- 6-(4-Phenyl-benzyloxy-methyl) guvacine. Synthesis, GABA uptake inhibitor and muscarinic properties
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6-(4-Phenyl-benzyloxy-methyl) guvacine was synthesized. Surprisingly the compound was devoid of the γ-aminobutyric acid (GABA) uptake inhibitory activity of its parent compound guvacine, but instead showed affinities for the muscarinic M1 and M2 receptors.
- Bisel, Philippe,Gies, Jean Pierre,Schlewer, Gilbert,Wermuth, Camille G.
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- Nuclearity growth towards Ni(ii) cubane in self-assembly with 2-hydroxymethyl pyridine (hmpH) and 5-ethoxycarbonyl-2-hydroxymethyl pyridine (5-ehmpH)
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Self-assembly of NiX2 (X = Br or OAc) with 2-hydroxymethyl pyridine (hmpH) and 5-ethoxycarbonyl-2-hydroxymethyl pyridine (5-ehmpH) results in six new Ni(ii) complexes viz. [Ni(hmpH)2(H2O) 2]Br2 (1), [Ni4(hmp)4(-OAc) 4] (2), [Ni2(-Br)2(5-ehmpH)4]Br 2·0.33MeCN·0.67H2O (3), [Ni(5-ehmpH) 3]Br2·0.33MeOH (4), [Ni4(5-ehmp) 4(H2O)4Br4] (5) and [Ni 4(5-ehmp)4(-OAc)2(OAc)2(H 2O)2] (6), all of which have different chemical compositions and structures. Complexes 2, 5 and 6, however, share a common cubane [Ni4O4] core in which the deprotonated alkoxypyridine serves as a bridge-chelate. The others (viz.1, 3, 4) are mono- or dinuclear with the alkoxypyridine remaining in its native acid form.
- Zhang, Wen-Hua,Sulaiman, Norlela Binte,Tio, P. X. Shaun,Hor, T. S. Andy
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- PHARMACEUTICAL COMPOUNDS
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The invention provides a composition of matter which: ? (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or ? (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 %
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Page/Page column 116-117
(2021/04/02)
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- PYRROLE DERIVATIVES AS PLK1 INHIBITORS
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The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof. The compounds are useful in the treatment of cancers.
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Page/Page column 115; 116
(2018/11/22)
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- PROCESS FOR THE PREPARATION OF 2,4- OR 2,5-PYRIDINEDICARBOXYLIC ACID AND COPOLYMERS DERIVED THEREFROM
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The present invention relates to processes for the formation of pyridinedicarboxylic acid (PDCA), in particular, 2,4-pyridinedicarboxylic acid (2,4-PDCA) and 2,5-pyridinedicarboxylic acid (2,5-PDCA), and mono- and diester derivatives thereof, from 3,4-dihydroxybenzoic acid, via a biocatalytic reaction using, for example, a protocatechuate dioxygenase such as protocatechuate 4,5-dioxygenase or protocatechuate 2,3-dioxygenase, and a nitrogen source. The invention also relates to copolymers that comprise the pyridinedicarboxylic acid monomers and derivatives thereof, processes for the formation of the copolymers and uses for the copolymers.
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Paragraph 0200-0201
(2018/06/09)
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- A pair of highly biotolerated diamagnetic and paramagnetic iron(II) complexes displaying electroneutrality
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A pair of structurally analogous macrocyclic iron(ii) complexes with a magnetic off-on relationship is reported that exhibit electroneutrality at neutral pH and high stability in physiological media. This has been achieved by external charge compensation using nicotinate pendent arms. No contact toxicity was observed for cells up to 4 mM for the low-spin and 2 mM for the high-spin complex. These results are a necessary precursor to the future design of turn-on probes with elevated biotolerance.
- Wang,Gondrand,Touti,Hasserodt
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p. 15391 - 15395
(2015/09/07)
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- A Ca2+-, Mg2+-, and Zn2+-Based Dendritic Contractile Nanodevice with Two pH-Dependent Motional Functions
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A contractile dendritic motional device is reported where metal ions with biological importance - Ca2+ (the main regulatory and signaling species of the natural muscles), Mg2+, and Zn2+ - initiate two kinds of motional functions. The first motional function is the metal-ion-induced contraction of a linear strand into a Z-shaped dinuclear complex, and the second one is the change of the height of Z-shaped complexes via transmetalation. By means of the pH-dependent counterligand tren, the two motional features of the machine can depend on alternate additions of acid and base. An optical response is associated with the conversion of the linear form (which is yellow) into the metalated Z-shaped one (which is red).
- Stadler, Adrian-Mihail,Karmazin, Lydia,Bailly, Corinne
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supporting information
p. 14570 - 14574
(2016/01/25)
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- NITROIMIDAZOXADIAZOCINE COMPOUNDS
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This invention relates to nitroimidazoxadiazocine compounds having the general Formula I, pharmaceutical compositions and uses of the same. The invention also relates to methods of making such nitroimidazoxadiazocine compounds of Formula I.
