- Efficient discovery of fluorescent chemosensors based on a biarylpyridine scaffold
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(Figure Presented) The discovery of several fluorescent chemosensors for Hg(II) and Ag(I) In mixed aqueous solution Is reported. The ease with which these fluorlonophores were prepared from a common core underscores the utility of conformational restriction as a signaling mechanism. In addition, for the first time, significant changes were observed In biarylpyridlne emission wavelength, allowing ratlometric detection of Hg(II) and Ag(I). Finally, on the basis of computational analyses, beneficial structural modifications were predicted for the next generation of chemosensors.
- Malashikhin, Sergey A.,Baldridge, Kim K.,Finney, Nathaniel S.
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Read Online
- Square tiling by square macrocycles at the liquid/solid interface: Co-crystallisation with one- or two-dimensional order
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We have systematically investigated the self-assembled monolayers of seven bimolecular mixtures of square-shaped pyridinophanes and cyclophanes bearing alkoxy or alkoxycarbonyl substituents in the presence of the tropylium ion as a marker of pyridinophane
- Tahara, Kazukuni,Gotoda, Jun,Carroll, Calden N.,Hirose, Keiji,Defeyter, Steven,Tobe, Yoshito
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- Multi-functionalized 2,2′:6′,2″-terpyridines
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In this contribution, Stille-type cross-coupling procedure is shown to be an easy and universal way to prepare a variety of functionalized terpyridines. They may be functionalized in one step with different substituents at the outer pyridine rings and at
- Heller, Marcel,Schubert, Ulrich S.
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Read Online
- Functionalized 2,2′-bipyridines and 2,2′:6′,2″-terpyridines via stille-type cross-coupling procedures
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Stille-type cross-coupling procedures are utilized in order to prepare a variety of functionalized 2,2′-bipyridines and 2,2′:6′,2″-terpyridines. Such N-heterocyclic compounds are of great interest as chelating ligands for transitionmetal ions in the field of supramolecular chemistry. Various mono- and disubstitued 2,2′-bipyridines were synthesized in high yields and multigram scales using a modular design principle. The terpyridines may be functionalized in one step with different substituents at the outer pyridine rings and at the 4′-position of the centered ring, leading to multifunctionalized compounds. The initially obtained methyl ester and ethyl ester groups can be simply converted into bromomethyl and hydroxymethyl groups which allow further functionalization reactions.
- Heller, Marcel,Schubert, Ulrich S.
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- Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity
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To obtain a new anticancer drug, we focused on FER tyrosine kinase. Starting with high-throughput screening with our in-house chemical library, compound 1, which has a pyridine moiety, was found. Referring to their X-ray crystal structure with FES proto-oncogene tyrosine kinase, as a surrogate of FER followed by chemical modification including scaffold hopping of the pyridine template, we discovered pyrido-pyridazinone derivatives with potent FER kinase inhibitory activity. Here, we disclose the structure-activity relationship on the scaffold and representative compound 21 (DS21360717), which showed in vivo antitumor efficacy in a subcutaneous tumor model.
- Taniguchi, Toru,Inagaki, Hiroaki,Baba, Daichi,Yasumatsu, Isao,Toyota, Akiko,Kaneta, Yasuyuki,Kiga, Masaki,Iimura, Shin,Odagiri, Takashi,Shibata, Yoshihiro,Ueda, Kiyono,Seo, Maki,Shimizu, Hiroki,Imaoka, Tomoki,Nakayama, Kiyoshi
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supporting information
p. 737 - 742
(2019/04/01)
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- 2 Tyrosine kinase mediated signal transduction inhibitors
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Disclosed herein are compounds of Formula (), and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, X, X, X, X, X, and n are as defined herein, pharmaceutical compositions comprising same, and methods of preparation and use.
