- Multi-substituted amine compound and its preparation and use (by machine translation)
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The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)
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Paragraph 0883; 0887-0890
(2018/04/27)
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- Multicomponent Diene-Transmissive Diels-Alder Sequences Featuring Aminodendralenes
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1-Aminodecalins were prepared from acyclic precursors by combining the powerful twofold diene-transmissive Diels-Alder chemistry of [3]dendralenes with the simplicity of enamine formation. On mixing at ambient temperature, a simple dienal condenses with a primary or secondary amine to generate the enamine, a 1-amino-[3]dendralene in situ, and this participates as a double diene in a sequence of two Diels-Alder events with separate dienophiles. Overall, four C-C bonds and one C-N bond are formed. Mechanistic insights into these reactions are provided by means of density functional theory calculations.
- Tan, Siu Min,Willis, Anthony C.,Paddon-Row, Michael N.,Sherburn, Michael S.
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supporting information
p. 3081 - 3085
(2016/03/12)
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- Copper-Catalyzed Amino Lactonization and Amino Oxygenation of Alkenes Using O-Benzoylhydroxylamines
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A copper-catalyzed amino lactonization of unsaturated carboxylic acids has been achieved as well as the analogous intermolecular three-component amino oxygenation of olefins. The transformation features mild conditions and a remarkably broad substrate sco
- Hemric, Brett N.,Shen, Kun,Wang, Qiu
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supporting information
p. 5813 - 5816
(2016/06/09)
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- MONOSUBSTITUTED DIAZABENZIMIDAZOLE CARBENE METAL COMPLEXES FOR USE IN ORGANIC LIGHT EMITTING DIODES
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An organic electronic device, preferably an organic light-emitting diode (OLED), comprising at least one metal-carbene complex comprising one, two or three specific bidentate diazabenzimidazole carbene ligands;a light-emitting layer comprising said metal-carbene complex as emitter material, preferably in combination with at least one host material;the use of said metal-carbene complex in an OLED;an apparatus selected from the group consisting of stationary visual display units, mobile visual display units, illumination units, units in items of clothing, units in handbags, units in accessoires, units in furniture and units in wallpaper comprising said organic electronic device, preferably said OLED, or said light-emitting layer;the metal-carbene complex comprising one, two or three specific bidentate diazabenzimidazole carbene ligands mentioned above and a process for the preparation of said metal-carbene complex.
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Page/Page column 104
(2015/01/16)
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- Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
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The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
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Paragraph 1822
(2013/03/26)
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- TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
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The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
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Page/Page column 125
(2012/03/10)
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- NOVEL POLYMERIZABLE MONOMER, AND MATERIAL FOR ORGANIC DEVICE, HOLE INJECTION/TRANSPORT MATERIAL, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENT AND ORGANIC ELECTROLUMINESCENT ELEMENT EACH COMPRISING POLYMER (POLYMERIC COMPOUND) OF THE POLYMERIZABLE MONOMER
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A polymerizable monomer represented by the following formula (1) wherein at least one of Ar1 to Ar3 is substituted by a group represented by the following formula (2) and which is substituted by one or more groups comprising a polymerizable functional group. Ar1 to Ar3 are a substituted or unsubstituted aryl group having 6 to 40 ring carbon atoms, Ar6 is a substituted or unsubstituted aryl group having 6 to 40 ring carbon atoms and Ar4 and Ar5 are a substituted or unsubstituted arylene group having 6 to 40 ring carbon atoms.
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- Pinene-derived iminodiacetic acid (PIDA): A powerful ligand for stereoselective synthesis and iterative cross-coupling of C(sp3) boronate building blocks
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Efficient access to chiral C(sp3) boronates in stereochemically pure form is critical for realizing the substantial potential of such building blocks in complex-molecule synthesis. We herein report that a pinene-derived iminodiacetic acid (PIDA) ligand enables the highly diastereoselective synthesis of a wide range of oxiranyl C(sp3) boronates from the corresponding olefins. These oxiranyl PIDA boronates, in turn, can be readily transformed into unprecedented stable α-boryl aldehydes via a novel 1,2-migration of the boronate group that proceeds with complete maintenance of stereochemical purity. B-Protected haloboronic acids containing dual sp3-hybridized C centers are readily accessible via this platform, and the herein demonstrated capacity for stereocontrolled iterative C(sp3) cross-coupling with this novel type of bifunctional reagent to access a medicinally important chiral small-molecule target in highly enantioenriched form represents a substantial advance for the building-block-based approach to synthesis.
