- NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES
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The present invention discloses compounds according to Formula (I), wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, Y, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
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Paragraph 0448
(2020/12/11)
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- Total synthesis of diaportheone A
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Diaportheone A (1), a chromone natural product was previously isolated from the endophytic fungi Diaporthe sp. P 133. Its structure was established by spectroscopic methods, however, its absolute configuration remained undefined. This study dealt on the total synthesis of diaportheone A (1) utilizing the cyclization and in situ thermal syn-elimination of a β-ketosulfoxide. The C-1R absolute configuration of the natural product was established by X-ray crystallography of the synthetic diaportheone A (1) (>99% ee) and comparison with the optical rotation.
- Tan, Mario A.,Züger, Patrik Peter,Roggo, Silvio
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- N,B-bidentate boryl ligand-supported iridium catalyst for efficient functional-group-directed C-H borylation
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Convenient silylborane precursors for introducing N,B-bidentate boryl ligands onto transition metals were designed, prepared, and employed in ready formation of irdium(IIl) complexes via Si-B oxidative addition. A practical, efficient catalytic ortho-borylation reaction of arenes with a broad range of directing groups was developed using an in situ generated catalyst from the silylborane preligand 3c and [IrCl(COD)]2.
- Wang, Guanghui,Liu, Li,Wang, Hong,Ding, You-Song,Zhou, Jing,Mao, Shuai,Li, Pengfei
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supporting information
p. 91 - 94
(2017/05/16)
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- OPIOID RECEPTOR MODULATORS
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The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, 0, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alky
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Page/Page column 142
(2016/06/14)
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- 2-PYRIDYLOXY-3-ESTER-4-ETHER OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prev
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Page/Page column 53
(2015/06/25)
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- Circumambulatory movement of negative charge ("ring walk") during gas-phase dissociation of 2,3,4-trimethoxybenzoate anion
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A dramatic "ortho effect" was observed during gas-phase dissociation of ortho-, meta-, and para-methoxybenzoate anions. Upon activation under mass spectrometric collisional activation conditions, anions generated from all three isomers undergo a CO2 loss. Of the m/z 107 ions generated in this way, only the 1-dehydro-2-methoxybenzene anion from the ortho isomer underwent an exclusive formaldehyde loss. A peak for a formaldehyde loss in the spectra of 2,4-, 2,5-, and 2,6-dimethoxybenzoates and the absence of an analogous peak from 3,4- and 3,5-dimethoxy derivatives confirmed that this is a diagnostically useful ortho-isomer-specific phenomenon. Moreover, the spectrum from 2,3-dimethoxybenzoic acid showed peaks for two consecutive formaldehyde losses. The 1-dehydro-2,3,4-trimethoxybenzene anion (m/z 167) generated from 2,3,4-trimethoxybenzoate in this way endures three consecutive eliminations of formaldehyde units. For this, the negative charge, initially located on position 1, circumambulates to position 2, then to position 3, and finally to position 4 to form the final phenyl anion. The proposed stepwise fragmentation pathway, which resembles the well-known E1cB-elimination mechanism, is supported by tandem mass spectrometric observations made with 2-[13C 2H3]methoxy-3-[13C]methoxy-4-methoxybenzoic acid, and ab initio calculations. In addition, the spectra of ions such as 1-dehydro-3,4-dimethoxybenzene anion show peaks for consecutive methyl radical losses, a feature that establishes the 1,2-relationship between the two methoxy groups.
- Herath, Kithsiri B.,Weisbecker, Carl S.,Singh, Sheo B.,Attygalle, Athula B.
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p. 4378 - 4389
(2014/06/09)
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- BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
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The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
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Paragraph 0469
(2014/09/30)
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- Stereoselective Formal Synthesis of (-)-Salicylihalamides A and B Via Prins Cyclisation
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A stereoselective and convergent formal approach to Salicylihalamide A and B is achieved through our recently developed strategy for the construction of polyketide precursors via Prins cyclisation. The approach mainly relies upon reductive opening of 1-iodomethyl cyclic ethers, Mitsunobu inversion and ring closing metathesis along with Prins cyclisation.
