shimabukuro, Atsushi,Nishiyama, Toshihiko,Ogawa, Seiji,Matsunaga, Yoko,Tsukamoto, Kohki,Okada, Yutaka,Matsumoto, Ryoji,Nambu, Fumio,Oumi, Rie,Odagaki, Yoshihiko,Katagi, Jun,Yano, Koji,Tani, Kousuke,Nakai, Hisao,Toda, Masaaki
, p. 6935 - 6948 (2012/01/05)
To identify an orally available drug candidate, a series of 3-benzoylaminophenylacetic acids were synthesized and evaluated as prostaglandin D2 (PGD2) receptor antagonists. Some of the compounds tested were found to exhibit excellent
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity
Leonard, Kristi,Marugan, Juan Jose,Raboisson, Pierre,Calvo, Raul,Gushue, Joan M.,Koblish, Holly K.,Lattanze, Jennifer,Zhao, Shuyuan,Cummings, Maxwell D.,Player, Mark R.,Maroney, Anna C.,Lu, Tianbao
, p. 3463 - 3468 (2007/10/03)
The disruption of the p53-Hdm2 protein-protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.
Heterocyclic thrombin inhibitors. Part 2: Quinoxalinone derivatives as novel, potent antithrombotic agents
Ries, Uwe J.,Priepke, Henning W. M.,Hauel, Norbert H.,Handschuh, Sandra,Mihm, Gerhard,Stassen, Jean M.,Wienen, Wolfgang,Nar, Herbert
, p. 2297 - 2302 (2007/10/03)
Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have been discovered. Nanomolar inhibition of both coagulation enzymes resulted in very potent antithrombotic activity in vitro.
Benzimidazoles having antithrombotic activity
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, (2008/06/13)
The present invention relates to new benzimidazoles of general formula whereinRa to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain
Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
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, (2008/06/13)
The present invention relates to 5-membered heterocyclic condensed benzoderivatives of formula wherein Ra to Rc, A, X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. The compounds of the above formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of formula I, and the compounds of the above formula I wherein Rc denotes one of the following amidino groups and the tautomers and stereoisomers thereof have valuable pharmacological properties, particularly an antithrombotic activity.