- Li, Junqi,Burke, Martin D.
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supporting information; experimental part
p. 13774 - 13777
(2011/10/09)
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- FUROPYRIDINE COMPOUNDS AND USES THEREOF
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The present invention provides a compound of formula (I); a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Page/Page column 171
(2011/11/06)
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- PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS
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Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
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Page/Page column 85
(2009/02/11)
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- CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.
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Page/Page column 23
(2009/01/23)
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- CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems ofthe industrialized world In formula I, A-B is an arylamide moiety
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Page/Page column 24
(2009/01/23)
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- Catalytic enantioselective allyl- and crotylboration of aldehydes using chiral diol·SnCl4 complexes. Optimization, substrate scope and mechanistic investigations
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We report a novel class of C2-symmetric chiral diols derived from the hydrobenzoin skeleton. The combination of these diols with SnCl 4 under Yamamoto's concept of Lewis acid assisted Bronsted acidity (LBA catalysis) leads to high levels of asymmetric induction in the allylboration of aldehydes by commercially available allylboronic acid pinacol ester 1a. The corresponding homoallylic alcohol products of synthetically useful aliphatic aldehydes are obtained in excellent yields with up to 98:2 er. This combined acid manifold is also efficient in catalyzing the diastereo- and enantioselective crotylboration of aldehydes, thus providing the propionate units in >95:5 dr and up to 98:2 er. The X-ray crystal structure of the optimal diol·SnCl4 complex, Vivol (4m)·SnCl 4, unambiguously shows the Bronsted acidic character of this LBA catalyst and its highly dissymmetrical environment. Further controls have ruled out a possible boron transesterification mechanism with the chiral diol and point to LBA catalyst-derived activation of the pinacol allylic boronates 1. Due to slow dissociation of the diol·SnCl4 complex, a small excess of diol is required in order to suppress a competing racemic cycle catalyzed by free SnCl4.
- Rauniyar, Vivek,Zhai, Huimin,Hall, Dennis G.
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supporting information; experimental part
p. 8481 - 8490
(2009/02/02)
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- Isolation and X-ray structural characterization of tetraisopropylpyrene cation radical
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A practical synthesis of 1,3,6,8-tetraisopropylpyrene and the isolation and X-ray structural characterization of its monomeric cation radical salt are described. The Royal Society of Chemistry.
- Banerjee, Moloy,Vyas, Vijay S.,Lindeman, Sergey V.,Rathore, Rajendra
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p. 1889 - 1891
(2008/12/22)
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- CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.
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Page/Page column 50
(2009/01/23)
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- TRISUBSTITUTED AMINE COMPOUND
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The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
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Page/Page column 166-167
(2008/06/13)
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- Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
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The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 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 103
(2010/11/25)
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- Expanding organoboron chemistry: Epoxidation of potassium organotrifluoroborates
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Most organoboron reagents are highly susceptible to oxidation by a variety of oxidants. In these processes, the valuable carbon-boron bond is cleaved. The organotrifluoroborates examined in this contribution appear resistant to many common oxidants. Conse
- Molander, Gary A.,Ribagorda, Maria
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p. 11148 - 11149
(2007/10/03)
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- Substituted benzoylguanidines process for their preparation their use as a medicament or diagnostic and medicament containing them
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There are described benzoylguanidines of the formula I STR1 where R(1) is hydrogen, Hal, --NO2, --CN, --CF3, R(4)--SOm or R(5)R(6)N--SO2 --, where m is zero to 2, R(4) and R(5) are alk(en)yl or --Cn H
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- Asymmetric aldol reactions using (4R-trans)-2-(1-methylethenyl)-1,3,2-dioxaborolane-4,5-dicarboxylic acid, bis-ethyl ester, a chiral precursor of the acetone enolate
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(4R-trans)-2-(1-Methylethenyl)-1,3,2-dioxaborolane-4,5-dicarboxylic acid, bis-ethyl ester upon oxidation with trimethylamine oxide gives a chiral enol borate that condenses with aldehydes to give optically active 4-hydroxy-2-alkanones in 55-77percent yield and 41-65percent e.e.
- Boldrini, Gian Paolo,Lodi, Luisa,Tagliavini, Emilio,Trombini, Claudio,Umani-Ronchi, Achille
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