- MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
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- Selective aerobic oxidation of alkyl aromatics on Bi2MoO6 nanoplates decorated with Pt nanoparticles under visible light irradiation
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Pt/Bi2MoO6 nanoplates are efficient photocatalysts for the selective oxidation of saturated C-H bonds in alkyl aromatics under visible light illumination using O2 as an oxidant. This study opens a new window for direct C-H functionalization through the photocatalytic method based on cheap Bi2MoO6 semiconductor materials.
- Zhang, Bao,Yang, Xiaojing,Li, Jun,Cheng, Gang
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supporting information
p. 12194 - 12197
(2018/11/21)
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- 6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 48; 49
(2016/07/05)
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- METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 38
(2016/06/28)
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- ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 48-48
(2016/07/05)
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- FUSED HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Fused heteroaryl derivative compounds which are antagonists of orexin receptors are provided. The compounds can be used in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Also provided is a composition which comprises the compound can be use to prevent or treat such diseases in which orexin receptors are involved.
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Page/Page column 36; 37
(2016/07/27)
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- BRIDGED DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 45; 46
(2016/06/14)
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- Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors
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Inhibitors of Factor VIIa (FVIIa), a serine protease in the clotting cascade, have shown strong antithrombotic efficacy in preclinical thrombosis models with minimal bleeding liabilities. Discovery of potent, orally active FVIIa inhibitors has been largely unsuccessful because known chemotypes have required a highly basic group in the S1 binding pocket for high affinity. A recently reported fragment screening effort resulted in the discovery of a neutral heterocycle, 7-chloro-3,4-dihydroisoquinolin-1(2H)-one, that binds in the S1 pocket of FVIIa and can be incorporated into a phenylglycine FVIIa inhibitor. Optimization of this P1 binding group led to the first series of neutral, permeable FVIIa inhibitors with low nanomolar potency.
- Wurtz, Nicholas R.,Parkhurst, Brandon L.,Jiang, Wen,DeLucca, Indawati,Zhang, Xiaojun,Ladziata, Vladimir,Cheney, Daniel L.,Bozarth, Jeffrey R.,Rendina, Alan R.,Wei, Anzhi,Luettgen, Joseph M.,Wu, Yiming,Wong, Pancras C.,Seiffert, Dietmar A.,Wexler, Ruth R.,Priestley, E. Scott
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supporting information
p. 1077 - 1081
(2016/12/18)
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- Inclusion complex containing epoxy resin composition for semiconductor encapsulation
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The invention is an epoxy resin composition for sealing a semiconductor, including (A) an epoxy resin and (B) a clathrate complex. The clathrate complex is one of (b1) an aromatic carboxylic acid compound, and (b2) at least one imidazole compound represented by formula (II): wherein R2 represents a hydrogen atom, C1-C10 alkyl group, phenyl group, benzyl group or cyanoethyl group, and R3 to R5 represent a hydrogen atom, nitro group, halogen atom, C1-C20 alkyl group, phenyl group, benzyl group, hydroxymethyl group or C1-C20 acyl group. The composition has improved storage stability, retains flowability when sealing, and achieves an effective curing rate applicable for sealing delicate semiconductors.
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- Pincer thioamide and pincer thioimide palladium complexes catalyze highly efficient negishi coupling of primary and secondary alkyl zinc reagents at room temperature
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Pincer thioamide PdII complex 2 was prepared, and its reaction with cyclohexylzinc chloride yielded novel pincer thioimide PdII complex 3 besides Pd0 species. The structures of complexes 2 and 3 were confirmed by X-ray ana
- Wang, Haibo,Liu, Jing,Deng, Yi,Min, Tianyin,Yu, Ganxiang,Wu, Xiaojun,Yang, Zhen,Lei, Aiwen
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supporting information; experimental part
p. 1499 - 1507
(2009/08/07)
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- BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 167
(2008/12/07)
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- Protoberberins from Reissert Compounds VI [1]. Diastereoselective Synthesis and Relative Configuration of 2-Benzoyl-1-cyano-1-(1-phenylalkyl)-1,2-dihydroisoquinolines
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The alkylation of Reissert compounds 8 by sec-benzyl bromides 4, 7, and 10 diastereoselectively affords the title compounds 11 and 12. X-Ray structure analysis confirms an opposite configuration of the chiral centers in 11 and 12. The benzyl bromides 4, 7, and 10 are prepared by standard procedures.
- Reimann, Eberhard,Erdle, Wolfgang,Weigl, Claudia,Polborn, Kurt
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p. 313 - 326
(2007/10/03)
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- The Reactions of Carbene Intermediates from the Reaction of Trialkyl Phosphites with Dialkyl Benzoylphosphonates: Intramolecular Cyclisations of 2-Substituted Dialkyl Benzoylphosphonates
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The reaction of dialkyl aroylphosphonates 1 with trialkyl phosphites leads to the formation of carbene intermediates 3 via the anionic intermediates 2.The carbene intermediates 3 (R = 2-Me, 2-Prn, 2-Bun, 2-MeS, 2-EtO and 2-EtS) have
- Griffiths, D. Vaughan,Griffiths, Penelope A.,Karim, Khalku,Whitehead, Belinda J.
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p. 901 - 925
(2007/10/03)
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- Asymmetric syntheses of 1,6-dialkyl-1,4-cyclohexadiene derivatives
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Ortho-lithiation-alkylation of tertiary benzamide 3 provides a series of 2-substituted chiral benzatnides 3a-g (Scheme I). Birch reduction of 3a-j followed by alkylation of the resulting chiral amide enolate with Mel at -78 °C gives 1,6-di-alkyl-1,4-cyclohexadiene derivatives 4a-j with excellent diastereoselectivities (Table I). Applications of this asymmetric synthesis are illustrated by conversions of 4g to enantiomerically pure bicyclic lactone 9 and octalone 11 (Scheme III) and 4j to hexahydro-9-anthracenone 14 (Scheme IV).
- Schultz, Arthur G.,Green, Neal J.
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p. 4931 - 4936
(2007/10/02)
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- Reaction of O-Silylated Enolates of Carboxylic Esters with Benzyne. A Convenient Route to ortho-Alkylbenzoic Acids
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The reaction of O-silylated enolates of carboxylic esters with benzyne proceeds smoothly to afford ortho-alkylbenzoic acids in moderate yields.
- Ali, Syed Masarrat,Tanimoto, Shigeo
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p. 1465 - 1466
(2007/10/02)
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