- BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE
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Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide- 3 kinase (PI3K) modulation activity or function having the Formula (I) structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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Page/Page column 78; 79
(2017/01/26)
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- BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE
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Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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Paragraph 0185-0186
(2017/01/23)
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- Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments
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Efficient syntheses of chiral fragments derived from chiral amino alcohols are described. Several unique scaffolds were readily accessed in 1-5 synthetic steps leading to 45 chiral fragments, including oxazolidinones, morpholinones, lactams, and sultams. These fragments have molecular weights ranging from 100 to 255 Da and are soluble in water (0.085 to >15 mM).
- Haftchenary, Sina,Nelson, Shawn D.,Furst, Laura,Dandapani, Sivaraman,Ferrara, Steven J.,Bo?kovi?, ?arko V.,Figueroa Lazú, Samuel,Guerrero, Adrian M.,Serrano, Juan C.,Crews, Demarcus K.,Brackeen, Cristina,Mowat, Jeffrey,Brumby, Thomas,Bauser, Marcus,Schreiber, Stuart L.,Phillips, Andrew J.
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supporting information
p. 569 - 574
(2016/10/06)
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- Chemoselective room temperature E1cB N-N cleavage of oxazolidinone hydrazides from enantioselective aldehyde α-hydrazination: Synthesis of (+)-1,4-dideoxyallonojirimycin
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Room temperature E1cB N-N cleavage of oxazolidinone hydrazides via N-alkylation with diethyl bromomalonate and potassium or caesium carbonate as base in acetonitrile is presented. The new method has a much improved chemoselectivity, which is illustrated by a concise total synthesis of the piperidine iminosugar (+)-1,4-dideoxyallonojirimycin.
- Ferreira, Jasmin,Rees-Jones, Sophie C. M.,Ramaotsoa, Valerie,Msutu, Ath'enkosi,Hunter, Roger
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supporting information
p. 1545 - 1549
(2016/02/09)
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- BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS.
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This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1 , R2, R3 and R4 are as defined herein.
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Page/Page column 104
(2015/09/22)
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- NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE
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Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis
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Page/Page column 29
(2011/10/04)
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- A homogeneous catalyst for reduction of optically active esters to the corresponding chiral alcohols without loss of optical purities
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A ruthenium complex was found to catalyze the hydrogen reduction of esters under mild and neutral conditions. A variety of optically active esters can be reduced to the corresponding alcohols in excellent yield without loss of their optical purity or causing undesirable side reactions. Hydrogen reduction needs such simple operations - reaction, concentration, and purification - that the violent quench step and extraction step, which accompany conventional sodium borohydride or lithium aluminum hydride reduction, can be omitted.
- Kuriyama, Wataru,Ino, Yasunori,Ogata, Osamu,Sayo, Noboru,Saito, Takao
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supporting information; experimental part
p. 92 - 96
(2010/06/17)
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- Synthesis of ring-fused oxazolo- and pyrazoloisoquinolinones by a one-pot Pd-catalyzed carboxamidation and aldol-type condensation cascade process
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(Chemical Equation Presented) A three-component cascade process is described for the synthesis of ring-fused oxazolo- and pyrazoloisoquinolinones by a one-pot carboxamidation/aldol-type condensation reaction. The cascade process involves Pd-catalyzed carboxamidation of an aryl halide/active methylene compound with oxazolidinone or pyrazolidinone, and subsequent intramolecular base-catalyzed cyclization/dehydration through an aldol-type condensation process, to give ring-fused oxazolo- and pyrazoloisoquinolinones. This methodology provides an easy one-step approach to these important classesof nitrogen-containing heterocycles and can tolerate a wide array of functional groups, including ester, nitrile, methoxy, and halide.
- Chouhan, Gagan,Alper, Howard
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supporting information; experimental part
p. 6181 - 6189
(2009/12/24)
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- Highly diastereoselective dioxetane formation in the photooxygenation of enecarbamates with an oxazolidinone chiral auxiliary: Steric control in the [2 + 2] cycloaddition of singlet oxygen through conformational alignment
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The photooxygenation of oxazolidinone-substituted enecarbamates leads to diastereomerically pure dioxetanes. The high diastereoselectivity is rationalized in terms of effective π-facial control achieved by shielding one side of the double bond with the ch
- Adam, Waldemar,Bosio, Sara G.,Turro, Nicholas J.
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p. 8814 - 8815
(2007/10/03)
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- Regiospecific reductive ring cleavage of N-substituted aziridine-2-carboxylates and An aziridine-2-methanol via catalytic hydrogenation using Pd as a catalyst
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Regiospecific reductive ring cleavage was accomplished in the reaction of N-α-methylbenzyl substituted aziridine-2-carboxylate and aziridine-2-methanol under a catalytic hydrogenation condition. The regiospecificity was determined by the substituent at C-
- Yeonhwa, Lim,Won, Koo Lee
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p. 8431 - 8434
(2007/10/02)
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- A New Electrophilic Alaninol Synthon. A General Route to Oxazolidinones of D or (R)-2-Amino Alcohols from L-Serine
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A new electrophilic alaninol synthon, (S)-4-(4'-tolylsulfonyloxymethyl)oxazolidin-2-one, derived from serine, undergoes nucleophilic displacements with Gilman cuprates and/or Grignard/CuX reagents in high yields to provide (R)-4-substituted oxazolidinones.
- Sibi, Mukund, P.,Rutherford, Drew,Sharma, Rajiv
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p. 1675 - 1678
(2007/10/02)
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