- ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
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Page/Page column 453; 454
(2018/09/21)
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- ANGIOTENSIN-(1-7) ANALOGS AND METHODS RELATING THERETO
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Angiotensin (1-7) analogs are provided. The analogs contain one or more substitutions with non-natural amino acid cis-3-(aminomethyl)cyclobutanecarboxylic acid (ACCA). Also provided are methods of making such analogs and methods for using such analogs as
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Paragraph 0143; 0145
(2017/07/06)
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- Synthesis and reduction reactions of pyridones and 5-acyl-2-methoxypyridines
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The synthesis of a series of pyridones, from their 2-hydroxypyridine or 2-methoxypyridine precursors, is described, along with studies into their reductions to saturated heterocycles. A number of 5-acylpyridones were prepared and were evaluated as substrates for asymmetric transfer hydrogenation prior to conversion to saturated heterocycles. The enantioselective reduction of 5-acetyl-1-benzylpyrimidine-2,4(1H,3H)-dione is also described.
- Bisset, Alexander A.,Dishington, Allan,Jones, Teyrnon,Clarkson, Guy J.,Wills, Martin
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p. 7207 - 7220
(2017/09/12)
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- Synthesis of a conformationally constrained δ-amino acid building block
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Conformationally restricted amino acids are important components in peptidomimetics and drug design. Herein, we describe the synthesis of a novel, non-proteinogenic constrained delta amino acid containing a cyclobutane ring, cis-3(aminomethyl)cyclobutane
- O'Reilly, Elaine,Pes, Lara,Ortin, Yannick,Mueller-Bunz, Helge,Paradisi, Francesca
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p. 511 - 518
(2013/07/27)
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- Synthesis of (±)-strychnofoline via a highly convergent selective annulation reaction
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Studies aimed at preparing (±)-strychnofoline by total synthesis are detailed. The route described makes use of a recently developed MgI 2-mediated ring-expansion reaction of spiro[cyclopropan-1,3′- oxindole] with a cyclic disubstituted aldimin
- Lerchner, Andreas,Carreira, Erick M.
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p. 8208 - 8219
(2007/10/03)
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- A short synthesis of (±)-cytisine
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The synthesis of racemic cytisine 1 has been completed using (i) N-selective alkylation of 6-bromopyridone with bromide 6 and (ii) Pd(o) mediated intramolecular a-arylation of lactam 8 as key steps to achieve rapid assembly of the tricyclic core skeleton of the lupin alkaloids.
- Botuha, Candice,Galley, Carl M. S.,Gallagher, Timothy
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p. 1825 - 1826
(2007/10/03)
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- First total synthesis of (±)-strychnofoline via a highly selective ring-expansion reaction
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An efficient synthesis of the antitumor alkaloid (±)-strychnofoline is documented. Key to the development of the highly convergent strategy delineated is the coupling of a cyclic imine with spiro[cyclopropan-1,3'-oxindole], which takes place in a highly d
- Lerchner, Andreas,Carreira, Erick M.
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p. 14826 - 14827
(2007/10/03)
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