- FIBROBLAST GROWTH FACTOR 23 ANTAGONISTS AND RELATED COMPOSITIONS AND METHODS
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This disclosure relates to small molecule inhibitors of Fibroblast growth factor 23 (FGF-23) and related compositions and methods of treatment.
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Page/Page column 25-26; 34-35
(2019/05/15)
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- Transient-Ligand-Enabled ortho-Arylation of Five-Membered Heterocycles: Facile Access to Mechanochromic Materials
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Reported herein is the first example of a direct arylation of heteroarenes by a transient-ligand-directed strategy without the need to construct and deconstruct the directing group. A wide range of heteroarenes undergoes the coupling with diverse aryl iod
- Li, Bijin,Seth, Kapileswar,Niu, Ben,Pan, Lei,Yang, Huiwen,Ge, Haibo
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supporting information
p. 3401 - 3405
(2018/02/28)
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- GOLD-CATALYZED C-C CROSS-COUPLING OF BORON- AND SILICON-CONTAINING ARYL COMPOUNDS AND ARYLDIAZONIUM COMPOUNDS BY VISIBLE-LIGHT
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The present invention relates to a method for producing (functionalized) biaryls by employing a visible-light-driven, gold-catalyzed C-C cross-coupling reaction system involving boron- and silicon-containing aryl compounds and aryldiazonium compounds. Moreover, the present invention relates to the use of such boron- and silicon-containing aryl compounds and aryldiazonium compounds, as well as related gold catalysts, in the manufacture of (functionalized) biaryls.
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Page/Page column 24; 25; 30; 32
(2018/07/29)
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- COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I) wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
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Paragraph 0314; 0487; 0488
(2018/02/27)
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- Photosensitizer-Free, Gold-Catalyzed C–C Cross-Coupling of Boronic Acids and Diazonium Salts Enabled by Visible Light
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The first photosensitizer-free visible light-driven, gold-catalyzed C–C cross-couplings of arylboronic acids and aryldiazonium salts are reported. The reactions can be conducted under very mild conditions, using a catalytic amount of tris(4-trifluoromethyl)phosphinegold(I) chloride [(4-CF3-C6H4)3PAuCl] with methanol as the solvent allowing an alternative access to a variety of substituted biaryls in moderate to excellent yields with broad functional group tolerance. (Figure presented.).
- Witzel, Sina,Xie, Jin,Rudolph, Matthias,Hashmi, A. Stephen K.
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supporting information
p. 1522 - 1528
(2017/05/05)
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- Ruthenium(0)-Catalyzed C-H Arylation of Aromatic Imines under Neutral Conditions: Access to Biaryl Aldehydes
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The first ruthenium(0)-catalyzed C-H bond arylation of aromatic imines with arylboronates under neutral conditions is reported. This versatile method provides rapid access to a wide range of biaryl aldehydes that are difficult to assemble using traditional methods with high atom economy. A new hydrogen acceptor for Ru(0) arylation has been identified. This atom-economical strategy has potential for an array of direct applications in Ru(0)-catalyzed C-H bond arylations using removable directing groups. An indole synthesis by a sequential one-pot, multiple C-H activation protocol is reported.
- Hu, Feng,Szostak, Michal
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p. 4186 - 4189
(2016/09/09)
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- χ-shaped bis(areno)-1,4-dihydropyrrolo[3,2-b]pyrroles generated by oxidative aromatic coupling
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A synthesis of dihydropyrrolo[3,2-b]pyrroles fused with two peripheral arenes or heterocyclic units has been realized through the concise route. These nearly planar compounds were prepared starting from assembling the central core via condensation of 2-aryl or 2-heteroarylbenzaldehydes with aromatic amines and diacetyl, followed by double intramolecular oxidative aromatic coupling. This two-step procedure afforded the desired products in overall yields of 5-36%, and it tolerates structural diversity of starting materials. All the final dyes exhibit strong blue fluorescence in solution.
- Krzeszewski, Maciej,Gryko, Daniel T.
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p. 2893 - 2899
(2015/03/18)
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- New non-annulated thiophenylamides
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0307; 0308
(2015/07/15)
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- NON-ANNULATED THIOPHENYLAMIDES AS INHIBITORS OF FATTY ACID BINDING PROTEINI(FABP) 4 AND/OR 5
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The invention provides novel compounds having the general formula (I), wherein R1, R2, R3, R4, R5, R6 , R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 81; 82
(2014/04/03)
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- Thieno[2,3-c]iosquinolines for use as inhibitors of parp
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Heterocyclic derivatives, including derivatives of thieno[2,3-c]isoquinolin-3-one and their use in therapy as inhibitors of poly(ADP-ribose) polymers (PARP), for use in the prevention and treatment of tissue damage due to ischaemia and reperfusion, degene
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- Towards new neuroprotective agents: Design and synthesis of 4H-thieno[2,3-c] isoquinolin-5-one derivatives as potent PARP-1 inhibitors
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An excessive activation of poly(ADP-ribose) polymerase-1 (PARP-1), a nuclear enzyme able to catalyze the transfer of ADP-ribose from NAD to acceptor proteins, is involved in the progression of neuronal damage after brain insult. Potent and selective PARP-
- Pellicciari, Roberto,Camaioni, Emidio,Costantino, Gabriele,Marinozzi, Maura,Macchiarulo, Antonio,Moroni, Flavio,Natalini, Benedetto
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p. 851 - 858
(2007/10/03)
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- Process for opening cyclopropane rings
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Process for ring opening compounds of the formula STR1 in which R1 is heteroaryl or aryl, R2 is a leaving group, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aralkyl,
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- Photochemical Synthesis of Phenyl-2-thienyl Derivatives
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The irradiation (in benzene solution) of 5-bromo- and 5-iodo-thiophene-2-carbaldehyde or the corresponding methyl ketones furnishes the corresponding 5-phenyl derivatives.The same reactivity for other halogenothiophenes is reported: 3,5-dibromothiophene-2-carbaldehyde furnishes the 3-bromo-5-phenyl-2-thienyl derivative while the corresponding di-iodo compound yields 3,5-diphenylthiophene-2-carbaldehyde.In contrast, 5-acetyl-2,3-di-iodothiophene furnishes only the photosubstitution pruduct at C-5.Generally the iodine-containing compounds are more reactive and more stable under the reaction conditions than ones bearing bromine, in agreement with previous reports on the corresponding furan photochemistry.
- Antonioletti, Roberto,Auria, Maurizio D',Onofrio, Franco D',Piancatelli, Giovanni,Scettri, Arrigo
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p. 1755 - 1758
(2007/10/02)
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