- PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES
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Pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts are disclosed, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha- synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, the compounds are used as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. Futher, the compounds are useful for measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
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Page/Page column 140
(2016/01/01)
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- Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
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The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification studies which led to compounds such as 42 with lower clearance, greater brain exposure and longer half life compared to earlier analogs.
- Bowers, Simeon,Truong, Anh P.,Jeffrey Neitz,Hom, Roy K.,Sealy, Jennifer M.,Probst, Gary D.,Quincy, David,Peterson, Brian,Chan, Wayman,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergely,Pan, Hu,Lin, May,Yao, Nanhua,Artis, Dean R.,Zhang, Heather,Chen, Linda,Dryer, Mark,Samant, Bhushan,Zmolek, Wes,Wong, Karina,Lorentzen, Colin,Goldbach, Erich,Tonn, George,Quinn, Kevin P.,Sauer, John-Michael,Wright, Sarah,Powell, Kyle,Ruslim, Lany,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
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scheme or table
p. 5521 - 5527
(2011/10/09)
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- A Facile and Novel Synthesis of 1,6-Naphthyridin-2(1H)-ones
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A new and convenient procedure for the synthesis of 1,6-naphthyridin-2(1H)-ones and their derivatives is described.In the first scheme 5-acetyl-6--1,2-dihydro-2-oxo-3-pyridinecarbonitrile (4) obtained by the reaction of N,N-dimet
- Singh, Baldev,Lesher, George Y.
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p. 2085 - 2091
(2007/10/02)
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- A General Approach to the Synthesis of 1,6-, 1,7-, and 1,8-Naphthyridines
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A new three-step procedure for pyridine annulation is described and illustrated with efficient syntheses of various 1,6-, 1,7-, and 1,8-naphthyridin-2-ones as well as 6-chloroquinolin-2-one.The regiospecific ortho metalation and subsequent formylation of
- Turner, James A.
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p. 4744 - 4750
(2007/10/02)
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- Condensed Heteroaromatic Ring Systems. IV. Synthesis of Naphthyridine Derivatives by Cyclization of Aminopyridineacrylic Esters
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The reaction of aminohalopyridines with ethyl acrylate in the presence of palladium(II)acetate and triarylphosphine gave ethyl aminopyridineacrylates.The cyclization of the resulting acrylates under basic conditions gave naphthyridinones having a carbostyril-type moiety.Keywords- intramolecular cyclization; palladium catalyst; ethyl acrylate; naphthyridinone; pyridineacrylic ester
- Sakamoto, Takao,Kondo, Yoshinori,Yamanaka, Hiroshi
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p. 4764 - 4768
(2007/10/02)
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- A new and convenient method for the amination of 1,6- and 1,7-naphthyridines using potassium amide/liquid ammonia/potassium permanganate
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Treatment of 3-nitro-1,6-naphthyridine, its 2-chloro-, 2-ethoxy- and 2-amino derivatives, with liquid ammonia, containing potassium permanganate, gave the corresponding 2-X-4-amino-3-nitro-1,6-naphthyridines (X=H, Cl, OEt, NH2).From 1H NMR spectroscopy sound evidence for the intermediacy of 2-X-4-amino-1,4-dihydro-3-nitro-1,6-naphthyridine is obtained.Similarly, from 5,8-dichloro(dibromo)-1,7-naphthyridine, the corresponding 2-amino-5,8-dichloro(dibromo)-1,7-naphthyridines were formed on treatment with liquid ammonia/potassium amide/potassium permanganate. 1H NMR evidence for the intermediary C-2 ?-adduct has been obtained.
- Wozniak, M.,Plas, H. C. van der,Tomula, M.,Veldhuizen, A. van
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p. 359 - 363
(2007/10/02)
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- NOVEL NAPHTHYRIDINES
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Novel naphthyridines having a 3-amino-2-OR-propoxy substituent are disclosed. The compounds have β-adrenergic blocking and immediate onset antihypertensive activities.
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