869897-98-3Relevant academic research and scientific papers
Allylamine derivative as well as preparation method and application thereof
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Paragraph 0304; 0305; 0308; 0309, (2021/06/02)
The invention relates to an allylamine derivative as well as a preparation method and application thereof, and in particular, relates to a compound represented by a formula I, or a stereoisomer, a tautomer, a polymorphic substance, a solvate, an N-oxide, an isotope labeled compound, a metabolite, a prodrug or ester thereof, or a pharmaceutically acceptable salt thereof. The compound has a higher inhibitory activity against vascular adhesion protein 1/semicarbazide sensitive amine oxidase, a good selectivity against monoamine oxidase and diamine oxidase; and additionally, in some embodiments, the mixture has a high in vivo bioavailability as well as safety.
Rhodium(III)-Catalyzed C-H Activation: Annulation of Petrochemical Feedstocks for the Construction of Isoquinolone Scaffolds
Barber, Joyann S.,Kong, Dehuan,Li, Wei,McAlpine, Indrawan J.,Nair, Sajiv K.,Sakata, Sylvie K.,Sun, Nicole,Patman, Ryan L.
supporting information, p. 202 - 206 (2021/01/14)
We describe a simple and robust procedure for the Rh(III)-catalyzed [4+2] cycloaddition of feedstock gases enabled through C-H activation. A diverse set of 3,4-dihydroisoquinolones and 3-methylisoquinolones have been prepared in good to excellent yields.
INHIBITORS OF CATHEPSIN B
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, (2009/08/18)
The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis. The compounds of Formula (I) are also useful for treating subjects with both HCV and fibrosis in a mammal, particularly liver fibrosis, and subjects affirmatively diagnosed or at risk for both HCV and liver fibrosis.
HCV INHIBITORS
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Page/Page column 69-70, (2008/06/13)
The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
1-ARYL-4-SUBSTITUTED ISOQUINOLINES
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Page/Page column 55-56, (2010/02/14)
1-Aryl-4-substituted isoquinolines analogues of Formula (I) and Formula (II) are provided, as follows : wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) and (II) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines, which are useful as probes for the localization of C5a receptors.
