- Preparation method of 1, 4, 6, 7-tetrahydro-5H-pyrazolo [4, 3-c] pyridine derivative
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The invention relates to a preparation method of a 1, 4, 6, 7-tetrahydro-5H-pyrazolo [4, 3-c] pyridine derivative, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: constructing a pyrazole ring
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- NOVEL INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 172-173
(2020/11/13)
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- Structure-Activity Relationship in Pyrazolo[4,3- c]pyridines, First Inhibitors of PEX14-PEX5 Protein-Protein Interaction with Trypanocidal Activity
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Trypanosoma protists are pathogens leading to a spectrum of devastating infectious diseases. The range of available chemotherapeutics against Trypanosoma is limited, and the existing therapies are partially ineffective and cause serious adverse effects. Formation of the PEX14-PEX5 complex is essential for protein import into the parasites' glycosomes. This transport is critical for parasite metabolism and failure leads to mislocalization of glycosomal enzymes, with fatal consequences for the parasite. Hence, inhibiting the PEX14-PEX5 protein-protein interaction (PPI) is an attractive way to affect multiple metabolic pathways. Herein, we have used structure-guided computational screening and optimization to develop the first line of compounds that inhibit PEX14-PEX5 PPI. The optimization was driven by several X-ray structures, NMR binding data, and molecular dynamics simulations. Importantly, the developed compounds show significant cellular activity against Trypanosoma, including the human pathogen Trypanosoma brucei gambiense and Trypanosoma cruzi parasites.
- Dawidowski, Maciej,Kalel, Vishal C.,Napolitano, Valeria,Fino, Roberto,Schorpp, Kenji,Emmanouilidis, Leonidas,Lenhart, Dominik,Ostertag, Michael,Kaiser, Marcel,Kolonko, Marta,Tippler, Bettina,Schliebs, Wolfgang,Dubin, Grzegorz,M?ser, Pascal,Tetko, Igor V.,Hadian, Kamyar,Plettenburg, Oliver,Erdmann, Ralf,Sattler, Michael,Popowicz, Grzegorz M.
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p. 847 - 879
(2020/02/04)
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- NOVEL INDOLIZINE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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- NOVEL PHENYL AND PYRIDYL UREAS ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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- DIAZEPINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF HEPATITIS B INFECTIONS
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Provided herein are compounds of formula (I) and (V) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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- OXADIAZEPINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF HEPATITIS B INFECTIONS
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Provided herein are compounds of formula (IA) and (III) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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- PHENOXYMETHYL DERIVATIVES
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The invention provides novel compounds having the general formula (I), wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 364
(2017/03/21)
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- DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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- PHOSPHODIESTERASE 10 INHIBITORS
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Provided are certain quinazolines of formular (I) or (II) that are PDElO inhibitors, pharmaceutical compositions, containing the same and processes for preparing the same. Also provided are methods of treating diseases treatable by PDElO enzyme such as ob
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Page/Page column 85
(2010/11/26)
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- CONDENSED PYRAZOLE DERIVATIVES AS PPAR AGONISTS II
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The invention discloses compounds of formula (I) wherein: R is a carboxylic acid or a derivative thereof; R1 and R2 are independently H or alkyl, or together R1 and R2 form an alkylene group; L1 is a
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Page/Page column 51
(2010/11/26)
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- CINNOLINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS
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The present invention is directed tojcjnnoline compounds of formula (I) that are PDE 1 inhibitors, pharmaceutical compositions containing such compounds and process for preparing such compounds. This invention is also directed to methods of treating diseases treatable by inhibition of PDElO enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 53
(2010/11/28)
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- CINNOLINE AND QUINAZOLINE DERIVATES AS PHOSPHODIESTERASE 10 INHIBITORS
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The present invention is directed to cinnoline and quinazoline compounds of formula (I) that are PDE10 inhibitors, pharmaceutical compounds containing the same and processes for preparing the same. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme such as obesity, non-insulin dependent diabetes, schizophrenia or bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 72
(2010/11/28)
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