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Palle Jakobsen

Jorgen Drejer

Peter Madsen

Thomas Hoeg-Jensen

Patrick William Garibay

Jane Marie Lundbeck

Marit Kristiansen

Janos Tibor Kodra

Thomas Boerglum Kjeldsen

Peter Faarup

Tina Moeller Tagmose

Anders Bendtz Kanstrup

Karsten Lundgren

Preben H Olesen

Svend Havelund

Ib Jonassen

Egon Persson

Lars Naerum

Thomas Børglum Kjeldsen

Tina Møller Tagmose

Tine Glendorf

Jacob Sten Petersen

Ole Hvilsted Olsen

Lars Christian Petersen

Anker S Jorgensen

Ursula Sonnewald

Frantisek Hubalek

Anders Klarskov Petersen

Svend Ludvigsen

Niels Christian Kaarsholm

Helle Birk Olsen

Ulrich Sensfuss

Ulla Ribel-Madsen

Dorte Bjerre Steensgaard

János Tibor Kodra

Christian Fledelius

Leif No slashedrskov-Lauritsen

Soren Ostergaard

Helle Worsaae

Dorte Xenia Gram

Jane Marie Lundbech

Stefan Lutz Richter

Leif N&oslash;rskov-Lauritsen

Niels Westergaard

Birgitte So Slashedkilde

Jorgen Dreger

Henrik Klitgaard

Jaanos Tibor Kodra

Anker Steen Jo Slashedrgensen

Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H.

Protease stabilized acylated insulin analogues

Novel acylated insulin analoges exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analoges contain B25H and A14E or A14H.

An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.

Insulin analogues with an acyl and alkylene glycol moiety

Protease stabilized, acylated insulin analogues

The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.

Insulin derivative

The present invention is related to insulin derivatives having a side chain attached either to the &#x3b1;-amino group of the N-terminal amino acid residue of B chain or to an &#x3b5;-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethyleneglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from &#x2014;NHand &#x2014;COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.

Insulin derivatives

PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regular insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.

PEGylated, extended insulins

The present invention relates to novel ligands for the HisZnsites of the R-state insulin hexamer having the formula A-B-C-D-X (III), wherein: A is a chemical group which reversibly binds to a HisZnsites of an insulin hexamer; B is a linker; C is a fragment consisting of 0 to 5 neutral amino acids; D is a fragment comprising 1 to 20 positively charged groups independently selected from amino or guanidino groups; and X is &#x2014;OH, &#x2014;NHor a diamino group. The present invention also relates to R-state insulin hexamers comprising such ligands, and aqueous insulin preparations comprising such R-state insulin hexamers.

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Aromatic compounds

The present invention relates to (2R,3R,4R)-3,4-dihydroxy-2-hydroxymethylpyrrolidine and other substituted 2-methylpyrrolidines and their use for inhibiting liver glycogen phosphorylase.

Method of inhibiting liver glycogen phosphorylase with 2-alkylpyrrolidines

The invention relates to compounds inhibiting the activation of FX to FXa by TF/FVIIa. The compounds are anticoagulants. The invention also relates to a method of identifying a drug candidate.

FVIIa/TF activity inhibiting compounds

FVlla/TF activity inhibiting compounds

Heterocyclic compounds regulating clotting

Disclosed are compounds of formula (I) ##STR1## wherein R1 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, Q or aryl;

4,5,6,7-tetrahydro-thieno(2,3-C)pyridine derivatives

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Vaerloese, Denmark

Palle Jakobsen