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Page/Page column 67
(2013/06/05)
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- Towards the synthesis of substituted porphyrins by a pyridyl group bearing a reactive functionality
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Pyridyl-substituted porphyrins bearing a reactive functionality were prepared via Suzuki cross-coupling reactions and resulted in very good yields. These compounds are precursors of new porphyrin architectures able to coordinate two metals: one in the porphyrin core and the second around the pyridyl moiety. During the coupling reactions, a higher reactivity of a chloro picolyl group was evidenced compared to a bromo function on the same reacting molecule.
- Ojaimi, Maya El,Habermeyer, Benoit,Gros, Claude P.,Barbe, Jean-Michel
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experimental part
p. 469 - 480
(2011/03/20)
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- Enantioselective Fujiwara-Moritani indole and pyrrole annulations catalyzed by chiral palladium(II)-NicOx complexes
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The catalytic asymmetric Fujiwara-Moritani ring closures of several indole-and pyrrole-based cyclization precursors are reported. These unprecedented oxidative palladium(II)-catalyzed annulations allow for the formation of a stereogenic quaternary carbon atom, and decent levels of enantiocontrol are seen in 5-exo-trig cyclizations (54% ee for an indole and 76% ee for a pyrrole) while 6-exo-trig ring closures afford essentially racemic material. Novel oxazoline ligands with a nicotine platform (NicOx) are pivotal for good catalytic turnover as conventional PyOx ligands failed to produce acceptable chemical yields. The preparation of these NicOx ligands as well as the syntheses of the cyclization precursors are described in detail.
- Schiffner, Julia A.,Woeste, Thorsten H.,Oestreich, Martin
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supporting information; experimental part
p. 174 - 182
(2010/04/02)
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids
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Nipecotic acid derivatives bearing an aryl iminoxymethyl side chain at the position 6 were synthesised and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives 2, 3 the introduction of the oxime function in the s
- N'Goka, Victor,Stenb?l, Tine B.,Krogsgaard-Larsen, Povl,Schlewer, Gilbert
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p. 889 - 895
(2007/10/03)
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- The preparation of pyridinecarboxylates from chloropyridines by the palladium-catalyzed alkoxycarbonylation
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The preparation of pyridinecarboxylates and pyridinedicarboxylates by alkoxycarbonylation of chloropyridines with carbon monoxide in the presence of palladium acetate and 1,1'-bis(diphenylphosphino)ferrocene is described. The process uses readily available starting materials and affords pyridinecarboxylates in good to very good yields.
- Bessard, Yves,Crettaz, Roger
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p. 2589 - 2602
(2007/10/03)
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- A new planar chiral bipyridine ligand
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Combined methods of cyclophane and bipyridine synthesis open the way to the new planar-chiral 2,2'-bipyridine 1, whose CD spectrum is strongly dependent on metal salts. The absolute configuration of the chiral precursor 2 could be assigned by comparison of experimental and theoretical CD spectra. The usefulness of planar chirality in heterocyclic transition metal ligands is revealed in experiments towards stereoselective catalysis using 1.
- Wo?rsdo?rfer, Udo,Vo?gtle, Fritz,Nieger, Martin,Waletzke, Mirko,Grimme, Stefan,Glorius, Frank,Pfaltz, Andreas
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p. 597 - 602
(2007/10/03)
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- Certain substituted phenoxy-methyl phenyl-methoxy benzenes having antiviral activity
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A compound represented by formula I wherein Ar1 and Ar2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C1 -C10) alkyl, (C1 -C10) alkoxy, halogen, carbamyl, (C1 -C10) alkoxycarbonyl, oxazoyl, and (C1 -C10) alkyl substituted by halogen, (C1 -C10) alkoxy, hydroxy, or (C1 -C10) alkoxycarbonyl; M is STR1 (C4 -C8) alkylene, (C4 -C8) alkenylene or (C4 -C8)-alkynylene; O is oxygen; or pharmaceutically acceptable salts thereof. as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
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- Aromatic Retinoic Acid Analogues. 2. Synthesis and Pharmacological Activity
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Aromatic analogues of (E)-1-(4-carboxyphenyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl)butadiene (1b) and its ethyl ester (1a) were synthesized as potential chemopreventive agents for the treatment of epithelial cancer and such skin diseases as psoriasis and cystic acne.The phenyl ring of 1 was replaced by 2-fluorophenyl, 2-methoxyphenyl, thienyl, furanyl, and pyridyl groups.The 1-fluorobutadiene analogue of 1 was also synthesized.With exception for the furanyl analogue, these compounds demonstrated good activity in reversing keratinization in hamster tracheal organ culture and in inhibiting the induction of ornithine decarboxylase in mouse epidermis by a tumor promoter.
- Dawson, Marcia I.,Chan, Rebecca,Hobbs, Peter D.,Chao, Wan-ru,Schiff, Leonard J.
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p. 1282 - 1293
(2007/10/02)
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- Colouring Matters from Fly Agaric, VII. - Constitution and Synthesis of Muscaflavin
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The constitution of the yellow dihydroazepine amino acid muscaflavin, isolated from mushrooms, has been established as 1a.This was confirmed by a biomimetic synthesis of the DL ester 1b, starting from pyridylalanine 12a via the glutaconic dialdehyde inter
- Barth, Hubert,Burger, Guenther,Doepp, Heinrike,Kobayashi, Makoto,Musso, Hans
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p. 2164 - 2179
(2007/10/02)
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