- THERAPEUTIC COMPOUNDS AND METHODS OF USE
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The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
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Paragraph 0783; 0784; 0785
(2021/05/21)
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- COMPETITIVE AND NONCOMPETITIVE INHIBITORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M5
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Arylsulfonamides of 4-heteroaryl-piperidines, and their derivatives, are competitive and non-competitive inhibitors of the muscarinic acetylcholine receptor M5 (mAChR M5) and have utility in the treatment of psychiatric disorders such as substa
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Paragraph 00404
(2021/11/26)
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- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
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Paragraph 0668-0670
(2021/04/23)
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- Palladium-Catalyzed Chemoselective Oxidative Addition of Allyloxy-Tethered Aryl Iodides: Synthesis of Medium-Sized Rings and Mechanistic Studies
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This Letter describes a Pd-catalyzed Tsuji-Trost-type/Heck reaction with allyloxy-tethered aryl iodides and aziridines. The strategy provides efficient access to benzannulated medium-sized rings via intermolecular cyclization. The substrate aryl iodide ha
- Liu, Ce,Li, Yuke,Shi, Wei-Yu,Ding, Ya-Nan,Zheng, Nian,Liu, Hong-Chao,Liang, Yong-Min
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supporting information
p. 4311 - 4316
(2021/05/26)
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- Synthesis of All-Carbon Quaternary Centers by Palladium-Catalyzed Olefin Dicarbofunctionalization
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The redox-neutral dicarbofunctionalization of tri- and tetrasubstituted olefins to form a variety of (hetero)cyclic compounds under photoinduced palladium catalysis is described. This cascade reaction process was used to couple styrenes or acryl amides with a broad range of highly decorated olefins tethered to aryl or alkyl bromides (>50 examples). This procedure enables one or two contiguous all-carbon quaternary centers to be formed in a single step. The products could be readily diversified and applied in the synthesis of a bioactive oxindole analogue.
- Koy, Maximilian,Bellotti, Peter,Katzenburg, Felix,Daniliuc, Constantin G.,Glorius, Frank
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supporting information
p. 2375 - 2379
(2020/01/24)
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- Nickel-catalyzed removal of alkene protecting group of phenols, alcohols via chain walking process
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An efficient nickel-catalyzed removal of alkene protection group under mild condition with high functional group tolerance through chain walking process has been established. Not only phenolic ethers, but also alcoholic ethers can be tolerated with the retention of stereocenter adjacent to hydroxyl group. The new reaction brings the homoallyl group into a start of new type of protecting group.
- Meng, Chenkai,Niu, Haolin,Ning, Juehan,Wu, Wengang,Yi, Jun
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supporting information
(2020/02/04)
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- Iron-catalyzed protodehalogenation of alkyl and aryl halides using hydrosilanes
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A simple and efficient iron-catalyzed protodehalogenation of alkyl and aryl halides using phenylhydrosilane is disclosed. The reaction utilizes FeCl3 without the requirement of ligands. Unactivated alkyl and aryl halides were successfully reduced in good yields; sterically hindered tertiary halides were also reduced including the less reactive chlorides. The scalability of this methodology was demonstrated by a gram-scale synthesis with a catalyst loading as low as 0.5 mol%. Notably, disproportionation of phenylsilane leads to diphenylsilane that further reduces the halides. Preliminary mechanistic studies revealed a non-radical pathway and the source of hydrogen is PhSiH3via deuterium labeling studies. Our methodology represents simplicity and provides a good alternative to typical tin, aluminum and boron hydride reagents.
- Pilli, Ramadevi,Balakrishnan, Venkadesh,Chandrasekaran, Revathi,Rasappan, Ramesh
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supporting information
p. 1749 - 1753
(2019/02/20)
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- Green Organocatalytic Synthesis of Dihydrobenzofurans by Oxidation-Cyclization of Allylphenols
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A green and cheap protocol for the synthesis of dihydrobenzofurans via an organocatalytic oxidation of o -allylphenols is presented. The use of 2,2,2-trifluoroacetophenone and H 2 O 2 as the oxidation system, leads to a highly useful synthetic method, where a variety of substituted o -allylphenols were cyclized in high yields..
