29639-77-8Relevant academic research and scientific papers
Design, synthesis and evaluation of MCH receptor 1 antagonists - Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414
Müller, Stephan G.,Heckel, Armin,Kley, J?rg T.,Lehmann, Thorsten,Lustenberger, Philipp,Oost, Thorsten,Roth, Gerald J.,Rudolf, Klaus,Arndt, Kirsten,Lenter, Martin,Lotz, Ralf R.H.,Maier, Gerd-Michael,Markert, Michael,Schindler, Marcus,Stenkamp, Dirk
, p. 3264 - 3269 (2015/07/08)
Abstract Despite recent approvals of anti-obesity drugs there is still a high therapeutic need for alternative options with higher efficacy in humans. As part of our MCH-R1 antagonist program for the treatment of obesity, a series of biphenylacetamide HTS
An in situ acidic carbon dioxide/glycol system for aerobic oxidative iodination of electron-rich aromatics catalyzed by Fe(NO3)3·9H2O
Ma, Ran,Huang, Cheng-Bin,Liu, An-Hua,Li, Xue-Dong,He, Liang-Nian
, p. 4308 - 4312 (2015/01/08)
An environmentally benign CO2/glycol reversible acidic system was developed for the iron(iii)-catalyzed aerobic oxidative iodination of electron-rich aromatics without the need for any conventional acid additive or organic solvent. Notably, moderate to high isolated yields (up to 97%) of the aryl iodides were attained with comparable regioselectivity when ferric nitrate nonahydrate was used as the catalyst with molecular iodine under 1 MPa of CO2.
The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy)caffeine analogues
Strydom,Bergh,Petzer
, p. 513 - 518 (2013/01/15)
Previous studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an IC 50 value of 0.383M towards MAO-B. In an attempt to improve on the inhibition potency of this compound and to discover highly potent reversible MAO-B inhibitors, in the present study, a series of 8-(2-phenoxyethoxy)caffeine analogues containing various substituents on C4 of the phenoxy ring, were synthesized and evaluated as inhibitors of human MAO-A and -B. The results show that the 8-(2-phenoxyethoxy)caffeine analogues are selective and reversible MAO-B inhibitors with the most potent homologue, 8-{2-[4-(trifluoromethyl) phenoxy]ethoxy}caffeine, exhibiting an IC50 value of 0.061μM. These highly potent inhibitors are useful leads in the design of therapies for neurodegenerative disorders such as Parkinsons disease. Georg Thieme Verlag KG Stuttgart New York.
Synthesis of new cores and their use in the preparation of polyester dendrimers
Twibanire, Jean-D'Amour K.,Al-Mughaid, Hussein,Grindley, T. Bruce
experimental part, p. 9602 - 9609 (2011/01/03)
Six dendrimer and dendron cores terminated by hydroxyl groups that are neither phenolic nor cleavable by hydrogenolysis have been prepared in a consistent one-pot manner from terminal allyl groups by reduction of the product of reductive ozonolysis. Some of the terminal allyl derivatives are new and others have been prepared by new methods. The well-known O-benzylidene derivative of 2,2′-bis(hydroxymethyl)propanoic acid was shown to be the cis-stereoisomer. A new AB3-type anhydride, tris(benzyloxymethyl) acetic anhydride has been prepared. It was demonstrated that these cores and dendrons could be assembled into first and second generation homo- and mixed polyester dendrimers.
NEW PYRIDAZINE DERIVATIVES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
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Page/Page column 96, (2008/12/06)
The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
Quick assembly of 1,4-diphenyltriazoles as probes targeting β-amyloid aggregates in Alzheimer's disease
Qu, Wenchao,Kung, Mei-Ping,Hou, Catherine,Oya, Shunichi,Kung, Hank F.
, p. 3380 - 3387 (2008/02/08)
Accumulation of β-amyloid aggregates (Aβ) in the brain is linked to the pathogenesis of Alzheimer's disease (AD). We report a novel approach for producing 1,4-diphenyltriazoles as probes for targeting Aβ aggregates in the brain. The imaging probes, a seri
NOVEL HETEROCYCLIC AMIDE DERIVATIVES HAVING DIHYDROOROTATE DEHYDROGENASE INHIBITING ACTIVITY
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Page/Page column 60; 61, (2010/10/20)
Novel heterocyclic amide derivatives having pharmacological effects, that is, compounds represented by the general formula (1) or salts thereof: (1) wherein X1-X2 is S-CH2 or the like; R1 is alkyl or the like; p is 0 to 7; R2 is hydrogen, alkyl, or the like; R3 is hydrogen, alkyl, or the like; Y1-Y2 is CH=CH or the like; R4 is halogeno, alkyl, or the like; q is 0 to 4; and R5 is halogeno, hydrogen, alkyl, or the like.
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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Page/Page column 34, (2010/02/14)
The present invention relates to alkyne compounds of general formula I wherein the groups and radicals A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one alkyne according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
NOVEL ALKYNE COMPOUNDS WITH AN MCH-ANTAGONISTIC ACTION AND MEDICAMENTS CONTAINING SAID COMPOUNDS
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Page/Page column 82, (2010/02/14)
The invention relates to alkyne compounds of general formula (I), in which the groups and radicals A, B, W, X, Y, Z, R1 and R2 are defined as cited in claim 1. The invention also relates to medicaments containing at least one inventive alkyne. As a result of the antagonistic action against the MCH-receptor, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, in particular adiposity and diabetes.
NOVEL ALKYNE COMPOUNDS HAVING AN MCH ANTAGONISTIC EFFECT AND MEDICAMENTS CONTAINING THESE COMPOUNDS
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Page/Page column 221-222, (2008/06/13)
The invention relates to alkyne compounds of general formula (I), in which groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings as cited in Claim 1. The invention also relates to medicaments containing at least one inventive alkyne. The MCH receptor antagonistic effect renders the inventive medicaments suitable for treating metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia and diabetes.
