Patent application number | Description | Published |
20080241102 | Polymeric Prodrug with a Self-Immolative Linker - A cascade carrier linked prodrug is described which comprises a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier. | 10-02-2008 |
20110009315 | LONG-ACTING TRANSIENT POLYMER CONJUGATES OF EXENDIN - Long-acting polymer exendin-4 or exendin agonist derivatives of the formula Pol-L-E are provided wherein Pol is a polymer, L is a releasing linker undergoing slow autohydrolysis and E is an exendin or exendin agonist. These exendin or exendin agonists are slowly released from Pol-L upon administration to a living organism. The derivatives are useful e.g. for the treatment of diabetes mellitus. | 01-13-2011 |
20110053848 | PRODRUG COMPRISING A DRUG LINKER CONJUGATE - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L | 03-03-2011 |
20110112021 | PEGYLATED RECOMBINANT HUMAN GROWTH HORMONE COMPOUNDS - A chemically modified human Growth Hormone (rhGH) prepared by attaching a transient linker which comprises a polyethylene glycol. The chemically modified protein may have a much longer lasting rhGH activity than that of the unmodified rhGH, enabling reduced dose and scheduling opportunities and the modified rhGH may not cause lipoatrophy. Also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial. | 05-12-2011 |
20110172390 | Protein-Proteophore Complexes - The application relates to a composition comprising a hyperbranched polymer attached to a core and a biologically active moiety. The biologically active moiety is attached to the core by means of a substantially non-enzymatically cleavable linker L. The composition can be used to deliver the biologically active moiety to its target. | 07-14-2011 |
20110223230 | HYDROGEL FORMULATIONS - A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety. | 09-15-2011 |
20120156259 | Biodegradable Polyethylene Glycol Based Water-Insoluble Hydrogels - The present invention relates to biodegradable polyethylene glycol based water-insoluble hydrogels comprising backbone moieties which are interconnected by hydrolytically degradable bonds, the backbone moieties further comprising reactive functional groups, wherein the water-insoluble hydrogel is further characterized in that the ratio between the time period for the complete degradation of the hydrogel by hydrolysis of the degradable bonds into water-soluble degradation products comprising one or more backbone moieties and the time period for the release of the first 10 mol-% of water-soluble degradation products comprising one or more backbone moieties based on the total amount of backbone moieties in the hydrogel is greater than 1 and equal to or less than 2. The invention further relates to conjugates of such hydrogels with ligands or ligating groups, prodrugs and pharmaceutical compositions as well as their use in a medicament. | 06-21-2012 |
20120156260 | Prodrugs Containing an Aromatic Amine Connected By an Amido Bond to a Linker - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein an aromatic amine containing biologically active moiety is connected (bound) by an amido bound to a linker. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments. | 06-21-2012 |
20120183616 | LONG ACTING INSULIN COMPOSITION - The present invention relates to a pharmaceutical composition comprising an insulin compound in a concentration that is sufficient to maintain a therapeutically effective level of the insulin compound in blood plasma for at least 3 days characterized by having a pharmacokinetic profile in vivo with substantially no burst of the insulin compound. The present invention further relates to the use of an insulin compound for preparing said pharmaceutical composition as well as a kit of parts comprising said pharmaceutical composition. | 07-19-2012 |
20120184489 | PRODRUGS COMPRISING AN INSULIN LINKER CONJUGATE - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L | 07-19-2012 |
20120191039 | CARRIER LINKED PRAMIPEXOLE PRODRUGS - The present invention relates to a carrier linked pramipexole prodrug or a pharmaceutical acceptable salt thereof, wherein pramipexole is bound via a linker to a polymeric carrier. The invention also relates to pharmaceutical compositions comprising said polymeric pramipexole prodrug and their use as medicaments. | 07-26-2012 |
20120253071 | Sterilization of biodegradable hydrogels - The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties. | 10-04-2012 |
20120277253 | SUBCUTANEOUS PALIPERIDONE COMPOSITION - The present invention relates to pharmaceutical composition for subcutaneous injection comprising a paliperidone compound wherein the composition releases the paliperidone with an immediate onset of action and continuously for at least 3 weeks, and wherein the composition has a pharmacokinetic profile in vivo with substantially no burst release of the paliperidone. The compositions are useful as medicaments for the treatment of psychotic disorders and diseases. | 11-01-2012 |
20130053405 | CARRIER LINKED PALIPERIDONE PRODRUGS - The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent Paliperidone carrier conjugate of formula (I) | 02-28-2013 |
20130150281 | POLYMERIC PRODRUG WITH SELF-IMMOLATIVE LINKER - A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier. | 06-13-2013 |
20130189328 | PRODRUGS COMPRISING AN EXENDIN LINKER CONJUGATE - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an exendin linker conjugate D-L, wherein D represents an exendin moiety; and -L is a non-biologically active linker moiety -L | 07-25-2013 |
20140243254 | Polymeric Hyperbranched Carrier-Linked Prodrugs - The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein POL is a polymeric moiety, each Hyp is independently a hyperbranched moiety, each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs and methods of treatment. | 08-28-2014 |
20140296150 | Carrier-Linked Treprostinil Prodrugs - The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH). | 10-02-2014 |
20140296257 | High-Loading Water-Soluable Carrier-Linked Prodrugs - The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment. | 10-02-2014 |
20140303245 | Sustained Release Composition of Prostacyclin - The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension. | 10-09-2014 |
20140323402 | Protein Carrier-Linked Prodrugs - The present invention relates to water-soluble protein carrier-linked prodrugs wherein the protein carrier comprises an amino acid sequence consisting of at least 100 amino acid residues forming random coil conformation and comprising alanine, serine and proline residues. It further relates to pharmaceutical compositions comprising said water-soluble protein carrier-linked prodrugs, their use as a medicament as well as methods of treatment and administration. | 10-30-2014 |
20150057221 | PRODRUG COMPRISING A DRUG LINKER CONJUGATE - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L | 02-26-2015 |
20150087688 | PRODRUGS OF HYDROXYL-COMPRISING DRUGS - The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a biologically active moiety-linker conjugate D-L, wherein D is a hydroxyl-comprising biologically active moiety; and L is a promoiety comprising a moiety L | 03-26-2015 |