919085-52-2Relevant academic research and scientific papers
PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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, (2020/01/11)
Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
Discovery of O-(3-carbamimidoylphenyl)-l-serine amides as matriptase inhibitors using a fragment-linking approach
Goswami, Rajeev,Wohlfahrt, Gerd,Mukherjee, Subhendu,Ghadiyaram, Chakshusmathi,Nagaraj, Jwala,Satyam, Leena K.,Subbarao, Krishnaprasad,Gopinath, Sreevalsam,Krishnamurthy, Narasimha R.,Subramanya, Hosahalli S.,Ramachandra, Murali
supporting information, p. 616 - 620 (2015/01/30)
Matriptase is a cell-surface trypsin-like serine protease of epithelial origin, which cleaves and activates proteins including hepatocyte growth factor/scatter factor and proteases such as uPA, which are involved in the progression of various cancers. Here we report a fragment-linking approach, which led to the discovery of O-(3-carbamimidoylphenyl)-l-serine amides as potent matriptase inhibitors. The co-crystal structure of one of the potent inhibitors, 6 in complex with matriptase catalytic domain validated the working hypothesis guiding the development of this congeneric series and revealed the structural basis for matriptase inhibition. Replacement of a naphthyl group in 6 with 2,4,6-tri-isopropyl phenyl resulted in 10 with improved matriptase inhibition, which exhibited significant primary tumor growth inhibition in a mouse model of prostate cancer. Compounds such as 10, identified using a fragment-linking approach, can be explored further to understand the role of matriptase as a drug target in cancer and inflammation.
CYCLIC ANILINOPYRIDINOTRIAZINES AS GSK-3 INHIBITORS
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Page/Page column 37, (2008/06/13)
The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
NEW OXABISPIDINE COMPOUNDS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS
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Page/Page column 79-80, (2010/11/27)
There is provided compounds of formula I, [Chemical formula should be inserted here. Please see paper copy] wherein R1 to R4 , R41 to R46 and Z have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias
