- RNAI AGENTS FOR INHIBITING EXPRESSION OF BETA-ENAC, COMPOSITIONS THEREOF, AND METHODS OF USE
-
Described are RNAi agents, compositions that include RNAi agents, and methods for inhibition of a beta-ENaC (SCNN1B) gene. The beta-ENaC RNAi agents and RNAi agent conjugates disclosed herein inhibit the expression of a beta-ENaC gene. Pharmaceutical comp
- -
-
Paragraph 0239; 0247;0251
(2021/05/07)
-
- ANTICANCER COMPOUNDS
-
The present invention discloses compounds for inhibition of uncontrolled cell proliferation particularly in cancer stem cells. Particularly, the invention relates to compounds of Formula III to XIV for the treatment of cancer, such as breast and prostate cancer.
- -
-
-
- MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
-
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
- -
-
Paragraph 00632
(2018/09/12)
-
- NOVEL PHENYL NAPTHOL DERIVATIVE
-
Phenylnaphthol derivatives represented by the following general formula (1), wherein, R 1 to R 3 are hydrogen atoms, alkyl groups or aryl groups, and R 2 and R 3 may be bonded together to form an aliphatic hydrocarbon ring or a heterocyclic ring, a and b are, respectively, integers of 0 to 4, R 4 and R 5 are hydroxyl groups, alkyl groups, haloalkyl groups, cycloalkyl groups, alkoxy groups, amino groups, heterocyclic groups having a nitrogen atom as a hetero atom and are bonded together via the nitrogen atom, cyano groups, nitro groups, formyl groups, hydroxycarbonyl groups, alkylcarbonyl groups, alkoxycarbonyl groups, halogen atoms, aralkylgroups, aralkoxy groups, aryloxy groups, aryl groups, heteroaryl groups bonded together via a carbon atom in the ring, alkylthio groups, cycloalkylthio groups, arylthio groups or heteroarylthio groups, and if R 4 or R 5 are present in a plural number, the plurality of R 4 or the plurality of R 5 may be the same or different, or 2 R 4 s or 2 R 5 s may be bonded together to form an alicyclic hydrocarbon ring or a heterocyclic ring. The compounds are useful as intermediate products for the synthesis of, for example, photochromic compounds.
- -
-
Paragraph 0256-0258
(2016/12/01)
-
- NOVEL PHENYLNAPHTHOL DERIVATIVES
-
Phenylnaphthol derivatives represented by the following general formula (1), wherein, R1 to R3 are hydrogen atoms, alkyl groups or aryl groups, and R2 and R3 may be bonded together to form an aliphatic hydrocarbon ring or a heterocyclic ring, a and b are, respectively, integers of 0 to 4, R4 and R5 are hydroxyl groups, alkyl groups, haloalkyl groups, cycloalkyl groups, alkoxy groups, amino groups, heterocyclic groups having a nitrogen atom as a hetero atom and are bonded together via the nitrogen atom, cyano groups, nitro groups, formyl groups, hydroxycarbonyl groups, alkylcarbonyl groups, alkoxycarbonyl groups, halogen atoms, aralkyl groups, aralkoxy groups, aryloxy groups, aryl groups, heteroaryl groups bonded together via a carbon atom in the ring, alkylthio groups, cycloalkylthio groups, arylthio groups or heteroarylthio groups, and if R4 or R5 are present in a plural number, the plurality of R4 or the plurality of R5 may be the same or different, or 2 R4s or 2 R5s may be bonded together to form an alicyclic hydrocarbon ring or a heterocyclic ring. The compounds are useful as intermediate products for the synthesis of, for example, photochromic compounds.
- -
-
Paragraph 0180; 0181; 0182
(2016/06/06)
-
- Facile synthesis of lipophilic δ-amino acid conjugates from 4-alkoxy-dithionaphthoic acids
-
(Chemical Equation Presented) Novel 4-alkoxy-dithionaphthoic acids were prepared and shown to be valuable synthons for δ-amino acid conjugates. These dithioacids are efficiently synthesized and purified, stable to storage, and easily derivatized to facilitate thioacylation chemistry. To this end, we have demonstrated dithionaphthoic acids (6) to successfully undergo coupling with both protected and unprotected amino acids, giving rise to stable thioamide conjugates (8 and 9). Copyright Taylor & Francis Group, LLC.
- Worth, Anna C.,Needham, Catherine E.,Franklin, Donald B.,Lampkins, Andrew J.
