- ATF6 MODULATORS AND USES THEREOF
-
Compounds (I) as modulators of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.
- -
-
Paragraph 178
(2021/04/17)
-
- Asymmetric Magnesium-Catalyzed Hydroboration by Metal-Ligand Cooperative Catalysis
-
Asymmetric catalysis with readily available, cheap, and non-toxic alkaline earth metal catalysts represents a sustainable alternative to conventional synthesis methodologies. In this context, we describe the development of a first MgII-catalyzed enantioselective hydroboration providing the products with excellent yields and enantioselectivities. NMR spectroscopy studies and DFT calculations provide insights into the reaction mechanism and the origin of the enantioselectivity which can be explained by a metal-ligand cooperative catalysis pathway involving a non-innocent ligand.
- Falconnet, Alban,Magre, Marc,Maity, Bholanath,Cavallo, Luigi,Rueping, Magnus
-
supporting information
p. 17567 - 17571
(2019/11/13)
-
- Silylative Kinetic Resolution of Racemic 1-Indanol Derivatives Catalyzed by Chiral Guanidine
-
Efficient kinetic resolution of racemic 1-indanol derivatives was achieved using triphenylchlorosilane by asymmetric silylation in the presence of chiral guanidine catalysts. The chiral guanidine catalyst (R,R)-N-(1-(β-naphthyl)ethyl)benzoguanidine was found to be highly efficient as only 0.5 mol % catalyst loading was sufficient to catalyze the reaction of various substrates with appropriate conversion and high s-values (up to 89). This catalyst system was successfully applied to the gram-scale silylative kinetic resolution of racemic 1-indanol with high selectivity.
- Yoshimatsu, Shuhei,Yamada, Akira,Nakata, Kenya
-
p. 452 - 458
(2018/02/19)
-
- Selective, Scalable Synthesis of C60-Fullerene/Indene Monoadducts Using a Microwave Flow Applicator
-
The synergy of continuous processing and microwave heating technologies has unlocked scalable (g/h), safe and efficient reaction conditions for synthesis of fullerene/indene-based organic photovoltaic acceptor materials in a nonchlorinated solvent with levels of productivity unparalleled by previous syntheses. The microwave flow reactor sustains high temperature while employing short residence times, reaction conditions which uniquely allow the selective synthesis of fullerene/indene monoadducts. Design of experiments analysis revealed residence time as the most crucial factor for conversion and selectivity control.
- Barham, Joshua P.,Tanaka, Satoko,Koyama, Emiko,Ohneda, Noriyuki,Okamoto, Tadashi,Odajima, Hiromichi,Sugiyama, Jun-Ichi,Norikane, Yasuo
-
p. 4348 - 4354
(2018/04/26)
-
- Synthesis of Indole-Dihydroisoquinoline Sulfonyl Ureas via Three-Component Reactions
-
Isoquinolines activated with sulfamoyl chlorides were reacted with indoles in a 3-component reaction to generate a library of dihydroisoquinoline derivatives. Using a differential protecting group strategy, products could be further derivatised. Synthesis of isoquinoline starting materials using several different methods is also described.
- Pearson, Stuart E.,Fillery, Shaun M.,Goldberg, Kristin,Demeritt, Julie E.,Eden, Jonathan,Finlayson, Jonathan,Patel, Anil
-
p. 4963 - 4981
(2018/12/13)
-
- COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
-
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
- -
-
Page/Page column 134; 135
(2017/09/15)
-
- HISTONE DEMETHYLASE INHIBITORS
-
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
- -
-
Paragraph 001050; 001051; 001057; 001058
(2014/06/24)
-
- NOVEL 3-HYDROXY-5-ARYLISOXAZOLE DERIVATIVE
-
[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
- -
-
Page/Page column 59
(2012/09/10)
-
- Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors
-
Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure-activity relationship of a series of hydroxamate BoNT/A inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.
- Capkova, Katerina,Yoneda, Yoshiyuki,Dickerson, Tobin J.,Janda, Kim D.
-
p. 6463 - 6466
(2008/04/02)
-
- Tricyclic indeno-pyrrole derivatives as serotonin receptor modulators
-
The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
- -
-
Page/Page column 11
(2008/06/13)
-
- Catalytic enantioselective Negishi reactions of racemic secondary benzylic halides
-
This report describes the first enantioselective cross-couplings of racemic secondary benzylic halides, specifically, nickel-catalyzed Negishi reactions of bromides and chlorides. The catalyst components are commercially available and air-stable, and the reaction is not highly oxygen- or moisture-sensitive (it can be set up in the air). The method has been applied to the catalytic enantioselective synthesis of intermediates employed by others in the generation of bioactive compounds (e.g., trikentrin A and an androgen receptor agonist). Copyright
- Arp, Forrest O.,Fu, Gregory C.
-
p. 10482 - 10483
(2007/10/03)
-
- Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/- indanes and structurally modified derivatives: Potent and selective inhibitors of aldosterone synthase
-
Elevated aldosterone levels are key effectors for the development and progression of congestive heart failure and myocardial fibrosis. Recently, we proposed inhibition of aldosterone synthase (CYP11B2) as an innovative strategy for the treatment of these
- Ulmschneider, Sarah,Müller-Vieira, Ursula,Klein, Christian D.,Antes, Iris,Lengauer, Thomas,Hartmann, Rolf W.
-
p. 1563 - 1575
(2007/10/03)
-
- Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: Potent inhibitors of aldosterone synthase
-
Elevated plasma aldosterone levels play a detrimental role in certain forms of congestive heart failure and myocardial fibrosis. We proposed aldosterone synthase (CYP11B2) as a novel target for the treatment of these diseases. In this study, the synthesis
- Ulmschneider, Sarah,Müller-Vieira, Ursula,Mitrenga, Markus,Hartmann, Rolf W.,Oberwinkler-Marchais, Sandrine,Klein, Christian D.,Bureik, Matthias,Bernhardt, Rita,Antes, Iris,Lengauer, Thomas
-
p. 1796 - 1805
(2007/10/03)
-
- Compounds that modulate PPAR activity and methods of preparation
-
This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.
- -
-
-