- Triandafillidi, Ierasia,Sideri, Ioanna K.,Tzaras, Dimitrios Ioannis,Spiliopoulou, Nikoleta,Kokotos, Christoforos G.
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supporting information
p. 4254 - 4260
(2017/09/12)
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- Pushing the Limits of Neutral Organic Electron Donors: A Tetra(iminophosphorano)-Substituted Bispyridinylidene
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A new ground-state organic electron donor has been prepared that features four strongly π-donating iminophosphorano substituents on a bispyridinylidene skeleton. Cyclic voltammetry reveals a record redox potential of ?1.70 V vs. saturated calomel electrode (SCE) for the couple involving the neutral organic donor and its dication. This highly reducing organic compound can be isolated (44 %) or more conveniently generated in situ by a deprotonation reaction involving its readily prepared pyridinium ion precursor. This donor is able to reduce a variety of aryl halides, and, owing to its redox potential, was found to be the first organic donor to be effective in the thermally induced reductive S N bond cleavage of N,N-dialkylsulfonamides, and reductive hydrodecyanation of malonitriles.
- Hanson, Samuel S.,Doni, Eswararao,Traboulsee, Kyle T.,Coulthard, Graeme,Murphy, John A.,Dyker, C. Adam
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supporting information
p. 11236 - 11239
(2016/07/06)
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- Synthesis and biological evaluation of novel n-[(7-pyridin-4-yl-2, 3-dihydro-benzofuran-2-yl) methyl]-(4-methyl-1, 2, 3-thiadiazole-5-yl) formamide as a potent immunosuppressant agent
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N-[(7-pyridin-4-yl-2, 3-dihydro-benzofuran-2-yl) methyl]-(4-methyl-1, 2, 3-thiadiazole-5-yl)-Formamide (1) was synthesized and its immunosuppressive activity was evaluated. The results showed it had highly immunosuppressive activity and can be studied as lead compound in the development of immunosuppressant agent.
- Fan, Chen,Wang, Yubin,Lu, Peng,Xue, Xiaojian,She, Jinxiong
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p. 375 - 379
(2014/03/21)
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- Silver-mediated trifluoromethylation-iodination of arynes
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An unprecedented silver-mediated vicinal trifluoromethylation-iodination of arynes that quickly introduces CF3 and I groups onto aromatic rings in a single step to give o-trifluoromethyl iodoarenes has been developed. A new reactivity of AgCF3 has been revealed, and 2,2,6,6-tetramethylpiperidine plays an important role in this difunctionalization reaction.
- Zeng, Yuwen,Zhang, Laijun,Zhao, Yanchuan,Ni, Chuanfa,Zhao, Jingwei,Hu, Jinbo
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supporting information
p. 2955 - 2958
(2013/04/10)
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- Electron transfer promoted photochemical reductive radical cyclization reactions of allyl 2-bromoaryl ethers
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Tin-free, photoinduced electron transfer promoted reductive radical cyclization reactions of allyl 2-bromoaryl ethers in the presence of NaOH in 2-PrOH were found to take place efficiently to give 3-methyl-2,3- dihydrobenzofurans. In contrast to conventio
- Yoshimi, Yasuharu,Kanai, Hirotomo,Nishikawa, Keisuke,Ohta, Yasushi,Okita, Yoshiki,Maeda, Kousuke,Morita, Toshio
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supporting information
p. 2419 - 2422
(2013/06/26)
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- 5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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Page/Page column 43
(2011/02/24)
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- NEW COMPOUNDS 574
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome,
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Page/Page column 27
(2010/06/13)
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- Regioselective iron-catalyzed decarboxylative allylic etherification
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[Chemical Equation Presented] An anionic iron complex catalyzes the decarboxylative allylation of phenols to form allylic ethers in high yield. The allylation is regioselective rather than regiospecific. This suggests that the allylation proceeds through π-allyl iron intermediates in contrast to related allylations of carbon nucleophiles that have been proposed to proceed via π-allyl complexes. Ultimately, iron catalysts have the potential to replace more expensive palladium catalysts that are typically utilized for decarboxylative couplings.
