- Modified iRNA agents
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The present invention provides effective motifs for RNA agents conjugated to at least one ligand, which are advantageous for the in vivo delivery of iRNA duplex agents. Additionally, the present invention provides methods of making these compositions, as well as methods of introducing these iRNA duplex agents into cells using these compositions, e.g., for the treatment of various disease conditions.
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- AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND PROCESSES FOR PREPARING THEM
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The invention relates to new amino acid derivatives of general formula (I), wherein B, T, Z, Y, V and n are defined as in claim 1, the tautomers, diastereomers and enantiomers thereof, the mixtures thereof and the salts thereof, particularly their physiologically acceptable salts with inorganic or organic acids or bases which have valuable pharmacological properties, particularly selective NPY-antagonist properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
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- Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
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NPY-antagonistic compounds of the formula STR1 Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N 2-bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N 2-[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N 2-(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N 2-(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl) phenyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N 5-(Aminoiminomethyl)-N 2-(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N 5-methyl-ornithinamide-hydrochloride; (F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N 2-(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N. sup. 2-(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-argininamide-bis-(trifluoroacetate); and,(H) (R)-N. sup.2-(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl) phenyl]methyl]-argininamide-trifluoroacetate.
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- AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND THEIR USE IN THE TREATMENT OF OBESITY
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Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.
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- NEW COUPLING REAGENTS IN PEPTIDE CHEMISTRY
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2-(1H-Benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HBTU) has been applied as coupling reagent to solid phase peptide synthesis.Furthermore, a general synthetic procedure for new derivatives of different N-hydroxy compounds has been developed.They either act as excellent activating reagents causing low racemization during condensation of peptide segments or are useful tools for the formation of active esters suitable for couplings in mixed aqueous / organic media, respectively.
- Knorr, Reinhard,Trzeciak, Arnold,Bannwarth, Willi,Gillessen, Dieter
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p. 1927 - 1930
(2007/10/02)
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