- Yadav,Venkateswar Rao,Purushothama Rao,Sridhar Reddy,Prasad
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scheme or table
p. 457 - 460
(2011/09/14)
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- Synthesis and structural pattern recognition of 5-(2′-alkoxycarbonyl- substituted phenoxy)furfural derivatives
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The ethyl 5-(2′-alkoxycarbonyl-substituted phenoxy)furan-2- carboxylates (1C-13C) showed good antiplatelet aggregation,1) anti-allergic2) and anti-inflammatory activities.2) A series of 5-(2′-alkoxycarbonyl-substituted phenoxy)furfurals (1F-13F) were prepared for comparing the above activities. The objectives of this research are the synthesis and structural pattern recognition of compounds 1F-13F. The Silica Gel 60 column chromatography method was employed to separate and purify pure compounds 1F-13F by three solvent systems. For the structure elucidation of compounds 1F-13F, four spectroscopic methods were used: electron impact mass (EI-MS), UV-VIS, IR and NMR spectrometers. With the help of spectrometers, investigations can be performed on spectroscopic data. A simple methodology for recognizing structural patterns was carried out with the aid of statistical analysis designed to establish the classification model of the structural skeleton in this research. It was found that compounds 1C-13C and 1F-13F have similar chemical profiles and are clustered into one group. The pattern plots revealed valuable information and showed good correlation between compounds 1C-13C and 1F-13F. These findings correlate directly with the resulting spectroscopic data. These results with those obtained by EI-MS and NMR patterns give insight into a reliable pattern recognition for determining both 1C-13C and 1F-13F skeletons.
- Chang, Chia-Lin
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experimental part
p. 550 - 556
(2009/12/31)
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- Synthesis of xanthones, thioxanthones, and acridones by the coupling of arynes and substituted benzoates
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The reaction of silylaryl triflates, CsF, and ortho-heteroatom-substituted benzoates affords a general and efficient way to prepare biologically interesting xanthones, thioxanthones, and acridones. This chemistry presumably proceeds by a tandem intermolecular nucleophilic coupling of the benzoate with an aryne and a subsequent intramolecular electrophilic cyclization.
- Zhao, Jian,Larock, Richard C.
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p. 583 - 588
(2007/10/03)
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- De novo formal synthesis of (-)-apicularen A via an iterative asymmetric hydration sequence
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(Chemical Equation Presented) A de novo approach to the formal total synthesis of the macrolide natural product (-)-apicularen A has been achieved in 18 steps'from achiral starting materials. Both the absolute and relative stereochemistries of apicularen A were introduced by a Sharpless asymmetric dihydroxylation, a π-allyl-palladium catalyzed reduction, a stereoselective reduction, and a base-promoted transannulation to install the C-9 stereocenter.
- Li, Miaosheng,O'Doherty, George A.
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p. 6087 - 6090
(2007/10/03)
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- Hydroxy-methoxybenzoic methyl esters: Synthesis and antifeedant activity on the pine weevil, Hylobius abietis
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The pine weevil Hylobius abietis (L.) (Coleoptera: Curculionidae) feeds on the bark of coniferous seedlings and is the economically most important forestry restocking pest in large parts of Europe. Substances with an antifeedant effect may offer an environmentally friendly alternative to insecticides for the protection of planted seedlings. Bioassays were performed on commercial and synthetic methyl hydroxy-methoxybenzoates in order to determine their possible antifeedant activity. Two methyl hydroxy-methoxybenzoates were synthesized by esterification and mono-O-methylation of two dihydroxybenzoic acids. A regioselective protection-deprotection strategy was used in the synthetic pathway of the other non-commercial esters, esterification and selective pivaloylation of the less-hindered hydroxyl group of other commercial dihydroxybenzoic acids gave diester intermediates, which then were O-methylated before methanolysis of the pivaloyl group which yielded the desired non-commercial methyl hydroxy-methoxybenzoates. The five synthesized methyl hydroxy-methoxybenzoic esters were complemented with commercial samples of the five other isomers of methyl hydroxy-methoxybenzoate and spectrometric data were collected for the complete set of isomers. All ten isomers were tested for their antifeedant effect on the pine weevil. The effect varied considerably among the hydroxy-methoxybenzoic esters. Methyl 2-hydroxy-3-methoxybenzoate showed the highest effect and may thus be a candidate for practical use in pine weevil pest management.