- Trivedi, Rushi,Tunge, Jon A.
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supporting information; experimental part
p. 5650 - 5652
(2010/02/28)
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- MACROCYCLIC GHRELIN RECEPTOR MODULATORS AND METHODS OF USING THE SAME
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The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
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Page/Page column 42-43
(2008/12/07)
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- Characterization of thyroid hormone receptor α (TRα)-specific analogs with varying inner- and outer-ring substituents
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Analogs of the TRα-specific thyromimetic CO23 were synthesized and analyzed in vitro using competitive binding and transactivation assays. Like CO23, all analogs bind to both thyroid hormone receptor subtypes with about the same affinity; however, modification of CO23 by derivatization of the 3′ position of the outer-ring or replacement of the inner-ring iodides with bromides attenuates binding. Despite lacking a preference in binding to TRα, all analogs display TRα-specificity in transactivation assays using U2OS and HeLa cells. At best, several agonists exhibit an approximately 6-12-fold preference in transactivation when tested with TRα in HeLa cells. One analog, CO24, showed in vivo TRα-specific action in a tadpole metamorphosis assay.
- Ocasio, Cory A.,Scanlan, Thomas S.
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p. 762 - 770
(2008/09/17)
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- Stereomanipulation of (η5-1-arylcyclohexadienyl)iron complexes
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A crystallographic investigation comparing five 1-aryl-substituted tricarbonyl[(1-5-η)-cyclohexadienyl]iron(1+) salts demonstrates that introducing additional electron density on the aromatic ring increases π overlap between the arene and the cyclohexadienyl ligand, thus flattening the structures sufficiently to make available a conformation in which nucleophiles can approach the site of substitution, despite the steric blockade of o-benzyl substituents. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Anson, Christopher E.,Malkov, Andrei V.,Roe, Caroline,Sandoe, Elizabeth J.,Stephenson, G. Richard
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p. 196 - 213
(2008/09/18)
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- Benzodioxane and benzodioxolane derivatives and uses thereof
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Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, n, m, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
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Page/Page column 69-70
(2010/11/24)
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- Azidosubstituted arylboronic acids: Synthesis and Suzuki-Miyaura cross-coupling reactions
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Arylboronic acids having a remote azido group were prepared from the corresponding azidosubstituted aryl bromides via lithiation and treatment with trialkyl borates. Preparative yields were achieved when the starting aryl bromides possessed ortho-alkoxy groups, which would stabilize the intermediate aryllithium species. Conventional Suzuki cross-coupling of the arylboronic acids proceeded generally well with retention of azido group; however, sometimes azidomethyl fragment underwent oxidative transformation into a nitrile.
- Sviridov, Sergey I.,Vasil'ev, Andrei A.,Sergovskaya, Natalia L.,Chirskaya, Marina V.,Shorshnev, Sergey V.
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p. 2639 - 2647
(2007/10/03)
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- DIHYDROBENZOFURAN COMPOUNDS AND USES THEREOF
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Dihydrobenzofuran compounds of Formula (I), including salts, prodrugs, hydrates and solvates thereof, that act as 5-HT2 receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in anima
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Page/Page column 34
(2010/02/15)
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- FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS
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Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.
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Page/Page column 108
(2010/10/20)
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- On the Reactivity of o-Lithioaryl Ethers: Tandem Anion Translocation and Wittig Rearrangement
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(matrix presented) Allyl and benzyl 2-lithioaryl ethers, generated by bromine-lithium exchange in THF, undergo a new tandem anion translocation-[1,2]-Wittig rearrangement allowing the isolation of the corresponding benzylic alcohols.