-
experimental part
p. 2694 - 2706
(2012/07/28)
-
- Sterically congested adamantylnaphthalene quinone methides
-
Five new (2-adamantyl)naphthol derivatives (5-9, quinone methide precursors, QMP) were synthesized and their photochemical reactivity was investigated by preparative photolyses, fluorescence spectroscopy, and laser flash photolysis (LFP). Excitation of QMP 5 to S1 leads to efficient excited state intramolecular proton transfer (ESIPT) coupled with dehydration, giving quinone methide QM5 which was characterized by LFP (in CH 3CN-H2O, λmax = 370 nm, τ = 0.19 ms). On irradiation of QMP 5 in CH3OH-H2O (4:1), the quantum yield of methanolysis is Φ = 0.70. Excitation of naphthols QMP 6-8 to S1 in CH3CN leads to photoionization and formation of naphthoxyl radicals. In a protic solvent, QMP 6-8 undergo solvent-assisted PT giving QM6 or zwitterion QM8 that react with nucleophiles delivering adducts, but with a significantly lower quantum efficiency. QMP 9 in a protic solvent undergoes two competitive processes, photosolvolysis via QM9 and solvent-assisted PT to carbon atom of the naphthalene giving zwitterion. QM9 has been characterized by LFP (in CH3CN-H2O, λmax > 600 nm, τ = 0.9 ms). In addition to photogenerated QMs, two stable naphthalene QMs, QM10 and QM11 were synthesized thermally and characterized by X-ray crystallography. QM10 and QM11 do not react with H2O but undergo acid-catalyzed fragmentation or rearrangement. Antiproliferative activity of 5-9 was investigated on three human cancer cell lines. Exposure of MCF-7 cells treated with 5 to 300 nm irradiation leads to an enhanced antiproliferative effect, in accordance with the activity being due to the formation of QM5.
- Veljkovic, Jelena,Uzelac, Lidija,Molcanov, Kresimir,Mlinaric-Majerski, Kata,Kralj, Marijeta,Wan, Peter,Basaric, Nikola
-
experimental part
p. 4596 - 4610
(2012/08/27)
-
- A new ring bromination method for aromatic compounds under solvent-free conditions with NBS/Al2O3
-
Alumina supported N-bromosuccinimide was found to be an efficient reagent for ring bromination of a number of aromatic compounds under solvent-free conditions. In the absence of the alumina the reactions are slow and some of the substrates are recovered unchanged. Under the reaction conditions aromatic oximes are converted into the corresponding carbonyl compounds. The method is simple, safe and rapid.
- Imanzadeh, Gholamhassan K.,Zamanloo, Mohammad R.,Eskandari, Habibollah,Shayesteh, Keyvan
-
p. 151 - 153
(2007/10/03)
-
- Structure-Activity Relationships of Potent, Selective Inhibitors of Neuronal Nitric Oxide Synthase Based on the 6-Phenyl-2-aminopyridine Structure
-
The synthesis and structure-activity relationships of a series of 6-phenyl-2-aminopyridines that potently and selectively inhibit the neuronal isoform of nitric oxide synthase (nNOS) are described. Compound 14bi from this series exhibits potent in vivo activity in harmaline-induced cGMP formation in rat cerebellum, a functional model of nNOS inhibition, and in the PCP-induced hypermotility model in the rat. These results suggest that 14bi may be a useful reagent for evaluating potential therapeutic applications of nNOS inhibitors in the central nervous system.
- Lowe III, John A.,Qian, Weimin,Drozda, Susan E.,Volkmann, Robert A.,Nason, Deane,Nelson, Robert B.,Nolan, Charles,Liston, Dane,Ward, Karen,Faraci, Steve,Verdries, Kim,Seymour, Pat,Majchrzak, Michael,Villalobos, Anabella,White, W. Frost
-
p. 1575 - 1586
(2007/10/03)
-
- 2-aminopyridines containing fused ring substituents
-
The present invention relates to 2-aminopyridine derivatives of the formula wherein G, R1 and R2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.
- -
-
-
- The synthesis and biological activity of two analogs of the anti-HIV alkaloid michellamine B
-
Two simplified analogs of the dimeric naphthalenyltetrahydroisoquinoline alkaloid michellamine B [4',4''-didesmethoxy-2',2''-didesmethylmichellamine B and 6,8-dihydroxy-5-(1',1''-dihydroxy-2',2''-binaphthalen-4'-yl)-1R,3R-dim ethyl-1,2,3,4-tetrahydroisoqu
- Upender,Pollart,Liu,Hobbs,Olsen,Chao,Bowden,Crase,Thomas,Pandey,Lawson,Dawson
-
p. 1371 - 1385
(2007/10/03)
-