- An efficient method for the preparation of 4-alkoxy-substituted thieno[2,3-b]pyridines
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An efficient method for the preparation of 4-alkoxy-substituted thieno[2,3-b]pyridines is described. The key intermediates, 4-alkoxy-2-chloro-3- cyanopyridines, were synthesized from a variety of alcohols by nucleophilic substitution with 3-cyano-2,4-dich
- Saito, Keiji,Naito, Satoru,Shinozuka, Tsuyoshi
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p. 1491 - 1501
(2014/07/07)
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- Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain
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Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active in the
- Sasikumar,Qiang, Li,Burnett, Duane A.,Greenlee, William J.,Li, Cheng,Heimark, Larry,Pramanik, Birendra,Grilli, Mariagrazia,Bertorelli, Rosalia,Lozza, Gianluca,Reggiani, Angelo
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scheme or table
p. 3199 - 3203
(2010/03/03)
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- THIENOPYRIDINE DERIVATIVES
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The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.
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Page/Page column 142
(2010/11/26)
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- FUSED TRICYCLIC MGLUR1 ANTAGONISTS AS THERAPEUTIC AGENTS
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In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1-R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, part
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Page/Page column 45; 55-56
(2010/11/26)
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- Synthesis of 1,4-dihydro-2-methyl-4-oxo-nicotinic acid: Ochiai's route failed
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The synthesis of 1,4-dihydro-2-methyl- and 1,4-dihydro-1,2-dimethyl-4-oxo-nicotinic acids was accomplished following a route other than Ochiai's procedure, which yielded the isomer 1,6-dihydro-2-methyl-6-oxo-nicotinic acid ethyl ester, and not the 4-oxo-derivative, as reported. Analytical data confirmed the identity of the two isomer oxo-nicotinic acids. UV-vis and potentiometric preliminary data showed that Al(III) does not form complexes with 1,6-dihydro-2-methyl-6-oxo-nicotinic acid ethyl ester in solution, as expected, but with 1,4-dihydro-2-methyl-4-oxo-nicotinic acid.
- Ferlin, Maria Grazia,Di Marco, Valerio B.,Dean, Annalisa
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p. 6222 - 6227
(2007/10/03)
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- Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists
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SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative alloste
- Zheng, Guo Zhu,Bhatia, Pramila,Daanen, Jerome,Kolasa, Teodozyj,Patel, Meena,Latshaw, Steven,El Kouhen, Odile F.,Chang, Renjie,Uchic, Marie E.,Miller, Loan,Nakane, Masaki,Lehto, Sonya G.,Honore, Marie P.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
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p. 7374 - 7388
(2007/10/03)
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- Structure-driven HtL: Design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity
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The design and synthesis of a new series of c-Jun N-terminal kinase inhibitors are reported. The novel series of substituted amino indazoles were designed based on a combination of hits from high-throughput screening and X-ray crystal structure informatio
- Stocks, Michael J.,Barber, Simon,Ford, Rhonan,Leroux, Frederic,St-Gallay, Steve,Teague, Simon,Xue, Yafeng
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p. 3459 - 3462
(2007/10/03)
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