- Improved Receptors for Dibutylmalonic Acid
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New molecular receptors with a dibenzacridine skeleton bearing functional groups complementary to dibutylmalonic acid have been developed.
- Mussons, Luisa,Raposo, Cesar,Crego, Mercedes,Anaya, Josefa,Caballero, Cruz,Moran, Joaquin R.
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- Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands
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A series of novel α-tetralone and α-tetralol derivatives was synthesized, and their binding affinities for 5-HT2A and D 2 receptors, the most important targets implicated in the anti-schizophrenia drug action, were evaluated to eluci
- Carro, Laura,Torrado, María,Ravi?a, Enrique,Masaguer, Christian F.,Lage, Sonia,Brea, José,Loza, María I.
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- Chirochromism-photochromism by epimerization: Search for a liquid crystal phototrigger
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A new class of photochromic reactions was investigated as a possible trigger for phase transitions in liquid crystals. Chirochromic compounds have two chiral units. One unit is fixed, and the other can be switched with light. A series of diastereomeric co
- Zhang, Mingbao,Schuster, Gary B.
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- Substituted 9-Diethylaminobenzo[ a]phenoxazin-5-ones (Nile Red Analogues): Synthesis and Photophysical Properties
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Nile Red is a benzo[a]phenoxazone dye containing a diethylamino substituent at the 9-position. In recent years, it has become a popular histological stain for cellular membranes and lipid droplets due to its unrivaled fluorescent properties in lipophilic environments. This makes it an attractive lead for chemical decoration to tweak its attributes and optimize it for more specialized microscopy techniques, e.g., fluorescence lifetime imaging or two-photon excited fluorescence microscopy, to which Nile Red has never been optimized. Herein, we present synthesis approaches to a series of monosubstituted Nile Red derivatives (9-diethylbenzo[a]phenoxazin-5-ones) starting from 1-naphthols or 1,3-naphthalenediols. The solvatochromic responsiveness of these fluorophores is reported with focus on how the substituents affect the absorption and emission spectra, luminosity, fluorescence lifetimes, and two-photon absorptivity. Several of the analogues emerge as strong candidates for reporting the polarity of their local environment. Specifically, the one- and two-photon excited fluorescence of Nile Red turns out to be very responsive to substitution, and the spectroscopic features can be finely tuned by judiciously introducing substituents of distinct electronic character at specific positions. This new toolkit of 9-diethylbenzo[a]phenoxazine-5-ones constitutes a step toward the next generation of optical molecular probes for advancing the understanding of lipid structures and cellular processes.
- Hornum, Mick,Mulberg, Mads W.,Szomek, Maria,Reinholdt, Peter,Brewer, Jonathan R.,Wüstner, Daniel,Kongsted, Jacob,Nielsen, Poul
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p. 1471 - 1488
(2021/01/13)
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- METHODS FOR MAKING QUINOLINYLDIAMINES
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The present disclosure provides methods for making quinolinyldiamine products from quinolinyl starting materials. In addition, the quinolinyldiamines can be used as ligands or ligand precursors for catalysts, e.g. for use in olefin polymerization.
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Paragraph 0253-0254
(2020/03/23)
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- THERAPEUTIC COMPOUNDS
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The invention provides compounds of formula (I): wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof. The compounds are SIRT2 inhibitors and are useful for treating SIRT2 associated conditions.
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Paragraph 0264; 0265; 0316
(2017/01/23)
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- Silver(I)-Promoted ipso-Nitration of Carboxylic Acids by Nitronium Tetrafluoroborate
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A novel and efficient method for the regioselective nitration of a series of aliphatic and aromatic carboxylic acids to their corresponding nitro compounds using nitronium tetrafluoroborate and silver carbonate in dimethylacetamide has been described. This transformation is believed to proceed via the alkyl-silver or aryl-silver intermediate, which subsequently reacts with the nitronium ion to form nitro substances. Mild reaction conditions, tolerant of a broad range of functional groups, and formation of only the ipso-nitrated products are the key features of this methodology when compared to known methods for syntheses of nitroalkyls and nitroarenes.
- Natarajan, Palani,Chaudhary, Renu,Venugopalan, Paloth
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p. 10498 - 10504
(2015/11/18)
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- NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF
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The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
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Paragraph 0563
(2013/10/08)
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- NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF
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The present invention relates to compounds of formula (I): wherein R6 is -CONH2 or a -C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
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Page/Page column 110
(2013/10/22)
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- Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins
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A series of novel tricyclic triazine-di-N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either hemisphere, resulted in TTO analogues that displayed hypoxia-selective cytotoxicity in vitro. Optimal rates of hypoxic metabolism and tissue diffusion coefficients were achieved with fused cycloalkyl rings in combination with both the 3-aminoalkyl or 3-alkyl substituents linked to weakly basic soluble amines. The selection was further refined using pharmacokinetic/pharmacodynamic model predictions of the in vivo hypoxic potency (AUCreq) and selectivity (HCD) with 12 TTO analogues predicted to be active in vivo, subject to the achievement of adequate plasma pharmacokinetics.
