- Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th
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Dissociation of transthyretin (TTR) tetramers may lead to misfolding and aggregation of proamyloidogenic monomers, which underlies TTR amyloidosis (ATTR) pathophysiology. ATTR is a progressive disease resulting from the deposition of toxic fibrils in tiss
- Cioffi, Christopher L.,Raja, Arun,Muthuraman, Parthasarathy,Jayaraman, Aravindan,Jayakumar, Srinivasan,Varadi, Andras,Racz, Boglarka,Petrukhin, Konstantin
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p. 9010 - 9041
(2021/07/19)
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- ANTI-PAIN COMPOUND AND PREPARATION METHOD THEREFOR
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Disclosed are a compound represented by the general Formula (I), or a stereisomer, tautomer, derivative, prodrug or pharmaceutically acceptable salt thereof, and a method for preparing the compound and use of the compound in manufacture of a medicament for treating a neuropathic pain and/or neuropathic pain syndrome or a medicament for combating an inflammation: wherein R1 is selected from hydrogen, halogen, alkyl, cyano and haloalkyl, R2 and R3 are independently selected from hydrogen, halogen, alkyl, haloalkyl and nitro, and R1, R2 and R3 are not hydrogen at the same time; furthermore, when either R2 or R3 is nitro or halogen, the other two of R1, R2 and R3 are not hydrogen at the same time. The compound has good effects in treating a neuropathic pain and/or neuropathic pain syndrome and good effects in combating an inflammation, and has not side effects such as addiction.
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Paragraph 0075-0076
(2020/11/23)
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- Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region
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Pyroglutamate-modified amyloid β peptides (pGlu-Aβ) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-Aβ peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative t
- Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Ann, Jihyae,Cui, Minghua,Park, Gyungseo,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo
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supporting information
p. 1035 - 1049
(2018/02/12)
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- ISOXAZOLE ANALOGS AS FXR AGONISTS AND METHODS OF USE THEREOF
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The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
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Paragraph 0271
(2018/04/20)
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- OXABOROLE ESTERS AND USES THEREOF
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The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.
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Page/Page column 89
(2017/12/05)
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- TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE
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The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
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Paragraph 00523
(2017/03/28)
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- Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrin αiIbβ3
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A series of novel RGD mimetics containing phthalimidine fragment was designed and synthesized. Their antiaggregative activity determined by Born's method was shown to be due to inhibition of fibrinogen binding to αIIbβ3. Molecular docking of RGD mimetics to αIIbβ3 receptor showed the key interactions in this complex, and also some correlations have been observed between values of biological activity and docking scores. The single crystal X-ray data were obtained for five mimetics.
- Krysko, Andrei A.,Samoylenko, Georgiy V.,Polishchuk, Pavel G.,Fonari, Marina S.,Kravtsov, Victor Ch.,Andronati, Sergei A.,Kabanova, Tatyana A.,Lipkowski, Janusz,Khristova, Tetiana M.,Kuz'Min, Victor E.,Kabanov, Vladimir M.,Krysko, Olga L.,Varnek, Alexandre A.
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p. 4646 - 4661
(2013/07/26)
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- Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture
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The RNA replication machinery of HCV is a multi-subunit membrane-associated complex. NS5A has emerged as an active component of HCV replicase, possibly involved in regulation of viral replication and resistance to the antiviral effect of interferon. We report here substituted piperazinyl-N-(aryl)benzamides as potent inhibitors of HCV replication exerted via modulation of the dimerization of NS5A.
- Conte, Immacolata,Giuliano, Claudio,Ercolani, Caterina,Narjes, Frank,Koch, Uwe,Rowley, Michael,Altamura, Sergio,Francesco, Raffaele De,Neddermann, Petra,Migliaccio, Giovanni,Stansfield, Ian
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scheme or table
p. 1779 - 1783
(2009/12/03)
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- PYRROLIDINE DERIVATIVES AS ERK INHIBITORS
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Disclosed are the ERK inhibitors of Formula (1.0): and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (1.0).
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Page/Page column 181-182
(2010/11/28)
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