- A highly efficient synthesis of 2-[3-aminopropyl]-5,6,7,8-tetrahydronaphthyridine via a double Suzuki reaction and a Chichibabin cyclization
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Synthesis of 2-[3-aminopropyl]-5,6,7,8-tetrahydronaphthyridine was accomplished via a one-pot double Suzuki reaction followed by deprotection and a highly regioselective intramolecular Chichibabin cyclization. A variety of reactions conditions were screened for the Chichibabin cyclization including choice of base, solvent and reaction temperature.
- Palucki, Michael,Hughes, David L,Yasuda, Nobuyoshi,Yang, Chunhua,Reider, Paul J
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- RNAI AGENTS FOR INHIBITING EXPRESSION OF HIF-2 ALPHA (EPAS1), COMPOSITIONS THEREOF, AND METHODS OF USE
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The present disclosure relates to RNAi agents, for example, double stranded RNAi agents, able to inhibit HIF-2 alpha ( EPAS1 ) gene expression. Also disclosed are pharmaceutical compositions that include HIF-2 alpha RNAi agents and methods of use thereof. The HIF-2 alpha RNAi agents disclosed herein may be linked or conjugated to targeting ligands (such as compounds that have affinity for integrins, including alpha-v-beta-3 and alpha-v-beta-5 integrins) and pharmacokinetic (PK) enhancers, to facilitate the delivery to cells and tissues, including to clear cell renal cell carcinoma (ccRCC) cells and tumors. Delivery of compositions comprising the HIF-2 alpha RNAi agents in vivo provides for inhibition of HIF-2 alpha gene expression. The HIF-2 alpha RNAi agents can be used in methods of treatment of various diseases and disorders, including ccRCC.
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Paragraph 0240; 0266; 0300
(2020/07/25)
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- FLUORINATED TETRAHYDRONAPHTHYRIDINYL NONANOIC ACID DERIVATIVES AND USES THEREOF
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The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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Page/Page column 27; 60
(2016/09/15)
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- COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE
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This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administrat
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Page/Page column 27
(2016/10/11)
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- Fluorinated 3-(2-Oxo-3-(3-Arylpropyl)Imidazolidin-1-yl)-3-Arylpropanoic Acid Derivatives
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The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
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Paragraph 0300; 0315
(2014/08/19)
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- An efficient synthesis of an alphavbeta3 antagonist.
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A practical preparation of an alpha(v)beta(3) antagonist is reported. The antagonist consists of three key components, a tetrahydronaphthyridine moiety, a beta-alanine moiety, and a central imidazolidone moiety. The tetrahydronaphthyridine component was p
- Yasuda, Nobuyoshi,Hsiao,Jensen, Mark S,Rivera, Nelo R,Yang, Chunhua,Wells, Kenneth M,Yau, James,Palucki, Michael,Tan, Lushi,Dormer, Peter G,Volante, Ralph P,Hughes, David L,Reider, Paul J
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p. 1959 - 1966
(2007/10/03)
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- Methods for the synthesis of 5,6,7,8-tetrahydro-1,8-naphthyridine fragments for αvβ3 integrin antagonists
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The preparation of 3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propan-1- amine 2a and 3-[(7R)-7-methyl-5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl]propan-1- amine 2b, key intermediates in the synthesis of αvβ 3 antagonists, is described. The syntheses rely on the efficient double Sonogashira reactions of 2,5-dibromopyridine 3 with acetylenic alcohols 4a/4b and protected propargylamines 10a-e followed by Chichibabin cyclizations of 3,3′-pyridine-2,5-diyldipropan-1-amines 9a/9b.
- Hartner, Frederick W.,Hsiao, Yi,Eng, Kan K.,Rivera, Nelo R.,Palucki, Michael,Tan, Lushi,Yasuda, Nobuyoshi,Hughes, David L.,Weissman, Steven,Zewge, Daniel,King, Tony,Tschaen, Dave,Volante
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p. 8723 - 8730
(2007/10/03)
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- Process and intermediates to a tetrahydro-[1,8]- Naphthyridine
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A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of αv integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
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- Process and intermediates to a tetrahydro-[1,8]-naphthyridine
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A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of αv integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
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