- Legrand, Sacha,Nordlander, G?ran,Nordenhem, Henrik,Borg-Karlson, Anna-Karin,Unelius, C. Rikard
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p. 829 - 835
(2007/10/03)
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- Therapeutic uses of di-aryl acid derivatives
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The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
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- New procedures for the selective synthesis of 2(2H)-pyranone derivatives and 3-aryl-4-iodoisocoumarins
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5-Iodo-2(2H)-pyranone derivatives have been selectively synthesized by reaction of stereodefined methyl 2-en-4-ynoates with iodine in MeCN, CH2Cl2 or C6H6 at 20°C (Method C) or by treatment of these esters with
- Biagetti, Matteo,Bellina, Fabio,Carpita, Adriano,Stabile, Paolo,Rossi, Renzo
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p. 5023 - 5038
(2007/10/03)
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- Synthesis of the core structure of apicularen a by transannular cyclization.
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[reaction: see text] An approach to the macrocyclic core of apicularen A is described. Thus, cross-coupling of the aryl triflate 7 with the vinylstannane 19 provided the styrene 20. Deprotection led to the dihydroxy acid 22. Through a size-selective macro
- Kuehnert, Sven M,Maier, Martin E
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p. 643 - 646
(2007/10/03)
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- Synthesis of a model system for the macrocyclic subunit of the oximidines
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Cross-coupling reaction of aryl triflate 1 and vinyl stannane 13 provided salicylic acid derivative 15. This compound was converted to the dihydroxy acid 16, which provided in a size-selective macrolactonization the two macrolides 17 and 18 in a ratio of 60:40. Compound 17 is a model of the macrocyclic core of the oximidines.
- Scheufler,Maier
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p. 1221 - 1224
(2007/10/03)
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- Regioselectivity in the Reductive Cleavage of Pyrogallol Derivatives: Reductive Electrophilic Substitution of Acetals of 2,3-Dimethoxyphenol
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Acetals of 2,3-dimethoxyphenol were used as the starting materials for the transformation of 1,2,3-trioxygenated benzenes into various 1-oxygenated-2,3-dicarbon-substituted benzenes, via regioselective reductive electrophilic substitution of the 2-methoxy
- Azzena, Ugo,Melloni, Giovanni,Pisano, Luisa
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p. 261 - 266
(2007/10/02)
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- Reductive Electrophilic Substitution of Pyrogallol Derivatives: Synthesis of 2,3-Disubstituted Phenols
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1,2-Dimethoxy-3-methoxymethoxybenzene, 1, was used as the starting material for the transformation of a 1,2,3-trioxybenzene into various 1-oxy-2,3-dicarbobenzenes, via regioselective reductive electrophilic substitution of the 2-methoxy group followed by
- Azzena, Ugo,Melloni, Giovanni,Pisano, Luisa
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p. 5635 - 5638
(2007/10/02)
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- SELECTIVE MONO O-ALKYLATION OF γ-RESORCYLYC ESTERS
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The use of diethylazodicarboxylate/triphenylphosphine for the selective mono-O-alkylation of γ-resorcylic esters is described.
- Bass, R. J.,Banks, B. J.,Snarey, M.
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p. 769 - 770
(2007/10/02)
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