67600-79-7Relevant academic research and scientific papers
Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
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, (2011/04/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Page/Page column 115, (2010/08/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
Preparation of new monomers aza-β3-aminoacids for solid-phase syntheses of aza-β3-peptides
Busnel, Olivier,Baudy-Floc'h, Miche?le
, p. 5767 - 5770 (2008/02/09)
The preparation of new Nβ-Fmoc-protected aza-β3-amino acids (aza-β3-aa) with proteinogenic side chains as well as their Nβ-Fmoc, Nβ-Cbz or Nβ-Boc aza-β3-amino esters (from Pro, Asn, Asp, Glu, Gln) by successive nucleophilic substitutions will be described.
The first synthesis of 1,5-diazacyclooctan-2-one and differentially protected 1,5-diazacyclooctanes
Sherrill, Ronald G.
, p. 7053 - 7056 (2008/03/12)
An efficient, high-yielding synthesis of 1,5-diazacyclooctan-2-one and subsequent elaboration to a differentially protected 1,5-diazacyclooctane is disclosed.
Facile scalable reduction of N-acylated dihydropyrazoles
Curtis, Michael D.,Hayes, Nancy C.,Matson, Patricia A.
, p. 5035 - 5038 (2007/10/03)
The reduction of a variety of highly functionalized N-acylated dihydropyrazoles (1) with BH3-pyridine is described. The process through which this unexpectedly difficult reduction was discovered and developed is reported. A facile atom-efficien
Convergent synthesis of 2,3-bisarylpyrazolones through cyclization of bisacylated pyrazolidines and hydrazines
Brugel, Todd A.,Hudlicky, Tomas,Clark, Michael P.,Golebiowski, Adam,Sabat, Mark,Endoma, Mary Ann A.,Bui, Vu,Adams, David,Laufersweiler, Matthew J.,Maier, Jennifer A.,Bookland, Roger G.,De, Biswanath
, p. 3195 - 3198 (2007/10/03)
Cyclization of various bisacylated hydrazines and pyrazolidines using DBU or sodium hydride leads to the formation of various mono-, bi- and tricyclic pyrazolone scaffolds in 41-98% yield. The convergent nature by which the precyclization intermediates are constructed allows for rapid derivatization about the pyrazolone core.
Formation of unnatural cyclic amino acid equivalent from the simple cyclic hydrazine
An, Duk Keun,Kim, Hye-Min,Kim, Min Sung,Kang, Seung Kyu,Ha, Jae Du,Kim, Sung Soo,Choi, Joong-Kwon,Ahn, Jin Hee
, p. 2379 - 2383 (2007/10/03)
An alternative method for the synthesis of unnatural cyclic amino acid equivalent from the simple cyclic hydrazine via oxidation and cyanation was developed.
Synthesis, molecular modeling and biological evaluation of aza-proline and aza-pipecolic derivatives as FKBP12 ligands and their in vivo neuroprotective effects
Wilkinson, Douglas E.,Thomas IV, Bert E.,Limburg, David C.,Holmes, Agnes,Sauer, Hansjorg,Ross, Douglas T.,Soni, Raj,Chen, Yi,Guo, Hong,Howorth, Pamela,Valentine, Heather,Spicer, Dawn,Fuller, Mike,Steiner, Joseph P.,Hamilton, Gregory S.,Wu, Yong-Qian
, p. 4815 - 4825 (2007/10/03)
Nonimmunosuppressant ligands, exemplified by GPI 1046 (1), for the peptidyl-prolyl isomerase FKBP12 have been found to unexpectedly possess powerful neuroprotective and neuroregenerative effects in vitro and in vivo. We have extensively explored the thera
New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same
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, (2008/06/13)
A compound of the formula: STR1 wherein R1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: STR2 in which R5 is hydrogen or acyl and R6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R2 is hydrogen or lower alkyl; or R1 and R2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower )alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R3 is hydrogen or lower alkyl; and R4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.