- Hay, Michael P.,Hicks, Kevin O.,Pchalek, Karin,Lee, Ho H.,Blaser, Adrian,Pruijn, Frederik B.,Anderson, Robert F.,Shinde, Sujata S.,Wilson, William R.,Denny, William A.
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supporting information; experimental part
p. 6853 - 6865
(2009/12/03)
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- M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: Serominic compounds
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Chronic low-dose treatment of rats with the psychomimetic drug, phencyclidine, induces regionally specific metabolic and neurochemical changes in the CNS that mirror those observed in the brains of schizophrenic patients. Recent evidence suggests that drugs targeting serotoninergic and muscarinic receptors, and in particular 5-HT7 antagonists and M4 agonists, exert beneficial effects in this model of schizophrenia. Compounds that display this combined pattern of activity we refer to as serominic compounds. Based upon leads from natural product screening, we have designed and synthesised such serominic compounds, which are principally arylamidine derivatives of tetrahydroisoquinolines, and shown that they have the required serominic profile in ligand binding assays and show potential antipsychotic activity in functional assays.
- Suckling, Colin J.,Murphy, John A.,Khalaf, Abedawn I.,Zhou, Sheng-ze,Lizos, Dimitris E.,van Nhien, Albert Nguyen,Yasumatsu, Hiroshi,McVie, Allan,Young, Louise C.,McCraw, Corinna,Waterman, Peter G.,Morris, Brian J.,Pratt, Judith A.,Harvey, Alan L.
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p. 2649 - 2655
(2008/02/02)
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- TRICYCLIC 1,2,4-TRIAZINE OXIDES AND COMPOSITIONS THEREFROM FOR THERAPEUTIC USE IN CANCER TREATMENTS
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The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula: (I); and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
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Page/Page column 126
(2008/06/13)
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- COMPOUNDS HAVING SEROTONIN 5-HT17 RECEPTOR ANTAGONIST ACTIVITY AND MUSCARINIC M4 RECEPTOR AGONIST ACTIVITY AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS
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The present invention relates to novel treatments for schizophrenia, based on the concept of identifying agents capable of selectively binding to the serotonin 5-HT7 and muscarinic M4 receptors and the use of such compounds in treating schizophrenia. The present invention also relates to novel amidine compounds for treating schizophrenia, a method of manufacturing such compounds, pharmaceutical formulations comprising said compounds, as well as medical uses and methods of treatment using said compounds.
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Page/Page column 47-48
(2008/06/13)
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- Benzocycloalkene compounds, their production and use
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A compound of the formula wherein R1and R2are H, a hydrocarbon group or a heterocyclic group, or R1and R2are combinedly a spiro ring; R3is a hydrocarbon group, a substituted amino group, a substituted
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- Sulfonamide-substituted compounds, process for their preparation, their use as a medicament or diagnostic, and a medicament comprising them
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Compounds of formula I in which R(1) to R(8) and X have the meanings indicated in the specification, are useful for the production of medicaments having K+ channel-blocking action; in particular for the production of a medicament for the treatment or prophylaxis of stimulated gastric acid secretion; of ulcers of the stomach and of the intestinal region; of reflux esophagitis; of diarrhea; of all types of arrhythmias, including ventricular and supraventricular arrhythmias; and of reentry arrhythmias and for the prophylaxis of sudden heart death as a result of ventricular fibrillation.
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- Carboxamides and anilides
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Described herein are compounds of the formula STR1 wherein R1 signifies hydrogen, lower-alkyl or a cation; R2 signifies hydrogen, lower-alkyl, lower-alkoxy or halogen; M signifies --CONH-- or --NHCO--; X and Y are each independently selected from the group consisting of >CR3 R4 and --CONR5 --; Z signifies >CR6 R7 ; R3, R4, R6 and R7 are each independently selected from the group consisting of hydrogen and lower-alkyl; R5 signifies alkyl; and n signifies 0, 1 or 2; provided that at least one of X or Y is --CONR5 -- which is bonded to the phenyl ring via the N atom. These compounds are useful in the treatment and prophylaxis of neoplasms, dermatoses and aging of the skin.
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- Synthesis and Evaluation of N,N-Di-n-propyltetrahydrobenzindol-7-amine and Related Congeners as Dopaminergic Agonists
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An evaluation of 6-indole (4), its rigid analogue N,N-di-n-propyl-5,6,7,8-tetrahydrobenzindol-7-amine (5), and some related congeners, for ability to suppress serum prolactin in reserpinized rats, revealed modest biological a
- Nichols, David E.,Cassady, John M.,Persons, Paul E.,Yeung, Ming C.,Clemens, James A.,Smalstig, E. Barry
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p. 2128 - 2134
(2007/10/02)
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