- Barluenga, Jose,Fananas, Francisco J.,Sanz, Roberto,Marcos, Cesar,Trabada, Marta
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p. 1587 - 1590
(2007/10/03)
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- Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 1. Discovery and optimization of salicylaldehyde thiosemicarbazone thrombopoietin mimics
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High-throughput screening has resulted in the discovery of thiosemicarbazone thrombopoietin mimics. A shared pharmacophore hypothesis between this series and a previously identified class, the pyrazol-4-ylidenehydrazines, led to the rapid optimization of
- Duffy, Kevin J.,Shaw, Anthony N.,Delorme, Evelyne,Dillon, Susan B.,Erickson-Miller, Connie,Giampa, Leslie,Huang, Yifang,Keenan, Richard M.,Lamb, Peter,Liu, Nannan,Miller, Stephen G.,Price, Alan T.,Rosen, Jon,Smith, Heather,Wiggall, Kenneth J.,Zhang, Lihua,Luengo, Juan I.
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p. 3573 - 3575
(2007/10/03)
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- Thermodynamic, spectroscopic, and density functional theory studies of allyl aryl and prop-1-enyl aryl ethers. Part 1. Thermodynamic data of isomerization
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A chemical equilibration study of the relative thermodynamic stabilities of seventy isomeric allyl aryl ethers (a) and (Z)-prop-1-enyl aryl ethers (b) in DMSO solution has been carried out. From the variation of the equilibrium constant with temperature the Gibbs energies, enthalpies, and entropies of isomerization at 298.15 K have been evaluated. Because of their low enthalpies, the (Z)-prop-1-enyl aryl ethers are strongly favored at equilibrium, the Gibbs energies of the a→b isomerization ranging from -12 to -23 kJ mol-1. The entropy contribution is negligible in most reactions, but occasionally small positive values less than +10 J K-1 mol-1 of the entropy of isomerization are found. The equilibration studies were also extended to involve two pairs of related isomeric ethers with a Me substituent on C(2) of the olefinic bond. The Me substituent was found to increase the relative thermodynamic stability of the allylic ethers by ca. 3.4 kJ mol-1.
- Taskinen, Esko
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p. 1824 - 1834
(2007/10/03)
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- Selectivity in the tandem cyclization - Carboxylation reaction of unsaturated haloaryl ethers catalyzed by electrogenerated nickel complexes
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The electrochemical reduction of a series of 2-haloaryl ethers containing allyl and propargyl groups under CO2 allows the synthesis of benzofuranacetic acid derivatives. This novel intramolecular cyclization- carboxylation reaction is carried out in single-compartment cells and is catalyzed by [Ni(cyclam)Br2].
- Olivero,Du?ach
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p. 1885 - 1891
(2007/10/03)
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- Induction of radical cyclizations with the 10-methyl-9,10-dihydroacridine / NaBH4 photocatalytic system
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The radical cyclization of suitably unsaturated aromatic halides, such as 1-allyloxy-2-halobenzenes (1a-d), can be induced with the 10-methyl-9,10-dihydroacridine / NaBH4 photocatalytic system in DMF. The method is preparatively useful with the most reactive halides.
- Boisvert, Guy,Giasson, Richard
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p. 6587 - 6590
(2007/10/02)
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- 2,3-Dihydro-7-benzofurancarboxylic Acids
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The syntheses of a series of title compounds 1 a-f bearing methyl groups in the heterocyclic part were described.Depending on the substitution pattern the Claisen rearrangement (path A) or the methodology of directed lithiations (path B) were used as the
- Stanetty, Peter,Koller, Herbert,Puerstinger, Gerhard
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p. 883 - 891
(2007/10/02)
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- THE REACTIONS OF ALLYL o-BROMOARYL ETHERS, N-ALLYL o-BROMOACETANILIDE, AND RELATED COMPOUNDS WITH TRIBUTYLTIN HYDRIDE IN THE PRESENCE OF ACTIVATED OLEFINS
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o-Bromophenyl allyl ether, N-allyl o-bromoacetanilide, and related compounds reacted with tributyltin hydride in the presence of activated olefins to give 2,3-dihydrobenzofuran, 2,3-dihydroindole, and analogous derivatives in modest yields respectively vi
- Togo, Hideo,Kikuchi, Osamu
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p. 373 - 381
(2007/10/02)
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- Benzopyran compounds, derivatives of prostaglandins
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Novel compounds of the following general formula: STR1
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