16635-00-0Relevant articles and documents
Design, synthesis, and SAR analysis of novel selective σ1 ligands
Collina, Simona,Loddo, Guya,Urbano, Mariangela,Linati, Laura,Callegari, Athos,Ortuso, Francesco,Alcaro, Stefano,Laggner, Christian,Langer, Thierry,Prezzavento, Orazio,Ronsisvalle, Giuseppe,Azzolina, Ornella
, p. 771 - 783 (2007)
A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to σ1 and σ2 receptors. Many compounds exhibited nanomolar affinity for σ1 subtype receptor with good selectivity over σsub
CARBAMOYLOXYMETHYL TRIAZOLE CYCLOHEXYL ACIDS AS LPA ANTAGONISTS
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Paragraph 1030-1032, (2018/01/18)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Terminal-Selective Functionalization of Alkyl Chains by Regioconvergent Cross-Coupling
Dupuy, Stéphanie,Zhang, Ke-Feng,Goutierre, Anne-Sophie,Baudoin, Olivier
supporting information, p. 14793 - 14797 (2016/11/23)
Hydrocarbons are still the most important precursors of functionalized organic molecules, which has stirred interest in the discovery of new C?H bond functionalization methods. We describe herein a new step-economical approach that enables C?C bonds to be constructed at the terminal position of linear alkanes. First, we show that secondary alkyl bromides can undergo in situ conversion into alkyl zinc bromides and regioconvergent Negishi coupling with aryl or alkenyl triflates. The use of a suitable phosphine ligand favoring Pd migration enabled the selective formation of the linear cross-coupling product. Subsequently, mixtures of secondary alkyl bromides were prepared from linear alkanes by standard bromination, and regioconvergent cross-coupling then provided access to the corresponding linear arylation product in only two steps.
Formation of enehydrazine intermediates through coupling of phenylhydrazines with vinyl halides: Entry into the Fischer indole synthesis
Zhan, Fuxu,Liang, Guangxin
supporting information, p. 1266 - 1269 (2013/03/13)
Cut to the chase: Direct formation of an enehydrazine, an intermediate in the classic Fischer indole synthesis, solves the regioselectivity problem associated with indolization. This approach not only achieves selective synthesis of indoles through proper selection of the vinyl halide, but also leads to quick construction of desoxyeseroline and esermethole, as well as the key structural motif in the Akuammiline alkaloid vincorine. Copyright
Identification of a potent and selective ρ1 receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells
Rossi, Daniela,Pedrali, Alice,Urbano, Mariangela,Gaggeri, Raffaella,Serra, Massimo,Fernández, Leyden,Fernández, Michael,Caballero, Julio,Ronsisvalle, Simone,Prezzavento, Orazio,Schepmann, Dirk,Wuensch, Bernhard,Peviani, Marco,Curti, Daniela,Azzolina, Ornella,Collina, Simona
scheme or table, p. 6210 - 6224 (2011/12/02)
Herein we report the synthesis, drug-likeness evaluation, and in vitro studies of new sigma (ρ) ligands based on arylalkenylaminic scaffold. For the most active olefin the corresponding arylalkylamine was studied. Novel arylalkenylamines generally possess
1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU)-promoted efficient and versatile aza-Michael addition
Yeom, Chang-Eun,Kim, Mi Jeong,Kim, B. Moon
, p. 904 - 909 (2007/10/03)
A convenient and versatile method was developed for aza-Michael addition using a substoichiometric amount of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). Various nitrogen nucleophiles were efficiently introduced to α,β-unsaturated carbonyl compounds employing 0.5 equiv of DBU. Furthermore, other heteroatomic nucleophiles could also be introduced successfully under the same reaction conditions.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 30, (2010/02/14)
The present invention relates to inhibitors of serotonin and/or norepinephrine reuptake and specifically provides compounds of formula (I): wherein A is selected from -O- and -S-; X is selected from C1-C8 alkyl, C2-C8 alkenyl, and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from phenyl, pyrrolidinyl, piperidinyl, morpholinyl, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; Y is selected from (a), (b), (c), (d), (e), (f) where R3, R4and R5 are independently selected from hydrogen, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; R6 and R7 are independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; R8 is selected from chloro, bromo, iodo, C1-C4alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; R1 and R2 are each independently hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; or compositions thereof and methods of using the same.
THIADIAZOLES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 122, (2010/02/12)
Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).
ISOTHIAZOLE DIOXIDES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 125-126, (2010/02/13)
Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 70, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.