332099-01-1Relevant articles and documents
IDO inhibitors
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Paragraph 0113-0115, (2019/01/05)
The invention discloses novel compounds used as indoleeamine-pyrrole-2,3-dioxygenase (IDO) inhibitors, and specifically discloses the compounds represented by a formula (I) shown in the description and pharmaceutically-acceptable salts of the compounds. The invention also discloses an application of the compounds represented by the formula (I) and the pharmaceutically-acceptable salts of the compounds in preparation of a medicament for treating tumors.
Diamine derivatives
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, (2008/06/13)
A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: Potent human histamine H4 antagonists
Venable, Jennifer D.,Cai, Hui,Chai, Wenying,Dvorak, Curt A.,Grice, Cheryl A.,Jablonowski, Jill A.,Shah, Chandra R.,Kwok, Annette K.,Ly, Kiev S.,Pio, Barbara,Wei, Jianmei,Desai, Pragnya J.,Jiang, Wen,Nguyen, Steven,Ling, Ping,Wilson, Sandy J.,Dunford, Paul J.,Thurmond, Robin L.,Lovenberg, Timothy W.,Karlsson, Lars,Carruthers, Nicholas I.,Edwards, James P.
, p. 8289 - 8298 (2007/10/03)
Three series of H4 receptor ligands,- derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H 4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H4 antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.