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Paragraph 0399-0401; 0589-0592;
(2019/09/17)
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- NOVEL PTEFB INHIBITING MACROCYCLIC COMPOUNDS
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The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
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Page/Page column 101
(2018/10/25)
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- POTASSIUM CHANNEL MODULATORS
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Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
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Paragraph 0193-0194
(2018/01/14)
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- NOVEL MACROCYCLIC SULFONDIIMINE COMPOUNDS
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The present invention relates to novel macrocyclic sulfondiimine compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
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Page/Page column 102
(2017/08/01)
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- NOVEL MODIFIED MACROCYCLIC COMPOUNDS
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The present invention relates to novel modified macrocyclic compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
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Page/Page column 154; 155
(2017/08/01)
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- NOVEL MACROCYCLIC COMPOUNDS
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The present invention relates to novel macrocyclic compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
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Page/Page column 107
(2015/11/27)
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- BICYCLIC INHIBITORS OF ALK
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The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
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Page/Page column 79
(2012/08/07)
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- Vectorial electron transfer in donor-photosensitizer-acceptor triads based on novel bis-tridentate ruthenium polypyridyl complexes
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The first examples of rodlike donor-photosensitizer-acceptor arrays based on bis-2,6-di(quinolin-8-yl)pyridine RuII complexes 1a and 3a for photoinduced electron transfer have been synthesized and investigated. The complexes are synthesized in a convergent manner and are isolated as linear, single isomers. Time-resolved absorption spectroscopy reveals long-lived, photoinduced charge-separated states (τCSS (1a)=140 ns, τCSS (3a)=200 ns) formed by stepwise electron transfer. The overall yields of charge separation (≥50% for complex 1a and ≥95% for complex 3a) are unprecedented for bis-tridentate RuII polypyridyl complexes. This is attributed to the long-lived excited state of the [Ru(dqp)2]2+ complex combined with fast electron transfer from the donor moiety following the initial charge separation. The rodlike arrangement of donor and acceptor gives controlled, vectorial electron transfer, free from the complications of stereoisomeric diversity. Thus, such arrays provide an excellent system for the study of photoinduced electron transfer and, ultimately, the harvesting of solar energy.
- Kumar, Rohan J.,Karlsson, Susanne,Streich, Daniel,Jensen, Alice Rolandini,Jaeger, Michael,Becker, Hans-Christian,Bergquist, Jonas,Johansson, Olof,Hammarstroem, Leif
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experimental part
p. 2830 - 2842
(2010/06/20)
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- Synthesis of 2,6-di(pyrazol-1-yl)-4-bromomethylpyridine, and its conversion to other 2,6-di(pyrazol-1-yl)pyridines substituted at the pyridine ring
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Two routes to 2,6-di(pyrazol-1-yl)-4-hydroxymethylpyridine (1) from 2,6-dihydroxy-isonicotinic acid, in four and six steps, are reported. Reaction of 1 with 48% HBr yields 2,6-di(pyrazol-1-yl)-4-bromomethylpyridine (2), which is a powerful precursor to a range of new tridentate ligands for transition metals functionalised at the pyridine ring. As a proof of principle, we describe the further elaboration of 2 to give two 2,6-di(pyrazol-1-yl)pyridines bearing nucleobase substituents, and the back-to-back ligand 1,2-bis[2,6-di(pyrazol-1-yl)pyrid-4-yl]ethane. Crystal structures of two of these new derivatives are presented.
- Elha?k, Jér?me,Pask, Christopher M.,Kilner, Colin A.,Halcrow, Malcolm A.
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p. 291 - 298
(2007/10/03)
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- Reversing the discovery paradigm: A new approach to the combinatorial discovery of fluorescent chemosensors
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We report here a new approach to the discovery of fluorescent chemosensors in which a new signaling mechanism allows a core fluorophore to be used in a combinatorial search for new binding events, thus reversing the reigning discovery paradigm. Copyright
- Mello, Jesse V.,Finney, Nathaniel S.
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p. 10124 - 10125
(2007/10/03)
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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- Electron transfer in a hydrogen-bonded assembly consisting of porphyrin-diimide
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Electron-transfer reactions in an H-bonded assembly composed of a diacylaminopyridine bearing zinc porphyrin and 1,8:4,5-naphthalenetetracarboxylic diimide(Ka = 2.8 × 102 dm3 mol-1) in benzene occur with kCS = 4.1 × 1010 s-1 and kCR = 3.7 × 109 s-1, while the corresponding covalently linked model with a comparable distance and energy gap undergoes electron transfer with kCS = 9.9 × 1010 s-1 and kCR = 6.7 × 108 s-1.
- Osuka, Atsuhiro,Yoneshima, Ryusho,Shiratori, Hideo,Okada, Tadashi,Taniguchi, Seiji,Mataga, Noboru
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p. 1567 - 1568
(2007/10/03)
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- Pesticidal cyclopropyl-2,4-dieneamides
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The present Application discloses pesticidally active compounds of the formula (I): or a salt thereof, wherein Q is an monocyclic aromatic ring. or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each optionally substituted, or Q is a dihalovinyl group or a group R6 --C C-- where R6 is C1-4 alkyl, tri C1-4 alkylsilyl, halogen or hydrogen; Q1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C1-3 alkyl. halo, C1-3 haloalkyl, alkynyl, or cyano; R2,R3, R4 and R5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo. C1-4 alkyl or C1-4 haloalkyl; X is oxygen or sulphur; and R1 is selected from hydrogen and C1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C1-6 alkoxy. their preparation, pesticidal compositions containing them and their use against pests.
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