52117-01-8Relevant academic research and scientific papers
PROCESS FOR PREPARING N-ACETYL(L)-4-CYANOPHENYLALANINE Ac-(L)-Phe(4-CN)-OH AND N-ACETYL-(L)-p-AMIDINOPHENYLALANINE-CYCLOHEXYLGLYCINE-BETA-(3-N-METHYLPYRIDINIUM)-ALANINE Ac-(L)-pAph-Chg-PalMe(3)-NH2
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, (2008/06/13)
The present invention is related to a novel process for preparing N-acetyl-(L)-4-cyanophenylalanine by resolving the racemic compound N-acetyl-(D, L)-4-cyanophenylalanine ethyl ester, and a novel process to prepare a stereoisomer of Ac-(L)-pAph-Chg-PalMe(
Antithrombotic quinoxazolines
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, (2008/06/13)
Quinoxazolines having antithrombotic activity. Exemplary of those disclosed are: 4-{[6-(N-carboxymethyl-quinolin-8-yl-sulphonylamino)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, 4-{[6-(1-(N-cyclopentyl-carboxymethylcarbonylamino)-cyclo-propyl)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, and 4-{[7-(N-carboxymethylaminocarbonyl-ethylamino)-4-methyl-quinolin-2-yl]-oxo}-benzamidine.
N-acylamino acid amide compounds and intermediates for preparation thereof
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, (2008/06/13)
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.
Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
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, (2008/06/13)
The present invention relates to 5-membered heterocyclic condensed benzoderivatives of formula wherein Ra to Rc, A, X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. The compounds of the above formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of formula I, and the compounds of the above formula I wherein Rc denotes one of the following amidino groups and the tautomers and stereoisomers thereof have valuable pharmacological properties, particularly an antithrombotic activity.
Rational design of selective thrombin inhibitors
Kim, Sangsoo,Hwang, Sang Yeul,Kim, Young Kwan,Yun, Mikyung,Oh, Yeong Soo
, p. 769 - 774 (2007/10/03)
Thrombin inhibitors with functionalized benzamidines as surrogates for arginine were designed, synthesized, and characterized. Amino acid sequence difference in the position 190 between thrombin and trypsin was exploited in the design to enhance selectivity over trypsin. A representative compound 6 showed high potency (Ki of 45.5 nM) and extremely high specificity over trypsin (over 10,000 fold).
Thrombus imaging using technetium-99m-labeled high-potency GPIIb/IIIa receptor antagonists. Chemistry and initial biological studies
Pearson, Daniel A.,Lister-James, John,McBride, William J.,Wilson, David M.,Martel, Lawrence J.,Civitello, Edgar R.,Dean, Richard T.
, p. 1372 - 1382 (2007/10/03)
Platelet-specific compounds which are radiolabeled with γ-emitting radionuclides may be particularly useful for the noninvasive in vivo detection of thrombi. The synthesis of peptides which are potent inhibitors of platelet aggregation and which contain a chelator for the radionuclide technetium-99m are described. The target compounds were designed such that stable, oxotechnetium(V) species could be prepared where the site of metal coordination was well defined. A strategy was employed where the pharmacophore -Arg-Gly-Asp-(RGD), or RGD mimetic, was constrained in a ring which was formed by the S-alkylation of a cysteine residue with an N-terminal chloroacetyl group. Binding affinities were enhanced by the replacement of arginine with the arginine mimetics S-(3-aminopropyl)cysteine and 4- amidinophenylalanine. Further enhancements could be obtained by the synthesis of oligomers which contained two or more rings containing receptor binding regions. The increase in binding affinity seen was more than that expected from a simple stoichiometric increase of pharmacophore. The most potent compounds described had IC50s of approximately 0.03 μM for the inhibition of human platelet aggregation. Two of the more potent peptides (P280 and P748) were labeled with technetium-99m and assessed in a canine thrombosis model. The 99mTc complexes of the peptides prepared in this work hold promise as thrombus imaging agents due to their high receptor binding affinity, ease of preparation, and expected rapid pharmacokinetics.
Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors
Chauvel,Coric,Llorens-Cortes,Wilk,Roques,Fournie- Zaluski
, p. 1339 - 1346 (2007/10/02)
Aminopeptidase A (APA) and aminopeptidase N (APN) are two metallopeptidases which have been suggested to be involved in the enzymatic cascade of the renin-angiotensin system. APA liberates angotensin III from angiotensin II by releasing the N-terminal asp
Amino acids and peptides having a modified tyrosine residue, their preparation and their application as medicaments
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, (2008/06/13)
These compounds are represented by formula (I), in which each of R1 R2 =H, C1 -C8 alkyl, C3 -C7 cycloalkyl, or aromatic; (when R1 =H, R2 can be an amine function-prote
Antihypertensive compositions containing an aryl-substituted alanine azo and an arylhydrazino-propionic acid
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, (2011/03/17)
Novel pharmaceutical compositions are disclosed. The compositions comprise an aryl substituted alanine and a substituted phenyl hydrazino propionic acid. The compositions are useful for treating hypertension.
